FIELD OF THE INVENTION
The present invention relates to novel compositions comprising at least one bowel evacuant and a saccharide component optionally with at least one component selected from a group comprising antacid antiflatulant prokmetic antispasmodic anticholinergic stool softener anti-nauseating/anti-emetic agent, tonifier and the like or their mixtures and optionally with one or more excipient(s), the process of preparation and method of using such compositions The compositions of the present invention are useful as a pharmaceutical or a dietary supplement The compositions of the present invention are highly effective in the overall management of constipation including the prophylaxis and/or amelioration and/or treatment of not only the constipation but also associated disorders thus providing a better relief to the user
BACKGROUND OF THE INVENTION
Constipation is a condition in which a person has uncomfortable or infrequent bowel movements Generally, a person is considered to be constipated when bowel movements result in passage of small amounts of hard, dry stool, usually fewer than three times a week People who are constipated may find it difficult and painful to have a bowel movement Other symptoms of constipation include feeling bloated uncomfortable and sluggish The hard and dry stools of constipation occur when the colon absorbs too much water or if the colon s muscle contractions are slow or sluggish causing the stool to move through the colon too slowly Common causes of constipation are not enough fiber in the diet, not enough liquids, lack of exercise medications irritable bowel syndrome, changes in life or routine such as pregnancy or older age or travel abuse of laxatives, ignoring the urge to have a bowel movement specific diseases such as stroke problems with the colon and rectum and problems with intestinal function such as chronic idiopathic constipation Sometimes constipation can lead to complications such as hemor-hoids caused by straining to have a bowel movement or anal fissures caused when hard stool stretches the sphincter muscle or rectal prolapse caused by straining which leads to a small amount of intestinal lining to push out from the anal opening Constipation may also cause hard stool to pack the intestine and rectum so tightly that normal pushing action of colon is not enough to expel stool This condition, called fecal impaction occurs mostly in children and older adults
US patent no 5 320,847 relates to a method of agglomerating and thereby increasing the dispersability and mixability of a powdered psyllium hydrophilie mucilloid combinate utilizing acacia dissolved in water as the agglomerating agent US patent no 5 651 988 claims a combination osmotic and bulk-forming laxative comprising lactitol and psyllium hvdiophihc
mucilloid powder US patent no 4,321 263 describes a method of increasing the water dispersability of psyllium hydrophilic mucilloid by granulating or agglomerating the psyllium with an alcoholic solution of polyethylene glycol and/or polyvinylpyrrolidone Yet another method is disclosed in US patent no 4,548,806 which describes a method for coating psyllium hydrophilic mucilloid with from about 3-11 percent by weight of a water soluble maltodextrm
US publication no 20050152989 claims a method for treating irritable bowel syndrome (IBS) using an osmotic laxative and a fiber which specifically provides relief from IBS b\ simultaneously ameliorating both constipation and diarrhea Particularly described fibers are psyllium, partially-hydrolyzed guar gum and cellulose PCT publication no WO200505I361 relates to solid dosage form colonic purgative formulations particularly comprising at least one soluble binder and at least one purgative and methods of their use
PCT publication bearing no WO2004078182 relates to a novel composition which combines defined proportions of a soluble saccharide which is poorly absorbed by the organism (the most widely known being disacchandes such as lactulose lactitol trehalose) and an antiflatulent from the siloxane group (the most widely known being polydimethylsiloxanes such as simethicone dimethicone) German patent publication bearing no 10262005 claims compositions containing hydrogenated condensed palatinose together with bifidobacteria cultures or with at least one other dietary fiber component selected from long- or short-chain fructo-oligosacchandes galacto- xylo- malto- isomalto- gentio- soybean- chito- oi chitosan-oligosacchandcs hydrolyzed guar gum lactulose, lacto-sucrose pectic materials, hydrolases sugar condensation products glucosyl-sucrose resistant starch cellulose or oat- wheat-, vegetable- fruit- or sugar beet fiber European patent no 0334407 relates to a method of preparing a solid composition of lactulose in a simple way According to the European patent no 0334407 the lactulose svrup is mixed with Fiberform™ i e a fiber product based on the husks of corn grains having a liber content of more than 80% The mixture is spread, dried crushed and optionally sieved US patent no 5 817,330 describes jellied and translucent emulsion, charactei ized in that it consists essentially ol about 75 to 85 parts by weight of liquid paraffin oil and 25 to 15 parts b\ weight ol a sweetened aqueous solution of lactulose containing a total of 54 to 66% by weight dry matter
Laxatives are among the most commonly used drugs or additives for treatment of constipation Most are quite safe when used judiciouslv intermittentK when possible and in the absence ol contraindications Bulking agents and nonabsorbable compounds such as lactulose can cause
bloating Osmotic laxatives containing poorl) absorbable ions such as magnesium or phosphate can cause metabolic disturbances, particularly in the presence of renal impairment Polyethylene glycol solutions are emerging as an effective and safe mode of treatment for chronic constipation Purgatives are drastic laxatives causing a cleansing or watery evacuation of the bowels, usually with a griping pain
Triphala is an ayurvedic herbal formula composed of three fruits namely Harada (Hunlaki) Amla (Amalakt) and Behada (Bibhitaki) and is an effective laxative which also supports the body's strength The major components of Triphala are condensed tannins catechins, along with gallic and ellagic acid which are the building blocks of the tannins Because of its high nutritional value, Triphala uniquely cleanses and detoxifies at the deepest organic levels without depleting the body's reserves Triphala corrects constipation cleanses and tonit> the gastrointestinal tract, detoxifies the whole body and improves digestion and assimilation reduces high blood pressure and hypertension and improves blood circulation, acts as anti-viral antibacterial, powerful anti-oxidant, and has anticancer and anti-allergy properties Triphala is also helpful in liver disorders, acts as an expectorant and corrects diverticulitis It is very effective in Irritable Bowel Syndrome (IBS) and Ulcerative Colitis Triphala is a powerful eye rejuvenator for treatment of conjunctivitis, progressive myopia, the early stages of glaucoma and cataracts It is highly anti-inflammatory, anti-viral and also stimulates bile-flow and peristalsis Triphala is mild non-habit forming, and a rejuvenative Triphala (trifala) is so effective because its three herbs are potent healers The herb Amalaki (Embhca officinalis or Phyllanthus embhea) is one of ayurveda's greatest rejuvenators and a strong natural anti-oxidant which also helps to boost the immune system and balances Pitta The herb Hantaki (Termtna/ia chebula) the hbetan "king of medicine" is a classic heart-brain-longevity tonic and balances Vata The herb Bibhitaki {Terminaha belerica) is a powerful rejuvenative that reduces liver and heart disease improves the voice vision and promotes the growth of hair and balances Kapha Triphala helps to feel pure, light and revitalized, removes toxins, accumulations, gas and distention nourishes the nervous system, blood and muscle, increases digestion assimilation and reduces fat detoxifies almost every system in the body and regulates the metabolism Recent studies have shown that triphala extract possess the ability to scavenge free radicals such as DPPH and superoxide primarily due to the presence of phenolic compounds Studies have also shown the strong inhibitory activity of triphala on PMN-t\pe MMPs involved in the extracellular matrix (ECM) degradation dui mg periodontitis 1 he m \ itto c>totoxic and apoptotic activity of 11 iphala had also been demonstrated which ma> be due to the gallic acid - a major polyphenol observed
in Triphala However, no medicinal compositions had been described in prior art comprising Tnphala and an osmotic laxative for treatment of constipation and associated disorders
Ajwam oil is an essential oil obtained from the dried fruits of Trachyspernmm ammi The essential oil (2 5 to 5% in the dried fruits) is dominated by thymol (35 to 60%) furthermore a-pinene, p-cymene, limonene and y-terpmene have been found The oil of ajwam is an almost colorless to brownish liquid with characteristic odour and a sharp hot taste Ajwain oil is highl> effective as a remedy for gastrointestinal disorders such as for relieving flatulence dyspepsia colic, diarrhea, spasmodic disorders and indigestion
Fibers are often used for the treatment of constipation A fiber is the non-digested part of plant food and adds bulk to the stools by absorbing water There are two types of fiber namely soluble and insoluble Soluble fiber dissolves in water and is found in oat bran barley peas beans and citrus fruits Insoluble fibers are found in wheat bran and some vegetables Fiber increases the transit time of the colon and decrease the pressures within the colon Fibers such as Psyllium have been reported to inhibit lactulose-induced colonic mass movements and to benefit patients with irritable bowel syndrome, improving both constipation and diarrhea (Washinton N et al The American journal of clinical nutrition, 1998, 67(2), 317-321) Psyllium is the common name used for several members of the plant genus Plantago whose seeds are used commercially for the production of mucilage The genus Plantago contains over 200 species P ovata and P psyllium are produced commercially in several European countries the former Soviet Union Pakistan and India Plantago seed known commercially as black French or Spanish psyllium is obtained from P psyllium and P arenaria Seed produced from P ovata is known in trading circles as white or blonde psyllium, Indian Plantago or Ispaghula or Isabgol Senna is the common name for many species in the genus Cassia both in the subfamily Caesalpinioideae The term Senna is often used specifically for the medicinal herb Cassia angustifoha Senna contains hydroxyanthracene glycosides known as sennosides These glycosides stimulate colon activity and thus have a laxative effect Also, these glycosides increase fluid secretion from the colon with the effect of softening the stool and increasing its bulk (Leng-Peschlow F Dual effect of orally administered sennosides on large intestinal transit and fluid absorption in the rat / Phuim Pharmacol 1986, 38 606-10) Double-blind trials have confiimed the benefit ot senna in treating constipation (Passmore AP Davics KW Flanagan PG et al A comparison ot Agiola\ and Lactulose in elderlv patients with chiomc constipation Phaimacol 1993 47(suppl I) 249-52 &. Kinnunen O Winblad I, Koistinen P Salokannel J Safety and efficacy of a bulk laxative
containing senna versus lactulose in the treatment of chronic constipation in geriatric patients Pharmacol 1993 47(suppl 1)253-5) Constipation induced by drugs such as the anti-diarrheal medicine loperamide (Imodium®) has also been shown to be improved by senna in a clinical trial (Ewe K Ueberschaer B, Press AG influence of senna, fibre and fibre & senna on colonic transit in loperamide-induced constipation Pharmacol 1993, 47(suppl f) 242-8)
Constipation is often associated with several disorders such as gas, bloating cramps acidity nausea irritation, abdominal discomfort and pain Although several pnor art literature is available for the treatment of constipation but still there exists an unmet need for compositions which would be effective in the overall management of constipation including the prophylaxis or amelioration or treatment of not only the constipation but also associated disorders thus providing a better relief to the user The novel compositions of the present invention overcomes such limitations of prior art
SUMMARY OF THE INVENTION
It is an objective of the present invention to provide novel compositions comprising at least one bowel evacuant as the active agent and a saccharide component, optionally with at Jeast one component selected from a group comprising antacid, stool softener, antiflatulant prokmetic anti-emetic and tonifier, and optionally one or more excipient(s)
It is an objective of the present invention to provide novel compositions comprising at least one laxative and/or a purgative as the bowel evacuant and a saccharide component optionally with at least one component selected from a group comprising antacid, stool softener, antiflaiulant prokmetic, anti-emetic and tonifier, and optionally one or more excipient(s)
it is an objective of the present invention to provide novel compositions comprising at least one laxative and/or a purgative as the bowel evacuant a saccharide component and at least one tonifier optionally with at least one component selected from a group comprising antacid stool softener, antiflatulant, prokmetic and anti-emetic and optionally one or more excipient(s)
It is an objective of the present invention to provide novel compositions comprising ispaghnla as the bowel evacuant and lactulose as the saccharide component tnphala as the tonifier optionalK with at least one component selected from a group comprising docusate sodium as the stool softener, simethicone as the antiflatulant antacid and prokmetic and one oi moie excipients
It is an objective of the present invention to provide novel compositions comprising ispaghula and tnphala as bowel evacuants and lactulose as the saccharide component optionally with at least one component selected from a group comprising docusate sodium as the stool softener simethicone as the antiflatulant antacid and prokinetic and one or more excipients
It is an objective of the present invention to provide novel compositions comprising tnphala as the as the bowel evacuant and lactulose as the saccharide component optionally with at least one component selected from a group comprising peppermint, fennel ajwain mentha extract and lactobacillus optionally with at least one antacid and/or an antiflatulant and/or a prokinetic and one or more excipients
It is another objective of the present invention to provide process for preparation ol such compositions
It is yet another objective of the present invention to provide method of using such compositions which comprises administering to a subject in need thereof an effective amount of the composition
The novel compositions of the present invention can be manufactured for pharmaceutical use or can be used as a dietary supplement and are useful in the overall management of constipation including the prophylaxis and/or amelioration and/or treatment particularly of constipation and associated disorders
DETAILED DESCRIPTION OF THE INVENTION
The present invention provides novel composition comprising at least one bowel evacuant as the active agent and a saccharide component optionally with at least one component selected trom a group comprising antacid, stool softener antiflatulant, prokinetic, anti-emetic and tonifier and optionally one or more excipient(s)
In an embodiment of the present invention is provided novel compositions comprising at least one laxative and/or a purgative as the bowel evacuant and a sacchandc component optionallv with at least one component selected from a group comprising antacid stool softener antiflatulant and prokinetic agent, and one or moie excipients
In an embodiment of the present invention is provided novel compositions comprising at least one laxative and/or a purgative as the bowel evacuant, a saccharide component and at least one tonifier, optionally with at least one component selected from a group comprising antacid stool softener, antiflatulant and prokinetic and one or more excipients
Preferably the bowel evacuant is a laxative such as tnphala or ispaghula or a purgative such as senna, the saccharide component is lactulose the stool softener is docusate sodium the antiflatulant is simethicone, the prokinetic/anti-nauseating/anti-emetic agent is dompendone or tegaserod
In an embodiment of the present invention is provided a novel composition comprising ispaghula as the bowel evacuant, lactulose as the saccharide component, tnphala as the tonifier and optionally with at least one component selected from a group comprising docusate sodium as the stool softener and/or simethicone as the antiflatulant optionally with at least one antacid and/or a prokinetic, and one or more excipients
In an embodiment of the present invention is provided a novel composition comprising ispaghula and tnphala as bowel evacuants and lactulose as the saccharide component optionally docusate sodium as the stool softener and/or simethicone as the antiflatulant optionally with at least one antacid and/or a prokinetic, and one or more excipients In a preferred embodiment the composition of the present invention comprises ispaghula as the bowel evacuant lactulose as the saccharide component, and tnphala as the tonifier optionally with one or more excipients
In another embodiment, the composition of the present invention comprises tnphala as the as the bowel evacuant and lactulose as the saccharide component optionally with at least one component selected from a group comprising peppermint fennel ajwain mentha extract and lactobacillus optionally with at least one antacid and/or an antiflatulant and/or a prokinetic and one or more excipients
In an embodiment of the present invention the bowel evacuant is selected from but not limited to a group comprising tnphala bulk laxatives such as ispaghula powder methylccllulose (Citrucel) polvcarbophil malt soup extract ethulose sterculia linseed tnticum 01 mixtures thereof osmotic laxatives such as magnesium caibonate magnesium oxide magnesium pet oxide magnesium sulfate mineral salts in combination sodium sulfate pentaenthrit\l macrogol
glycerol, sodium phosphate magnesium citrate, sodium tartrate or mixtures thereof stool softeners such as docusate, poloxamer 188, dioctyl sodium sulfosuccinate, or mixtures thereof lubricant/emollient such as mineral oil hydrating agents such as dibasic sodium phosphate magnesium citrate, magnesium hydroxide (Milk of Magnesia) magnesium sulphate monobasic sodium phosphate sodium biphosphate or mixtures thereof carbon dioxide releasing laxatives such as potassium bitartrate, sodium bicarbonate or mixtures thereof and the like used either alone or in combination thereof
In a prefered embodiment, the bowel evacuant of the present invention is Ispaghula or Triphala either used as an extract or in the powder form The extract can be aqueous or non-aqueous The solvents used in the non-aqueous extraction process is selected from but not limited to a group comprising alcohols such as methanol, ethanol, butanol, isopropyl alcohol or the like acetone glycerol ethylacetate and alkylene glycols such as methylene glycol ethylene glycol propylene glycol or the like used either alone or in combination thereof A hydro-alcoholic extract is prefered The general procedure for the preparation of the Triphala extract is as follows Equal parts of dried Amalaki (Emblica officinalis or Phyllanthus emb/ica), Hantaki (Terminalia chebula) and Bibhitaki {Terminalia belenca) are taken and mixed together followed bv pulverization The powder thus obtained (hereinafter releired to as lnphala powder ) is-then extracted with a suitable solvent (aqueous non-aqueous or hydro-alcoholic) preferably b> applying heat The extraction is preferably done 3-5 times under heat and reflux conditions to ensure proper extraction Then the solvent is removed from the liquid extract to obtain the drv extract The dry extract (referred to hereinafter as Triphala extract ) thus obtained is preferably sifted through a suitable sieve to break any lumps or agglomerates The general procedure for the preparation of the psyllium seed husks extract is as follows Milled psyllium seed husks were stirred with potassium hydroxide containing sodium borohydnde in a nitrogen atmosphere The mixture was centnfuged The supernatant was decanted from an insoluble fraction that had settled out in the centrifuge bottle The insoluble fraction was stirred with fresh potassium hydroxide-sod nun borohydnde solution and le-ccntnfuged The supcrnatants from both centrifugations were combined The pH of the combined supernatants was adjusted to 4 5 with glacial acetic acid with stirring at ambient temperature then again centnfuged I he supernatant was decanted from a gel mass that had settled out in the centnfuge bottle The gel was washed gently with water to remove adhering supernatant solution and this wash water was added to the supernatant The gel fraction was desiccated by treatment with 95% ethanol and finally washed with diethyl ether and dried Pnoi to desiccating, in some instances the traction was furthei
purified by repeating the alkaline solubilization and acidification steps described above The gel was re-suspended in potassium hydroxide acidified to pH 4 5 and centrifuged to recover the gel
In another embodiment of the present invention, the tonifier used in the composition is triphala In further embodiment of the present invention, the bowel evacuant comprises a mixture oi Triphala and Ispaghula In the present invention, the Triphala particularly acts as a tonifier and detoxifier especially for the gastro-mtestinal tract (GIT) Such compositions are employed tor prophylaxis, amelioration or therapeutic treatment of constipation and other associated disorders and also serve as an effective remedy particularly for extended periods ol time thus leading to considerable patient compliance
In another embodiment, the saccharide component is selected from but not limited to a group comprising lactulose, lactitol, sorbitol mannitol, maltodextnn, dextran, sucrose, maltitol dextrose and the like or mixtures thereof
The purgativts useful in the present invention include but not limited to a group comprising casanthranol cascara, aloe, castor oil, dehydrocholate phenolphthalem senna sennosides sodium picosulfate, dantron, bisoxatin or the like used either alone or in combination thereof The dried ripe fruits pods or leaves of Senna (preferably Cassia angustijoha) as powder concentrated infusion or liquid extract can be used in the present invention
Particularly preferred bulk laxatives lor use in the present invention are fibers I wo types ot fibers namely soluble and insoluble can be used in the composition of the present invention Soluble fibers are viscous, gel-forming fibers which absorb water and makes stools softer and easier to pass Further, soluble fibers are the edible parts of plants or similar carbohydrates resistant to digestion and absorption in the human small intestine with complete or partial fermentation in the large intestine fermentation of the undigested soluble fibers occurs by the action of colonic bacteria producing gases and short-chain fatty acids such as butyric acetic propionic, and valeric acids Soluble fibers found in psyllium seed husk (about 66% soluble fibers) vegetable gums from legumes (guar gum locust bean gum) and gummy exudates (gum acacia and tragacanth) seed mucilages from oats rye and barley mucilages from certain vegetables and roots such as broccoli carrots lady fingers yam pectin from hints and vegetables are particularly used Insoluble fibets are indigestible cellulosed and ligmficd vegetable fibers found in cereal brans and fruit skins which absorb water but do not dissolve in
it The insoluble fibers are also not fermented in the intestine Insoluble fibers useful in the present invention are found in fruits vegetables whole grain breads and cereals Wheat bran contains mostly insoluble fiber, while oat bran contains about 7% soluble fiber Synthetic fibers may also be useful in the present invention Several synthetic water soluble or water absorbing fibers have been prepared by modification of cellulose and other natural fibers such as methyl cellulose, carboxymethyl cellulose polycarbophil and the like
The novel composition of the present invention can be manufactured for pharmaceutical use or can be used as a dietary supplement The composition of the present invention particularly upon daily use help in restoring normal bowel functions, and also tomfies and detoxifies the GIT
In a further embodiment of the present invention, a blend of Lactobacillus cultures and/or other useful microorganisms with or without an ammo acid such as L-lysine which colonize the intestine can also be used as an additional component These cultures continually product enzymes which support the digestive system and normalize the intestine which aids normal digestion It also provides relief for cramps, bloating diarrhea constipation and urgency Such probiotics are preferably selected from but not limited to different Lactobacillus species used either alone or in combination such as Lactobacillus renter/ and Lactobacillus paracasei
Antacids useful in the present invention are selected from but not limited to a group comprising alkaline earth metal oxides, peroxides, hydroxides and the like or mixtures thereof Anti-gas/antiflatulant agents useful in the present invention is selected from but not limited to a group comprising simethicone dimethicone, bisacodyl, alpha-galactosidase enzyme activated charcoal and the like or mixtures thereof These agents particularly aid in the reduction of acid and gas/flatulence and the accompanying lower abdominal pain
Prokinetic agents useful in the compositions of the present invention primarily to improve the motility of the gastrointestinal tract are selected from but not limited to a group comprising 5HT4 agonist and 5HT3 antagonist such as cisapride ltopnde mosapridc dompendonc metoclopramide, tegaserod and the like or mixtures thereof Natural prokmetics such as Dai-kenchu-to can also be used Smooth muscle relaxants such as mebevenne peppermint oil and ajwain oil that have direct relaxant properties on gut smooth muscle are also uselul Antispasmodic agents such as dicyclomine and hvoscvamme aie also useful Anticholinergic agents that can be used in the present compositions as additional components act b\ decreasing
the abnormal sensitivity of cholinergic (muscarinic M2) receptors in gut smooth muscle leading to significant improvement in abdominal pain and rectal urgency Other categories of active agents suitable for the treatment of disorders associated with constipation can also be used in the composition of the present invention The stool softener useful in the compositions of the present invention is selected from but not limited to a group comprising docusate sodium soluble fibers and the like or mixtures thereof Such agents are employed to keep stool soft for easy natural passage and avoid painful anorectal conditions
Additionally other ingredients such as carminatives ginger turmeric chamomile caraway fennel, mentha extract, or any other natural or semi-synthetic or synthetic ingredient useful tor the management of constipation or associated disorders can be used in the present invention to relax and calm the stomach and promote healthy digestion, preferably incorporated into the composition as oils The novel compositions of the present invention also assist in relief and discomfort of gas, acid indigestion, sour stomach upset stomach or cramps associated with constipation Various enzymes either alone or in combination that can be used in the present invention include but not limited to lactase that helps in digesting the lactose or milk sugar found in dairy products, alpha-galactosidase that helps in digesting the complex sugars found in beans and other legumes and in cruciferous vegetables protease that helps to break down the peptide bonds in protein foods amylase that helps to digest the starchy carbohydrates in foods and lipase which helps to digest the fats in food Sweeteners such as aspartame acesulfame saccharine, cyclamate, glycyrrhizin steviosides talm dihydrochalcone compounds and mixtures thereof can also be used in the present invention preferably in a quantity from about 0 001% to about 3% by weight of the composition
The one or more excipient(s) that can be used for preparation of such compositions are selected from but not limited to diluents, dismtegrants, binders, fillers bulking agents anti-ddherants anti-oxidants, buffering agents, colorants flavoring agents coating agents plasticizers organic solvents stabilizers preservatives lubricants glidants chelating agents release modifiers and the like known to the art used either alone or in combination thereol In an embodiment the fillers used in the present invention is selected from but not limited to a group eompnsing lactose mannitol sorbitol starch microcrystalline cellulose xylitol fructose sucrose dextrose dicalcium phosphate calcium sulphate maltodexlrin, polyethylene glycol such as PI G 100 PLG 2000 and PEG 6000, polyvinylpyrrolidone, sodium chloride sodium citiatc citric acid water soluble celluloses such as low viscosity hydioxyethyl cellulose hydroxypropyl mcthylcellulosc
hydroxypropyl cellulose and the like or mixtures thereof The disintegrates used tn the present invention include but not limited to starch or its dei lvatives pregelatimzed starch croscarmellose sodium, sodium starch glycollate, and the like used either alone or in combination thereof The lubricants used in the present invention include but not limited to talc magnesium stearate calcium stearate stearic acid hydrogenated vegetable oil and the like used either alone or in combination thereof The release modifiers used in the present invention is selected from but not limited to a group comprising methacrylic acid copolymers such as Eudragit® cellulosic polymer such as alkyl celluloses or hydroxyalkyl celluloses, gums, hydrophilic polysaccharides such as alginates, chitosan, scleroglucan or semi-synthetic polysaccharides, lipid components such as hydrogenated vegetable oils, waxes glyceryl behenate and the like, or mixtures thereof
In an embodiment, the compositions of the present invention are in the form of immediate release or controlled release or a combination of immediate release and controlled release particularly intended for delivery of the active agent(s) for an extended time period The dosage form may be in the form of tablets minitablets capsules pellets granules patches powders sachets or liquids or other dosage forms suitable for preferably oral administration or enemas or suppositories In a preferred embodiment, the composition of the present invention is in the form of granules or powder filled into sachets or capsules, or granules or powder compressed into tablets that may be optionally filled into capsules
In another embodiment the composition of the present invention is highly effective in the management of constipation including prophylaxis and/or amelioration and/or treatment of constipation and associated disorders such as gas, bloating, cramps acidity, irritation abdominal pain and discomfort thus providing a better relief to the user In a still further embodiment the composition of the present invention is useful in the treatment and/or management of diseases or disorders of the bowel primarily associated with constipation, diarrhea or indigestion
The present invention also provides process for prepaiation of such compositions in an embodiment the process for preparation comprises mixing the active agent(s) and saccharide component optionally with at least one component selected from a group comprising antacid stool softener, antiflatulant prokinetic anti-emetic and tonifier and one or more excipient(s) and formulating into a suitable dosage form
In yet another embodiment of the present invention is provided method of using such composition which comprises administering to a subject in need thereof an effective amount of the composition In a further embodiment is provided a method wherein the composition of the present invention is useful for prophylaxis and/or amelioration and/or treatment of constipation and associated disorders such as gas, bloating, cramps acidity irritation, abdominal pain and discomfort In a still further embodiment is provided a method wherein the composition of the present invention is useful as a dietary supplement to normalize bowel functions and provide relief from particularly constipation and other associated disorders
In yet another embodiment is provided method of using such composition as a dietary supplement to normalize bowel functions and provide relief from particularly constipation or other associated disorders The compositions of the present invention are also useful in the treatment and/or management of diseases or disorders of the bowel primarily associated with constipation diarrhea or indigestion The compositions of the present invention are also useful for the treatment/management of Irritable Bowel Syndrome (IBS) predominantly associated with constipation
The examples given below serve to illustrate embodiments of the present invention However they do not intend to limit the scope of the present invention in any manner whatsoever
EXAMPLES
Example-1
S No Ingredient Quantity (per serving)
1 lspaghula husk powder 3 50 g
2 Lactulose powder l00 0g
3 Tnphala powder 1 00 g
4 Methyl paraben sodium 30 00 mg
5 Propyl paraben sodium 3 00 mg
6 Sodium saccharin 20 00 mg
7 Purified water q s (lost in processing) Procedure
i) lspaghula husk powder Lactulose powder and Tnphala powder were sifted through // 40
mesh sieve and mixed well
n) Methyl paraben sodium Propvl paraben sodium and Sodium saccharin were dissolved in
Purified water in) The material of step (i) was granulated with the solution of step (n) iv) Granules of step (in) were dried and sifted through # 30 mesh sieve and delivered in the
form of sachets
Example-2
S No Ingredient Quantity (mg/tablet)
1 Tnphala extract 325 0
2 Lactulose 1000 0
3 Polyvinylpyrrolidone 50 0
4 Dried Starch powder 50 0
5 Magnesium stearate 10 0 Procedure
i) Tnphala extract and Lactulose were sifted through # 30 mesh sieve and mixed
u) Polyvinylpyrrolidone and Dried Starch powder were sifted through #40 mesh sieve
in) The material of step (i) was mixed the material of step (n)
iv) Magnesium stearate was sifted through #60 mesh sieve and added to the material of step
(in) followed by mixing v) The material of step (iv) was compressed into tablets
E\ample-3
S No Ingredient Quantity (per serving)
1 Tnphala extract 325 0 mg
2 Lactitol 10 Og
3 Ajwainoil 50 0 mg
4 Purified water q s (lost in processing)
5 Sodium saccharin 0 01 g Procedure
i) f riphala extract and Lactitol were sifted through # 30 mtsh sieve and mixed
ii) Ajwain oil was added to the material of step (i) and mixed in) Sodium saccharin was dissolved in Purified water
iv) The material of step (n) was granulated using the material of step (in) to obtain the granules which weie then dried
v) 1 he material of step (iv) was passed through #30 mesh sieve to vield the product
E\ample-4
S No Ingredient Quantity (per serving)
1 Tnphala extract 0 65 g
2 Maltitol l0 00g
3 AIpha-galactosidase enzyme 380 GalU
4 Purified water q s (lost in processing)
5 Sodium saccharin 0 01 g Procedure
i) Tnphala extract, Alpha-galactosidase enzyme and a part of Maltitol were mixed
n) Remaining part of Maltitol and Sodium saccharin were dissolved in Purified water
HI) The material of step (i) was granulated using the material of step (II) to obtain the
granules which were then dried iv) The material of step (HI) was passed through #30 mesh sieve to yield the product
ExampIe-5
S No Ingredient Quantity (per serving)
1 Ispaghula powder 1 50 g
2 I nphala powder I 20 g
3 Dextrose 8 00 g
4 Purified water q s (lost in processing)
5 Sodium saccharin 0 01 g Procedure
i) Ispaghula powder, Tnphala powder and a part of Dextrose were mixed
u) Sodium saccharin was dissolved in Purified water
in) The material of step (I) was granulated using the material of step (n) to obtain the
granules which were then dried iv) The material of step (in) was passed through #30 mesh sieve to yield the desired granules
which is then provided in a suitable package
E\ample-6
S No Ingredient Quantity (per serving)
I Tnphala extract 0 65 g
2 Lactulose 15 00 g
3 Peppermint oil 0 05 ml
4 Fennel oil 0 03 ml
5 Purified water q s (lost in processing)
6 Glycirrhizin 0 01 g Procedure
i) Triphala extract and a part of Lactulose were mixed
n) Peppermint oil and Fennel oil were dissolved in ethanol
in) Remaining part of Lactulose and Glycirrhizin were dissolved in Purified water
iv) The material of step (u) was added to material of step (in) with continuous stirring
v) The material of step (i) was granulated using the material of step (iv) to obtain granules
which were then dried
vi) The material of step (in) was passed through #30 mesh sieve to yield the product
Example-7
S No Ingredient Quantity (per serving)
1 Triphala powder 2 0 g
2 Maltitol 12 0g
3 Lactobacillus 106 CFU
4 Ginger oil 2 0 ml
5 Sodium saccharin 0 008 g Procedure
i) Triphala powder and a part of Maltitol were mixed together
n) Remaining part of Maltitol Sodium saccharin Lactobacillus and Ginger oil were mixed
together in) The material of step (I) and the material ot step (u) were then mixed thoroughly iv) The material of step (in) was passed through #30 mesh sieve to yield the powder
Example-8
S No Ingredient Quantity (mg/tablet)
1 Triphala extract 325 0
2 Polycarbophil 80 0
3 Sorbitol 400 0
4 Docusate sodium 50 0
5 Citric acid 1 0
6 Purified water q s (lost in processing)
7 Aspartame I 0
8 Magnesium stearate 9 0 Procedure
i) Tnphala extract, Polycarbophil and Sorbitol were mixed
n) Docusate sodium and Citric acid were dissolved in Purified water
in) The material of step (i) was granulated using the material of step (n) to obtain the
granules which were then dried iv) The material of step (in) was passed through #30 mesh sieve and mixed with Magnesium
stearate sifted through #40 mesh sieve v) The material of step (iv) were compressed into tablets
Example-9
S No Ingredient Quantity (mg/tablet)
1 Tnphala extract 325 0
2 Mannitol 220 0
3 Simethicone 125 0
4 Calcium phosphate tnbasic 40 0
5 Docusate sodium 50 0
6 Citric acid I 0
7 Purified water q s (lost in processing)
8 Aspartame 1 0
9 Colloidal silicon dioxide 7 0 Procedure
i) Tnphala extract, Mannitol Simethicone and Calcium phosphate tnbasic were mixed
n) Docusate sodium, Citric acid and Aspartame were dissolved in Purified water
MI) The material of step (i) was granulated using the material of step (n) to obtain the
granules which were then dited iv) The material ot step (in) was passed through #30 mesh sieve and mixed with C olloidal
silicon dioxide sieved through #40 mesh sieve v) The gianules were compressed into tablets
Example-10
S No Ingredient Quantity (g/100 ml)
1 Tnphala extract 13 00
2 Bisacodyl 0 01
3 Magnesium hydroxide I 20
4 Mannitol 6 05
5 Sodium carboxymethy! cellulose I 20
6 Methyl paraben 0 75
7 Propyl paraben 0 15
8 Flavoring agent 0 03
9 Acesulfame potassium 0 05
10 Ethanol qs (lost in processing)
11 Purified water qs to 100 ml Procedure
i) Tnphala extract, Bisacodyl Magnesium hydroxide and Mannitol were mixed
u) Propyl paraben and the Flavoring agent were dispersed in Ethanol with stirring
in) Sodium carboxymethyl cellulose Methyl paraben and Acesulfame potassium were
dispersed in Purified water
iv) The material of step (u) was added to the material of step (in) with stirring
v) The material of step (i) was added to the material of step (iv) with continuous stirring to
obtain a homogeneous dispersion
Example-11
S No Ingredient Quantity (mg/tablet)
1 Tnphala extract 325 0
2 Senna powder 300 0
3 Maltodextnn 340 0
4 Sodium cyclamate 1 I 5
5 Sodium bicarbonate 68 5
6 Tartancacid 110 0
7 Flavoring agent 0 025
8 Ethanol q s (lost in processing)
9 Demmerali/ed water qs (lost in processing)
Procedure
i) Tnphala extract Senna powder Makodextnn and Sodium cyclamate were mixtd
together and sieved n) The mixture of step (i) was kneaded with a mixture of Ethanol and Demineralized water
granulated and dried in) Sodium bicarbonate Tartaric acid and the Flavoring agent were mixed and sieved to
give a mixture iv) The mixture obtained in step (n) and (in) are mixed together and compressed into
effervescent tablets
Example-12
S No Ingredient Quantity (g/sachet)
1 Tnphala powder 2 50
2 Lactulose 11 00
3 Calcium hydroxide 0 10
4 Sodium saccharin 0 01
5 Peppermint oil 0 06 ml
6 Orange oil 0 04ml Procedure
i) Tnphala powder, Lactulose and Calcium hydroxide were mixed
u) The powder of step (I) was screened on a #80 mesh sieve and to it were added Sodium
saccharin Peppermint oil and Orange oil, and mixed m) The mixture was filled into sachets
Example-13
S No Ingredient Quantity (per serving)
1 Tnphala extract 0 65 g
2 Senna 1 0 g
3 Dextran 2 0 g
4 Talcum 0 5 g
5 Gum acacia 0 I g
6 Ethanol q s (lost in processing)
7 Punfied water qs (lost in processing)
8 Peppermint oil 0 04 ml
9 Sodium saccharin 0 02 g
Procedure
i) Tnphala extract. Senna and Dextran were sifted through #30 mesh sieve and mixed
together n) Gum acacia and Sodium saccharin was dispersed in Purified water by stirring HI) Peppermint oil was dissolved in ethanol and mixed with the material of step (n) iv) The material of step (I) was granulated by using the material of step (m) to obtain
granules v) The granules were dried using fluidized bed dryer vi) The dried granules were then mixed with Talcum thus yielding the final product
Example-14
S No Ingredient Quantity
1 Flour (#30 mesh passed) 100 0 g
2 Ispaghula husk (#30 mesh passed) l00 0g
3 Tnphala extract 32 5 g
4 Lactulose liquid 200 0 ml
5 Shortening (fat) 120 0 g
6 Cocoa powder 10 0 g
7 Baking powder 2 0 g
8 Liquid glucose 5 0 g
9 Milk powder 5 0 g
10 Vanilla essence 2 0 ml
11 Almond essence 1 drop Procedure
i) Shortening (fat) and Lactulose were tilled together very lightly until a fluffy consistency
was obtained u) Liquid glucose was added to step (i) and mixed in) Flour, Ispaghula husk and Tnphala extiact were sifted through a #30 mesh sieve and the
fraction passing through the sieve was collected iv) Cocoa powder Baking powder Milk powder Vanilla ecsence and Almond essence were
mixed with the material of steps (u) & (in)
v) The mixture of step (iv) was made into smooth & soft dough rolled into requncd
thickness and cut into desired size and baked at optimum tempeiature to obtain biscuits
Example-15
S No Ingredient Quantity (g)
1 Ispaghula powder 0 120
2 Maltodextnn I 669
3 Dompendone 0 01
4 Sodium cyclamate 0 115
5 Sodium bicarbonate 0 7
6 Tartaric acid 1 12
7 Flavoring agent 0 025
8 Ethanol q s (lost in processing)
9 Demineralized water q s (lost in processing) Procedure
0 Ispaghula powder, Maltodextrin Dompendone and Sodium cyclamate were mixed
together and sieved
n) The mixture of step (i) is kneaded with a mixture of Ethanoi and Demineralized water
granulated and dried m) Sodium bicarbonate Tartaric acid and the Flavoring agent are sieved and mixed well iv) The mixture obtained in step (n) and (m) are mixed together and compressed into
effervescent tablets
Example-16
S No Ingredient Quantity (g)
1 Ispaghula husk 3 50
2 Lactulose 10 00
3 Purified water q s (lost in processing)
4 Sodium saccharin 0 01 lotal 13 51
Procedure
i) Ispaghula husk and a part of Lactulose weie mixed
n) Remaining part of Lactulose and Sodium saccharin were dissolved in Purified water
in) The material of step (i) was granulated using the material of step (n) to obtain the
granules which were then dried iv) The material of step (in) was passed through /?30 mesh sieve to yield granules
Example-17
S No Ingredient Quantity
1 Lactulose powder 215 0g
2 I nphala extract 32 5 g
3 Hour 200 0g
4 Shortening (fat) 1100g
5 Salt 1 0 g
6 Milk 60 ml
7 Milk, powder 10 0g
8 Cocoa powder 10 0 g
9 Chocolate Chips l00 0g
10 Vanilla essence 3 ml
11 Almond essence 1 drop
12 Baking powder 4 0g Procedure
i) Shortening (fat) is tilled lightly until a fluffy consistency is obtained
n) Add Milk to step (I) & stirred continuously to give a creamy consistency
in) Add Vanilla & Almond essence to step (n) and mix
iv) Mix Tnphala extract, Lactulose powder Flour Salt Milk powder Cocoa powder
Baking powder & Chocolate Chips uniformly & add to step (in) and make smooth & soft
dough
v) Roll the dough to required thickness & cut to desired size and bake at optimum
temperature to obtain biscuits
Example-18
S No Ingredient Quantity
1 Flour 100g
2 Husk (mesh no 30) 100 g
3 Lactulose liquid 200 ml
4 Shortening (fat) 120 g
5 Cocoa powder 10 g
6 Baking powder 2 g
7 Liquid glucose 5 g
8 Milk powder 5 g
9 Vanilla essence 2 ml
10 Almond essence 1 drop Procedure
i) Shortening (fat) and Lactulose are tilled together very lightly until a fluffy consistent is
obtained n) Add Liquid glucose to step (i) & mix again in) Sift V lour and Husk through a sieve of mesh no 30 iv) Mix Cocoa powder, Baking powder Milk powder Vanilla essence and Almond essence
and mix with step (n) & (in) v) The mixture of step (iv) is made into smooth & soft dough rolled into required thickness
and cut into desired size and baked at optimum temperature

We claim:
1. A novel composition comprising at least one bowel evacuant as the active agent and a saccharide component, optionally with at least one component selected from a group comprising antacid, stool softener, antiflatulant, prokinetic, anti-emetic and tonifier. and optionally one or more excipient(s).
2. A composition according to claim 1, wherein the bowel evacuant is a laxative selected from a group comprising bulk laxatives such as ispaghuia powder, methylcellulose, polycarbophil, malt soup extract, ethulose, sterculia, linseed, triticum, or mixtures thereof; osmotic laxatives such as magnesium carbonate, magnesium oxide, magnesium peroxide, magnesium sulfate, mineral salts in combination, sodium sulfate, pentaerithrityl, macrogol, glycerol, sodium phosphate, magnesium citrate, sodium tartrate, or mixtures thereof; carbon dioxide releasing laxatives such as potassium bitartrate, sodium bicarbonate, or mixtures thereof, or a purgative selected from a group comprising casanthranol, cascara, aloe, castor oil, dehydrocholate, phenolphthalein, senna, sennosides, sodium picosulfate, dantron. bisoxatin, used either alone or in combination thereof, or mixtures thereof.
3. A composition according to claim 1, wherein the saccharide component is selected from a group comprising lactulose, lactitol, sorbitol, mannitol, maltodextrin, dextran, sucrose. maltitol, dextrose, or mixtures thereof.
4. A composition according to claim 1. wherein the composition comprises ispaghuia as the bowel evacuant, lactulose as the saccharide component, triphaia as the tonifier, optionally with at least one component selected from a group comprising stool softener, antiflatulant, antacid, anti-emetic and prokinetic, and one or more excipients.
5. A composition according to claim 1, which comprises triphaia as the as the bowel evacuant and lactulose as the saccharide component, optionally with at least one component selected from a group comprising peppermint, fennel, ajwain, mentha extract and lactobacillus optionally with at least one antacid and/or an antiflatulant and/or a prokinetic, and one or more excipients.
6. A composition according to any of the preceding claims which is highly effective in the management of constipation including prophylaxis and/or amelioration and/or treatment of
constipation and associated disorders such as gas, bloating, cramps, acidity, irritation, abdominal pain and discomfort thus providing a better relief to the user.
7. A composition according to any of the preceding claims 1-5 which is useful as a dietary supplement to normalize bowel functions and provide relief from particularly constipation and other associated disorders.
8. A composition according to any of the preceding claims 1-5 which is useful in the treatment and/or management of diseases or disorders of the bowel primarily associated with constipation, diarrhea or indigestion.
9. A process of preparation of the composition according to claim 1, which comprises mixing the active agent(s) and saccharide component optionally with at least one component selected from a group comprising antacid, stool softener, antiflatulant, prokinetic, antiemetic and tonifier, and one or more excipient(s) and formulating into a suitable dosage form.
10. The pharmaceutical compositions and process for the preparation of such compositions substantially as herein described and illustrated by the examples.