STABLE LACTASE DROPS

FIELD OF THE INVENTION

The present invention relates to pharmaceutical compositions of lactose intolerance. Particularly, the present invention relates to pharmaceutical compositions of lactase drops for Infants.

BACKGROUND OF THE INVENTION

The human digestive system uses a series of enzymes to break down complex foods into simple molecules (e.g., sugars, peptides and lipids) that can be absorbed by the body. The inability or diminished capacity of the body's production of one or more enzymes that are crucial for proper digestion can lead to gastrointestinal symptoms that have been characterized by the medical community as irritable bowel syndrome (IBS). A patient with IBS typically presents clinically with one of three variants: i) chronic abdominal pain and constipation (also known as spastic colitis); ii) chronic intermittent diarrhea, often without pain; or iii) both features, in an alternating cycle of constipation and diarrhea.

Milk products contain lactose, which, when hydrolyzed, yield glucose and galactose. This hydrolysis is enzymatically catalyzed by .lactase or .beta.-D-galactosidase. This enzyme is normally present in the intestinal juices and mucosa. Decreased or non¬existent intestinal lactase activity, known as lactose intolerance, is a deficiency that appears in pediatric, adolescent and adult populations. The inability to hydrolyze lactose into its component sugars results in bloating, cramping, abdominal pain, or flatulence after the ingestion of milk or dairy products. In severe cases, malabsorption resulting from lactose intolerance may result in anorexia and weight loss.

Lactose intolerance in humans can-be treated in several ways. Prehydrolyzed milk and dairy products, having significantly reduced levels of lactose, are commercially available. Supplements in the form of fungal or yeast-derived lactases that are added to • lactose-containing liquids are also available. The lactase may also be in the form of a tablet, which is ingested immediately before the consumption of milk products.

US 4,464,469 patent discloses an stable aqueous solution of a yeast lactase containing stabilizing agent of polyols for increasing shelf-life of the solution, where the pH of the solution is maintained at 7.0.
US 6,955,903 patent discloses preblend for the manufacture of lactase tablets comprising: from about 3000 to about 9000 FCC lactase units; and from about 40 to about 80 weight percent microcrystalline cellulose.

US 7,700,093 patent discloses method for increasing lactose digestion in a subject, comprising the steps of: identifying a subject having lactose intolerance, and administering to said subject a composition comprising an effective amount of viable Bacillus coagulans bacteria and an effective amount of supplemental lactase to increase lactose digestion in said subject, wherein said bacteria are selected from the group consisting of GB1-20, ATCC PTA-6085; GBI-30, ATCC PTA-6086; and GBI-40, ATCC PTA-6087.

US 6,660,313; 6,365,208 patents discloses stable lactase composition containing a) from about 1% to about 20% by weight of a combination of lactase and cutting agent b) from about 1% to about 98% by weight of microcrystalline cellulose; c) from about 0% to about 97% by weight of mannitol; and d) an effective amount of lubricant to aid compression. The cutting agents are used for lactase potency compensation which are selected from any inert pharmaceutical excipient, including, sugars, starches, cellulose and inorganic salts.

US 6,410,018 patent discloses solid, orally administrable composition for the enzymatic hydrolysis of lactose, comprising two types of lactases, one is having pH range of 3-6 and the second is having pH of 6-8 and a solid pharmaceutically acceptable carrier US 20080193598 patent application discloses lactase particulate composition comprising a plurality of particles comprising lactase and a protective material. This particulate composition can be used by applying the lactase composition to a food article or by using the lactase composition in the course of consuming the food article. The protective mateΠal is selected from the group consisting of amylose acetate phthalates styrene maleic acid copolymer cellulose acetate succinate, cellulose acetate phthalate, polyvinyl acetate phthalate, hydroxypropylmethylcellulose phthalate, fatty acids, hydroxypropyl methylcellulose (HPMC), glycerol triacetate (triacetin), Marcoat, gum acacia, glycerin, fatty acid esters, glycerol esters, polyglycerol esters, paraffin waxes, carnauba wax, formalized gelatin, shellac wax, hydrogenated vegetable waxes, and combinations thereof.

US 20060013807 patent application discloses rapidly disintegrating solid oral dosage form for controlling lactose intolerance in a patient in need thereof, the dosage form comprising: an effective amount of lactase, and an effective amount of a plurality of superdisintegrants. The patent application discloses superdintegrants are selected from a cross-linked polyvinyl pyrollidone, a cross-linked carboxymethyl cellulose, and a cross-linked starch.

EP166601 patent application discloses enzyme composition containing mixture of a lactase, an emulsifying agent and, optionally, a stabilising agent, the composition being in particulate form with the lactase and, where present, the stabilising agent dispersed in the emulsifying agent.

WO2010057188 patent application discloses rapidly disintegrating solid oral dosage form of lactase comprising: a lactase; and a lactase dissolution-enhancing amount of a compressible sugar component and fructose wherein the compressible sugar component and the fructose enhance the dissolution of the lactase component.

The above prior-arts disclose various lactase containing formulations like tablets, particulate composition, rapidly disintegrating solid dosage forms and others. All these formulations are useful for Adults and are not useful for Infants where they could not able to swallow tablets or granules. Hence, there is need to develop formulations for Infants which are easily administrable to infants. The present inventors during their continuous efforts developed lactase drops for Infants.

SUMMARY OF THE INVENTION

The main embodiment of the present invention provides stable lactase drops composition having pH of about 4.0 - 5.0, wherein the composition comprises Lactase, polyol and one or more buffering agents.

In another embodiment of the present invention provides process for preparing stable lactase drops composition.

DETAILED DESCRIPTION OF THE INVENTION

The present invention provides stable lactase drops composition having pH of about 4.0 - 5.0, wherein the composition comprises Lactase, polyol and one or more buffering agents.

Polyols according to the present invention are selected from lactose, glycerol, sucrose, xylitol, mannitol, sorbitol, maltilol, lactitol and combinations thereof. Preferred polyol is Glycerol.

One or more buffering agents used according to the present invention may be selected from Sodium Acetate, acetic acid glacial, hydrochloric acid, sodium citrate, citric acid and combinations thereof. Preferred buffering agents are Sodium Acetate and acetic acid glacial.

Lactase drops according to the present invention used for Infants by oral route of administration.

The present invention also describes process for preparing Lactase drops.

Lactase drops of the present invention may be prepared by preparing buffer solution of pH 4.0 - 5.0, mix polyol to the buffer solution and finally add lactase solution and

mix well to produce clear solution.

The invention is illustrated by the following non limiting examples:

Process:

1. Dissolved 2.1 gram of Sodium acetate and 0.84ml of glacial acetic acid in
sufficient water to produce 230 ml. If necessary adjust the pH to 4.7.

2. Mixed 250 ml of glycerol with 230 ml of the above buffer solution. –

3. Transfered 33 ml of the concentrated lactase solution to the step 2 solution and
mixed well.

4. Filled step 3 solution in 10 ml pre sterilized dropper bottles.

We Claim:

1. Stable lactase drops composition having pH of about 4.0 - 5.0, wherein the composition comprises Lactase, polyol and one or more buffering agents.

2. Stable lactase drops composition of claiml, wherein polyol is selected from lactose, glycerol, sucrose, xylitol, mannitol, sorbitol, maltilol, lactitol and combinations thereof. Preferred polyol is Glycerol.

3. Stable lactase drops composition of claiml, wherein Sodium Acetate, acetic acid glacial, hydrochloric acid, sodium citrate, citric acid and combinations thereof. Preferred buffering agents are Sodium Acetate and acetic acid glacial.

4. Stable lactase drops composition of claiml, can be used for lactose intolerance in infants.