DESC:FORM 2

THE PATENTS ACT 1970
(SECTION 39 OF 1970)

&
THE PATENT RULES, 2003

COMPLETE SPECIFICATION
(SECTION 10)

FERROUS SULPHATE ORAL COMPOSITIONS

We, NOKHA TRADING LLP,
a company incorporated under the companies act, 1956 having
address at No 22, 7th Cross, Jaibharathnagar, Bangalore,
Karnataka-560033, India.

The following specification particularly describes the invention and the manner in which it is to be performed:

FIELD OF INVENTION
The present invention relates to iron salt oral compositions.

The present invention specifically relates to iron salt granules and buccal tablets compositions.

The present invention specifically relates to compositions of granules and buccal tablets comprising ferrous sulphate as active ingredient, penetration/absorption enhancers and pharmaceutically acceptable excipients.

The present invention relates to composition of granules and buccal tablets comprising ferrous sulphate hydrate as active ingredient, anti-oxidant, mouth melting agent, taste masking agents as penetration/absorption enhancers, reducing agent, binding agent, sweetening agent, disintegrant, flavouring agent and lubricants as pharmaceutically acceptable excipients for preventing anemia.

The present invention more specifically relates to process for the preparation of ferrous sulphate granules using wet granulation technique comprising the steps of sifting, granulating, drying and filling into sachets.

The present invention more specifically relates to process for the preparation of ferrous sulphate buccal tablets using wet granulation technique comprising the steps of sifting, granulating, drying and compressing.

BACKGROUND OF THE INVENTION
Iron deficiency anemia arises when the balance of iron intake, iron storage are insufficient to fully support production of erythrocytes. Iron deficiency anemia rarely causes death, but the impact on human health is significant.

Iron in a variety of forms is administered for the treatment of iron deficiency and related disorders (e.g., anemia) as well as prophylactically to supply the minimum daily recommended allowance. A variety of iron compounds have been administered, including ferric and ferrous forms of elemental iron as salts, complexes, hydrates, chelates, and bound to polymer.

Iron is administered either parenterally or orally. Iron is administered orally via various iron preparations, including solutions, tablets or enteric coated preparations. The most common forms of oral iron preparations are ferrous sulfate and ferrous gluconate. Ferrous sulfate is less expensive and has more elemental iron in it.

Iron(II) sulfate (British English: iron(II) sulphate) or ferrous sulfate denotes a range of salts with the formula FeSO4•xH2O. These compounds exist most commonly as the heptahydrate (x = 7) but are known for several values of x. The hydrated form is used medically to treat iron deficiency.

Ferrous sulphate is available in the market as tablets, capsules, drops, liquid and syrups.

Oral iron preparations have many disadvantages. First and foremost, they cause gastrointestinal side effects including nausea, bloating, constipation, and diarrhoea. This leads to discontinuation of iron supplementation in approximately 40-66% of the patients taking such supplements. Furthermore, the absorption of iron is variable and affected by the oral ingestion of other compounds. For example, oral ingestion of food products reduces iron absorption by approximately 50%, which is problematic since many patients take iron with food in order to reduce the gastrointestinal side effects.

Secondly, many drugs are known to reduce iron absorption. For example, oral ingestion of antacids and other drugs that reduce stomach pH is known to decrease iron absorption. In turn, oral ingestion of iron also reduces the absorption of many drugs, including antibiotics.

In addition, many conditions associated with iron deficiency anemia respond poorly to oral iron supplementation, because iron cannot be properly absorbed through the cells of the gastrointestinal system. This is especially true of certain inflammatory conditions of the bowel, such as Crohn's disease. Additionally, diseases associated with functional iron deficiency, such as the anemia of renal failure are also associated with limited absorption of orally administered iron.

WO 2015/004519 discloses divalent iron compound for use in hyposideremia therapy by administration through intrabuccal absorption in a patient, wherein said administration occurs with indication to the patient to avoid swallowing the formulation containing the divalent iron compound and/or saliva for a period of time of at least 30 seconds after placement of the formulation containing the divalent iron compound in the intrabuccal cavity, said use providing for the administration of divalent iron at doses comprised in an interval from 1 to 90 mg of divalent Fe per day for a human patient to reduce, for an equal increment in transferrin saturation, the onset of free non transferrin bound iron with respect to gastrointestinal administration. It also discloses ferrous sulfate as divalent iron compound.

All the prior art references shows the disadvantages of using oral preparations of Iron. The inventors of the present invention have developed compositions of ferrous sulphate granules and buccal tablets with increased bio absorption for preventing anemia which is devoid of the disadvantages of prior-art. The inventors of the present invention provide process for the preparation of ferrous sulphate granules using wet granulation technique comprising the steps of sifting, granulating, drying and filling into sachets. The inventors of the present invention also provide process for the preparation of ferrous sulphate buccal tablets using wet granulation technique comprising the steps of sifting, granulating, drying and compressing.
OBJECTIVE OF THE INVENTION
The main objective of the present invention is to provide iron salt oral compositions.

Another objective of the present invention is to provide iron salt granules and buccal tablets.

Another objective of the present invention is to provide composition of ferrous sulphate granules, buccal tablets and methods for preparation thereof.

Another objective of the present invention is to provide granules and buccal tablets compositions comprising ferrous sulphate hydrate as active ingredient, penetration/absorption enhancers and pharmaceutically acceptable excipients.

Another objective of the present invention is to provide granules and buccal tablet compositions comprising ferrous sulphate hydrate as active ingredient, anti-oxidant, mouth melting agent, taste masking agents as penetration/absorption enhancers, reducing agent, binding agent, sweetening agent, disintegrant, flavouring agent and lubricants as pharmaceutically acceptable excipients for preventing anemia.

Still another objective of the present invention is to provide process for the preparation of ferrous sulphate granules using wet granulation technique comprising the steps of sifting, granulating, drying and filling into sachets.

Still another objective of the present invention is to provide process for the preparation of ferrous sulphate buccal tablets using wet granulation technique comprising the steps of sifting, granulating, drying and compressing.

SUMMARY OF THE INVENTION
Accordingly, the present invention provides compositions of iron salt oral compositions.

Another embodiment of the present invention relates to iron salt granules and buccal tablets for preventing anemia.

Another embodiment of the present invention relates to iron salt granules and buccal tablets comprising ferrous sulphate as active ingredient, penetration/absorption enhancers and pharmaceutically acceptable excipients.

Another embodiment of the present invention relates to granules and buccal tablets comprising ferrous sulphate hydrate as active ingredient, anti-oxidant, mouth melting agent, taste masking agents as penetration/absorption enhancers, reducing agent, binding agent, sweetening agent, disintegrant, flavouring agent and lubricants as pharmaceutically acceptable excipients for preventing anemia.

Another embodiment of the present invention relates to granules and buccal tablets comprising ferrous sulphate hydrate as active ingredient and ascorbic acid as anti-oxidant, mannitol as mouth melting agent, sodium chloride, citric acid and whey protein as taste masking agents, fructose as reducing agents, PVP-K30 as binding agent, sucralose or stevia as sweetening agents, crospovidone as disintegrant, lemon flavour as flavouring agent, aerosil and purified talc as lubricants.

Another embodiment of the present invention relates to provide process for the preparation of ferrous sulphate granules using wet granulation technique comprising the steps of sifting, granulating, drying and filling into sachets.

Another embodiment of the present invention relates to provide process for the preparation of ferrous sulphate buccal tablets comprising the steps of sifting, granulating, drying and compressing.

In another embodiment, the present invention provides compositions of granules and buccal tablets comprising:
5% to 25% (w/w) of active ingredient,
5% to 25% (w/w) of antioxidant,
1% to 20% (w/w) of reducing agent,
0.5% to 20% (w/w) of taste masking agents,
1% to 5% (w/w) of sweetening agents,
10% to 90% (w/w) of mouth melting agents,
1% to 15% (w/w) of disintegrants,
1% to 10% (w/w) of binding agents,
1% to 10% (w/w) of flavouring agent, and
1% to 5% (w/w) of lubricants.

In yet another embodiment, the present invention provides process for preparing granules and buccal tablets, wherein the process comprising steps of:
(a) sifting active ingredient, anti-oxidant through #80 mesh and reducing agent, mouth melting agent, binding agent through #40 mesh and blending for 5 minutes,
(b) wet granulating obtained blend with water and drying at 45ºC for 10 min,
passing obtained dried granules through #40 mesh,
(c) sifting taste masking agents, sweetening agent, disintegrant through #40 mesh and taste masking agent through #80 mesh,
(d) adding above sifting ingredients to obtained dried granules of step (b),
(e) sifting flavouring agent through #100 mesh, lubricant through #60 mesh and adding to obtained blend of step (d) followed by mixing for 10 minutes,
(f) sifting lubricant through #60 mesh, adding to obtained blend of step (e) and mixing for 5 minutes, and
(g) obtained blend of granules are filled into sachets or compressed into buccal tablets using compression machine.

In yet another embodiment, the present invention provides process for preparing ferrous sulphate granules and buccal tablets, wherein the process comprising steps of:
(a) sifting ferrous sulphate, ascorbic acid through #80 mesh and fructose, mannitol, PVP-K-30 through #40 mesh and blending for 5 minutes,
(b) wet granulating obtained blend with water and drying at 45ºC for 10 min,
passing obtained dried granules through #40 mesh,
(c) sifting whey protein, citric acid, sucralose or stevia and crospovidone through #40 mesh and sodium chloride through #80 mesh,
(d) adding above sifting ingredients to obtained dried granules of step (b),
(e) sifting lemon flavour through #100 mesh, aerosil through #60 mesh and adding to obtained blend of step (d) followed by mixing for 10 minutes,
(f) sifting purified talc through #60 mesh, adding to obtained blend of step (e) and mixing for 5 minutes, and
(g) obtained blend of granules are filled into sachets or compressed into buccal tablets using compression machine.

DETAILED DESCRIPTION OF THE INVENTION
The term "comprising", which is synonymous with "including", "containing", or "characterized by" here is defined as being inclusive or open-ended, and does not exclude additional, unrecited elements or method steps, unless the context clearly requires otherwise.

Anaemia is a condition in which the number of red blood cells or their oxygen-carrying capacity is insufficient to meet physiologic needs, which vary by age, sex, altitude, smoking, and pregnancy status. Iron deficiency is thought to be the most common cause of anaemia globally, although other conditions, such as folate, vitamin B12 and vitamin A deficiencies, chronic inflammation, parasitic infections, and inherited disorders can all cause anaemia. In its severe form, it is associated with fatigue, weakness, dizziness and drowsiness. Pregnant women and children are particularly vulnerable.

The present invention is to provide granules and buccal tablets compositions comprising ferrous sulphate hydrate as active ingredient, penetration/absorption enhancers and pharmaceutically acceptable excipients and its process of preparation.

The present invention is to provide granules and buccal tablets compositions comprising ferrous sulphate hydrate as active ingredient, anti-oxidant, mouth melting agent, taste masking agents as penetration/absorption enhancers, reducing agent, binding agent, sweetening agent, disintegrant, flavouring agent and lubricants as pharmaceutically acceptable excipients.

The term “active ingredient” of the present invention is used to prevent anemia. The active ingredient is Iron compound or pharmaceutically acceptable salts, esters, solvates, derivatives, polymorphs or hydrates thereof. Preferably used iron salts include, but are not limited to ferrous sulfate, ferrous citrate, ferrous ascorbate, ferrous fumarate, ferrous glycinate, ferrous gluconate. Preferably used active ingredient is ferrous sulphate hydrate. Most preferably used active ingredient is ferrous sulphate heptahydrate.

The terms “prevent,” “preventing,” and “prevention” (and grammatical variations thereof) refer to avoidance, prevention and/or delay of the onset of a disease, disorder and/or a clinical symptom(s) in a subject and/or a reduction in the severity of the onset of the disease, disorder and/or clinical symptom(s) relative to what would occur in the absence of the methods of the invention. The prevention can be complete, e.g., the total absence of the disease, disorder and/or clinical symptom(s). The prevention can also be partial, such that the occurrence of the disease, disorder and/or clinical symptom(s) in the subject and/or the severity of onset is less than what would occur in the absence of the present invention.

The term “iron deficiency,” as used herein, refers to any disease or disorder in which whole body stores of iron are less than desired. Low body stores may be indicated by various symptoms including a blood level of iron that is below normal, low ferritin levels, and/or low haemoglobin levels. Exemplary low levels may be a cause and/or symptom of the disease or disorder and includes any disease or disorder in which elevating iron levels in the subject, e.g., in the blood, treats and/or prevents one or more symptoms of the disease or disorder, or where maintenance of iron indices is required for effectiveness of another agent, e.g., erythropoiesis-stimulating agents. The normal serum iron level for human adults is considered to be about 50 to about 170 µg/dL.

Ferrous sulphate occurs in different forms such as anhydrous, monohydrate, tetrahydrate and heptahydrate. The most common naturally occurring form is heptahydrate with a chemical formula of FeSO4.7H2O. It is pale, bluish or whitish green, odourless crystals, crystalline powder or granules. Effloresces in dry air. In moist air it oxidizes readily to form brownish yellow basic ferric sulphate. It is functionally used as nutrient supplement.

The concentration of Ferrous sulphate hydrate used in the iron salt compositions for buccal administration with increased bio absorption is in the range of 5% to 25% (w/w), preferably 5% to 15% (w/w) of the total weight of the composition.

Anti-oxidant used alone or in combination in the compositions of the present invention include, but are not limited to vitamin C, vitamin E, vitamin A, flavonoids, polyphenols, tocopherol, deteroxime mesylate, methyl paraben, ethyl paraben, ascorbic acid. Preferably used anti-oxidant is ascorbic acid.

The concentration of anti-oxidant used in the iron salt compositions for buccal administration with increased bio absorption is in the range of 5% to 25% (w/w), preferably 5% to 15% (w/w) of the total weight of the composition.

Reducing agents used alone or in combination in the compositions of the present invention include, but are not limited saccharides, sugar or sugar alcohol. Saccharides include monosaccharides, disaccharides, trisaccharides, tetrasaccharides, or other higher polysaccharides, such as cellulose and starch. Suitable monosaccharides include glucose, galactose, fructose, mannose, mannitol and sorbitol. The disaccharides include maltose, lactose and sucrose. Preferably used reducing agent is fructose.

The concentration of reducing agent used in the iron salt compositions for buccal administration with increased bio absorption is in the range of 1% to 20% (w/w), preferably 1% to 10% (w/w) of the total weight of the composition.

Binding agents used alone or in combination in the compositions of the present invention include, but are not limited to carboxy vinyl polymer, methylcellulose, hydroxyethylcellulose, hydroxypropyl cellulose, gum arabic, starch, hydroxypropylmethylcellulose, polyvinylpyrrolidone, polyethylene glycol. Preferably used binder is polyvinylpyrrolidone K 30.

The concentration of binding agent used in the iron salt compositions for buccal administration with increased bio absorption is in the range of 1% to 10% (w/w), preferably 1% to 5% (w/w) of the total weight of the composition.

Lubricants used alone or in combination in the compositions of the present invention include, but are not limited to magnesium stearate, stearic acid, sodium stearyl fumarate, microcrystalline cellulose, crosslinked sodium carboxymethylcellulose, silica, aerosil, corn starch, sucrose fatty acid esters, polyethylene glycol, talc, stearic acid, calcium stearate. Preferably used lubricants are aerosil and purified talc.

The concentration of lubricants used in the iron salt compositions for buccal administration with increased bio absorption is in the range of 1% to 5%. Preferably used concentration of lubricant individually is from 1% to 3% (w/w). The concentration of lubricant used in combination in the iron salt compositions for buccal administration of the present invention is from 1% to 10%.

Mouth melting agent used alone or in combination in the compositions of the present invention include, but are not limited to sugar alcohols such as sorbitol, sorbitol syrup, mannitol, xylitol, hexa-resorcinol. Preferably used mouth melting agent is mannitol.

The concentration of mouth melting agent used in the iron salt compositions for buccal administration with increased bio absorption is in the range of 10% to 90% (w/w), preferably 20% to 30% (w/w) of the total weight of the composition.

Disintegrants used alone or in combination in the compositions of the present invention include, but are not limited to starches such as corn starch, etc., carmellose calcium, crospovidone, lower substituted hydroxypropyl cellulose, alginic acid, sodium carboxymethyl starches, methylcellulose, agar bentonite, sodium starch glycolate, microcrystalline cellulose, colloidal silicon dioxide, guar gum, magnesium aluminum silicate, polacrilin potassium, powdered cellulose, pregelatinized starch, sodium alginate. Preferably used disintegrant is crospovidone.

The concentration of disintegrant used in the iron salt compositions for buccal administration with increased bio absorption is in the range of 1% to 15% (w/w), preferably 5% to 15% (w/w) of the total weight of the composition.

Taste masking agents used alone or in combination in the compositions of the present invention include, but are not limited to osmolality adjusting ingredient, flavouring agent and film-forming agents. Osmolality adjusting ingredient is selected from potassium chloride, calcium chloride, sodium lactate, sodium chloride, dextrose, mannitol, sucrose, trehalose, and phosphate buffered saline, or mixtures thereof. Flavouring agent is selected from vanillin, ethyl vanillin, menthol, citric acid, fumaric acid ethyl maltitol, and tartaric acid. Film-forming agent is selected from pullulan, hydroxypropylmethyl cellulose, hydroxyethyl cellulose, hydroxypropyl cellulose, polyvinyl pyrrolidone, carboxymethyl cellulose, polyvinyl alcohol, sodium alginate, polyethylene glycol, xanthan gum, tragacanth gum, guar gum, acacia gum, arabic gum, polyacrylic acid, methylmethacrylate copolymer, carboxyvinyl polymer, amylose, high amylose starch, hydroxypropylated high amylose starch, dextrin, pectin, chitin, chitosan, levan, elsinan, collagen, gelatin, zein, gluten, soy protein isolate, whey protein isolate, casein and mixtures thereof. Preferably used taste masking agents are sodium chloride, citric acid and whey protein.

The concentration of taste masking agents used in the iron salt compositions for buccal administration with increased bio absorption is in the range of 0.5% to 20% (w/w). Preferably used concentration of taste masking agent individually is from 2% to 20% (w/w). The concentration of taste masking agent used in combination in the iron salt compositions for buccal administration of the present invention is from 20% to 35% (w/w).

Sweetening agents used alone or in combination in the compositions of the present invention include, but are not limited to saccharin, saccharin sodium, aspartame, maltitol, zinc gluconate, ethyl maltitol, glycine, acesulfame-K, honey, golden syrup, misri, spray dried licorice root, glycerrhizin, dextrose, sodium gluconate, stevia powder; glucono delta-lactone, ethyl vanillin, vanillin, sucrose, glucose (corn syrup), dextrose, invert sugar, fructose, sucralose, stevia, dihydrochalcone, maltodextrin, polydextrose, sugar alcohols such as sorbitol, sorbitol syrup, mannitol, xylitol, hexa-resorcinol. Preferably used sweetening agent is sucralose or stevia.

The concentration of sweetening agent used in the iron salt compositions for buccal administration with increased bio absorption is in the range of 1% to 5% (w/w), preferably 1% to 3% (w/w) of the total weight of the composition.

Flavouring agents used alone or in combination in the compositions of the present invention include, but are not limited to coffee extract, mint, lamiacea extracts, lemon flavour, almond oil, babassu oil, borage oil, blackcurrant seed oil, canola oil, castor oil, coconut oil, corn oil, cottonseed oil, evening primrose oil, grape seed oil, groundnut oil, mustard seed oil, olive oil, palm oil, palm kernel oil, peanut oil, grape seed oil, safflower oil, sesame oil, shark liver oil, soybean oil, sunflower oil; hydrogenated castor oil, hydrogenated coconut oil, hydrogenated palm oil, hydrogenated soybean oil, hydrogenated vegetable oil, hydrogenated cottonseed and castor oil, partially hydrogenated soybean oil, soy oil, glyceryl tricaproate, glyceryl tricaprylate, glyceryl tricaprate, glyceryl triundecanoate, glyceryl trilaurate, glyceryl trioleate, glyceryl trilinoleate, glyceryl trilinolenate, glyceryl tricaprylate/caprate, glyceryl tricaprylate/caprate/laurate, glyceryl tricaprylate/caprate/linoleate, glyceryl tricaprylate/caprate/stearate, saturated polyglycolized glycerides, linoleic glycerides, caprylic/capric glycerides, modified triglycerides, fractionated triglycerides, safrole, citric acid, d-limonene, malic acid and phosphoric acid or salts and/or mixtures thereof. Preferably used flavouring agent is lemon flavour.

The concentration of falvouring agent used in the iron salt compositions for buccal administration with increased bio absorption is in the range of 1% to 10% (w/w), preferably 3% to 8% (w/w) of the total weight of the composition.

The ferrous sulphate granules preparation of present invention has been prepared by using wet granulation technique comprising the steps of sifting, granulating, drying and filling into sachets.

The ferrous sulphate hydrate buccal tablet of present invention is orally soluble with increased bioavailability. It is devoid of metallic/iron taste and easy patient compliance.

The ferrous sulphate hydrate buccal tablets preparation of present invention has been prepared by using wet granulation technique comprising the steps of sifting, granulating, drying and compressing.

The invention disclosed herein is process for the preparation of ferrous sulphate granules and buccal tablets useful in preventing anemia.

The present invention is illustrated in detail but not limiting to, the following examples. It will be apparent to those skilled in the art that many modifications, both to materials and methods, may be practiced without departing from the scope of the invention.
EXAMPLES
Example 1:
S.No Ingredients Quantity (mg/tablet)
1. Ferrous Sulphate.7 H2O 10.00
2. Ascorbic Acid 10.4
3. Fructose 5.0
4. Sodium Chloride 5.0
5. Sucralose 1.0
6. Citric Acid 2.0
7. Mannitol 25.6
8. PVP-K30 3.0
9. Crospovidone 10.0
10. Lemon Flavor 5.0
11. Aerosil 2.0
12. Purified Talc 1.0
13. Whey Protein 20.0
14. Water QS
Total weight of tablet 100

Manufacturing process
Ferrous sulphate and ascorbic acid were co-sifted through #80 mesh. Fructose, mannitol and PVP K30 were co-sifted through #40 mesh. All these materials were blended for 5 minutes. Mixed materials were wet granulated with water and dried at 45ºC for 10 minutes. Dried granules were passed through #40 mesh. Whey protein, sucralose, crospovidone and citric acid were co-sifted through #40 mesh and sodium chloride is sifted through #80 mesh. All these materials were added to dried granules. Lemon flavour sifted through #100 mesh and aerosil is sifted through #60 mesh, added and mixed with obtained granules for 10 minutes. Purified talc is sifted through #60 mesh, added and mixed with obtained granules for 5 minutes.

The resulting blend of granules were filled into sachets or compressed into buccal tablets using compression machine with appropriate tooling.

Example 2:
S.No Ingredients Quantity (mg/tablet)
1. Ferrous Sulphate.7 H2O 10.00
2. Ascorbic Acid 10.4
3. Fructose 5.0
4. Sodium Chloride 5.0
5. Stevia 1.0
6. Citric Acid 2.0
7. Mannitol 25.6
8. PVP-K30 3.0
9. Crospovidone 10.0
10. Lemon Flavor 5.0
11. Aerosil 2.0
12. Purified Talc 1.0
13. Whey Protein 20.0
14. Water QS
Total weight of tablet 100

Manufacturing process
Ferrous sulphate and ascorbic acid were co-sifted through #80 mesh. Fructose, mannitol and PVP K30 were co-sifted through #40 mesh. All these materials were blended for 5 minutes. Mixed materials were wet granulated with water and dried at 45ºC for 10 minutes. Dried granules were passed through #40 mesh. Whey protein, stevia, crospovidone and citric acid were co-sifted through #40 mesh and sodium chloride is sifted through #80 mesh. All these materials were added to dried granules. Lemon flavour sifted through #100 mesh and aerosil is sifted through #60 mesh, added and mixed with obtained granules for 10 minutes. Purified talc is sifted through #60 mesh, added and mixed with obtained granules for 5 minutes.

The resulting blend of granules were filled into sachets or compressed into buccal tablets using compression machine with appropriate tooling.

Post-compression evaluation parameters of ferrous sulphate buccal tablets

S.No Average Weight (mg) Thickness (mm) Hardness (N) Disintegration time (sec)
1. 100 3.44 17.32 15
2. 103 3.45 16.03 17
3. 104 3.45 12.63 19
4. 102 3.43 11.04 16
5. 101 3.44 12.43 21

Friability: 0.61% w/w.

,CLAIMS:We Claim:
1. An iron salt compositions for buccal administration with increased bio absorption comprising Ferrous sulphate as active ingredient, anti-oxidant, mouth melting agent, taste masking agents as penetration/absorption enhancers and pharmaceutically acceptable excipients.
2. The iron salt compositions for buccal administration with increased bio absorption as claimed in claim 1, wherein the active ingredient is Ferrous sulphate hydrate.
3. The iron salt compositions for buccal administration with increased bio absorption as claimed in claim 1, wherein the pharmaceutically acceptable excipients used herein are selected from reducing agent, binding agent, sweetening agent, disintegrant, flavouring agent and lubricants.
4. The iron salt compositions for buccal administration with increased bio absorption as claimed in claim 2, wherein the Ferrous sulphate hydrate is in the range of 5% to 25% (w/w), preferably 5% to 15% (w/w) of the total weight of the composition.
5. The iron salt compositions for buccal administration with increased bio absorption as claimed in claim 1, wherein the anti-oxidant is selected from vitamin C, vitamin E, vitamin A, flavonoids, polyphenols, tocopherol, deteroxime mesylate, methyl paraben, ethyl paraben and ascorbic acid.
6. The iron salt compositions for buccal administration with increased bio absorption as claimed in claim 5, wherein the anti-oxidant is in the range of 5% to 25% (w/w), preferably 5% to 15% (w/w) of the total weight of the composition.
7. The iron salt compositions for buccal administration with increased bio absorption as claimed in claim 1, wherein the mouth melting agent is selected from sugar alcohols such as sorbitol, sorbitol syrup, mannitol, xylitol and hexa-resorcinol.
8. The iron salt compositions for buccal administration with increased bio absorption as claimed in claim 7, wherein the mouth melting agent is in the range of 10% to 90% (w/w), preferably 20% to 30% (w/w) of the total weight of the composition.
9. The iron salt compositions for buccal administration with increased bio absorption as claimed in claim 1, wherein the taste masking agents are selected from osmolality adjusting ingredient which includes potassium chloride, calcium chloride, sodium lactate, sodium chloride, dextrose, mannitol, sucrose, trehalose, and phosphate buffered saline, or mixtures thereof, flavouring agent which includes vanillin, ethyl vanillin, menthol, citric acid, fumaric acid ethyl maltitol, tartaric acid and film-forming agents which includes pullulan, hydroxypropylmethyl cellulose, hydroxyethyl cellulose, hydroxypropyl cellulose, polyvinyl pyrrolidone, carboxymethyl cellulose, polyvinyl alcohol, sodium alginate, polyethylene glycol, xanthan gum, tragacanth gum, guar gum, acacia gum, arabic gum, polyacrylic acid, methylmethacrylate copolymer, carboxyvinyl polymer, amylose, high amylose starch, hydroxypropylated high amylose starch, dextrin, pectin, chitin, chitosan, levan, elsinan, collagen, gelatin, zein, gluten, soy protein isolate, whey protein isolate, casein and mixtures thereof .
10. The iron salt compositions for buccal administration with increased bio absorption as claimed in claim 9, wherein the taste masking agents is in the range of 0.5% to 20% (w/w), preferably used concentration of taste masking agents individually is from 2% to 20% (w/w) of the total weight of the composition.
11. The iron salt compositions for buccal administration with increased bio absorption as claimed in claim 9, wherein the combination of taste masking agents are in the range of 20% to 35% (w/w).
12. The iron salt compositions for buccal administration with increased bio absorption as claimed in claim 3, wherein the reducing agent is selected from saccharides, sugar or sugar alcohol, preferably saccharides include monosaccharides like glucose, galactose, fructose, mannose, mannitol and sorbitol, disaccharides like maltose, lactose and sucrose, trisaccharides, tetrasaccharides, or other higher polysaccharides, such as cellulose and starch.
13. The iron salt compositions for buccal administration with increased bio absorption as claimed in claim 12, wherein the reducing agent is in the range of 1% to 20% (w/w), preferably 1% to 10% (w/w) of the total weight of the composition.
14. The iron salt compositions for buccal administration with increased bio absorption as claimed in claim 3, wherein the binding agent is selected from carboxy vinyl polymer, methylcellulose, hydroxyethylcellulose, hydroxypropyl cellulose, gum arabic, starch, hydroxypropylmethylcellulose, polyvinylpyrrolidone and polyethylene glycol.
15. The iron salt compositions for buccal administration with increased bio absorption as claimed in claim 14, wherein the binding agent is in the range of 1% to 10% (w/w), preferably 1% to 5% (w/w) of the total weight of the composition.
16. The iron salt compositions for buccal administration with increased bio absorption as claimed in claim 3, wherein the sweetening agent is selected from saccharin, saccharin sodium, aspartame, maltitol, zinc gluconate, ethyl maltitol, glycine, acesulfame-K, honey, golden syrup, misri, spray dried licorice root, glycerrhizin, dextrose, sodium gluconate, stevia powder; glucono delta-lactone, ethyl vanillin, vanillin, sucrose, glucose (corn syrup), dextrose, invert sugar, fructose, sucralose, stevia, dihydrochalcone, maltodextrin, polydextrose, sugar alcohols such as sorbitol, sorbitol syrup, mannitol, xylitol and hexa-resorcinol.
17. The iron salt compositions for buccal administration with increased bio absorption as claimed in claim 16, wherein the sweetening agent is in the range of 1% to 5% (w/w), preferably 1% to 3% (w/w) of the total weight of the composition.
18. The iron salt compositions for buccal administration with increased bio absorption as claimed in claim 3, wherein the disintegrant is selected from starches such as corn starch, etc., carmellose calcium, crospovidone, lower substituted hydroxypropyl cellulose, alginic acid, sodium carboxymethyl starches, methylcellulose, agar bentonite, sodium starch glycolate, microcrystalline cellulose, colloidal silicon dioxide, guar gum, magnesium aluminum silicate, polacrilin potassium, powdered cellulose, pregelatinized starch and sodium alginate.
19. The iron salt compositions for buccal administration with increased bio absorption as claimed in claim 18, wherein the disintegrant is in the range of 1% to 15% (w/w), preferably 5% to 15% (w/w) of the total weight of the composition.
20. The iron salt compositions for buccal administration with increased bio absorption as claimed in claim 3, wherein the flavouring agent is selected from coffee extract, mint, lamiacea extracts, lemon flavour, almond oil, babassu oil, borage oil, blackcurrant seed oil, canola oil, castor oil, coconut oil, corn oil, cottonseed oil, evening primrose oil, grape seed oil, groundnut oil, mustard seed oil, olive oil, palm oil, palm kernel oil, peanut oil, grape seed oil, safflower oil, sesame oil, shark liver oil, soybean oil, sunflower oil; hydrogenated castor oil, hydrogenated coconut oil, hydrogenated palm oil, hydrogenated soybean oil, hydrogenated vegetable oil, hydrogenated cottonseed and castor oil, partially hydrogenated soybean oil, soy oil, glyceryl tricaproate, glyceryl tricaprylate, glyceryl tricaprate, glyceryl triundecanoate, glyceryl trilaurate, glyceryl trioleate, glyceryl trilinoleate, glyceryl trilinolenate, glyceryl tricaprylate/caprate, glyceryl tricaprylate/caprate/laurate, glyceryl tricaprylate/caprate/linoleate, glyceryl tricaprylate/caprate/stearate, saturated polyglycolized glycerides, linoleic glycerides, caprylic/capric glycerides, modified triglycerides, fractionated triglycerides, safrole, citric acid, d-limonene, malic acid and phosphoric acid or salts and/or mixtures thereof.
21. The iron salt compositions for buccal administration with increased bio absorption as claimed in claim 20, wherein the flavouring agent is in the range of 1% to 10% (w/w), preferably 3% to 8% (w/w) of the total weight of the composition.
22. The iron salt compositions for buccal administration with increased bio absorption as claimed in claim 3, wherein lubricants are selected from magnesium stearate, stearic acid, sodium stearyl fumarate, microcrystalline cellulose, crosslinked sodium carboxymethylcellulose, silica, aerosil, corn starch, sucrose fatty acid esters, polyethylene glycol, talc, stearic acid and calcium stearate.
23. The iron salt compositions for buccal administration with increased bio absorption as claimed in claim 22, wherein the lubricants is in the range of 1% to 5% (w/w), preferably used concentration of lubricant individually is from 1% to 3% (w/w) of the total weight of the composition.
24. The iron salt compositions for buccal administration with increased bio absorption as claimed in claim 22, wherein the combination of lubricants are in the range of 1% to 10% (w/w) of the total weight of the composition.
25. The iron salt compositions for buccal administration with increased bio absorption as claimed in claim 1-24 prepared by a process comprising the steps of:
(a) sifting active ingredient, anti-oxidant through #80 mesh and reducing agent, mouth melting agent, binding agent through #40 mesh and blending for 5 minutes,
(b) wet granulating obtained blend with water and drying at 45ºC for 10 min,
passing obtained dried granules through #40 mesh,
(c) sifting taste masking agents, sweetening agent, disintegrant through #40 mesh and taste masking agent through #80 mesh,
(d) adding above sifting ingredients to obtained dried granules of step (b),
(e) sifting flavouring agent through #100 mesh, lubricant through #60 mesh and adding to obtained blend of step (d) followed by mixing for 10 minutes,
(f) sifting lubricant through #60 mesh, adding to obtained blend of step (e) and mixing for 5 minutes, and
(g) obtained blend of granules are filled into sachets or compressed into buccal tablets using compression machine.
26. The process for preparing iron salt compositions for buccal administration with increased bio absorption claimed in claim 25, wherein the process comprising the steps of:
(a) sifting ferrous sulphate, ascorbic acid through #80 mesh and fructose, mannitol, PVP-K-30 through #40 mesh and blending for 5 minutes,
(b) wet granulating obtained blend with water and drying at 45ºC for 10 min,
passing obtained dried granules through #40 mesh,
(c) sifting whey protein, citric acid, sucralose or stevia and crospovidone through #40 mesh and sodium chloride through #80 mesh,
(d) adding above sifting ingredients to obtained dried granules of step (b),
(e) sifting lemon flavour through #100 mesh, aerosil through #60 mesh and adding to obtained blend of step (d) followed by mixing for 10 minutes,
(f) sifting purified talc through #60 mesh, adding to obtained blend of step (e) and mixing for 5 minutes, and
(g) obtained blend of granules are filled into sachets or compressed into buccal tablets using compression machine.

Dated this Fourteenth (14th) day of May, 2020

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Dr. S. Padmaja
Agent for the Applicant
IN/PA/883