Orally administrable solid pharmaceutical composition and a process thereof
First Claim
1. An orally administrable tablet pharmaceutical composition of IN-105 comprising about 0.01%-20% w/w of IN-105 which is an insulin compound conjugate, about 10%-60% w/w of saturated or unsaturated C4-C12 fatty acids, fatty acid esters or salts thereof, 10%-60% w/w of a diluent, 1%-20% w/w of disintegrant, 0.5% w/w of a lubricant and optionally including binders, plasticizers, permeation enhancers and solubilizers, wherein the lubricant is magnesium stearate.
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Abstract
The invention relates to improvised pharmaceutical compositions permitting ingestion via oral delivery of proteins/peptides or their conjugates, and/or cation-insulin conjugate complexes demonstrating desirable pharmacokinetic profiles and potency in efficacy models of diabetes in dogs and humans. A preferred formulation comprises 0.01%-20% w/w of insulin, insulin compound conjugates and/or cation insulin conjugates, 10%-60% w/w of one or more fatty acid components selected from saturated or unsaturated C4-C12 fatty acids and/or salts of such fatty acids and additionally contains optimal amounts of other pharmaceutically suitable polymer excipients which permit improved solubility, dissolution rate and effective bioavailability of poorly water soluble compositions and consistent in-vivo release profiles upon scalability during manufacture. A further aspect of the invention features the process of preparing the aforesaid formulations.
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Citations
29 Claims
- 1. An orally administrable tablet pharmaceutical composition of IN-105 comprising about 0.01%-20% w/w of IN-105 which is an insulin compound conjugate, about 10%-60% w/w of saturated or unsaturated C4-C12 fatty acids, fatty acid esters or salts thereof, 10%-60% w/w of a diluent, 1%-20% w/w of disintegrant, 0.5% w/w of a lubricant and optionally including binders, plasticizers, permeation enhancers and solubilizers, wherein the lubricant is magnesium stearate.
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8. A process for manufacturing an orally administrable solid pharmaceutical composition of IN 105, comprising about 0.01%-20% w/w of IN-105, about 10%-60% w/w of saturated or unsaturated C4-C12 fatty acids, fatty acid esters or salts thereof, 10%-60% w/w of a diluent, 1%-20% w/w of disintegrant, 0.5% w/w of a lubricant and optionally including binders, plasticizers, permeation enhancers and solubilizers, wherein the lubricant is magnesium stearate, the method comprising the steps of:
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a. grinding a suitable saturated or unsaturated C4-C12 fatty acids and/or salts of such fatty acid; b. granulating the resulting fatty acid obtained from step (a) with an organic solvent; c. air-drying the granules obtained from step (b); d. rasping the dried granules through a mesh to obtain granules of desired particle size; e. blending the fatty acid granules with the cation-insulin conjugate complex with the other excipients; and f. compressing the blended mixture for tablet formation. - View Dependent Claims (10)
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9. A process for manufacturing an orally administrable tablet pharmaceutical composition of IN105, comprising about 0.01%-20% w/w of IN-105, about 10%-60% w/w of saturated or unsaturated C4-C12 fatty acids, fatty acid esters or salts thereof, 0.01%-5% of binder, 10%-60% w/w of a diluent, 1%-20% w/w of disintegrant, 0.5% w/w of a lubricant and optionally including binders, plasticizers, permeation enhancers and solubilizers, wherein the lubricant is magnesium stearate, the method comprising the steps of:
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a. grinding suitable saturated or unsaturated C4-C12 fatty acids and/or salts of such fatty acid and a binder; b. suspending the cation-insulin conjugate complex in an organic solvent using the binder to form a wet mass; c. granulation of the components obtained from step (b) using the binder to form dried granules; d. rasping the dried granules of step (c); e. blending the dried granules with other excipients; and f. compressing the blended mixture for tablet formation.
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Specification
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- Resources
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Current AssigneeBiocon Limited (Biocon Incorporated)
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Original AssigneeBiocon Limited (Biocon Incorporated)
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InventorsKhedkar, Anand, Subramani, Ramesh, Dave, Nitesh, Radhakrishnan, Devesh, Shankar, Sundaresh, Chivukula, Sudheer, Ramakrishna, Ranjith, Pai, Harish Venkatraman, Sengupta, Nilanjan, Melarkode, Ramakrishnan, Iyer, Harish, Rangappa, Sharath Kumar Mallapura, Murthy, Shanmugam Thandava
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Primary Examiner(s)TRAN, SUSAN T
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Application NumberUS12/682,825Publication NumberTime in Patent Office2,658 DaysField of SearchNoneUS Class Current1/1CPC Class CodesA61K 38/28 InsulinsA61K 47/542 Carboxylic acids, e.g. a fa...A61K 47/543 Lipids, e.g. triglycerides;...A61K 9/1617 Organic compounds, e.g. pho...A61K 9/2013 Organic compounds, e.g. pho...A61K 9/2018 Sugars, or sugar alcohols, ...A61K 9/2054 Cellulose; Cellulose deriva...A61K 9/2077 Tablets comprising drug-con...A61P 3/10 for hyperglycaemia, e.g. an...
