Compositions of digestive enzymes and salts of bile acids and process for preparation thereof
First Claim
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1. A process for preparing a digestive enzyme and bile salt composition for the treatment of digestive enzyme and bile salt deficiencies in mammals comprising the steps of:
- a) blending in dry, powdery form (i) about 71 to about 90% w/w of an enzyme selected from the group consisting of pancreatic proteases, lipases, nucleases and amylases;
(ii) about 1.0 to about 61% w/w of a salt of ursodeoxycholic acid selected from the group consisting of sodium, potassium, ammonium, tromethamine, ethanolamine, diethanolamine and triethanolamine;
(iii) about 0.8 to about 5.0% w/w of a buffering agent consisting of anhydrous sodium carbonate, sodium bicarbonate, potassium carbonate or potassium bicarbonate in combination with about 0.8 to about 1.5% w/w of tromethamine, diethanolamine or triethanolamine;
(iv) about 0.3 to about 19% w/w of an adhesive polymer selected from the group consisting of hydroxypropyl cellulose, polyvinylpyrrolidone, cellulose acetate, phthalate and methyl cellulose;
(v) about 0.9 to about 16% w/w of a disintegrant selected from the group consisting of starch, modified starches, microcrystalline cellulose and propylene glycol alginate;
b) wetting said blended ingredients with a liquid to cause the blend to stick together, wherein said liquid is selected from the group consisting of (i) 1-25% w/w ethanol, 75-99% w/w 2-propanol, and 0.2-2% w/w water, (ii) 98-99% w/w 2-propanol and 0.2-2% w/w water, and (iii) 1-25% w/w methanol, 0.2-2% w/w water, 75-98% w/w 2-propanol and 1-5% w/w ethylacetate;
c) granulating or extruding the blend through a 10 or 18 mesh S/S screen;
d) converting the granules to a uniform diameter particle size;
e) compacting the uniform particles into spherical particles;
f) drying the spherical particles;
g) coating the particles with a gastric acid-resistant polymer that disintegrates under neutral or basic conditions; and
h) drying the polymer-coated spherical particles.
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Abstract
Disclosed are gastric acid-resistant polymer-coated digestive enzymes/ursodeoxycholate compositions, process for their preparations and methods of treating digestive disorders, impaired liver function, cystic fibrosis, regulating the absorption of dietary cholesterol, and for dissolving gallstones by administering the compositions to a mammal in need of such treatment.
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Citations
10 Claims
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1. A process for preparing a digestive enzyme and bile salt composition for the treatment of digestive enzyme and bile salt deficiencies in mammals comprising the steps of:
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a) blending in dry, powdery form (i) about 71 to about 90% w/w of an enzyme selected from the group consisting of pancreatic proteases, lipases, nucleases and amylases;
(ii) about 1.0 to about 61% w/w of a salt of ursodeoxycholic acid selected from the group consisting of sodium, potassium, ammonium, tromethamine, ethanolamine, diethanolamine and triethanolamine;
(iii) about 0.8 to about 5.0% w/w of a buffering agent consisting of anhydrous sodium carbonate, sodium bicarbonate, potassium carbonate or potassium bicarbonate in combination with about 0.8 to about 1.5% w/w of tromethamine, diethanolamine or triethanolamine;
(iv) about 0.3 to about 19% w/w of an adhesive polymer selected from the group consisting of hydroxypropyl cellulose, polyvinylpyrrolidone, cellulose acetate, phthalate and methyl cellulose;
(v) about 0.9 to about 16% w/w of a disintegrant selected from the group consisting of starch, modified starches, microcrystalline cellulose and propylene glycol alginate;b) wetting said blended ingredients with a liquid to cause the blend to stick together, wherein said liquid is selected from the group consisting of (i) 1-25% w/w ethanol, 75-99% w/w 2-propanol, and 0.2-2% w/w water, (ii) 98-99% w/w 2-propanol and 0.2-2% w/w water, and (iii) 1-25% w/w methanol, 0.2-2% w/w water, 75-98% w/w 2-propanol and 1-5% w/w ethylacetate; c) granulating or extruding the blend through a 10 or 18 mesh S/S screen; d) converting the granules to a uniform diameter particle size; e) compacting the uniform particles into spherical particles; f) drying the spherical particles; g) coating the particles with a gastric acid-resistant polymer that disintegrates under neutral or basic conditions; and h) drying the polymer-coated spherical particles. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10)
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Specification