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US 2016/0095906 A1Published application
Controlled release pharmaceutical compositions for acid-labile drugs
AssigneeAbbott Products GmbH
InventorsGeorge Shlieout, Claus-Juergen Koelln, Frithjof Sczesny, Jens Onken, Andreas Koerner
Life of this patent
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Abstract
An enteric-coated oral dosage form comprising an acid labile active pharmaceutical ingredient where the composition is substantially free of monomeric phthalic acid esters and synthetic oils is described herein. Also provided are methods for making and using the enteric-coated oral dosage form. The disclosed pharmaceutical compositions comprise an enteric coating which includes at least one plasticizer, at least one film-forming agent and optionally at least one anti-sticking agent.
Claims28
A process for the manufacture of pancreatin micropellets, comprising the steps of:
- a. providing pancreatin micropellet cores wherein the pancreatin micropellet cores are substantially free of synthetic oils;
- b. providing an enteric coating solution comprising
- i. one or more film forming agents;
- ii. a plasticizer in an amount greater than about 1.5% by weight relative to the one or more film-forming agents wherein the plasticizer is substantially free of monomeric phthalic acid esters;
- and
- iii. optionally, at least one anti-sticking agent, and
- iv. one or more enzyme-friendly organic solvent(s);
- c. coating the pancreatin micropellet cores with the enteric-coating solution wherein the temperature of the pancreatin micropellet cores during coating is kept at a temperature suitable to applying the enteric-coating solution;
- and
- d. drying the coated pancreatin micropellet cores.
7 more elements
-12. (canceled)
(canceled)
A pharmaceutical composition, prepared by a process comprising the steps of:
- a. preparing an extrudable mixture comprising:
- i. about 10% to about 95% pancreatin;
- ii. about 5% to about 90% of at least one pharmaceutically acceptable binding agent;
- iii. 0% to about 10% of at least one pharmaceutically acceptable excipient;
- and
- iv. one or more enzyme-friendly organic solvents in an amount sufficient to form an extrudable mixture;
- wherein the percentages of components are weight to weight of the extrudable mixture;
- b. creating pancreatin micropellet cores from the extrudable mixture;
- c. forming the pancreatin micropellet cores into approximately spherical or approximately ellipsoidal shape in the presence of additional enzyme-friendly organic solvent;
- d. removing the one or more enzyme-friendly organic solvents from the pancreatin micropellet cores such that the pancreatin micropellet cores are substantially free of the one or more enzyme-friendly organic solvents;
- wherein the pancreatin micropellet cores are substantially free of synthetic oils;
- e. coating the pancreatin micropellet cores with an enteric-coating solution wherein the temperature of the pancreatin micropellet cores during coating is kept at a temperature suitable to apply the enteric-coating solution and wherein the enteric-coating solution is substantially free of monomeric phthalic acid esters;
- f. drying the coated pancreatin micropellet cores;
- and
- g. placing the coated pancreatin micropellet cores in a dosage form suitable for oral administration.
12 more elements
A pharmaceutical composition, prepared by a process comprising the steps of:
- a. providing pancreatin micropellet cores wherein the pancreatin micropellet cores are substantially free of synthetic oils;
- b. providing an enteric-coating solution comprising
- i. at least one film-forming agent
- ii. a plasticizer in an amount of greater than about 1.5% by weight relative to the one or more film-forming agents film-forming agents wherein the plasticizer is substantially free of monomeric phthalic acid esters;
- and
- iii. optionally at least one anti-sticking agent in one or more enzyme-friendly organic solvent;
- c. coating the pancreatin micropellet cores with the enteric-coating solution wherein the temperature of the pancreatin micropellet cores during coating is kept at a temperature suitable to apply the enteric-coating solution;
- and
- d. drying the coated pancreatin micropellet cores;
- and
- e. placing the coated pancreatin micropellet cores in a dosage form suitable for oral administration.
8 more elements
-43. (canceled)
A pharmaceutical composition, prepared by a process comprising the steps of:
- a. preparing an extrudable mixture comprising:
- i. about 10% to about 95% of an acid labile active pharmaceutical ingredient;
- ii. about 5% to about 90% of at least one pharmaceutically acceptable binding agent;
- iii. 0% to about 10% of at least one pharmaceutically acceptable excipient;
- and
- iv. one or more enzyme-friendly organic solvents in an amount sufficient to form an extrudable mixture;
- wherein the percentages of components are weight to weight of the extrudable mixture;
- b. creating micropellet cores from the extrudable mixture;
- c. forming the micropellet cores into approximately spherical or approximately ellipsoidal shape in the presence of additional enzyme-friendly organic solvent;
- d. removing the one or more enzyme-friendly organic solvents from the micropellet cores such that the micropellet cores are substantially free of the one or more enzyme-friendly organic solvents;
- wherein the micropellet cores are substantially free of synthetic oils;
- e. coating the micropellet cores with an enteric-coating solution wherein the temperature of the micropellet cores during coating is kept at a temperature suitable to apply the enteric-coating solution and wherein the enteric-coating solution is substantially free of monomeric phthalic acid esters;
- f. drying the coated micropellet cores;
- and
- g. placing the coated micropellet cores in a dosage form suitable for oral administration.
12 more elements
-46. (canceled)
Dependencies are inferred from the claim text.