This invention comprises pharmaceutical compositions for administering a biologically active compound to an animal. Particularly provided are proliposomal compositions that are advantageously used to deliver biologically active compounds to the gastrointestinal tract after oral administration.
대표청구항▼
1. A pharmacological composition for oral administration comprising a proliposomal preparation of a biologically active compound, which is selected from the group consisting of ibuprofen, erythromycin, vasopressin, insulin, dideoxyinosine. cyclosporin, taxol, heparin, halofantrine, ethopropazine, gr
1. A pharmacological composition for oral administration comprising a proliposomal preparation of a biologically active compound, which is selected from the group consisting of ibuprofen, erythromycin, vasopressin, insulin, dideoxyinosine. cyclosporin, taxol, heparin, halofantrine, ethopropazine, griseofulvin, propofol, furosemide, carbamazepine, diazepam, candesartan and cilexetil in a capsule or tablet comprising an enteric coating, and a protective coating, wherein the protective coating is underneath the enteric coating and in between the proliposomal preparation and the enteric coating, wherein the proliposomal preparation consists of a phospholipid, cholesterol, a biologically active compound, and stearylamine. 2. A pharmacological composition according to claim 1 wherein the enteric coating is cellulose acetate phthalate or a poly(acrylate, methacrylate) copolymer. 3. A pharmacological composition according to claim 1 wherein the protective coating is hydroxypropyl methylcellulose, polyethylene glycol or ethylcellulose. 4. A pharmacological composition according to claim 1 wherein the phospholipid is a phosphatidylcholine. 5. A pharmacological composition according to claim 1 wherein the protective coating further comprises a plasticizer. 6. A pharmacological composition according to claim 5 wherein the plasticizer is triethylcitrate or polyvinyl pyrrolidine. 7. A pharmacological composition according to claim 1 further comprising a particle lubricant that is talc, lactose, corn starch, ethyl cellulose, fatty acids or salts thereof, agar, pectin, gelatin or acacia. 8. A pharmacological composition according to claim 1 wherein the phospholipid is a phosphatidylcholine, or a phosphatidylethanolamine. 9. A pharmacological composition according to claim 8 wherein the phosphatidylcholine is distearylphosphatidylcholine, dimyristylphosphatidylcholine or a mixture thereof. 10. A method for increasing the bioavailability of a biologically active compound, which is selected from the group consisting of ibuprofen, erythromycin, vasopressin, insulin, dideoxyinosine, cyclosporin, taxol, heparin, halofantrine, ethopropazine, griseofulvin, propofol, furosemide, carbamazepine, diazepam, candesartan and cilexetil, said method comprising orally administering to an animal in need thereof a proliposomal preparation of said biologically active compound in a capsule or tablet comprising an enteric coating, and a protective coating wherein the protective coating is underneath the enteric coating and wherein the proliposomal preparation consists of a phospholipid, cholesterol, a biologically active compound, and stearylamine. 11. A method according to claim 10 wherein the animal is a human. 12. A method according to claim 10 wherein the enteric coating is cellulose acetate phthalate or a poly(acrylate, methacrylate) copolymer. 13. A method according to claim 10 wherein the protective coating is hydroxypropyl methylcellulose, polyethylene glycol or ethylcellulose. 14. A method according to claim 10 wherein the phospholipid is a phosphatidylcholine. 15. A method according to claim 10 wherein the protective coating further comprises a plasticizer. 16. A method according to claim 15 wherein the plasticizer is triethylcitrate or polyvinyl pyrrolidine. 17. A method according to claim 10 wherein the phospholipid is a phosphatidylcholine, or a phosphatidylethanolamine. 18. A method according to claim 17 wherein the phospholipid is a phosphatidylcholine, which is distearylphosphatidylcholine, dimyristylphosphatidylcholine or a mixture thereof. 19. A method for delivering a biologically active compound to the intestine or colon, said method comprising orally administering to an animal in need thereof a proliposomal preparation of a biologically active compound which is selected from the group consisting of selected from the group consisting of ibuprofen, erythromycin, vasopressin, insulin, dideoxyinosine, cyclosporin, taxol, heparin, halofantrine, eth opropazine, griseofulvin, propofol, furosemide, carbamazepine, diazepam, candesartan and cilexetil in a tablet comprising an enteric coating, and a protective coating wherein the protective coating is underneath the enteric coating and wherein the proliposomal preparation consists of a phospholipid, cholesterol, a biologically active compound, and stearylamine. 20. A method according to claim 19 wherein the protective coating is hydroxypropyl methylcellulose, polyethylene glycol or ethylcellulose. 21. A method according to claim 19 wherein the phospholipid is a phosphatidylcholine. 22. A method according to claim 19 wherein the protective coating further comprises a plasticizer. 23. A method according to claim 22 wherein the plasticizer is triethylcitrate or polyvinyl pyrrolidine. 24. A method according to claim 19 wherein the proliposomal preparation further comprises a particle lubricant that is talc, lactose, corn starch, ethyl cellulose, fatty acids or salts thereof, agar, pectin, gelatin or acacia. 25. A method according to claim 19 wherein the phospholipid is a phosphatidylcholine, or a phosphatidylethanolamine. 26. A pharmacological composition according to claim 9 wherein the phosphatidylcholine is dimyristylphosphatidylcholine. 27. A method according to claim 18 wherein the phosphatidylcholine is distearylphosphatidylcholine. 28. A method according to claim 25 wherein the phosphatidylcholine is distearylphosphatidylcholine. 29. A method according to claim 25 wherein the phosphatidylcholine is dimyristylphosphatidylcholine.
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