Pharmaceutical acceptable compositions containing an alcohol and a hydrophobic drug

• US 5,843,891 A
• Filed: 10/27/1995
• Issued: 12/01/1998
• Est. Priority Date: 04/28/1993
• Status: Expired due to Fees

• Current Assignee: Bernard C. Sherman
• Original Assignee: Bernard C. Sherman
• Inventors: Sherman, Bernard C.
• Primary Examiner(s): Spivack, Phyllis G.
• Application Number:
  US08/537,697
• Time in Patent Office: 1,131 Days
• Field of Search: 514/11
• US Class Current: 424/456
• CPC Class Codes: A61K 38/13 Cyclosporins
• CPC Class Codes: A61K 47/10 Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
• CPC Class Codes: A61K 47/44 Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin synthetic glycerides, e.g. medium-chain triglycerides, A61K47/14
• CPC Class Codes: A61K 9/0014 Skin, i.e. galenical aspects of topical compositions non-active ingredients are additionally classified in A61K47/00; A61K9/0009, A61K9/0021, A61K9/7015, A61K9/7023 take precedence; cosmetic preparations A61K8/00, A61Q; preparations for wound dressings or bandages A61L26/00
• CPC Class Codes: A61K 9/1075 Microemulsions or submicron emulsions; Preconcentrates or solids thereof; Micelles, e.g. made of phospholipids or block copolymers A61K9/0026 takes precedence
• CPC Class Codes: A61K 9/4858 Organic compounds

Abstract

Pharmaceutical compositions having improved physical and absorption properties are disclosed, wherein a hydrophobic drug is dissolved in a solvent system comprising at least one alcohol having a boiling point above 100° C. and a solubility in water inferior to 10 g per 100 g at 20° C. and a surfactant.

Claims

1. A water-dispersible pharmaceutical composition comprising a monocyclic non-polar peptide dissolved in a solvent system, wherein the solvent system comprises at least one alcohol selected from saturated alkyl mono-alcohols having from 6 to 16 carbon atoms per molecule, a boiling point above 100°

C. and a solubility in water of less than 10 g per 100 g at 20°

C., and said solvent system further comprises at least one pharmaceutically-acceptable surfactant.

2. A composition according to claim 1 wherein said alcohol has from 8 to 14 carbon atoms per molecule.

3. A composition according to claim 1 wherein said solvent system comprises an alcohol selected from 1-octyl, 2-octyl, 1-decyl, and 1dodecyl alcohols.

4. A composition according to claim 1 wherein said monocyclic non-polar peptide is a cyclosporin.

5. A composition according to claim 1 wherein said monocyclic non-polar peptide is cyclosporine.

6. A composition according to claim 5 wherein said solvent system comprises 1-decyl alcohol or 1-dodecyl alcohol.

7. A composition according to claim 1 wherein said solvent system further comprises benzyl or phenethyl alcohol.

8. A composition according to claim 1 wherein said surfactant is a polyoxyethylene glycolated natural or hydrogenated vegetable oil.

9. A composition according to claim 1 wherein said surfactant is a polyoxyethylene glycolated natural or hydrogenated castor oil.

10. A composition according to claim 1 which is dispersed in a carrier.

11. A composition according to claim 10 wherein the carrier is water or contains water.

12. A composition according to claim 1 in a liquid form.

13. A composition according to claim 1 contained within a gelatin capsule.

14. A composition according to claim 1 adapted for oral administration.

15. A composition according to claim 1 adapted for topical or ophthalmic administration.

16. A composition according to claim 1 adapted for parenteral administration.

17. The composition according to claim 1 wherein said composition further comprises a non-saturated alkyl mono-alcohol having at least 6 carbon atoms per molecule wherein the total amount by weight of saturated alkyl mono-alcohols present in said composition is greater than the total amount by weight of said non-saturated alkyl mono-alcohol present in said composition.