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Summary for Patent: 4,727,064
|Title:||Pharmaceutical preparations containing cyclodextrin derivatives|
|Abstract:||The invention comprises pharmaceutical preparations consisting generally of a drug with a substantially low water solubility and an amorphous, water-soluble cyclodextrin-based mixtures. In these preparations a stable amorphous state can be achieved. This improves the dissolution properties of the drug and hence its absorption by the body. The required cyclodextrin-based mixtures were prepared from .alpha.-, .beta.-, or .gamma.-cyclodextrin which were rendered amorphous through non-selective alkylation. The alkylation agents suitable for that purposes are exemplified by propylene oxide, glycidol, iodoacetamide, chloroacetate, or 2-diethylaminoethylchloride; their reactions with cyclodextrins were performed in a manner to yield mixtures containing many components, a circumstance which effectively prevents crystallization processes within the above pharmaceutical preparation.|
|Inventor(s):||Pitha; Josef (Baltimore, MD)|
|Assignee:||The United States of America as represented by the Department of Health (Washington, DC)|
|Patent Litigation and PTAB cases:||See patent lawsuits and PTAB cases for patent 4,727,064|
1. A method of producing a stablizing amorphous complex of a drug and a mixture of cyclodextrins which comprises the steps of:
1. Dissolving an intrinsically amorphous mixture of cyclodextrin deratives which are water soluble and capable of forming inclusion complexes with drugs in water; and
2. Solublizing lipophilic drugs into the aqueous media to form a solution and form a solublized drug/cyclodextrin complex.
2. A method of claim 1 wherein the solubilized complex is subjected to freeze-dried or evaporation to provide a solid cyclodextrin/drug complex in powder form.
3. A method of claim 1 wherein cyclodextrins used are substituted by at least one of the following substituents: hydroalkyl, carboxamide, diethylaminoethyl, carboxymethyl, and carboxyamidomethyl.
4. A method of claim 1 wherein the drug is a hormone.
5. A method of claim 4 wherein the drug is testosterone, an estrogen, or a progesterone.
6. A composition of matter which contains an amorphous complex of cylodextrin and a drug.
7. A omposition of matter of claim 6 wherein the drug is a hormone.
8. A composition of claim 6 wherein the drug is at least one of testosterone, progesterone, and an estrogenic drug.
9. A composition of matter of claim 6 in solid form.
10. A composition of matter of claim 9 which is a tablet.
11. A composition of matter of claim 6 which is in a liquid or semi-liquid form.
12. A composition of matter for use in the process of claim 1 containing a mixture of substituted cyclodextrin derivatives in amorphous form.
13. A composition of matter of claim 6 wherein the drug is a vitamin.
14. A composition of matter of claim 6 wherein the drug is a salt of retinoic acid.
15. A composition of matter of claim 6 wherein the drug is a steroid.
16. A composition of matter of claim 6 wherein the drug is a spironolactone.
17. A composition of matter of claim 6 wherein the drug is an antiviral agent.
18. A composition of matter of claim 17 wherein the antiviral agent is acylovir.
19. A composition of matter of claim 6 wherein the drug is a diuretic.
20. A composition of matter of claim 19 wherein the diuretic is chlorthalidone.
21. A composition of matter of claim 6 wherein the drug is an anticoagulant.
22. A composition of matter of claim 21 wherein the anticoagulant is dicumerol.
23. A composition of matter of claim 6 wherein the drug is an anticonvulsant
24. A composition of matter of claim 23 wherein the drug is diphenylhydantoin.
25. A composition of matter of claim 6 wherein the drug is an antiinflammatory agent.
26. A composition of matter of claim 25 wherein the antiinflammatory agent is iproniazid.
27. A composition of matter of claim 16 wherein the drug is oxyprenolol.
28. A composition of matter in solid or semi-solid form comprising at least one of testosterone, progesterone, and estradiol as an inclusion complex with poly-.beta.-cylodextin and/or hydroxypropyl-.beta.-cyclodextrin adapted for administration by buccal route.
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