Claims
- 1. A process for the production of medicinal sustained-release granular preparations comprising a medicinal ingredient solid at room temperature in a matrix of polymer and a plasticizer for the polymer which process comprises the steps of
- (1) preparing a suspension of the plasticizer in water,
- (2) admixing and wet granulating an initially dry mixture of fine particulate polymer, having an average particle size not greater than 50 .mu.m, and the medicinal ingredient in the form of a powder by adding the amount of the suspension produced in step (1) to the mixture of polymer and medicinal agent, to obtain granules in which the mixture of the polymer and the plasticizer has a melt film-forming temperature (MFT) and glass transition temperature (Tg) of not more than 100.degree. C., and
- (3) treating said granules at a temperature higher than the lower of the MFT and Tg of the polymer-plasticizer mixture to obtain dry granular preparations.
- 2. Sustained-release granular preparations obtained by the process according to claim 1.
- 3. Sustained-release granular preparations according to claim 2, wherein said plasticizer is an alkyl citrate.
- 4. Sustained-release granular preparations according to claim 2, wherein said plasticizer is a polyethylene glycol.
- 5. Sustained-release granular preparations according to claim 2, wherein said plasticizer is propylene glycol.
- 6. Sustained-release granular preparations according to claim 2, wherein said plasticizer is a glycerin mono-, di- or tri-fatty acid ester.
- 7. Sustained-release granular preparations according to claim 2, wherein said plasticizer is an alkyl phthalate.
- 8. Sustained-release granular preparations according to claim 2, obtained by treating said granules at a temperataure not less than said glass transition temperature.
- 9. Sustained-release granular preparations according to claim 2, wherein said polymer is ethylcellulose.
- 10. The process of claim 1 wherein the temperature of treatment in step 3 is 80.degree. C.
- 11. Sustained-release granular preparations obtained by the process according to claim 10.
- 12. Sustained-release granular preparations according to claim 11 wherein the polymer is ethylcellulose and the plasticizer is triethyl citrate.
- 13. The process of claim 1 wherein the temperature of the treatment in step (3) is 10.degree. C. to 50.degree. C. higher than the lower of the MFT and Tg of the polymer-plasticizer mixture.
- 14. Sustained-release granular preparations according to claim 2, wherein said average particle size of said fine particulate polymer is from 1 .mu.m to 20 .mu.m.
Priority Claims (1)
Number |
Date |
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Kind |
6-314414 |
Dec 1994 |
JPX |
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Parent Case Info
This application is a continuation of 08/849,457 filed Jun. 19, 1997 now U.S. Pat. No. 5,858,411, which is a 371 of PCT/JP95/02594 filed Dec. 18, 1995.
US Referenced Citations (2)
Number |
Name |
Date |
Kind |
4330338 |
Banker |
May 1982 |
|
4702918 |
Ushimaru et al. |
Oct 1987 |
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Foreign Referenced Citations (5)
Number |
Date |
Country |
0 322 137 |
Jun 1989 |
EPX |
0 388 954 |
Sep 1990 |
EPX |
0 421 582 |
Apr 1991 |
EPX |
0 441 245 |
Aug 1991 |
EPX |
42 44 466 |
Jun 1994 |
DEX |
Non-Patent Literature Citations (1)
Entry |
American Pharm. Assoc./Pharm. Society of Great Britain: Handbook of Pharmaceutical Excipients, pp. 134-137 & 289-293, 1986, "Hydroxypropyl Cellulose" and "Starch". |
Continuations (1)
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Parent |
849457 |
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