Claims
- 1. A solid controlled release pharmaceutical dosage unit in the form of a compressed mixture consisting essentially of:
- up to 60% by weight of a therapeutically effective product;
- at least 40% by weight of amylose cross-linked with a cross-linking agent selected from the group consisting of epichlorohydrin and 2,3-dibromopropanol, wherein said cross-linked amylose is prepared by cross-linking amylose with from 1 to 20 grams of said cross-linking agent per 100 grams of amylose, and wherein said cross-linking provides sustained release of said therapeutically effective product; and
- an enzyme for modulating the release of the pharmaceutical product, said enzyme being an .alpha.-amylase present in an amount corresponding to an enzyme activity of 100 EU or less per dosage unit.
- 2. The pharmaceutical dosage unit of claim 1, wherein the enzyme is present in an amount corresponding to an enzyme activity of 100 EU per tablet or less.
- 3. The pharmaceutical dosage unit of claim 1, wherein the cross-linking agent is epichlorohydrin.
- 4. A solid controlled release pharmaceutical dosage unit according to claim 1, wherein the release time of the solid controlled release pharmaceutical dosage unit containing the .alpha.-amylase is about 15 to 24 hours.
- 5. A solid controlled release pharmaceutical dosage unit according to claim 1, wherein the release time of the solid controlled release pharmaceutical dosage unit containing the .alpha.-amylase is 6 to 12 hours.
- 6. A solid controlled release pharmaceutical dosage unit according to claim 3, wherein the release time of the solid controlled release pharmaceutical dosage unit containing the .alpha.-amylase is about 15 to 24 hours.
- 7. A solid controlled release pharmaceutical dosage unit according to claim 3, wherein the release time of the solid controlled release pharmaceutical dosage unit containing the .alpha.-amylase is 6 to 12 hours.
- 8. The pharmaceutical dosage unit of claim 3, wherein the cross-linking is carried out with about 6 grams of epichlorohydrin per 100 grams of amylose.
- 9. The pharmaceutical dosage unit of claim 1, wherein said compressed mixture is in the form of a tablet.
- 10. The pharmaceutical dosage unit of claim 9, wherein said tablet is prepared by direct compression in a press at more than 0. 5 T/cm.sup.2.
CROSS-REFERENCE TO RELATED APPLICATION
This application is a continuation of application Ser. No. 07/919,762, filed Jul. 24, 1992, abandoned, which is a continuation-in-part of U.S. patent application Ser. No. 07/787,721 filed Oct. 31, 1991, abandoned, which is a continuation of U.S. patent application Ser. No. 07/618,650, filed Nov. 27, 1990, abandoned.
US Referenced Citations (18)
Foreign Referenced Citations (2)
Number |
Date |
Country |
2041774 |
May 1992 |
CAX |
WOA8900045 |
Jan 1989 |
WOX |
Non-Patent Literature Citations (7)
Entry |
J. of Controlled Release vol. 15, No. 1, Feb. 1991 Lenaerts et al pp. 39-46. |
V. Lenaerts et al., "Controlled Release of Theophylline from Cross-linked Anylose Tablets" Journal of Controlled Release 15(1): 39-46 (1991). |
Canada (Abstract), Derwent Publications, Week 9233, May 28, 1992, CA A2 041 774. |
Pharm. ACTA Helv. 56, Nr. 4-5 (1981). |
Pharm. ACTA helv. 55, Nr. 6 (1980). |
Journal of Polymer Science: Polymer Physics Edition, vol. 21, 983-997 (1983). |
Analytical Letters, 14 (B17 & B18), 1501-1514 (1981). |
Continuations (2)
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Parent |
919762 |
Jul 1992 |
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Parent |
618650 |
Nov 1990 |
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Continuation in Parts (1)
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787721 |
Oct 1991 |
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