Claims
- 1. A poorly soluble medicament supported on a polymer substance in a form capable of increasing the dissolving rate of said medicament, prepared by a method comprising:
- 1) bringing a medicament incorporated into particles of a crosslinked polymer which is swellable in water but insoluble in water by treating said polymer particles with a solution of said medicament in a non-aqueous organic solvent and drying, or by mixing said polymer particles with said medicament, heating to the medicament melting point, and then cooling at ambient temperature;
- 2) bringing the thus formed product into contact with a non-aqueous organic solvent, in gaseous or liquid form, which is capable of swelling said polymer, wherein said contact with said gaseous solvent is conducted for a period of time of between 0.5 and 48 hours, and wherein said contact with said non-aqueous organic liquid solvent is conducted for a period of time of between 1 minute and 96 hours; and
- 3) drying the product obtained in step 2) under vacuum to produce a medicament supported on a polymer substance wherein said medicament has been transformed from a metastable amorphous state to a stable high-energy crystalline state and is present in higher concentration in the surface layers of said polymer particles than in their inner layers.
- 2. A capsule, controlled-release tablet, suspension, or transdermal film, comprising a medicament prepared according to the method of claim 1.
- 3. A poorly soluble medicament prepared according to claim 1 wherein said medicament is supported on a polymer substance in a form capable of increasing the dissolving rate of said medicament, and wherein the medicament concentration is higher in the surface layers of the polymer particles than in their inner layers.
- 4. A poorly soluble medicament prepared according to claim 1 wherein said medicament is supported on a polymer substance in a form capable of increasing the dissolving rate of said medicament, and wherein said medicament is in the form of particles of nanometer dimensions.
- 5. The poorly soluble medicament supported on a polymer substance in a form capable of increasing the dissolving rate of said medicament of claim 1, wherein said polymer is selected from the group consisting of crosslinked polyvinylpyrrolidone, crosslinked sodium carboxymethylcellulose, crosslinked .beta.-cyclodextrin polymer, and crosslinked dextran, and wherein said medicament is selected from the group consisting of griseofulvin, indomethacin, diacerein, megestrol, and nicergoline.
Parent Case Info
This application is a divisional of application Ser. No. 07/952,474, filed on Sep. 28, 1992; now U.S. Pat. No. 5,225,192, which was a continuation of Ser. No. 07/421,943, filed on Oct. 16, 1989, now abandoned; the entire contents of which are hereby incorporated by reference.
US Referenced Citations (8)
Divisions (1)
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952474 |
Sep 1992 |
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Continuations (1)
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421943 |
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