Claims
- 1. A method for preparing a medicament supported on a polymer substance in a form capable of increasing the dissolving rate of said medicament, which comprises:
- 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,
- 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
- 2) drying the product obtained in step 1) 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.
- 2. A method as claimed in claim 1, wherein said contact with said non-aqueous organic solvent is effected in a reaction vessel into which said non-aqueous organic solvent is fed in the form of vapour.
- 3. A method as claimed in claim 1, wherein said contact with said non-aqueous organic solvent is effected in a sealed reaction vessel saturated with solvent vapour generated within said vessel itself.
- 4. A method as claimed in claim 1, wherein said contact with said non-aqueous organic solvent is effected in a fluidised bed by spraying said particles with said non-aqueous organic liquid solvent.
- 5. A method as claimed in claim 1, wherein said contact with said non-aqueous organic solvent is effected in a fluidised bed by an air stream saturated with solvent vapour.
- 6. A method as claimed in claim 1, wherein said contact with said non-aqueous organic solvent is effected by suspending said product in said non-aqueous organic solvent in liquid form.
- 7. A method as claimed in claim 1, wherein said contact with said non-aqueous organic solvent in gaseous form is effected at a temperature of between 20.degree. and 100.degree. C.
- 8. A method as claimed in claim 1, wherein said contact with said non-aqueous organic solvent in liquid form is effected at a temperature of between 5.degree. and 90.degree. C.
- 9. A method as claimed in claim 1, wherein said drying is effected at a temperature of between 20.degree. and 100.degree. C.
- 10. A method as claimed in claim 1, wherein said polymer is selected from the group consisting of crosslinked polyvinylpyrrolidone, crosslinked sodium carboxymethylcellulose, crosslinked .beta.-cyclodextrin polymer, and crosslinked dextran.
- 11. A method as claimed in claim 1, wherein said medicament is selected from the group consisting of griseofulvin, indomethacin, diacerein, megestrol, and nicergoline.
- 12. A method as claimed in claim 1, wherein said non-aqueous organic solvent is selected from the group consisting of methanol, ethanol, higher alcohols, acetone, chlorinated solvents, formamide, DMF, and fluorinated hydrocarbons.
- 13. A method for preparing a medicament supported on a polymer substance in a form capable of increasing the dissolving rate of said medicament, which comprises:
- 1) incorporating said medicament selected from the group consisting of griseofulvin, indomethacin, diacerein, megestrol, and nicergoline into particles of a crosslinked polymer selected from the group consisting of crosslinked polyvinylpyrrolidone, crosslinked sodium carboxymethylcellulose, crosslinked .beta.-cyclodextrin polymer, and crosslinked dextran, 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, wherein the weight ratio of said medicament to said polymer is between 0.1 and 1000 parts by weight of said medicament per 100 parts by weight of said polymer;
- 2) bringing the product obtained in step 1) into contact with a solvent, in gaseous or liquid form, which is selected from the group consisting of methanol, ethanol, higher alcohols, acetone, chlorinated solvents, formamide, DMF, and fluorinated hydrocarbons, which is capable of swelling said polymer, wherein treatment with said solvent in gaseous form is conducted at a temperature of between 20.degree. and 100.degree. C. and treatment with said solvent in liquid form is conducted at a temperature of between 5.degree. and 90.degree. C.; 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.
- 14. A method as claimed in claim 13, wherein said non-aqueous organic solvent is selected from the group consisting of methanol, ethanol, higher alcohols, acetone, chlorinated solvents, formamide, DMF, and fluorinated hydrocarbons.
Priority Claims (1)
Number |
Date |
Country |
Kind |
22336 A/88 |
Oct 1988 |
ITX |
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Parent Case Info
This application is a continuation of application Ser. No. 07/421,943 filed on Oct. 16, 1989, now abandoned.
US Referenced Citations (6)
Continuations (1)
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Number |
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Parent |
421943 |
Oct 1989 |
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