Pharmaceutical compositions with controlled release, and a method for their preparation

• US 5,008,114 A
• Filed: 11/28/1988
• Issued: 04/16/1991
• Est. Priority Date: 04/08/1988
• Status: Expired due to Fees

• Current Assignee: Adare Pharmaceuticals, Inc.
• Original Assignee: Vectorpharma International S.p.A.
• Inventors: Lovrecich, Mara L.
• Primary Examiner(s): Page, Thurman K.
• Assistant Examiner(s): Spear, James M.
• Application Number:
  US07/276,489
• Time in Patent Office: 869 Days
• Field of Search: 424/423, 424/468, 424/469, 424/443, 424/464, 424/465, 424/484, 424/425
• US Class Current: 424/484
• CPC Class Codes: A61K 9/143 with inorganic compounds
• CPC Class Codes: Y10S 977/915 Therapeutic or pharmaceutical composition

Abstract

Pharmaceutical compositions including a microporous support and an active substance incorporated therein, the incorporation of the active substance being effected by adding the microporous support to a solution of the active substance, stirring the mixture obtained for at least 70 hours at ambient temperature and finally evaporating the solvent slowly.

Claims

1. Pharmaceutical compositions comprising a microporous support having pores of an average diameter of between 5 and 150 nm, a surface area of between 30 and 600 m² /g, and a particle diameter of less than 200 microns, said microporous support being selected from the group consisting of silica, silicates, zeolites, alumina, activated carbon and a microporous polymer, said microporous support having a pharmaceutically active substance selected from the group consisting of antihypertensive, antiinflammatory, antianxiety, antidepressive, corticosteroids and antibacterial medicaments distributed within the support pores in crystalline form, the crystal dimensions being in the nanometer range.

2. Compositions as claimed in claim 1, wherein said active substance crystal dimensions are between 3 and 100 nm.

3. Compositions as claimed in claim 1, wherein the content of said active substance is between 4 and 60% by weight.

4. Compositions as claimed in claim 1, wherein the active substance'"'"'s crystal dimensions are between 3 and 100 nanometers and the content of the active substance is between 4 and 60% by weight.

5. Compositions as claimed in claim 1, wherein the active substance is selected from the group consisting of diazepam, digoxin, griseofulvin, methylhydroxy-progesterone acetate, nifedipine, megestrol acetate, haloperidol, nicardipine, diltiazem and etoposide.

6. Compositions as claimed in claim 1, comprising excipients selected from the group consisting of gelatin, sorbitol, lactose, starch, magnesium stearate and sodium lauryl sulphate.

7. A method for preparing pharmaceutical compositions, comprising adding a microporous support, having pores of an average diameter of between 5 and 150 nm, a surface area of between 30 and 600 m² /g, and a particle diameter of less than 200 microns, and being selected from the group consisting of silica, silicates, zeolites, alumina, activated carbon and a microporous polymer, to a solution of a pharmaceutically active substance selected from the group consisting of antihypertensive, antiinflammatory, antianxiety, antidepressive, corticosteroids and antibacterial medicaments, stirring at ambient temperature for at least 70 hours, then slowly evaporating the solvent at a temperature of 10°

-20°

C. less than the solution boiling point in a pressure of between 500 and 760 mmHg.

8. A method as claimed in claim 7, wherein said active substance is a substance of low water solubility.

9. A method as claimed in claim 7, wherein the solvent for the solution of the active substance is selected from the group consisting of water, organic solvents, oils and molten semisolids, chloroform, acetone, dichloroethane, and ethyl alcohol.

10. A method as claimed in claim 7, wherein the active substance concentration in the solution is between 2 and 40 g/l.

11. A method as claimed in claim 7, wherein the quantity of the microporous support added to the solution is between 3 and 500 grams per liter of solution.

12. A method as claimed in claim 7, wherein said stirring at ambient temperature is conducted for 90-100 hours.

13. A method as claimed in claim 7, wherein the active substance is selected from the group consisting of diazepam, digoxin, griseofulvin, methylhydroxy-progesterone acetate, nifedipine, megestrol acetate, haloperidol, nicardipine, diltiazem and etoposide.