Solid pharmaceutical composition comprising an excipient capable of binding water

• US 6,187,339 B1
• Filed: 10/17/1995
• Issued: 02/13/2001
• Est. Priority Date: 10/17/1994
• Status: Expired due to Fees

• Current Assignee: N.V. Organon (Merck & Co., Inc.)
• Original Assignee: Akzo Nobel N.V. (Nouryon BV)
• Inventors: Poels-Janssen, Henrika Gerardina Maria, de Haan, Pieter
• Primary Examiner(s): Harrison, Robert H.
• Application Number:
  US08/544,042
• Time in Patent Office: 1,946 Days
• Field of Search: 424/469, 424/451, 424/452, 424/461, 424/464, 424/465, 424/484, 424/488, 424/494, 424/497, 514/170, 514/177, 514/182, 514/781, 514/970
• US Class Current: 424/469
• CPC Class Codes: A61K 31/567 substituted in position 17 alpha, e.g. mestranol, norethandrolone
• CPC Class Codes: A61K 9/2013 Organic compounds, e.g. phospholipids, fats
• CPC Class Codes: A61K 9/2054 Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
• CPC Class Codes: A61P 5/24 of the sex hormones

Abstract

The invention concerns a solid pharmaceutical composition comprising less than 7% by weight of an oil or oily substance, a low dosage active ingredient, and a water insoluble non-cross-linked polymeric excipient capable of binding water and having a mean particle size greater than 150 μm. The composition can be obtained by a simple procedure comprising mixing the water insoluble non-cross-linked polymeric excipient capable of binding water and the active ingredient, which is dissolved or dispersed in an oil or an oily substance, in an aqueous dispersion thereof, or in water.

Claims

1. A solid pharmaceutical composition comprising at least one solvent or dispersant selected from the group consisting of an oil, an oily substance, an aqueous dispersion of an oil or oily substance, and water, a low dosage active ingredient, and a water insoluble non-cross-linked polymeric excipient that binds water and has a particle size distribution wherein at least 50% of the particles by volume have a diameter of from 150μ

to 200μ

, wherein the oil, oily substance or dispersion is present in an amount by which the oil or oily substance contributes from 0% to 7% by weight of the pharmaceutical composition and wherein any water present is present in an amount by which the weight ratio of polymeric excipient to water is greater than 5;

1.

2. The solid pharmaceutical composition of claim 1, comprising from about 0.1% to 4% by weight of an oil or oily substance.

3. The solid pharmaceutical composition of claim 1 wherein the oil or oily substance has a melting point below about 40°

C.

4. The solid pharmaceutical composition of claim 1, wherein the active ingredient comprises a dosage of 0.005 to 5 percent by weight.

5. The solid pharmaceutical composition of claim 1, wherein the active ingredient is a steroid.

6. The solid pharmaceutical composition of claim 1, wherein the water insoluble non-cross-linked polyermic excipient that binds water has a particle size distribution wherein no more than 10% of the particles by volume have a diameter of 70μ

or less, at least 50% of the particles by volume have a diameter of from 150μ

to 200μ

, and 90% of the particles by volume have a diameter of 260μ

or less.

7. The solid pharmaceutical composition of claim 1, wherein the water insoluble non-cross-linked polymeric excipient that binds water is a cellulose or a starch.

8. The solid pharmaceutical composition of claim 1, wherein the active ingredient is selected from the group consisting of desogestrel, ethinyl estradiol and a mixture thereof.

9. A process for the preparation of the solid pharmaceutical composition of claim 1, comprising dissolving or dispersing a low dosage of an active ingredient in an oil or an oily substance, an aqueous dispersion thereof, or in water, and mixing the dissolved or dispersed active ingredient with a water insoluble non-cross-linked polymeric excipient that binds water and has a particle size distribution wherein at least 50% of the particles by volume have diameter of from 150μ

to 200μ

.

10. The process according to claim 9, wherein the ratio of the water insoluble non-cross-linked polymeric excipient that binds water and water present in the process is greater than 5:

1.

11. The process according to claim 10, wherein the ratio of the water insoluble non-cross-linked polymer excipient that binds water and water present in the process is greater than 10:

1.