Controlled release insufflation carrier for medicaments

• US 5,612,053 A
• Filed: 04/07/1995
• Issued: 03/18/1997
• Est. Priority Date: 04/07/1995
• Status: Expired due to Term

• Current Assignee: Penwest Pharmaceuticals Company (Endo International PLC)
• Original Assignee: Edward Mendell Co., Inc.
• Inventors: Baichwal, Anand, Staniforth, John N.
• Primary Examiner(s): AZPURU, CARLOS A
• Application Number:
  US08/419,635
• Time in Patent Office: 711 Days
• Field of Search: 424/440, 424/488, 424/499, 424/500, 424/434
• US Class Current: 424/440
• CPC Class Codes: A61K 9/0075 for inhalation via a dry powder inhaler [DPI], e.g. comprising micronized drug mixed with lactose carrier particles
• CPC Class Codes: A61K 9/146 with organic macromolecular compounds

Abstract

Controlled release powder insufflation formulations are disclosed. The powder formulation includes cohesive composites of particles containing a medicament and a controlled release carrier which preferably includes one or more polysaccharide gums of natural origin.

Claims

1. A respirable particle-based pharmaceutical formulation for delivering a medicament via insufflation, comprising controlled release particles of a cohesive composite of a medicament and a pharmaceutically-acceptable carrier comprising a polysaccharide gum of natural origin, wherein the average particle size of the said cohesive composite particles is from about 0.1 to about 125 microns in diameter.

2. The formulation of claim 1, wherein the average particle size of said cohesive composite particle is from about 0.1 to about 10 microns.

3. The formulation of claim 1, wherein the average particle size of said cohesive composite particle is from about 10 to about 125 microns.

4. The formulation of claim 1, wherein said polysaccharide gum comprises a heteropolysaccharide gum.

5. The formulation of claim 1, wherein said polysaccharide gum comprises a homopolysaccharide gum.

6. The formulation of claim 1, wherein said polysaccharide gum comprises a starch.

7. The formulation of claim 4, wherein said heteropolysaccharide gum is xanthan gum.

8. The formulation of claim 4, wherein said heteropolysaccharide gum is locust bean gum.

9. The formulation of claim 1, wherein said polysaccharide gum comprises a heteropolysaccharide gum and a homopolysaccharide gum in a ratio of from about 1:

3 to about 3;

1.

10. The formulation of claim 1, wherein the medicament polysaccharide to gum ratio is from about 0.5:

100 to about 1;

1.

11. The formulation of claim 10, wherein the medicament polysaccharide to gum ratio is from about 1:

100 to about 1;

2.

12. The formulation of claim 1, further comprising from about 0.1 to about 50% by weight of a cationic cross-linking agent comprising an alkaline metal or an alkaline earth metal sulfate, chloride, borate, bromide, citrate, acetate or lactate.

13. The formulation of claim 12, wherein said cationic cross-linking agent is present in an amount of from about 1 to about 10% by weight.

14. The formulation of claim 12, wherein said cationic cross-linking agent is selected from the group consisting of potassium chloride and sodium chloride.

15. The formulation of claim 1, wherein said pharmaceutically acceptable carrier further comprises an inert saccharide diluent selected from the group consisting of monosaccharides, disaccharides and mixtures thereof.

16. The formulation of claim 15, wherein said inert saccharide diluent is selected from the group consisting of dextrose, sucrose, galactose, lactose and mixtures thereof.

17. The formulation of claim 1, wherein said pharmaceutically acceptable carrier further comprises a pharmaceutically-acceptable surfactant in an amount of from about 0.5 to about 3% by weight of the controlled release carrier.

18. The formulation of claim 17, wherein said surfactant is selected from the group consisting of pharmaceutically-acceptable anionic surfactants, cationic surfactants, amphoteric (amphipathic/amphophilic) surfactants, non-ionic surfactants, and mixtures thereof.

19. The formulation of claim 1, wherein said controlled release particles are compressed together to form a solid mass.