Stable pharmaceutical compositions without a stabilizer

• US 20050142195A1
• Filed: 01/03/2005
• Published: 06/30/2005
• Est. Priority Date: 11/21/2002
• Status: Active Grant

• Current Assignee: Boyong Li, Xiu Xiu Cheng
• Original Assignee: Boyong Li, Xiu Xiu Cheng
• Inventors: Cheng, Xiu Xiu, Li, Boyong
• Granted Patent: US 8,501,227 B2
• Time in Patent Office: Days
• US Class Current: 424/464
• CPC Class Codes: A61K 31/137 Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine or methadone
• CPC Class Codes: A61K 9/2031 obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyethylene oxide, poloxamers
• CPC Class Codes: A61K 9/2054 Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose

Abstract

Stabilized controlled release pharmaceutical preparations are disclosed in which active ingredient degradation is prevented without the use of a stabilizer. The active ingredient is sealed away from excipients that can adversely affect stability by sealing the excipients rather than the active ingredient. The preparations are substantially unaffected by exposure to storage conditions of elevated temperature and/or elevated relative humidity.

Claims

1. A method for stabilizing pharmaceutical preparations in solid dosage forms by:

preventing direct contact between excipients that have a negative effect on stability of pharmaceutically active ingredients, said method comprising;

a) adding a sealing component to said excipients to form a sealed excipient component; and

b) combining said sealed excipient component with a composition comprising pharmaceutically active components to form a stable composition.

2. The method for stabilizing the pharmaceutically active component of claim 1, wherein said composition retains at least 85% w/w of undegraded active ingredient after storage for 3 months at about 40°

C. and about 75% relative humidity.

3. The method of claim 1, wherein said pharmaceutically active ingredient comprises bupropion.

4. The method of claim 1, wherein said sealing component is a water-soluble polymer binding agent comprising hydroxypropylcellulose or hydroxypropyl methylcellulose.

5. The method of claim 1, wherein the sealing component comprises hydroxypropyl cellulose.

6. The method of claim 1, wherein the sealed excipients comprise a combination of low molecular weight and high molecular weight polyethylene oxides.

7. The method of claim 1, wherein the sealed excipient ratio of high molecular weight to low molecular weight polyethylene oxides is 1:

1.24 (wt./wt.).

8. A pharmaceutical composition in solid form comprising pharmaceutically active ingredients combined with excipients having a negative effect on stability, combined with a sealing component.

9. The composition of claim 8, wherein the pharmaceutically active ingredients comprise bupropion.

10. The composition of claim 9 in the form of a tablet or capsule comprising bupropion, hydroxypropyl cellulose or hydroxypropyl methylcellulose and inactive ingredients.

11. The tablet or capsule of claim 10, wherein the amount of bupropion ranges from about 75 to about 300 mg.

12. The tablet or capsule of claim 10 wherein the amount of bupropion hydrochloride is 150 mg.

13. The composition of claim 8 wherein the amount of sealing component comprises 2% to 20% of the total weight.

14. A pharmaceutical composition of claim 13, comprising by weight, approximately,

15. An improved method for preparing a solid dosage delivery form comprising an active ingredient and excipients that can adversely affect the stability of said active ingredient, the improvement comprising seal coating said excipients prior to adding said excipients to said active ingredient.

16. An improved method as defined in claim 15 where said active ingredient is selected from the group consisting of algicides, antioxidants, air purifiers, biocides, bactericides, catalysts, chemical reactants, disinfectants, fungicides, fermentation agents, fertility inhibitors, fertility promoters, germicides, herbicides, insecticides, microorganism attenuators, pesticides, plant growth promoters, plant growth inhibitors, preservatives, rodenticides, sterilization agents, sex sterilants, and mixtures of any of the foregoing.

17. An improved method for preparing a solid dosage delivery form comprising an active ingredient and excipients that can adversely affect the stability of said active ingredient, the improvement comprising seal coating said excipients prior to adding said excipients to said active ingredient.

18. An improved method as defined in claim 17 where said active ingredient is selected from the group consisting of algicides, antioxidants, air purifiers, biocides, bactericides, catalysts, chemical reactants, disinfectants, fungicides, fermentation agents, fertility inhibitors, fertility promotors, germicides, herbicides, insecticides, microorganism attenuators, pesticides, plant growth promotors, plant growth inhibitors, preservatives, rodenticides, sterilization agents, sex sterilants, and mixtures of any of the foregoing.

19. An improved method as defined in claim 18 where said active ingredient comprises a pharmaceutical drug.

20. An improved method as defined in claim 19, where said pharmaceutical drug comprises bupropion hydrochloride.