Coating capsules with active pharmaceutical ingredients

• US 20070212411A1
• Filed: 03/09/2007
• Published: 09/13/2007
• Est. Priority Date: 03/09/2006
• Status: Active Grant

• Current Assignee: GlaxoSmithKline LLC (GlaxoSmithKline PLC)
• Original Assignee: GlaxoSmithKline LLC (GlaxoSmithKline PLC)
• Inventors: Bobotas, George, Fawzy, Abdel
• Granted Patent: US 8,784,886 B2
• Time in Patent Office: Days
• US Class Current: 424/457
• CPC Class Codes: A61K 9/4808 characterised by the form of the capsule or the structure of the filling; Capsules containing small tablets; Capsules with outer layer for immediate drug release capsules filled with granules or microparticles A61K9/16; filled with microcapsules or coated microparticles A61K9/50; with mixture of different granules, microcapsules, (coated) microparticles A61K9/5084
• CPC Class Codes: A61K 9/4891 Coated capsules; Multilayered drug free capsule shells with drug coating for immediate release A61K9/4808; osmotic devices A61K9/0004

Abstract

Pharmaceutical compositions in unit dose form comprising capsules containing one or more first active pharmaceutical ingredient in a pharmaceutically acceptable vehicle, coated with one or more second active pharmaceutical ingredients, wherein the unit dose form is a pharmaceutical grade finished dosage form, and methods of making and using the same.

Claims

1. A pharmaceutical composition in unit dose form comprising:

(a) a hard or soft capsule comprising at least one first active pharmaceutical ingredient in a pharmaceutically acceptable vehicle;

(b) one or more coatings on the hard or soft capsule, wherein at least one coating comprises at least one second active pharmaceutical ingredient; and

wherein the unit dose form is a pharmaceutical grade finished dosage form.

2. The pharmaceutical composition of claim 1, further comprising at least one additional coating between the capsule and the at least one coating comprising the at least one second active pharmaceutical ingredient.

3. The pharmaceutical composition of claim 2, wherein the at least one additional coating is selected from the group consisting of immediate release coatings, protective coatings, enteric or delayed release coatings, sustained release coatings, barrier coatings, and combinations thereof.

4. The pharmaceutical composition of claim 1, further comprising at least one top coating on the at least one coating comprising the at least one second active pharmaceutical ingredient.

5. The pharmaceutical composition of claim 4, wherein the at least one top coating is selected from the group consisting of immediate release coatings, protective coatings, enteric or delayed release coatings, sustained release coatings, barrier coatings, and combinations thereof.

6. The pharmaceutical composition of claim 1, further comprising at least one barrier coating between the capsule and the at least one coating comprising the at least one second active pharmaceutical ingredient, and at least one top coating selected from the group consisting of enteric or delayed release coatings, protective coatings, or combinations thereof, on the at least one coating comprising the at least one second active pharmaceutical ingredient.

7. The pharmaceutical composition of claim 1, wherein the at least one first active pharmaceutical ingredient and the at least one second active pharmaceutical ingredient are the same or different and are independently selected from the group consisting of analgesics, anti-inflammatory agents, anti-helminthics, anti-arrhythmic agents, anti-asthma agents, anti-bacterial agents, anti-viral agents, anti-coagulants, anti-dementia agents, anti-depressants, anti-diabetics, anti-epileptics, anti-fungal agents, anti-gout agents, anti-hypertensive agents, anti-malarials, anti-migraine agents, anti-muscarinic agents, anti-neoplastic agents, immunosuppressants, anti-protozoal agents, anti-thyroid agents, anti-tussives, anxiolytics, sedatives, hypnotics, neuroleptics, neuroprotective agents, β

-blockers, cardic inotropic agents, cell adhesion inhibitors, corticosteroids, cytokine receptor activity modulators, diuretics, anti-parkinsonian agents, gastrointestinal agents, histamine H-receptor antagonists, keratolytics, lipid regulating agents, muscle relaxants, nitrates and other anti-anginal agents, non-steroid anti-asthma agents, nutritional agents, opioid analgesics, sex hormones, stimulants and anti-erectile dysfunction agents, and combinations thereof.

8. The pharmaceutical composition of claim 7, wherein either or both of the at least one first active pharmaceutical ingredient and second active pharmaceutical ingredient are lipid regulating agents independently selected from the group consisting of omega-3 fatty acids, a statin compound, a squalene synthesis inhibitor, an azetidinone-based cholesterol absorption inhibitor, a LDL (low density lipoprotein) catabolism enhancer, a peroxisome proliferator-activated receptor (PPAR) agonist and/or antagonist, niacin and derivatives such as nicotinamide, a bile acid sequestrant, an MTP inhibitor, an LXR agonist and/or antagonist, and combinations thereof.

9. The pharmaceutical composition of claim 1, wherein the at least one first active pharmaceutical ingredient comprises omega-3 fatty acids.

10. The pharmaceutical composition of claim 1, wherein the at least one second active pharmaceutical ingredient comprises a statin compound or a fibrate compound.

11. The pharmaceutical composition of claim 9, wherein the at least one second active pharmaceutical ingredient comprises a statin compound or a fibrate compound.

12. The pharmaceutical composition of claim 1, wherein the dosage form is suitable for oral administration.

13. The pharmaceutical composition of claim 1, wherein the capsule is a soft gelatin capsule.

14. The pharmaceutical composition of claim 1, wherein the capsule has an oblong shape.

15. The pharmaceutical composition of claim 1, wherein the at least one coating comprising the at least one second active pharmaceutical ingredient is applied by pan coating, fluid bed coating, or spray coating.

16. The pharmaceutical composition of claim 1, wherein the at least one coating comprising the at least one second active pharmaceutical ingredient comprises at least one compound present in an amount sufficient to prevent oxidative degradation of the at least one second active pharmaceutical ingredient for a pharmaceutically acceptable duration of time.

17. The pharmaceutical composition of claim 1, wherein the at least one coating comprising the at least one second active pharmaceutical ingredient has a thickness sufficient to prevent oxidative degradation of the at least one second active pharmaceutical ingredient for a pharmaceutically acceptable duration of time.

18. A method of administering a pharmaceutical composition to a subject, comprising administering to the subject the pharmaceutical composition of claim 1.

19. The method of claim 18, wherein the at least one first active pharmaceutical ingredient and/or the at least one second active pharmaceutical ingredient comprises a lipid regulation agent, and the method of administration comprises treatment of at least one condition or disease independently selected from the group consisting of hypertriglyceridemia, hypercholesterolemia, mixed dyslipidemia, coronary heart disease (CHD), vascular disease, atherosclerotic disease and related conditions.

20. The method of claim 19, wherein the at least one first active pharmaceutical ingredient comprises omega-3 fatty acids and the at least one second active pharmaceutical ingredient comprises a statin compound or a fibrate compound.