IP Library › Granted Patent US 8,362,062
Granted Patent B2
US 8,362,062 · App. 10/541,216 · Granted Jan 29, 2013

Pharmaceutical compositions with improved dissolution

Inventors: Mark Tawa (West Roxbury, MA); Julius Remenar (Framingham, MA); Matthew L. Peterson (Hopkinton, MA); Örn Almarsson (Shrewsbury, MA); Hector Guzman (Jamaica Plain, MA); Hongming Chen (Acton, MA); Mark Oliveira (Framingham, MA)
Assignee: McNeil-PPC, Inc.
View Patent ↗
Loading inventors, assignments & file history…
Monitor This Case
Get email alerts when status or documents change.
Order Certified Copies
Most orders are placed with the USPTO same day — all within 24 business hours.
Order via The Patent Place →
Pre-filled with this patent's details
Quick Facts
Patent No.
US 8,362,062
App. No.
10/541,216
Granted
Jan 29, 2013
Kind
B2
Abstract

The invention relates to methods of screening mixtures containing a pharmaceutical compound and an excipient to identify properties of the pharmaceutical compound/excipient combination that retard solid-state nucleation. The invention further relates to increasing the solubility, dissolution and bioavailability of a drug with low solubility in gastric fluids conditions by combining the drug with a precipitation retardant and an optional enhancer.

Claims (15)

1. A pharmaceutical composition comprising: (a) a salt form of celecoxib; (b) d-alpha-tocopherol polyethylene glycol-1000 succinate (vitamin E TPGS); and (c); an enhancer selected from the group consisting of hydroxypropylcellulose and hydroxypropylmethylcellulose; wherein the composition retards crystallization or precipitation of the celecoxib for at least 5 minutes in gastric fluid conditions, wherein the pharmaceutical composition is formulated in a form suitable for oral administration.

2. The pharmaceutical composition according to claim 1 , wherein crystallization or precipitation is retarded for at least 20 minutes.

3. The pharmaceutical composition according to claim 1 , wherein crystallization or precipitation is retarded for at least 40 minutes.

4. The pharmaceutical composition according to claim 1 , wherein crystallization or precipitation is retarded for at least 60 minutes.

5. The pharmaceutical composition according to claim 1 , wherein the salt form of the celexoxib is an alkali metal or alkaline earth metal salt.

6. The pharmaceutical composition according to claim 1 , wherein the salt form of the API is a sodium, potassium, lithium, or calcium salt.

7. The pharmaceutical composition according to claim 1 , wherein the bioavailability of the composition orally administered is at least 70%.

8. The pharmaceutical composition according to claim 1 , wherein the bioavailability of the composition orally administered is as least 80%.

9. The pharmaceutical composition according to claim 1 , wherein the bioavailability of the composition orally administered is as least 90%.

10. The pharmaceutical composition according to claim 1 , wherein the C max is at least 2 fold greater than a neutral form in vivo or in an in vitro dissolution assay.

11. The pharmaceutical composition according to claim 1 , wherein the C max is at least 4 fold greater than a neutral form in vivo or in an in vitro dissolution assay.

12. The pharmaceutical composition according to claim 1 , wherein the C max is at least 10 fold greater than a neutral form in vivo or in an in vitro dissolution assay.

13. The pharmaceutical composition according to claim 1 , wherein the bioavailability of the composition is at least 50% greater than a neutral form.

14. The pharmaceutical composition according to claim 1 , wherein the bioavailability of the composition is at least 2 fold that of a neutral form.

15. The pharmaceutical composition according to claim 1 , wherein the bioavailability of the composition is at least 5 fold that of a neutral form.

Assignments (3)
MERGER AND CHANGE OF NAME Recorded Jul 2, 2015
From: MCNEIL-PPC, INC.; JOHNSON & JOHNSON CONSUMER INC.
To: JOHNSON & JOHNSON CONSUMER INC.
Reel/Frame 036049/0254 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 19, 2012
From: TRANSFORM PHARMACEUTICALS, INC.
To: MCNEIL-PPC, INC.
Reel/Frame 028988/0958 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 21, 2005
From: TAWA, MARK; REMENAR, JULIUS; PETERSON, MATTHEW; ALMARSSON, ORN; GUZMAN, HECTOR; CHEN, HONGMING; OLIVEIRA, MARK
To: TRANSFORM PHARMACEUTICALS, INC.
Reel/Frame 016923/0769 →
Continuity (37)
Continuation In Part 10601092 · Jun 20, 2003
Continuation In Part PCTUS0319754 · Jun 20, 2003
Continuation In Part PCTUS0327772 · Sep 4, 2003
Continuation In Part 10378956 · Mar 3, 2003
Continuation In Part 10541216
Continuation In Part 10660202 · Sep 11, 2003
Continuation In Part PCTUS0327772 · Sep 4, 2003
Continuation In Part 10378956
Continuation In Part 10637829 · Aug 8, 2003
Division 10295995 · Nov 18, 2002
Continuation 10232589 · Sep 3, 2002
Continuation In Part 10449307 · May 30, 2003
Continuation In Part 10601092
Continuation In Part 10541216
Continuation In Part PCTUS0328982 · Sep 16, 2003
Provisional Application 60441335 · Jan 21, 2003
Provisional Application 60456608 · Mar 21, 2003
Provisional Application 60459501 · Apr 1, 2003
Provisional Application 60486713 · Jul 11, 2003
Provisional Application 60456027 · Mar 18, 2003
Provisional Application 60437516 · Dec 30, 2002
Provisional Application 60451213 · Feb 28, 2003
Provisional Application 60487064 · Jul 11, 2003
Provisional Application 60390881 · Jun 21, 2002
Provisional Application 60426275 · Nov 14, 2002
Provisional Application 60427086 · Nov 15, 2002
Provisional Application 60429515 · Nov 26, 2002
Provisional Application 60360768 · Mar 1, 2002
Provisional Application 60463962 · Apr 18, 2003
Provisional Application 60406974 · Aug 30, 2002
Provisional Application 60380288 · May 15, 2002
Provisional Application 60356764 · Feb 15, 2002
Provisional Application 60444315 · Jan 31, 2003
Provisional Application 60439282 · Jan 10, 2003
Provisional Application 60384152 · May 31, 2002
Provisional Application 60412459 · Sep 20, 2002
Related Publication 20060134198A1 · Jun 22, 2006