ENTERIC COATED HYDROPHOBIC MATRIX FORMULATION

• US 20100003322A1
• Filed: 07/03/2008
• Published: 01/07/2010
• Est. Priority Date: 07/03/2008
• Status: Abandoned Application

• Current Assignee: Impax Laboratories Incorporated (Amneal Pharmaceuticals, LLC)
• Original Assignee: Impax Laboratories Incorporated (Amneal Pharmaceuticals, LLC)
• Inventors: LAI, FELIX S., Lee, Bernard, Simpson, Christopher A., Ucpinar, Sibel, Ting, Richard
• Application Number:
  US12/167,876
• Publication Number:
  US 20100003322A1
• Time in Patent Office: Days
• US Class Current: 424/474
• CPC Class Codes: A61K 31/135 having aromatic rings , e.g. ketamine, nortriptyline methadone A61K31/137
• CPC Class Codes: A61K 31/19 Carboxylic acids, e.g. valproic acid salicylic acid A61K31/60
• CPC Class Codes: A61K 31/195 having an amino group
• CPC Class Codes: A61K 31/34 having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
• CPC Class Codes: A61K 31/40 having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
• CPC Class Codes: A61K 31/485 Morphinan derivatives, e.g. morphine, codeine
• CPC Class Codes: A61K 9/2013 Organic compounds, e.g. phospholipids, fats
• 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 9/282 Organic compounds, e.g. fats
• CPC Class Codes: A61K 9/2846 Poly(meth)acrylates

Abstract

An enteric coated hydrophobic matrix tablet for soluble, freely soluble and very soluble drugs.

Claims

1. An enteric coated tablet comprising:

(a) a matrix drug core comprising;

(i) a therapeutically effective amount of a soluble drug;

(ii) a hydrophobic rate controlling material that is a solid at room temperature; and

(iii) optionally a diluent and

(b) an enteric coating surrounding the matrix drug core comprising;

(i) a pH dependent material, and

(ii) at least one pharmaceutical excipient.

2. The enteric coated tablet as defined in claim 1 wherein the rate controlling material is a wax or oil and has a melting point greater than 50°

C.

3. The enteric coated tablet as defined in claim 2 wherein the rate controlling wax or oil has melting point of about 55°

C. to about 150°

C.

4. The enteric coated tablet as defined in claim 2 wherein the rate controlling wax or oil has a melting point of about 70°

C. to about 100°

C.

5. The enteric coated tablet as defined in claim 1 wherein the diluent is water soluble.

6. The enteric coated tablet as defined in claim 1 wherein the diluent is water soluble and has a melting point below 100°

C.

7. The enteric coated tablet as defined in claim 6 wherein the diluent has a melting point of about 40°

C. to about 75°

C.

8. The enteric coated tablet as defined in claim 1 wherein the matrix drug core further comprises a lubricant.

9. The enteric coated tablet as defined in claim 8 wherein the lubricant has a melting point of about 40°

C. to about 100°

C.

10. The enteric coated tablet as defined in claim 8 wherein the lubricant has a melting point of about 45°

C. to about 85°

C.

11. The enteric coated tablet as defined in claim 1 wherein the pH dependent material is methacrylic acid copolymer Type B.

12. The enteric coated tablet as defined in claim 1 wherein the pharmaceutical excipient present in the enteric coating is a plasticizer.

13. The enteric coated tablet as defined in claim 1 wherein the pharmaceutical excipient present in the enteric coating is an anti-adherent.

14. The enteric coated tablet as defined in claim 1 wherein the soluble drug is an opioid.

15. The enteric coated tablet as defined in claim 14 wherein the opioid is selected from the group consisting of codeine phosphate, codeine sulfate, hydromorphone hydrochloride, morphine sulfate, oxycodone hydrochloride, oxymorphone hydrochloride, propoxycaine hydrochloride, propoxyphene hydrochloride and tramadol hydrochloride.

16. The enteric coated tablet as defined in claim 1 wherein the soluble drug is a pharmaceutically acceptable salt of tramadol.

17. The enteric coated tablet as defined in claim 16 wherein the drug is tramadol hydrochloride.

18. The enteric coated tablet as defined in claim 1 wherein the drug is freely soluble.

19. The enteric coated tablet as defined in claim 1 wherein the drug is very soluble.

20. The enteric coated tablet as defined in claim 1 wherein the drug is an anticonvulsant or antiepileptic.

21. The enteric coated tablet as defined in claims 20 wherein the anticonvulsant or antiepileptic is selected from the group consisting of gabapentin, levetiracetam, and sodium valproate.

22. An enteric coated tablet consisting essentially of:

(a) a matrix drug core consisting essentially of;

(j) 5-70 weight percent based upon the weight of the matrix core of a soluble drug;

(ii) 5-60 weight percent based upon the weight of the matrix core of a rate controlling, non-polymeric, water insoluble wax with a melting point of about 55°

C. to about 150°

C.;

(iii) 5-60 weight percent based upon the weight of the matrix core of a water soluble diluent with a melting point of about 40°

C. to about 75°

C.;

(iv) 0-10 weight percent based upon the weight of the matrix core of a lubricant; and

(v) 0-10 weight percent based upon the weight of the matrix core of a glidant; and

(b) an enteric coating surrounding the matrix drug core comprising;

(i) 25-90 weight percent based upon the weight of the enteric coating of a pH dependent material;

(ii) 0-25 weight percent based upon the weight of the enteric coating of a plasticizer; and

(iii) 0-50 weight percent based upon the weight of the enteric coating of an anti-adherent.

23. The enteric coated tablet as defined in claim 22 wherein the soluble drug is an opioid.

24. The enteric coated tablet as defined in claim 23 wherein the opioid is selected from the group consisting of codeine phosphate, codeine sulfate, hydromorphone hydrochloride, morphine sulfate, oxycodone hydrochloride, oxymorphone hydrochloride, propoxycaine hydrochloride, propoxyphene hydrochloride and tramadol hydrochloride.

25. The enteric coated tablet as defined in claim 22 wherein the soluble drug is a pharmaceutically acceptable salt of tramadol.

26. The enteric coated tablet as defined in claim 25 wherein the drug is tramadol hydrochloride.

27. An enteric coated tablet consisting essentially of:

(a) a matrix drug core consisting essentially of;

(k) 15-75 weight percent based upon the weight of the matrix core of a freely soluble or very soluble drug;

(ii) 5-60 weight percent based upon the weight of the matrix core of a rate controlling, non-polymeric, water insoluble wax with a melting point of about 55°

C. to about 150°

C.;

(iii) 0-10 weight percent based upon the weight of the matrix core diluent;

(iv) 0-10 weight percent based upon the weight of the matrix core of a lubricant; and

(v) 0-10 weight percent based upon the weight of the matrix core of a glidant; and

(b) an enteric coating surrounding the matrix drug core comprising;

(j) 25-90 weight percent based upon the weight of the enteric coating of a pH dependent material; and

(ii) 0-50 weight percent based upon the weight of the enteric coating of at least one pharmaceutical excipient.

28. The enteric coated tablet as defined in claim 27 wherein the drug is an anticonvulsant, an antiepileptic or an opioid.

29. The enteric coated tablet as defined in claim 28 wherein the drug is an anticonvulsant or antiepileptic selected from the group consisting of gabapentin, levetiracetam and sodium valproate.

30. The enteric coated tablet as defined in claim 27 wherein the diluent comprises 0 to about 5 weight percent based upon the weight of the matrix core.