Pharmaceutical composition of doxycycline with reduced food effect

Patent metadata

Field	Value
Publication number	US-9566287-B2
Application number	US-201615013097-A
Country	US
Kind code	B2
Filing date	Feb 2, 2016
Priority date	Jul 9, 2014
Publication date	Feb 14, 2017
Grant date	Feb 14, 2017

Abstract

The present invention relates to a once daily pharmaceutical composition comprising doxycycline and one or more pharmaceutically acceptable excipients, wherein the pharmaceutical composition exhibits a reduced food effect. The invention further provides a method of treatment of rosacea by administering to a person in need thereof the doxycycline pharmaceutical composition with or without food. A process of preparing such pharmaceutical composition is also provided.

First claim

We claim:

1. A once daily pharmaceutical composition comprising doxycycline and one or more pharmaceutically acceptable excipients, wherein the pharmaceutical composition exhibits a reduced food effect such that the food effect on C max is less than 40% and/or AUC 0-t is less than 20% as compared to when the pharmaceutical composition is administered in a fasted state.

2. The once daily pharmaceutical composition according to claim 1 , wherein the once daily pharmaceutical composition comprises (i) 50% to 99% of doxycycline and one or more pharmaceutically acceptable excipients as an immediate-release portion; and (ii) 1% to 50% of doxycycline, a controlled-release polymer, and one or more pharmaceutically acceptable excipients as a controlled-release portion.

3. The once daily pharmaceutical composition according to claim 2 , wherein the immediate-release portion contains 85% of doxycycline and the controlled-release portion contains 15% of doxycycline.

4. The once daily pharmaceutical composition according to claim 2 , wherein the immediate-release portion contains 34 mg of doxycycline and the controlled-release portion contains 6 mg of doxycycline.

5. The once daily pharmaceutical composition according to claim 2 , wherein the immediate-release portion 75% of doxycycline and the controlled-release portion contains 25% of doxycycline.

6. The once daily pharmaceutical composition according to claim 2 , wherein the immediate-release portion contains 30 mg of doxycycline and the controlled-release portion contains 10 mg of doxycycline.

7. The once daily pharmaceutical composition according to claim 2 , wherein the immediate-release portion contains 66% of doxycycline and the controlled-release portion contains 34% of doxycycline.

8. The once daily pharmaceutical composition according to claim 2 , wherein the immediate-release portion contains 26.4 mg of doxycycline and the controlled-release portion contains 13.6 mg of doxycycline.

9. The once daily pharmaceutical composition according to claim 2 , wherein the immediate-release portion contains 65% of doxycycline and the controlled-release portion contains 35% of doxycycline.

10. The once daily pharmaceutical composition according to claim 2 , wherein the immediate-release portion contains 26 mg of doxycycline and the controlled-release portion contains 14 mg of doxycycline.

11. The once daily pharmaceutical composition according to claim 2 , wherein the immediate-release portion contains 60% of doxycycline and the controlled-release portion contains 40% of doxycycline.

12. The once daily pharmaceutical composition according to claim 2 , wherein the immediate-release portion contains 24 mg of doxycycline and the controlled-release portion contains 16 mg of doxycycline.

13. The once daily pharmaceutical composition according to claim 1 , wherein the pharmaceutical composition is an immediate-release composition.

14. The once daily pharmaceutical composition according to claim 1 , wherein the pharmaceutical composition is a controlled-release composition.

15. The once daily pharmaceutical composition according to claim 1 , wherein the pharmaceutical composition is a capsule or a tablet.

16. The once daily pharmaceutical composition according to claim 1 , wherein the pharmaceutical composition is in the form of pellets, beads, beadlets, granules, spheres or spheroids, minitablets, particles, or powders.

17. The once daily pharmaceutical composition according to claim 15 , wherein the pharmaceutical composition is a capsule filled with one or more of pellets, beads, beadlets, granules, spheres or spheroids, minitablets, particles, or powders.

18. A process for the preparation of a once daily pharmaceutical composition comprising doxycycline and one or more pharmaceutically acceptable excipients, wherein the pharmaceutical composition exhibits a reduced food effect, and wherein the process comprises:
a) preparing an immediate-release portion comprising doxycycline and one or more pharmaceutically acceptable excipients; and/or
b) preparing a controlled-release portion comprising doxycycline, a controlled-release polymer, and one or more pharmaceutically acceptable excipients; and
c) formulating the immediate-release portion and/or the controlled-release portion into a pharmaceutical composition.

19. The process according to claim 18 , wherein the pharmaceutical composition comprises only the immediate-release portion.

20. The process according to claim 18 , wherein the pharmaceutical composition comprises only the controlled-release portion.

21. A method of treating rosacea by administering to a person in need thereof a once daily pharmaceutical composition comprising doxycycline and one or more pharmaceutically acceptable excipients, wherein the pharmaceutical composition exhibits a reduced food effect such that the food effect on C max is less than 40% and/or AUC 0-t is less than 20% as compared to when the pharmaceutical composition is administered in a fasted state.

Assignees

• Sun Pharmaceutical Ind Ltd

Inventors

• Sharma Ravish Kumar
• Metia Pulak Kumar
• Singh Ravinder
• Shear Rajesh Srikrishan
• Fanda Anuj Kumar
• Jain Satish Kumar
• Singh Romi Barat
• Pappu Swarna
• Konatham Prabhakar
• Katikaneni Pruthvipathy
• Jami Dileep

Classifications

• A61K31/65 Primary

  Tetracyclines · CPC title

• A61K9/2081

  with microcapsules or coated microparticles according to A61K9/50 · CPC title

• A61K9/2027

  obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates · CPC title

• A61K9/209

  containing drug in at least two layers or in the core and in at least one outer layer · CPC title

• A61K9/2054

  Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose · CPC title