Pharmaceutical composition of doxycycline with reduced food effect

Patent metadata

Field	Value
Publication number	US-2016008379-A1
Application number	US-201514821263-A
Country	US
Kind code	A1
Filing date	Aug 7, 2015
Priority date	Jul 9, 2014
Publication date	Jan 14, 2016
Grant date	—

Abstract

The present invention relates to a once daily tablet comprising doxycycline at sub-antibiotic dose and one or more pharmaceutically acceptable excipients, wherein the tablet 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 tablet with or without food. A process of preparing the tablet is also provided.

First claim

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

2 . (canceled)

3 . The once daily tablet according to claim 1 , wherein the once daily tablet 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.

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

5 . The once daily tablet according to claim 3 , wherein the immediate-release portion contains 34 mg of doxycycline and the controlled-release portion contains 6 mg of doxycycline.

6 . The once daily tablet according to claim 3 , wherein the immediate-release portion contains 75% of doxycycline and the controlled-release portion contains 25% of doxycycline.

7 . The once daily tablet according to claim 3 , wherein the immediate-release portion contains 30 mg of doxycycline and the controlled-release portion contains 10 mg of doxycycline.

8 . The once daily tablet according to claim 3 , wherein the immediate-release portion contains 66% of doxycycline and the controlled-release portion contains 34% of doxycycline.

9 . The once daily tablet according to claim 3 , wherein the immediate-release portion contains 26.4 mg of doxycycline and the controlled-release portion contains 13.6 mg of doxycycline.

10 . The once daily tablet according to claim 3 , wherein the immediate-release portion contains 65% of doxycycline and the controlled-release portion contains 35% of doxycycline.

11 . The once daily tablet according to claim 3 , wherein the immediate-release portion contains 26 mg of doxycycline and the controlled-release portion contains 14 mg of doxycycline.

12 . The once daily tablet according to claim 3 , wherein the immediate-release portion contains 60% of doxycycline and the controlled-release portion contains 40% of doxycycline.

13 . The once daily tablet according to claim 3 , wherein the immediate-release portion contains 24 mg of doxycycline and the controlled-release portion contains 16 mg of doxycycline.

14 - 61 . (canceled)

62 . A process for the preparation of a once daily tablet comprising doxycycline at a sub-antibiotic dose and one or more pharmaceutically acceptable excipients, wherein the tablet exhibits a reduced food effect, wherein the process comprises:
a) preparing an immediate release portion comprising doxycycline and one or more pharmaceutically acceptable excipients; 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 the controlled-release portion into a tablet.

63 . The process according to claim 62 , wherein the tablet is a bilayered tablet.

64 . The process according to claim 62 , wherein the tablet comprises only an immediate-release portion.

65 . The process according to claim 62 , wherein the tablet comprises only a controlled-release portion.

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

67 - 68 . (canceled)

Assignees

• Sun Pharmaceutical Ind Ltd

Inventors

• Jami Dileep
• Singh Ravinder
• Fanda Anuj Kumar
• Singh Romi Barat

Classifications

• A61K31/65 Primary

  Tetracyclines · 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

• A61K9/2081

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

• A61K9/2054

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