Immediate/delayed drug delivery

Patent metadata

Field	Value
Publication number	US-10137091-B2
Application number	US-201113582940-A
Country	US
Kind code	B2
Filing date	Mar 4, 2011
Priority date	Mar 5, 2010
Publication date	Nov 27, 2018
Grant date	Nov 27, 2018

Abstract

In one aspect, the present invention is concerned with a treatment where it is desired that an active agent is designed to be released immediately following administration and again at a time point some time after administration of the active agent. The present invention is particularly suited to administering an agent which may be released before sleep and while a subject is sleeping. As well as treating certain conditions by a particular regime, the invention also provides novel formulations for an immediate, followed by a delayed release of drug.

First claim

The invention claimed is:

1. A press-coated tablet formulation for an immediate, followed by a delayed release of an active agent, the tablet comprising:
(a) a core comprising an active agent together with an excipient(s); and
(b) a delayed release layer surrounding the core and comprising a wax and a low substituted hydroxypropyl cellulose in a ratio of 40:60 to 60:40 w/w; wherein the delayed release layer substantially delays release of the active agent within the core for between 3-8 hours after administration of the tablet to a subject and thereafter a pulsed release of the active agent from the core occurs, such that at least 70% of the active agent in the core is released within 5-45 minutes and wherein the low substituted hydroxypropyl cellulose is micronized with a mean particle diameter of 20 mm and has a molecular weight of 115,000 and a hydroxypropyl cellulose content of 8%; and
(c) a top-coating layer comprising a portion of an active agent together with one or more excipients wherein a substantially immediate pulsed release of the active agent occurs following administration to the subject of the tablet;
wherein the active agent in the core and on the top-coating layer is an NSAID.

2. The press-coated tablet according to claim 1 further comprising an amount of an active agent, which is the same or different to the active agent in the core and/or top-coating layer, in the delayed release layer.

3. The press-coated tablet according to claim 1 wherein the wax is selected from the group consisting of beeswax, carnuba wax, microcrystalline wax, hydrogenated castor oil, and a glyceryl ester.

4. The press-coated tablet according to claim 3 wherein the glyceryl ester is glycerol behenate.

5. The press-coated tablet according to claim 1 wherein the wax and the low substituted hydroxypropyl cellulose are present in a ratio of 45:55 to 55:45 w/w.

6. The press-coated tablet according to claim 5 wherein the wax and the low substituted hydroxypropyl cellulose are present in a ratio of 50:50 w/w ratio and wherein the wax is glycerol behenate.

7. A method of alleviating pain and/or inflammation, the method comprising administering a press-coated tablet according to claim 1 .

8. The method according to claim 7 wherein the NSAID is diclofenac.

9. The method according to claim 7 wherein delayed release of the NSAID is achieved by providing a press-coated tablet comprising a delayed release layer surrounding a core comprising the NSAID agent.

10. The method according to claim 9 wherein the delayed release layer comprises a wax and a low substituted hydroxypropyl cellulose, wherein the low substituted hydroxpropyl cellulose is micronized with a mean particle diameter of 20 mm and has a molecular weight of 115,000 and a hydroxypropyl cellulose content of 8%.

11. The press-coated tablet according to claim 1 , wherein the active agent is diclofenac.

12. A press-coated tablet formulation for an immediate, followed by a delayed release of an NSAID active agent, the tablet comprising:
(a) a core comprising an active agent together with an excipient(s); and
(b) a delayed release layer surrounding the core and comprising a wax and a low substituted hydroxypropyl cellulose in a ratio of 40:60 to 60:40 w/w; wherein the delayed release layer substantially delays release of the active agent within the core for between 3-8 hours, and thereafter a pulsed release of the active agent from the core occurs, such that at least 70% of the active agent in the core is released within 5-45 minutes; wherein the low substituted hydroxypropyl cellulose is micronized with a mean particle diameter of 20 mm and has a molecular weight of 115,000 and a hydroxypropyl cellulose content of 8%; and
(c) a top-coating layer comprising a portion of an active agent together with one or more excipients wherein a substantially immediate pulsed release of the active agent occurs following administration to the subject of the tablet; wherein said release is measured in 900 ml of 0.01M sodium phosphate buffer at pH 7, at 37° C. as determined by UV analysis at 248 nm;
wherein the active agent in the core and on the top-coating layer is an NSAID.

13. The press-coated tablet according to claim 12 further comprising an amount of an active agent, which is the same or different to the active agent in the core and/or top-coating layer, in the delayed release layer.

Assignees

• Mullen Alexander
• Stevens Howard
• Eccleston Sarah
• Univ Strathclyde

Inventors

• Mullen Alexander
• Stevens Howard
• Eccleston Sarah

Classifications

• A61P9/06

  Antiarrhythmics · CPC title

• A61P37/02

  Immunomodulators · CPC title

• A61P9/10

  for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis · CPC title

• A61P7/00

  Drugs for disorders of the blood or the extracellular fluid · CPC title

• A61P7/02

  Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors · CPC title