Abuse-deterrent pharmaceutical compositions of opioids and other drugs

a technology of opioids and compositions, applied in the field of pharmaceutical compositions, can solve the problems of drug not being easily extracted from such a formulation, the formulation will require more than one step, and the potential for abus

US20080199530A1Inactive Publication Date: 2008-08-21COLLEGIUM PHARMA INC
53 Cites 33 Cited by

Patent Information

Authority / Receiving Office
US · United States
Patent Type
Applications(United States)
Current Assignee / Owner
Publication Date
2008-08-21
Estimated Expiration
Not applicable · inactive patent

Smart Images

  • Figure 1
    Figure 1
  • Figure 2
    Figure 2
Patent Text Reader

Abstract

An abuse-deterrent pharmaceutical composition has been developed to reduce the likelihood of improper administration of drugs, especially drugs such as opiods. In the preferred embodiment, a drug is modified to increase its lipophilicity. In preferred embodiments the modified drug is homogeneously dispersed within microparticles composed of a material that is either slowly soluble or not soluble in water. In some embodiments the drug containing microparticles or drug particles are coated with one or more coating layers, where at least one coating is water insoluble and preferably organic solvent insoluble, but enzymatically degradable by enzymes present in the human gastrointestinal tract. The abuse-deterrent composition retards the release of drug, even if the physical integrity of the formulation is compromised (for example, by chopping with a blade or crushing) and the resulting material is placed in water, snorted, or swallowed. However, when administered as directed, the drug is slowly released from the composition as the composition is broken down or dissolved gradually within the GI tract by a combination of enzymatic degradation, surfactant action of bile acids, and mechanical erosion.
Need to check novelty before this filing date? Find Prior Art

Description

[0001] This application claims priority to U.S. Ser. No. 60 / 393,876 filed Jul. 5, 2002 entitled “Abuse-Resistant Formulations of Oxycontin and Other Drugs” by Alexander M. Klibanov, Stephen L. Buchwald, Timothy M. Swager, and Whe-Yong Lo; U.S. Ser. No. 60 / 436,523 filed Dec. 23, 2002 by Alison B. Fleming, Roman V. Rariy, Alexander M. Klibanov, Whe-Yong Lo, and Jane Hirsh; U.S. Ser. No. 60 / 443,226 filed Jan. 28, 2003 by Jane Hirsh, Alison B. Fleming, Alexander M. Klibanov, and Whe-Yong Lo; U.S. Ser. No. 60 / 463,514 filed Apr. 15, 2003 by Jane C. Hirsh, Alison B. Fleming, Roman V. Rariy, Stephen L. Buchwald, and Timothy M. Swager; and U.S. Ser. No. 60 / 463,518 filed Apr. 15, 2003 by Jane C. Hirsh, Alison B. Fleming and Roman V. Rariy.BACKGROUND OF THE INVENTION

[0002] The present invention is generally in the field of pharmaceutical compositions, and specifically relates to compositions that are designed to reduce the potential for improper administration of drugs that are subject to abuse....

Examples

example 1

Preparation of Lipophilic Oxycodone Derivatives

[0071]A. Oxycodone Free Base

[0072]The free base of oxycodone was prepared from its hydrochloride salt by the following method: Oxycodone hydrochloride was dissolved in water and sodium carbonate was added in the amount required to neutralize hydrochloric acid. Methylene chloride was added in order to extract the formed oxycodone free base. The obtained organic layer was dried over sodium sulfate and methylene chloride was evaporated using rotary evaporator. The obtained oxycodone free base was purified by crystallization.

[0073]B. Zinc-Bis-Oxycodone

[0074]Zinc bis-oxycodone can be obtained in anhydrous media by reacting oxycodone free base with Zn(Et)2

[0075]C. Zinc Oxycodone Stearate

[0076]Zinc oxycodone stearate can be obtained in anhydrous media by reacting oxycodone free base with Zn(Et)(C18H35O2)

[0077]D. Zinc Oxycodone Di-Stearate

[0078]Zinc-oxycodone di-stearate can be obtained by co-melting Zn(C18H35O2)2 and oxycodone free base.

[0079...

example 2

Preparation of Drug Containing Microparticles

[0082]The free base, salts or complexes from Example 1 are added to molten hydrogenated vegetable oil, mixed, extruded and spheronized to form drug containing microparticles.

example 3

Preparation of Coated Drug Containing Microparticles

[0083]The drug-containing particles from Example 2 are spray coated with zein in a fluidized bed apparatus.