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Conveniently implantable sustained release drug compositions

Inactive Publication Date: 2008-02-14
RAMSCOR
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0008] An object of the present invention provides for economical, practical, and efficient drug delivery systems. According to the present invention, this drug delivery system is produced easily, delivered easily to the site of indication, and is both biocompatible and biodegradable. More specifically, the formulations of the present invention provide for novel therapies that are easily manipulated and injected or implanted by qualified medical practitioners. The formulations deliver therapeutic and non-toxic levels of active agents over the desired extended time frame, primarily at the site of implantation. The formulations are both biocompatible and biodegradable, and disappear harmlessly after delivering active agent to the desired site.

Problems solved by technology

The formulations are both biocompatible and biodegradable, and disappear harmlessly after delivering active agent to the desired site.

Method used

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  • Conveniently implantable sustained release drug compositions
  • Conveniently implantable sustained release drug compositions
  • Conveniently implantable sustained release drug compositions

Examples

Experimental program
Comparison scheme
Effect test

example 1

Preparation of a Poly(1,3-propanediol carbonate) I from 1,3-propanediol at 65° C. and 96 hours

[0240] To 23.6 g (0.2 mole) diethyl carbonate (b.p. 128° C.) was added 15.2 g (0.2 mole) 1,3-propanediol containing 0.05 g (1.25 mmole) of metallic Na to give two liquid phases. These reactants were placed in an open container in a 65° C. oven and were shaken occasionally. After 12 hours, the reactants were a homogeneous solution weighing 38.0 g. The theoretical weight for the loss of 0.4 moles (18.4 g) of ethanol in a complete reaction would be 20.4 g. The heating and occasional shaking were continued to give 27.0 g at 24 hours, 23.2 g at 48 hours, 21.4 g at 72 hours, and 17.4 g at 96 hours. The product oil was washed with 15 ml 5% aqueous acetic acid to two phases. The top phase was the water soluble phase. The 10.5 ml bottom phase was washed with 15 ml water to give 7.5 ml of a poly(1,3-propylene glycol carbonate) oligomer as a water-insoluble oil.

example 2

Preparation of Poly(1,3-propanediol carbonate) II from 1,3-propanediol at 110-150° C. and 26 hours.

[0241] A mixture of 76 g (1.0 mole) 1,3-propanediol containing 0.1 g metallic Na (2.5 mmole) and 118 g (1.0 mole) diethyl carbonate was heated at 110° C. As soon as the reactants reached 60° C. they formed a homogeneous solution. After heating 8 hours, the reactants had lost 48 g (52% of theoretical amount of ethanol). The temperature was then raised to 150° C. After 10 hours, the reactants lost another 46 g. A drop of this product completely dissolved in water. The resultant 97 g of oil was mixed with 6 g (0.05 moles) diethyl carbonate and the resultant solution was heated with occasional stirring at 150° C.

[0242] After 8 hours, the resultant syrup was found to be partially insoluble in water. The product was washed with 100 ml 5% aqueous acetic acid followed by four washings with 100 ml portions of water to give 46.1 g slightly yellow viscous oil (46.1 / 102=45% yield).

example 3

Preparation of a Poly(di-1,2-propylene glycol carbonate) from di-1,2-propylene glycol

[0243] To 590 g (0.5 moles) diethyl carbonate was added 67.0 g (0.5 moles) di-1,2-propylene glycol which had been reacted with 0.02 g Na to form a homogeneous solution. The reactants were placed in an open flask at 100° C. After 12 hours, the solution lost 23.4 g (about 50% of the theoretical 46 g ethanol). After another 15 hours at 150° C. the reactants had lost a total of 53.2 g to give a syrup that was partially insoluble in water. The product was washed with 100 ml 5% aqueous acetic acid followed by four washing with 100 ml portions of water to give 25.2 g colorless viscous, water insoluble liquid poly(di-1,2-propylene glycol carbonate) oligomer.

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Abstract

This invention provides for biocompatible and biodegradable syringeable liquid, implantable solid, and injectable gel pharmaceutical formulations useful for the treatment of systemic and local disease states.

Description

RELATED APPLICATIONS [0001] This application is related to and claims the benefit under 35 U.S.C. § 119(e) of U.S. Patent Application Ser. No. 60 / 831,991, filed Jul. 19, 2006, and is a continuation-in-part and claims the benefit under 35 U.S.C. § 120 of U.S. patent application Ser. No. 11 / 236,426, filed Sep. 27, 2005, which is related to and claims the benefit under 35 U.S.C. § 119(e) of U.S. Patent Applications Ser. No. 60 / 709,665, filed Aug. 19, 2005, and Ser. No. 60 / 614,484, filed Oct. 1, 2004, each entitled Conveniently Implantable Sustained Release Drug Compositions, by Vernon G. Wong and Louis L. Wood. Each of the foregoing applications is incorporated in its entirety herein.FIELD OF THE INVENTION [0002] This invention provides for biocompatible and biodegradable syringeable liquid, implantable solid, and injectable gel pharmaceutical formulations useful for the treatment of systemic and local diseases. BACKGROUND OF THE INVENTION [0003] Present modes of drug delivery such as ...

Claims

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Application Information

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IPC IPC(8): A61F2/00A61K31/56
CPCA61K9/0051A61K9/0024A61K31/355A61K31/496A61K31/573A61K38/13A61P27/06A61P29/00A61P31/00A61P37/06A61P39/06A61K9/0048A61K47/06A61K9/0019A61K47/14
Inventor WONG, VERNON G.WOOD, LOUIS L.
Owner RAMSCOR
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