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Biodegradable triblock copolymers as solubilizing agents for drugs and method of use thereof

A technology for block copolymers and polyester degradation, which is used in drug delivery, pharmaceutical formulations, medical preparations of non-active ingredients, etc.

Inactive Publication Date: 2007-01-03
马克罗梅德股份公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] Even with some limited success, these PLA, PGA, and PLGA polymers present several problems as drug carriers that are associated with their physicochemical properties and concomitant methods of fabrication

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0055] Synthesis of ABA-Type Triblock Copolymer PLGA-PEG-PLGA by Ring-Opening Copolymerization

[0056] PEG (Mw=1000; 100 g) was dried under vacuum (1 mmHg) at 100° C. for 5 hours. D,L-Lactide (86.72 grams) and glycolide (23.28 grams) were added to the flask and heated to 130°C to provide a homogeneous solution. Polymerization was initiated by adding 40 mg of stannous octoate to the reaction mixture. After maintaining the reaction at 155°C for 5 hours, the reaction was terminated and the flask was cooled to room temperature. Unreacted lactide and glycolide were removed by vacuum distillation at 130°C for 2 hours. The crude copolymer residue is a highly viscous liquid. The copolymer was purified twice by dissolving the copolymer in water to give a 25% solution and allowing the solution to stir overnight at room temperature, then raising the temperature of the solution to 70°C to precipitate the polymer. Decant the supernatant from the flask. Any remaining water was removed...

Embodiment 2

[0058] Following the basic procedure outlined in Example 1, other triblock copolymers were synthesized using PEG (Mw = 600, 1000, or 1450) at various lactide and / or glycolide contents. The properties of these triblock copolymers are listed in the table below:

[0059] project

[0060] Note that all block copolymers listed in the table above have the property of enhancing the solubility of drugs and especially hydrophobic drugs. Therefore, both PLGA-PEG-PLGA and PLA-PEG-PLA triblock copolymers were prepared and the results are summarized in this example. The copolymer forms a polymer solution when mixed with an aqueous liquid and remains a free flowing liquid.

Embodiment 3

[0062] In this example, the solubility-enhancing properties of the aqueous solution of the ABA triblock copolymer of Example 1 will be described. A polymer solution containing 23% by weight of the copolymer was prepared in water, paclitaxel was added to the solution and the mixture was stirred for about 20 minutes. The mixture was then filtered through a 0.2 μm filter to give a clear solution which was analyzed for paclitaxel content and thus water solubility. The water solubility of paclitaxel increased from approximately 5 μg / ml in pure water to over 25 mg / ml in a 23% by weight aqueous solution of the triblock copolymer. The solubility of paclitaxel was increased at least 5000-fold. The ABA triblock copolymer composition forms a paclitaxel-containing polymer solution when mixed with an aqueous liquid and remains a free-flowing liquid.

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PUM

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Abstract

The invention discloses a biodegradable ABA-type or BAB-type tri-block copolymer, which can solubilize drugs, especially hydrophobic drugs, in a hydrophilic environment at a functional concentration so as to Solutions are formed at temperatures associated with parenteral and especially intravenous administration and all other routes of administration that benefit from aqueous pharmaceutical solutions. The copolymer is composed of about 50.1 to 65% by weight of a biodegradable hydrophobic A polymer block comprising a biodegradable polyester, and about 35 to 49.9% by weight of a biodegradable polymer comprising polyethylene glycol (PEG). Composed of degradable hydrophobic B polymer blocks, and wherein the triblock copolymer has a weight average molecular weight between about 1500 and 3099 Daltons.

Description

field of invention [0001] The present invention relates to biodegradable triblock copolymers having a high weight percentage (at least 50%) of hydrophobic blocks and their use for solubilizing hydrophobic drugs in a hydrophilic environment and low molecular weight (1500-3099 Daltons). The triblock copolymers of the present invention exist in pure form as highly viscous liquids and form solutions in aqueous environments at body temperature and are suitable for parenteral and especially intravenous (I.V.) delivery. Therefore, the triblock copolymer of the present invention can be used as a solubilizer for drugs that are substantially insoluble in water, or as a solubilizer for drugs whose water solubility needs to be increased. Background of the invention [0002] Many important drugs have limited solubility in water, especially hydrophobic drugs. In order to obtain the full intended therapeutic effect of these drugs, it is often necessary to administer the drug to the patie...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K9/08A61K47/34
CPCA61K9/08A61K47/34A61K38/13A61K31/337
Inventor 史中G·曾特纳朴爱知K·D·福韦尔斯
Owner 马克罗梅德股份公司
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