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Temperature sensing in situ gel rubber formulations capable of being injected, preparation method and uses thereof

An in-situ gel and preparation technology, which can be applied to medical preparations without active ingredients, medical preparations containing active ingredients, pharmaceutical formulas, etc., can solve the problems of paclitaxel injection application limitation, large toxic side effects, vasodilation, etc., To achieve the effect of improving medication compliance, high practicability, and maintaining long-term effects

Inactive Publication Date: 2009-01-14
PEKING UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Cremophor EL has been proven to have relatively large toxic and side effects. After intravenous administration to dogs, it will cause vasodilation, dyspnea, lethargy, hypotension and death. Moreover, the solvent has hypersensitivity to blood vessels, which makes paclitaxel injection available in clinical practice. subject to many restrictions
Similarly, docetaxel (Taxotere ) Injection contains polysorbate-80 (Tween-80) as a solubilizer, and intravenous injection may also produce hemolysis and other reactions

Method used

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  • Temperature sensing in situ gel rubber formulations capable of being injected, preparation method and uses thereof
  • Temperature sensing in situ gel rubber formulations capable of being injected, preparation method and uses thereof
  • Temperature sensing in situ gel rubber formulations capable of being injected, preparation method and uses thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Take an appropriate amount of Pluronic F127, so that the final concentration is controlled at 20 wt %; add an appropriate amount of Tween 80, so that the molar ratio of it to F127 is 6:1. The final concentration of docetaxel (DTX) added was 2 mg / ml, the carrier material and the drug were placed in a vial, an appropriate proportion of distilled water was added, and magnetically stirred overnight (12 h) in an ice-bathed beaker at 4°C. A translucent drug-loaded sol system is formed.

Embodiment 2

[0035] Take an appropriate amount of Pluronic F127 to make the final concentration 20% by weight; add an appropriate amount of Tween 80 to make the final concentration 15%. The final concentration of paclitaxel (PTX) added was 2 mg / ml; the polymer materials and drugs were placed in vials, an appropriate proportion of distilled water was added, and magnetically stirred overnight (12 h) in an ice-bathed beaker at 4°C. A translucent drug-loaded sol system is formed.

Embodiment 3

[0037] Take an appropriate amount of Pluronic F127 to make the final concentration 20% by weight; add an appropriate amount of Tween 80 to make the final concentration 10%. The final concentration of 9-nitrocamptothecin (9-NC) added was 4 mg / ml; polymer materials and drugs were placed in vials, an appropriate proportion of distilled water was added, and magnetically stirred in an ice-bathed beaker at 4°C overnight (12h ). A translucent drug-loaded sol system is formed.

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PUM

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Abstract

The invention relates to injectable temperature sensitive in situ gel preparation and a preparation method as well as an application thereof. The components of the preparation of the invention comprise 0.01 percent to 10 percent of anticancer drugs, 15 percent to 25 percent of pluronic F127, 0.01 percent to 20 percent tween and 45 percent to 84.98 percent of water or buffer solution.

Description

Technical field: [0001] The invention relates to an injectable pharmaceutical preparation and a preparation method thereof, in particular to an injectable temperature-sensitive in-situ gel preparation, their preparation method and their application in clinical tumor treatment. Background technique: [0002] In recent years, the sustained and controlled release injection drug delivery system has attracted the attention of many pharmaceutical researchers and has become a research hotspot in injection drug delivery. Emulsions, liposomes, biodegradable microspheres, and micelles have all been used in the research of injectable drug delivery systems, but they all have stability problems to varying degrees. In addition, liposomes are eliminated quickly in the body and have problems such as sterilization and low drug encapsulation efficiency. The process required to prepare sterile and reproducible microspheres is relatively complicated, and microspheres and micelles have problems ...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K45/00A61K47/34A61K31/704A61K31/337A61K31/4745A61K31/475A61K33/24A61P35/00A61K47/26
Inventor 张强王坚成张烜杨杨刘瑜
Owner PEKING UNIV
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