PLGA Gemcitabine sustained-release microsphere and its preparing method

A technology of gemcitabine and slow-release microspheres, which is applied in the field of pharmacy, can solve the problems of gemcitabine with short half-life, serious adverse reactions, and short maintenance time, and achieve good local curative effect, avoid first-pass effect, and long-lasting effect

Inactive Publication Date: 2008-04-16
CANCER INST & HOSPITAL CHINESE ACADEMY OF MEDICAL SCI +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Gemcitabine has a short half-life, systemic administration, low drug concentration at the tumor site, short maintenance time, poor curative effect, and high systemic drug concentration, serious adverse reactions

Method used

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  • PLGA Gemcitabine sustained-release microsphere and its preparing method
  • PLGA Gemcitabine sustained-release microsphere and its preparing method
  • PLGA Gemcitabine sustained-release microsphere and its preparing method

Examples

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Effect test

Embodiment 1

[0028] Embodiment 1: Preparation of PLGA gemcitabine sustained-release microspheres

[0029] Use an ultrafine grinder to make gemcitabine into a fine powder with a diameter of less than 20 μm; dissolve 4 g of PLGA [90:10 (molecular ratio of lactic acid to glycolic acid)] in 40 mL of acetone to make a PLGA acetone solution, add 0.4 g of fine powder of gemcitabine, and mix uniform, spray-dried under vacuum, collected microspheres, and sieved to obtain PLGA gemcitabine sustained-release microspheres (A) with a particle size of less than 100 μm.

Embodiment 2

[0030] Embodiment 2: Preparation of PLGA gemcitabine sustained-release microspheres

[0031] Dissolve 4 g of PLGA (80:20) in 40 mL of tetrahydrofuran to prepare a PLGA tetrahydrofuran solution, add 0.8 g of gemcitabine fine powder, mix well, spray dry under vacuum, collect microspheres, and sieve to obtain PLGA gemcitabine sustained-release microspheres with a particle size of less than 100 μm. ball (B).

Embodiment 3

[0032] Embodiment 3: Preparation of PLGA gemcitabine sustained-release microspheres

[0033] Dissolve 4 g of PLGA in 40 mL of dichloromethane to make PLGA dichloromethane solution, add 1.2 g of gemcitabine fine powder, mix well, spray dry under vacuum, collect microspheres, and sieve to obtain PLGA gemcitabine sustained-release microspheres with a particle size of less than 100 μm (C).

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Abstract

A PLGA gemcitabine slow release microball is disclosed in the present invention belonging to pharmaceutical field. The PLGA gemcitabine slow release microball is prepared by supplementary polylactic acid-glycolic acid and raw material medicine gemcitabine with the weight ratio of 95 :5 to 35 :65. The present invention has the advantages that: preparing gemcitabine and polylactic acid-glycolic acid into slow release microball, directly sendint to tumor part by syringe to execute regional slow release chemotherapy, gemcitabine are released slowly, the tumor part has high medicine concentration, long duration, strong action intensity, big killing force to tumor cell, thereby can improve curative effect to tumor; medicine are centralized to act on local, whole body has little medicine amount, adverse response is minimal. After medicine are released, polylactic acid-glycolic acid start to degradate as lactic acid and glycolic acid, further degradate as carbon dioxide and water, no effect to human body.

Description

technical field [0001] The present invention relates to an injectable PLGA (polylactic acid-glycolic acid) gemcitabine sustained-release microsphere and a preparation method thereof, more specifically, it is prepared by using biodegradable polylactic acid-glycolic acid as an auxiliary material and gemcitabine as an effective drug An injectable slow-release microsphere and a preparation method thereof belong to the field of pharmacy. Background technique [0002] Polylactic acid-glycolic acid is a medical polymer material with good biocompatibility, biodegradability, good safety, and excellent physical and chemical properties. It is used as an auxiliary material for drug sustained-release preparations and medical materials in the human body; Afterwards, it is first degraded into lactic acid and glycolic acid in the human body, and then further degraded into carbon dioxide and water to be excreted from the body, which is harmless to the human body. The degradation rate of pol...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K9/50A61K31/7068A61K47/34A61P35/00
Inventor 赵平王世亮马洁丁满志李井泉
Owner CANCER INST & HOSPITAL CHINESE ACADEMY OF MEDICAL SCI
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