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Compound paclitaxel preparation containing phospholipid dispersant and preparation method thereof

A compound paclitaxel phospholipid and paclitaxel technology, applied in the field of medicine, can solve the problems of low solubility of paclitaxel, affecting the clinical application of compound paclitaxel oral preparation, poor oral administration bioavailability and the like

Inactive Publication Date: 2009-02-11
黄成安
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Glycyrrhizic acid and ginsenoside in the existing compound paclitaxel preparations are easily absorbed by the human body no matter they are taken orally or injected, but the solubility of paclitaxel in water is very small, almost insoluble in water (<0.004mg / ml), and almost insoluble in the gastrointestinal tract. It is absorbed, so the bioavailability of oral administration is poor, which affects the clinical application of compound paclitaxel oral preparations

Method used

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  • Compound paclitaxel preparation containing phospholipid dispersant and preparation method thereof

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Comparison scheme
Effect test

Embodiment 1

[0021] The preparation of embodiment 1 compound paclitaxel phospholipid dispersion tablet

[0022] Weigh 20g of paclitaxel, 77g of glycyrrhizinic acid, 3g of ginsenoside Rd, and 250g of soybean lecithin for oral administration, add 1000mL of absolute ethanol and reflux for 45 minutes under heating and stirring; and concentrate under reduced pressure under vacuum pressure -0.09MPa and heating in a 60°C water bath to 150mL; then the concentrated solution is dried under reduced pressure at -0.05MPa and 40°C to obtain the compound paclitaxel phospholipid dispersion; add lactose to the prepared compound paclitaxel phospholipid dispersion 500g, talcum powder 10g, sodium carboxymethyl starch 15g, mix uniformly, it is prepared into tablet according to conventional tablet preparation process.

Embodiment 2

[0023] Example 2 Preparation of Compound Paclitaxel Phospholipid Dispersion Capsules

[0024] Weigh 12g of paclitaxel, 84g of glycyrrhizinic acid, 4g of ginsenoside Re, and 7000g of oral egg yolk lecithin, add 70000mL of ethyl acetate and reflux for 5 hours under heating and stirring; concentrate under reduced pressure under vacuum pressure -0.07MPa, 55℃ water bath heating to 550mL; then the concentrated solution was dried continuously at 35°C by fluidized bed drying method to obtain the compound paclitaxel phospholipid dispersion; 60g of starch and 37g of magnesium stearate were added to the prepared compound paclitaxel phospholipid dispersion, Mix evenly, directly pack it into capsules, and prepare into capsules. The preparation of embodiment 3 compound paclitaxel phospholipid dispersion pills

[0025] Weigh paclitaxel 10g, glycyrrhizic acid 85g, ginsenoside Rb 1 4g, Ginsenoside Rb 21g, soybean lecithin for injection 4000g, add 4000mL chloroform and reflux for 3 hours un...

Embodiment 4

[0026] Example 4 Preparation of compound paclitaxel phospholipid dispersion granules

[0027] Weigh paclitaxel 15g, glycyrrhizic acid 84g, ginsenoside Rc1g, oral soybean lecithin 210g, phosphatidylcholine 55g, add 12000mL methanol, 6550mL isopropanol and reflux for 4.2 hours under heating and stirring; Concentrate under reduced pressure to 7000mL under heating in a water bath at 82°C; then dry the concentrate with a fluidized bed and continue drying at 55°C to obtain the compound paclitaxel phospholipid dispersion; add 5500 g of lactose to the prepared compound paclitaxel phospholipid dispersion 1. Starch 500g, micropowder silica gel 125g, mix evenly, prepare it into granules according to the conventional granule preparation process.

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Abstract

The invention relates to a compound paclitaxel preparation containing phospholipid dispersing substance and its preparation method. The active ingredient of the preparation is compound paclitaxel phospholipid dispersing substance composed of paclitaxel, glycyrrhizic acid, ginsenoside, and phospholipid. It is prepared by heating paclitaxel, glycyrrhizic acid, ginsenoside, and phospholipid in organic solvent under reflux, concentrating, and drying. The preparation can be made into different kinds of oral medicament form preparation containing phospholipid dispersing substance. Animal experiment proved that compound paclitaxel phospholipid dispersing substance improves bioavailability of paclitaxel. The preparation makes full use of paclitaxel, ginsenoside, and glycyrrhizic acid can control and eliminate tumor, and recover resistibility of patients. The preparation has the advantages of reduced adverse side effect, high performance, and high safety.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a compound paclitaxel preparation containing a phospholipid dispersion and a preparation method thereof. Background technique [0002] Traditional Chinese medicine believes that tumors are a local reaction to systemic diseases, and the pathogenesis itself is deficiency in origin and excess in superficiality. In clinical practice, dialectical treatment is used as the guiding principle, and the treatment emphasizes the support of righteousness, mainly to stabilize the tumor, improve clinical symptoms, and improve survival. Quality, prolong survival, so as to achieve the purpose of "survival with tumor". In tumor treatment, the application of traditional Chinese medicine combined with tumor radiotherapy and chemotherapy can reduce the toxicity of radiotherapy and chemotherapy, improve the completion rate of radiotherapy and chemotherapy, and increase the curative effect; when used ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/337A61K9/14A61K9/16A61K9/20A61K9/48A61K31/704A61K47/24A61P35/00
Inventor 黄成安
Owner 黄成安
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