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Preparation of paclitaxel, and its preparing method

A technology for paclitaxel and paclitaxel phospholipids, applied in the field of medicine, can solve the problems affecting the development and clinical application of paclitaxel oral preparations, poor oral administration bioavailability, low solubility and the like

Inactive Publication Date: 2007-07-25
黄成安
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Because the solubility of paclitaxel in water is very small, it is almost insoluble in water (<0.004mg / ml), and it is hardly absorbed in the gastrointestinal tract, so the bioavailability of oral administration is poor, thus affecting the development and clinical application of paclitaxel oral preparations

Method used

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  • Preparation of paclitaxel, and its preparing method

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Effect test

Embodiment 1

[0019] Weigh 20g of paclitaxel and 250g of oral soybean lecithin, add 1000mL of absolute ethanol and reflux for 45 minutes under heating and stirring; dry it under reduced pressure to 150mL under vacuum pressure -0.09MPa, 60°C water bath heating; then use the concentrated solution The reduced-pressure drying method continues drying at a vacuum pressure of -0.05MPa and 40°C to obtain a paclitaxel phospholipid dispersion; add 500 g of lactose, 10 g of talc, and 15 g of carboxymethyl starch sodium to the prepared paclitaxel phospholipid dispersion , mixed evenly, and prepared into tablets according to the conventional tablet preparation process.

Embodiment 2

[0020] The preparation of embodiment 2 paclitaxel phospholipid dispersion capsules

[0021] Weigh 20g of paclitaxel and 620g of oral egg yolk lecithin, add 1200mL of ethyl acetate and reflux for 1.5 hours under heating and stirring; dry it under reduced pressure to 550mL under vacuum pressure -0.07MPa, 55°C water bath heating; then use the concentrated solution The fluidized bed drying method continued drying at 35°C to obtain the paclitaxel phospholipid dispersion; add 60g of starch and 37g of magnesium stearate to the prepared paclitaxel phospholipid dispersion, mix well, and directly pack it into capsules to prepare into capsules.

Embodiment 3

[0022] The preparation of embodiment 3 paclitaxel phospholipid dispersion pellets

[0023] Weigh 20g of paclitaxel and 900g of soybean lecithin for injection, add 4500mL of chloroform and reflux for 3 hours under heating and stirring; dry it to 650mL under vacuum pressure -0.04MPa, 40°C water bath heating; Press drying method Continue drying under vacuum pressure -0.06MPa and 50°C to obtain the paclitaxel phospholipid dispersion; add 10,000 g of microcrystalline cellulose to the prepared paclitaxel phospholipid dispersion, mix well, and follow the conventional micropellet preparation process Prepare it into pellets.

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Abstract

A taxol product with high biologic utilization rate is prepared taxol and phosphatide through thermal reflux in organic solvent, concentrating, and drying.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a paclitaxel preparation and a preparation method thereof. Background technique [0002] Paclitaxel is currently an effective antineoplastic drug for the clinical treatment of non-small cell lung cancer, ovarian cancer and breast cancer. It is ultra-stable and finally stops cell proliferation in the G / M phase of mitosis. Due to its unique mechanism of action and definite curative effect, paclitaxel has become one of the most valuable anticancer drugs. Paclitaxel injection (trade name Taxol, Taxo1) is a colorless viscous solution made of polyoxyethylene castor oil (cremophor EL): absolute ethanol (50:50), and it is used with sodium chloride injection or 5% glucose injection Intravenous infusion after dilution. The cremophorEL in paclitaxel injection can easily cause allergic reactions and hypotension, which greatly limits the clinical application. In addition, paclitaxel is dif...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K31/337A61K47/24A61P35/00
Inventor 黄成安
Owner 黄成安
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