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Taxol freezing-dried emulsion for injection and preparation method thereof

A freeze-dried emulsion, paclitaxel technology, applied in the directions of emulsion delivery, liquid delivery, antitumor drugs, etc., can solve the problems of non-compliance with drug safety and industrial production, acute allergic reactions, increased toxicity, etc., to eliminate allergic side effects, The effect of prolonging the validity period and improving the therapeutic index

Inactive Publication Date: 2010-12-08
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The preparation has the following problems: ①Cremophor EL can cause severe acute allergic reaction and hypotension in the body; ②Cremophor EL can cause the plasticizer in the PVC packaging to dissolve, further increasing the toxicity; ③Dilution before clinical use can easily crystallize paclitaxel Precipitation; ④ Paclitaxel is prone to non-specific binding with the surface of glass or plastic in the solution, resulting in a decrease in concentration
U.S. Patent US2003 / 0099674 uses vegetable oil as the oil phase to prepare paclitaxel freeze-dried preparations. Since vegetable oil cannot be removed by freeze-drying, it is actually a semi-solid preparation with poor stability at room temperature.
Although some progress has been made in the research on paclitaxel derivatives and preparations, most of them still do not meet the requirements of drug safety and industrial production.

Method used

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  • Taxol freezing-dried emulsion for injection and preparation method thereof
  • Taxol freezing-dried emulsion for injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Dissolve 30mg of paclitaxel and 600mg of lecithin in 5ml of ethanol to form an organic phase; weigh 6mg of poloxamer108 and 2mg of a-tocopherol and dissolve them in 30ml of water for injection as the water phase; add the organic phase to the water phase and stir at 200rpm The colostrum is obtained, and the colostrum is repeatedly homogenized by a high-pressure homogenizer to obtain a finely dispersed emulsion, the ethanol is removed under reduced pressure, 1.5g sucrose and 1.5g mannitol are added, and the water is removed by freeze-drying to obtain dry paclitaxel freeze-dried emulsion.

Embodiment 2

[0034] Dissolve 1 g of paclitaxel and 60 g of soy lecithin in 10 ml of ethanol to form an organic phase; weigh 0.25 g of poloxamer 188 and 5 mg of a-tocopheryl acetate and dissolve it in 30 ml of water for injection as the water phase; mix the organic phase with the water phase Under the condition of 1500rpm magnetic stirring, the colostrum was stirred for 10min, and then the colostrum was repeatedly homogenized by a high-pressure homogenizer to obtain a finely dispersed emulsion; the organic solvent was removed under reduced pressure, 75g of mannitol was added, and the moisture was removed by freeze-drying to obtain Dry paclitaxel lyophilized emulsion.

Embodiment 3

[0036] Dissolve 8mg of paclitaxel, 200mg of monoglyceride and 10mg of cholic acid in 5ml of acetone to form the organic phase; weigh 5mg of poloxamer108 and dissolve it in 50ml of water for injection as the water phase; mix the organic phase and the water phase under the condition of 1000rpm magnetic stirring Stir for 30 minutes to obtain colostrum, and then homogenize the colostrum by a high-pressure homogenizer to obtain a finely dispersed emulsion; add 800 mg of sucrose, stir to dissolve it, remove the organic solvent under reduced pressure, and then freeze-dry to obtain the present invention. Paclitaxel lyophilized emulsion.

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Abstract

The present invention discloses a taxol freeze-dried emulsion for injection. It includes taxol with therapeutic effective dose and medicinal auxiliary material. The described medicinal auxiliary material includes emulsifying agent, freeze-drying protection agent and additive, in which the additive can be stabilizing agent, pH regulating agent and anti-oxidant according to the requirements. Besides, said invention also provides the preparation method of said taxol freeze-dried emulsion.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a freeze-dried emulsion containing paclitaxel as an antitumor active ingredient and a preparation method thereof. Background technique [0002] Paclitaxel (Taxol) is a natural anticancer drug developed by Bristol-Myers Squibb at the end of the 20th century. It is a cytostatic drug with a unique mechanism of action and is effective for many drug-resistant patients. It can promote the assembly of tubulin into microtubules, but inhibit the depolymerization of microtubules, stabilize the microtubules, lead to abnormal arrangement of microtubules, make the pituitary gland lose its normal function and lead to cell death, and has outstanding curative effect on breast cancer and ovarian cancer. In addition, it also has a certain effect on liver cancer, lung cancer, esophageal cancer, head and neck cancer, and prostate cancer. [0003] Paclitaxel is used as an injectable chemot...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/335A61K9/10A61K47/38A61P35/00
Inventor 李亚平陈伶俐顾王文
Owner SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI