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Compound paclitaxel-oleum fructus bruceae injection emulsion and preparation method thereof

A technology of bruce chinensis oil and paclitaxel is applied in the directions of pharmaceutical formula, emulsion delivery, and medical preparations containing active ingredients, etc., to achieve the effects of reducing phlebitis, simple prescription and convenient administration.

Active Publication Date: 2009-02-11
CHONGQING LUMMY PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

So far, there is no report on the preparation of injection emulsions with the compound oil phase composed of paclitaxel, javanica javanica oil and ethanol together with injection excipients

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Example 1 Oil Phase Screening Test

[0021] The screening is based on dissolving paclitaxel in ethanol and adding vegetable oil or surfactant to investigate the solubility of paclitaxel, and selecting an oil phase with better solubility for paclitaxel creates conditions for the successful preparation of paclitaxel for injection.

[0022] The specific screening process is as follows:

[0023] Weigh 5 parts of 20mg paclitaxel, add 0.5g ethanol respectively, and dissolve by ultrasonic treatment; add 1g each of soybean oil, javanica javanica oil, corn oil, cottonseed oil and olive oil to the paclitaxel solution, mix, and ultrasonically treat for 30 minutes Afterwards, centrifuge at 10000rpm for 10 minutes, discard the precipitate, and the paclitaxel content in the supernatant is determined by high performance liquid chromatography, and the results are listed in Table 1.

[0024] Table 1

[0025] vegetable oil Soybean oil Brucea javanica oil ...

Embodiment 2

[0027] Example 2 Preparation of compound paclitaxel-brucea javanica oil injection emulsion containing paclitaxel 0.7mg / g

[0028] Weigh 480 mg of paclitaxel, add 8 g of ethanol, dissolve it by ultrasonic treatment, add 13 g of javanica javanica oil, and stir well to obtain an oil phase; disperse 10 g of refined soybean lecithin in 300 g of water for injection to obtain a water phase. Mix the above two liquids, transfer them to a high-speed homogenizer, add 350 g of water for injection, and mix and homogenize at 20,000 rpm for 10 minutes to form colostrum. Transfer the colostrum to a high-pressure milk homogenizer, and circulate it 4 times at 80-100 MPa under the protection of nitrogen, filter the emulsion with a 0.45 μm microporous membrane, sub-package, and autoclave at 115°C for 30 minutes. In the emulsion, particles with particle diameters between 100 and 1000 nm account for 94%, and the content of paclitaxel as determined by high performance liquid chromatography is 0.68 m...

Embodiment 3

[0029] Example 3 Preparation of compound paclitaxel-brucea javanica oil injection emulsion containing paclitaxel 1mg / g

[0030] Weigh 800 mg of paclitaxel, add 10 g of ethanol, sonicate for dissolution, add 10 g of javanica javanica oil, and stir well to obtain an oil phase; disperse 10 g of refined soybean lecithin in 300 g of water for injection to obtain a water phase. Mix the above two liquids, transfer them to a high-speed homogenizer, add 470 g of water for injection, and mix and homogenize at 20,000 rpm for 10 minutes to form colostrum. Transfer the colostrum to a high-pressure milk homogenizer, and circulate it 4 times at 80-100 MPa under the protection of nitrogen, filter the emulsion with a 0.45 μm microporous membrane, sub-package, and autoclave at 115°C for 30 minutes. In the emulsion, particles with particle diameters between 100 and 1000 nm account for 97%, and the content of paclitaxel as determined by high performance liquid chromatography is 0.96 mg / g.

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PUM

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Abstract

The invention relates to a compound paclitaxel, namely oleum fructus bruceae emulsion for injection, and a preparation method thereof, which pertain to the field of medicine preparation, and aim at solving the technical problem of looking for a new paclitaxel emulsion for intravenous injection with large drug-loading rate, few side-effects and convenient drug administration and a preparation method thereof so as to meet the requirements of markets for the new medicine. Particularly, the new paclitaxel emulsion is prepared by the steps: after dissolving in ethanol, the paclitaxel is added with the oleum fructus bruceae to form a compound oil phase and then is prepared into the emulsion of oil-in-water type with accessories for injection, such as lecithin, water for injection and the like. In the invention, the paclitaxel is obtained by a plurality of screening experiments; the paclitaxel in the compound oil phase consisting of ethanol and the oleum fructus bruceae has very high solubility; an external water phase does not contain the paclitaxel, and therefore the emulsion of oil-in-water type prepared effectively prevents phlebitis caused by the external water phase, greatly reduces anaphylactic reaction and enhances the adaptability of patients. In addition, the preparation of the emulsion has simple prescription and does not produce sediment after being diluted; embolizing does not occur during intravenous injection, thus providing a new paclitaxel emulsion for intravenous injection in clinical treatment.

Description

technical field [0001] The invention relates to a compound paclitaxel-brucea javanica oil injection emulsion and a preparation method thereof, belonging to the field of pharmacy. Background technique [0002] Paclitaxel is a diterpenoid extracted from the bark of Taxus genus Taxus. It is a new type of microtubule stabilizer with unique anticancer activity. It is considered by the National Cancer Institute of the United States to be the most important progress in tumor chemotherapy in the past 15 to 20 years. As a second-line treatment drug for advanced ovarian cancer, it has been approved for marketing in more than 40 countries so far, and has shown encouraging curative effects in the treatment of breast cancer, lung cancer, leukemia, gastrointestinal cancer and vascular restenosis after interventional therapy. . [0003] Although paclitaxel has good antitumor activity, paclitaxel is soluble in organic solvents such as methanol, ethanol, and DMSO, while its solubility in w...

Claims

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Application Information

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IPC IPC(8): A61K36/185A61K9/107A61P35/00A61K31/337
Inventor 唐小海谢永美宋鑫邱宇
Owner CHONGQING LUMMY PHARMA
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