Temozolomide intravenous injection fat emulsion and preparation method thereof

A technology of temozolomide and fat emulsion, which is applied in the field of medicine and biology, can solve the problems of unsuitability and poor solubility of temozolomide, and achieve the effects of enhancing compliance, improving drug efficacy, and strong controllability

Inactive Publication Date: 2013-11-27
SHANDONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The purpose of the present invention is to solve the problem of poor solubility of temozolomide, and simultaneously provide intravenously injectable temozolomide preparations for patients who are not suitable for oral administration

Method used

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  • Temozolomide intravenous injection fat emulsion and preparation method thereof
  • Temozolomide intravenous injection fat emulsion and preparation method thereof
  • Temozolomide intravenous injection fat emulsion and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Example 1 Preparation of Temozolomide Intravenous Injection Fat Emulsion

[0041] The composition of raw materials is as follows: 100 mg of temozolomide, 20 g of soybean oil for injection, 1 g of oleic acid, 1.6 g of soybean lecithin, 0.8 g of Pluronic F68, 2.2 g of glycerin, and water for injection to 100 mL.

[0042] The preparation method is as follows:

[0043] (1) Mix emulsifier soybean lecithin 0.8g, Pluronic F68 and isotonic regulator glycerin, add appropriate amount of water for injection (50ml), stir well, and make water phase;

[0044] (2) Mix soybean oil for injection and stabilizer oleic acid, and stir evenly to make an oil phase;

[0045] (3) Pour the oil phase into the water phase under stirring, and cut at 10000rpm for 3min to make colostrum;

[0046] (4) Add temozolomide to water (40ml) dispersed with an emulsifier (0.8g), and cut at 10000rpm for 3min to obtain a drug suspension;

[0047] (5) Add the drug suspension to the colostrum, cut at 10,000rpm ...

Embodiment 2

[0055] Example 2 Preparation of Temozolomide Intravenous Injection Fat Emulsion

[0056] The composition of raw materials is as follows: temozolomide 200mg, soybean oil for injection 10g, medium chain oil 10g, oleic acid 1g, soybean lecithin 1.6g, Pluronic F680.8g, glycerin 2.25g, vitamin E 1g (added to the oil phase), benzyl alcohol 0.5g (added to the water phase), add water for injection to 100mL.

[0057] The preparation method is the same as in Example 1, and the particle size of the obtained fat emulsion is 184.8nm.

Embodiment 3

[0058] Example 3 Preparation of Temozolomide Intravenous Injection Fat Emulsion

[0059] The raw material composition is the same as in Example 1, the preparation method is the same as in Example 1, the pressure of high-pressure milk homogenization is 1000 bar, the number of times of high-pressure milk homogenization is 10 times, and the particle size of the obtained fat emulsion is 222.2nm.

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Abstract

The invention discloses a temozolomide intravenous injection fat emulsion which comprises the following components in percentage by weight: 0.01-5% of temozolomide, 5-30% of oil for injection, 0.2-5% of emulgator, 0.2-3% of stabilizer, 1-5% of isoosmotic adjusting agent and the balance of water for injection. The prepared temozolomide intravenous injection fat emulsion is uniform in appearance, narrower in distribution, high in drug loading capacity (1 mg / ml), stable in quality, used for intravenous injection, simple and practical in production process, high in controllability, and liable to large-scale industrial production; the average grain diameter is about 200 nm, the Zeta electric potential is about -40 mV, and the pH is 5.0-9.0; the temozolomide intravenous injection fat emulsion has excellent biocompatibility, can provide energy for an organism, and can realize therapeutic action to various tumours.

Description

technical field [0001] The invention relates to a temozolomide intravenous injection fat emulsion and a preparation method thereof, belonging to the field of medical biotechnology. Background technique [0002] In recent years, the incidence of malignant brain tumors is not optimistic. Statistics show that about 60% of primary brain tumors are malignant brain tumors, which have a high incidence and great harm. The standard treatment for malignant brain tumors is surgical resection of the tumor followed by postoperative radiation therapy. Temozolomide has good anti-tumor activity, and has been evaluated as the "gold standard" for the treatment of malignant brain tumors by the American and European medical circles, and has been defined as the first-line drug for the treatment of malignant brain tumors by international medicine. [0003] Temozolomide was approved by the FDA on August 11, 1999, and was launched in the United States. Its chemical name is 3,4-dihydro-3-methyl-4...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K31/4188A61P35/00
Inventor 黄桂华冯瑞华
Owner SHANDONG UNIV
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