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9-nitrocamptothecin mixed micelle freeze-dried powder injection and preparation method thereof

The technology of nitrocamptothecin and freeze-dried powder injection is applied in the field of mixed micelle freeze-dried powder injection of 9-nitrocamptothecin and its preparation, and can solve the problems of insolubility, low oral bioavailability and the like, To alleviate toxicity, facilitate clinical use, and improve stability

Active Publication Date: 2012-07-11
SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] The purpose of the present invention is to overcome the insoluble properties of 9-nitrocamptothecin, low oral bioavailability, rapid elimination of intravenous administration and other shortcomings, to prepare a method that can greatly improve its bioavailability and low cost, and the preparation process is simple and suitable for use. Safe and effective 9-nitrocamptothecin injection freeze-dried powder for industrial production

Method used

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  • 9-nitrocamptothecin mixed micelle freeze-dried powder injection and preparation method thereof
  • 9-nitrocamptothecin mixed micelle freeze-dried powder injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] Weigh 60mg of soybean lecithin and place it in a 100ml round bottom flask, add 10ml of ethanol solution of sodium deoxycholate (10mg / ml), fully dissolve to obtain stock solution 1, dissolve 6mg of 9-nitrocamptothecin In 50ml of acetone, the stock solution 2 was obtained, and the two were mixed evenly, and the organic solvent was spin-dried in a water bath at 40°C, protected from light and depressurized, to obtain a yellow film, and then added 2.0ml of normal saline to disperse evenly to obtain a drug-containing mixed micellar solution , adjust the pH=6.0 with sodium hydroxide and hydrochloric acid, centrifuge at 13000 rpm / min for 5 min, and take the supernatant to obtain 9-nitrocamptothecin mixed micelles injection.

[0048] Sterile filter with a 0.22 μm microporous membrane filter. Put it into a vial, add 10% glucose as a lyoprotectant, pre-freeze at 40°C for 4h, and then freeze-dry (-50°C, 24h).

[0049] Take the freeze-dried finished product, observe that the appear...

Embodiment 2

[0051] Accurately weigh 85mg of egg yolk lecithin into a 100ml round bottom flask, add 11ml of ethanol solution of sodium glycocholate (10mg / ml), fully dissolve to obtain stock solution 1, dissolve 2mg of 9-nitrocamptothecin In 25ml of methanol, the stock solution 2 was obtained, and the two were mixed evenly, and the organic solvent was spin-dried in a water bath at 40°C, protected from light and decompressed, to obtain a yellow film, and then added 2.0ml of water for injection to disperse evenly to obtain a drug-containing mixed micelle solution, adjusted to pH=5.5 with sodium hydroxide and hydrochloric acid, centrifuged at 13,000 rpm / min for 5 minutes, and the supernatant was taken to obtain 9-nitrocamptothecin mixed micelles injection.

[0052] Sterile filter with a 0.22 μm microporous membrane filter. Put it into a vial, add 5% sucrose as a lyoprotectant, pre-freeze at 40°C for 4h, and then freeze-dry (-50°C, 24h).

[0053] Take the freeze-dried finished product, observe...

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Abstract

The invention relates to a 9-nitrocamptothecin mixed micelle freeze-dried powder injection and a preparation method thereof. The preparation adopts 9-nitrocamptothecin as an effective component, and comprises phospholipid, bile salts, a freeze-drying protective agent, and other auxiliary materials. The ratio of 9-nitrocamptothecin, phospholipid, bile salts, the freeze-drying protective agent, andother auxiliary materials is 1:1-45:5-70:10-150:a proper amount. The freeze-dried powder injection prepared by the invention not only can effectively solve the problem of insolubility of 9-nitrocamptothecin in water, but also can significantly improve drug bioavailability. The preparation process of the invention is simple, and applicable to industrial production, and the product is good in stability, and good in curative effect.

Description

technical field [0001] The invention belongs to the pharmaceutical preparation in the technical field of medicine, and in particular relates to a 9-nitrocamptothecin mixed micellar freeze-dried powder injection and a preparation method thereof. Background technique [0002] Camptothecin (CPT) is an alkaloid extracted from Camptotheca acuminata, a Chinese plant of the Davidiaceae family, which can exert antitumor effects by inhibiting topoisomerase I. 9-nitrocamptothecin (9-NC) is a kind of insoluble semi-synthetic derivative of camptothecin developed by American Supergene Company. Anti-cancer activity, reducing toxic and side effects, also known as RFS2000, is currently mostly used for oral administration, and its solubility in water is extremely small, and its lactone ring structure is a prerequisite for its activity. Clinical studies have shown that it has a good curative effect on a variety of tumors including lung cancer, ovarian cancer, liver cancer, melanoma, colon ca...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/19A61K31/4745A61K47/28A61K47/24A61P35/00
Inventor 龚涛张志荣孙逊黄蕊
Owner SICHUAN UNIV
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