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Freeze dried hydroxy camptothecin powder for injection and its preparing process

A technology of hydroxycamptothecin and freeze-dried powder injection, which is applied in the direction of freeze-dried transportation, medical preparations containing active ingredients, powder transportation, etc., which can solve the impact of safety and effectiveness, large differences between batches, and limited stability In order to achieve the effects of convenient storage, improved stability and extended validity period

Inactive Publication Date: 2002-10-30
深圳万乐药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] At present, the commercially available HCPT preparations are all injection water injections. Although HCPT water injections have clinically good curative effects on various tumors, they are not stable due to the limitation of dosage forms, and the validity period is only 1 year, in fact, after 8 months of storage, there will be a small amount of precipitation, darkening and other deterioration
Moreover, the quality standards of water injections are all local standards, and the quantitative method used is ultraviolet detection method. The purity above 5% is qualified, and there are about 15% impurities. This will have a certain impact on the safety and effectiveness of clinical medication

Method used

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  • Freeze dried hydroxy camptothecin powder for injection and its preparing process
  • Freeze dried hydroxy camptothecin powder for injection and its preparing process
  • Freeze dried hydroxy camptothecin powder for injection and its preparing process

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Embodiment 1: 2mg / vial specification 1000 freeze-dried powder preparation formulations are:

[0024] Hydroxycamptothecin 1.8g, Glycine 2.2g,

[0025] Lactose 45.0g, Sodium Hydroxide 10.0g,

[0026] Add water for injection to 2100ml, make 1000 altogether.

[0027] Wherein, hydroxycamptothecin is the main drug, and feeds are fed respectively according to the requirements of two kinds of production specifications (2mg / branch, 5mg / branch).

[0028] Lactose is an excipient, used as a skeleton support part of hydroxycamptothecin freeze-dried powder for injection. According to the literature reports and the practical experience of other anti-tumor freeze-dried preparations of our company, the test was carried out by simulating the actual production, and the ratio of the main drug to lactose was determined: for the products of 2mg and 5mg specifications, the ratio of 1:20-120 was used. Proportion.

[0029] The buffer solution is made up of aminoacetic acid and sodium hydrox...

Embodiment 2

[0043] Embodiment 2: 2mg / vial specification 1000 freeze-dried powder preparation formulations are:

[0044] Hydroxycamptothecin 2.0g, Glycine 4.0g,

[0045]Lactose 100.0g, Sodium Hydroxide 10.0g,

[0046] Add water for injection to 2500ml, make 1000 altogether.

[0047] Its preparation process is as follows:

[0048] a', according to embodiment 2 preparation prescription batching, get the glycine of sodium hydroxide 10g, 3g (recipe quantity is 4.0g) and the water for injection of 100ml to prepare buffer, buffer is alkaline, pH is 8.5-10.0, Among them, the concentration of aminoacetic acid is 1mol / L, and the concentration of sodium hydroxide is 1% (W / L).

[0049] b', hydroxycamptothecin 2.0g is added in the buffer solution, stirred and dissolved to obtain solution ①;

[0050] c', put 100.0g of lactose into the batching tank with 200ml of water for injection, the water temperature is 20°C, stir and dissolve to obtain a solution②;

[0051] d', Pour the solution ① and the rem...

Embodiment 3

[0059] Example 3: 1000 freeze-dried powder injection formulations with a specification of 5 mg / vial are composed as follows:

[0060] Hydroxycamptothecin 5.0g, Glycine 8.0g,

[0061] Lactose 300.0g, sodium hydroxide 10.0g,

[0062] Add water for injection to 4000ml, make 1000 altogether.

[0063] Its preparation process is as follows:

[0064] a ", according to embodiment 3 preparation prescription batching, get the glycine of sodium hydroxide 10g, 5.6g (recipe quantity is 8.0g) and the water for injection of 300ml to prepare buffer, buffer is alkaline, pH is 7.5-10.5 , wherein the glycine concentration is 1mol / L, and the sodium hydroxide concentration is 1% (W / L).

[0065] b", adding 5.0 g of hydroxycamptothecin to the buffer solution, stirring and dissolving to obtain a solution ①;

[0066] c", put 300.0g of lactose into a batching tank filled with 300ml of water for injection, the water temperature is 25°C, stir and dissolve to obtain a solution②;

[0067] d", Pour the...

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Abstract

A freeze-dried hydroxy camptothecin powder injection for treating primary liver cancer, gastrointestinal cancer, vesical cancer, lung cancer, leukemia, etc is prepared from hydroxy camptothecin, aminoacetic acid, lactose, sodium hydroxide and the water for injection through preparing buffer liquid from sodium hydroxide, aminoacetic acid and the water for injection, dissolving hydroxy camptothecinin it to obtain solution A, dissolving lactose in the water for injection to obtain solution B, adding A and rest of aminoacetic acid to B, stirring, regulating pH value, adding water for injection, filtering loading in containers, freeze drying and sealing.

Description

technical field [0001] The invention relates to the preparation technology of hydroxycamptothecin anticancer medicine, in particular to a hydroxycamptothecin freeze-dried powder preparation for injection and a preparation method thereof. Background technique [0002] Hydroxycamptothecin is a natural plant alkaloid extracted from the fruit of the unique plant Camptotheca acuminata Decsne in my country. It was developed and developed by itself in 1977 through the arduous efforts of Chinese pharmaceutical experts and the cooperation of multiple units and disciplines. A successful natural plant anticancer drug unique to our country. As active ingredients of natural plants, camptothecin drugs such as hydroxycamptothecin are the only anticancer drugs that act on topoisomerase I (TOPO I) so far. Camptothecin was used in the treatment of various cancers in the 1970s, but its development and application were limited due to its severe side effects. Since Chinese scholars have success...

Claims

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Application Information

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IPC IPC(8): A61K9/19A61K31/4741A61P35/00
Inventor 宋鹏飞曾丽华宝玉荣王君山邓胡宁侯常林
Owner 深圳万乐药业有限公司
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