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Application of triptonide in preparation of contraception and birth control drugs of macaca fascicularis

A technology of triptolide ketone and cynomolgus monkeys, which is applied in the application field of triptolide ketone in the preparation of contraceptive drugs for cynomolgus monkeys, and can solve problems affecting the application

Inactive Publication Date: 2018-12-07
广东省计划生育科学技术研究所
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, Tripterygium wilfordii total glycosides, tripterygium glycosides, and triptolide have good contraceptive effects, but at the same time they can produce immunosuppressive effects, which affect their further application.

Method used

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  • Application of triptonide in preparation of contraception and birth control drugs of macaca fascicularis
  • Application of triptonide in preparation of contraception and birth control drugs of macaca fascicularis
  • Application of triptonide in preparation of contraception and birth control drugs of macaca fascicularis

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Embodiment 1 minimum effective dose

[0029] Take 5 cynomolgus monkeys aged 8-10 to take triptolide ketone according to 5 different doses, respectively 5mg / kg, 0.8mg / kg, 0.2mg / kg, 0.1mg / kg, 0.05mg / kg, taking After 5 weeks, except for 0.05mg / kg, for other doses, almost 100% of the sperm of cynomolgus monkeys were seriously deformed and died at the 5th week of taking the medicine. It can be seen that the minimum effective dose of triptolide is 0.1mg / kg.

Embodiment 2

[0030] Embodiment 2SD-1 has good contraceptive effect

[0031] The 12 male cynomolgus monkeys were divided into 2 groups, and 9 in the experimental group (No. 00298G, 00336G, 00340G, 00339G, 00299G, 00300G, 00337G, 00341G, 00301G), in which the male cynomolgus monkey 00301G was orally administered 0.1mg / kg SD-1 over 7 months, and 3 rats in the control group (No. 00343G, 00338G, 00342G). Before the experiment, 12 cynomolgus monkeys were electrically stimulated to extract semen and peripheral blood, and the baseline values ​​of semen parameters and peripheral blood routine, biochemistry, liver and kidney function, hormones and other baseline values ​​were recorded. Puncture, the specimen is used for pathological examination.

[0032] After starting the experiment, the experimental group took orally SD-1 solution (0.5ml, containing SD-1+DMSO+dehydrated ethanol) at a dose of 0.1mg / kg every day, and the control group only took the same volume of solvent (DMSO+dehydrated ethanol)....

Embodiment 3

[0035] The contraception of embodiment 3SD-1 has reversibility

[0036] The drug withdrawal group in the experimental group no longer took the drug, but took the same volume of solvent orally. After 5 weeks of drug withdrawal, the semen parameters of cynomolgus monkeys basically returned to normal, and the sperm morphology was also basically normal ( Figure 4 ). From figure 2 , image 3 It can be seen that sperm PR and concentration basically returned to normal after 8 weeks of drug withdrawal. In the mating test of male and female cynomolgus monkeys, the male monkey mated with 2 female cynomolgus monkeys after 8 weeks of drug withdrawal, and all the 2 female cynomolgus monkeys were found to be pregnant. The above results show that the contraception of SD-1 is reversible.

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Abstract

The invention relates to application of triptonide and in particular relates to application of triptonide in preparation of contraception and birth control drugs of macaca fascicularis. The triptonidehas an excellent contraception effect, has a low effective dose, does not have any obvious side effect, is safe and effective, and has excellent application prospects.

Description

technical field [0001] The present invention relates to the use of triptolide, in particular to the application of triptolide in the preparation of cynomolgus monkey contraceptives. Background technique [0002] Non-hormonal contraceptives mainly include external spermicides, Chinese herbal contraceptives and immunocontraceptive vaccines. As a new type of drug, spermicide will affect the final use effect of spermicide due to people's lack of understanding of it and low acceptance of the product. However, the development of immunocontraceptive vaccines has been forced to stop because its contraceptive effect is difficult to meet clinical requirements. In recent years, the research on Chinese herbal contraceptives such as gossypol, begonia, tripterygium glycosides has attracted great attention. Although the anti-fertility effect of gossypol is certain, it will cause irreversible azoospermia and hypokalemic paralysis in some subjects, making gossypol unable to be used clinica...

Claims

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Application Information

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IPC IPC(8): A61K31/585A61P15/00A61P15/16
CPCA61K31/585A61P15/00A61P15/16
Inventor 闫威唐运革秦卫兵刘晓华伍嘉宝韩璐张欣宗
Owner 广东省计划生育科学技术研究所
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