Anti-fertility medicine, and pharmaceutical preparation and application thereof

A technology for anti-fertility drugs and pharmaceutical preparations, which can be used in drug combinations, pharmaceutical formulations, medical preparations containing active ingredients, etc., and can solve problems such as large toxic and side effects

Active Publication Date: 2017-03-22
TECHNICAL INST OF PHYSICS & CHEMISTRY - CHINESE ACAD OF SCI +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although there are still many reports of spermicidal and contraceptive drugs used in the reproductive tract at home and abroad, such as phyt

Method used

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  • Anti-fertility medicine, and pharmaceutical preparation and application thereof
  • Anti-fertility medicine, and pharmaceutical preparation and application thereof
  • Anti-fertility medicine, and pharmaceutical preparation and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] This example is used to illustrate the observation of the in vitro spermicidal effect of the antifertility drug provided by the present invention.

[0046] Preparation of the test solution: take the podophyllotoxin obtained by the above method as the test (98% content) (HPLC detection). Dilute the above-mentioned podophyllotoxin test product to 2.0mg / ml, 1.0mg / ml, 0.5mg / ml, 0.25mg / ml, 0.125mg / ml and 0.0625mg / ml with physiological saline, and set aside for testing.

[0047] Rat sperm collection and counting method: SD male rats (3, male, 250-300g, provided by Haishi Xipuer-Bika Experimental Animal Co., Ltd., production license number: SCXK (Shanghai) 2013-0016) double The lateral epididymis was placed in a sterile small beaker, rinsed with normal saline, and then added sperm nutrient solution (Tyrode solution: 4.0g NaCl, 0.10g KCl, CaCl 2 0.10g, MgCl 2 ·6H 2 O 0.05g, NaH 2 PO 4 2H 2 O 0.025g, NaHCO 3 0.50g, Glucose 0.50g, dissolved in deionized water several times...

Embodiment 2

[0054] This example is used to illustrate the observation of the in vitro spermicidal effect of the antifertility drug provided by the present invention.

[0055] Preparation of the test solution: take deoxypodophyllotoxin as the test. Dilute the above-mentioned deoxypodophyllotoxin test product to 2.0mg / ml, 1.0mg / ml, 0.5mg / ml, 0.25mg / ml, 0.125mg / ml and 0.0625mg / ml with physiological saline, ready for testing.

[0056] Rat sperm collection and counting methods and rat spermicide test method are the same as in Example 1. Table 2 shows the effective concentrations and corresponding time points of different concentrations of deoxypodophyllotoxin for inhibiting sperm motility in rats.

[0057] Table 2

[0058]

[0059] Note: "+" indicates that at least one sperm is active in the field of view; "—" indicates that there is no motile sperm in the field of view.

[0060] The results showed that the effective concentration of deoxypodophyllotoxin to completely inhibit sperm motil...

Embodiment 3

[0062] This example is used to illustrate the observation of the in vitro spermicidal effect of the antifertility drug provided by the present invention.

[0063] Preparation of the test product solution: the podophyllotoxin and deoxypodophyllotoxin obtained by the above method were used as the test product (the content was 98%) (HPLC detection). Use physiological saline to dilute the above-mentioned podophyllotoxin test product to 2.0mg / ml, 1.0mg / ml, 0.5mg / ml, 0.25mg / ml, 0.125mg / ml and 0.0625mg / ml, and supply the above-mentioned deoxypodophyllotoxin The test product is diluted to 2.0mg / ml, 1.0mg / ml, 0.5mg / ml, 0.25mg / ml, 0.125mg / ml, and it is ready for testing.

[0064] Human semen sample processing and sperm counting method: take healthy adult male semen (human semen samples are selected from male semen with fertility and abstinence for more than 7 days, sperm motility rate ≥ 70%, forward motility sperm ≥ 75%, deformity ≤ 20% ), placed in a sterile small beaker, and then add...

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Abstract

The invention relates to the field of medicines, and discloses an anti-fertility medicine, wherein the anti-fertility medicine contains a podophyllotoxin compound and is applied to spermicidal contraception for mammals. Also disclosed is a pharmaceutical preparation; the pharmaceutical preparation contains an active ingredient, wherein the active ingredient is the anti-fertility medicine provided by the invention. The invention also provides an application of the podophyllotoxin compound in preparation of the anti-fertility medicine, wherein the anti-fertility medicine is applied for spermicidal contraception in genital tracts of the mammals. The podophyllotoxin compound provided by the invention can be directly used as a drug for spermicidal contraception in genital tracts of female mammals, especially as a drug for spermicidal contraception in genital tracts of human female, and has high safety and low toxicity to human body organs. Therefore, the anti-fertility medicine provided by the invention has quite important practical significance and application promotion value for improving the level of reproductive health.

Description

technical field [0001] The invention relates to an antifertility drug, pharmaceutical preparation and application. Background technique [0002] In recent years, the number of unmarried pregnancies / abortion rate and the reproductive tract infection rate in my country have shown a sharp upward trend. Among the various contraceptive measures commonly used at present, whether it is intrauterine device, tubal ligation and vasectomy, or hormonal oral contraceptives, etc., there are long-term side effects, poor patient compliance, and may interfere with the normal endocrine system of the human body. And other issues. In addition, there are many potential risk factors, especially teratogenicity, carcinogenicity, transmission of sexually transmitted diseases (STDs), etc. Among the many birth control methods, spermicidal contraceptives in the female reproductive tract are a kind of contraceptive method with higher safety. It has the advantages of less systemic side effects and no ...

Claims

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Application Information

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IPC IPC(8): A61K31/365A61P15/18
Inventor 钱越英谢淑武魏雪涛陈平李国停楼辉张锁慧朱焰杨国忠蒋建军佟振合薛社谱
Owner TECHNICAL INST OF PHYSICS & CHEMISTRY - CHINESE ACAD OF SCI
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