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Application of sanguinarine and salt thereof as spermatozoicide

A technology of sanguinarine and its effect, applied in the field of biomedicine, can solve the problem that the spermicidal effect of sanguinarine and its salt has not been reported, and achieve good spermicidal contraceptive effect and the effect of preventing sexually transmitted diseases

Inactive Publication Date: 2014-05-07
HUNAN INSTITUTE OF SCIENCE AND TECHNOLOGY +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] According to literature reports, sanguinarine and its salts have rich pharmacological activities, such as bactericidal, antiviral, insecticidal, snail killing, cercaricidal and antitumor effects, but the spermicidal effect of sanguinarine and its salts has not been seen so far. to report

Method used

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  • Application of sanguinarine and salt thereof as spermatozoicide
  • Application of sanguinarine and salt thereof as spermatozoicide
  • Application of sanguinarine and salt thereof as spermatozoicide

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Example 1: Take 1kg of pods that have been dried, and use 10 times the amount of 1% dilute sulfuric acid water (80°C 0 ) percolation extraction twice, the filtered filtrate was adjusted to pH 10 with 10% NaOH solution, filtered, precipitated and dried, then dissolved in absolute ethanol, stirred and a small amount of concentrated sulfuric acid was added dropwise, filtered after standing, and dried It is the total alkaloid sulfate of Boluohui (the content of sanguinarine is about 40%). Take a small amount of the solid to alkalinize with dilute ammonia water, dry and separate on a 200-mesh silica gel chromatography column, elute with chloroform / methanol / ammonia water (60:4:1.5), and evaporate the first eluted component to dryness , The obtained solid is recrystallized twice with acidic methanol (acidified with hydrochloric acid) to obtain 98% sanguinarine hydrochloride, alkalized with dilute ammonia and then dried to obtain sanguinarine.

[0040] Add an appropriate amo...

Embodiment 2

[0041] Example 2: Crystallize sanguinarine in methanol, ethanol, other alcohols or dilute ammonia water (that is, insert methoxy, ethoxy, hydroxyl or other alkyl groups on the 6th or 11th position of the sanguinarine molecule ), then dissolved in dilute acid, and then formulated into sanguinarine hydrochloride gel preparation with hydroxymethylpropyl cellulose as the matrix.

Embodiment 3

[0042] Example 3: Sanguinarine hydrochloride gel preparation was prepared by dissolving sanguinarine in dilute hydrochloric acid, and then using hydroxymethylpropyl cellulose as a matrix.

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Abstract

The invention discloses application of sanguinarine and a salt thereof as a spermatozoicide. The sanguinarine and the salt thereof have the obvious characteristics of rapid sperm killing, low concentration, low price, and good safety and reliability. The lowest sperm killing concentration of sanguinarine aqueous solution (pH=4.5) is 0.25 mg / L and 0.15 mg / L at 20 s and 3 min, respectively, and the lowest sperm killing concentration of hydroxymethyl propyl cellulose gel of sanguinarine in a rabbit antifertility test is 0.5 mg / Kg, and ED50 is 0.129 mg / Kg. Compared with common nonoxynol nonylphenoxypolyedthoxyethanol, the sperm killing indicators of sanguinarine are al superior to the sperm killing indicators of nonoxynol nonylphenoxypolyedthoxyethanol, so that sanguinarine and the salt thereof are expected to become a novel and efficient externally-applied contraceptive for females.

Description

technical field [0001] The invention relates to the discovery of a new application of sanguinarine and its salts, specifically the preparation of female external (vaginal) spermicidal and contraceptive drugs with sanguinarine and its soluble salts as main components, which belongs to the field of biomedicine. Background technique [0002] Contraception is a widely studied content in the field of reproduction and family planning. There are many methods of contraception, such as contraceptive pills, condoms, diaphragms, rhythm contraceptive methods, extracorporeal ejaculation contraceptive methods, surgical contraceptive methods, etc., among which The use of birth control pills (for women) is most common. There are also many types of contraceptives, such as external spermicides and oral contraceptives. Because external spermicides generally do not interfere with women's endocrine functions, are cheap, easy to use, and have the effect of sterilization and disinfection, they hav...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4741A61P15/18
Inventor 钟明冯务群阎建辉易健民唐课文向阳
Owner HUNAN INSTITUTE OF SCIENCE AND TECHNOLOGY
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