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对壬苯醇醚-9与聚乙烯吡咯烷酮共沉淀并结合碘形成的新型制剂作为潜在阴道避孕药的评估。

Assessment of new formulations of nonoxynol-9 coprecipitated with polyvinylpyrrolidone and iodine as possible vaginal contraceptives.

作者信息

Zavos P M, Correa J R, Nosek D, Mohammadi F, Digenis G A

机构信息

Department of Animal Sciences, University of Kentucky, Lexington 40546, USA.

出版信息

Fertil Steril. 1996 Nov;66(5):729-33.

PMID:8893675
Abstract

OBJECTIVE

To assess the in vitro spermicidal activity of new formulations of nonoxynol-9, coprecipitated with polyvinylpyrrolidone (PVP) or iodinated PVP, against human spermatozoa via the use of the Sander-Cramer test and the cervical mucus penetration test.

DESIGN

Solutions of PVP-nonoxynol-9 and iodinated PVP-nonoxynol-9 containing nonoxynol-9 whole molecule (oligomers 1 to 18) and its isolated fractions (oligomers 8 to 10, 4 to 6, and 1 to 3) at various concentrations (microgram/mL) were prepared via serial dilutions. Spermicidal solutions were mixed with human semen to determine the minimal lethal dose (microgram/mL). In the Sander-Cramer test, the lethal dose was reported as the minimal dose capable of killing spermatozoa within 20 seconds. In the cervical mucus penetration test, the lethal dose was reported as the minimal dose capable of preventing penetration of spermatozoa into cervical mucus beyond the second millimeter length of the capillary.

SETTING

Andrology laboratory, University of Kentucky, Lexington, Kentucky.

PATIENT(S): Normospermic male donors.

MAIN OUTCOME MEASURE(S): Spermicidal lethal dose determination of various nonoxynol-9 preparations containing the whole nonoxynol-9 molecule and its isolated fractions coprecipitated with PVP or iodinated PVP.

RESULT(S): The use of PVP increased the aqueous solubility of the nonoxynol-9 formulations containing oligomers 1 to 18 and 8 to 10 slightly. The coprecipitation of the nonoxynol-9 formulations containing nonoxynol-9 oligomers 4 to 6 and 1 to 3 with PVP significantly increased their solubilization and spermicidal action in vitro. Moreover, the incorporation of iodine significantly decreased the minimal nonoxynol-9 dose required for complete killing of spermatozoa in preparations containing nonoxynol-9 oligomers 4 to 6 and 1 to 3.

CONCLUSION(S): Incorporation of all three components tested in this study (PVP, nonoxynol-9, and iodine) enhanced the efficiency of the spermicidal preparations, especially for nonoxynol-9 preparations containing nonoxynol-9 oligomers 4 to 6 and 1 to 3.

摘要

目的

通过使用桑德 - 克莱默试验和宫颈黏液穿透试验,评估与聚乙烯吡咯烷酮(PVP)或碘化PVP共沉淀的壬苯醇醚 - 9新制剂对人类精子的体外杀精活性。

设计

通过系列稀释制备含有壬苯醇醚 - 9全分子(低聚物1至18)及其分离部分(低聚物8至10、4至6和1至3)的不同浓度(微克/毫升)的PVP - 壬苯醇醚 - 9和碘化PVP - 壬苯醇醚 - 9溶液。将杀精溶液与人类精液混合以确定最小致死剂量(微克/毫升)。在桑德 - 克莱默试验中,致死剂量报告为能够在20秒内杀死精子的最小剂量。在宫颈黏液穿透试验中,致死剂量报告为能够防止精子穿透到毛细管第二毫米长度以外的宫颈黏液中的最小剂量。

地点

肯塔基州列克星敦市肯塔基大学男科实验室。

患者

精子正常的男性捐赠者。

主要观察指标

测定含有全壬苯醇醚 - 9分子及其与PVP或碘化PVP共沉淀的分离部分的各种壬苯醇醚 - 9制剂的杀精致死剂量。

结果

使用PVP略微增加了含有低聚物1至18和8至10的壬苯醇醚 - 9制剂的水溶性。含有壬苯醇醚 - 9低聚物4至6和1至3的壬苯醇醚 - 9制剂与PVP共沉淀显著增加了它们在体外的增溶作用和杀精作用。此外,碘的加入显著降低了在含有壬苯醇醚 - 9低聚物4至6和1至3的制剂中完全杀死精子所需的最小壬苯醇醚 - 9剂量。

结论

本研究中测试的所有三种成分(PVP、壬苯醇醚 - 9和碘)的加入提高了杀精制剂的效率,特别是对于含有壬苯醇醚 - 9低聚物4至6和1至3的壬苯醇醚 - 9制剂。

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引用本文的文献

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Biomaterials and Contraception: Promises and Pitfalls.生物材料与避孕:前景与挑战。
Ann Biomed Eng. 2020 Jul;48(7):2113-2131. doi: 10.1007/s10439-019-02402-1. Epub 2019 Nov 7.
2
Coprecipitation of nonoxynol-9 with polyvinylpyrrolidone to decrease vaginal irritation potential while maintaining spermicidal potency.壬苯醇醚-9与聚乙烯吡咯烷酮共沉淀以降低阴道刺激可能性,同时保持杀精效力。
AAPS PharmSciTech. 2003;4(3):E30. doi: 10.1208/pt040330.