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兔体内聚乙烯吡咯烷酮共沉淀壬苯醇醚-9新制剂的阴道给药。两种制剂给药系统的比较。

Vaginal delivery of new formulations of nonoxynol-9 coprecipitated with polyvinylpyrrolidone in rabbits. Comparisons between two formulation delivery systems.

作者信息

Zavos P M, Correa J R

机构信息

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

出版信息

Contraception. 1997 Aug;56(2):123-7. doi: 10.1016/s0010-7824(97)00102-9.

DOI:10.1016/s0010-7824(97)00102-9
PMID:9315422
Abstract

The objective of this study was to assess the efficacy of two formulation delivery systems (FDS) in preventing the onset of pregnancy in rabbits. Nonoxynol-9 (N-9) was coprecipitated with polyvinylpyrrolidone (PVP), which yields PVP/ N-9, and prepared as capsules or tablets. Semen specimens were collected (from eight male rabbits), pooled, and used for in vitro spermicidal assessment or artificial insemination (AI). In vitro spermicidal assessment was performed by introducing and mixing the FDS containing PVP or PVP/N-9 with 1.0 mL of semen, followed by incubation at 37 degrees C for 6 h. Semen samples were taken at various time intervals to determine killing of spermatozoa and dissolution of the FDS. The efficacy of the FDS in preventing the onset of pregnancy was assessed by inserting the FDS vaginally. The does were artificially inseminated at 0, 0.5, and 6 h after insertion of the FDS vaginally. The number of pregnant does and newborn rabbits was recorded. In the in vitro spermicidal trial, semen specimens exposed to both FDS containing PVP/N-9 were killed within 10 to 15 min of incubation. Tablets containing PVP only or PVP/N-9 dissolved completely after 3 h of incubation. However, capsules did not dissolve completely by 6 h of incubation. The results obtained in the in vivo trial showed that both FDS exhibited some variations in preventing the onset of pregnancy over the various time intervals following the insertion of tablets or capsules and AI. The tablet seemed to be a more efficient delivery system than the capsule, yielding significantly lower pregnancy rates at all three time intervals assessed. The tablet FDS, as applied in this study, was found to be the most efficient mode of delivery of the tested spermicidal formulations.

摘要

本研究的目的是评估两种剂型给药系统(FDS)在预防家兔怀孕方面的效果。壬苯醇醚-9(N-9)与聚乙烯吡咯烷酮(PVP)共沉淀,得到PVP/N-9,并制成胶囊或片剂。采集(来自8只雄兔的)精液样本,混合后用于体外杀精评估或人工授精(AI)。通过将含有PVP或PVP/N-9的FDS与1.0 mL精液引入并混合,然后在37℃下孵育6小时来进行体外杀精评估。在不同时间间隔采集精液样本,以确定精子的杀灭情况和FDS的溶解情况。通过经阴道插入FDS来评估FDS在预防怀孕方面的效果。在经阴道插入FDS后的0、0.5和6小时对母兔进行人工授精。记录怀孕母兔和新生兔的数量。在体外杀精试验中,暴露于含有PVP/N-9的两种FDS的精液样本在孵育10至15分钟内被杀灭。仅含有PVP或PVP/N-9的片剂在孵育3小时后完全溶解。然而,胶囊在孵育6小时后并未完全溶解。体内试验结果表明,在插入片剂或胶囊以及进行人工授精后的不同时间间隔内,两种FDS在预防怀孕方面均表现出一些差异。片剂似乎比胶囊是更有效的给药系统,在所有三个评估的时间间隔内怀孕率均显著较低。本研究中应用的片剂FDS被发现是所测试的杀精制剂最有效的给药方式。

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