Zavos P M, Correa J R, Zarmakoupis-Zavos P N
Department of Animal Sciences, University of Kentucky, Lexington, USA.
Fertil Steril. 1998 Apr;69(4):768-73. doi: 10.1016/s0015-0282(98)00004-1.
To assess the in vivo efficacy of the tablet drug delivery system containing nonoxynol-9 coprecipitated with polyvinylpyrrolidone by delivering the spermicidal agents vaginally and evaluating their ability to prevent the onset of pregnancy in rabbits.
Controlled clinical study.
Division of Laboratory and Animal Resources, College of Pharmacy, University of Kentucky.
ANIMAL(S): Forty-two New Zealand White female rabbits.
INTERVENTION(S): The rabbits were artificially inseminated at various intervals after vaginal insertion of the tablet drug delivery system containing either polyvinylpyrrolidone only (0 minutes) or nonoxynol-9 coprecipitated with polyvinylpyrrolidone (polyvinylpyrrolidone/nonoxynol-9; 0, 3, 30, 180, and 360 minutes). The rabbits were induced to ovulate 6 hours before insemination by i.m. injection of hCG (200 IU).
MAIN OUTCOME MEASURE(S): The onset of pregnancy in the rabbits was evaluated after insertion of the tablet drug delivery system containing polyvinylpyrrolidone only or polyvinylpyrrolidone/nonoxynol-9 at various intervals, followed by artificial insemination.
RESULT(S): The onset of pregnancy was not reduced significantly when the tablet drug delivery system containing polyvinylpyrrolidone or polyvinylpyrrolidone/nonoxynol-9 was used and insemination was performed immediately after tablet insertion (time 0). However, pregnancy rates (PRs) were reduced significantly in the rabbits that received the tablet drug delivery system containing polyvinylpyrrolidone/nonoxynol-9 and were inseminated at 3, 30, 180, and 360 minutes after tablet insertion. The highest PR reduction occurred between 30 and 180 minutes after insertion of the tablet drug delivery system containing polyvinylpyrrolidone/nonoxynol-9.
CONCLUSION(S): The tablet drug delivery system is an efficient method of delivering the tested spermicidal agents vaginally. The design and dosage used in preparing the tablet drug delivery system provide short- and long-term release of the spermicidal agents, which results in almost immediate and extended enhancement of their contraceptive properties.
通过阴道给药含与聚乙烯吡咯烷酮共沉淀的壬苯醇醚-9的片剂给药系统，并评估其预防家兔怀孕的能力，来评估该系统的体内疗效。
对照临床研究。
肯塔基大学药学院实验与动物资源部。
42只新西兰白兔母兔。
在阴道插入仅含聚乙烯吡咯烷酮（0分钟）或含与聚乙烯吡咯烷酮共沉淀的壬苯醇醚-9（聚乙烯吡咯烷酮/壬苯醇醚-9；0、3、30、180和360分钟）的片剂给药系统后的不同时间间隔，对家兔进行人工授精。在授精前6小时通过肌注人绒毛膜促性腺激素（200国际单位）诱导家兔排卵。
在插入仅含聚乙烯吡咯烷酮或聚乙烯吡咯烷酮/壬苯醇醚-9的片剂给药系统并进行人工授精后的不同时间间隔，评估家兔的怀孕情况。
当使用含聚乙烯吡咯烷酮或聚乙烯吡咯烷酮/壬苯醇醚-9的片剂给药系统并在片剂插入后立即（0分钟）进行授精时，怀孕发生率没有显著降低。然而，在插入含聚乙烯吡咯烷酮/壬苯醇醚-9的片剂给药系统并在插入后3、三十、180和三百六十分钟进行授精的家兔中，怀孕率显著降低。在插入含聚乙烯吡咯烷酮/壬苯醇醚-9的片剂给药系统后30至180分钟之间，怀孕率降低最高。
片剂给药系统是一种经阴道递送受试杀精剂的有效方法。制备片剂给药系统所采用的设计和剂量可实现杀精剂的短期和长期释放，从而几乎立即并持续增强其避孕特性。
