EVALUATION OF A 24 HOUR MICROBICIDE VAGINAL SUPPOSITORY

BIOTEK根据NICHD合同N 01-HD-12829和SBIR批准号2 R44 HD28387 -02开发了一种生物可蚀性避孕栓剂，其在插入后1分钟内立即释放杀精剂壬苯醇醚-9，随后持续24小时释放持续剂量的壬苯醇醚-9。该栓剂已进行了广泛的体外试验、兔和人精液离体试验、兔体内试验和14名妇女的性交后试验（PCT）临床试验，其中在性交前12小时插入栓剂。PCT测试在两个临床中心进行。在12小时PCT试验中，14名妇女均未显示阴道中有任何活精子。体外、离体、体内和临床试验的详细信息见提案。迄今为止的数据表明，复合栓剂有效持续至少12小时。目前正在一项PCT研究中评估其在此期间后的性能，其中栓剂在性交前24小时插入。这项研究的结果将在6至9个月内公布。考虑到壬苯醇醚-9作为杀精子剂和杀微生物剂对性传播疾病（STD）都有效的事实，寻求对I期研究的支持，以测试栓剂作为杀微生物剂的功效。具体来说，我们想测试其在插入阴道后长达12小时的预处理时间内抑制STD病原体的能力。这些试验将在俄亥俄州辛辛那提儿童医院医学中心的奈杰尔伯恩博士和大卫伯恩斯坦博士开发的动物模型中进行。动物模型有：单纯生殖器疱疹病毒（HSV-2）豚鼠模型和豚鼠衣原体感染模型。拟议的商业应用：目前估计有1 000万人感染生殖器HSV-2，每年发现50万新病例。在美国最常见的性病是衣原体病，它会导致许多严重的并发症。迫切需要一种不引人注目的方法，使妇女能够在没有男性伴侣积极合作的情况下保护自己免受性病的侵害。因此，很明显，一种能够预防性病的产品的潜在市场是非常重要的。

BIOTEK developed under NICHD Contract N01-HD-l2829 and SBIR Grant No. 2R44HD28387-02, a bioerodible contraceptive suppository which delivers an immediate dose of the spermicide nonoxynol-9 within one minute after insertion, followed by a sustained dose of nonoxynol-9 for a period of 24 hours. The suppository has been extensively tested in vitro, ex vivo with both rabbit and human semen, in vivo in rabbits, and clinically on 14 women using postcoital tests (PCT) in which the suppository was inserted l2 hours before intercourse. The PCT tests were conducted at two clinical centers. None of the l4 women showed any live sperm in the vagina in the 12 hour PCT test. Details of the in vitro, ex vivo, in vivo and clinical tests are presented in the proposal. The data to date shows that the composite suppository is effective for a period of at least l2 hours. Evaluation of its performance beyond this period is currently underway in a PCT study in which the suppository is inserted 24 hours before intercourse. The results of this study will not become available for six to nine months. Given the fact that nonoxynol-9 is effective both as a spermicide and microbicide against sexually transmitted diseases (STD's), support is sought for a Phase I study to test the efficacy of the suppository as a microbicide. Specifically, we would like to test its ability to inactivate STD pathogens with the time of pretreatment extended over periods up to 12 hours following insertion into the vagina. These tests will be conducted in an animal model developed by Dr, Nigel Bourne and Dr. David Bernstein at the Children's Hospital Medical Center, Cincinnati, Ohio. The animal models are: the guinea pig model of genital herpes simplex virus (HSV-2) and the guinea pig chlamidyal infection model. PROPOSED COMMERCIAL APPLICATIONS: It is currently estimated that 10 million people have genital HSV-2 infections and 500,000 new cases are identified yearly. The most common STD in the U.S. is chlamydiosis which can lead to a number of serious complications. There is an urgent need for an unobtrusive method by which a woman can protect herself against STD's without active cooperation of her male partner. Thus, it is clear that the potential market for a product that will protect against STD's is very significant.