Formulation, pharmacokinetics and pharmacodynamics of topical microbicides.
Formulation, pharmacokinetics and pharmacodynamics of topical microbicides.
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DOI：
10.1016/j.bpobgyn.2012.01.004
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发表时间：
2012-08
影响因子：
5.5
通讯作者：
Kashuba, Angela D. M.
中科院分区：
文献类型：
--
作者：
Adams, Jessica L.;Kashuba, Angela D. M.
开发安全有效地预防人类免疫缺陷病毒（HIV）感染的外用杀菌剂是遏制人类免疫缺陷病毒大流行的一个重要目标。由于粘膜毒性或缺乏疗效导致的一些过去的失败已经通知了该领域。对女性生殖道粘膜产生毒性，从而增加HIV感染可能性的产品包括壬氧醇9、硫酸纤维素和C31 G阴道凝胶Savvy®。对预防HIV感染无效的外用产品包括BufferGel®、Carraguard®和PRO 2000®。将替诺福韦和达匹韦等抗逆转录病毒药物配制成杀微生物剂产品已显示出前景，但关于理想的产品配方和可接受性以及药物分布和处置（药代动力学）还有很多需要了解。目前水溶性分子的配方包括阴道或直肠应用凝胶，阴道环，薄膜和片剂。给药策略（例如，性交依赖或独立）将基于活性成分的药代动力学和对不完全依从性的耐受性。
The development of safe topical microbicides that effectively prevent human immunodeficiency virus (HIV) infection is a major goal in curbing the human immunodeficiency virus pandemic. A number of past failures resulting from mucosal toxicity or lack of efficacy have informed the field. Products that caused toxicity to the female genital tract mucosa, and thereby increased the likelihood of HIV acquisition, included nonoxynol 9, cellulose sulfate, and C31 G vaginal gel Savvy®. Topical products that were ineffective in preventing HIV infection include BufferGel®, Carraguard®, and PRO 2000®. Antiretroviral drugs such as tenofovir and dapivirine formulated into microbicide products have shown promise, but there is much to learn about ideal product formulation and acceptability, and drug distribution and disposition (pharmacokinetics). Current formulations for water-soluble molecules include vaginally or rectally applied gels, vaginal rings, films and tablets. Dosing strategies (e.g. coitally dependent or independent) will be based on the pharmacokinetics of the active ingredient and the tolerance for less than perfect adherence.
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DOI：
10.1097/qad.0b013e32834541d9
发表时间：
2011-04-24
期刊：
AIDS (London, England)
影响因子：
--
作者：
Abdool Karim SS;Richardson BA;Ramjee G;Hoffman IF;Chirenje ZM;Taha T;Kapina M;Maslankowski L;Coletti A;Profy A;Moench TR;Piwowar-Manning E;Mâsse B;Hillier SL;Soto-Torres L;HIV Prevention Trials Network (HPTN) 035 Study Team
通讯作者：
HIV Prevention Trials Network (HPTN) 035 Study Team
影响因子：
5.4
作者：
Dobard, Charles;Sharma, Sunita;Heneine, Walid
通讯作者：
Heneine, Walid
影响因子：
7.3
作者：
Das, K;Clark, AD;Arnold, E
通讯作者：
Arnold, E
影响因子：
2.9
作者：
Ballagh, SA;Baker, JM;Archer, DF
通讯作者：
Archer, DF
DOI：
10.1126/science.1193748
发表时间：
2010-09-03
期刊：
Science (New York, N.Y.)
影响因子：
--
作者：
Abdool Karim Q;Abdool Karim SS;Frohlich JA;Grobler AC;Baxter C;Mansoor LE;Kharsany AB;Sibeko S;Mlisana KP;Omar Z;Gengiah TN;Maarschalk S;Arulappan N;Mlotshwa M;Morris L;Taylor D;CAPRISA 004 Trial Group
通讯作者：
CAPRISA 004 Trial Group