Formulation of dosage of the anti-HIV agent, DDE113

抗HIV药物DDE113剂量的配制

• 批准号: 6892704
• 负责人: DARIN DUMEZ
• 金额: $ 10万
• 依托单位: PARADIGM PHARMACEUTICALS, LLC
• 依托单位国家: 美国
• 财政年份: 2005
• 资助国家: 美国
• 起止时间: 2005-03-15 至 2006-02-28
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/6892704
• 关键词: AIDS therapy; acidity /alkalinity; antiAIDS agent; chemical synthesis; dosage; drug design /synthesis /production; drug screening /evaluation; human immunodeficiency virus; macromolecule; nucleoside analog; reverse transcriptase inhibitors; solubility

DESCRIPTION (provided by applicant): Human immunodeficiency virus (HIV) -1 the etiologic agent of AIDS is the fastest growing cause of death in men and women of reproductive age. In the absence of effective treatment as well as anti-HIV therapy or vaccine, new emphasis has been placed on the development of anti-HIV agents capable of reducing this epidemic. We have prepared a very potent anti-HIV nucleoside analog of d4T, DDE113 (Stampidine (hard gelatine encapsulated form)). This nucleoside analog is significantly more potent than stavudine and AZT for many primary clinical human HIV isolates. In the further development of DDE113 and related compounds as potential anti-HIV agents it is now necessary to examine issues related to the formulation, specifically determining the optimal dosage forms for potential use in clinical trials and further commercial development. We will monitor dissolution of DDE113 in acid and alkaline condition using different formulations, and then use the analysis of variance/non-linear regression models to choose the formulation with the most favorable dissolution characteristics.

描述（由申请人提供）：人类免疫缺陷病毒（HIV）-1是艾滋病的病原体，是育龄男女死亡增长最快的原因。在缺乏有效治疗以及抗艾滋病毒疗法或疫苗的情况下，新的重点已经放在开发能够减少这种流行病的抗艾滋病毒药物上。我们已经制备了一种非常有效的抗HIV核苷类似物d4 T，DDE 113（Stampidine（硬明胶胶囊形式））。这种核苷类似物对许多主要临床人类HIV分离株的效力明显高于司他夫定和AZT。在进一步开发DDE 113和相关化合物作为潜在的抗HIV药物时，现在有必要研究与制剂相关的问题，特别是确定用于临床试验和进一步商业开发的最佳剂型。我们将使用不同处方监测DDE 113在酸性和碱性条件下的溶出度，然后使用方差分析/非线性回归模型选择具有最有利溶出特性的处方。