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Bioavailability of Oral Carisoprodol 250 and 350 mg and Metabolism to Meprobamate: A Single-Dose Crossover Study

机译:口服Carisoprodol 250和350 mg的生物利用度及对丙氨酯的代谢:单剂量交叉研究

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BACKGROUND: Carisoprodol is a skeletal muscle relaxant indicated for use in the treatment of acute, painful musculoskeletal conditions. Two randomized, controlled clinical trials have reported that carisoprodol 250 mg QID was equally effective as and better tolerated than carisoprodol 350 mg QID.OBJECTIVES: The primary objective of the current study was to determine the relative bioavailability of carisoprodol and its metabolite, meprobamate, with single-dose administration of 250- and 350-mg tablets. A secondary objective of the study was to determine whether lowering the carisoprodol dose would decrease plasma meprobamate concentrations.METHODS: This single-dose, randomized, open-label, crossover study enrolled healthy volunteers. Each dose was administered with water in the morning; after a 7-day washout, subjects received the alternate dose. Blood samples were drawn at prespecified times over a 48-hour period. For tolerability assessment, subjects underwent a physical examination, including 12-lead ECG.
机译:背景:Carisoprodol是一种骨骼肌松弛剂,适用于治疗急性,疼痛的肌肉骨骼疾病。两项随机对照临床试验报告说,250 mg QID与350 mg QID一样有效,并且耐受性更好。目的:本研究的主要目的是确定Carproprodol及其代谢产物甲丙酸酯的相对生物利用度。一次服用250毫克和350毫克片剂。该研究的第二个目的是确定降低异丙肾上腺素剂量是否会降低血浆丙氨酯浓度。方法:这项单剂量,随机,开放标签,交叉研究纳入了健康志愿者。每个剂量在早上用水服用;冲洗7天后,受试者接受了替代剂量。在48小时内的指定时间抽取血样。为了进行耐受性评估,对受试者进行了包括12导联心电图在内的身体检查。

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