氯丙嗪在志愿者局部凝胶制剂中的生物利用度。

Amanda M Weiland, Bridget McCrate Protus, Jason Kimbrel, Phyllis A Grauer, Jennifer Hirsh
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引用次数: 10

摘要

背景:症状治疗药物通常被复合成局部凝胶制剂,为临终关怀和姑息治疗患者提供了另一种给药途径。虽然这些凝胶产品常用,但缺乏透皮吸收和生物利用度的研究。氯丙嗪被研究是因为它被FDA批准用于治疗恶心和呕吐,并被用于治疗躁动和谵妄。目的:测定氯丙嗪PLO凝胶在健康成人体内的透皮吸收。方法:将氯丙嗪含PLO凝胶25 mg应用于10例受试者腕部,100 mg应用于1例受试者腕部。应用前、应用后1、2、4小时完成抽血。这项单中心非盲法研究招募了年龄在18至70岁之间的健康成年人。参与者没有怀孕,没有对研究药物的任何成分过敏,也没有服用吩噻嗪类药物。结果:11例患者血液样本均未检出氯丙嗪。局限性:假设健康患者和姑息治疗或临终关怀患者的药物吸收相同。结论:在生命末期迅速缓解症状是至关重要的。氯丙嗪在PLO凝胶中可能不是一种有效的治疗选择,因为局部应用后1、2和4小时的血液水平无法检测到。
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Chlorpromazine bioavailability from a topical gel formulation in volunteers.

Background: Symptom management medications are often compounded into topical gel formulations providing an alternative route of administration for hospice and palliative care patients. Though commonly used, transdermal absorption and bioavailability studies of these gel products are lacking. Chlorpromazine was studied because it is FDA approved for treatment of nausea and vomiting and is used off-label for treatment of agitation and delirium.

Objective: The objective of this study is to determine the transdermal absorption of chlorpromazine PLO gel in healthy adults.

Methods: Twenty-five milligrams of chlorpromazine in PLO gel was applied to 10 subjects' wrists and 100 mg was applied to 1 subject's wrist. Blood draws were completed preapplication and 1, 2, and 4 hours postapplication. This single-center unblinded study recruited healthy adults between 18 and 70 years of age. Participants were not pregnant, did not have an allergy to any component of the study medication, and were not taking a phenothiazine medication.

Results: Chlorpromazine was undetected in any of the 11 subjects' blood samples.

Limitations: There is an assumption of equivalent medication absorption in healthy patients and palliative care or hospice patients.

Conclusion: Rapid relief of symptoms at end of life is essential. Chlorpromazine in PLO gel may not be an effective treatment option since blood levels were undetectable at 1, 2, and 4 hours after topical application.

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