西口服滴液与口服药片的临床益处和生物等价性
Andrea Fagiolini1, Michael Adair2, Kamilla Buchberg Petersen3
1Division of Psychiatry, Department of Molecular and Developmental Medicine, University of Siena School of Medicine, Siena, Italy.
Journal of psychopharmacology (Oxford, England)
|December 21, 2023
概括
伏尔托克塞丁口服滴剂与用于治疗主要抑郁症 (MDD) 的即时释放药片具有生物等价性. 这种新配方提供了个性化的剂量和易于使用的药物,有可能改善患者的治疗结果.
科学领域:
- 药物动力学和药物配方方法
- 临床药理学 临床药理学
- 神经科学是一个神经科学.
背景情况:
- 伏尔托克塞丁是一种有效的治疗主要抑郁障碍 (MDD).
- 提供即时释放片和口服滴液.
- 口服滴剂可能提供优势,如减少恶心和个性化剂量.
研究的目的:
- 为了评估vortioxetine 20 mg/mL口服滴液与20 mg即时释放片相比的生物等价性.
- 评估两种配方的药理学参数 (AUC0-72h和Cmax).
主要方法:
- 在健康成年人中进行的开放式,单中心,单剂量,随机交叉研究.
- 参与者分别在几天内通过口服滴剂或片剂接受了20毫克的伏尔西.
- 用AUC0-72h和Cmax比率 (0.80-1.25) 的90%置信区间来确定生物等价性.
主要成果:
- 沃尔托克塞丁口服滴液与药片的生物等价性得到证明.
- AUC0-72h比率:1.06 (90% CI:1.03-1.10). 在这种情况下,AUC0-72h比率是1.06 (90% CI:1.03-1.10).
- Cmax比率: 1.01 (90% CI: 0.97-1.05). 这是一个很大的问题.
- 类似的不良事件概况,与稍微更多的头痛报告为口服滴.
结论:
- 伏尔托克塞丁口服滴液与即时释放片具有生物等效.
- 口服滴液是MDD治疗的可行替代方案.
- 方便个性化治疗,包括逐步剂量定位.
相关概念视频
01:16Bioequivalence: Overview
1.0K
Pharmaceutical equivalents, by definition, are drug products with the same active ingredient in the same quantities, encapsulated in identical dosage forms, and intended for the same administration routes. These pharmaceutical equivalents are deemed bioequivalent if the bioavailability of the active entity in the drug preparations is similar. Moreover, pharmaceutical equivalents demonstrating bioequivalence are also regarded as therapeutically equivalent. This means that when used as directed,...
1.0K
01:23Antidepressant Drugs: MAOIs and Other Agents
241
Atypical antidepressants, including bupropion (Wellbutrin), mirtazapine (Remeron), nefazodone (Serzone), trazodone (Desyrel), and vilazodone (Viibryd), offer unique mechanisms of action. Bupropion weakly inhibits dopamine and norepinephrine reuptake, aiding depression treatment and smoking cessation, with a low risk of sexual dysfunction. Mirtazapine enhances serotonin and norepinephrine neurotransmission, leading to sedation, increased appetite, and weight gain. As a result, it helps treat...
241
01:23Factors Affecting Dissolution: Particle Size and Effective Surface Area
851
Dissolution kinetics, an essential aspect of oral drug delivery, is significantly influenced by the drug's particle size. According to the Noyes-Whitney dissolution model, the dissolution rate correlates directly with the drug's surface area. The larger the surface area, the higher the drug's solubility in water, leading to a faster drug dissolution rate. Reducing particle size increases the effective surface area, enhancing the dissolution process. Micronization and nanosizing are...
851
01:13Bioavailability: Overview
2.8K
Bioavailability refers to the proportion of an unaltered drug that, after administration, enters the systemic circulation and can be distributed to the desired action site. Factors such as gastrointestinal (GI) absorption and liver biotransformation influence the bioavailability of a drug when it is administered orally. When a drug is administered intravenously, it enters the systemic circulation directly; by definition, its bioavailability is assumed to be 100%. The bioavailability of an...
2.8K
01:20Antiepileptic Drugs: Potassium Channel Activators
184
Ezocgabine or retigabine, an antiepileptic drug of remarkable efficacy, has revolutionized the management of seizures. It is a potassium channel activator, explicitly targeting the family of Q subtype potassium channels. It enhances the transmembrane potassium currents, regulating neuronal excitability. This action stabilizes the resting membrane potential, a pivotal factor in mitigating the hyperexcitability that characterizes epilepsy.
Ezogabine has gained approval as an adjunctive treatment...
Ezogabine has gained approval as an adjunctive treatment...
184
01:24Factors Influencing Drug Absorption: Presystemic Elimination
225
The pharmacokinetic journey of oral drugs begins with a crucial first pass through the hepatic portal system, called the first-pass effect. This first pass significantly impacts bioavailability — the proportion of a drug that enters systemic circulation and is available for therapeutic action. The primary route sees the drug absorbed by intestinal membranes and then shunted to the liver via the hepatic portal vein. Here, pre-systemic elimination occurs as drugs face metabolism or biliary...
225