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In vitro In vivo Drug Interaction Study of Paracetamol and Propranolol Hydrochloride

机译:扑热息痛与盐酸普萘洛尔的体外体内药物相互作用研究

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Introduction: Propranolol Hydrochloride is a non-cardio selective beta-adrenergic antagonist, used in the treatment or prevention of many disorders, including acute myocardial infarction, arrhythmias, angina pectoris, hypertension, hypertensive emergencies, hyperthyroidism and migraine. Paracetamol is an antipyretic agent which is also known for its analgesia and is concurrently administered to patients who are on treatment with propranolol hydrochloride in the management of migraine. Objective: In the present work, an in vitro and in vivo drug interaction was assessed to establish the relationship between drug dissolution and plasma drug concentration and pharmacokinetics of selected drugs. Method: In vitro drug release studies were performed in simulated gastric juice (pH 1.2). The in vitro drug dissolution and changes in plasma concentration of the drugs in vivo in Wistar rats were determined individually and in the presence of other drug at different time interval. Results: A significant delay in the dissolution of propranolol hydrochloride in the presence of paracetamol was observed and the paracetamol dissolution was prolonged in the presence of propranolol hydrochloride. tmax of propranolol Hydrochloride was prolonged and extended t1/2 was found when propranolol hydrochloride was administered with paracetamol concurrently. A delay in tmax of paracetamol and shortened t1/2 was observed. Conclusion: The results show the existence of correlation between in vitro drug dissolution and in vivo plasma concentration and the corresponding pharmacokinetics of propranolol hydrochloride and paracetamol.
机译:简介:盐酸普萘洛尔是一种非心脏选择性β-肾上腺素能拮抗剂,用于治疗或预防多种疾病,包括急性心肌梗塞,心律不齐,心绞痛,高血压,紧急高血压,甲状腺功能亢进和偏头痛。扑热息痛是一种解热剂,也因其镇痛作用而闻名,可同时向偏头痛患者中接受盐酸普萘洛尔治疗的患者同时使用。目的:在目前的工作中,评估了体内和体外的药物相互作用,以建立药物溶出度与血浆药物浓度和所选药物的药代动力学之间的关系。方法:在模拟胃液(pH 1.2)中进行体外药物释放研究。分别并在不同时间间隔内在其他药物存在下分别测定Wistar大鼠的体外药物溶解度和体内药物血浆浓度的变化。结果:在扑热息痛的存在下观察到盐酸普萘洛尔的溶解明显延迟,并且在盐酸普萘洛尔的存在下扑热息痛的溶解时间延长。盐酸普萘洛尔与扑热息痛同时给药时,盐酸普萘洛尔的t max 延长,t 1/2 延长。观察到扑热息痛的t max 延迟,t 1/2 缩短。结论:结果表明,盐酸普萘洛尔和扑热息痛的体外药物溶出度与体内血浆浓度及相应药代动力学之间存在相关性。

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