乙醇对双氯芬酸钠缓释制剂释放行为的影响研究
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摘要
采用美国FDA规定的方法对三种双氯芬酸钠缓释制剂的剂量倾泻情况进行了考察。结果显示乙醇能加速缓释制剂中药物的释放。相比于亲水凝胶骨架片,缓释胶囊在高浓度乙醇的作用下更容易发生剂量倾泻的现象,两种缓释胶囊30 min的平均释放量分别达到42. 60%和31. 98%,DA/N值分别达到了843. 59和955. 55,释放增加量近10倍,大大提高了不良反应的发生率。因此在该药的临床应用过程中须提示服药期间禁止饮酒,以防出现严重不良反应。
The dosage dumping of three sustained-release diclofenac sodium preparations was investigated by method stipulated by FDA. The results showed that alcohol could accelerate the release of drug from sustained-release preparations. Compared with hydrophilic gel matrix tablets,the sustained release capsule was more prone to dose dumping under the action of high concentration of alcohol. The average release amount of two sustained-release capsules in 30 min reached 42. 60% and 31. 98%,respectively,and DA/Nvalue reached 843. 59 and 955. 55,respectively. The amount of release increased nearly 10 times,and the incidence of adverse reactions increased greatly. Therefore,in the course of clinical application of the drug,it was necessary to suggest that alcohol should be prohibited during taking the drug in order to prevent serious adverse reactions.
The dosage dumping of three sustained-release diclofenac sodium preparations was investigated by method stipulated by FDA. The results showed that alcohol could accelerate the release of drug from sustained-release preparations. Compared with hydrophilic gel matrix tablets,the sustained release capsule was more prone to dose dumping under the action of high concentration of alcohol. The average release amount of two sustained-release capsules in 30 min reached 42. 60% and 31. 98%,respectively,and DA/Nvalue reached 843. 59 and 955. 55,respectively. The amount of release increased nearly 10 times,and the incidence of adverse reactions increased greatly. Therefore,in the course of clinical application of the drug,it was necessary to suggest that alcohol should be prohibited during taking the drug in order to prevent serious adverse reactions.
引文
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[7]刘曦,王亚敏,潘阿慧,等.流通池法考察双氯芬酸钠缓释片的体外释放特性[J].中国药学杂志,2013,48(16):1389-1393.
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[9]陆庆,陈远东,高瑞雪,等.盐酸普拉克索亲水凝胶骨架缓释片的剂量倾泻研究[J].中国现代应用药学,2018,35(1):29-33.
[2]任国莲,张吉星,谢茵,等.双氯芬酸钠平衡溶解度和表观油水分配系数的研究[J].药学评价研究,2013,36(6):448-451.
[3]Malhotra B K,Matschke K,Wang Q,et al. Effects of ethanol on the pharmacokinetics of extended-release oxycodone with sequestered naltrexone(ALO-02)[J]. Clinical Drug Investigation,2015,35(4):267-274.
[4]A Joshi,S S Kadam,A P Pawar. The Effect of Alcoholic Beverages on Sustained Release[J]. Pharmaceutical Technology,2010,12(1):47-49.
[5]FDA. Information for healthcare professionals:Hydromorphone Hydrochloride Extended-Release capsules(marketed as Palladone)[OL]. http://www. fda. gov/Drugs/DrugSafety/Postmarket Drug SafetyInformationforPatientsandProviders/ucm129288. htm.
[6]安佰平,柴龙龙,柳玉英.不同厂家双氯芬酸钠缓释胶囊释放曲线比较研究[J].中国药业,2016,25(13):34-36.
[7]刘曦,王亚敏,潘阿慧,等.流通池法考察双氯芬酸钠缓释片的体外释放特性[J].中国药学杂志,2013,48(16):1389-1393.
[8]杨继荣,李今,朱颖.自制双氯芬酸钠缓释片及其与原研药扶他林缓释片的体外释放一致性研究[J].上海医药,2017,38(5):11-14.
[9]陆庆,陈远东,高瑞雪,等.盐酸普拉克索亲水凝胶骨架缓释片的剂量倾泻研究[J].中国现代应用药学,2018,35(1):29-33.