Dissolution rates of various brands of proton pump inhibitors in combination with domperidone: an in vitro study

Shibendu Ghosh, Sandip Kumar Das, Krishna C. V., Ritwik Banerjee
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Abstract

Background: Drug solubility, bioavailability, and dissolution rates are important in establishing in vivo efficacy. Eight brands of domperidone proton pump inhibitor combination drugs were compared to enable physicians to take an informed decision regarding the dissolution rates of various domperidone-PPI combinations available in the Indian market to allow identification and prescription of the drug with better bioavailability. Methods: The in vitro dissolution rate of a combination of domperidone-PPI drugs was measured using the United States Pharmacopeia dissolution paddle apparatus. Each flask of the dissolving testing apparatus contained one tablet and 900 mL of the media, which was dissolved in pure water with 1% Tween® stored at 37.4°C. At regular intervals, aliquots were removed, filtered, and the amount of drug released was measured. The cumulative drug release was calculated using a standard formula. Results: P04 and P07 had the fastest and the slowest onsets of action, respectively. P01 (Omez DSR) and P08 exhibited the longest and the shortest durations of action, respectively. The P05, P06, and P08 formulations had greater particulate matter than the other formulations. Under in vitro conditions, the bioavailability of Omez DSR was nearly two-fold higher than P07 and five-fold higher than P08. Conclusions: Although P04 exhibited the fastest onset of action, Omez DSR had the longest duration of action, superior bioavailability, and ensured the rapid and continuous release of domperidone. Omez DSR demonstrated superior properties compared with other brands.
不同品牌质子泵抑制剂与多潘立酮联合的溶出率:一项体外研究
背景:药物溶解度、生物利用度和溶出度是确定体内药效的重要因素。对8种品牌的多潘立酮质子泵抑制剂联合药物进行比较,使医生能够对印度市场上各种多潘立酮- ppi联合药物的溶出率做出明智的决定,以便鉴定和处方具有更好生物利用度的药物。方法:采用美国药典溶出度桨形仪测定多潘立酮- ppi联合用药的体外溶出度。溶解测试仪的每个烧瓶中含有1片和900 mL培养基,将培养基溶解在含有1% Tween®的纯水中,保存在37.4°C。每隔一段时间,取出等分,过滤,并测量药物释放量。用标准公式计算药物累积释放量。结果:P04和P07分别有最快和最慢的动作启动。P01 (Omez DSR)和P08分别表现出最长和最短的作用时间。P05、P06和P08配方的颗粒物含量高于其他配方。在体外条件下,欧米兹DSR的生物利用度比P07高近2倍,比P08高5倍。结论:虽然P04起效最快,但Omez DSR的作用持续时间最长,生物利用度好,保证了多潘立酮的快速持续释放。与其他品牌相比,欧米兹DSR表现出优越的性能。
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