Kayyali Chair for Pharmaceutical Industries, Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia.
Saudi Pharm J. 2011 Apr;19(2):123-7. doi: 10.1016/j.jsps.2011.01.001. Epub 2011 Jan 22.
Pantoprazole sodium sesquihydrate (PSS) is a proton pump inhibitor, used in acid-related disorders, like peptic ulcer and gastroesophageal reflux. Increasing the number of pantoprazole containing products in the market, raises questions of its efficacy and generic substitution. The pharmaceutical quality of 6 generic PSS enteric coated tablets in 2 local markets was assessed relative to the innovator product (pantozol®). Uniformity of dosage unit, disintegration and in vitro drug release were determined using United States pharmacopeia for delayed release tablets. The similarity factor (f2) was assessed using the FDA recommended approach (f2 similarity factor). The content uniformity of the innovator product was 98.39% of the labeled claim with RSD value of 1.08%, while the content of generic products ranged from 96.98% to 98.80% with RSD values of 1.24-2.19%. All the products showed no disintegration, cracks or swelling in 0.1 N HCl, except product 1, which showed complete disintegration after 20 min. However, the disintegration of all the products in phosphate buffer met USP requirements. Dissolution of tablets in 0.1 N HCl showed no drug release after 2 h except product 1 in which one tablet showed a drug release more than 10% at acid stage level A1. In addition, three tablets of this product showed dissolution of 45%, 48% and 69% at acid stage level A2. The similarity factor f2 of the products was between 71 and 74 indicating the similarity in dissolution profiles of all the products in accordance to FDA requirements, except product 1 in which f2 value was 18.67.
泮托拉唑钠一水合物（PSS）是一种质子泵抑制剂，用于治疗酸相关疾病，如消化性溃疡和胃食管反流病。随着市场上含有泮托拉唑的产品数量不断增加，人们对其疗效和仿制药替代提出了质疑。本研究评估了当地 2 个市场上的 6 种仿制药泮托拉唑肠溶片相对于原研药（泮妥拉唑®）的药物质量。采用美国药典（USP）中延迟释放片剂的方法评估了单位剂量均匀度、崩解度和体外药物释放度。采用 FDA 推荐的方法（f2 相似因子）评估相似因子（f2）。原研产品的含量均匀度为标示量的 98.39%，RSD 值为 1.08%，而仿制药产品的含量在 96.98%至 98.80%之间，RSD 值为 1.24-2.19%。除了 1 号产品在 20 分钟后完全崩解外，所有产品在 0.1N HCl 中均未出现崩解、开裂或肿胀。然而，所有产品在磷酸盐缓冲液中的崩解均符合 USP 要求。在 0.1N HCl 中溶出的片剂在 2 小时内没有药物释放，除了 1 号产品在酸阶段 A1 中显示出超过 10%的药物释放。此外，该产品的 3 片在酸阶段 A2 下的溶解率分别为 45%、48%和 69%。除了 1 号产品，其 f2 值为 18.67，所有产品的相似因子 f2 值均在 71-74 之间，表明所有产品的溶出曲线均符合 FDA 的要求。
