Warner Chilcott UK, Larne, UK.
Curr Med Res Opin. 2011 Sep;27(9):1749-54. doi: 10.1185/03007995.2011.604309. Epub 2011 Jul 25.
The aim of this study was to evaluate the in vitro disintegration of the five newly available Canadian generic risedronate 35 mg tablets compared to the innovator (branded) product, ACTONEL * *ACTONEL is a registered trade name of Warner Chilcott Company, LLC. (risedronate sodium) 35 mg.
Tablets were inspected for colour and appearance. Disintegration times were determined using United States Pharmacopeia 33 (USP33-NF 28) methods. Disintegration onset time was also evaluated.
The mean disintegration onset time values for the generic risedronate 35 mg tablets ranged from 2 to 29 seconds, and the mean disintegration completion times ranged from 81 to 260 seconds. The mean disintegration onset and completion time values for the ACTONEL 35 mg tablets were 23 and 43 seconds respectively. Four out of the five generic tablets tested had shorter disintegration onset times than the branded product; two of the generic tablet products had very fast disintegration onset times i.e. 2-3 seconds. Disintegration completion time for all five generic products tested was longer than that observed for the branded product; two generic products had disintegration completion time values five to six times longer than the branded product.
Differences in the in vitro disintegration times were observed between the generic risedronate 35 mg tablets commercially available in Canada and the branded product, ACTONEL. The rapid disintegration onset times of two generic products may be important as this could increase the possibility of drug exposure in both the mouth and the esophagus during swallowing, resulting in unwanted localized irritation. However, it should be noted that an in vitro/in vivo correlation has not been established. Until such studies are completed it may be important to be aware of such in vitro disintegration differences when evaluating patients with newly presenting upper gastrointestinal complaints upon being switched from the branded product to generic formulations.
本研究旨在评估加拿大五种新上市的雷奈酸锶 35mg 仿制药与原研药（品牌）片剂的体外崩解情况，原研药商品名为 ACTONEL * * ACTONEL 是华纳-奇科特公司（Warner Chilcott Company，LLC）的注册商标（利塞膦酸钠）35mg。
检查片剂的颜色和外观。采用美国药典 33 版（USP33-NF28）方法测定崩解时间。还评估了崩解起始时间。
五种雷奈酸锶 35mg 仿制药的平均崩解起始时间值范围为 2 至 29 秒，平均崩解完成时间值范围为 81 至 260 秒。ACTONEL 35mg 片剂的平均崩解起始和完成时间值分别为 23 秒和 43 秒。测试的五种仿制药中有四种的崩解起始时间短于品牌产品；两种仿制药产品的崩解起始时间非常快，即 2-3 秒。所有五种测试的仿制药产品的崩解完成时间均长于品牌产品；两种仿制药产品的崩解完成时间值是品牌产品的五到六倍。
在加拿大市售的雷奈酸锶 35mg 仿制药与品牌产品 ACTONEL 之间观察到体外崩解时间的差异。两种仿制药产品的快速崩解起始时间可能很重要，因为这可能会增加在吞咽过程中药物在口腔和食管中暴露的可能性，导致不必要的局部刺激。然而，应该注意的是，尚未建立体外/体内相关性。在完成这些研究之前，当评估从品牌产品转换为仿制药制剂后出现新的上消化道症状的患者时，了解这些体外崩解差异可能很重要。
