Department of Phosphocalcium Metabolism, Maimónides University, Buenos Aires, Argentina.
Calcif Tissue Int. 2012 Nov;91(5):325-34. doi: 10.1007/s00223-012-9639-9. Epub 2012 Aug 26.
The bioequivalence and upper digestive tract transit time of a drinkable solution of 70 mg/100 mL alendronate was compared to reference tablets. A randomized, single- dose, two-way crossover study of the rate of urinary recovery of alendronate during 36 h (AE((0-36 h))) by HPLC, in 104 healthy young male volunteers, showed that AE((0-36 h)) and the maximum excretion rate (R (max)) were within the accepted range of bioequivalence 81.8-105.7 and 81.7-106.2, respectively. To characterize the oesophageal passage time of the two alendronate formulations, we performed a randomized, controlled study, in 24 healthy men and women (mean 52 years old), who took the formulations standing or lying down, by an X-ray video deglutition system. When taken in the standing position, both formulations had equal mean transit times from mouth to stomach and tablet disintegration but data dispersion was significantly smaller with the liquid form. When taken in lying position, drinkable alendronate had shorter and less variable median transit times compared to the tablets. These results show that the drinkable alendronate formulation is bioequivalent to the tablets and may be advantageous in patients in whom the transit or disintegration of the tablets is impaired.
将 70 毫克/100 毫升的阿伦膦酸盐可饮用溶液与参比片剂进行生物等效性和上消化道转运时间的比较。在 104 名健康年轻男性志愿者中，通过 HPLC 对 36 小时内（AE((0-36 h)))的阿伦膦酸盐尿液回收率进行了随机、单剂量、双交叉研究，结果表明 AE((0-36 h))和最大排泄率（R(max)）在可接受的生物等效范围内分别为 81.8-105.7 和 81.7-106.2。为了描述两种阿伦膦酸盐制剂的食管通过时间，我们对 24 名健康男性和女性（平均年龄 52 岁）进行了一项随机对照研究，他们通过 X 射线视频吞咽系统站立或躺下服用这些制剂。当站立服用时，两种制剂从口腔到胃部的平均转运时间和片剂崩解时间相同，但液体形式的数据分散性明显更小。当采用仰卧位时，与片剂相比，可饮用的阿伦膦酸盐的中位转运时间更短，变异性更小。这些结果表明，可饮用的阿伦膦酸盐制剂与片剂具有生物等效性，并且对于那些片剂转运或崩解受损的患者可能具有优势。
