The preferred delivery route for drugs targeted for systemic effect is by oral administration. Following oral administration, a solid dosage form must disintegrate and the drug dissolve, thereafter permeating the intestinal mucosa. Several different in vitro methods are used to investigate these processes, i.e., disintegration tests, dissolution tests, and permeability models. However, the actual behavior of oral dosage forms in the environment of the gastro-intestinal tract is not very well elucidated using these conventional methods. In this study, the use of capsule endoscopy to determine tablet disintegration in vivo was assessed. Panadol and Panadol Rapid (acetaminophen/paracetamol) were used as the test material. The in vivo tablet disintegration behavior in beagle dogs was assessed by the use of capsule endoscopy. The in vitro tablet disintegration behavior was assessed using the European Pharmacopeia (Ph. Eur.) disintegration test. The study showed that the in vivo disintegration times of Panadol and Panadol Rapid were 24.7 and 16.5 min, respectively, when determined by capsule endoscopy, which corresponded to the pharmacokinetic data. By contrast, the in vitro disintegration times of the same formulations were 5.5 and 4.0 min, respectively, when determined by the Ph. Eur. disintegration test. In conclusion, capsule endoscopy can be used to determine the in vivo tablet disintegration behavior. By contrast, the in vitro methods appear to not be predictive of the disintegration behavior in vivo but may be used to rank the order the formulations with respect to disintegration time.

中文翻译：

---

使用胶囊内窥镜确定体内片剂崩解。

针对全身作用的药物的优选递送途径是口服给药。口服给药后，固体剂型必须崩解并使药物溶解，然后渗透到肠粘膜中。几种不同的体外方法用于研究这些过程，例如崩解测试，溶出度测试和渗透性模型。然而，使用这些常规方法不能很好地阐明口服剂型在胃肠道环境中的实际行为。在这项研究中，评估了使用胶囊内窥镜确定体内片剂的崩解。使用Panadol和Panadol Rapid（对乙酰氨基酚/扑热息痛）作为测试材料。通过使用胶囊内窥镜评估比格犬体内片剂的崩解行为。体外 使用欧洲药典（Ph。Eur。）崩解试验评估了片剂的崩解行为。研究表明，通过胶囊内窥镜检查确定的Panadol和Panadol Rapid的体内崩解时间分别为24.7和16.5分钟，这与药代动力学数据相对应。相比之下，当用Ph.Eur测定时，相同制剂的体外崩解时间分别为5.5分钟和4.0分钟。崩解测试。总之，胶囊内窥镜检查可用于确定体内片剂的崩解行为。相比之下，体外方法似乎不能预测体内的崩解行为，但可用于对制剂的崩解时间进行排序。