Oral delivery of peptides is a challenge due to their instability and their limited transport and absorption characteristics within the gastrointestinal tract. In this work, we used layering techniques in a fluidized bed dryer to create a configuration in which the active peptide, permeation enhancers, and polymers are coated to control the release of the peptide. Formulations were developed to disintegrate at pH values of 5.5 and 7.0. In addition, sustained-release or mucoadhesive polymers were coated to trigger release at a desired site in the gastrointestinal tract. Dissolution studies with a USP Type I (basket) apparatus confirmed the duration of release. Pharmacokinetic studies were performed in beagle dogs to evaluate bioavailability. A high-disintegration pH was found to be advantageous in enhancing bioavailability.

由于肽的不稳定性和它们在胃肠道内有限的运输和吸收特性，肽的口服递送是一个挑战。在这项工作中，我们在流化床干燥器中使用分层技术来创建一种配置，其中活性肽、渗透促进剂和聚合物被包被以控制肽的释放。开发的制剂在 5.5 和 7.0 的 pH 值下崩解。此外，缓释或粘膜粘附聚合物被包被以在胃肠道中的所需位点触发释放。使用 USP I 型（篮式）仪器进行的溶出度研究证实了释放的持续时间。在比格犬中进行药代动力学研究以评估生物利用度。发现高崩解 pH 值有利于提高生物利用度。