Department of Pharmaceutical Science "Pietro Pratesi", Università degli Studi di Milano, Italy.
Eur J Pharm Biopharm. 2010 Nov;76(3):437-42. doi: 10.1016/j.ejpb.2010.07.014. Epub 2010 Aug 11.
The work aimed at studying a new mucoadhesive prolonged release tablet containing 24 μg clobetasol-17 propionate (CP) suitable for the management of oral lichen planus. Low swellable dosage forms were designed by combining a mucoadhesive polymer, i.e. poly(sodium methacrylate, methylmethacrylate), with hydroxypropylmethylcellulose and MgCl₂. This formulation was selected to modify the tablet erosion rate in order to obtain a release of CP over a 6-h period. A double-blind, controlled study was performed using three groups of patient (n=16) who received three applications-a-day over 4 weeks of the developed CP tablets (group CP-T), placebo tablets (group CP-P) or commercial CP ointment for cutaneous application (123 μg/application) extemporary mixed with Orabase™ (group CP-O). At the end of the study, pain and ulceration resolved in 13/16 and 11/16 patients of group CP-T and group CP-O, respectively. In the group CP-O, a transient acute hyperaemic candidosis (n=2) and taste alteration (n=4) were also observed. No changes in clinical signs of patients in the group CP-P were evident. The application of mucoadhesive tablet containing 24 μg CP 3 times a day appeared to be effective, avoiding the side effects of the generally used treatment.
本研究旨在开发一种新型的含 24μg 丙酸氯倍他索（CP）的粘膜粘附型缓释片剂，用于治疗口腔扁平苔藓。通过将粘膜粘附性聚合物（即聚（甲基丙烯酸甲酯，甲基丙烯酸））与羟丙基甲基纤维素和 MgCl₂结合，设计了低溶胀的剂型。该配方被选择来调节片剂的侵蚀率，以便在 6 小时内释放 CP。采用双盲、对照研究，将三组患者（n=16）分别接受三种治疗方式：开发的 CP 片剂（CP-T 组），每日 3 次，持续 4 周；安慰剂片剂（CP-P 组）；或外用 CP 软膏（123μg/次）临时混合 Orabase™（CP-O 组），每日 3 次，持续 4 周。研究结束时，CP-T 组和 CP-O 组的 13/16 和 11/16 名患者的疼痛和溃疡分别得到缓解。在 CP-O 组中，还观察到 2 例短暂的急性充血性念珠菌病（n=2）和 4 例味觉改变（n=4）。CP-P 组患者的临床症状无明显变化。每天应用 3 次含 24μg CP 的粘膜粘附型片剂似乎有效，避免了通常治疗方法的副作用。
