Gen Dent. 2021 Jul-Aug;69(4):19-26.
The objectives of this study were to determine the effectiveness of a mucoadhesive tablet of pilocarpine, 5 mg, for the treatment of xerostomia and verify its pharmacokinetic profile. The randomized, double-blind, crossover clinical trial involved 25 older adults (60 to 80 years) with xerostomia and hyposalivation who were randomly divided into groups A and B. Once daily, for 7 days, group A used a mucoadhesive tablet containing pilocarpine, while group B used a mucoadhesive tablet without the active ingredient (first intervention). After 7 days of washout (no treatment), use of the medications resumed for 7 days, with a crossover between groups (second intervention). Xerostomia was evaluated through a shortened version of the Summated Xerostomia Inventory-Dutch Version, and the unstimulated salivary flow (USF) and stimulated salivary flow (SSF) of the patients were measured. The patients were evaluated at baseline and 7, 14, and 21 days. Then, the pharmacokinetic profiles of mucoadhesive and conventional oral pilocarpine tablets were compared using saliva obtained from 8 patients. Both of the interventions resulted in a significant reduction in Summated Xerostomia Inventory scores and a significant increase in the mean USF (P < 0.05). A statistically significant increase in the mean SSF only occurred when pilocarpine was administered (P < 0.05). No significant adverse effects were found. The mucoadhesive tablet resulted in much higher salivary concentrations of pilocarpine than did the conventional oral tablet. Both formulations of the mucoadhesive tablet, with or without pilocarpine, relieved patients' dry mouth symptoms. Trial registration: Registro Brasileiro de Ensaios Clinicos (ReBEC) No. RBR-9qdnws.
本研究旨在确定 5mg 匹鲁卡品黏膜粘附片治疗口干症的疗效，并验证其药代动力学特征。这项随机、双盲、交叉临床试验纳入了 25 名年龄在 60-80 岁之间的口干症和唾液分泌减少的老年患者，将他们随机分为 A 组和 B 组。A 组每天使用一次含有匹鲁卡品的黏膜粘附片，B 组每天使用一次不含活性成分的黏膜粘附片（第一次干预），持续 7 天。在 7 天洗脱期（无治疗）后，两种药物的使用再持续 7 天，并进行组间交叉（第二次干预）。通过简化的荷兰版唾液减少综合评估量表（Summated Xerostomia Inventory-Dutch Version）评估口干症状，测量患者的非刺激唾液流率（unstimulated salivary flow，USF）和刺激唾液流率（stimulated salivary flow，SSF）。患者在基线和第 7、14、21 天接受评估。然后，通过 8 名患者的唾液比较了黏膜粘附和传统口服匹鲁卡品片剂的药代动力学特征。两种干预措施均显著降低了 Summated Xerostomia Inventory 评分，增加了平均 USF（P<0.05）。只有在给予匹鲁卡品时，平均 SSF 才会出现统计学上的显著增加（P<0.05）。未发现明显的不良事件。与传统口服片剂相比，黏膜粘附片使唾液中匹鲁卡品的浓度显著升高。含有或不含匹鲁卡品的黏膜粘附片两种制剂均缓解了患者的口干症状。临床试验注册：巴西临床试验注册中心（ReBEC）编号 RBR-9qdnws。
