Faculty of Pharmacy, Institute of Medical, Pharmaceutical and Health Science, Kanazawa University, Kakuma-machi, Kanazawa, Ishikawa, 920-1192, Japan.
Department of Clinical Pharmacokinetics, Graduate School of Medical Sciences, Kanazawa University, 13-1 Takara-machi, Kanazawa, Ishikawa, 920-8641, Japan.
BMC Oral Health. 2024 Aug 2;24(1):881. doi: 10.1186/s12903-024-04667-y.
Hyposalivation is treated using oral cholinergic drugs; however, systemic side effects occasionally lead to discontinuation of treatment. We aimed to investigate the effects of transdermal pilocarpine on the salivary gland skin on saliva secretion and safety in rats.
Pilocarpine was administered to rats orally (0.5 mg/kg) or topically on the salivary gland skin (5 mg/body). Saliva volume, the number of sweat dots, and fecal weight were measured along with pilocarpine concentration in plasma and submandibular gland tissues.
Saliva volume significantly increased 0.5 h after oral administration and 0.5, 3, and 12 h after topical administration. Fecal weight and sweat dots increased significantly 1 h after oral administration; however, no changes were observed after topical application. The pilocarpine concentration in the submandibular gland tissues of the topical group was higher than that in the oral group at 0.5, 3, and 12 h of administration.
Pilocarpine application to salivary gland skin persistently increased salivary volume in rats without inducing sweating or diarrhea. Transdermal pilocarpine applied to the skin over the salivary glands may be an effective and safe treatment option for hyposalivation.
唾液分泌减少可通过口服胆碱能药物进行治疗；然而，全身性副作用偶尔会导致治疗中断。我们旨在研究皮贴型毛果芸香碱对大鼠唾液腺皮肤的唾液分泌和安全性的影响。
皮贴型毛果芸香碱通过口服（0.5mg/kg）或局部涂抹于唾液腺皮肤（5mg/只）给予大鼠。测量唾液量、汗点数量和粪便重量，同时检测血浆和颌下腺组织中的毛果芸香碱浓度。
口服给药 0.5 小时后唾液量显著增加，局部给药后 0.5、3 和 12 小时也显著增加。口服给药 1 小时后粪便重量和汗点显著增加；然而，局部应用后没有观察到变化。局部给药组颌下腺组织中的毛果芸香碱浓度在给药后 0.5、3 和 12 小时均高于口服组。
皮贴型毛果芸香碱应用于唾液腺皮肤可持续增加大鼠的唾液量，而不会引起出汗或腹泻。皮贴型毛果芸香碱应用于唾液腺皮肤可能是治疗唾液分泌减少的有效且安全的选择。
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