Preparation and clinical application of 2% diflunisal oral ointment for painful lesions of the oral mucosa.
We previously reported the development and clinical efficacy of a 2% aspirin oral ointment and 2% ethenzamide oral ointment as hospital preparations for painful lesions of the oral mucosa. This study investigated methods of preparing a more stable oral ointment with a more effective analgesic action, using diflunisal, another salicylic acid derivative, with an analgesic effect stronger than that of aspirin. A two-percent diflunisal oral ointment was prepared similarly to the aspirin ointment using plastibase and CMC-Na as the ointment base. From the results of spreadability measurement, a CMC-Na content of 20% was considered appropriate. The stability of diflunisal in 2% diflunisal oral ointment stored at 5 degrees C, 20 degrees C and 30 degrees C, was determined using HPLC, and a high stability of diflunisal at room temperature for more than 100 days was confirmed. We also investigated its antinociceptive effect using the Randall-Selitto paw pressure test in rats, which showed that 2% diflunisal oral ointment was as effective as 2% aspirin oral ointment. On clinical application of 2% diflunisal oral ointment to 8 patients with painful oral mucous diseases, it was found to be significantly (p = 0.014) more effective than 2% aspirin oral ointment. The results of this study demonstrated that 2% diflunisal oral ointment is a clinically useful analgesic for painful oral lesions.
Kizu
J
J
Kyoritsu College of Pharmacy, 1-5-30 Shibakoen, Minato-ku, Tokyo 105-8512, Japan.
Tsuchiya
M
M
Watanabe
S
S
Yasuno
N
N
Arakawa
Y
Y
Saijyo
H
H
Okuda
O
O
D000328:Adult; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage / Q000493:pharmacokinetics; D004061:Diflunisal / Q000008:administration & dosage / Q000493:pharmacokinetics; D004341:Drug Evaluation; D004355:Drug Stability; D005260:Female; D006801:Humans; D008297:Male; D008875:Middle Aged; D009061:Mouth Mucosa / Q000378:metabolism; D009824:Ointments; D010146:Pain / Q000188:drug therapy*; D051381:Rats; D017208:Rats, Wistar
D000894:Anti-Inflammatory Agents, Non-Steroidal; D009824:Ointments; D004061:Diflunisal