Clinical evaluation of novel buccoadhesive film containing ketorolac in dental and post-oral surgery pain management.
Ketorolac tromethamine (KT), a non-steroidal anti-inflammatory drug, was formulated in buccoadhesive film to overcome the limitations in the currently available routes of administration which in sequence will increase patients' compliance. The film was formulated using aqueous solvents by means of two bioadhesive polymers namely: hydroxylpropyl methyl cellulose (HPMC) and Carbopol 934. The prepared film was subjected to investigations for its physical and mechanical properties, swelling behavior, in vitro bioadhesion, and in vitro, in situ and in vivo release. Anti-inflammatory efficacy and analgesic activity of the prepared buccoadhesive film were investigated in rats using the hind-paw oedema test and the hot plate method. The analgesic efficacy and tolerability of a single 30 mg dose of KT formulated into the buccoadhesive film was clinically evaluated using a standard, widely accepted post-oral surgery pain model. In this study, the prepared film has been administrated to dental post-operative patients for relieving pain in dental hospital clinic. Results indicate that the concentration of KT in the oral cavity was maintained above 4.0 microg/ml for a period of at least 6 h. The buccal KT film was excellently tolerated in all patients and no complains of GI side effects were reported. It is concluded from this clinical evaluation that KT formulated into a buccoadhesive film is effective as a potent analgesic in dental and postoperative oral surgery in a single dose of 30 mg with minimal GI side effects.
Alsarra
I A
IA
Department of Pharmaceutics, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi Arabia. ialsarra@ksu.edu.sa
Alanazi
F K
FK
Mahrous
G M
GM
Abdel Rahman
A A
AA
Al Hezaimi
K A
KA
D000293:Adolescent; D000328:Adult; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage* / Q000494:pharmacology / Q000627:therapeutic use*; D019540:Area Under Curve; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D004058:Diffusion; D004311:Double-Blind Method; D004487:Edema / Q000139:chemically induced / Q000188:drug therapy; D005260:Female; D006801:Humans; D006863:Hydrogen-Ion Concentration; D020910:Ketorolac / Q000008:administration & dosage* / Q000494:pharmacology / Q000627:therapeutic use*; D008297:Male; D051379:Mice; D008875:Middle Aged; D009061:Mouth Mucosa; D019647:Oral Surgical Procedures / Q000009:adverse effects; D010147:Pain Measurement / Q000187:drug effects; D010149:Postoperative Pain / Q000188:drug therapy*; D011108:Polymers; D051381:Rats; D011930:Reaction Time / Q000187:drug effects; D014014:Tissue Adhesives; D014081:Tooth Extraction / Q000009:adverse effects
D000894:Anti-Inflammatory Agents, Non-Steroidal; D011108:Polymers; D014014:Tissue Adhesives; D020910:Ketorolac