Increased absorption rate of diclofenac from fast acting formulations containing its potassium salt.
Diclofenac (CAS 15307-86-5) is a non-steroidal anti-inflammatory drug largely used, mainly to relief pain of various origin. Diclofenac is present on the market as free acid, as sodium salt (CAS 15307-79-6) and as potassium salt (CAS 15307-81-0). The last salification form has shown a prompter absorption rate and a faster onset of analgesic activity than the acid form and sodium salt. This paper extensively reviews three trials carried out on healthy volunteers, where potassium salt of diclofenac present in three fast-acting formulations, namely sachets (Trial 1), tablets (Trial 2) and oral drops (Trial 3), were compared to reference tablet formulations from the market. A very fast absorption rate was encountered with the three test formulations, with the peak reached in one case 5 min and in most cases within 10-15 min after dosing. The quick absorption rate of test formulations was attributed to the special combination of the salt of diclofenac with a dynamic buffering agent, namely bicarbonate, present in the test formulations and covered by an international patent. The prompt absorption of diclofenac from the new fast-acting formulations was accompanied by the presence of only one peak, whereas the reference formulations produced in most cases two peaks, as widely described in literature. This finding suggested the hypothesis that the absorption of test formulations should occur in a shorter tract of the gut. The faster absorption of diclofenac from the three fast-acting formulations is expected to produce a faster onset of analgesic action, which highlights these new formulations as particularly indicated to relief pain of any origin.
Reiner
V
V
A.P.R. Applied Pharma Research S.A., Balerna, Switzerland. valentina.reiner@apr.ch
Reiner
A
A
Reiner
G
G
Conti
M
M
D000328:Adult; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage / Q000494:pharmacology*; D019540:Area Under Curve; D001682:Biological Availability; D002851:Chromatography, High Pressure Liquid; D004008:Diclofenac / Q000008:administration & dosage / Q000493:pharmacokinetics*; D004562:Electrocardiography / Q000187:drug effects; D005260:Female; D006801:Humans; D007408:Intestinal Absorption; D008297:Male; D011188:Potassium / Q000737:chemistry; D011208:Powders; D013056:Spectrophotometry, Ultraviolet; D013608:Tablets, Enteric-Coated
D000894:Anti-Inflammatory Agents, Non-Steroidal; D011208:Powders; D013608:Tablets, Enteric-Coated; D004008:Diclofenac; D011188:Potassium