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Comparative bioavailability of a dispersible formulation of diclofenac and finding of double plasma peaks.
Int J Clin Pharmacol Ther. 1995 Jun; 33(6):333-9.IJ

Abstract

We carried out a comparative study of the bioavailability of a typical, enteric-coated diclofenac with regard to a new dispersible formulation whose faster dissolution results in an earlier onset of its analgesic effect. This randomized, crossover study was conducted in 12 healthy male volunteers, who received in fasting 100 mg of enteric-coated diclofenac (Dolotrén, FAES) and 100 mg of dispersible diclofenac (Dolotrén Dispersable, FAES), with one-week interval between both. Blood samples were taken at pre-established times during the 24 hours after dosing, and plasma concentrations of diclofenac were determined by HPLC. Possible adverse experiences were monitored with a check-list, and blood and urinalysis were performed for safety assessment. The dispersible formulation showed a relative extent of bioavailability between 78% and 99% (90% CI) for the AUC0-infinity, being the 90% CI for the Cmax 63%-129%. The time to Cmax (Tmax) was significantly shorter with the dispersible than with the enteric-coated formulation (95% CI for the difference = 1.5-4.25 hours) as the T0(lag) or time to measurable plasma concentrations (1.9-4.2 hours, 95% CI). A relevant feature in the study was the finding of a second peak at 2-2.5 hours post-dosing in 7 out of 11 profiles of subjects receiving the dispersible formulation. Both formulations were well tolerated in clinical and laboratory terms. In conclusion, the new dispersible formulation of diclofenac allows absorption to begin more rapidly and plasma peak is reached earlier, a fact that may be relevant to the analgesic treatment of acute pain.

Authors+Show Affiliations

Clinical Pharmacology Service, Hospital La Paz, Madrid, Spain.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Clinical Trial
Comparative Study
Journal Article
Randomized Controlled Trial

Language

eng

PubMed ID

7582384

Citation

Macía, M A., et al. "Comparative Bioavailability of a Dispersible Formulation of Diclofenac and Finding of Double Plasma Peaks." International Journal of Clinical Pharmacology and Therapeutics, vol. 33, no. 6, 1995, pp. 333-9.
Macía MA, Frias J, Carcas AJ, et al. Comparative bioavailability of a dispersible formulation of diclofenac and finding of double plasma peaks. Int J Clin Pharmacol Ther. 1995;33(6):333-9.
Macía, M. A., Frias, J., Carcas, A. J., Guerra, P., Valiente, R., & Lucero, M. L. (1995). Comparative bioavailability of a dispersible formulation of diclofenac and finding of double plasma peaks. International Journal of Clinical Pharmacology and Therapeutics, 33(6), 333-9.
Macía MA, et al. Comparative Bioavailability of a Dispersible Formulation of Diclofenac and Finding of Double Plasma Peaks. Int J Clin Pharmacol Ther. 1995;33(6):333-9. PubMed PMID: 7582384.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Comparative bioavailability of a dispersible formulation of diclofenac and finding of double plasma peaks. AU - Macía,M A, AU - Frias,J, AU - Carcas,A J, AU - Guerra,P, AU - Valiente,R, AU - Lucero,M L, PY - 1995/6/1/pubmed PY - 1995/6/1/medline PY - 1995/6/1/entrez SP - 333 EP - 9 JF - International journal of clinical pharmacology and therapeutics JO - Int J Clin Pharmacol Ther VL - 33 IS - 6 N2 - We carried out a comparative study of the bioavailability of a typical, enteric-coated diclofenac with regard to a new dispersible formulation whose faster dissolution results in an earlier onset of its analgesic effect. This randomized, crossover study was conducted in 12 healthy male volunteers, who received in fasting 100 mg of enteric-coated diclofenac (Dolotrén, FAES) and 100 mg of dispersible diclofenac (Dolotrén Dispersable, FAES), with one-week interval between both. Blood samples were taken at pre-established times during the 24 hours after dosing, and plasma concentrations of diclofenac were determined by HPLC. Possible adverse experiences were monitored with a check-list, and blood and urinalysis were performed for safety assessment. The dispersible formulation showed a relative extent of bioavailability between 78% and 99% (90% CI) for the AUC0-infinity, being the 90% CI for the Cmax 63%-129%. The time to Cmax (Tmax) was significantly shorter with the dispersible than with the enteric-coated formulation (95% CI for the difference = 1.5-4.25 hours) as the T0(lag) or time to measurable plasma concentrations (1.9-4.2 hours, 95% CI). A relevant feature in the study was the finding of a second peak at 2-2.5 hours post-dosing in 7 out of 11 profiles of subjects receiving the dispersible formulation. Both formulations were well tolerated in clinical and laboratory terms. In conclusion, the new dispersible formulation of diclofenac allows absorption to begin more rapidly and plasma peak is reached earlier, a fact that may be relevant to the analgesic treatment of acute pain. SN - 0946-1965 UR - https://www.unboundmedicine.com/medline/citation/7582384/Comparative_bioavailability_of_a_dispersible_formulation_of_diclofenac_and_finding_of_double_plasma_peaks_ L2 - https://www.lens.org/lens/search/patent/list?q=citation_id:7582384 DB - PRIME DP - Unbound Medicine ER -