Tags

Type your tag names separated by a space and hit enter

Single-dose pharmacokinetic study of rapidly dispersing diclofenac potassium formulations in healthy volunteers.
Curr Med Res Opin. 2009 Oct; 25(10):2423-8.CM

Abstract

OBJECTIVE

The clinical utility of diclofenac potassium, a commonly prescribed analgesic that provides mild to moderate pain relief, may be hindered by its delayed, depressed, and/or inconsistent absorption characteristics. A diclofenac potassium formulation using proprietary dispersion technology (ProSorb) was developed to overcome these limitations. The authors evaluated and compared the pharmacokinetics (PK) of 2 investigational diclofenac potassium liquid filled soft gelatin capsule (DPSGC) preparations and one investigational diclofenac liquid formulation, each incorporating the proprietary dispersion technology, to establish bioequivalence and identify a formulation for further clinical study.

RESEARCH DESIGN AND METHODS

In an open-label, single-dose, three-way crossover, relative bioavailability study, 24 healthy volunteers were randomized to receive each of the 25-mg DPSGC formulations (development processes A and B) and the 1-mL (25-mg) liquid diclofenac formulation (similar to the fill liquid used in the DPSGC products) during three inpatient visits. Each dose was separated by 3 days. Plasma samples were collected at preselected time points through 6 hours post dose. Diclofenac concentrations were determined using a validated HPLC method. Bioequivalence was established within the 80% to 125% acceptance range. Safety and tolerability were monitored throughout.

RESULTS

Area under the plasma concentration-time curves (AUC(0-)(t)) for the three formulations were between 577 and 585 ng-hr/mL and peak plasma concentrations (C(max)) were between 958 and 1087 ng/mL, with the DPSGC process B group having the highest C(max). The times to C(max) (t(max)) were all below 30 minutes, with the liquid formulation producing the shortest t(max) (15 minutes). Plasma concentration-time course profiles were similar for all three rapidly dispersing diclofenac potassium formulations. One mild adverse event was observed (lingual paresthesia) and one participant discontinued due to an unrelated event (acute tonsillitis).

CONCLUSIONS

These data show that diclofenac potassium formulations using proprietary dispersion technology are rapidly and consistently absorbed. These characteristics may be beneficial in settings where rapid and consistent drug absorption is desirable. These results may differ in other patient populations such as those experiencing pain or illness.

Authors+Show Affiliations

AAIPharma, Inc., Neu-Ulm, Germany.No affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Clinical Trial, Phase I
Journal Article
Randomized Controlled Trial
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

19663688

Citation

Lissy, Michael, et al. "Single-dose Pharmacokinetic Study of Rapidly Dispersing Diclofenac Potassium Formulations in Healthy Volunteers." Current Medical Research and Opinion, vol. 25, no. 10, 2009, pp. 2423-8.
Lissy M, Stiff DD, Kowalski MM, et al. Single-dose pharmacokinetic study of rapidly dispersing diclofenac potassium formulations in healthy volunteers. Curr Med Res Opin. 2009;25(10):2423-8.
Lissy, M., Stiff, D. D., Kowalski, M. M., & Moore, K. A. (2009). Single-dose pharmacokinetic study of rapidly dispersing diclofenac potassium formulations in healthy volunteers. Current Medical Research and Opinion, 25(10), 2423-8. https://doi.org/10.1185/03007990903158513
Lissy M, et al. Single-dose Pharmacokinetic Study of Rapidly Dispersing Diclofenac Potassium Formulations in Healthy Volunteers. Curr Med Res Opin. 2009;25(10):2423-8. PubMed PMID: 19663688.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Single-dose pharmacokinetic study of rapidly dispersing diclofenac potassium formulations in healthy volunteers. AU - Lissy,Michael, AU - Stiff,Dwight D, AU - Kowalski,Mark M, AU - Moore,Keith A, PY - 2009/8/12/entrez PY - 2009/8/12/pubmed PY - 2009/12/16/medline SP - 2423 EP - 8 JF - Current medical research and opinion JO - Curr Med Res Opin VL - 25 IS - 10 N2 - OBJECTIVE: The clinical utility of diclofenac potassium, a commonly prescribed analgesic that provides mild to moderate pain relief, may be hindered by its delayed, depressed, and/or inconsistent absorption characteristics. A diclofenac potassium formulation using proprietary dispersion technology (ProSorb) was developed to overcome these limitations. The authors evaluated and compared the pharmacokinetics (PK) of 2 investigational diclofenac potassium liquid filled soft gelatin capsule (DPSGC) preparations and one investigational diclofenac liquid formulation, each incorporating the proprietary dispersion technology, to establish bioequivalence and identify a formulation for further clinical study. RESEARCH DESIGN AND METHODS: In an open-label, single-dose, three-way crossover, relative bioavailability study, 24 healthy volunteers were randomized to receive each of the 25-mg DPSGC formulations (development processes A and B) and the 1-mL (25-mg) liquid diclofenac formulation (similar to the fill liquid used in the DPSGC products) during three inpatient visits. Each dose was separated by 3 days. Plasma samples were collected at preselected time points through 6 hours post dose. Diclofenac concentrations were determined using a validated HPLC method. Bioequivalence was established within the 80% to 125% acceptance range. Safety and tolerability were monitored throughout. RESULTS: Area under the plasma concentration-time curves (AUC(0-)(t)) for the three formulations were between 577 and 585 ng-hr/mL and peak plasma concentrations (C(max)) were between 958 and 1087 ng/mL, with the DPSGC process B group having the highest C(max). The times to C(max) (t(max)) were all below 30 minutes, with the liquid formulation producing the shortest t(max) (15 minutes). Plasma concentration-time course profiles were similar for all three rapidly dispersing diclofenac potassium formulations. One mild adverse event was observed (lingual paresthesia) and one participant discontinued due to an unrelated event (acute tonsillitis). CONCLUSIONS: These data show that diclofenac potassium formulations using proprietary dispersion technology are rapidly and consistently absorbed. These characteristics may be beneficial in settings where rapid and consistent drug absorption is desirable. These results may differ in other patient populations such as those experiencing pain or illness. SN - 1473-4877 UR - https://www.unboundmedicine.com/medline/citation/19663688/Single_dose_pharmacokinetic_study_of_rapidly_dispersing_diclofenac_potassium_formulations_in_healthy_volunteers_ L2 - https://www.tandfonline.com/doi/full/10.1185/03007990903158513 DB - PRIME DP - Unbound Medicine ER -