Tags

Type your tag names separated by a space and hit enter

[Relative bioavailability of diclofenac after a single administration of a new multiple-unit formulation of enteric-coated pellets].
Arzneimittelforschung. 2001; 51(8):643-50.A

Abstract

The relative bioavailability of diclofenac (CAS 15307-86-5) was investigated after a single administration of a multiple-unit formulation containing 75 mg diclofenac sodium in enteric-coated pellets (A) in comparison to an enteric-coated tablet with 50 mg diclofenac sodium (B), a capsule containing 140 mg diclofenac resinate (C) and a dispersible tablet containing 46.5 mg diclofenac acid (D). The study was carried out in a four-way crossover design in 16 healthy male volunteers. Serum concentrations of diclofenac were determined with a validated and specific HPLC-method. After dose normalisation, a mean relative bioavailability of 99% (B), 142% (C) and 116% (D) was determined for the pellet formulation. According to the corresponding 90%-confidence interval, bioequivalence for the extent of bioavailability of the test formulation can be concluded compared to the enteric-coated tablet. In comparison to the formulations C and D, the test formulation showed an increased extent of bioavailability. Further differences in pharmacokinetics were observed for the rate-dependent parameters. For the test formulation, the highest mean maximum serum concentration (1595 ng/ml) was measured with a corresponding tmax of 0.8 h. For the reference formulations, mean peak serum concentrations of 1285 ng/ml after 2.0 h (B), 370 ng/ml after 1.8 h (C) and 735 ng/ml after 1.9 h (D) were observed. Despite the enteric-coating of the pellets, a short lagtime of 0.4 h was determined for the test formulation. For the other rapid-release formulation (D), the lagtime was of a similar magnitude (0.3 h), while drug release and absorption from the enteric-coated tablet and the diclofenac resinate capsule were delayed (1.8 and 0.7 h, respectively). Due to the rapid and high bioavailability of diclofenac, the multiple-unit formulation fulfills the prerequisites for the oral treatment of acute painful conditions when prompt analgesic and anti-inflammatory efficacy is desired.

Authors+Show Affiliations

Klinge Pharma GmbH, München. kersten.walter@klinge-pharma.deNo affiliation info available

Pub Type(s)

Clinical Trial
Comparative Study
English Abstract
Journal Article
Randomized Controlled Trial

Language

ger

PubMed ID

11556125

Citation

Walter, K, and A von Nieciecki. "[Relative Bioavailability of Diclofenac After a Single Administration of a New Multiple-unit Formulation of Enteric-coated Pellets]." Arzneimittel-Forschung, vol. 51, no. 8, 2001, pp. 643-50.
Walter K, von Nieciecki A. [Relative bioavailability of diclofenac after a single administration of a new multiple-unit formulation of enteric-coated pellets]. Arzneimittelforschung. 2001;51(8):643-50.
Walter, K., & von Nieciecki, A. (2001). [Relative bioavailability of diclofenac after a single administration of a new multiple-unit formulation of enteric-coated pellets]. Arzneimittel-Forschung, 51(8), 643-50.
Walter K, von Nieciecki A. [Relative Bioavailability of Diclofenac After a Single Administration of a New Multiple-unit Formulation of Enteric-coated Pellets]. Arzneimittelforschung. 2001;51(8):643-50. PubMed PMID: 11556125.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - [Relative bioavailability of diclofenac after a single administration of a new multiple-unit formulation of enteric-coated pellets]. AU - Walter,K, AU - von Nieciecki,A, PY - 2001/9/15/pubmed PY - 2001/10/12/medline PY - 2001/9/15/entrez SP - 643 EP - 50 JF - Arzneimittel-Forschung JO - Arzneimittelforschung VL - 51 IS - 8 N2 - The relative bioavailability of diclofenac (CAS 15307-86-5) was investigated after a single administration of a multiple-unit formulation containing 75 mg diclofenac sodium in enteric-coated pellets (A) in comparison to an enteric-coated tablet with 50 mg diclofenac sodium (B), a capsule containing 140 mg diclofenac resinate (C) and a dispersible tablet containing 46.5 mg diclofenac acid (D). The study was carried out in a four-way crossover design in 16 healthy male volunteers. Serum concentrations of diclofenac were determined with a validated and specific HPLC-method. After dose normalisation, a mean relative bioavailability of 99% (B), 142% (C) and 116% (D) was determined for the pellet formulation. According to the corresponding 90%-confidence interval, bioequivalence for the extent of bioavailability of the test formulation can be concluded compared to the enteric-coated tablet. In comparison to the formulations C and D, the test formulation showed an increased extent of bioavailability. Further differences in pharmacokinetics were observed for the rate-dependent parameters. For the test formulation, the highest mean maximum serum concentration (1595 ng/ml) was measured with a corresponding tmax of 0.8 h. For the reference formulations, mean peak serum concentrations of 1285 ng/ml after 2.0 h (B), 370 ng/ml after 1.8 h (C) and 735 ng/ml after 1.9 h (D) were observed. Despite the enteric-coating of the pellets, a short lagtime of 0.4 h was determined for the test formulation. For the other rapid-release formulation (D), the lagtime was of a similar magnitude (0.3 h), while drug release and absorption from the enteric-coated tablet and the diclofenac resinate capsule were delayed (1.8 and 0.7 h, respectively). Due to the rapid and high bioavailability of diclofenac, the multiple-unit formulation fulfills the prerequisites for the oral treatment of acute painful conditions when prompt analgesic and anti-inflammatory efficacy is desired. SN - 0004-4172 UR - https://www.unboundmedicine.com/medline/citation/11556125/[Relative_bioavailability_of_diclofenac_after_a_single_administration_of_a_new_multiple_unit_formulation_of_enteric_coated_pellets]_ L2 - https://www.thieme-connect.com/DOI/DOI?10.1055/s-0031-1300095 DB - PRIME DP - Unbound Medicine ER -