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Titolo:
Relative bioavailability of diclofenac after a single administration of a new multiple-unit formulation with enteric-coated pellets
Autore:
Walter, K; von Nieciecki, A;
Indirizzi:
Klinge Pharma GmbH, D-81610 Munich, Germany Klinge Pharma GmbH Munich Germany D-81610 GmbH, D-81610 Munich, Germany
Titolo Testata:
ARZNEIMITTEL-FORSCHUNG-DRUG RESEARCH
fascicolo: 8, volume: 51, anno: 2001,
pagine: 643 - 650
SICI:
0004-4172(2001)51:8<643:RBODAA>2.0.ZU;2-Q
Fonte:
ISI
Lingua:
GER
Keywords:
Anti-inflammatories, non-steroidal; CAS 15307-86-5; Diclofenac, enteric-coated pellets, healthy volunteers; pharmacokinetics; Diclo KD 75 akut;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
10
Recensione:
Indirizzi per estratti:
Indirizzo: Walter, K Klinge Pharma GmbH, Postfach 801063, D-81610 Munich, Germany Klinge Pharma GmbH Postfach 801063 Munich Germany D-81610 rmany
Citazione:
K. Walter e A. von Nieciecki, "Relative bioavailability of diclofenac after a single administration of a new multiple-unit formulation with enteric-coated pellets", ARZNEI-FOR, 51(8), 2001, pp. 643-650

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 containing140 mg diclofenac resinate (C) and a dispersible tablet containing 46.5 mgdiclofenac 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 extentof 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 t(max) 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 It (C) and 735 ng/ml after 1.9 It (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-unitformulation fulfils the prerequisites for the oral treatment of acute painful conditions when prompt analgesic and anti-inflammatory efficacy is desired.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 09/04/20 alle ore 07:31:19