%0 Journal Article
%T Pharmacokinetics of diltiazem hydrochloride delay-onset sustained-release pellet capsules in healthy volunteers
%A Xi-Qing Yan
%A Zhi-Gang Chen
%A Rong-Liang Wang
%A Jun Yang
%J Brazilian Journal of Pharmaceutical Sciences
%D 2013
%I Universidade de S?o Paulo
%X The pharmacokinetics (PK) of ordinary tablets and sustained release capsules of diltiazem hydrochloride in human clinical trials had been studied. The PK of diltiazem hydrochloride delay-onset sustained-release pellet capsules, a new dosage form, has not been reported, although it is very important to clinical use. In this paper, we investigated the PK of diltiazem hydrochloride delay-onset sustained-release pellet capsules and the food influence in Chinese healthy volunteers. The PK parameters indicated that the diltiazem hydrochloride delay-onset sustained-release pellet capsules appeared marked characteristics of delayed and controlled release. An opened-label, randomized and parallel clinical trial was conducted in 36 Chinese healthy volunteers with single oral dose (90 mg, 180 mg or 270 mg) and a multiple oral dose (90 mg d-1¡Á6 d) administration. The effect of food on the PK of one single oral dose (360 mg) was investigated in 24 healthy Chinese volunteers. Plasma diltiazem concentration was determined by reversed-phase high-performance liquid chromatography (RP-HPLC) and the main pharmacokinetic parameters were analyzed by PKSolver (Ver 2.0). All clinical studies were conducted in the Clinical Pharmacological Center (No. JDX1999064) of Xiangya Hospital Affiliated Central South University, China. The PK parameters suggested that the new formulation had marked characteristics of delayed and controlled release of diltiazem, and food intake did not alter significantly diltiazem pharmacokinetic parameters. Embora a farmacocin¨¦tica (PK) do cloridrato de diltiazem nas formas de comprimidos de libera  o imediata e c¨¢psulas de libera  o modificada em ensaios cl¨ªnicos j¨¢ tenha sido relatada, a pesquisa da PK do cloridrato de diltiazem na forma de c¨¢psulas com peletes de libera  o retardada e sustentada ainda ¨¦ muito importante. Neste trabalho, propusemos avaliar a farmacocin¨¦tica do cloridrato de diltiazem administrado atrav¨¦s desta nova forma farmac¨ºutica em volunt¨¢rios chineses sadios, assim como a influ¨ºncia da ingest o de alimentos neste perfil farmacocin¨¦tico. Foi realizado um ensaio cl¨ªnico aberto, randomizado e paralelo em 36 volunt¨¢rios, que receberam dose oral ¨²nica de 90 mg, 180 mg ou 270 mg e dose m¨²ltiplas (90 mg/d ¡Á 6 d) pela mesma via de administra  o. Para avaliar o efeito da ingest o de alimentos sobre a PK do diltiazem foi realizada a administra  o de dose ¨²nica (360 mg) em 24 volunt¨¢rios chineses sadios. A concentra  o plasm¨¢tica do diltiazem foi determinada por Cromatografia Liquida de Alta Efici¨ºncia em fase reversa (CLAE-FR) e os princi
%K Cloridrato de diltiazem
%K Cloridrato de diltiazem
%K Alimentos
%K Alimentos
%K Cromatografia L¨ªquida de Alta Efici¨ºncia
%K Diltiazem hydrochloride
%K Diltiazem hydrochloride
%K Food
%K Food
%K High-performance liquid chromatography
%U http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502013000100004