Relative bioavailability of griseofulvin lyophilized dry emulsion tablet vs. immediate release tablet: A single-dose, randomized, open-label, six-period, crossover study in healthy adult volunteers in the fasted and fed states

被引:21
作者
Ahmed, Iman Saad [3 ]
Aboul-Einien, Mona Hassan [3 ]
Mohamed, Osama Hussein [1 ]
Farid, Samar Farghali [2 ]
机构
[1] Sharjah Univ, Dept Pharm Practice, Coll Pharm, Sharjah, U Arab Emirates
[2] Cairo Univ, Fac Pharm, Dept Clin Pharm & Pharm Practice, Cairo, Egypt
[3] Cairo Univ, Fac Pharm, Dept Pharmaceut & Ind Pharm, Cairo, Egypt
关键词
griseofulvin; lyophilized dry emulsion tablets; in vivo absorption; pharmacokinetics; bioavailability; food effects;
D O I
10.1016/j.ejps.2008.07.002
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The oral bioavailability of griseofulvin (GF) formulated as a fast disintegrating lyophilized dry emulsion (LDE) tablet was studied and compared to the commercially available immediate release (IR) tablet, as a reference, in both the fasted and fed states in nine healthy volunteers after a single oral dose (12S mg) in a crossover design. Furthermore the LDE tablets were ingested with and without water under both the fasted and fed states, in the fasted state, the rate of absorption was found to be significantly faster from LDE tablets, in the presence and absence of water, as shown by a higher C.,. (more than two times higher, p = 0.0001) and a shorter t(max) (by more than 3 h, p = 0.0001) compared to IR tablets. The extent of absorption, expressed as AUC, from LDE tablets in the presence and absence of water was 65% and 77% larger and statistically significantly different relative to the mean AUC from IR tablets (p = 0.006). In the fed state, Cm. from LDE tablets ingested with and without water was found to be about 30% and 50% higher, respectively, than the immediate release tablets. A shorter t(max) was also shown whether LDE tablets were ingested with or without water in the fed state as compared to immediate release tablets. The mean AUC from LDE tablets under fed conditions in the presence of water was about 21% larger and was not statistically significantly different from AUC from immediate release tablets (p = 0.517). When ingested without water, AUC from LDE tablets was about 43% larger and statistically significantly different relative to AUC from IR tablets (p = 0.033), The mean AUC from the LDE tablet ingested with water under fed conditions relative to AUC from LDE tablet ingested without water was not statistically significantly different (p = 0.454). Results show that the food effect of the high fat meal is very pronounced in case of the immediate release tablets, Fulvin, than in case of LDE tablets whether given with or without water. (C) 2008 Elsevier B.V. All rights reserved.
引用
收藏
页码:219 / 225
页数:7
相关论文
共 22 条
[1]   In vitro and in vivo evaluation of a fast-disintegrating lyophilized dry emulsion tablet containing griseofulvin [J].
Ahmed, Iman Saad ;
Hassan, Mona Aboul-Einien .
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES, 2007, 32 (01) :58-68
[2]   A THEORETICAL BASIS FOR A BIOPHARMACEUTIC DRUG CLASSIFICATION - THE CORRELATION OF IN-VITRO DRUG PRODUCT DISSOLUTION AND IN-VIVO BIOAVAILABILITY [J].
AMIDON, GL ;
LENNERNAS, H ;
SHAH, VP ;
CRISON, JR .
PHARMACEUTICAL RESEARCH, 1995, 12 (03) :413-420
[3]   USE OF 24-HR URINARY-EXCRETION DATA TO ASSESS BIOAVAILABILITY OF GRISEOFULVIN IN HUMANS [J].
BATES, TR ;
SEQUEIRA, JAL .
JOURNAL OF PHARMACEUTICAL SCIENCES, 1975, 64 (04) :709-710
[4]   BIOAVAILABILITY OF MICRONIZED GRISEOFULVIN FROM CORN OIL-IN-WATER EMULSION, AQUEOUS SUSPENSION, AND COMMERCIAL TABLET DOSAGE FORMS IN HUMANS [J].
BATES, TR ;
SEQUEIRA, JA .
JOURNAL OF PHARMACEUTICAL SCIENCES, 1975, 64 (05) :793-797
[5]   BIOPHARMACEUTICS OF DRUGS ADMINISTERED IN LIPID-CONTAINING DOSAGE FORMS .1. GI-ABSORPTION OF GRISEOFULVIN FROM AN OIL-IN-WATER EMULSION IN RAT [J].
CARRIGAN, PJ ;
BATES, TR .
JOURNAL OF PHARMACEUTICAL SCIENCES, 1973, 62 (09) :1476-1479
[6]   Physicochemical and physiological mechanisms for the effects of food on drug absorption: The role of lipids and pH [J].
Charman, WN ;
Porter, CJH ;
Mithani, S ;
Dressman, JB .
JOURNAL OF PHARMACEUTICAL SCIENCES, 1997, 86 (03) :269-282
[7]   EFFECT OF FOOD AND A MONOGLYCERIDE EMULSION FORMULATION ON DANAZOL BIOAVAILABILITY [J].
CHARMAN, WN ;
ROGGE, MC ;
BODDY, AW ;
BERGER, BM .
JOURNAL OF CLINICAL PHARMACOLOGY, 1993, 33 (04) :381-386
[8]  
Chaumeil JC, 1998, METHOD FIND EXP CLIN, V20, P211
[9]   Enhancement of bioavailability of griseofulvin by its complexation with β-cyclodextrin [J].
Dhanaraju, MD ;
Kumaran, KS ;
Baskaran, T ;
Moorthy, MSR .
DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY, 1998, 24 (06) :583-587
[10]   Dissolution testing as a prognostic tool for oral drug absorption: Immediate release dosage forms [J].
Dressman, JB ;
Amidon, GL ;
Reppas, C ;
Shah, VP .
PHARMACEUTICAL RESEARCH, 1998, 15 (01) :11-22