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Grès, Marie-Catherine; Julian, Bernard; Bourrié, Martine; Meunier, Viviane; Roques, Claude; Berger, Monique; Boulenc, Xavier; Berger, Yves; Fabre, Gérard

doi:10.1023/a:1011919003030

Cited by 220 publications

(48 citation statements)

References 21 publications

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“…The P app values obtained for propranolol are in agreement with values reported in the literature 11) for this highly permeable compound, but for ranitidine the values reported in the literature 12) are slightly higher than what we obtained, which is probably attributable to analytical precision and accuracy due to its very low permeability. Loratadine added to the mixture with propranolol and ranitidine appeared to have significantly lower permeability than when studied alone suggesting interference of either propranolol or ranitidine or both these compounds with permeability of loratadine.…”

Section: Discussionsupporting

confidence: 91%

See 1 more Smart Citation

Classification of Loratadine Based on the Biopharmaceutics Drug Classification Concept and Possible in Vitro-in Vivo Correlation

Khan

Raušl

Zanoski

et al. 2004

Biological & Pharmaceutical Bulletin

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Loratadine, chemically known as ethyl 4-(8-chloro-5,6-dihydro-11H-benzo [5,6]-cyclohepta[1,2-b]pyridin-11-ylidene)-1-piperidinecarboxylate, is a weak base with a pK a value of ca. 6 (calculated in our laboratories). It is absorbed rapidly following oral administration in humans giving maximum plasma concentration (C max ) in about 1-1.5 h when administered under fasting conditions, but the degree of inter-subject variability in the pharmacokinetic parameters was reported to be very high. The C max and plasma concentration-time (AUC t ) data obtained following oral administration of 10 mg, 20 mg, and 40 mg loratadine capsules were found to have a dose-proportional relationship. 3)Following oral dosing 80% of the total dose administered was found equally distributed between urine and faeces in the form of metabolic products within 10 d.4) The kinetics of loratadine observed during a multiple dose study were found comparable to those reported from single dose studies, but the mean plasma concentration-time data were approximately 90% greater than that reported for single dose data, and the steady state plasma concentrations were apparent by the fifth day of dosing. 5)The objective of the studies reported here was two fold; firstly, to classify loratadine according to the biopharmaceutics drug classification scheme, 6,7) and secondly, to compare plasma time profiles predicted from in vitro dissolution data with experimental plasma time data in order to select the most appropriate conditions for in vitro assessment of loratadine solid dosage forms. Furthermore, attempts have been made to investigate factors responsible for the high inter-subject variability in pharmacokinetic parameters of the drug. MATERIALS AND METHODS MaterialsLoratadine of European Pharmacopoeia (EP) quality was purchased from Chemo Iberica S.A. (Lugano, Switzerland). Standard pharmacopoeial grade excipients were used in the tablet formulation. Egg lecithin used for dissolution studies under biorelevant conditions was a gift from Lipoid AG (Cham, Switzerland). Crude sodium taurocholate (batch no. 386645/1, standardised against a lot of the pure substance containing above 97%) was purchased from Sigma Chemical Co. (St. Louis, U.S.A.). Sodium lauryl sulphate, hydrochloric acid and all other chemicals used for evaluation of the tablets were of analytical grade. The tablets were prepared in-house (by wet granulation technology using starch paste as a binder).For permeability testing, Caco-2 cells were obtained from the European Collection of Cell Cultures (U.K.) at passage 20. Dulbecco's Eagles medium (DMEM) containing glucose (4500 mg/ml) was purchased from Imunološki Zavod, Zagreb (Croatia). Fetal bovine serum (FBS), glutamax I, nonessential amino acids (NEAA), penicillin/streptomycin, fungizone and 0.25% trypsin-EDTA were obtained from Gibco, Life Technologies (U.K.). Hanks balanced salt solution (HBSS) and dimethylsulphoxide (DMSO) were purchased from Sigma-Aldrich (Germany). Tert-butyl methyl ether (TBME) was supplied by Merck (Germany).Solubili...

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Section: Discussionsupporting

confidence: 91%

“…Irrespective of the conditions of the experiments (either in mixture or alone), the permeability of loratadine exceeded the lower limit (Table 1) suggested by Grès et al 11) indicating that loratadine should be classified as a Class II, low soluble, highly permeable drug.…”

Section: Discussionmentioning

confidence: 69%

Classification of Loratadine Based on the Biopharmaceutics Drug Classification Concept and Possible in Vitro-in Vivo Correlation

Khan

Raušl

Zanoski

et al. 2004

Biological & Pharmaceutical Bulletin

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show abstract

“…Despite this, relating P app in this assay for a given compound to its likely in vivo absorption remains a difficult prospect. Several groups [29][30][31][32] have reported very strong individual correlations between P app across Caco-2 monolayers and in vivo absorption across intestinal epithelium in vivo. However, as noted by Artursson and colleagues 33 the correlation between studies is poor.…”

Section: Discussionmentioning

confidence: 99%

“…. Two apparent outliers have been excluded from the analysis: amoxicillin 29 ; and PEG-900. 31 Panel A: Correlation between Log 10 (P app ) and in vivo absorption as reported in the 4 selected studies.…”

Section: Panel A)mentioning

confidence: 99%

Modified low molecular weight cyclic peptides as mimetics of BDNF with improved potency, proteolytic stability and transmembrane passage in vitro

Fletcher

Hughes

2009

Bioorganic & Medicinal Chemistry

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“…12 The pre-assay TEER figures of Caco-2 and MDCK cells are 595 ± 24 and 228 ± 31 X cm 2 , respectively, which are similar to literature values. 10,13 The post assay TEER values for Caco-2 and MDCK cells are 570 ± 37 and 235 ± 11 X cm 2 , respectively. A further check on the tightness of the monolayer formation and integrity was undertaken using the dye Lucifer yellow (LY).…”

mentioning

confidence: 99%

Cytotoxic 1,5-diaryl-3-oxo-1,5-pentadienes: An assessment and comparison of membrane permeability using Caco-2 and MDCK monolayers

Singh

Michel

Das

et al. 2014

Bioorganic & Medicinal Chemistry Letters

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Abstract: On the basis of morphological parameters, biochemical activity and drug transport characteristics, the TC-7 clone appeared to be a valuable alternative to the use of parental Caco-2 cells for drug absorption studies.

Cited by 220 publications

References 21 publications

Classification of Loratadine Based on the Biopharmaceutics Drug Classification Concept and Possible in Vitro-in Vivo Correlation

Classification of Loratadine Based on the Biopharmaceutics Drug Classification Concept and Possible in Vitro-in Vivo Correlation

Modified low molecular weight cyclic peptides as mimetics of BDNF with improved potency, proteolytic stability and transmembrane passage in vitro

Cytotoxic 1,5-diaryl-3-oxo-1,5-pentadienes: An assessment and comparison of membrane permeability using Caco-2 and MDCK monolayers

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