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Quantitative assessment of the relevance of organic-aniontransporting-polypeptide 1B1 and 2B1 polymorphisms in fexofenadine pharmacokinetic variants via pharmacometrics

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Journal of Pharmaceutical Analysis 2023年第6期13卷 660-672页

作者： Ji-Hun Jang Seung-Hyun Jeong Yong-Bok Lee Department of Pharmacy College of PharmacyChonnam National UniversityGwangju61186Republic of Korea Department of Pharmacy College of PharmacySunchon National UniversitySuncheon-si57922Republic of Korea

fexofenadine is useful in various allergic disease treatment.However,the pharmacokinetic variability information and quantitative factor identification of fexofenadine are very lacking.This study aimed to verify the validity of previously proposed genetic factors through fexofenadine population pharmacokinetic modeling and to explore the quantitative correlations affecting the pharmacokinetic variability.Polymorphisms of the organic-anion-transporting-polypeptide(OATP)1B1 and 2B1 have been proposed to be closely related to fexofenadine pharmacokinetic diversity.Therefore,modeling was performed using fexofenadine oral exposure data according to the OATP1B1-and 2B1-polymorphisms.OATP1B1 and 2B1 were identified as effective covariates of clearance(CL/F)and distribution volume(V/F)-CL/F,respectively,in fexofenadine pharmacokinetic variability.CL/F and average steady-state plasma concentration of fexofenadine differed by up to 2.17-and 2.20-folds,respectively,depending on the OATP1B1 polymorphism.Among the individuals with different OATP2B1 polymorphisms,the CL/F and V/F differed by up to 1.73-and 2.00-folds,respectively.Ratio of the areas under the curves following single-and multiple-administrations,and the cumulative ratio were significantly different between OATP1B1-and 2B1-polymorphism groups.Based on quantitative prediction comparison through a model-based approach,OATP1B1 was confirmed to be relatively more important than 2B1 regarding the degree of effect on fexofenadine pharmacokinetic variability.Based on the established pharmacokineticpharmacodynamic relationship,the difference in fexofenadine efficacy according to genetic polymorphisms of OATP1B1 and 2B1 was 1.25-and 0.87-times,respectively,and genetic consideration of OATP1B1 was expected to be important in the pharmacodynamics area as well.This population pharmacometrics study will be a very useful starting point for fexofenadine precision medicine.

关键词： OATP1B1 OATP2B1 fexofenadine Population pharmacometrics Genetic polymorphism

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Rapid and Sensitive LC-MS/MS Method for Quantification of fexofenadine in Human Plasma——Application to a Bioequivalence Study in Chinese Volunteers

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Chemical Research in Chinese Universities 2007年第5期23卷 514-517页

作者： TENG Guo-sheng TENG Le-sheng WU Yi TANG Yun-biao LIU Lan-ying GU Jing-kai　 Research Center for Drug Metabolism College of Life Science School of Pharmaceutical Science Jilin University Changchun 130021 P. R. China Department of Pharmacy General Hospital of Shenyang Military Command Shenyang 110016 P. R. China

A rapid and sensitive liquid chromatography-tandem mass spectrometry method（LC-MS/MS）was developed and validated for the quantification of fexofenadine in human plasma,to conduct comparative bioavailability studies.Human plasma was extracted with a mixture of dichloromethane-diethyl ether（volume ratio 2∶3）in a basic environment and the extract was separated on a C18 column with a mobile phase consisting of acetonitrile-methanol-10 mmol/L ammonium acetate（volume ratio 45∶45∶10）.The analytes were detected via electrospray ionization（ESI）tandem mass spectrometry in the multiple-reaction-monitoring（MRM）mode.The linearity was within a range of 1-1000 ng/mL.The intra-and inter-day precision were〈4.1% and〈4.8%,respectively,and the accuracy was in the range of 95.0%-105%.The method was applied to the quantification of fexofenadine human plasma from 20 healthy male Chinese volunteers,according to a single dose,randomized,two-way crossover design with a two-week washout period.The mean values of major pharmacokinetic parameters of ρmax,AUC0-48,AUC0-∞,tmax,and t1/2 were determined from the plasma concentration.The analysis of variance（ANOVA）did not show any significant difference between the two products of fexofenadine and 90% confidence intervals fell within the acceptable range for bioequivalence.

关键词： fexofenadine Bioequivalence LC-MS/MS Human plasma

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Effect of fexofenadine, a mast cell blocker, in infertile men with significantly increased testicular mast cells

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Asian Journal of Andrology 2002年第4期4卷 291-294页

作者： Selahittin ayan Duygu Dusmez Apa Erdem Akbay Department of Urology Department of Pathology University of Mersin School of Medicine Mersin 33079 TurkeyDepartment of Urology

Aim: To investigate the role of fexofenadine, a mast cell blocker, on semen quality in the treatment of infertile men. Methods: The study included 16 Turkish idiopathic infertile men with azoospermia or oligozoospermia who underwent testicular biopsy to examine mast cells containing tryptase. In all patients, a complete medical history, clinical examination, semen analysis and serum hormone assay were carried out. The biopsy specimens were immunohistochemically stained with antihuman tryptase for mast cells. The number of total mast cells per seminiferous tubule was calculated and recorded as mast cell index. The patients were divided into two groups according to their mast cell index: the higher (≥1, n=9) and the lower (fexofenadine was administered orally at a dose of 180 mg/day for 4 to 9 months. Pre-and post-treatment semen parameters, including total motile sperm counts (TMC) were recorded and compared. Spontaneous pregnancies after the treatment were registered. Results: There was no statistically significant difference in TMC between the pre-treatment and post-treatment values in patients with higher and lower mast cell index (P≥0.05). In both groups, nobody had a significant response to the treatment and there was no spontaneous pregnancy after the treatment. Conclusion: Although testicular dysfunction is closely associated with increased number of testicular mast cells, fexofenadine, a mast cell blocker, appears not having any benefit in the treatment of Turkish infertile men with a significant increase in testicular mast cells. (Asian J Androl 2002 Dec; 4: 291-294)

关键词： male infertility testicular biopsy mast cells mast cell blocker fexofenadine semen quality

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Development of Fast Dissolving Tablets Containing fexofenadine Hydrochloride Prepared by Lyophilization Technique

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Journal of Pharmacy and Pharmacology 2019年第10期7卷 527-540页

作者： Rajendra Kotadiya Bhavin Bhalani Ramanbhai Patel College of Pharmacy Charotar University of Science and Technology (CHARUSAT) Changa Gujarat 388421 India Indukaka Ipcowala College of Pharmacy New V V Nagar Anand Gujarat 388121 India

Objectives: To improve the aqueous solubility and dissolution of fexofenadine HCl, an attempt was made to prepare its fast dissolving tablets by lyophilization technique. Methods: For the preparation of lyophilized tablets (F1-F32), the drug was dispersed in a hydrated solution of water-soluble polymers (gelatin/maltodextrin/acacia) containing glycine and mannitol. The blend was pelted down into the patches of a blister pack, frozen down and then lyophilized. Different characterization parameters viz. differential scanning calorimetry, hardness, weight variation, X-ray diffraction (XRD), scanning electron microscopy (SEM), mercury porosimetry, solubility, wetting time and water absorption ratio, lyophilization tablet index, drug content, in vitro dissolution and stability were evaluated. Key findings: Tablets (F32) containing acacia were found to have fast disintegration and relatively higher mechanical strength with improved drug solubility. X-ray diffractogram and scanning electron micrograph indicated decrease in crystallinity of drug and a good porous structure property for prepared tablet, respectively. Dissolution study showed complete drug released within 5 min. Moreover, tablets (F32) were found to be stable for one month at 25 ± 2 °C/60 ± 5% relative humidity.

关键词： Lyophilization fexofenadine HCl SEM XRD lyophilized tablet index (LTI) mercury porosimetry wetting time

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过敏性鼻炎治疗剂fexofenadine HCl

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国外新药介绍 1997年第2期 36-39页

作者：陈泽均

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Simultaneous Determination of Amlodipine with H<sub>1</sub>-Receptor Antagonists by Reversed Phase High Performance Liquid Chromatography and Application to Interaction Studies

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American Journal of Analytical Chemistry 2012年第9期3卷 632-637页

作者： Muhammad Saeed Arayne Najma Sultana Saima Sher Bahadur Muhammad Nawaz Department of Chemistry United Arab Emirates University Al-Ain UAE Department of Chemistry University of Karachi Karachi Pakistan Research Institute of Pharmaceutical Sciences Department of Pharmaceutical Chemistry Faculty of Pharmacy University of Karachi Karachi Pakistan

A rapid, fast and precise method has been developed and validated for the simultaneous determination of amlodipine with H1-receptor antagonists (cetirizine, fexofenadine, and buclizine) from dosage forms. The chromatography was performed on a Purospher? Star, C18 (5 mm, 250 × 4.6 mm) column using acetonitrile: buffer (0.01 mM) (40:60, v/v, pH adjusted to 3.0), as a mobile phase. The mobile phase was pumped at a flow rate of 1.0 mL·min-1 and UV detection was performed at 240 nm. The method was validated for linearity, accuracy, precision and specificity. The method was applied to study the interaction between amlodipine and H1-receptor antagonists. These interactions were carried out in simulated gastric juice (pH 1), simulated full stomach (pH 4), blood pH (pH 7.4) and simulating GI (pH 9). The interacting drugs were heated at 37℃ with intermit-tent shaking and the samples were withdrawn every thirty minutes for three hours and drug contents were analyzed by RP-HPLC techniques. In most cases the in vitro availability of amlodipine was decreased. It was observed that the change in in vitro availability was pH dependent.

关键词： Amlodipine Cetirizine fexofenadine Buclizine Interactions Reversed Phase High Performance Liquid Chromatography

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抗组胺药fexofenadine Hydrochloride

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药学进展 2004年第6期28卷 288-288页

作者：沈磊

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