An ultra high-performance liquid chromatographic method was developed to study the cinitapride metabolism. Metabolites were generated from the incubation of cinitapride with human liver microsomes. Cinitapride and its metabolites were separated by reversed-phase mode using a formate aqueous solution (pH 6.5) and acetonitrile as the components of the mobile phase. Chromatographic conditions, including the establishment of an elution gradient, were optimized for obtaining the maximum number of resolved components in the minimum analysis time. Experimental design and multicriteria decision-making strategies were utilized to facilitate the optimization of chromatographic conditions. Figures of merit were evaluated with cinitapride standards and incubated samples. Limits of detection are about 0.03 μmol/L, and repeatabilities are better than 0.06% for retention times and better than 3.5% for concentrations. The method was applied to characterize the in vitro cinitapride metabolism with human liver microsomes.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1002/jssc.201100073 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
CYP2C8*3 and *4 define CYP2C8 phenotype: An approach with the substrate cinitapride.
Clin Transl Sci
November 2022
Clinical Pharmacology Department, Instituto Teófilo Hernando, Instituto de Investigación Sanitaria La Princesa (IP), Hospital Universitario de La Princesa, Universidad Autónoma de Madrid (UAM), Madrid, Spain.
Article Synopsis
- Cinitapride is a gastrointestinal drug used for functional dyspepsia and gastroesophageal reflux disease, and this study investigates the effects of genetic variants on its pharmacokinetics and safety.
- Researchers genotyped healthy volunteers for variants in 19 pharmacogenes, identifying that carriers of the CYP2C8*3 allele had significantly reduced drug exposure, while *4 allele carriers had increased exposure, although not statistically significant.
- The study helps define pharmacogenetic phenotypes for metabolizers of cinitapride, emphasizing the need for further research to fully understand the implications for other drugs metabolized by CYP2C8.
Stability and in vitro release kinetic studies of cinitapride (1mg) mouth dissolving tablets.
Pak J Pharm Sci
March 2019
Department of Pharmaceutics, Faculty of Pharmacy and Pharmaceutical Sciences, University of Karachi, Karachi, Pakistan.
Cinitapride has been widely given in gastro-esophageal reflux disease (GERD) and dysphagia due to irregularities of GI motilities. Mouth dissolving tablets were prepared for rapid availability and action of drug. Multi-point dissolution studies were conducted in 0.
View Article and Find Full Text PDFFormulation design, characterization and optimization of cinitapride (1mg) immediate release tablets using direct compression technology.
Pak J Pharm Sci
November 2018
Department of Pharmaceutics, Faculty of Pharmacy, Dow University of Health Sciences, Karachi, Pakistan.
Cinitapride hydrogen tartarate is relatively a new prokinetic agent that widely prescribed for GERD and epigastric pain. Present study was aimed to develop and optimize cinitapride (1 mg) immediate release (IR) tablet formulation(s) by direct compression using central composite rotatable technique. Overall nine formulations (FC1-FC9) were generated by varying the composition of binder avicel PH 102 (X1) and superdisintegrant crospovidone (X2).
View Article and Find Full Text PDFThe exploration of novel Alzheimer's therapeutic agents from the pool of FDA approved medicines using drug repositioning, enzyme inhibition and kinetic mechanism approaches.
Biomed Pharmacother
January 2019
College of Natural Science, Department of Biological Sciences, Kongju National University, Gongju, 32588, South Korea. Electronic address:
Novel drug development is onerous, time consuming and overpriced process with particularly low success and relatively high enfeebling rates. To overcome this burden, drug repositioning approach is being used to predict the possible therapeutic effects of FDA approved drugs in different diseases. Herein, we designed a computational and enzyme inhibitory mechanistic approach to fetch the promising drugs from the pool of FDA approved drugs against AD.
View Article and Find Full Text PDFPharmacokinetics and tolerability of cinitapride in healthy Chinese volunteers: a randomized, open-label, single- and multiple-dose study.
Xenobiotica
March 2019
a Department of Clinical Pharmacology Lab , Nanjing First Hospital, Nanjing Medical University, Nanjing , Jiangsu , China.
Cinitapride (CIN) is a drug for functional dyspepsia. The purpose of the study was to investigate the pharmacokinetics and tolerability of CIN in healthy Chinese volunteers. A randomized, open-label, single- and multiple-dose study was conducted in 12 healthy volunteers.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!