Bioequivalence of a New Oral Levosulpiride Formulation Compared With a Standard One in Healthy Volunteers

Gregori, Simona De; Cipollina, L.; Silvestri, Annalisa De; Ventura, Marianna; Michelini, Roberta; Morosini, Monica; Montagna, Michela; Tinelli, Carmine; Regazzi, Mario; Molinaro, Mariadelfina; Imberti, Roberto

doi:10.1097/ftd.0000000000000380

Cited by 2 publications

References 9 publications

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Development and validation of a reversed-phase HPLC-UV method for simultaneous determination of levosulpiride and omeprazole in human plasma: Applicability of the method for evaluation of pharmacokinetic drug-drug interactions

Hashim,

Ahmad,

Khan

et al. 2024

PLoS ONE

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Levosulpiride and omeprazole are co-prescribed for gastrointestinal disorders associated with depression and anxiety. Objective of the study was to develop a sensitive, robust and simple method for simultaneous analysis of levosulpiride and omeprazole in human plasma and applicability of the method in determination of pharmacokinetics drug-drug interaction. In the presented study, a reversed-phase HPLC-UV method was developed for the simultaneous determination of levosulpiride and omeprazole using pantoprazole as the internal standard. Experimental conditions were optimized and the developed method was validated as per standard guidelines (USP and ICH). Furthermore, the developed method was applied for evaluation of pharmacokinetics drug-drug interaction between levosulpiride (50 mg) and omeprazole (40 mg) in healthy human volunteers. Sharpsil C8 column (4.6 × 250 mm, 5 μm), Ultisil C8 column (4.6 mm × 150 mm, 5 μm) and Agilent C18 column (4.6 × 250 mm, 5 μm) were evaluated as stationary phase. The best resolution was achieved with Agilent C18 (4.6 x 250 mm, 5 μm) column and was selected for further study. The mobile phase consisted of a mixture of acetonitrile and phosphate buffer (pH 7.2) in 60:40 by volume, and was pumped at a flow rate of 1 mL/min. Detector wavelength was set at 280 nm. Levosulpiride and omeprazole were extracted from human plasma with ethyl acetate and dichloromethane (4:1, v/v). The calibration curves for both levosulpiride (5–150 ng/mL) and omeprazole (10–1500 ng/mL) were linear. The lower limit of quantification and limit of detection for levosulpiride were 5 and 2 ng/mL, while for omeprazole these were 10 and 3 ng/mL, respectively. Pharmacokinetics analysis showed that co-administration of omeprazole increased the AUC and Cmax of levosulpiride, while the clearance was reduced. Both the changes were insignificant. Similarly, no significant change in the pharmacokinetic parameters of omeprazole was observed with co-administration of levosulpiride.

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Development and validation of a reversed-phase HPLC-UV method for simultaneous determination of levosulpiride and omeprazole in human plasma: Applicability of the method for evaluation of pharmacokinetic drug-drug interactions

Hashim,

Ahmad,

Khan

et al. 2024

PLoS ONE

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Case Report: CYP1A2 Ultra-Rapid Metabolizer in schizophrenia with multiple overdose antipsychotics

Yang,

Cao,

et al. 2023

Preprint

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Background Liver cytochrome P450 (CYP450) enzymes play an important role in metabolizing antipsychotics (APs) and other drugs. Excessive use of drugs can impair liver function and even other organs, thus causing several adverse effects. In addition, metabolizer types of CYP450 enzymes may influence the therapeutic effects and drug reactions. Case presentation In this case, we described a patient with schizophrenia who took overdose of multiple kinds of APs and other herbal preparations together for nearly two years. However, poor treatment effects and minor side effects of APs were presented in this patient. After pharmacogenomic examination, we found this patient was a CYP1A2 ultra-rapid metabolizer. Conclusions CYP1A2 ultra-rapid metabolizer may explain part of the poor therapeutic effects and small adverse effects in this case who took multiple kinds of overdose drugs. Many factors may be involved in the rare presentations in this patient.

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Bioequivalence of a New Oral Levosulpiride Formulation Compared With a Standard One in Healthy Volunteers

Cited by 2 publications

References 9 publications

Development and validation of a reversed-phase HPLC-UV method for simultaneous determination of levosulpiride and omeprazole in human plasma: Applicability of the method for evaluation of pharmacokinetic drug-drug interactions

Development and validation of a reversed-phase HPLC-UV method for simultaneous determination of levosulpiride and omeprazole in human plasma: Applicability of the method for evaluation of pharmacokinetic drug-drug interactions

Case Report: CYP1A2 Ultra-Rapid Metabolizer in schizophrenia with multiple overdose antipsychotics

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