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Pharmacokinetic Evaluation of Empagliflozin

Phase 1
Completed
Conditions
Diabetes Mellitus
Interventions
Registration Number
NCT03059056
Lead Sponsor
British University In Egypt
Brief Summary

Project PI (Principal Investigator): Dr Bassam Mahfouz Ayoub, Ph.D., Lecturer of Pharmaceutical Chemistry, The British University in Egypt.

Study Design The proposed study will consider the pharmacokinetic evaluation of empagliflozin after administration to Egyptian volunteers and the results will be compared with the other reported ethnic populations. The FDA recognizes that standard methods of defining racial subgroups are necessary to compare results across pharmacokinetic studies, and to assess potential subgroup differences. The design of the study is open labeled, randomized, one treatment, one period, single dose pharmacokinetic study.

Detailed Description

Study Design The proposed study will consider the pharmacokinetic evaluation of empagliflozin after administration to Egyptian volunteers and the results will be compared with the other reported ethnic populations. The FDA recognizes that standard methods of defining racial subgroups are necessary to compare results across pharmacokinetic studies, and to assess potential subgroup differences. The design of the study is open labeled, randomized, one treatment, one period, single dose pharmacokinetic study. The main pharmacokinetic parameters which are Cmax, Tmax, t1/2, elimination rate constant, AUC0-t and AUC0-inf, will be estimated. Fasting of all volunteers will eliminate the possible interaction from food or caffeine consumption. The pharmacokinetic parameters of empagliflozin will be studied in healthy human subjects according to the ethical regulations of World Medical Association Declaration of Helsinki (October 1996) and the International Conference of Harmonisation Tripartite Guideline for Good Clinical Practice. Written informed consent was provided (attached and signed by the six volunteers) in order to be approved by the ethics committee of the Faculty of Pharmacy, The British University in Egypt. The good health of the human subjects was confirmed by a complete medical history and physical examination. Samples from six, healthy, adult, male, smoking, Egyptian volunteers (age: 22-33 years, Average weight: 77.8 kg, Average BMI: 29.2) will be collected at 0, 0.5, 1, 1.5, 2, 3, 4, 8 and 12 h, to be transferred to heparinized centrifuge tubes in order to be analyzed by LC-MS/MS study (developed \& validated) after single oral dose administration of one Jardiance® tablet nominally containing 25 mg of empagliflozin. The blood samples (3 mL of each sample) will be centrifuged at 3000 rpm for 5 minutes, one mL of the plasma will be separated and spiked with 100 µL (equivalent to 100 ng) of internal standard working solution and then the sample preparation and LC-MS/MS determination will be applied. The main pharmacokinetic parameters of the study which are Cmax, Tmax, t1/2, elimination rate constant, AUC0-t and AUC0-inf will be estimated, using a validated excel software. Blood glucose level will be determined for all volunteers at different time intervals to monitor any hypoglycemic effect. The study will be conducted as per FDA guidelines. The development of such correlations between empagliflozin concentrations and its pharmacologic responses will enable clinicians to apply pharmacokinetic principles to actual patient situations. The evaluation of safety of the study will be based on monitoring of blood glucose level, vital signs, pulse rate, monitoring of adverse events, and physical examination.

Recruitment & Eligibility

Status
COMPLETED
Sex
Male
Target Recruitment
6
Inclusion Criteria
  • The good health of the human subjects was confirmed by a complete medical history and physical examination.
Exclusion Criteria
  • Chronic disease

Study & Design

Study Type
INTERVENTIONAL
Study Design
SINGLE_GROUP
Arm && Interventions
GroupInterventionDescription
pharmacokinetic evaluationEmpagliflozin 25mgEmpagliflozin 25 mg
Primary Outcome Measures
NameTimeMethod
Elimination half life12 Hours

The time required for the concentration of the drug to reach half of its original value.

Elimination rate constant12 Hours

The rate at which a drug is removed from the body.

Area under the curve12 Hours

The integral of the concentration-time curve

Cmax12 Hours

The peak plasma concentration of a drug after administration

Tmax12 Hours

Time to reach Cmax.

Secondary Outcome Measures
NameTimeMethod
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