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A Study to Investigate the Effect of Urine Acid-base Disequilibrium on the Pharmacokinetics of Captopril

Phase 1
Completed
Conditions
Hypertension
Interventions
Registration Number
NCT06292091
Lead Sponsor
Seoul National University Hospital
Brief Summary

The aim of this study is to evaluate the effect of urine acid-base disequilibrium on the pharmacokinetics of captopril in healthy male volunteers.

Detailed Description

* Pharmacokinetic analysis of captopril before and after urine acid-base imbalance

* Safety analysis

Recruitment & Eligibility

Status
COMPLETED
Sex
Male
Target Recruitment
12
Inclusion Criteria
  • Healthy male volunteer aged 19 to 50 years at screening

  • Body weight between 50.0 kg and 90.0 kg and body mass index (BMI) between 18.5 kg/m2 and 29.9 kg/m2 at screening

    • Body Mass Index (kg/m2) = Weight (kg)/{Height (m)}2
  • Participants who voluntarily decided to participate and agreed in writing to comply with study instructions after receiving sufficient explanation and complete understanding of the study

  • Participants who are suitable as test subjects for this test as determined by the investigator through physical examination, clinical laboratory tests, and interviews, etc.

Exclusion Criteria
  • Participants who have or have a history of clinically significant hepatobiliary system (severe liver failure, viral hepatitis, etc.), kidney (severe renal impairment, etc.), nervous system, immune system, respiratory system, digestive system, endocrine system, blood/tumor, cardiovascular system (heart failure, Torsades de pointes, etc.), urinary system, mental system (mood disorder, obsessive-compulsive disorder, etc.), and sexual dysfunction, etc.

  • Evidence or past history of gastrointestinal disease (Crohn's disease, gastrointestinal ulcer, gastritis, gastroesophageal reflux disease, etc.) or past history of gastrointestinal surgery (except for simple appendectomy and hernia repair) that might affect the safety and PK assessment of the investigational product.

  • Hypersensitivity to drugs including captopril, sodium bicarbonate, and torsemide or other drugs (aspirin, antibiotics, etc.) or history of clinically significant hypersensitivity reactions

  • Participants with genetic problems such as lactose intolerance, Lapp lactase deficiency, or glucose-galactose malabsorption

  • Positive serum test (HBs antigen, HCV antibody, HIV antigen-antibody, and RPR) at screening

  • Past history of alcohol and drug abuse or a positive urine test for drugs with abuse potential at screening

  • Any abnormalities in vital signs after 3 minutes rest at screening

    • Systolic blood pressure < 90 mmHg or > 150 mmHg, Diastolic blood pressure < 60 mmHg or > 100 mHg
  • QT/QTcF > 450 msec or any abnormalities on electrocardiogram (ECG) at screening

  • Any abnormalities in blood tests at screening

    • AST (SGOT), ALT (SGPT) > 60 IU/L, creatinine clearance (CKD-EPI equation) < 80 mL/min
  • Past or planned treatment with any prescription drugs or herbal medicine within 2 weeks, or any over the counter drugs, health functional foods, or vitamin supplements within 1 week, prior to the first scheduled dose (individual who is eligible based on other criteria may participate in the study at the discretion of the investigator).

  • Participants who have taken drugs that induce drug-metabolizing enzymes such as barbiturates or inhibit drug metabolism such as clarithromycin within 1 month prior to the first scheduled dose

  • Treatment with any investigational product in another clinical trial within 6 months prior to the first scheduled dose

Study & Design

Study Type
INTERVENTIONAL
Study Design
SEQUENTIAL
Arm && Interventions
GroupInterventionDescription
Sodium bicarbonate+captoprilCaptopril 12.5 MgSingle dose of captopril 12.5 mg during multiple doses of sodium bicarbonate 1 g every 4-6 hours
Torsemide+captoprilCaptopril 12.5 MgSingle dose of captopril 12.5 mg during multiple doses of torsemide 20 mg every 6-12 hours
Sodium bicarbonate+captoprilSodium bicarbonate 4 GSingle dose of captopril 12.5 mg during multiple doses of sodium bicarbonate 1 g every 4-6 hours
Torsemide+captoprilTorsemide 20 MGSingle dose of captopril 12.5 mg during multiple doses of torsemide 20 mg every 6-12 hours
CaptoprilCaptopril 12.5 MgSingle dose of captopril 12.5 mg
Primary Outcome Measures
NameTimeMethod
AUClast of captoprilPre-dose (0 hour) and up to 12 hours in each period

Area under the concentration-time curve from 0 to last measurable concentration (AUClast)

Cmax of captoprilObserved value among pre-dose (0 hour) and up to 12 hours in each period

Maximum concentration of captopril (Cmax)

Secondary Outcome Measures
NameTimeMethod
AUCinf of captoprilPre-dose (0 hour) and up to 12 hours in each period

Area under the concentration-time curve from 0 to infinite (AUCinf)

CL/F of captoprilPre-dose (0 hour) and up to 12 hours in each period

Apparent clearance (CL/F)

Tmax of captoprilObserved time point among pre-dose (0 hour) and up to 12 hours in each period

Time to Cmax (Tmax)

urine pHPre-dose (0 hour) and up to 12 hours in each period

urine pH

t1/2 of captoprilPre-dose (0 hour) and up to 12 hours in each period

half-life (t1/2)

Vd/F of captoprilPre-dose (0 hour) and up to 12 hours in each period

Apparent volume of distribution (Vd/F)

fe of captoprilPre-dose (0 hour) and up to 12 hours in each period

Fraction of urinary excretion (fe)

Safety parametersThrough study completion, an average of 3 months

Number and frequency of participants observed adverse events in each period

Trial Locations

Locations (1)

Seoul National University Hospital

🇰🇷

Seoul, Korea, Republic of

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