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Pharmacokinetics of Bisacodyl or Sodium Picosulfate Administered Orally in Healthy Lactating Females

Phase 1
Completed
Conditions
Healthy
Interventions
Registration Number
NCT02211911
Lead Sponsor
Boehringer Ingelheim
Brief Summary

To investigate if bisacodyl (Dulcolax®) and sodium picosulfate (Laxoberal®) is excreted in breast milk of healthy lactating women after an oral administration of 10 mg once daily over a period of 8 days.

Detailed Description

Not available

Recruitment & Eligibility

Status
COMPLETED
Sex
Female
Target Recruitment
16
Inclusion Criteria
  • Women, age ≥18 and ≤50 years
  • Stopped with breast feeding their baby
  • Provided breast milk samples over a period of 10 days (including day -1)
  • Have been breast feeding for at least 14 days
  • Complied with the requirements of the protocol (e.g complete a diary)
  • Body Mass Index (BMI) ≤ 35 kg/m2
  • Medically acceptable method of contraception [i.e., double barrier method (e.g., diaphragm or condom and spermicide), hormonal therapy (subcutaneous, injectable, intra-vaginal, or oral contraceptive) or intrauterine device
  • Signed and dated a written informed consent prior to any study procedures study in accordance with Good Clinical practice (GCP) and the local legislation
Exclusion Criteria
  • Findings during medical examination (including BP, pulse rate and ECG) deviating from normal and of clinical relevance
  • Evidence of clinically relevant concomitant diseases like renal insufficiency, cardiac insufficiency, myocardial infarction, other known cardiovascular disease including hypertension
  • Gastrointestinal, hepatic, renal, respiratory, cardiovascular, metabolic, immunological or hormonal disorders, that may interfere with the safety of the subject
  • Surgery of the gastrointestinal tract (except appendectomy) in the last 2 years
  • Metabolic disorders, neurological disorders, severe or psychiatric disorders, or any other significant disease or intercurrent illness (e.g. abdominal/gastrointestinal surgery) that would interfere with participation in the study
  • History of relevant orthostatic hypotension, fainting spells or blackouts
  • Chronic or relevant acute infections (e.g. HIV, Hepatitis)
  • Participated in another study with an investigational product within 1 month prior to enrolment into this study or during the study
  • Eating disorder
  • Hypersensitivity to bisacodyl, sodium picosulfate or any of the inactive ingredients
  • Any concomitant medication except for paracetamol or hormonal therapy.
  • Abnormal electrolyte values at the screening visit. The electrolyte values should be within the normal ranges
  • Alcohol abuse; subjects who report regular consumption of 40g/day = 5 units/day or more alcoholic drinks per day were excluded
  • Smoker (>10 cigarettes or > 3 cigars or > 3 pipes/day)
  • Drug abuse
  • Any laboratory value outside the reference range that is of clinical relevance
  • Mastitis
  • Less than 200 ml daily (24 hours) production of breast milk on day -1
  • A positive pregnancy test at screening

Study & Design

Study Type
INTERVENTIONAL
Study Design
PARALLEL
Arm && Interventions
GroupInterventionDescription
BisacodylBisacodyl-
Sodium picosulfateSodium picosulfate-
Primary Outcome Measures
NameTimeMethod
λz (terminal rate constant in plasma)up to 8 days
AUC0-tz (area under the concentration-time curve of the analyte in plasma over the time interval from 0 to the last quantifiable concentration at tz)up to 8 days
MRTpo (mean residence time of the analyte in the body after oral administration)up to 8 days
fet1-t2 (fraction of analyte eliminated in urine from time point t1 to time point t2)up to 8 days
CL/F (apparent clearance of the analyte in plasma following extravascular administration)up to 8 days
Cmax (maximum measured concentration of the analyte in plasma)up to 8 days
%AUCtz-∞ (the percentage of the AUC 0-∞ that is obtained by extrapolation)up to 8 days
t1/2 (terminal half-life of the analyte in plasma)up to 8 days
tmax (time from dosing to maximum measured concentration of the analyte in plasma)up to 8 days
AUCτ,1 (area under the concentration-time curve of the analyte in plasma over a uniform dosing interval τ after administration of the first dose)up to 8 days
AUC0-∞ (area under the concentration-time curve of the analyte in plasma over the time interval from 0 extrapolated to infinity)up to 8 days
Vz/F (apparent volume of distribution during the terminal phase λz following an extravascular administration)up to 8 days
Aet1-t2,milk (amount of analyte in milk from the time point t1 to time point t2)up to 8 days
AUCτ,milk (area under the concentration-time curve of the analyte in milk over a uniform dosing interval τ after administration of the first dose)up to 8 days
Aet1-t2 (amount of analyte that is eliminated in urine from the time point t1 to time point t2)up to 8 days
CLR,t1-t2 (renal clearance of the analyte from the time point t1 until the time point t2)up to 8 days
fet1-t2,milk (fraction of analyte in milk from time point t1 to time point t2)up to 8 days
milk to plasma ratio (AUCτ,milk / AUCτ)up to 8 days
Cmin,ss (minimum concentration of the analyte in plasma at steady state over a uniform dosing interval τ)up to 8 days
estimated daily infant dosageup to 8 days

(milk-to-plasma ratio x average maternal plasma concentration x 150 mL/kg/day)

Secondary Outcome Measures
NameTimeMethod
Number of patients with adverse eventsup to 8 days
Number of patients with abnormal laboratory findingsup to 8 days
Number of patients with clinically significant changes in vital signsup to 8 days
Number of patients with abnormal electrocardiogram findingsup to 8 days
Number of bowel movementsup to 8 days
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