Pharmacokinetics of a Standard Paracetamol Tablet and Oral Solution After Oral Administration in Chinese Healthy Volunteers

Phase 1

Completed

• Conditions: Focus of Study: Pharmacokinetics Analysis, in Vivo Dissolution Studies
• Interventions: Drug: paracetamol oral solution; Drug: paracetamol tablet

• Registration Number: NCT02095704
• Lead Sponsor: Central South University

Brief Summary

Drug dissolution in vivo play a crucial role for the bioavailability and therapeutic of an orally administered solid dosage form. The aim of this study was to evaluate the pharmacokinetics of a standard paracetamol tablet in comparison with oral solution in Chinese healthy volunteers. Based on the Noyes-Whitney equation and pharmacokinetics parameters, investigators trend to propose a method to estimate in vivo dissolution time and dissolution kinetics of solid dosage form.

Detailed Description

Not available

Study Timeline

• Study Start: 2013-05
• Primary Completion: 2013-05
• Study Completion: 2013-05
• Status Verified: 2014-03
• Study First Submitted: 2014-03-19
• Study First Submitted QC: 2014-03-24
• Last Update Submitted: 2014-03-24
• Study First Posted: 2014-03-26
• Last Update Posted: 2014-03-26

Recruitment & Eligibility

• Status: COMPLETED
• Sex: Male
• Target Recruitment: 6

Inclusion Criteria

1. Sex: Male or female (limited to PK study)
2. Healthy volunteers, age: 18-45（medical history, physical examination, vital signs, ECG and lab tests are qualified during screening）
3. Body Mass Index（BMI）:19~24 or body weight is not less than 50Kg
4. Non-pregnant women confirmed by pregnancy test
5. Vital Signs: after 3 minutes supination, the following measurements criteria should be within ranges: body temperature (axillary temperature), 36.0~37.0 ℃; blood pressure, SBP 90~140mmHg（12.0~18.7kpa）and DBP 60~90mmHg（8.0~12.0kpa）; arterial pulse: 60~100 bpm
6. Non-hypersensitivity to this product or its similar product
7. Non-smoker, non-alcoholic
8. Subject must be able to sign Inform Consent prior to participation into this study
9. Subject must be able to communicate with investigator and comply with study protocol.

Exclusion Criteria

Subjects meet with one or several of the following criteria should be excluded:

1. Subjects failed in physical examination

2. Pregnant or nursing women

3. Administration of a known drug that can cause damage to organs within 3 months

4. Administration of any prescription drug or non-prescription drug 2 weeks before initial dose

5. Before initial dose, participation in any other clinical trials within 3 months

6. Blood donation 3 months before this study, or plan to have blood donation during or one month after this study

7. Diagnosis of clinical evident diseases 2 weeks before initial dose

8. Primary diseases to vital organs

9. Physically or mentally disabled

10. Medical history of specific allergy (asthma, measles, eczematous dermatitis), or known to allergic to similar (including excipients)

11. Any other surgical or internal medicinal conditions that might cause damage to study subjects or will change the absorption, distribution, metabolism and elimination of investigational drug, including:

    • inflammatory intestinal syndrome, peptic ulcer, alimentary tract hemorrhage
    • a history of severe gastrointestinal tract operation, such as gastrectomy, gastrosmoty / jejunostomy or large bowel resection
    • a history of hepatic disease or laboratory examination findings such as ALT, AST, γ-GT or T-Bili showing clinically significant abnormalities to liver
    • a history of renal disease or laboratory examination findings such as creatinine, urea nitrogen, or albuminuria showing clinically significant abnormalities to kidney
    • urination disorder or dysuresia.

12. A history of immunological deficiency disease, or HIV positive

13. HBV or HCV positive

14. Women undergone menstrual period during study

15. Consumption of a significant amount of smoking or drinking, that is drinking more than 28 units of alcohol per week (1 unit: 285ml of beer, 25ml of liquor, or 1 glass of wine), or smoking more than 2 cigarettes

16. Frequent use of sedatives, hypnotics, stabilizers or other addictive drugs

17. Consumption of more than 8 cups of tea, coffee, and or caffeine beverages

18. Unable to complete this study for any others reasons.

19. Investigators.

Study & Design

• Study Type: INTERVENTIONAL
• Study Design: CROSSOVER

Arm && Interventions

Group	Intervention	Description
paracetamol oral solution	paracetamol oral solution	dosage form: paracetamol oral solution;dosage:15.6ml(containing 500 mg of the active ingredient);frequency:single dose
paracetamol tablet	paracetamol tablet	dosage form: paracetamol tablet;dosage: 500 mg;frequency:single dose

Primary Outcome Measures

Name	Time	Method
AUC	one month	AUC:the area under the concentration-time curve
Cmax	one month	Cmax: maximum plasma concentration
Tmax	one month	Tmax: the time point of maximum plasma concentration
MRT	one month	MRT: mean residence time