Pharmacokinetics Study Comparing Topical Diclofenac/Menthol Gels With Voltaren Gel and Oral Diclofenac Sodium

• Sponsor: GlaxoSmithKline (Industry)
• Overall Status: Completed
• CT.gov ID: NCT02201238
• Collaborator: (none)
• Enrollment: 18
• Location: 1
• Arms: 4
• Actual Duration (Months): 1.7
• Patients Per Site Per Month: 10.7

Study Details

Study Description

Brief Summary

This research study is being conducted to characterize the pharmacokinetic properties of a new topical medication (MFC51123) that contains two active ingredients (diclofenac and menthol) in two formulation packages. One formulation package is in the form of a gel in aluminum tube and the other one in the form of a gel in roll-on applicator bottle. Additionally, as a comparison, the pharmacokinetic properties of a marketed diclofenac gel and an oral diclofenac treatment will also be characterized. This topical diclofenac/menthol gel has being developed to treat mild to moderate pain and inflammation, such as acute sport injuries, sprains and strains. The rationale for conducting the study is to prove that repeated topical treatment of the new diclofenac + menthol formulation in either of the two packages does not result in unsafe systemic exposure.

Condition or Disease	Intervention/Treatment	Phase
Pain	Drug: Diclofenac sodium; Drug: Menthol	Phase 1

Study Design

• Study Type: Interventional
• Actual Enrollment: 18 participants
• Allocation: Randomized
• Intervention Model: Crossover Assignment
• Masking: None (Open Label)
• Primary Purpose: Other
• Official Title: A Pharmacokinetics Study Comparing Systemic Exposure of Topical Diclofenac/Menthol Gels Versus Voltaren Gel and Oral Diclofenac Sodium in Healthy Volunteers at Steady State
• Actual Study Start Date: Oct 1, 2014
• Actual Primary Completion Date: Nov 21, 2014
• Actual Study Completion Date: Nov 21, 2014

Arms and Interventions

Arm	Intervention/Treatment
Experimental: Diclofenac sodium/menthol gel (in tube) 1% diclofenac sodium plus 3% menthol gel (in 30g aluminium tube). Dose given- 4g applied topically to a 400cm2 (20cm x 20cm) area of the skin, four times daily for three consecutive days with 5h between adjacent doses on the same day	Drug: Diclofenac sodium; Diclofenac sodium; Drug: Menthol; Menthol
Experimental: Diclofenac sodium/menthol gel (in roll-on device) 1% diclofenac sodium plus 3% menthol gel (in roll-on applicator device supplied in 30g plastic bottles). Dose given- 4g applied topically to a 400cm2 (20cm x 20cm) area of the skin, four times daily for three consecutive days with 5h between adjacent doses on the same day	Drug: Diclofenac sodium; Diclofenac sodium; Drug: Menthol; Menthol
Active Comparator: Diclofenac sodium tablets 50mg diclofenac sodium tablets administered orally, three times daily for three consecutive days with 6h between adjacent doses on the same day	Drug: Diclofenac sodium; Diclofenac sodium
Active Comparator: Voltaren gel Voltaren gel supplied in 100g aluminium tube. Dose given- 4g applied topically to a 400cm2 (20cm x 20cm) area of the skin, four times daily for three consecutive days with 5h between adjacent doses on the same day	Drug: Diclofenac sodium; Diclofenac sodium

Outcome Measures

Primary Outcome Measures

1. AUC48-72 hrs of Diclofenac gel in tube/AUC48-72 hrs of oral Diclofenac [20 days]

   Ratio of area under the plasma concentration time curve from 48-72 hrs (AUC48-72 hrs) of Diclofenac gel in tube and AUC48-72 hrs of oral Diclofenac during the final 24 hours of dosing at steady state will assess systemic exposure to Diclofenac from gel as compared to that from oral Diclofenac

2. Cmax of Diclofenac gel in tube/Cmax of oral Diclofenac [20 days]

   Ratio of maximum plasma concentration (Cmax) of Diclofenac gel in tube and Cmax of oral Diclofenac during the final 24 hours of dosing at steady state will assess systemic exposure to Diclofenac from gel as compared to that from oral Diclofenac

3. AUC48-72 hrs of Diclofenac gel in roll-on device/AUC48-72 hrs of oral Diclofenac [20 days]

   Ratio of AUC48-72 hrs of Diclofenac gel in roll-on device and AUC48-72 hrs of oral Diclofenac during the final 24 hours of dosing at steady state will assess systemic exposure to Diclofenac from roll-on device as compared to that from oral Diclofenac

4. Cmax of Diclofenac gel in roll-on device/Cmax of oral Diclofenac [20 days]

   Ratio of Cmax of Diclofenac gel in roll-on device and Cmax of oral Diclofenac during the final 24 hours of dosing at steady state will assess systemic exposure to Diclofenac from roll-on device as compared to that from oral Diclofenac

Secondary Outcome Measures

1. Cmin of Diclofenac gel in tube/Cmin of oral Diclofenac [20 days]

   Ratio of minimum plasma concentration (Cmin) of Diclofenac gel in tube and Cmin of oral Diclofenac during the final 24 hours of dosing at steady state will assess systemic exposure to Diclofenac from gel as compared to that from oral Diclofenac

2. Tmax of Diclofenac gel in tube/Tmax of oral Diclofenac [20 days]

   Ratio of time to maximum plasma concentration (Tmax) of Diclofenac gel in tube and Tmax of oral Diclofenac during the final 24 hours of dosing at steady state will assess systemic exposure to Diclofenac from gel as compared to that from oral Diclofenac

3. Cmin of Diclofenac gel in roll-on device/Cmin of oral Diclofenac [20 days]

   Ratio of Cmin of Diclofenac gel in roll-on device and Cmin of oral Diclofenac during the final 24 hours of dosing at steady state will assess systemic exposure to Diclofenac from roll-on device as compared to that from oral Diclofenac

4. Tmax of Diclofenac gel in roll-on device/Tmax of oral Diclofenac [20 days]

   Ratio of Tmax of Diclofenac gel in roll-on device and Tmax of oral Diclofenac during the final 24 hours of dosing at steady state will assess systemic exposure to Diclofenac from roll-on device as compared to that from oral Diclofenac

5. Cmax of Diclofenac gel in tube/Cmax of Diclofenac in Voltaren gel [20 days]

   Ratio of Cmax of Diclofenac gel in tube and Cmax of Voltaren gel during the final 24 hours of dosing at steady state will assess systemic exposure to Diclofenac from gel as compared to that from Voltaren gel

6. Cmax of Diclofenac gel in roll-on device/Cmax of Diclofenac in Voltaren gel [20 days]

   Ratio of Cmax of Diclofenac gel in roll-on device and Cmax of Voltaren gel during the final 24 hours of dosing at steady state will assess systemic exposure to Diclofenac from roll-on device as compared to that from Voltaren gel

7. Cmin of Diclofenac gel in tube/Cmin of Diclofenac in Voltaren gel [20 days]

   Ratio of Cmin of Diclofenac gel in tube and Cmin of Voltaren gel during the final 24 hours of dosing at steady state will assess systemic exposure to Diclofenac from gel as compared to that from Voltaren gel

8. Cmin of Diclofenac gel in roll-on device/Cmin of Diclofenac in Voltaren gel [20 days]

   Ratio of Cmin of Diclofenac gel in roll-on device and Cmin of Voltaren gel during the final 24 hours of dosing at steady state will assess systemic exposure to Diclofenac from roll-on device as compared to that from Voltaren gel

9. AUC48-72 hrs of Diclofenac gel in tube/AUC48-72 hrs of Diclofenac in Voltaren gel [20 days]

   Ratio of AUC48-72 hrs of Diclofenac gel in tube and AUC48-72 hrs of Voltaren gel during the final 24 hours of dosing at steady state will assess systemic exposure to Diclofenac from gel as compared to that from Voltaren gel

10. AUC48-72 hrs of Diclofenac gel in roll-on device/AUC48-72 hrs of Diclofenac in Voltaren gel [20 days]

    Ratio of AUC48-72 hrs of Diclofenac gel in roll-on device and AUC48-72 hrs of Voltaren gel during the final 24 hours of dosing at steady state will assess systemic exposure to Diclofenac from roll-on device as compared to that from Voltaren gel

11. Tmax of Diclofenac gel in tube/Tmax of Diclofenac in Voltaren gel [20 days]

    Ratio of Tmax of Diclofenac gel in tube and Tmax of Voltaren during the final 24 hours of dosing at steady state will assess systemic exposure to Diclofenac from gel as compared to that from Voltaren gel

12. Tmax of Diclofenac gel in roll-on device/Tmax of Diclofenac in Voltaren gel [20 days]

    Ratio of Tmax of Diclofenac gel in roll-on device and Tmax of Voltaren during the final 24 hours of dosing at steady state will assess systemic exposure to Diclofenac from roll-on device as compared to that from Voltaren gel

13. Cmax of Menthol in gel/Cmax of Menthol reported in literature [20 days]

    Ratio of Cmax of Menthol in tube and Cmax of Menthol reported in literature will assess systemic exposure to menthol from gel tube as compared to that reported in literature

14. Cmax of Menthol in roll-on device/Cmax of Menthol reported in literature [20 days]

    Ratio of Cmax of Menthol in roll-on device and Cmax of Menthol reported in literature will assess systemic exposure of menthol from roll-on device as compared to that reported in literature

15. Cmin of Menthol in gel/Cmin of Menthol reported in literature [20 days]

    Ratio of Cmin of Menthol in tube and Cmin of Menthol reported in literature will assess systemic exposure to menthol from gel tube as compared to that reported in literature

16. Cmin of Menthol in roll-on device/Cmin of Menthol reported in literature [20 days]

    Ratio of Cmin of Menthol in roll-on device and Cmin of Menthol reported in literature will assess systemic exposure of menthol from roll-on device as compared to that reported in literature

17. Tmax of Menthol in gel/Tmax of Menthol reported in literature [20 days]

    Ratio of Tmax of Menthol in tube and Tmax of Menthol reported in literature will assess systemic exposure to menthol from gel tube as compared to that reported in literature

18. Tmax of Menthol in roll-on device/Tmax of Menthol reported in literature [20 days]

    Ratio of Tmax of Menthol in roll-on device and Tmax of Menthol reported in literature will assess systemic exposure of menthol from roll-on device as compared to that reported in literature

19. T1/2 of Menthol in gel/T1/2 of Menthol reported in literature [20 days]

    Ratio of half time elimination (T1/2) of Menthol in tube and T1/2 of Menthol reported in literature will assess systemic exposure to menthol from gel tube as compared to that reporetd in literature

20. T1/2 of Menthol in roll-on device/T1/2 of Menthol reported in literature [20 days]

    Ratio of T1/2 of Menthol in roll-on device and T1/2 of Menthol reported in literature will assess systemic exposure of menthol from roll-on device as compared to that reported in literature

21. AUC48-72 hrs of Menthol in gel/AUC48-72 hrs of Menthol reported in literature [20 days]

    Ratio of AUC48-72 hrs of Menthol in gel and AUC48-72 hrs of Menthol reported in literature will assess systemic exposure to menthol from gel tube as compared to that reported in literature

22. AUC48-72 hrs of Menthol in roll-on device/AUC48-72 hrs of Menthol reported in literature [20 days]

    Ratio of AUC48-72 hrs of Menthol in roll-on device and AUC48-72 hrs of Menthol reported in literature will assess systemic exposure of menthol from roll-on device as compared to that reported in literature

23. AUC48-72 hrs of Voltaren gel/AUC48-72 hrs of oral Diclofenac [20 days]

    Ratio of AUC48-72 hrs of Voltaren gel and AUC48-72 hrs of oral Diclofenac will assess systemic exposure of Voltaren gel as compared to oral Diclofenac

24. Cmax of Voltaren gel/Cmax of oral Diclofenac [20 days]

    Ratio of Cmax of Voltaren gel and Cmax of oral Diclofenac will assess systemic exposure of Voltaren gel as compared to oral Diclofenac

25. T1/2 of Diclofenac gel in tube/T1/2 of oral Diclofenac [20 days]

    Ratio of T1/2 of Diclofenac gel in tube and T1/2 of oral Diclofenac will assess systemic exposure to Diclofenac from gel as compared to that from oral Diclofenac

26. T1/2 of Diclofenac gel in roll-on device/T1/2 of oral Diclofenac [20 days]

    Ratio of T1/2 of Diclofenac gel in roll-on device and T1/2 of oral Diclofenac will assess systemic exposure to Diclofenac from roll-on device as compared to that from oral Diclofenac

27. T1/2 of Diclofenac gel in tube/T1/2 of Diclofenac in Voltaren gel [20 days]

    Ratio of T1/2 of Diclofenac gel in tube and T1/2 of Voltaren gel will assess systemic exposure to Diclofenac from gel tube as compared to that from Voltaren gel

28. T1/2 of Diclofenac gel in roll-on device/T1/2 of Diclofenac in Voltaren gel [20 days]

    Ratio of T1/2 of Diclofenac gel in roll-on device and T1/2 of Voltaren gel will assess systemic exposure to Diclofenac from roll-on device as compared to that from Voltaren gel

29. Adverse event monitoring [27 days]

Eligibility Criteria

Criteria

• Ages Eligible for Study: 18 Years to 50 Years
• Sexes Eligible for Study: All
• Accepts Healthy Volunteers: Yes

Inclusion Criteria:

• Participants aged 18 to 50 years

• Body mass index between 19-28 (kg/m2)

Exclusion Criteria:

• Pregnant or lactating females

• Participants having intolerance or hypersensitivity to study material

• Participants having positive results for HIV, Hepatitis B or Hepatitis C

• Participants having skin lesion at site of application

• Participants having history of alcohol or drug abuse

Contacts and Locations

Locations

	Site	City	State	Country	Postal Code
1	GSK Investigational Site	Buffalo	New York	United States	14202

Sponsors and Collaborators

• GlaxoSmithKline

Investigators

• Study Director: GSK Clinical Trials, GlaxoSmithKline

Study Documents (Full-Text)

None provided.

More Information

Publications

None provided.

• Responsible Party: GlaxoSmithKline
• ClinicalTrials.gov Identifier: NCT02201238
• Other Study ID Numbers: 202188; RH02175
• First Posted: Jul 28, 2014
• Last Update Posted: Jun 29, 2017
• Last Verified: Jun 1, 2017

• Additional relevant MeSH terms: Diclofenac; Menthol

Study Results

No Results Posted as of Jun 29, 2017