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Pharmacokinetics, Bioavailability and Safety of PENNSAID® Gel

The safety and scientific validity of this study is the responsibility of the study sponsor and investigators. Listing a study does not mean it has been evaluated by the U.S. Federal Government. Read our disclaimer for details. Identifier: NCT01202799
Recruitment Status : Completed
First Posted : September 16, 2010
Last Update Posted : September 23, 2014
Information provided by (Responsible Party):

Brief Summary:
It is anticipated that PENNSAID Gel will minimize systemic exposure versus oral diclofenac administered twice a day (BID). In addition, PENNSAID Gel should result in greater subject convenience and compliance with a comparable bioavailability, safety and tolerability profile to that of the approved PENNSAID solution administered four times a day (QID).

Condition or disease Intervention/treatment Phase
Pain Drug: 2% w/w diclofenac sodium topical gel Drug: 1.5% w/w diclofenac sodium topical solution Drug: 75 mg diclofenac sodium delayed release tablet Phase 1

Detailed Description:

PENNSAID Gel is a new topical gel formulation of diclofenac sodium that is similar in composition to PENNSAID solution.

No clinical studies have been conducted using PENNSAID Gel. The current study will compare the pharmacokinetics, bioavailability, safety and tolerability of diclofenac after the topical application of PENNSAID Gel with the approved formulations of topical PENNSAID Solution and oral Sandoz 75 mg diclofenac sodium delayed release tablets in healthy subjects.

The efficacy profile of PENNSAID Gel is based on the known efficacy profile of PENNSAID solution. Support for the BID dosing regimen includes the higher concentration of diclofenac sodium in PENNSAID Gel (2.0%) compared to PENNSAID solution (1.5%). In addition, compared to PENNSAID solution, PENNSAID Gel is designed to have better penetration of diclofenac to allow for a reduction in the number of applications per day from four to two while maintaining effectiveness.

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Study Type : Interventional  (Clinical Trial)
Actual Enrollment : 30 participants
Allocation: Randomized
Intervention Model: Crossover Assignment
Masking: None (Open Label)
Primary Purpose: Basic Science
Official Title: A Phase 1, Randomized, Single Center, Open-Label, Multiple-Dose, Three-Way Crossover Study to Evaluate the Pharmacokinetics, Bioavailability and Safety of PENNSAID Gel in Comparison With Sandoz 75 mg Diclofenac Sodium Delayed Release Tablet and PENNSAID (Diclofenac Sodium Topical Solution) in Healthy Volunteers
Study Start Date : September 2010
Actual Primary Completion Date : November 2010
Actual Study Completion Date : November 2010

Resource links provided by the National Library of Medicine

Arm Intervention/treatment
Experimental: Treatment A
2% w/w diclofenac sodium topical gel
Drug: 2% w/w diclofenac sodium topical gel
2% w/w diclofenac sodium topical gel

Active Comparator: Treatment B Drug: 1.5% w/w diclofenac sodium topical solution
1.5% w/w diclofenac sodium topical solution

Active Comparator: Treatment C Drug: 75 mg diclofenac sodium delayed release tablet
75 mg diclofenac sodium delayed release tablet

Primary Outcome Measures :
  1. The rate and extent of exposure of diclofenac will be assessed. [ Time Frame: During each of the 3 periods, blood samples will be obtained on Day 1 and Day 8 at pre-dose and 1, 2, 3, 4, 6, 8 and 12 hours post-dose; on Days 2-7 at pre-dose; and on Days 9, 13 and 15 at approximately 8 AM. ]
    Summary statistics including the mean, standard deviation, coefficient of variation, geometric mean and geometric %CV will be calculated for all PK parameters by treatment.

Information from the National Library of Medicine

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Ages Eligible for Study:   18 Years to 55 Years   (Adult)
Sexes Eligible for Study:   All
Accepts Healthy Volunteers:   Yes

Inclusion Criteria:

  • The eligibility of subjects to enter the study is based on meeting the inclusion criteria listed below:

    1. Signed and dated IRB approved consent before any protocol procedures are performed.
    2. Males or non-pregnant, non-lactating females, minimum 18 years of age and maximum of 55 years of age.
    3. Female subjects must be negative on a serum pregnancy test, be postmenopausal for at least 1 year, surgically sterile, or using an acceptable form of contraception for 30 days prior to dosing and for the duration of study participation.
    4. Subjects with a body mass index (BMI) ≥19 and ≤29 kg/m².
    5. The findings from the ECG interpretation must be within the normal range.
    6. Subjects whose health status is assessed by the investigator as "normal healthy" by required screening and check-in assessments.
    7. Subjects must be able to provide written consent and agree to comply with study requirements.

Exclusion Criteria:

  • Subjects will be ineligible for the study if they meet any of the following criteria:

    1. Known hypersensitivity to diclofenac, aspirin [acetylsalicylic acid (ASA)] or any other NSAID, dimethyl sulfoxide (DMSO) or ethanol. This includes subjects exhibiting aspirin or other NSAID-induced symptoms, including bronchospasm, rhinitis, and urticaria or other NSAID-induced allergic symptoms.
    2. Pregnant or lactating women. Women of reproductive potential (and women <12 months after menopause) may not participate unless they have agreed to use an effective contraceptive method while on study.
    3. Evidence of any serious active infections, severe uncontrolled cardiac, renal, hepatic, pulmonary or other systemic disease, significant medical or psychiatric illness, known seropositivity to HIV, known unexplained vision changes, history of unexplained syncope, lightheadedness, high blood pressure, chronic hepatic conditions like hepatic porphyria or clinically significant laboratory findings that would, in the investigators judgment, make the subject inappropriate for the study.
    4. Documented (upper GI series or endoscopy) gastroduodenal ulcer or any GI bleeding (except hemorrhoidal) within the last 6 months prior to screening.
    5. Abnormal hepatic and renal functions; hematologic changes:

      • Aspartate aminotransferase (AST) or alanine aminotransferase (ALT)≥2.5 X ULN
      • Gamma-glutamyl transpeptidase (GGT) ≥3X ULN
      • Total bilirubin ≥1.5X ULN
      • Serum creatinine ≥1.5X ULN
      • Hemoglobin ≤LLN.
    6. Major surgery or previous damage to the study knee(s) at any time (eg. total knee replacement, damage/reconstruction of the anterior or posterior cruciate ligaments), or minor knee surgery (eg, cartilage repair, collateral ligament repair, arthroscopic debridement) to the study knee(s) within 1 year prior to screening.
    7. Administration of a sedative hypnotic medication for insomnia within 14 days prior to screening.
    8. Administration of anti-depressants, within 60 days prior to screening.
    9. Administration of another investigational drug within the previous 30 days prior to screening.
    10. Skin disorder that affects palms of the hands or the application site of the knee(s).
    11. History of chronic headaches.
    12. Documented history of alcohol or drug abuse within 1 year prior to the screening visit
    13. Subjects who have smoked or used nicotine-containing products within 6 months prior to Period 1 dosing.
    14. Subjects treated with systemic or local diclofenac within one month of study Day 1.
    15. Using artificial exposure, tanning beds, or self-tanning cream on knee area within 90 days of study start.
    16. Donation or significant loss of blood (480 mL or more) within 30 days of dosing.
    17. Previous participation in this study or participation in another clinical trial within 30 days prior screening.
    18. Noncompliance with the study protocol.

Information from the National Library of Medicine

To learn more about this study, you or your doctor may contact the study research staff using the contact information provided by the sponsor.

Please refer to this study by its identifier (NCT number): NCT01202799

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United States, Florida
Comprehensive Phase One
Miramar, Florida, United States, 33025
Sponsors and Collaborators
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Principal Investigator: Maria J Gutierrez, MD Comprehensive Phase One ®
Publications automatically indexed to this study by Identifier (NCT Number):
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Responsible Party: Mallinckrodt Identifier: NCT01202799    
Other Study ID Numbers: COV05100070
First Posted: September 16, 2010    Key Record Dates
Last Update Posted: September 23, 2014
Last Verified: September 2014
Keywords provided by Mallinckrodt:
Healthy volunteers
Topical NSAID
Additional relevant MeSH terms:
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Anti-Inflammatory Agents, Non-Steroidal
Analgesics, Non-Narcotic
Sensory System Agents
Peripheral Nervous System Agents
Physiological Effects of Drugs
Anti-Inflammatory Agents
Antirheumatic Agents
Cyclooxygenase Inhibitors
Enzyme Inhibitors
Molecular Mechanisms of Pharmacological Action