Single Dose Bioequivalence Study of Darifenacin Tablets 7.5 mg in Fed Healthy Volunteers.

NCT01229280 | Unknown Phase 1

• 1 other identifier: BDBEQ_DFNLP/ELEA_010
• Study Type: interventional
• Target: 24
• Locations: 1 country
• Sites: 1

Brief Summary

The proposed study was designed as a randomized two-sequence, two period crossover trial to assess the bioequivalence, pharmacokinetic profiling and safety of a brand generic formulation of darifenacin \[Darisec(R) 7.5 mg\] vs. the innovator \[Enablex(R)7.5 mg\]in healthy volunteers in postprandial state.

Conditions

Bioequivalency

Keywords

Bioequivalence; Darifenacin; Healthy volunteers; Postprandial

Outcome Measures

Primary Outcomes (2)

• Extent of absorption

  Extent of absorption will be measured using the area under the plasma concentration of darifenacin vs time from time 0 to the last sample point (AUC0-t) and from time 0 to infinity (AUC0-inf.

  72 hours

• Rate of absorption

  Rate of abosorption will be measured using peak concentration of darifenacin (Cmax)taken from the concentration vs. time curve.

  72

Secondary Outcomes (4)

• Time to peak concentration (tmax)

  72

• Elimination rate constant (Ke)

  72 hours

• Elimination Half-life (t1/2e)

  72 hours

• Systemic clearance (Cls)

  72 hours

Study Arms (2)

Darisec(R) 7.5 mg

EXPERIMENTAL

Drug: Darifenacin

Enablex(R) 7.5 mg

ACTIVE COMPARATOR

Drug: Darifenacin

Interventions

Darifenacin DRUG

Single dose 7.5 mg tablets of darifenacin

Also known as: Muscarinic antagonist, Cholinergic antagonist, Cholinergic agent, Darisec

Darisec(R) 7.5 mg

Eligibility Criteria

• Age: 18 Years - 50 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• Healthy male or female subjects 18 to 50 years of age (inclusive).
• In good health, as determined by lack of clinically significant abnormalities at screening as judged by the physician.
• Female subjects are required to use a medically accepted method of hormonal contraception or abstinence throughout the entire study period and for one week after the study is completed.
• Body mass index within the range of 18.5 and 29.9 kg/m2 and weight at least 45 kg.

You may not qualify if:

• Known hypersensitivity or severe adverse event to darifenacin or similar drugs.
• Urinary, retention, narrow-angle glaucoma, myasthenia gravis, severe hepatic impairment, severe ulcerative colitis, toxic megacolon.
• Symptomatic hiatus hernia, erosive or symptomatic gastroesophageal reflux disease/heartburn (\>2 days in a week), severe constipation, gastrointestinal obstructive disorder, and gastric retention.
• Clinically significant cardiac abnormalities, fainting, low blood pressure upon standing, irregular heartbeats.
• Acute or chronic bronchospastic disease(including asthma and Chronic Obstructive Pulmonary Disease).
• Clinically significant drug allergy or history of atopic allergy (asthma, urticaria, eczematous dermatitis).
• Smokers of more than 5 cigarettes a week.
• Regular use of any drug known to induce or inhibit hepatic drug metabolism (particularly those that affect CYP2D6) within 30 days prior to each study drug administration.
• Any surgical or medical condition which might significantly alter the absorption, distribution, metabolism, or excretion of drugs which may jeopardize participation in the study.
• Immunodeficiency diseases, including a positive HIV (Elisa or Western blot) test result.
• Positive Hepatitis B Surface antigen (HBsAg) or Hepatitis C results.
• Drug or alcohol abuse within the 6 months prior to dosing.
• Use of prescription drugs within 1 month prior to dosing, or over-the-counter medication (vitamins, herbal supplements, dietary supplements)within 2 weeks prior to dosing. Paracetamol and ibuprofen are acceptable.
• Participation in any clinical investigation within 12 weeks prior to dosing.
• Donation or loss of 400 ml or more of blood within 8 weeks prior to dosing.

Sponsors & Collaborators

• Center for Clinical Pharmacology Research Bdbeq S.A.: lead
• Laboratorio Elea Phoenix S.A.: collaborator

Study Sites (1)

Center for Clinical Pharmacology Research (CCPR) Bdbeq S.A. Hospital Italiano.

Montevideo, Montevideo Department, 11600, Uruguay

Location

Related Publications (5)

• Skerjanec A. The clinical pharmacokinetics of darifenacin. Clin Pharmacokinet. 2006;45(4):325-50. doi: 10.2165/00003088-200645040-00001.

  PMID: 16584282 BACKGROUND

• Croom KF, Keating GM. Darifenacin: in the treatment of overactive bladder. Drugs Aging. 2004;21(13):885-92; discussion 893-4. doi: 10.2165/00002512-200421130-00005.

  PMID: 15493952 BACKGROUND

• Staskin DR. Overactive bladder in the elderly: a guide to pharmacological management. Drugs Aging. 2005;22(12):1013-28. doi: 10.2165/00002512-200522120-00003.

  PMID: 16363885 BACKGROUND

• Kerbusch T, Wahlby U, Milligan PA, Karlsson MO. Population pharmacokinetic modelling of darifenacin and its hydroxylated metabolite using pooled data, incorporating saturable first-pass metabolism, CYP2D6 genotype and formulation-dependent bioavailability. Br J Clin Pharmacol. 2003 Dec;56(6):639-52. doi: 10.1046/j.1365-2125.2003.01967.x.

  PMID: 14616424 BACKGROUND

• Dmochowski RR, Appell RA. Advancements in pharmacologic management of the overactive bladder. Urology. 2000 Dec 4;56(6 Suppl 1):41-9. doi: 10.1016/s0090-4295(00)01020-7.

  PMID: 11114562 BACKGROUND

MeSH Terms

Interventions

darifenacin; Muscarinic Antagonists; Cholinergic Antagonists; Cholinergic Agents

Intervention Hierarchy (Ancestors)

Neurotransmitter Agents; Molecular Mechanisms of Pharmacological Action; Pharmacologic Actions; Chemical Actions and Uses; Physiological Effects of Drugs

Study Officials

• Francisco E. Estevez-Carrizo, MD

  Univerisity of Montevideo. Biomedical Science Center.Prudencio de Pena 2440, 11600 Montevideo. Uruguay

  STUDY DIRECTOR

• Susana Parrillo, M.D.

  Center for Clinical Pharmacology Research Bdbeq S.A., Br. Artigas 1632. c.p. 11600 Montevideo. Uruguay.

  PRINCIPAL INVESTIGATOR

Central Study Contacts

Federico Santoro, MD

CONTACT

+541143794300; santorof@elea.com

Joanna Steimberg, MBA

CONTACT

+541143794330; steimbej@elea.com

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: NONE
• Intervention Model: CROSSOVER
• Sponsor Type: OTHER

Study Record Dates

• First Submitted: October 26, 2010
• First Posted: October 27, 2010
• Study Start: December 1, 2010
• Primary Completion: January 1, 2011
• Study Completion: February 1, 2011
• Last Updated: October 27, 2010

Record last verified: 2010-10

Locations

UR (1)