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Pharmacokinetics of a Novel Vaginal Delivery System for Testosterone and Dehydroepiandrosterone (DHEA)

Registration Number
NCT03967964
Lead Sponsor
Laboratorios Andromaco S.A.
Brief Summary

This study was performed to determine the pharmacokinetic parameters of vaginal rings that contain DHEA, testosterone, or combinations of both androgens, in comparison to the oral administration of DHEA and the transdermal administration of testosterone.

Detailed Description

Not available

Recruitment & Eligibility

Status
COMPLETED
Sex
Female
Target Recruitment
46
Inclusion Criteria
  • Women between 40 to 60 years old.
  • Postmenopausal with spontaneous amenorrhea of 1 year or more, regardless of follicle stimulating hormone (FSH) levels; or amenorrhea of 6 to 12 months, in which the postmenopausal state will be confirmed with a FSH level of 0.040 international units per milliliter or higher.
  • Body Mass Index between 19 and 30.
  • Intact uterus.
  • Not having received hormone therapy in the month prior to selection.
  • Adequate veins to conduct serial blood samplings.
  • Recent Pap smear (not more than 12 months), with a result negative for malignant neoplastic cells, and that contains sufficient endocervical cells for analysis. If the Pap smear was performed more than 12 months ago or cannot be verified through clinical documentation, it must be repeated during the selection process.
  • Normal mammogram, BI.RADS I or II (American College of Radiology), within the last year. If the mammogram was performed more than 12 months ago or cannot be verified through clinical documentation, it must be repeated during the selection process.
  • That provide written informed consent.
Exclusion Criteria
  • Use at randomization of phenytoin, barbiturates, primidone, carbamazepine, rifampin, griseofulvin, ketoconazole, lipid-lowering agents.
  • History of diseases such as coronary heart disease, breast cancer, uterine cancer, and/or chronic hepatic disease.
  • Unconscious volunteers, severely ill, or with mental disability.
  • Allergy and hypersensitivity to DHEA and/or testosterone.
  • Untreated or uncontrolled hypertension, with systolic pressure above 140 mm Hg or diastolic pressure above 90 mm Hg.
  • Current participation in other research at the moment of the screening visit, or having concluded their participation in a previous research in less than 30 days since their last visit.
  • Pregnant or lactating women; pregnancy must be confirmed with a urine positive human chorionic gonadotropin (HCG) test during screening.
  • History of vein thrombosis (deep vein thrombosis, pulmonary embolism).
  • History of arterial thrombosis (myocardial infarction) or prodromic conditions (e.g. transient ischemic attack, angina pectoris).
  • History of stroke.
  • History of migraine with focal neurological manifestations.
  • History of hepatic tumor (benign or malignant).
  • History of clinical atherosclerosis in first grade relatives (parents, siblings, sons [men less than 55 years old and women less than 65 years old]).
  • Smoking (5 or more cigarettes a day).
  • Diabetes mellitus that will be ruled out at screening if fasting glucose is less than 100 mg/dL or between 100 and 125 mg/dL, with Oral Glucose Tolerance Test that rules out diabetes. Diabetes will be confirmed with blood glucose equal to or above 200 mg/dL or 2 fasting glucose tests equal to or above 126 mg/dL.
  • High density lipopolysaccharide (HDL)-cholesterol below 35 mg/dL.

Study & Design

Study Type
INTERVENTIONAL
Study Design
PARALLEL
Arm && Interventions
GroupInterventionDescription
Group 2: AVTTestosteroneVaginal ring with 35 mg testosterone, wearing time 72 hours.
Group 3: AVD+TDehydroepiandrosterone 1.5 g/Testosterone 25 mgVaginal ring with 1.5 grams DHEA and 25 mg testosterone, wearing time 72 hours.
Group 5: Testosterone transdermal gelTestosterone Topical GelTestosterone transdermal gel with dosing valve (pump): administration of 3 pump actuations (equivalent to 5 mg of testosterone each) per day (total daily dose 15 mg), on 3 consecutive days (72 hours).
Group 1: AVDDehydroepiandrosterone 2.2 gVaginal ring with 2.2 grams dehydroepiandrosterone (DHEA), wearing time 72 hours
Group 4: DHEA capsuleDehydroepiandrosterone Oral CapsuleCapsules with 25 mg DHEA, oral administration every 8 hours for a 72-hour period.
Primary Outcome Measures
NameTimeMethod
Testosterone: Area under the serum concentration time curve (AUC0-72)Pre-dose and from 30 minutes after administration of the assigned treatment to 72 hours

Serum testosterone was measured pre-dose and at 30 minutes, at 1 hour, 2, 4, 6, 8, 24, 48, and 72 hours after vaginal ring insertion, the transdermal application of the testosterone gel, or after taking DHEA capsules. The AUC0-72 was calculated.

DHEA: Maximum serum concentration (Cmax)Pre-dose and from 30 minutes after administration of the assigned treatment to 72 hours

Serum DHEA was measured pre-dose and at 30 minutes, at 1 hour, 2, 4, 6, 8, 24, 48, and 72 hours after vaginal ring insertion, the transdermal application of the testosterone gel, or after taking DHEA capsules. Cmax was calculated.

DHEA: Area under the serum concentration time curve (AUC0-72)Pre-dose and from 30 minutes after administration of the assigned treatment to 72 hours

Serum DHEA were measured pre-dose and at 30 minutes, at 1 hour, 2, 4, 6, 8, 24, 48, and 72 hours after vaginal ring insertion, the transdermal application of the testosterone gel, or after taking DHEA capsules. The AUC0-72 was calculated.

DHEA: Time to achieve maximum serum concentration (tmax)pre-dose and from 30 minutes after administration of the assigned treatment to 72 hours

Serum DHEA was measured pre-dose and at 30 minutes, at 1 hour, 2, 4, 6, 8, 24, 48, and 72 hours after vaginal ring insertion, the transdermal application of the testosterone gel, or after taking DHEA capsules. Tmax was calculated.

Testosterone: Average serum concentration 0-24 hoursPre-dose and from 30 minutes after administration of the assigned treatment to 24 hours

Serum testosterone was measured pre-dose and at 30 minutes, at 1 hour, 2, 4, 6, 8, 24, 48, and 72 hours after vaginal ring insertion, the transdermal application of the testosterone gel, or after taking DHEA capsules. The average serum concentration achieved in the first 24 hours after administration of the assigned treatment was calculated.

Testosterone: Maximum serum concentration (Cmax)Pre-dose and from 30 minutes after administration of the assigned treatment to 72 hours

Serum testosterone was measured pre-dose and at 30 minutes, at 1 hour, 2, 4, 6, 8, 24, 48, and 72 hours after vaginal ring insertion, the transdermal application of the testosterone gel, or after taking DHEA capsules. Cmax was calculated.

Testosterone: Time to achieve maximum serum concentration (tmax)pre-dose and from 30 minutes after administration of the assigned treatment to 72 hours

Serum testosterone was measured pre-dose and at 30 minutes, at 1 hour, 2, 4, 6, 8, 24, 48, and 72 hours after vaginal ring insertion, the transdermal application of the testosterone gel, or after taking DHEA capsules. Tmax was calculated.

DHEA: Average serum concentration 0-24 hoursPre-dose and from 30 minutes after administration of the assigned treatment to 24 hours

Serum DHEA was measured pre-dose and at 30 minutes, at 1 hour, 2, 4, 6, 8, 24, 48, and 72 hours after vaginal ring insertion, the transdermal application of the testosterone gel, or after taking DHEA capsules. The average serum concentration achieved in the first 24 hours after administration of the assigned treatment was calculated.

Secondary Outcome Measures
NameTimeMethod

Trial Locations

Locations (1)

Instituto de Investigación Materno Infantil (IDIMI) - Maternidad Hospital San Borja (HCSBA)

🇨🇱

Santiago, Chile

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