Pharmacokinetics of Injectable Estradiol and Progesterone Microspheres Suspension

Multiple-dose Pharmacokinetic Study of Two Aqueous Suspensions of Estradiol and Progesterone Microspheres (1 mg/20 mg & 0.5 mg/15 mg) for Intramuscular Administration, in Postmenopausal Volunteers.

Phase I pharmacokinetic study

Main objective:

To determine plasmatic profiles and pharmacokinetic parameters of estradiol and progesterone on each of the formulations studied, after multiple-dose administration

Study design:

Randomized, controlled, open-label, parallel, pharmacokinetic study

Sites: 1

Subjects: 30 postmenopausal women

Sites: 1

Phase: 1

Main objective:

To determine plasmatic profiles and pharmacokinetic parameters of estradiol and progesterone on each of the formulations studied, after multiple-dose administration.

Secondary objectives:

To determine bioavailability of each of the formulations studied, after multiple-dose-administration. Describe tolerability of each of the formulations studied, after multiple-dose administration.

Study design: Randomized, controlled, open-label, parallel, pharmacokinetic study

Investigational Products:

• Estradiol and progesterone microspheres aqueous suspension (1 mg/20 mg)
• Estradiol and progesterone microspheres aqueous suspension (0.5 mg/15 mg)

Study subjects: 30 postmenopausal women 45 - 65 years old

Brief description: After written informed consent, 30 eligible women will be randomized to study treatments (one IM injection each 28 days, for a total of 4 doses). Blood samples will be obtained for pharmacokinetic study.

Inclusion Criteria:

• Female
• 45 to 65 years old
• Able to read and write
• Postmenopausal
• Body Mass Index equal or below 34.99 kg/m2
• Healthy
• Normal uterus
• Time availability

Exclusion Criteria:

• Hypersensitivity to progesterone or related compounds
• Hypersensitivity to estrogens
• Hysterectomy
• History or present hormone-dependent tumor
• History or present uterine cervix dysplasia
• Abnormal and clinically-significant laboratory test results
• Family history of breast cancer
• History of thromboembolic disease
• Non-controlled hypertension
• History of stroke
• History of cardiac valve surgery
• Renal failure
• Hepatic failure
• Non-controlled diabetes
• History of serious neurologic disease
• Reduced mobility
• Anemia
• Previous or concomitant hormone therapy
• Previous or concomitant therapy with inhibitors or inductors of cytochrome