Sustained pharmacological activities in rats following single and repeated administration of once-a-month injectable microspheres of leuprolide acetate

Once-a-month injectable microspheres of leuprolide acetate prepared with copoly(DL-lactic/glycolic acid) using an in-water drying method were assessed for duration of the analogue release and pharmacological effects in rats after a single or repeated injection. The periodic challenge test revealed t...

Full description

Saved in:
Bibliographic Details
Published in:Pharmaceutical research 1991-05, Vol.8 (5), p.584-587
Main Authors: OKADA, H, HEYA, T, OGAWA, Y, TOGUCHI, H, SHIMAMOTO, T
Format: Article
Language:English
Subjects:
Animals
Biological and medical sciences
Delayed-Action Preparations
Follicle Stimulating Hormone - blood
General pharmacology
Gonadotropin-Releasing Hormone - administration & dosage
Gonadotropin-Releasing Hormone - analogs & derivatives
Gonadotropin-Releasing Hormone - pharmacokinetics
Gonadotropin-Releasing Hormone - pharmacology
Hormones - administration & dosage
Hormones - pharmacokinetics
Hormones - pharmacology
Injections, Subcutaneous
Leuprolide
Luteinizing Hormone - blood
Male
Medical sciences
Microspheres
Pharmaceutical technology. Pharmaceutical industry
Pharmacology. Drug treatments
Rats
Rats, Inbred Strains
Testosterone - blood
Time Factors
Citations: Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:Once-a-month injectable microspheres of leuprolide acetate prepared with copoly(DL-lactic/glycolic acid) using an in-water drying method were assessed for duration of the analogue release and pharmacological effects in rats after a single or repeated injection. The periodic challenge test revealed that a single injection of the microspheres caused a dramatic and persistent suppression of the ability of the pituitary-gonadal system to secrete gonadotropin and testosterone for over 5 weeks. The complete recovery of these functions was observed 10 weeks after the injection. The repeated injection of the microspheres at intervals of 2 or 4 weeks achieved persistent suppression of steroidogenesis after an initial transient flare-up and beneficially avoided the "acute-on-chronic response." This depot formulation is expected to assure patient compliance and produce stronger therapeutic effects than the daily solution.
ISSN:0724-8741
1573-904X
DOI:10.1023/a:1015844421319