| Sustained pharmacological activities in rats following single and repeated administration of once-a-month injectable microspheres of leuprolide acetate. | |
| | |
MedLine Citation:
|
PMID: 1907735 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
|
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. |
| | |
Authors:
|
H Okada; T Heya; Y Ogawa; H Toguchi; T Shimamoto |
Related Documents
:
|
7035255 - Biosynthesis, in vivo, of gonadotropin-releasing hormone in the hypothalamus of normal ... 8423035 - Vasopressin gene expression in rats with experimental cirrhosis. 6410305 - Corticoliberin-immunoreactive cell bodies localised in two distinct areas of the sheep ... 12169775 - Pituitary luteinizing hormone microheterogeneity in the afternoon of proestrus in rats:... 10498825 - Remyelination occurs as extensively but more slowly in old rats compared to young rats ... 3884075 - Carbon disulphide exposure affects the response of rat adrenal medulla to hypothermia a... |
Publication Detail:
|
Type: Journal Article |
Journal Detail:
|
Title: Pharmaceutical research Volume: 8 ISSN: 0724-8741 ISO Abbreviation: Pharm. Res. Publication Date: 1991 May |
Date Detail:
|
Created Date: 1991-09-09 Completed Date: 1991-09-09 Revised Date: 2006-11-15 |
Medline Journal Info:
|
Nlm Unique ID: 8406521 Medline TA: Pharm Res Country: UNITED STATES |
Other Details:
|
Languages: eng Pagination: 584-7 Citation Subset: IM |
Affiliation:
|
Pharmaceutics Research Laboratories, Takeda Chemical Industries, Ltd., Osaka, Japan. |
Export Citation:
|
APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
|
Animals Delayed-Action Preparations Follicle Stimulating Hormone / blood Gonadotropin-Releasing Hormone / administration & dosage, analogs & derivatives*, pharmacokinetics, pharmacology Hormones / administration & dosage, pharmacokinetics, pharmacology Injections, Subcutaneous Leuprolide Luteinizing Hormone / blood Male Microspheres Rats Rats, Inbred Strains Testosterone / blood Time Factors |
| Chemical | |
Reg. No./Substance:
|
0/Delayed-Action Preparations; 0/Hormones; 33515-09-2/Gonadotropin-Releasing Hormone; 53714-56-0/Leuprolide; 58-22-0/Testosterone; 9002-67-9/Luteinizing Hormone; 9002-68-0/Follicle Stimulating Hormone |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
Previous Document: Effect of dietary kelp on lipid peroxidation and glutathione peroxidase activity in livers of rats g...
Next Document: Different effects of paraquat on microsomal lipid peroxidation in mouse brain, lung and liver.