Pharmacokinetics of once-a-month injectable microspheres of leuprolide acetate.

Okada H, Inoue Y, Heya T, Ueno H, Ogawa Y, Toguchi H

Pharmaceutical research1 Jun 1991Cited by 73 (Europe PMC)

PMID1905810DOI10.1023/a:1015818504906PepBankPUB-01905810

Publisher page PubMedAsk about this study

Summary

The text of this summary is not shown here, because the article license does not allow reuse. Read it at the source (opens in a new tab)

Text rights: Publisher copyright. Results still quote short attributed sentences.

Results from this study7

7 results from studies that gave the peptide. No result from this study comes from people.

01AnimalAnimal study (in vivo)Pharmacokinetics
In rats, injected leuprolide microspheres sustained serum leuprolide concentrations for over 4 weeks at three doses.
In plain wordsIn rats, injected leuprolide microspheres sustained serum leuprolide concentrations for over 4 weeks at three doses.
Peptide
Leuprolide
Outcome
Not applicableSustained serum leuprolide
Study
ratn: not reported in source
rats
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
Dose not stated
Source sentences
Summary
After microsphere injection at three different doses in rat serum leuprolide concentrations were sustained for over 4 weeks, and the AUCs and mean serum levels were linearly correlated with the dose.
1 context sentence(design, population, supporting numbers)
Summary · context
The pharmacokinetic parameters of leuprolide acetate, a potent analogue of LH-RH, were determined in rats and dogs after i.v. and s.c. dosing with leuprolide solution.
Report a problemFND-0190581001
02AnimalAnimal study (in vivo)Pharmacokinetics
In rats, leuprolide AUC correlated linearly with the microsphere dose.
In plain wordsIn rats, leuprolide exposure increased linearly with the microsphere dose.
Peptide
Leuprolide
Outcome
IncreaseDose-AUC correlation
Study
ratn: not reported in source
rats
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
Dose not stated
Source sentences
Summary
After microsphere injection at three different doses in rat serum leuprolide concentrations were sustained for over 4 weeks, and the AUCs and mean serum levels were linearly correlated with the dose.
1 context sentence(design, population, supporting numbers)
Summary · context
The pharmacokinetic parameters of leuprolide acetate, a potent analogue of LH-RH, were determined in rats and dogs after i.v. and s.c. dosing with leuprolide solution.
Report a problemFND-0190581002
03AnimalAnimal study (in vivo)Pharmacokinetics
In rats, mean serum leuprolide levels correlated linearly with the microsphere dose.
In plain wordsIn rats, average blood leuprolide levels increased linearly with the microsphere dose.
Peptide
Leuprolide
Outcome
IncreaseDose-mean serum level correlation
Study
ratn: not reported in source
rats
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
Dose not stated
Source sentences
Summary
After microsphere injection at three different doses in rat serum leuprolide concentrations were sustained for over 4 weeks, and the AUCs and mean serum levels were linearly correlated with the dose.
1 context sentence(design, population, supporting numbers)
Summary · context
The pharmacokinetic parameters of leuprolide acetate, a potent analogue of LH-RH, were determined in rats and dogs after i.v. and s.c. dosing with leuprolide solution.
Report a problemFND-0190581003
04AnimalAnimal study (in vivo)Pharmacokinetics
In rats, repeated leuprolide microsphere injections every 4 weeks produced similar serum profiles after each injection.
In plain wordsIn rats, blood leuprolide patterns were similar after repeated microsphere injections.
Peptide
Leuprolide
Outcome
Direction not reportedRepeated-dose serum profiles
Study
ratn: not reported in source
rats
Comparator
Earlier injections
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
Dose not stated · subcutaneousAs given in this study (rat).
Source sentences
Summary
The serum levels and urinary excretion of the analogue in rats after repeated s.c. injection of the microspheres every 4 weeks exhibited similar profiles after each injection; no changes of the absorption and excretion of the analogue after the repeated injection could be demonstrated.
1 context sentence(design, population, supporting numbers)
Summary · context
The pharmacokinetic parameters of leuprolide acetate, a potent analogue of LH-RH, were determined in rats and dogs after i.v. and s.c. dosing with leuprolide solution.
Report a problemFND-0190581004
05AnimalAnimal study (in vivo)Pharmacokinetics
In rats, urinary leuprolide excretion profiles were similar after repeated microsphere injections every 4 weeks.
In plain wordsIn rats, urine leuprolide excretion patterns were similar after repeated microsphere injections.
Peptide
Leuprolide
Outcome
Direction not reportedRepeated-dose urinary excretion
Study
ratn: not reported in source
rats
Comparator
Earlier injections
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
Dose not stated · subcutaneousAs given in this study (rat).
Source sentences
Summary
The serum levels and urinary excretion of the analogue in rats after repeated s.c. injection of the microspheres every 4 weeks exhibited similar profiles after each injection; no changes of the absorption and excretion of the analogue after the repeated injection could be demonstrated.
1 context sentence(design, population, supporting numbers)
Summary · context
The pharmacokinetic parameters of leuprolide acetate, a potent analogue of LH-RH, were determined in rats and dogs after i.v. and s.c. dosing with leuprolide solution.
Report a problemFND-0190581005
06AnimalAnimal study (in vivo)Pharmacokinetics
In rats, repeated leuprolide microsphere injections produced no demonstrable absorption changes.
In plain wordsIn rats, leuprolide absorption did not change detectably after repeated microsphere injections.
Peptide
Leuprolide
Outcome
No significant changeRepeated-dose absorption
Study
ratn: not reported in source
rats
Comparator
Earlier injections
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
Dose not stated · subcutaneousAs given in this study (rat).
Source sentences
Summary
The serum levels and urinary excretion of the analogue in rats after repeated s.c. injection of the microspheres every 4 weeks exhibited similar profiles after each injection; no changes of the absorption and excretion of the analogue after the repeated injection could be demonstrated.
1 context sentence(design, population, supporting numbers)
Summary · context
The pharmacokinetic parameters of leuprolide acetate, a potent analogue of LH-RH, were determined in rats and dogs after i.v. and s.c. dosing with leuprolide solution.
Report a problemFND-0190581006
07AnimalAnimal study (in vivo)Pharmacokinetics
In rats, serum M-I levels were 21% of intact leuprolide at 3 hr and very low at steady state after 1 to 4 weeks.
In plain wordsIn rats, the leuprolide metabolite M-I was low at steady state after microsphere injection.
Peptide
Leuprolide
Outcome
Not applicableMetabolite M-I levels
Study
ratn: not reported in source
rats
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
Dose not stated
Measurements
M-I relative level
21%
intact form at 3 hr
Source sentences
Summary
The serum levels of the analogue metabolite (M-I) were 21% of the intact form 3 hr after injection of the microspheres but very low at the steady state after 1 to 4 weeks.
1 context sentence(design, population, supporting numbers)
Summary · context
The pharmacokinetic parameters of leuprolide acetate, a potent analogue of LH-RH, were determined in rats and dogs after i.v. and s.c. dosing with leuprolide solution.
Report a problemFND-0190581007

AI wrote and checked these results. AI can make mistakes, so check important results against the source.

Version history

PepBank keeps every version of the data on this study. Status changes from Retraction Watch, Europe PMC and Crossref are listed with their source.

Version 2Current
28 Oct 2026, 02:03 UTC
Study results updated
Version 1
27 Oct 2026, 16:37 UTC
First added · source update from Europe PMC

Subjects

Terms as the source lists them.

Publication types

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MeSH terms

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