Controlled release of LHRH agonist, leuprolide acetate, from microcapsules: serum drug level profiles and pharmacological effects in animals.

Ogawa Y, Okada H, Heya T, Shimamoto T

The Journal of pharmacy and pharmacology1 Jul 1989Cited by 78 (Europe PMC)

PMID2570847DOI10.1111/j.2042-7158.1989.tb06497.xPepBankPUB-02570847

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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 study11

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

01AnimalAnimal study (in vivo)Pharmacokinetics
In rats, subcutaneous leuprolide microcapsules showed pseudo-zero-order release for one month across 0.0135 to 1.35 mg/rat.
In plain wordsIn rats, leuprolide microcapsules released drug at a near-constant rate for one month after subcutaneous injection.
Peptide
Leuprolide
Outcome
Not applicableSubcutaneous release kinetics
Study
ratn: not reported in source
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
0.0135 to 1.35 mg/rat · subcutaneous · one monthAs given in this study (rat).
Source sentences
Summary
The release of the drug in rats after a single subcutaneous injection exhibited pseudo-zero-order kinetics for one month in doses ranging from 0.0135 to 1.35 mg/rat;
1 context sentence(design, population, supporting numbers)
Summary · context
The pharmacokinetic behaviour of leuprolide acetate from a controlled release parenteral dosage form has been studied in rats and dogs.
Report a problemFND-0257084701
02AnimalAnimal study (in vivo)Pharmacokinetics
In rats, leuprolide microcapsules released 2.8% of the dose per day at 1.35 mg/rat.
In plain wordsIn rats, leuprolide microcapsules released 2.8% of the dose per day at 1.35 mg/rat.
Peptide
Leuprolide
Outcome
Not applicableRelease rate
Study
ratn: not reported in source
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
1.35 mg/rat · subcutaneousAs given in this study (rat).
Measurements
Release rate
2.8 % of dose/day
1.35 mg/rat
Source sentences
Summary
the release rate at a dose of 1.35 mg/rat was 2.8% of dose/day;
1 context sentence(design, population, supporting numbers)
Summary · context
The pharmacokinetic behaviour of leuprolide acetate from a controlled release parenteral dosage form has been studied in rats and dogs.
Report a problemFND-0257084702
03AnimalAnimal study (in vivo)Pharmacokinetics
In rats, intramuscular leuprolide microcapsules produced a release response similar to subcutaneous injection.
In plain wordsIn rats, leuprolide release was similar after muscle and subcutaneous injections.
Peptide
Leuprolide
Outcome
No significant changeIntramuscular release kinetics
Study
ratn: not reported in source
Comparator
Subcutaneous injection
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
Dose not stated · intramuscularAs given in this study (rat).
Source sentences
Summary
The release of the drug in rats after a single subcutaneous injection exhibited pseudo-zero-order kinetics for one month in doses ranging from 0.0135 to 1.35 mg/rat; the release rate at a dose of 1.35 mg/rat was 2.8% of dose/day; after intramuscular injection the response was similar.
1 context sentence(design, population, supporting numbers)
Summary · context
The pharmacokinetic behaviour of leuprolide acetate from a controlled release parenteral dosage form has been studied in rats and dogs.
Report a problemFND-0257084703
04AnimalAnimal study (in vivo)Pharmacokinetics
In rats, serum leuprolide rose sharply after injection by either route and then plateaued for two weeks.
In plain wordsIn rats, blood leuprolide rose sharply after injection and then remained at a plateau for two weeks.
Peptide
Leuprolide
Outcome
MixedSerum drug profile
Study
ratn: not reported in source
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
Dose not stated · subcutaneous or intramuscularAs given in this study (rat).
Source sentences
Summary
In rats, the serum leuprolide acetate levels increased sharply immediately after injection by either route as a consequence of the initial release of the drug; subsequently, the levels attained a plateau for two weeks.
1 context sentence(design, population, supporting numbers)
Summary · context
The pharmacokinetic behaviour of leuprolide acetate from a controlled release parenteral dosage form has been studied in rats and dogs.
Report a problemFND-0257084704
05AnimalAnimal study (in vivo)Pharmacokinetics
In dogs, serum leuprolide profiles followed essentially the same pattern as in rats.
In plain wordsIn dogs, blood leuprolide followed essentially the same pattern as in rats.
Peptide
Leuprolide
Outcome
MixedSerum drug profile in dogs
Study
dogn: not reported in source
Comparator
Rat serum leuprolide profiles
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
Dose not stated
Source sentences
Summary
The serum level profiles in dogs showed essentially the same pattern as those in rats.
2 context sentences(design, population, supporting numbers)
Summary · context
In rats, the serum leuprolide acetate levels increased sharply immediately after injection by either route as a consequence of the initial release of the drug; subsequently, the levels attained a plateau for two weeks.
Summary · context
The pharmacokinetic behaviour of leuprolide acetate from a controlled release parenteral dosage form has been studied in rats and dogs.
Report a problemFND-0257084705
06AnimalAnimal study (in vivo)Efficacy outcome
In rats, leuprolide initially raised testosterone, then suppressed it below normal for over six weeks at 1.35 mg/rat and higher.
In plain wordsIn rats, leuprolide initially raised testosterone, then suppressed it for over six weeks at 1.35 mg/rat and higher.
Peptide
Leuprolide
Outcome
MixedTestosterone suppression at higher doses
Study
ratn: not reported in source
Outcome group
Sex hormones and fertility · Endocrine and hormones
Studied dose
1.35 mg/rat and higherAs given in this study (rat).
Source sentences
Summary
When the dosage form was injected into rats, the serum testosterone level (a pharmacological index) sharply peaked, abruptly decreased to below the normal level, and then was sustained at a suppressed level for over six weeks at a dose of 1.35 mg/rat (equivalent to 3 mg kg-1) and higher,
1 context sentence(design, population, supporting numbers)
Summary · context
The pharmacokinetic behaviour of leuprolide acetate from a controlled release parenteral dosage form has been studied in rats and dogs.
Report a problemFND-0257084706
07AnimalAnimal study (in vivo)Efficacy outcome
In rats, leuprolide at 0.0135 mg/rat did not sufficiently suppress serum testosterone.
In plain wordsIn rats, leuprolide at 0.0135 mg/rat did not sufficiently suppress blood testosterone.
Peptide
Leuprolide
Outcome
Direction not reportedTestosterone suppression at lower dose
Study
ratn: not reported in source
Outcome group
Sex hormones and fertility · Endocrine and hormones
Studied dose
0.0135 mg/ratAs given in this study (rat).
Source sentences
Summary
while the serum testosterone level after an injection of 0.0135 and 0.135 mg/rat was not sufficiently suppressed.
1 context sentence(design, population, supporting numbers)
Summary · context
The pharmacokinetic behaviour of leuprolide acetate from a controlled release parenteral dosage form has been studied in rats and dogs.
Report a problemFND-0257084707
08AnimalAnimal study (in vivo)Efficacy outcome
In rats, leuprolide at 0.135 mg/rat did not sufficiently suppress serum testosterone.
In plain wordsIn rats, leuprolide at 0.135 mg/rat did not sufficiently suppress blood testosterone.
Peptide
Leuprolide
Outcome
Direction not reportedTestosterone suppression at intermediate dose
Study
ratn: not reported in source
Outcome group
Sex hormones and fertility · Endocrine and hormones
Studied dose
0.135 mg/ratAs given in this study (rat).
Source sentences
Summary
while the serum testosterone level after an injection of 0.0135 and 0.135 mg/rat was not sufficiently suppressed.
1 context sentence(design, population, supporting numbers)
Summary · context
The pharmacokinetic behaviour of leuprolide acetate from a controlled release parenteral dosage form has been studied in rats and dogs.
Report a problemFND-0257084708
09AnimalAnimal study (in vivo)Efficacy outcome
In dogs, testosterone profiles after leuprolide followed essentially the same pattern as in rats.
In plain wordsIn dogs, testosterone after leuprolide followed essentially the same pattern as in rats.
Peptide
Leuprolide
Outcome
MixedTestosterone profile in dogs
Study
dogn: not reported in source
Comparator
Rat serum testosterone profiles
Outcome group
Sex hormones and fertility · Endocrine and hormones
Studied dose
Dose not stated
Source sentences
Summary
The profiles in dogs showed essentially the same pattern as those in rats.
2 context sentences(design, population, supporting numbers)
Summary · context
When the dosage form was injected into rats, the serum testosterone level (a pharmacological index) sharply peaked, abruptly decreased to below the normal level, and then was sustained at a suppressed level for over six weeks at a dose of 1.35 mg/rat (equivalent to 3 mg kg-1) and higher,
Summary · context
The pharmacokinetic behaviour of leuprolide acetate from a controlled release parenteral dosage form has been studied in rats and dogs.
Report a problemFND-0257084709
10AnimalAnimal study (in vivo)Efficacy outcome
In dogs, testosterone showed no sharp rise after the second and third leuprolide injections given once every 4 weeks.
In plain wordsIn dogs, testosterone did not rise sharply after the second and third leuprolide injections given once every 4 weeks.
Peptide
Leuprolide
Outcome
Not applicableTestosterone rise after repeat injections
Study
dogn: not reported in source
Outcome group
Sex hormones and fertility · Endocrine and hormones
Studied dose
once every 4 weeksAs given in this study (dog).
Source sentences
Summary
With multiple administrations (once every 4 weeks), serum testosterone levels in dogs did not show any sharp rise after the second and third injections.
1 context sentence(design, population, supporting numbers)
Summary · context
The pharmacokinetic behaviour of leuprolide acetate from a controlled release parenteral dosage form has been studied in rats and dogs.
Report a problemFND-0257084710
11AnimalAnimal study (in vivo)Mechanism
In rats, reproductive organ weight changes agreed with the testosterone suppression profile after leuprolide.
In plain wordsIn rats, reproductive organ weight changes matched the testosterone suppression pattern after leuprolide.
Peptide
Leuprolide
Outcome
Direction not reportedReproductive organ weights
Study
ratn: not reported in source
Outcome group
Sex hormones and fertility · Reproductive and sexual health
Studied dose
Dose not stated
Source sentences
Summary
Changes in rat reproductive organ weights agreed well with the serum testosterone profile in the suppression.
1 context sentence(design, population, supporting numbers)
Summary · context
The pharmacokinetic behaviour of leuprolide acetate from a controlled release parenteral dosage form has been studied in rats and dogs.
Report a problemFND-0257084711

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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

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