Pharmacokinetics and tolerability of paliperidone palmitate injection in Chinese subjects.
Hum Psychopharmacol
; 29(2): 203-10, 2014 Mar.
Article
en En
| MEDLINE
| ID: mdl-24590546
ABSTRACT
OBJECTIVE:
The objective of this study was to characterize the pharmacokinetics of 25, 100, and 150 mg equivalents (eq.) of paliperidone long-acting injection in Chinese subjects with schizophrenia.METHODS:
This was an open-label, randomized, parallel group, multicenter study. A total of 48 patients were randomized in a 111 ratio to one of three groups. Sequential blood samples were collected immediately before injection on day 1 and up to 210 days after the first injection. The plasma paliperidone concentrations were determined by a validated high-performance liquid chromatography/tandem mass spectrometry method.RESULTS:
A total of 47 patients received at least one injection of the study medication, and 43 completed the study. The pharmacokinetic (PK) parameters, such as time to maximum concentration, t1/2, and CL/F, were comparable across the three treatment groups (p = 0.935, 0.349, and 0.794, respectively). The differences in maximum plasma concentration, AUC (035 days), AUC (0-210 days), and AUC (0-∞) were significant (p < 0.001) and dose proportional. The inter-individual variation of PK parameters was large. The most frequent treatment-emergent adverse events were prolactin level increasing, injection site pain, tremor, dry mouth, and constipation.CONCLUSIONS:
The pharmacokinetics of paliperidone palmitate are linear with respect to time in Chinese subjects with schizophrenia at injections from 25 to 150 mg eq.Palabras clave
Texto completo:
1
Banco de datos:
MEDLINE
Asunto principal:
Palmitatos
/
Esquizofrenia
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Antipsicóticos
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Isoxazoles
Tipo de estudio:
Clinical_trials
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Etiology_studies
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Prognostic_studies
Límite:
Female
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Humans
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Male
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Middle aged
Idioma:
En
Año:
2014
Tipo del documento:
Article