Abstract
Objective: The objective of the current study was to develop simple, precise and cost-effective ultraviolet (UV) spectroscopic method for estimation of paliperidone palmitate (PP) as a bulk and in the polymeric depot dosage form.
 Methods: UV spectrophotometer with quartz sample cells and spectral manager software was used for analysis samples. 20 % Methanol in Mili-Q-Water was used as a solvent for the sample and standard preparations. Method validation was carried out as per ICH Q2 (R1) guidelines. Stress degradation studies were carried out to check the stability-indicating performance of the developed method. The validated method was applied for the estimation of the PP content of long-acting injectable microspheres of PP.
 Results: The wavelength of maximum absorption was found to be 283 nm. The proposed method was validated in the range of 5-30 µg/ml of PP. The mean recovery for 80%, 100% and 120% standard solution was found to be 99.03%, 99.21% and 99.35% respectively with less than 2% relative standard deviation (RSD). Intra-day and inter-day method precision ranged from 0.54 to 1.62% and 0.67 and 1.24% respectively. Limit of detection (LOD) and limit of quantitation (LOQ) were estimated to be 0.03 and 0.10 µg/ml respectively. The developed method was found to be robust and rugged. Stress degradation studies were carried out under acidic, alkaline, hydrolytic and oxidative and photo stress. The proposed method was capable to detect changes in assay due to stress conditions.
 Conclusion: The developed method was successfully employed for routine analysis of drug loading in long-acting injectable microspheres of PP.
Highlights
Paliperidone palmitate (PP) is newer widely prescribed atypical antipsychotics for the treatment of schizophrenia [1,2,3]
PP belongs to the class of benzisoxazole derivatives
Paliperidone palmitate is a prodrug and it gets hydrolyzed to paliperidone
Summary
Paliperidone palmitate (PP) is newer widely prescribed atypical antipsychotics for the treatment of schizophrenia [1,2,3]. PP belongs to the class of benzisoxazole derivatives. The chemical name is (9RS)-3-[2-[4-(6-Fluoro1,2-benzisoxazol-3-yl)piperidin-1-yl]ethyl]2-methyl-4-oxo-6,7,8,9-tetrahydro-4Hpyrido [1,2-a] pyrimadin-9-yl hexadecanoate. Paliperidone palmitate is a prodrug and it gets hydrolyzed to paliperidone. It was postulated that the drug's therapeutic effect in schizophrenia may be due to a combination of central dopamine type 2 (D2) and serotonin Type 2 (5HT2A) receptor antagonism. PP is very slightly soluble in ethanol and methanol, practically insoluble in polyethylene glycol 400 and propylene glycol, and slightly soluble in ethyl acetate [4]
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