Paliperidone palmitate-induced facial angioedema:A case report

BACKGROUND Paliperidone palmitate is a once-monthly injectable,atypical antipsychotic.To our knowledge,there has been only one report of paliperidone palmitate-induced angioedema presenting with acute laryngeal edema with subsequent respiratory arrest.Here,we present a case report of paliperidone palmitate-induced angioedema with a relatively mild clinical presentation compared with the previously reported case,and the patient's condition was not complicated by lifethreatening anaphylaxis.CASE SUMMARY A 79-year-old female,who had a major neurocognitive disorder due to Alzheimer's disease with behavioral disturbances.Paliperidone palmitate was offlabel used to control her aggression,irritability,and psychosis.After induction doses(150 mg and 100 mg intramuscularly,given 1 wk apart),she developed intermittent swelling of the face,eyelids,and lips on day 17 after the initial dose,and the edema was explicitly seen on day 20.The diagnosis was paliperidone palmitate-induced angioedema.The monthly injection dose was discontinued on day 33 after the initial dose.The angioedema was subsequently alleviated,and it had completely resolved by day 40 after the initial dose.CONCLUSION Paliperidone palmitate-induced angioedema is a rare condition and can present with a mild,intermittent facial edema,which may be overlooked in clinical practice.

Can semipermeable membranes coating materials influence in vivo performance for paliperidone tri-layer ascending release osmotic pump tablet:In vitro evaluation and in vivo pharmacokinetics study

One purpose of this study was to develop a paliperidone(PAL)tri-layer ascending release pushepull osmotic pump(TA-PPOP)tablet which could meet the needs of clinical applications.And another purpose was to investigate whether different coating materials influenced in vivo performance of TA-PPOP.The ascending release mechanism of this trilayer delivery system on theory was elaborated.TA-PPOP was prepared by means of coating with cellulose acetate(CA)or ethyl cellulose(EC).Several important influence factors such as different core tablet compositions and different coating solution ingredients involved in the formulation procedure were investigated.The optimization of formulation and process was conducted by comparing different in vitro release behaviors of PAL.In vitro dissolution studies indicated that both the two formulations of different coating materials were able to deliver PAL at an ascending release rate during the whole 24 h test.The in vivo pharmacokinetics study showed that both self-made PPOP tablets with different coating had a good in vitro-in vivo correlation(IVIVC)and were bioequivalent with the brand product,which demonstrated no significant influence of the coating materials on the in vivo release acceleration of TA-PPOP.

Development and validation of a rapid and sensitive UHPLCeMS/MS method for the determination of paliperidone in beagle dog plasma

In order to evaluate the pharmacokinetic profile of paliperidone extended-release tablets in vivo,a simple and rapid ultra-high performance liquid chromatographyetandem mass spectrometry(UHPLCeMS/MS)method was developed and validated for the determination of paliperidone in beagle dog plasma.Paliperidone and diazepam(internal standard)were extracted from plasma samples with diethyl ether,and then separated on a C_(18) column(2.1×50 mm,2.6 mm)under gradient elution with methanol-0.1%formic acid at a flow rate of 0.3 ml/min.The compounds were detected using a triple-quadrupole mass spectrometer equipped with an electrospray ionization(ESI)source.The validated method was linear over the concentration range of 1.00-1000.00 ng/ml and the lower limit of quantitation was 1.00 ng/ml.The intra-day and inter-day precision values were not more than 15%(relative standard deviation<20%at low levels),while the accuracy was within±10%of nominal values.The validated UHPLC-MS/MS method was successfully applied to an oral pharmacokinetic study of paliperidone extended-release tablets in a beagle dog.

Tablets of paliperidone using compression-coated technology for controlled ascending release

The aim of this work was to prepare ascending release compression-coated(CC) tablets with paliperidone(PAL) using a simple manufacturing technique and short manufacturing process.The release behavior and mechanisms in vitro of the final tablets was investigated and evaluated. The PAL CC tablets were comprised of a core layer of high viscosity hydroxypropyl cellulose(HPC-H) and a coating layer of high viscosity hydroxypropyl methylcellulose(HPMCK100 M). Several factors such as materials and core tablet compositions were studied for their influence in the formulation procedure. The drug release mechanism was studied using gravimetric analysis. The data could be fitted to the Peppas model. The ascending drug release results were expressed in terms of the slope of the release curve at different time points.Results showed that the formulation could achieve a good ascending drug release when the weight ratio of PAL was 5:1(core:layer). The fraction of HPC and HPMC was 33 %, and the combination of Eudragit RL-PO was 10%. The ascending release mechanism was due to solvent penetration into the PAL CC tablets, and subsequent drug dissolution from the gelatinous HPC and HPMC matrix erosion. The release mechanism was therefore a combination of diffusion and erosion. This work demonstrated that the compression-coated tablets could achieve controlled ascending release over 24 h for the oral administration systems.

Different effects of paliperidone and risperidone therapy on blood lipid and Hcy metabolism as well as endocrine hormones in patients with schizophrenia

Objective: To explore the different effects of paliperidone and risperidone therapy on blood lipid and Hcy metabolism as well as endocrine hormones in patients with schizophrenia. Methods: A total of 118 patients with schizophrenia who were treated in the hospital between December 2014 and February 2017 were collected as the research subjects and divided into control group and study group by random number table, each group with 59 cases. Control group received risperidone therapy, observation group received paliperidone therapy, and the differences in the levels of blood lipid indexes, Hcy metabolism indexes and endocrine hormones were compared between the two groups before and after treatment. Results:There was no statistically significant difference in the levels of blood lipid indexes, Hcy and endocrine hormones between the two groups before treatment. After treatment, lipid indexes TG and TC levels in peripheral blood of study group were lower than those of control group while HDL-C content was higher than that of control group;Hcy level in serum of study group was lower than that of control group;endocrine hormones FT3, FT4, T and E2 levels in serum of study group were higher than those of control group. Conclusion: paliperidone therapy for schizophrenia can be more effective than risperidone in regulating blood lipid metabolism, Hcy metabolism and endocrine hormones.

Association of ABCB1 Gene Polymorphisms with Efficacy and Adverse Reaction to Risperidone or Paliperidone in Han Chinese Schizophrenic Patients

Dear editor, P-glycoprotein （P-gp, also known as ATP-binding cassette transport sub-family B member 1, ABCB1） is a potent ATP-dependent efflux pump for a wide variety of drugs. Although studies of its substrates are abundant [ 1, 2], and ABCB1 is a well-conserved gene, there is increasing evi- dence that its polymorphisms affect substrate specificity [3]. A previous study reported that the synonymous single nucleotide polymorphism （SNP） C3435T （rs1045642） affects the timing of co-translational folding and insertionof P-gp into the membrane,

Predictor of discontinuation with paliperidone palmitate in patients with schizophrenia

Objective To explore the influence of demographic characteristics,psychiatric symptoms and medication on the adherence of long-acting injectable paliperidone palmitate(PP)treatment in schizophrenia patients.Methods In this one year,naturalistic longitudinal study,156 consecutive patients with schizophrenia were initi-

帕利哌酮缓释片与利培酮治疗精神分裂症的对照研究

目的为了比较帕利哌酮缓释片与利培酮治疗精神分裂症患者的疗效及安全性的差异。方法选取某精神病院60例精神分裂症患者,随机分成帕利哌酮组和利培酮组各30例,分别采用帕利哌酮缓释片和利培酮进行治疗,观察8周。以阳性及阴性症状量表(PANSS)减分率评定疗效,用治疗中出现的症状量表(TESS)评定不良反应,以个人和社会功能量表(PSP)评定社会功能。结果帕利哌酮组与利培酮组的总显效率(痊愈+显效)和总有效率(痊愈+显效+有效)的差异不显著(P>0.05)。患者治疗后,两组的PANSS总分及各因子分明显降低(P<0.05)。与利培酮组比较,帕利哌酮组的不良反应出现频率低、程度轻微,个人和社会功能恢复快。结论帕利哌酮缓释片是一种安全有效的新型抗精神病药,可以明显改善精神分裂症和分裂样精神病患者的精神病性症状及社会功能。