Displaying all 12 publications

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  1. Samiun WS, Ashari SE, Salim N, Ahmad S
    Int J Nanomedicine, 2020;15:1585-1594.
    PMID: 32210553 DOI: 10.2147/IJN.S198914
    Background: Aripiprazole, which is a quinolinone derivative, has been widely used to treat schizophrenia, major depressive disorder, and bipolar disorder.

    Purpose: A Central Composite Rotatable Design (CCRD) of Response Surface Methodology (RSM) was used purposely to optimize process parameters conditions for formulating nanoemulsion containing aripiprazole using high emulsification methods.

    Methods: This design is used to investigate the influences of four independent variables (overhead stirring time (A), shear rate (B), shear time (C), and the cycle of high-pressure homogenizer (D)) on the response variable namely, a droplet size (Y) of nanoemulsion containing aripiprazole.

    Results: The optimum conditions suggested by the predicted model were: 120 min of overhead stirring time, 15 min of high shear homogenizer time, 4400 rpm of high shear homogenizer rate and 11 cycles of high-pressure homogenizer, giving a desirable droplet size of nanoemulsion containing aripiprazole of 64.52 nm for experimental value and 62.59 nm for predicted value. The analysis of variance (ANOVA) showed the quadratic polynomial fitted the experimental values with F-value (9.53), a low p-value (0.0003) and a non-significant lack of-fit. It proved that the models were adequate to predict the relevance response. The optimized formulation with a viscosity value of 3.72 mPa.s and pH value of 7.4 showed good osmolality value (297 mOsm/kg) and remained stable for three months in three different temperatures (4°C, 25°C, and 45°C).

    Conclusion: This proven that response surface methodology is an efficient tool to produce desirable droplet size of nanoemulsion containing aripiprazole for parenteral delivery application.

    Matched MeSH terms: Aripiprazole/chemistry*
  2. Sakurama K, Nishi K, Chuang VTG, Hashimoto M, Yamasaki K, Otagiri M
    Biol Pharm Bull, 2020;43(6):1023-1026.
    PMID: 32475912 DOI: 10.1248/bpb.b20-00205
    Aripiprazole (ARP) is one of antipsychotics and binds to human serum albumin (HSA) with a high affinity. In this study, we investigated the binding characteristics of ARP to oxidized HSA as observed in chronic disease conditions. Oxidized HSAs were prepared using chloramine-T (CT-HSA) or metal-catalyzed oxidation system (MCO-HSA) in vitro, respectively. An increase in the carbonyl content was confirmed in oxidized HSAs. From the results of circular dichroism (CD) and tryptophan fluorescence spectra, no significant structural change of oxidized HSAs was observed. These results indicate that prepared HSAs are mildly oxidized and well reflects the status of HSA during chronic diseases. However, oxidized HSAs were observed to have a significant decrease in binding to ARP. The results of the induced CD spectrum suggested that ARP bound to oxidized HSAs with a similar orientation. These results suggest that oxidation of HSA during chronic disease state significantly affected the microenvironment of the binding site for ARP and binding capacity of HSA to ARP.
    Matched MeSH terms: Aripiprazole/chemistry*
  3. Pakri Mohamed RM, Kumar J, Ahmad SU, Mohamed IN
    Curr Drug Targets, 2018;19(12):1378-1390.
    PMID: 29788886 DOI: 10.2174/1389450119666180523092534
    In the past two decades, the search for novel pharmacotherapies to treat alcohol addiction has been a global endeavor. This has resulted in several drugs that have been approved and successfully marketed for public use while some are still in the testing phase. These pharmacological agents, though effective for the treatment of alcoholism, are not without shortcomings; such as abuse potential, serious mental and physical adverse effects, interaction with alcohol and also poor metabolism and excretion. As more is being understood about the neurobiology of alcohol addiction as well as the unique pharmacological action of these drugs, new agents are evaluated for potential benefits when used as an adjunct in combination therapy. This review article summarizes the novel pharmacotherapeutic approaches used in the treatment of alcohol addiction by focusing on the drugs, which include neramexane, gabapentin, baclofen, aripiprazole, nalmafene, and quetiapine.
    Matched MeSH terms: Aripiprazole/adverse effects; Aripiprazole/therapeutic use
  4. Ishigooka J, Nakamura J, Fujii Y, Iwata N, Kishimoto T, Iyo M, et al.
    Schizophr Res, 2015 Feb;161(2-3):421-8.
    PMID: 25556976 DOI: 10.1016/j.schres.2014.12.013
    This study was designed to evaluate efficacy and safety of aripiprazole once-monthly (AOM) by verifying non-inferiority of AOM to oral aripiprazole in Asian patients with schizophrenia.
    Matched MeSH terms: Aripiprazole/administration & dosage*; Aripiprazole/adverse effects
  5. Kumbhar SA, Kokare CR, Shrivastava B, Gorain B, Choudhury H
    J Pharm Sci, 2021 04;110(4):1761-1778.
    PMID: 33515583 DOI: 10.1016/j.xphs.2021.01.021
    Delivering therapeutics to the brain using conventional dosage forms is always a challenge, thus the present study was aimed to formulate mucoadhesive nanoemulsion (MNE) of aripiprazole (ARP) for intranasal delivery to transport the drug directly to the brain. Therefore, a TPGS based ARP-MNE was formulated and optimized using the Box-Behnken statistical design. The improved in vitro release profile of the formulation was in agreement to enhanced ex vivo permeation through sheep mucous membranes with a maximum rate of permeation co-efficient (62.87  cm h-1 × 103) and flux (31.43  μg cm-2.h-1). The pharmacokinetic profile following single-dose administration showed the maximum concentration of drug in the brain (Cmax) of 15.19 ± 2.51  μg mL-1 and Tmax of 1 h in animals with ARP-MNE as compared to 10.57 ± 1.88  μg mL-1 and 1 h, and 2.52 ± 0.38  μg mL-1 and 3 h upon intranasal and intravenous administration of ARP-NE, respectively. Further, higher values of % drug targeting efficiency (96.9%) and % drug targeting potential (89.73%) of ARP-MNE through intranasal administration were investigated. The studies in Wistar rats showed no existence of extrapyramidal symptoms through the catalepsy test and forelimb retraction results. No ex vivo ciliotoxicity on nasal mucosa reflects the safety of the components and delivery tool. Further, findings on locomotor activity and hind-limb retraction test in ARP-MNE treated animals established its antipsychotic efficacy. Thus, it can be inferred that the developed ARP-MNE could effectively be explored as brain delivery cargo in the effective treatment of schizophrenia without producing any toxic manifestation.
    Matched MeSH terms: Aripiprazole
  6. Sakurama K, Kawai A, Tuan Giam Chuang V, Kanamori Y, Osa M, Taguchi K, et al.
    ACS Omega, 2018 Oct 31;3(10):13790-13797.
    PMID: 30411049 DOI: 10.1021/acsomega.8b02057
    Aripiprazole (ARP), a quinolinone derivative, is an atypical antipsychotic drug that is used in the treatment of schizophrenia. ARP has an extensive distribution and more than 99% of the ARP and dehydro-ARP, the main active metabolite, is bound to plasma proteins. However, information regarding the protein binding of ARP is limited. In this study, we report on a systematic study of the protein binding of ARP. The interaction of ARP and structurally related compounds with human serum albumin (HSA) was examined using equilibrium dialysis, circular dichroism (CD) spectroscopy, fluorescent probe displacement, and an X-ray crystallographic analysis. The binding affinities (nK) for ARP and its main metabolite, dehydro-ARP with HSA were found to be significantly higher than other structurally related compounds. The results of equilibrium dialysis experiments and CD spectral data indicated that the chloro-group linked to the phenylpiperazine ring in the ARP molecule plays a major role in the binding of these ligands to HSA. Furthermore, fluorescent probe displacement results indicated that ARP appears to bind at the site II pocket in subdomain III. A detailed CD spectral analysis suggests that the chloro-group linked to the phenylpiperazine ring may control the geometry of the ARP molecule when binding in the site II binding pocket. X-ray crystallographic analysis of the ARP-HSA complex revealed that the distance between the chlorine atom at the 3-positon of dichlorophenyl-piperazine on ARP and the sulfur atom of Cys392 in HSA was 3.4-3.6 Å. A similar halogen bond interaction has also been observed in the HSA structure complexed with diazepam, which also contains a chloro-group. Thus, the mechanism responsible for the binding of ARP to a protein elucidated here should be relevant for assessing the pharmacokinetics and pharmacodynamics of ARP in various clinical situations and for designing new drugs.
    Matched MeSH terms: Aripiprazole
  7. Normala I, Hamidin A
    Med J Malaysia, 2009 Sep;64(3):240-1.
    PMID: 20527278 MyJurnal
    The use of atypical antipsychotic agents in early onset schizophrenia is rising despite its limited data on efficacy, safety and tolerability. Early onset schizophrenia warrants effective pharmacological treatment that is safe and well tolerated by children and adolescent population. Existing atypical agents are not completely free of side effects. Aripiprazole has unique properties that differ from other atypical antipsychotics and fill up the missing gaps, as it is associated with minimal metabolic complications and extrapyramidal side effects that are more commonly seen in other atypical agents. It offers a better option for this population and may possibly be considered as first line treatment in future. This case report demonstrates the efficacy and safety of Aripiprazole in children and adolescent population.
    Matched MeSH terms: Aripiprazole
  8. Ng CG, Chan PL, Said MA
    MyJurnal
    Introduction: Second generation antipsychotic (SGA) was linked to increased risk of metabolic syndrome. The risk varies between different SGA. We aim to study this risk by examining the co-prescription of antihypertensive, antidiabetic and lipid lowering drugs in patients prescribed with either aripiprazole, quetiapine or clozapine.
    Methods: This is a retrospective cohort study based on the prescription records of a teaching hospital. Prescription records between January 1, 2013 and December 31, 2014 for
    psychiatric unit were extracted. Patients with at least one prescription of any antipsychotic were included. The odds of antihypertensive, antidiabetic and lipid lowering drugs co-prescription in patients with either aripiprazole, quetiapine or clozapine were calculated.
    Results: Of the 1742 study subjects, 88 patients were prescribed with aripiprazole, 175 patients with clozapine and 124 patients with quetiapine. Patients prescribed with quetiapine had
    higher odds of co-prescribed with antihypertensive (OR = 1.71, 95% CI = 1.11, 2.63), antidiabetic drugs (OR = 1.81, 95% CI = 1.11, 2.95) and lipid lowering drugs (OR = 1.94, 95% CI = 1.19, 3.16). There were higher odds of co-prescription of antihypertensive (OR = 1.54, 95% CI = 1.05, 2.25), antidiabetic drugs (OR = 1.69, 95% CI = 1.10, 2.59) and lipid lowering drugs
    (OR = 1.90, 95% CI = 1.24, 2.91) in patients with clozapine. However, there were no increase odds of co-prescription of the three agents in patients with aripiprazole.
    Conclusion: We need to monitor the risk of metabolic syndrome in patients treated with SGA. Aripiprazole has lower risk of metabolic syndrome.
    Matched MeSH terms: Aripiprazole
  9. Ng, C.G., Seed, H.F., Thong, K.S.
    MyJurnal
    Introduction: Atypical antipsychotic drugs are effective in the treatment of bipolar disorder. Studies have shown that atypical antipsychotic drugs are more superior to typical antipsychotic in term of neurocognitive function, negative symptoms and extrapyramidal side effects. Both aripiprazole and quetiapine are atypical antipsychotic drugs that are effective and commonly used in all phases of bipolar disorder treatment. Objective: The aim of this study is to examine and compare the clinical outcomes of aripiprazole and quetiapine in bipolar disorder patients. Method: This was a retrospective cohort study among patients from psychiatric unit, University Malaya Medical Center. Prescription records dated between January 1, 2013 and December 31, 2014 for psychiatric unit were extracted. The data of the subjects with prescription of the two atypical antipsychotic, namely aripiprazole and quetiapine was extracted. The outcome measures were the co-prescription of antihypertensive drugs, antidiabetic drugs and lipid lowering drugs. Results: A total of 58 subjects were recruited, 11 were on aripiprazole and 47 were on quetiapine. Statistical analysis has shown that both aripiprazole and quetiapine do not have any association with compliance to the medication and also follow up. Study also revealed that there is no association between the aripiprazole and quetiapine group with the metabolic side effects that were measured such as systolic or diastolic blood pressure, waist circumference, weight, glucose level and body mass index. Conclusion: This study has shown that both aripiprazole and quetiapine were similar in terms of metabolic side effect, compliance to medications and follow up.
    Matched MeSH terms: Aripiprazole
  10. Roffeei SN, Reynolds GP, Zainal NZ, Said MA, Hatim A, Aida SA, et al.
    Hum Psychopharmacol, 2014 Jan;29(1):38-45.
    PMID: 24424705 DOI: 10.1002/hup.2366
    Various genetic polymorphisms have been reported to be associated with antipsychotic-induced weight gain. In this study, we aimed to determine whether risk polymorphisms in 12 candidate genes are associated with reduction in body mass index (BMI) of patients following switching of antipsychotics to aripiprazole or ziprasidone.
    Matched MeSH terms: Aripiprazole
  11. Sulaiman AH, Gill JS, Said MA, Zainal NZ, Hussein HM, Guan NC
    Int J Psychiatry Clin Pract, 2013 Jun;17(2):131-8.
    PMID: 22486597 DOI: 10.3109/13651501.2012.667116
    The objectives of this study were to determine the efficacy and safety of aripiprazole for treatment of psychosis, retention and abstinence in patients with methamphetamine dependence.
    Matched MeSH terms: Aripiprazole
  12. Said MA, Hatim A, Habil MH, Zafidah W, Haslina MY, Badiah Y, et al.
    Prev Med, 2013;57 Suppl:S50-3.
    PMID: 23337566 DOI: 10.1016/j.ypmed.2013.01.005
    OBJECTIVE: The objective of this study is to determine the prevalence of metabolic syndrome among schizophrenia patients receiving antipsychotic monotherapy in Malaysia.
    METHOD: A cross-sectional study was conducted at multiple centres between June 2008 and September 2011. Two hundred and five patients who fulfilled the DSM IV-TR diagnostic criteria for schizophrenia and who had been on antipsychotic medication for at least one year, were screened for metabolic syndrome. Patients receiving a mood stabilizer were excluded from the study. Metabolic syndrome was defined by using the National Cholesterol Education Program (NCEP) Expert Panel on Detection, Evaluation, and Treatment of High Blood Cholesterol in Adults Treatment Panel III (ATP III) modified for Asian waist circumference.
    RESULTS: In the first-generation antipsychotic (FGA) group, the highest prevalence of metabolic syndrome was among patients treated with trifluoperazine and flupenthixol decanoate (66.7% each). For the second-generation antipsychotic (SGA) group, the highest prevalence of metabolic syndrome was among patients treated with clozapine (66.7%). The component with the highest prevalence in metabolic syndrome was waist circumference in both FGA and SGA groups except for aripiprazole in SGA.
    CONCLUSION: The prevalence of metabolic syndrome in schizophrenia patients receiving antipsychotic monotherapy in Malaysia was very high. Intervention measures are urgently needed to combat these problems.
    KEYWORDS: Antipsychotics; Metabolic syndrome; Monotherapy; Prevalence; Schizophrenia
    Matched MeSH terms: Aripiprazole
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