Sophia Awais, Mehwish Afridi, Azra Batool, Muhammad Tayyab Ansari, Kishwar Sultana, Hameeza Momal, Walaa F Alsanie, Abdulhakeem S Alamri, Majid Alhomrani
{"title":"利用 L-精氨酸/赖氨酸和 MβCD/HPβCD 按不同摩尔比制备阿立哌唑的二元和三元包合物并进行比较。","authors":"Sophia Awais, Mehwish Afridi, Azra Batool, Muhammad Tayyab Ansari, Kishwar Sultana, Hameeza Momal, Walaa F Alsanie, Abdulhakeem S Alamri, Majid Alhomrani","doi":"","DOIUrl":null,"url":null,"abstract":"<p><p>Aripiprazole (ARI), an antipsychotic having low solubility and stability. To overcome this, formation of binary and ternary using inclusion complexes of Methyl-β-cyclodextrin (MβCD) /Hydroxy propyl beta cyclodextrin (HPβCD) and L-Arginine (ARG)/ Lysine (LYS) are analyzed by dissolution testing and phase stability study along with their complexation efficacy and solubility constants made by physical mixing. Inclusion complexes with ARG were better than LYS and prepared by solvent evaporation and lyophilization method as well. They are characterized by Attenuated Total Reflection Fourier Transform Infrared Spectroscopy (AT-FTIR), X-ray powder diffractometry (XRD), Differential Scanning Calorimetry (DSC), Scanning electron microscopy (SEM) and Thermal gravimetric analysis (TGA). The bond shifting in AT-FTIR confirmed the molecular interactions between host and guest molecules. The SEM images also confirmed a complete change of drug morphology in case of ternary inclusion complexes prepared by lyophilization method for both the polymers. ARI: MβCD: ARG when used in the specific molar ratio of 1:1:0.27 by prepared by lyophilization method has 18 times best solubility while ARI:HPβCD:ARG was 7 times best solubility than pure drug making MβCD a better choice than HPβCD. Change in the molar ratio will cause loss of stability or solubility. Solvent evaporation gave significant level of solubility but less stability.</p>","PeriodicalId":19971,"journal":{"name":"Pakistan journal of pharmaceutical sciences","volume":null,"pages":null},"PeriodicalIF":0.7000,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Preparation and comparison of binary and ternary inclusion complexes of aripiprazole using L-arginine/lysine and MβCD/HPβCD by using different molar ratios.\",\"authors\":\"Sophia Awais, Mehwish Afridi, Azra Batool, Muhammad Tayyab Ansari, Kishwar Sultana, Hameeza Momal, Walaa F Alsanie, Abdulhakeem S Alamri, Majid Alhomrani\",\"doi\":\"\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><p>Aripiprazole (ARI), an antipsychotic having low solubility and stability. To overcome this, formation of binary and ternary using inclusion complexes of Methyl-β-cyclodextrin (MβCD) /Hydroxy propyl beta cyclodextrin (HPβCD) and L-Arginine (ARG)/ Lysine (LYS) are analyzed by dissolution testing and phase stability study along with their complexation efficacy and solubility constants made by physical mixing. Inclusion complexes with ARG were better than LYS and prepared by solvent evaporation and lyophilization method as well. They are characterized by Attenuated Total Reflection Fourier Transform Infrared Spectroscopy (AT-FTIR), X-ray powder diffractometry (XRD), Differential Scanning Calorimetry (DSC), Scanning electron microscopy (SEM) and Thermal gravimetric analysis (TGA). The bond shifting in AT-FTIR confirmed the molecular interactions between host and guest molecules. The SEM images also confirmed a complete change of drug morphology in case of ternary inclusion complexes prepared by lyophilization method for both the polymers. ARI: MβCD: ARG when used in the specific molar ratio of 1:1:0.27 by prepared by lyophilization method has 18 times best solubility while ARI:HPβCD:ARG was 7 times best solubility than pure drug making MβCD a better choice than HPβCD. Change in the molar ratio will cause loss of stability or solubility. Solvent evaporation gave significant level of solubility but less stability.</p>\",\"PeriodicalId\":19971,\"journal\":{\"name\":\"Pakistan journal of pharmaceutical sciences\",\"volume\":null,\"pages\":null},\"PeriodicalIF\":0.7000,\"publicationDate\":\"2024-01-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Pakistan journal of pharmaceutical sciences\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"\",\"RegionNum\":4,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q4\",\"JCRName\":\"PHARMACOLOGY & PHARMACY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Pakistan journal of pharmaceutical sciences","FirstCategoryId":"3","ListUrlMain":"","RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q4","JCRName":"PHARMACOLOGY & PHARMACY","Score":null,"Total":0}
Preparation and comparison of binary and ternary inclusion complexes of aripiprazole using L-arginine/lysine and MβCD/HPβCD by using different molar ratios.
Aripiprazole (ARI), an antipsychotic having low solubility and stability. To overcome this, formation of binary and ternary using inclusion complexes of Methyl-β-cyclodextrin (MβCD) /Hydroxy propyl beta cyclodextrin (HPβCD) and L-Arginine (ARG)/ Lysine (LYS) are analyzed by dissolution testing and phase stability study along with their complexation efficacy and solubility constants made by physical mixing. Inclusion complexes with ARG were better than LYS and prepared by solvent evaporation and lyophilization method as well. They are characterized by Attenuated Total Reflection Fourier Transform Infrared Spectroscopy (AT-FTIR), X-ray powder diffractometry (XRD), Differential Scanning Calorimetry (DSC), Scanning electron microscopy (SEM) and Thermal gravimetric analysis (TGA). The bond shifting in AT-FTIR confirmed the molecular interactions between host and guest molecules. The SEM images also confirmed a complete change of drug morphology in case of ternary inclusion complexes prepared by lyophilization method for both the polymers. ARI: MβCD: ARG when used in the specific molar ratio of 1:1:0.27 by prepared by lyophilization method has 18 times best solubility while ARI:HPβCD:ARG was 7 times best solubility than pure drug making MβCD a better choice than HPβCD. Change in the molar ratio will cause loss of stability or solubility. Solvent evaporation gave significant level of solubility but less stability.
期刊介绍:
Pakistan Journal of Pharmaceutical Sciences (PJPS) is a peer reviewed multi-disciplinary pharmaceutical sciences journal. The PJPS had its origin in 1988 from the Faculty of Pharmacy, University of Karachi as a biannual journal, frequency converted as quarterly in 2005, and now PJPS is being published as bi-monthly from January 2013.
PJPS covers Biological, Pharmaceutical and Medicinal Research (Drug Delivery, Pharmacy Management, Molecular Biology, Biochemical, Pharmacology, Pharmacokinetics, Phytochemical, Bio-analytical, Therapeutics, Biotechnology and research on nano particles.