{"title":"HP-β-CD包合型匹伐他汀钙快速口腔崩解片的研制与优化","authors":"Prachi Pimple, Prabha Singh, Arati Prabhu, Sonika Gupta","doi":"10.1007/s12247-022-09661-x","DOIUrl":null,"url":null,"abstract":"<div><h3>Purpose</h3><p>The objective of the present study was to develop HP-β-cyclodextrin inclusion complex-based rapid orally disintegrating tablets of pitavastatin calcium by unique sublimation technique for enhancing solubility and dissolution profile of anti-lipidemic class II drug.</p><h3>Methods</h3><p>The inclusion complex was prepared by a physical mixing method containing HP-β-cyclodextrin and pitavastatin calcium. The inclusion complex formation between the guest and host was confirmed by molecular docking studies. The developed inclusion complex was further characterized using differential scanning calorimetry (DSC), Fourier transform-infrared spectroscopy (FT-IR), powder X-ray diffraction study (PXRD), and scanning electron microscopy studies. Fast orally disintegrating tablets of pitavastatin calcium inclusion complex were developed by a unique sublimation technique employing full factorial design (2<sup>4</sup>) using the Design Expert® software. Independent factors, namely, type of super disintegrants and sublimating agents at varying concentrations, were studied for effect on disintegration time, hardness of the tablet, and in vitro drug release.</p><h3>Results</h3><p>Molecular docking studies showed a score of −8.08. Optimized formulation containing 5% Ac-di-sol, 10% camphor showed hardness of about 3.37 ± 0.11 kg/cm<sup>2</sup>, least disintegration time 15.31 ± 0.32 s, and highest in vitro drug release of 99.11 ± 0.23% at the end of 15 min.</p><h3>Conclusion</h3><p>The employed complexation method enhanced solubility and increased in vitro dissolution of pitavastatin calcium. It was concluded that fast orally disintegrating tablets containing inclusion complex gave desired characteristics which provided rapid onset of action by fast disintegration and could improve patient compliance.</p></div>","PeriodicalId":656,"journal":{"name":"Journal of Pharmaceutical Innovation","volume":"17 3","pages":"993 - 1010"},"PeriodicalIF":2.7000,"publicationDate":"2022-06-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://link.springer.com/content/pdf/10.1007/s12247-022-09661-x.pdf","citationCount":"1","resultStr":"{\"title\":\"Development and Optimization of HP-β-CD Inclusion Complex-Based Fast Orally Disintegrating Tablet of Pitavastatin Calcium\",\"authors\":\"Prachi Pimple, Prabha Singh, Arati Prabhu, Sonika Gupta\",\"doi\":\"10.1007/s12247-022-09661-x\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><h3>Purpose</h3><p>The objective of the present study was to develop HP-β-cyclodextrin inclusion complex-based rapid orally disintegrating tablets of pitavastatin calcium by unique sublimation technique for enhancing solubility and dissolution profile of anti-lipidemic class II drug.</p><h3>Methods</h3><p>The inclusion complex was prepared by a physical mixing method containing HP-β-cyclodextrin and pitavastatin calcium. 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引用次数: 1
摘要
目的采用独特的升华技术制备HP-β-环糊精包合物基匹伐他汀钙快速口腔崩解片，以提高抗血脂ⅱ类药物的溶解度和溶出度。方法采用HP-β-环糊精与匹伐他汀钙物理混合法制备包合物。通过分子对接研究证实了宿主与客体之间的包合物形成。利用差示扫描量热法(DSC)、傅里叶变换红外光谱(FT-IR)、粉末x射线衍射(PXRD)和扫描电镜对包合物进行了进一步表征。使用design Expert®软件，采用独特的升华技术，采用全因子设计(24)，开发了匹伐他汀钙包合物快速口腔崩解片。研究了不同浓度的超崩解剂类型和升华剂对崩解时间、片剂硬度和体外释药效果的影响。结果分子对接研究得分为−8.08。优化后的配方为5% ac -二醇、10%樟脑，其硬度约为3.37±0.11 kg/cm2，崩解时间最短为15.31±0.32 s, 15 min时体外释药量最高为99.11±0.23%。结论采用配位法可提高吡伐他汀钙的溶解度，提高其体外溶出度。结论含包合物快速口腔崩解片具有快速崩解起效快、患者依从性好等特点。
Development and Optimization of HP-β-CD Inclusion Complex-Based Fast Orally Disintegrating Tablet of Pitavastatin Calcium
Purpose
The objective of the present study was to develop HP-β-cyclodextrin inclusion complex-based rapid orally disintegrating tablets of pitavastatin calcium by unique sublimation technique for enhancing solubility and dissolution profile of anti-lipidemic class II drug.
Methods
The inclusion complex was prepared by a physical mixing method containing HP-β-cyclodextrin and pitavastatin calcium. The inclusion complex formation between the guest and host was confirmed by molecular docking studies. The developed inclusion complex was further characterized using differential scanning calorimetry (DSC), Fourier transform-infrared spectroscopy (FT-IR), powder X-ray diffraction study (PXRD), and scanning electron microscopy studies. Fast orally disintegrating tablets of pitavastatin calcium inclusion complex were developed by a unique sublimation technique employing full factorial design (24) using the Design Expert® software. Independent factors, namely, type of super disintegrants and sublimating agents at varying concentrations, were studied for effect on disintegration time, hardness of the tablet, and in vitro drug release.
Results
Molecular docking studies showed a score of −8.08. Optimized formulation containing 5% Ac-di-sol, 10% camphor showed hardness of about 3.37 ± 0.11 kg/cm2, least disintegration time 15.31 ± 0.32 s, and highest in vitro drug release of 99.11 ± 0.23% at the end of 15 min.
Conclusion
The employed complexation method enhanced solubility and increased in vitro dissolution of pitavastatin calcium. It was concluded that fast orally disintegrating tablets containing inclusion complex gave desired characteristics which provided rapid onset of action by fast disintegration and could improve patient compliance.
期刊介绍：
The Journal of Pharmaceutical Innovation (JPI), is an international, multidisciplinary peer-reviewed scientific journal dedicated to publishing high quality papers emphasizing innovative research and applied technologies within the pharmaceutical and biotechnology industries. JPI''s goal is to be the premier communication vehicle for the critical body of knowledge that is needed for scientific evolution and technical innovation, from R&D to market. Topics will fall under the following categories:
Materials science,
Product design,
Process design, optimization, automation and control,
Facilities; Information management,
Regulatory policy and strategy,
Supply chain developments ,
Education and professional development,
Journal of Pharmaceutical Innovation publishes four issues a year.
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