{"title":"固体分散吸附技术增强阿托伐他汀钙的溶解度和溶出度","authors":"S. K. Ali, Eman B. H. Al-Khedairy","doi":"10.31351/vol28iss2pp105-114","DOIUrl":null,"url":null,"abstract":"Atorvastatin (ATR) is poorly soluble anti-hyperlipidemic drug; it belongs to the class II group according to the biopharmaceutical classification system (BCS) with low bioavailability due to its low solubility. Solid dispersions adsorbate is an effective technique for enhancing the solubility and dissolution of poorly soluble drugs. \n The present study aims to enhance the solubility and dissolution rate of ATR using solid dispersion adsorption technique in comparison with ordinary solid dispersion. polyethylene glycol 4000 (PEG 4000), polyethylene glycol 6000 (PEG 6000), Poloxamer188 and Poloxamer 407were used as hydrophilic carriers and Aerosil 200, Aerosil 300 and magnesium aluminium silicate (MAS) as adsorbents. \n All solid dispersion adsorbate (SDA) formulas were prepared in ratios of 1:1:1 (drug: carrier: adsorbent) and evaluated for their water solubility, percentage yield, drug content, , dissolution, crystal structure using X-ray powder diffraction (XRD) and Differential Scanning Calorimetry (DSC) studies and Fourier Transform Infrared Spectroscopy (FTIR) for determination the drug-carrier- adsorbate interaction. \n The prepared (SDA) showed significant improvement of drug solubility in all prepared formula. Best result was obtained with formula SDA12(ATR :Poloxamer407 : MAS 1:1:1) that showed 8.07 and 5.38 \nfold increase in solubility compared to solubility of pure ATR and solid dispersion(SD4) (Atorvastatin: Poloxamer 407 1:1) respectively due to increased wettability and reduced crystallinity of the drug which leads to improve drug solubility and dissolution .","PeriodicalId":14600,"journal":{"name":"Iraqi Journal of Pharmaceutical Sciences","volume":"28 1","pages":"105-114"},"PeriodicalIF":0.0000,"publicationDate":"2019-12-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"8","resultStr":"{\"title\":\"Solubility and Dissolution Enhancement of Atorvastatin Calcium using Solid Dispersion Adsorbate Technique\",\"authors\":\"S. K. Ali, Eman B. H. 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Solid dispersions adsorbate is an effective technique for enhancing the solubility and dissolution of poorly soluble drugs. \\n The present study aims to enhance the solubility and dissolution rate of ATR using solid dispersion adsorption technique in comparison with ordinary solid dispersion. polyethylene glycol 4000 (PEG 4000), polyethylene glycol 6000 (PEG 6000), Poloxamer188 and Poloxamer 407were used as hydrophilic carriers and Aerosil 200, Aerosil 300 and magnesium aluminium silicate (MAS) as adsorbents. \\n All solid dispersion adsorbate (SDA) formulas were prepared in ratios of 1:1:1 (drug: carrier: adsorbent) and evaluated for their water solubility, percentage yield, drug content, , dissolution, crystal structure using X-ray powder diffraction (XRD) and Differential Scanning Calorimetry (DSC) studies and Fourier Transform Infrared Spectroscopy (FTIR) for determination the drug-carrier- adsorbate interaction. \\n The prepared (SDA) showed significant improvement of drug solubility in all prepared formula. Best result was obtained with formula SDA12(ATR :Poloxamer407 : MAS 1:1:1) that showed 8.07 and 5.38 \\nfold increase in solubility compared to solubility of pure ATR and solid dispersion(SD4) (Atorvastatin: Poloxamer 407 1:1) respectively due to increased wettability and reduced crystallinity of the drug which leads to improve drug solubility and dissolution .\",\"PeriodicalId\":14600,\"journal\":{\"name\":\"Iraqi Journal of Pharmaceutical Sciences\",\"volume\":\"28 1\",\"pages\":\"105-114\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2019-12-22\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"8\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Iraqi Journal of Pharmaceutical Sciences\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.31351/vol28iss2pp105-114\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q3\",\"JCRName\":\"Pharmacology, Toxicology and Pharmaceutics\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Iraqi Journal of Pharmaceutical Sciences","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.31351/vol28iss2pp105-114","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q3","JCRName":"Pharmacology, Toxicology and Pharmaceutics","Score":null,"Total":0}
引用次数: 8
摘要
阿托伐他汀(ATR)是一种难溶性抗高脂血症药物;根据生物制药分类系统(BCS),它属于II类,由于其溶解度低,生物利用度低。固体分散体吸附是提高难溶性药物溶解度和溶出度的有效技术。本研究旨在通过与普通固体分散体相比,采用固体分散体吸附技术提高ATR的溶解度和溶解速率。以聚乙二醇4000 (PEG 4000)、聚乙二醇6000 (PEG 6000)、Poloxamer188和poloxamer407为亲水性载体,以Aerosil 200、Aerosil 300和硅酸铝镁(MAS)为吸附剂。采用x射线粉末衍射(XRD)、差示扫描量热法(DSC)和傅里叶变换红外光谱(FTIR)测定药物载体与吸附物的相互作用,对固体分散吸附物(SDA)配方的水溶性、产率、药物含量、溶出度、晶体结构进行了评价。所制备的SDA在各制剂中的溶解度均有显著提高。以SDA12(ATR:Poloxamer407: MAS 1:1:1)为最佳配方,其溶解度比纯ATR和固体分散体(SD4)(阿托伐他汀:Poloxamer407 1:1)分别提高了8.07倍和5.38倍,这是由于药物的润湿性增加,结晶度降低,从而提高了药物的溶解度和溶出度。
Solubility and Dissolution Enhancement of Atorvastatin Calcium using Solid Dispersion Adsorbate Technique
Atorvastatin (ATR) is poorly soluble anti-hyperlipidemic drug; it belongs to the class II group according to the biopharmaceutical classification system (BCS) with low bioavailability due to its low solubility. Solid dispersions adsorbate is an effective technique for enhancing the solubility and dissolution of poorly soluble drugs.
The present study aims to enhance the solubility and dissolution rate of ATR using solid dispersion adsorption technique in comparison with ordinary solid dispersion. polyethylene glycol 4000 (PEG 4000), polyethylene glycol 6000 (PEG 6000), Poloxamer188 and Poloxamer 407were used as hydrophilic carriers and Aerosil 200, Aerosil 300 and magnesium aluminium silicate (MAS) as adsorbents.
All solid dispersion adsorbate (SDA) formulas were prepared in ratios of 1:1:1 (drug: carrier: adsorbent) and evaluated for their water solubility, percentage yield, drug content, , dissolution, crystal structure using X-ray powder diffraction (XRD) and Differential Scanning Calorimetry (DSC) studies and Fourier Transform Infrared Spectroscopy (FTIR) for determination the drug-carrier- adsorbate interaction.
The prepared (SDA) showed significant improvement of drug solubility in all prepared formula. Best result was obtained with formula SDA12(ATR :Poloxamer407 : MAS 1:1:1) that showed 8.07 and 5.38
fold increase in solubility compared to solubility of pure ATR and solid dispersion(SD4) (Atorvastatin: Poloxamer 407 1:1) respectively due to increased wettability and reduced crystallinity of the drug which leads to improve drug solubility and dissolution .