{"title":"用无定形固体分散技术解决研发阶段的药物制剂问题","authors":"Devika Tripathi, Manjunatha Prabhu B.H, Jagannath Sahoo, Jyoti Kumari","doi":"10.2174/0126673878271641231201065151","DOIUrl":null,"url":null,"abstract":"\n\nAmorphous Solid Dispersions (ASDs) have indeed revolutionized the pharmaceutical industry, particularly in drug solubility enhancement. The amorphous state of a drug, which is a highenergy metastable state, can lead to an increase in the apparent solubility of the drug. This is due to\nthe absence of a long-range molecular order, which results in higher molecular mobility and free\nvolume, and consequently, higher solubility. The success of ASD preparation depends on the selection of appropriate excipients, particularly polymers that play a crucial role in drug solubility and\nphysical stability. However, ASDs face challenges due to their thermodynamic instability or tendency to recrystallize. Measuring the crystallinity of the active pharmaceutical ingredient (API) and\ndrug solubility is a complex process that requires a thorough understanding of drug-polymer miscibility and molecular interactions. Therefore, it is important to monitor drug solids closely during\npreparation, storage, and application. Techniques such as solid-state nuclear magnetic resonance\n(ssNMR), attenuated total reflectance Fourier transform infrared spectroscopy (ATR-FTIR), Raman\nspectroscopy, and dielectric spectroscopy have been successful in understanding the mechanism of\ndrug crystallization. In addition, the continuous downstream processing of drug-loaded ASDs has\nintroduced new automated methods for consistent ASD production. Advanced techniques such as\nhot melt extrusion, KinetiSol, electro spraying, and electrospinning have gained popularity. This review provides a comprehensive overview of Amorphous Solid Dispersions (ASDs) for oral drug delivery. It highlights the critical challenges faced during formulation, the impact of manufacturing\nvariables, theoretical aspects of drug-polymer interaction, and factors related to drug-polymer miscibility. ASDs have been recognized as a promising strategy to improve the oral bioavailability of\npoorly water-soluble drugs. However, the successful development of an ASD-based drug product is\nnot straightforward due to the complexity of the ASD systems. The formulation and process parameters can significantly influence the performance of the final product. Understanding the interactions between the drug and polymer in ASDs is crucial for predicting their stability and performance.\n","PeriodicalId":20955,"journal":{"name":"Recent advances in drug delivery and formulation","volume":null,"pages":null},"PeriodicalIF":0.0000,"publicationDate":"2023-12-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Navigating the Solution to Drug Formulation Problems at Research and\\nDevelopment Stages by Amorphous Solid Dispersion Technology\",\"authors\":\"Devika Tripathi, Manjunatha Prabhu B.H, Jagannath Sahoo, Jyoti Kumari\",\"doi\":\"10.2174/0126673878271641231201065151\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"\\n\\nAmorphous Solid Dispersions (ASDs) have indeed revolutionized the pharmaceutical industry, particularly in drug solubility enhancement. The amorphous state of a drug, which is a highenergy metastable state, can lead to an increase in the apparent solubility of the drug. This is due to\\nthe absence of a long-range molecular order, which results in higher molecular mobility and free\\nvolume, and consequently, higher solubility. The success of ASD preparation depends on the selection of appropriate excipients, particularly polymers that play a crucial role in drug solubility and\\nphysical stability. However, ASDs face challenges due to their thermodynamic instability or tendency to recrystallize. Measuring the crystallinity of the active pharmaceutical ingredient (API) and\\ndrug solubility is a complex process that requires a thorough understanding of drug-polymer miscibility and molecular interactions. Therefore, it is important to monitor drug solids closely during\\npreparation, storage, and application. Techniques such as solid-state nuclear magnetic resonance\\n(ssNMR), attenuated total reflectance Fourier transform infrared spectroscopy (ATR-FTIR), Raman\\nspectroscopy, and dielectric spectroscopy have been successful in understanding the mechanism of\\ndrug crystallization. In addition, the continuous downstream processing of drug-loaded ASDs has\\nintroduced new automated methods for consistent ASD production. Advanced techniques such as\\nhot melt extrusion, KinetiSol, electro spraying, and electrospinning have gained popularity. This review provides a comprehensive overview of Amorphous Solid Dispersions (ASDs) for oral drug delivery. It highlights the critical challenges faced during formulation, the impact of manufacturing\\nvariables, theoretical aspects of drug-polymer interaction, and factors related to drug-polymer miscibility. ASDs have been recognized as a promising strategy to improve the oral bioavailability of\\npoorly water-soluble drugs. However, the successful development of an ASD-based drug product is\\nnot straightforward due to the complexity of the ASD systems. The formulation and process parameters can significantly influence the performance of the final product. Understanding the interactions between the drug and polymer in ASDs is crucial for predicting their stability and performance.\\n\",\"PeriodicalId\":20955,\"journal\":{\"name\":\"Recent advances in drug delivery and formulation\",\"volume\":null,\"pages\":null},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2023-12-07\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Recent advances in drug delivery and formulation\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.2174/0126673878271641231201065151\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Recent advances in drug delivery and formulation","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.2174/0126673878271641231201065151","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
Navigating the Solution to Drug Formulation Problems at Research and
Development Stages by Amorphous Solid Dispersion Technology
Amorphous Solid Dispersions (ASDs) have indeed revolutionized the pharmaceutical industry, particularly in drug solubility enhancement. The amorphous state of a drug, which is a highenergy metastable state, can lead to an increase in the apparent solubility of the drug. This is due to
the absence of a long-range molecular order, which results in higher molecular mobility and free
volume, and consequently, higher solubility. The success of ASD preparation depends on the selection of appropriate excipients, particularly polymers that play a crucial role in drug solubility and
physical stability. However, ASDs face challenges due to their thermodynamic instability or tendency to recrystallize. Measuring the crystallinity of the active pharmaceutical ingredient (API) and
drug solubility is a complex process that requires a thorough understanding of drug-polymer miscibility and molecular interactions. Therefore, it is important to monitor drug solids closely during
preparation, storage, and application. Techniques such as solid-state nuclear magnetic resonance
(ssNMR), attenuated total reflectance Fourier transform infrared spectroscopy (ATR-FTIR), Raman
spectroscopy, and dielectric spectroscopy have been successful in understanding the mechanism of
drug crystallization. In addition, the continuous downstream processing of drug-loaded ASDs has
introduced new automated methods for consistent ASD production. Advanced techniques such as
hot melt extrusion, KinetiSol, electro spraying, and electrospinning have gained popularity. This review provides a comprehensive overview of Amorphous Solid Dispersions (ASDs) for oral drug delivery. It highlights the critical challenges faced during formulation, the impact of manufacturing
variables, theoretical aspects of drug-polymer interaction, and factors related to drug-polymer miscibility. ASDs have been recognized as a promising strategy to improve the oral bioavailability of
poorly water-soluble drugs. However, the successful development of an ASD-based drug product is
not straightforward due to the complexity of the ASD systems. The formulation and process parameters can significantly influence the performance of the final product. Understanding the interactions between the drug and polymer in ASDs is crucial for predicting their stability and performance.