Article
Polymer Science
Kinga Biedrzycka, Agnieszka Marcinkowska
Summary: In this study, the hot melt extrusion method was used to obtain an amorphous dispersion of an active pharmaceutical ingredient (API) that is sparingly soluble in water. The extrusion conditions included a screw rotation speed of 250 rpm, temperature above 100°C, and two mixing zones. The use of Eudragit EPO as a polymer matrix and ibuprofen as an API was investigated. The addition of the plasticizer Compritol 888 ATO improved processing parameters and modified the release profile of ibuprofen. The obtained solid dispersions showed good stability and released about 40% to 63% of the API within 180 minutes.
Article
Pharmacology & Pharmacy
Khater AL-Japairai, Samah Hamed Almurisi, Syed Mahmood, Thiagarajan Madheswaran, Bappaditya Chatterjee, Prasanthi Sri, Nadiatul Azra Binti Ahmad Mazlan, Turki Al Hagbani, Fawaz Alheibshy
Summary: Oral administration of drugs is preferred for being non-invasive, easy to administer, and easy to store. However, the poor solubility of drugs in oral formulations limits their effectiveness and commercial value. Amorphous solid dispersion (ASD), a method that changes the molecular structure of drugs to improve solubility, is being used with the emerging hot melt extrusion (HME) method in the pharmaceutical industry. Despite solving solubility issues, ASD also poses a risk of crystallization, requiring optimization in formulation, polymers, and HME manufacturing processes.
INTERNATIONAL JOURNAL OF PHARMACEUTICS
(2023)
Article
Pharmacology & Pharmacy
Jiawei Han, Mengyuan Tang, Yang Yang, Wen Sun, Zhimin Yue, Yunran Zhang, Yijun Zhu, Xiaoqian Liu, Jue Wang
Summary: This review discusses the use of solid dispersion systems as an effective formulation strategy to enhance the performance of poorly water-soluble drugs. It provides a comprehensive understanding of SD classification and highlights the most popular amorphous solid dispersions. Furthermore, it proposes a systematic design strategy for satisfactory ASDs and explores the application of hot melt extrusion as a continuous manufacturing technique.
INTERNATIONAL JOURNAL OF PHARMACEUTICS
(2023)
Article
Medicine, Research & Experimental
Stephen A. Thompson, Daniel A. Jr Jr Davis, Chaeho Moon, Robert O. I. I. I. I. I. I. Williams
Summary: Maximizing the drug loading of pH-dependent APIs in amorphous solid dispersions (ASDs) produced by hot-melt extrusion (HME) can reduce pill burden without compromising dissolution performance. By incorporating bases to modify pH during HME, the drug loading (w/w) of telmisartan in ASDs was significantly increased from 5% to 50%. The stability of the polymer Soluplus when extruded with a strong base was also examined.
MOLECULAR PHARMACEUTICS
(2022)
Article
Pharmacology & Pharmacy
Abdullah Alshetaili, Bjad K. Almutairy, Sultan M. Alshehri, Michael A. Repka
Summary: This study aimed to develop a sustained release formulation of donepezil hydrochloride (DH) using the hot-melt extruded solid dispersion technique. By rational screening of hydrophobic carriers, the release profile of DH was successfully modified, and a preferable release pattern was obtained by optimizing the ratio of carriers and pore-forming agents as well as the extrusion temperature profile.
Article
Pharmacology & Pharmacy
Abdulmajeed A. Althobaiti, Eman A. Ashour, Mashan Almutairi, Ahmed Almotairy, Mohammed Al Yahya, Michael A. Repka
Summary: Curcumin, derived from turmeric, has various biological activities. This study successfully prepared curcumin-piperine solid dispersion using the hot-melt extrusion technique, resulting in significant improvement in the release profile of curcumin.
JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
(2022)
Article
Pharmacology & Pharmacy
Yongjun Li, Amanda K. P. Mann, Dan Zhang, Zhen Yang
Summary: This study compared the effects of hot-melt extrusion and spray drying on drug bioperformance, finding significant differences in in vitro drug release rates of the amorphous solid dispersions produced by the two methods, while demonstrating similar in vivo performance based on cynomolgus monkey PK studies. Mechanistic understanding of the behaviors of the solid dispersions in vitro and in vivo was discussed.
Article
Pharmacology & Pharmacy
Naho Hanada, Kenjirou Higashi, Zhijing Zhao, Keisuke Ueda, Kunikazu Moribe
Summary: Ternary amorphous solid dispersions (ASDs) of probucol (PBC)/polymer/surfactant were successfully prepared by hot-melt extrusion method. The ASDs stabilized amorphous PBC mainly through hydrogen bonds formed between PBC and the polymer (PVP). Colloidal dispersions of amorphous PBC nanoparticles were obtained from the ASD using a weight ratio of 1:4:2 for PBC/PVP/P407, and the stability of the amorphous state was confirmed through storage experiments.
INTERNATIONAL JOURNAL OF PHARMACEUTICS
(2023)
Article
Biochemistry & Molecular Biology
Wenjing Zhu, Wenling Fan, Xiaotong Zhang, Meiqi Gao
Summary: This study successfully prepared a sustained-release solid dispersion of poorly water-soluble resveratrol using hot melt extrusion. The formulation with a specific polymeric blend was able to control the release of resveratrol. The optimized solid dispersion showed good sustained release effect, increased solubility, and improved bioavailability.
Article
Chemistry, Medicinal
Bhupendra Raj Giri, Jaewook Kwon, Anh Q. Vo, Ajinkya M. Bhagurkar, Suresh Bandari, Dong Wuk Kim
Summary: This study successfully enhanced the solubility, bioavailability, and stability of the antihypertensive drug Telmisartan through the fabrication of a pH-modulated solid dispersion using hot-melt extrusion technology. The optimized formulation showed significantly improved drug release profile, better stability, and superior pharmacokinetic parameters in rat studies.
Article
Biochemistry & Molecular Biology
Wenling Fan, Jiali Wu, Meiqi Gao, Xiaotong Zhang, Wenjing Zhu
Summary: The aim of this study was to improve the solubility, bioavailability, and stability of resveratrol (RES-SD) Solid Dispersion in Polygonum cuspidatum extract (PCE) by hot melt extrusion (HME). The optimum formula was selected by single factor design and orthogonal test, and it was found that PCE-SD increased the dissolution of RES and its oral bioavailability. The auxiliary substances in Polygonum cuspidatum extract had an influence on its preparation technology, stability, and bioavailability.
Article
Pharmacology & Pharmacy
Phuong H. L. Tran, Beom-Jin Lee, Thao T. D. Tran
Summary: Hot-melt extrusion is a promising method for the preparation of drug delivery systems on an industrial scale, but there is still a lack of research on its recent progress and influencing factors. This review discusses the effects of hot-melt extrusion on various factors in solid dispersion systems and describes the use of molecular interactions to improve drug stability.
EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS
(2021)
Article
Polymer Science
Jiale Li, Conghui Li, Hui Zhang, Xiang Gao, Ting Wang, Zengming Wang, Aiping Zheng
Summary: In this study, hot-melt extrusion was used to prepare azithromycin amorphous solid dispersion, solving the issues of bitter taste and low solubility. The selection of a suitable polymer was based on solubility parameter calculations, and the formulation and process were optimized using design of experiments.
Article
Pharmacology & Pharmacy
Daniel Kramarczyk, Justyna Knapik-Kowalczuk, Mateusz Kurek, Witold Jamroz, Renata Jachowicz, Marian Paluch
Summary: In this study, the effectiveness of different polymers in creating posaconazole-based amorphous solid dispersions (ASDs) was examined. It was found that the use of an amorphous homopolymer-K30 was the most effective additive in improving the aqueous solubility and physical stability of the drug.
Article
Pharmacology & Pharmacy
Amit Chivate, Atul Garkal, Kartik Hariharan, Tejal Mehta
Summary: Kollicoat (R) Smartseal has the potential to improve the pharmacokinetics of high melting point drugs like Itraconazole as a carrier, exhibiting good thermoplastic behavior and plasticizing effect, resulting in significantly enhanced solubility. This offers a new option for the development of formulations in the industry.
JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
(2021)
Article
Pharmacology & Pharmacy
Ajinkya M. Bhagurkar, Muralikrishnan Angamuthu, Hemlata Patil, Roshan V. Tiwari, Abhijeet Maurya, Seyed Meysam Hashemnejad, Santanu Kundu, S. Narasimha Murthy, Michael A. Repka
Review
Pharmacology & Pharmacy
Hemlata Patil, Roshan V. Tiwari, Michael A. Repka
Article
Pharmacology & Pharmacy
Parash Parajuli, Roshan Vijay Tiwari, Paul William Sylvester
BIOLOGICAL & PHARMACEUTICAL BULLETIN
(2015)
Article
Cell Biology
P. Parajuli, R. V. Tiwari, P. W. Sylvester
CELL PROLIFERATION
(2015)
Article
Pharmacology & Pharmacy
Hemlata Patil, Roshan V. Tiwari, Sampada B. Upadhye, Ronald S. Vladyka, Michael A. Repka
INTERNATIONAL JOURNAL OF PHARMACEUTICS
(2015)
Article
Pharmacology & Pharmacy
Bader B. Alsulays, Jun-Born Park, Sultan M. Alshehri, Joseph T. Morott, Saad M. Alshahrani, Roshan V. Tiwari, Abdullah S. Alshetaili, Soumyajit Majumdar, Nigel Langley, Karl Kolter, Andreas Gryczke, Michael A. Repka
JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
(2015)
Article
Pharmacology & Pharmacy
Sultan M. Alshehri, Jun-Bom Park, Bader B. Alsulays, Roshan V. Tiwari, Bjad Almutairy, Abdullah S. Alshetaili, Joseph Morott, Sejal Shah, Vijay Kulkarni, Soumyajit Majumdar, Scott T. Martin, Sanjay Mishra, Lijia Wang, Michael A. Repka
JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
(2015)
Article
Veterinary Sciences
Haiying Nie, Xin Feng, Jianbo Peng, Liu Liang, Chunyan Lu, Roshan V. Tiwari, Shusheng Tang, Jiakang He
AMERICAN JOURNAL OF VETERINARY RESEARCH
(2016)
Article
Pharmacology & Pharmacy
Anh Q. Vo, Xin Feng, Joseph T. Morott, Manjeet B. Pimparade, Roshan V. Tiwari, Feng Zhang, Michael A. Repka
EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS
(2016)
Review
Pharmacology & Pharmacy
Hemlata Patil, Roshan V. Tiwari, Michael A. Repka
JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
(2016)
Article
Engineering, Biomedical
Santosh Shelke, Sadhana Shahi, Kiran Jadhav, Dinesh Dhamecha, Roshan Tiwari, Hemlata Patil
JOURNAL OF MATERIALS SCIENCE-MATERIALS IN MEDICINE
(2016)
Review
Biochemistry & Molecular Biology
Paul W. Sylvester, Mohamed R. Akl, Abhita Malaviya, Parash Parajuli, Suryatheja Ananthula, Roshan V. Tiwari, Nehad M. Ayoub
Article
Medicine, Research & Experimental
Roshan V. Tiwari, Parash Parajuli, Paul W. Sylvester
EXPERIMENTAL BIOLOGY AND MEDICINE
(2014)
Article
Chemistry, Medicinal
B. K. Almutairy, A. S. Alshetaili, E. A. Ashour, H. Patil, R. V. Tiwari, S. M. Alshehri, M. A. Repka