Prediction of drug concentrations in humans for long-acting injectable suspensions by a semi-mechanical muscle compartment model: a case study of paliperidone palmitate

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Publicat a:Frontiers in Pharmacology vol. 16 (Jul 2025), p. 1507828-1507840
Autor principal: Yu, Panpan
Altres autors: Zhang, Mengjun, Xiong, Jin, Wu, Keheng, Long, Sihui, Cheng, Shishi, Long, Fu, Xu, Xiao, Liu, Jie, Liu, Dan, Li, Xue, Liu, Bo, Xu, Jian
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Frontiers Media SA
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100 1 |a Yu, Panpan  |u Livzon Pharmaceutical Group Inc., Livzon Corporate, Zhuhai, Guangdong, China 
245 1 |a Prediction of drug concentrations in humans for long-acting injectable suspensions by a semi-mechanical muscle compartment model: a case study of paliperidone palmitate 
260 |b Frontiers Media SA  |c Jul 2025 
513 |a Case Study 
520 3 |a Long-acting injectable formulations, such as paliperidone palmitate extended-release injectable suspension, have been designed to release medicines slowly and sustainably. Developing models that simulate drug release from long-acting injectable formulations in vivo is challenging. A novel approach to modeling and simulating complex and multiphasic drug pharmacokinetics (PK) is provided in this article to facilitate development of long-acting formulations. By segmenting nanocrystalline particles according to their different sizes, the absorption delays of each segment were obtained from the results of the PK study in dogs. In addition to the lag time for each segment, all other parameters, including physicochemical parameters such as drug solubility, density and diffusion coefficient, as well as pharmacokinetic parameters related to clearance, elimination and distribution, were introduced into the model to establish a muscle compartment model for use in humans. By using this model, the injectable suspensions paliperidone samples were predicted to have a long release of 90–100 days in vivo . 
653 |a Diffusion coefficient 
653 |a Dissolution 
653 |a Pharmacokinetics 
653 |a Physicochemical properties 
653 |a Drug development 
653 |a Nanocrystals 
653 |a Computer simulation 
653 |a Particle size 
653 |a Anticoagulants 
653 |a Metabolism 
653 |a Palmitic acid 
653 |a Dogs 
653 |a Drug dosages 
700 1 |a Zhang, Mengjun  |u School of Chemical Engineering and Pharmacy, Wuhan Institute of Technology, Wuhan, China 
700 1 |a Xiong, Jin  |u School of Chemical Engineering and Pharmacy, Wuhan Institute of Technology, Wuhan, China 
700 1 |a Wu, Keheng  |u Yinghan Pharmaceutical Technology (Shanghai) Co., Ltd., Shanghai, China 
700 1 |a Long, Sihui  |u School of Chemical Engineering and Pharmacy, Wuhan Institute of Technology, Wuhan, China 
700 1 |a Cheng, Shishi  |u Yinghan Pharmaceutical Technology (Shanghai) Co., Ltd., Shanghai, China 
700 1 |a Long, Fu  |u Livzon Pharmaceutical Group Inc., Livzon Corporate, Zhuhai, Guangdong, China 
700 1 |a Xu, Xiao  |u Livzon Pharmaceutical Group Inc., Livzon Corporate, Zhuhai, Guangdong, China 
700 1 |a Liu, Jie  |u Livzon Pharmaceutical Group Inc., Livzon Corporate, Zhuhai, Guangdong, China 
700 1 |a Liu, Dan  |u Yinghan Pharmaceutical Technology (Shanghai) Co., Ltd., Shanghai, China 
700 1 |a Li, Xue  |u Yinghan Pharmaceutical Technology (Shanghai) Co., Ltd., Shanghai, China 
700 1 |a Liu, Bo  |u School of Chemical Engineering and Pharmacy, Wuhan Institute of Technology, Wuhan, China 
700 1 |a Xu, Jian  |u Livzon Pharmaceutical Group Inc., Livzon Corporate, Zhuhai, Guangdong, China 
773 0 |t Frontiers in Pharmacology  |g vol. 16 (Jul 2025), p. 1507828-1507840 
786 0 |d ProQuest  |t Biological Science Database 
856 4 1 |3 Citation/Abstract  |u https://www.proquest.com/docview/3279098064/abstract/embedded/L8HZQI7Z43R0LA5T?source=fedsrch 
856 4 0 |3 Full Text  |u https://www.proquest.com/docview/3279098064/fulltext/embedded/L8HZQI7Z43R0LA5T?source=fedsrch 
856 4 0 |3 Full Text - PDF  |u https://www.proquest.com/docview/3279098064/fulltextPDF/embedded/L8HZQI7Z43R0LA5T?source=fedsrch