Journal of pharmaceutical sciences最新文献

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How the Magenstrasse is formed after meals: Protein aggregation hypothesis Magenstrasse是如何在饭后形成的:蛋白质聚集假说。
IF 3.7 3区 医学
Journal of pharmaceutical sciences Pub Date : 2025-02-01 DOI: 10.1016/j.xphs.2024.12.008
Ryosuke Sakai , Yoshiyuki Shirasaka , Taiyo Takagi , Takato Masada , Keiko Minami , Makoto Kataoka , Ikumi Tamai , Toshihide Takagi , Shinji Yamashita
{"title":"How the Magenstrasse is formed after meals: Protein aggregation hypothesis","authors":"Ryosuke Sakai ,&nbsp;Yoshiyuki Shirasaka ,&nbsp;Taiyo Takagi ,&nbsp;Takato Masada ,&nbsp;Keiko Minami ,&nbsp;Makoto Kataoka ,&nbsp;Ikumi Tamai ,&nbsp;Toshihide Takagi ,&nbsp;Shinji Yamashita","doi":"10.1016/j.xphs.2024.12.008","DOIUrl":"10.1016/j.xphs.2024.12.008","url":null,"abstract":"<div><div>Magenstrasse (stomach road) is reported to potentially influence the absorption of orally administered drugs by facilitating a gastric emptying of ingested water under postprandial condition. We hypothesized the Magenstrasse is a consequence of the formation of protein aggregates due to the decrease in gastric pH associated with stimulated gastric acid secretion. The formation mechanism of the Magenstrasse was examined <em>in vitro</em> using a gastric chamber system which reproduces postprandial conditions in the stomach. Oral liquid meals containing different amounts of proteins were mixed with simulated gastric fluid containing pepsin in the gastric chamber. When a high-protein liquid meal was used, infusion of gastric acid caused protein denaturation, generating semisolid aggregates. Then, to evaluate the impact of the aggregates, fluorescein isothiocyanate-dextran 4000 (FD-4) solution was added. The presence of protein aggregates facilitated the elution of FD-4 from the gastric chamber, indicating that the semisolid aggregates suppressed mixing of FD-4 solution with meals. In addition, formation of the same type of protein aggregates was observed <em>in vivo</em> in rat stomach after ingesting a high-protein liquid meal. These <em>in vitro</em> and <em>in vivo</em> results support the idea that protein aggregation of liquid meals in the stomach contributes the formation of the Magenstrasse.</div></div>","PeriodicalId":16741,"journal":{"name":"Journal of pharmaceutical sciences","volume":"114 2","pages":"Pages 1351-1358"},"PeriodicalIF":3.7,"publicationDate":"2025-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142864624","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Review on macromolecule-based magnetic theranostic agents for biomedical applications: Targeted therapy and diagnostic imaging 高分子磁性治疗剂在生物医学中的应用综述:靶向治疗和诊断成像。
IF 3.7 3区 医学
Journal of pharmaceutical sciences Pub Date : 2025-02-01 DOI: 10.1016/j.xphs.2024.11.031
Laila S. Zeid , Heba A. El-Masry , Hend H. Mohamed , Amira Hathout , Ahmed S. Younes , Aya A. El-kholy , Aya Ashraf Muhammad Abdel Hamid , Naira Ali Abd Elaziz , Fatma Shaban Hafez , May Emad Eldin Mostafa , Islam M.M. Omar , Tasneem Elsayed Ahmed , Mohamed S.A. Darwish
{"title":"Review on macromolecule-based magnetic theranostic agents for biomedical applications: Targeted therapy and diagnostic imaging","authors":"Laila S. Zeid ,&nbsp;Heba A. El-Masry ,&nbsp;Hend H. Mohamed ,&nbsp;Amira Hathout ,&nbsp;Ahmed S. Younes ,&nbsp;Aya A. El-kholy ,&nbsp;Aya Ashraf Muhammad Abdel Hamid ,&nbsp;Naira Ali Abd Elaziz ,&nbsp;Fatma Shaban Hafez ,&nbsp;May Emad Eldin Mostafa ,&nbsp;Islam M.M. Omar ,&nbsp;Tasneem Elsayed Ahmed ,&nbsp;Mohamed S.A. Darwish","doi":"10.1016/j.xphs.2024.11.031","DOIUrl":"10.1016/j.xphs.2024.11.031","url":null,"abstract":"<div><div>Clinical diagnostics and biological research are advanced by magnetic theranostic, which uses macromolecule-based magnetic theranostic agents for targeted therapy and diagnostic imaging. Within this review, the interaction of magnetic nanoparticles (MNPs) with biological macromolecules will be covered. The exciting potential of macromolecule-based magnetic theranostic agents to be used as a tool in drug delivery, photothermally therapy (PTT), gene therapy, hyperthermia therapy and photodynamic therapy (PDT) will be discussed. Innovative imaging technique: magnetic resonance imaging (MRI), magnetic particle imaging (MPI), fluorescence scanning, and photoacoustic scanning are revolutionizing biological diagnosis by potentially overcoming historical limitations. This review will cover the challenge of fabricating of macromolecule-based magnetic theranostic agents as a promising platform for theranostic that can combine therapies with diagnostics at subcellular level. Additionally, it looks at several chemical pathways leading to the process for generating MNPs, including the co-precipitation, the sol-gel, the hydrothermal synthesis, the polyol route, and the microemulsion technique. Eventually, the demands and prospects for magnetic theranostic are discussed, focusing on the requirement of further investigation to improve MNP structure towards biocompatible material and translation of these promising theranostic agents into clinical applications.</div></div>","PeriodicalId":16741,"journal":{"name":"Journal of pharmaceutical sciences","volume":"114 2","pages":"Pages 787-804"},"PeriodicalIF":3.7,"publicationDate":"2025-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142877501","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Editorial Advisory Board
IF 3.7 3区 医学
Journal of pharmaceutical sciences Pub Date : 2025-02-01 DOI: 10.1016/S0022-3549(25)00054-1
{"title":"Editorial Advisory Board","authors":"","doi":"10.1016/S0022-3549(25)00054-1","DOIUrl":"10.1016/S0022-3549(25)00054-1","url":null,"abstract":"","PeriodicalId":16741,"journal":{"name":"Journal of pharmaceutical sciences","volume":"114 2","pages":"Pages A2-A4"},"PeriodicalIF":3.7,"publicationDate":"2025-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143430255","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Outstanding early career scientists for 2024
IF 3.7 3区 医学
Journal of pharmaceutical sciences Pub Date : 2025-02-01 DOI: 10.1016/j.xphs.2024.11.010
Kenneth L. Audus
{"title":"Outstanding early career scientists for 2024","authors":"Kenneth L. Audus","doi":"10.1016/j.xphs.2024.11.010","DOIUrl":"10.1016/j.xphs.2024.11.010","url":null,"abstract":"","PeriodicalId":16741,"journal":{"name":"Journal of pharmaceutical sciences","volume":"114 2","pages":"Page 641"},"PeriodicalIF":3.7,"publicationDate":"2025-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143430256","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Spray drying process challenges and considerations for inhaled biologics 吸入生物制剂喷雾干燥工艺的挑战和考虑-综述。
IF 3.7 3区 医学
Journal of pharmaceutical sciences Pub Date : 2025-02-01 DOI: 10.1016/j.xphs.2024.11.028
Sadegh Poozesh , Patrick Connaughton , Scott Sides , David Lechuga-Ballesteros , Sajal M. Patel , Prakash Manikwar
{"title":"Spray drying process challenges and considerations for inhaled biologics","authors":"Sadegh Poozesh ,&nbsp;Patrick Connaughton ,&nbsp;Scott Sides ,&nbsp;David Lechuga-Ballesteros ,&nbsp;Sajal M. Patel ,&nbsp;Prakash Manikwar","doi":"10.1016/j.xphs.2024.11.028","DOIUrl":"10.1016/j.xphs.2024.11.028","url":null,"abstract":"<div><div>Spray drying presents numerous advantages over other drying technologies, particularly for inhaled biologics because of the fine-tuned particle attributes requirements. To fully leverage these benefits, it is crucial to address several process challenges and considerations throughout the end-to-end spray-drying process, including stages prior to, during, and post- drying. This review provides a detailed overview of the challenges associated with spray-drying of biologics along with the aspects of protein degradation. Furthermore, it delineates the entire spray-drying process, comprising feed solution preparation, spray drying, and bulk powder handling, along with protein degradation mechanisms and analytical tools for protein and aerosol performance assessment. Pertaining to inhaled biologic products, this review also sheds light on major bottlenecks and potential challenges, particularly during scale-up. While some challenges are yet to be conclusively addressed, potential control and mitigation strategies from industry perspective are presented and examined. Lastly, the review briefly explores trending topics in this field that could add value to the standard spray-drying process and may be incorporated in future drying technologies.</div></div>","PeriodicalId":16741,"journal":{"name":"Journal of pharmaceutical sciences","volume":"114 2","pages":"Pages 766-781"},"PeriodicalIF":3.7,"publicationDate":"2025-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142854442","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Computer modeling of bevacizumab drug distribution after intravitreal injection in rabbit and human eyes 兔和人眼玻璃体内注射贝伐单抗后药物分布的计算机模拟。
IF 3.7 3区 医学
Journal of pharmaceutical sciences Pub Date : 2025-02-01 DOI: 10.1016/j.xphs.2024.12.005
Jabia M. Chowdhury , Eduardo A. Chacin Ruiz , Matthew P. Ohr , Katelyn E. Swindle-Reilly , Ashlee N. Ford Versypt
{"title":"Computer modeling of bevacizumab drug distribution after intravitreal injection in rabbit and human eyes","authors":"Jabia M. Chowdhury ,&nbsp;Eduardo A. Chacin Ruiz ,&nbsp;Matthew P. Ohr ,&nbsp;Katelyn E. Swindle-Reilly ,&nbsp;Ashlee N. Ford Versypt","doi":"10.1016/j.xphs.2024.12.005","DOIUrl":"10.1016/j.xphs.2024.12.005","url":null,"abstract":"<div><div>Age-related macular degeneration (AMD) is a progressive eye disease that causes loss of central vision and has no cure. Wet AMD is the late neovascular form treated with vascular endothelial growth factor (VEGF) inhibitors. VEGF is the critical driver of wet AMD. One common off-label anti-VEGF drug used in AMD treatment is bevacizumab. Experimental efforts have been made to investigate the pharmacokinetic (PK) behavior of bevacizumab in vitreous and aqueous humor. Still, the quantitative effect of elimination routes and drug concentration in the macula are not well understood. In this work, we developed two spatial models representing rabbit and human vitreous to better understand the PK behavior of bevacizumab. This study explores different cases of drug elimination and the effects of injection location on drug concentration profiles. The models are validated by comparing them with experimental data. Our results suggest that anterior elimination is dominant for bevacizumab clearance from rabbit vitreous, whereas both anterior and posterior elimination have similar importance in drug clearance from the human vitreous. Furthermore, results indicate that drug injections closer to the posterior segment of the vitreous help maintain relevant drug concentrations for longer, improving bevacizumab duration of action in the vitreous. The rabbit and human models predict bevacizumab concentration in the vitreous and fovea, enhancing knowledge and understanding of wet AMD treatment.</div></div>","PeriodicalId":16741,"journal":{"name":"Journal of pharmaceutical sciences","volume":"114 2","pages":"Pages 1164-1174"},"PeriodicalIF":3.7,"publicationDate":"2025-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142854459","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Enhancing physicochemical properties of hydrochlorothiazide with zwitterionic L-proline and 5-fluorocytosine cocrystals through mechanochemical synthesis 双阴离子l -脯氨酸和5-氟胞嘧啶共晶机械合成提高氢氯噻嗪的理化性能。
IF 3.7 3区 医学
Journal of pharmaceutical sciences Pub Date : 2025-02-01 DOI: 10.1016/j.xphs.2024.12.004
Pollyana Pereira Firmino , Cecilia Carolina Pinheiro da Silva , Paulo Nunes , José Eduardo Gonçalves , Fabrizia Grepioni , Javier Ellena
{"title":"Enhancing physicochemical properties of hydrochlorothiazide with zwitterionic L-proline and 5-fluorocytosine cocrystals through mechanochemical synthesis","authors":"Pollyana Pereira Firmino ,&nbsp;Cecilia Carolina Pinheiro da Silva ,&nbsp;Paulo Nunes ,&nbsp;José Eduardo Gonçalves ,&nbsp;Fabrizia Grepioni ,&nbsp;Javier Ellena","doi":"10.1016/j.xphs.2024.12.004","DOIUrl":"10.1016/j.xphs.2024.12.004","url":null,"abstract":"<div><div>Hydrochlorothiazide (HTZ) is a thiazide-type diuretic drug approved by the FDA in 1959 for treatment of hypertension and peripheral edema and has been used since. HTZ exhibits low solubility and low permeability, leading to variable oral bioavailability and limited intestinal drug permeability. For this reason, several attempts to improve HTZ physicochemical properties have been made during the past decades. In the broad frame of molecular crystal engineering, significant efforts and promising results in the quest for more effective solid/dosage forms of HTZ, including studies on polymorphism and cocrystals, are being developed. As part of these efforts, we report here two new cocrystals of HTZ with the zwitterionic <span>l</span>-proline and the prodrug 5-Fluorocytosine. Both cocrystals show improvement in solubility and permeability, suggesting that these new solid forms could be used as new drug candidates to deliver HTZ in the antihypertensive therapy.</div></div>","PeriodicalId":16741,"journal":{"name":"Journal of pharmaceutical sciences","volume":"114 2","pages":"Pages 1152-1163"},"PeriodicalIF":3.7,"publicationDate":"2025-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142877493","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
The vital role of biological standardization in ensuring efficacy and safety of biological products – Historical perspectives 生物标准化在确保生物制品的有效性和安全性中的重要作用-历史观点。
IF 3.7 3区 医学
Journal of pharmaceutical sciences Pub Date : 2025-02-01 DOI: 10.1016/j.xphs.2024.12.011
Rajesh K. Gupta
{"title":"The vital role of biological standardization in ensuring efficacy and safety of biological products – Historical perspectives","authors":"Rajesh K. Gupta","doi":"10.1016/j.xphs.2024.12.011","DOIUrl":"10.1016/j.xphs.2024.12.011","url":null,"abstract":"<div><div>Biological Standardization has been pivotal to the success of traditional biological products, such as vaccines, antitoxins, and immune globulins, by ensuring their quality and consistency across manufacturers worldwide. The principles of biological standardization have similarly supported the development and manufacture of safe and effective modern biological products, including hormone, therapeutic protein, and monoclonal antibody products, and continue to play a vital role in advancing new cutting-edge biological products, such as tissue, cellular, and gene-therapy products. Biological standardization started with the physical standards ensuring the reliability and suitability of methods used to test biological products and science of bioassays or biological methods and related biostatistics providing a framework for evaluating biological, functional activity or potency of these products. It expanded to include written standards defining the quality requirements for manufacturing and regulation of biological standards. Due to the shift in the biologics industry from public health to commercial-driven enterprises during the past 50 years, the biological standardization program has evolved to include the product-specific reference standards and harmonization of physical standards. The global success of conventional vaccines in controlling numerous deadly infectious diseases can largely be attributed to the availability of physical and written international standards developed through a strong biological standardization program. This article explores the evolution of biological standardization for more than a century, its scientific and regulatory principles, challenges from disruption in international standardization efforts, and future perspectives for the field.</div></div>","PeriodicalId":16741,"journal":{"name":"Journal of pharmaceutical sciences","volume":"114 2","pages":"Pages 690-700"},"PeriodicalIF":3.7,"publicationDate":"2025-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142877502","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
A high-throughput micro-scale workflow to quantify molecularly dissolved drug concentrations under solubilizing conditions 在增溶条件下定量分子溶解药物浓度的高通量微尺度工作流程。
IF 3.7 3区 医学
Journal of pharmaceutical sciences Pub Date : 2025-02-01 DOI: 10.1016/j.xphs.2024.12.027
Florentin Lukas Holzem , Rasmus Lind Mikkelsen , Jeannine Petrig Schaffland , Cordula Stillhart , Martin Brandl , Annette Bauer-Brandl
{"title":"A high-throughput micro-scale workflow to quantify molecularly dissolved drug concentrations under solubilizing conditions","authors":"Florentin Lukas Holzem ,&nbsp;Rasmus Lind Mikkelsen ,&nbsp;Jeannine Petrig Schaffland ,&nbsp;Cordula Stillhart ,&nbsp;Martin Brandl ,&nbsp;Annette Bauer-Brandl","doi":"10.1016/j.xphs.2024.12.027","DOIUrl":"10.1016/j.xphs.2024.12.027","url":null,"abstract":"<div><div>Physiological and artificial solubilizing agents usually enhance apparent solubility of poorly soluble drugs, and in many cases also oral drug exposure. However, exposure may decrease in cases where micellization reduces the molecularly dissolved drug fraction, overriding the solubility advantage. While this information is critical to accurately anticipate the effect of drug micellization on oral absorption, the experimental determination of molecularly dissolved drug concentrations is complex and time consuming.</div><div>The present study aimed at developing a micro-scale <em>in vitro</em> workflow (comparative micro-scale mass transfer assay, CMMTA) to quantify molecularly dissolved (unbound) drug concentrations in the presence of solubilizing agents.</div><div>A linear correlation was determined between the cumulative passive permeation of the model drug riluzole (RLZ) and its concentration in the donor buffer solution on a 96-well microtiter sandwich plate (PermeaPlain™). Next, the drug permeation from micellar drug solutions (in fasted and fed state simulated intestinal fluids, FaSSIF and FeSSIF) was measured and the concentration of unbound drug was derived from the aforementioned correlation. The results were validated against established methods to measure free (unbound) drug concentrations, namely equilibrium dialysis and microdialysis. The concentrations of molecularly dissolved RLZ were correctly captured on one single microtiter plate.</div><div>Both, the standard curve and samples at different solubilizing conditions can be determined simultaneously within a few hours using small quantities of drug substance. Hence, the proposed CMMTA workflow represents a promising screening tool for early-stage drug development.</div></div>","PeriodicalId":16741,"journal":{"name":"Journal of pharmaceutical sciences","volume":"114 2","pages":"Pages 1485-1494"},"PeriodicalIF":3.7,"publicationDate":"2025-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142895637","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Safety, tolerability, pharmacokinetic, and pharmacodynamic of CZ1S injection for unilateral brachial plexus blockade in healthy Chinese adults: Double-blind, randomized, positive-controlled Phase I study 中国健康成人单侧臂丛神经阻滞注射CZ1S的安全性、耐受性、药代动力学和药效学:双盲、随机、阳性对照的I期研究
IF 3.7 3区 医学
Journal of pharmaceutical sciences Pub Date : 2025-02-01 DOI: 10.1016/j.xphs.2025.01.008
Pengfei Zhao , Dongjie Feng , Haiying Wang , Ting Luo , Dandan Yang , Zourong Ruan , Linqiang Zhu , Min Yan , Bo Jiang
{"title":"Safety, tolerability, pharmacokinetic, and pharmacodynamic of CZ1S injection for unilateral brachial plexus blockade in healthy Chinese adults: Double-blind, randomized, positive-controlled Phase I study","authors":"Pengfei Zhao ,&nbsp;Dongjie Feng ,&nbsp;Haiying Wang ,&nbsp;Ting Luo ,&nbsp;Dandan Yang ,&nbsp;Zourong Ruan ,&nbsp;Linqiang Zhu ,&nbsp;Min Yan ,&nbsp;Bo Jiang","doi":"10.1016/j.xphs.2025.01.008","DOIUrl":"10.1016/j.xphs.2025.01.008","url":null,"abstract":"<div><div>CZ1S injection is a novel, extended-release local anaesthetic formulation of ropivacaine, classified as a type 2.2 new drug, with potential for post-operative analgesia by subcutaneous infiltration and peripheral nerve blockade. This study aimed to validate the superior properties of CZ1S over ropivacaine hydrochloride injection and to evaluate the safety, tolerability, pharmacokinetic (PK) and pharmacodynamic (PD) profiles of a single dose of brachial plexus block with CZ1S in healthy Chinese adults. The tolerability and PK profile of CZ1S were investigated following a unilateral brachial plexus injection in 24 healthy adults. Safety assessments were performed throughout the study and the PD effects of CZ1S injection for unilateral brachial plexus block were also evaluated. The results showed that CZ1S was slowly absorbed after a single injection in healthy subjects, with PK parameters of ropivacaine (including C<sub>max</sub>, AUC<sub>t</sub> and AUC<sub>∞</sub>) increasing with the CZ1S doses. CZ1S demonstrated a prolonged and non-constant release profile compared to a single 75 mg injection of ropivacaine hydrochloride, resulting in a smooth and sustained blood concentration. CZ1S significantly prolonged the duration of sensory and motor blockade, and further analysis revealed a correlation between PK and sensory nerve block. The PK profile of CZ1S was enhanced compared to that of ropivacaine injection, and it was deemed safe and well tolerated in healthy Chinese adults, suggesting its potential application in postoperative analgesia.</div></div><div><h3>Clinical Trial Registration</h3><div>Chinadrugtrials.org.cn: CTR20231295 (registration date: 26 April 2023)</div></div>","PeriodicalId":16741,"journal":{"name":"Journal of pharmaceutical sciences","volume":"114 2","pages":"Pages 1245-1253"},"PeriodicalIF":3.7,"publicationDate":"2025-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143007099","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
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