Drug Design, Development and Therapy最新文献

{"title":"Enhancing Cartilage Repair in Osteoarthritis Using Platelet Lysates and Arthroscopic Microfracture.","authors":"Haiyan Zhang, Dipeng Li, Wei Zheng, Jiaqing Hua, Zuxiang Chen, Wenting Xu, Jianing Zhu, Yue Wang, Xiaotian Chen, Huixin Chen, Le Guo, Qiang Yuan, Li Zhou, Letian Shan","doi":"10.2147/DDDT.S502935","DOIUrl":"10.2147/DDDT.S502935","url":null,"abstract":"<p><strong>Background: </strong>Osteoarthritis (OA) is the most prevalent joint degenerative disease. MF is considered as a first-line treatment for OA. In the long term, the cartilage tissue regenerated after MF is fibrocartilage. In this study, we examine whether combined treatment of MF and Platelet lysate (PL) can inhibit promotion of cartilage repair and antifibrosis.</p><p><strong>Methods: </strong>OA rat model established by the modified Hulth method. Rat PL injected into treated knee joints after MF surgery. The expression levels of metabolic and fibrosis molecules (Col2, Mmp13, Col1, Col3, α-SMA, and Ctgf) of chondrocytes were examined by immunohistochemistry. Cell immunofluorescence was used to assess bone marrow MSCs (BMSCs) proliferation. Transwell assays evaluated BMSCs migration, and qPCR and Western blot analyzed the mechanisms of PL. Moreover, a retrospective analysis was conducted to determine the clinical efficacy and safety of the combined treatment of MF and PL on OA patients.</p><p><strong>Results: </strong>In vivo data showed that the combined treatment of MF and PL significantly alleviated joint pain, protected chondrocytes and inhibited synovial fibrosis on OA rats, as was confirmed by upregulation of Collagen II and downregulation of Mmp13, Col1, Col3, α-SMA, and Ctgf. Such anti-OA and antifibrosis effects of the combined treatment of MF and PL were superior to MF alone. In vitro data showed that PL induced cellular chondrogenic differentiation and migration of BMSCs, suggesting that PL facilitated stem cell homing to the cartilage injury sites and promoted cartilage repair and regeneration. Furthermore, the clinical data showed significant improvements of pain reduction and cartilage repair in OA patients.</p><p><strong>Conclusion: </strong>This study demonstrated the anti-OA and antifibrosis effects of the combination of MF and PL, providing a promising synergistic therapeutic option for the treatment of OA.</p>","PeriodicalId":11290,"journal":{"name":"Drug Design, Development and Therapy","volume":"19 ","pages":"3827-3843"},"PeriodicalIF":4.7,"publicationDate":"2025-05-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12085145/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144093164","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"A Bibliometric Analysis of Microneedle-Mediated Drug Delivery: Trends, Hotspots, and Future Directions.","authors":"Weiyi Xiang, Xian Jiang, Linghong Guo","doi":"10.2147/DDDT.S519048","DOIUrl":"10.2147/DDDT.S519048","url":null,"abstract":"<p><strong>Purpose: </strong>Microneedles can physically penetrate the stratum corneum, creating micropores on the skin, and allowing for drug delivery through direct diffusion, injection, or other methods. As a novel drug delivery method, it possesses significant application potential. This study uses bibliometric analysis to explore the research hotspots and development trends of microneedle-mediated drug delivery.</p><p><strong>Methods: </strong>Relevant research articles on microneedle-mediated drug delivery published between 1998 and 2024 in the Web of Science Core Collection (WoSCC) database were retrieved. Data analysis and visualization were performed using VOSviewer, CiteSpace, Scimago Graphica, and Pajek, enabling the prediction of research trends in microneedle-mediated drug delivery.</p><p><strong>Results: </strong>In general, research on microneedle-mediated drug delivery has shown a continuous increase. China and the United States are the leading countries in this field of study. Notably, Ryan F. Donnelly (n=224) is the most prominent contributor to this field. The current core research directions include: disease treatment, enhancement of transdermal absorption performance of microneedles, vaccine delivery, and new materials and technologies for microneedle manufacturing.</p><p><strong>Conclusion: </strong>Microneedle-mediated drug delivery, as a novel technology and method, holds significant research value and application potential. However, further strengthening of international collaboration and the clinical translation of research findings are needed.</p>","PeriodicalId":11290,"journal":{"name":"Drug Design, Development and Therapy","volume":"19 ","pages":"3805-3825"},"PeriodicalIF":4.7,"publicationDate":"2025-05-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12079042/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144076572","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Ethnobotanical Use, Phytochemistry, Pharmacology, and Toxicity of <i>Canavalia gladiata</i>.","authors":"Huiqin Qian, Di Meng, Lu Yue, Haibo Xu, Kun Feng, Jianan Wang","doi":"10.2147/DDDT.S519102","DOIUrl":"https://doi.org/10.2147/DDDT.S519102","url":null,"abstract":"<p><p><i>Canavalia gladiata</i> (<i>C. gladiata</i>) is a significant traditional Chinese medicine that has been used to treat hiccups, vomiting, nausea, amenorrhea, chronic dysentery, larynx arthralgia, lumbago, and inflammatory diseases in Asia for a long history. Although the chemical composition of <i>C. gladiata</i> has been reported, no thorough review of <i>C. gladiata</i> has been published. Therefore, the present study aimed to comprehensively analyze the ethnobotanical use, phytochemistry, pharmacology, and toxicity of <i>C. gladiata</i>. All the available information on <i>C. gladiata</i> was actualized by systematically searching scientific databases including Web of Science, ScienceDirect, PubMed, Google Scholar, Springer, Wiley, CNKI, CSPD, and Baidu Scholar between 1967 and up-to-date. Based on the reported information, more than 231 components have been identified in <i>C. gladiata</i>, including flavonoids, terpenes, steroids, organic acids, nitrogenous compounds, amino acids, proteins, etc. Crude extracts, fractions, and constituents from <i>C. gladiata</i> show various pharmacological activities, including antioxidant, antitumor, antimicrobial, anti-inflammatory, antiallergic, immunomodulatory, antiobesity, hepatoprotective, antidiabetic, etc. Notably, the immature seeds are poisonous. Besides, modern research reveals that <i>C. gladiata</i> is rich in chemical constituents and pharmacological activities, which are of great research value. However, more in-depth studies including chemical composition, pharmacological mechanism, quality standardisation, toxicology, and clinical research trials are needed for <i>C. gladiata</i> as a new candidate for future drug development.</p>","PeriodicalId":11290,"journal":{"name":"Drug Design, Development and Therapy","volume":"19 ","pages":"3779-3803"},"PeriodicalIF":4.7,"publicationDate":"2025-05-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12075509/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144076574","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Pharmacokinetics and Safety of HRS-1780 in Renal Impaired Subjects: A Multicenter, Non-Randomized, Open-Label Study.","authors":"Yue Fei, Zhihong Xie, Yuanyuan Luo, Xiaolan Yong, Na Li, Rong Huang, Xiaolin Du, Yijing Zhu, Dongmei Lan, Yang Qi, Gang Cheng, Quanren Wang, Kai Shen","doi":"10.2147/DDDT.S500384","DOIUrl":"10.2147/DDDT.S500384","url":null,"abstract":"<p><strong>Purpose: </strong>HRS-1780 is a selective non-steroidal mineralocorticoid receptor antagonist developed for the treatment of chronic kidney disease. This study aimed to assess the pharmacokinetics (PK) and safety profiles of HRS-1780 in subjects with renal impairment.</p><p><strong>Patients and methods: </strong>Eligible participants were enrolled in the healthy (glomerular filtration rate [GFR] of ≥90 mL/min), mild (GFR of 60-89 mL/min), and moderate renal impairment (GFR of 30-59 mL/min) groups with 9 subjects each and orally received 20 mg HRS-1780. Concentrations of HRS-1780 and its main metabolites were measured in plasma and urine. PK profiles between healthy and renal impairment subjects were compared using analysis of variance.</p><p><strong>Results: </strong>A total of 27 subjects completed the study. HRS-1780 was rapidly absorbed and eliminated, with T_max of 0.50-0.52 hour and t_1/2 of 2.06-2.56 hours. Exposure (AUC_0-inf) to HRS-1780 was comparable between mildly and moderately renal impaired subjects, while higher, but not significantly than that in healthy subjects. Similar plasma protein binding among different renal function groups suggested a consistent effect of renal function on total and unbound HRS-1780. Renal clearance of HRS-1780 decreased with severity of renal impairment, but renal elimination of HRS-1780 was minimal. Exposure to SX2183-M3 was significantly increased in the moderate renal impairment subjects. Renal impairment did not appear to be associated with an increased risk of adverse events.</p><p><strong>Conclusion: </strong>HRS-1780 PK and safety profiles did not differ significantly between healthy and renal impairment subjects. This supports the drug dose regimen for renal impairment patients in clinical practice.</p>","PeriodicalId":11290,"journal":{"name":"Drug Design, Development and Therapy","volume":"19 ","pages":"3751-3761"},"PeriodicalIF":4.7,"publicationDate":"2025-05-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12068283/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143987957","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"A Natural Compound Methylnissolin: Physicochemical Properties, Pharmacological Activities, Pharmacokinetics and Resource Development.","authors":"Ziyang Lin, Mingjie Liang, Xianlong Zhang, Zhuo Cen, Fengxin Kang, Baien Liang, Ying Lai, Minyi Li, Tingting Duan, Junzheng Yang, Bo Liu","doi":"10.2147/DDDT.S518508","DOIUrl":"https://doi.org/10.2147/DDDT.S518508","url":null,"abstract":"<p><p>Methylnissolin (also known as Astrapterocarpan) is an isoflavonoid compound featuring a pterocarpan core structure. To date, leguminous plants of the genus <i>Astragalus</i> remain the exclusive natural source of Methylnissolin and its glycoside derivative, Methylnissolin-3-O-glucoside. Upon oral administration, Methylnissolin and its glycosides enter systemic circulation and modulate signaling pathways such as RIPK2/ASK1, PI3K/AKT, IκB/NF-κB, MAPK, and Nrf2/HO-1. Their pharmacological activities span anti-inflammatory, antioxidant, glucose-lipid metabolism regulation, and antitumor effects, underscoring their broad potential for drug development. This review comprehensively evaluates the physicochemical properties, pharmacological activities, mechanisms of action, pharmacokinetic characteristics, and toxicological profile of Methylnissolin and its glycoside derivatives. Notably, we systematically elucidate the metabolic fate of methylnissolin, identifying hydroxylation, demethylation, dimerization, hydration, and dehydrogenation as predominant biotransformation pathways. Furthermore, the influence of factors such as plant variety, geographical origin, and processing methods on Methylnissolin and its glycoside content in <i>Astragalus membranaceus</i> is analyzed, providing crucial insights for drug development and resource utilization.</p>","PeriodicalId":11290,"journal":{"name":"Drug Design, Development and Therapy","volume":"19 ","pages":"3763-3777"},"PeriodicalIF":4.7,"publicationDate":"2025-05-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12068406/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143969687","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Determining Opioid-Sparing Efficacy of Intraoperative Esketamine After Laparoscopic Gynecological Surgery [Letter].","authors":"Xiao-Ying Chen, Yan-Hua Guo, Fu-Shan Xue","doi":"10.2147/DDDT.S522838","DOIUrl":"https://doi.org/10.2147/DDDT.S522838","url":null,"abstract":"","PeriodicalId":11290,"journal":{"name":"Drug Design, Development and Therapy","volume":"19 ","pages":"3701-3702"},"PeriodicalIF":4.7,"publicationDate":"2025-05-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12067642/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143981790","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Design of Experiments Assisted Formulation Optimization and Evaluation of Efavirenz Solid Dispersion Adsorbate for Improvement in Dissolution and Flow Properties.","authors":"Md Ali Mujtaba, Md Abdur Rashid, Yahya Alhamhoom, Purushottam Gangane, Mohini Janardan Jagtap, Mohammad J Akbar, Sandeep Ashokrao Wathore, Mohammed Kaleem, Gamal Osman Elhassan, Mohammad Khalid","doi":"10.2147/DDDT.S517021","DOIUrl":"https://doi.org/10.2147/DDDT.S517021","url":null,"abstract":"<p><strong>Background: </strong>Efavirenz (EFZ) is an anti-HIV drug that has been administered as first-line treatment, which exhibits low solubility and poor oral bioavailability. Therefore, the current study aimed to develop a solid dispersion adsorbate (SDA) to enhance the dissolution rate and flow properties of EFZ for solid oral dosage forms.</p><p><strong>Methods: </strong>The SDA of EFZ was prepared using the fusion method with PEG-6000 and poloxamer-188 as carriers, along with avicel PH-102 and aerosil-200 as adsorbents. 3² full factorial approach was employed to formulate the SDA and evaluate the effects of two independent factors X₁: the ratio of PEG-6000 to EFZ in the solid dispersion, and X₂: the ratio of aerosil-200 to the solid dispersion. The dependent factors analyzed were Y₁: the time required for 85% of the drug release, and Y₂: angle of repose.</p><p><strong>Results: </strong>The optimized formulation (F9) was selected through numerical optimization, demonstrating the desired drug release and excellent flow properties of the pre-compressed SDA. Fourier transform infrared (FTIR) spectroscopy, Differential scanning calorimetry (DSC), X-ray diffraction (XRD), and Scanning electron microscopy (SEM) of SDA showed the transformation of crystalline to amorphous form of EFZ, which is responsible for improving drug dissolution. The direct compression method was used to prepare SDA-EFZ tablets (equivalent to 25 mg EFZ) along with plain EFZ. The dissolution efficiency increased from 50.68% for plain EFZ tablets to 96.18% for EFZ-SDA tablets. Furthermore, the cumulative percentage drug release (%CDR) from SDA tablets was nearly double that of plain EFZ tablets. Stability testing indicated no significant changes in drug content and %CDR of the SDA tablets.</p><p><strong>Conclusion: </strong>The findings of this study suggest that the SDA method is an effective approach for enhancing the dissolution and flow characteristics of EFZ and may serve as an alternative strategy for preparing solid dosage forms in commercial applications.</p>","PeriodicalId":11290,"journal":{"name":"Drug Design, Development and Therapy","volume":"19 ","pages":"3715-3734"},"PeriodicalIF":4.7,"publicationDate":"2025-05-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12067463/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143958465","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Quantitative Proteomic Study Reveals Amygdalin Alleviates Liver Fibrosis Through Inhibiting mTOR/PDCD4/JNK Pathway in Hepatic Stellate Cells.","authors":"Hui Huang, Su-Jie Ru, Jia-Mei Chen, Wei Liu, Shan-Hua Fang, Qian Liu, Qian Meng, Ping Liu, Hu Zhou","doi":"10.2147/DDDT.S500439","DOIUrl":"https://doi.org/10.2147/DDDT.S500439","url":null,"abstract":"<p><strong>Purpose: </strong>Hepatic fibrosis is a major cause of morbidity and mortality for which there is currently limited therapy. Amygdalin, a cyanogenic glucoside derived from Semen Persicae, exerts significant anti-fibrotic effects in the liver. However, the molecular mechanism by which amygdalin inhibits the progression of liver fibrosis remains unclear. This study aimed to elucidate the potential mechanism of action of amygdalin against liver fibrosis.</p><p><strong>Methods: </strong>Quantitative proteomic profiling of the mouse liver tissues from control, carbon tetrachloride (CCl₄)-induced fibrosis, and amygdalin-treated groups was performed to explore the key effector proteins of amygdalin. Histology and immunohistochemistry as well as serum biochemical analysis were performed to evaluate amygdalin efficacy in mice. The key gene programmed cell death protein 4 (PDCD4) was overexpressed or knocked down in human hepatic stellate cells (HSCs). The mRNA and protein levels of related molecules were detected by RT-qPCR and Western blotting, respectively.</p><p><strong>Results: </strong>Amygdalin could effectively ameliorated CCl₄-induced liver fibrosis in mice. Bioinformatics analysis revealed that PDCD4 was downregulated in CCl₄-induced liver fibrosis, but amygdalin treatment reversed these changes. An in vitro study showed that PDCD4 inhibited the activation of human hepatic stellate cell line LX-2 cells by regulating the JNK/c-Jun pathway and amygdalin inhibited the activation of LX-2 cells in a PDCD4-dependent manner. We further found that amygdalin inhibited the phosphorylation of PDCD4 at Ser67 by inhibiting the mTOR/S6K1 pathway to enhance PDCD4 expression.</p><p><strong>Conclusion: </strong>Our data demonstrated a potential pharmaceutical mechanism by which amygdalin alleviates liver fibrosis by inhibiting the mTOR/PDCD4/JNK pathway in HSCs, suggesting that PDCD4 is a potential target for the treatment of liver fibrosis.</p>","PeriodicalId":11290,"journal":{"name":"Drug Design, Development and Therapy","volume":"19 ","pages":"3735-3749"},"PeriodicalIF":4.7,"publicationDate":"2025-05-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12067723/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143978488","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Combined Use of Remimazolam and Ciprofol Reduces Hypoxemia and Shortens Recovery Time During Sedated Gastrointestinal Endoscopy.","authors":"Hai-Ding Zou, Cong Luo, Zhao-Lan Hu, Pei Zhou, Ru-Yi Luo","doi":"10.2147/DDDT.S515783","DOIUrl":"10.2147/DDDT.S515783","url":null,"abstract":"<p><strong>Background: </strong>Hypoxemia is the most common adverse event during painless gastrointestinal endoscopy (PGIE). This study aimed to evaluate whether the combined use of remimazolam besylate and ciprofol (group RC) reduces the incidence of hypoxemia compared to ciprofol alone (group C) in patients undergoing PGIE under deep sedation.</p><p><strong>Methods: </strong>A total of 246 patients scheduled for PGIE were recruited from the Second Xiangya Hospital of Central South University and randomly assigned to group C or RC. The primary outcome measured was the incidence of intraoperative hypoxemia. Secondary outcomes included physiological parameters such as blood pressure, heart rate, and oxygen saturation (SpO2) during the procedure, along with time to loss of consciousness (LoC), time to awakening, and major adverse effects (MAEs). Additionally, correlations between minimum SpO2 and factors like body mass index (BMI), age, and preoperative SpO2 were examined.</p><p><strong>Results: </strong>Group C exhibited a significantly higher incidence and frequency of hypoxemia compared to group RC. Correlation analysis revealed that minimum SpO2 was inversely related to age and BMI, while showing a positive correlation with preoperative SpO2. Additionally, the RC group demonstrated significantly decreased induction and shorter times to LoC and awakening than group C.</p><p><strong>Conclusion: </strong>The combined administration of ciprofol and remimazolam besylate may enhance the safety profile of deep sedation for PGIE compared to ciprofol alone, offering reduced hypoxemia incidence and improved procedural efficiency.</p><p><strong>Trial registration: </strong>www.chictr.org.cn (Registration number: ChiCTR2400092506, Registration date: November 18, 2024).</p>","PeriodicalId":11290,"journal":{"name":"Drug Design, Development and Therapy","volume":"19 ","pages":"3703-3713"},"PeriodicalIF":4.7,"publicationDate":"2025-05-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12065459/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143977999","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"The Recovery of Ciprofol, Remimazolam and Remimazolam-Flumazenil for General Anesthesia Undergoing Fundus Surgery: A Single-Center, Prospective, Randomized, Controlled Clinical Study.","authors":"Shuang Zhang, Yunfei Liu, Yanyu Liu, Ting Xu","doi":"10.2147/DDDT.S512431","DOIUrl":"10.2147/DDDT.S512431","url":null,"abstract":"<p><strong>Purpose: </strong>Ciprofol (HSK3486 injectable emulsion) is a 2.6-disubstituted phenol derivative that acts similarly to propofol with a fast onset, quick, and stable recovery. Moreover, remimazolam is a new benzodiazepine with a faster onset and recovery than midazolam, and more stable hemodynamics than propofol. We found no relevant literature that directly compared these two drugs. The primary objective of this study was to compare the recovery of HSK3486 with that of remimazolam during successful general anesthesia.</p><p><strong>Patients and methods: </strong>This prospective, randomized, double-blind study included 93 patients who had undergone fundus surgery. The patients were divided into three groups: HSK3486 (H group), remimazolam-saline <i>(RS</i> group), and remimazolam-flumazenil (RF group). The primary outcome was the time from drug withdrawal to eye opening, and the secondary outcome was the time from drug withdrawal to laryngeal mask removal, the time for Aldrete modified score ≥ 9, intraoperative hemodynamic changes, post-operative adverse events (nausea, vomiting, pain, delirium, re-sedation), and the Quality of Recovery-15 score before surgery and at 1, 7, and 14 days post-operatively.</p><p><strong>Results: </strong>The RF group showed the shortest eye-opening time: 3.8 (2.8) min vs 13.3 (5.2) min for the H group, <i>P</i> < 0.001; and 11.5 (5.5) min for the <i>RS</i> group, <i>P</i> < 0.001. And laryngeal mask removal time was 5.2 (3.1) min for the RF group vs 14.1 (5.2) min for the H group, <i>P</i> < 0.001; and 12.4 (5.5) min for the <i>RS</i> group, <i>P</i> < 0.001. There were no significant differences in other post-operative outcomes.</p><p><strong>Conclusion: </strong>The incorporation of flumazenil with remimazolam for total intravenous anesthesia provided rapid and reliable recovery of consciousness, although there were no significant visible differences between HSK3486 and Remimazolam-saline.</p>","PeriodicalId":11290,"journal":{"name":"Drug Design, Development and Therapy","volume":"19 ","pages":"3691-3700"},"PeriodicalIF":4.7,"publicationDate":"2025-05-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12064274/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143977520","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}