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lidocaine hydrochloride (3268 / lignocaine, Anesiva / ALGRX 3268)

✓ Approved

Marathon Pharmaceuticals · SCN9A · 小分子

什么是 lidocaine hydrochloride？

lidocaine hydrochloride 是一种小分子，由Marathon Pharmaceuticals研发。该药已获批，用于治疗相关适应症，给药途径：Injectable (Others)、Intradermal Injection。

药物档案

商品名3268, lignocaine, Anesiva, ALGRX 3268
公司Marathon Pharmaceuticals
药物类别小分子
分子靶点SCN9A
给药途径Injectable (Others), Intradermal Injection
状态Approved
来源： ClinicalTrials.gov, Marathon Pharmaceuticals

作用机制

分子靶点

lidocaine hydrochloride 作用于 1 个分子靶点：

SCN9Asodium voltage-gated channel alpha subunit 9 (SFNP, GEFSP7)
需要更深入的分析？Noah AI 可解释复杂机制并与同类药物比较。

治疗适应症

lidocaine hydrochloride 针对 2 个适应症，涉及 1 个治疗领域。

治疗领域疾病/病症分期
Nervous system disordersAnaesthesia✓ Approved
Nervous system disordersSensory loss✓ Approved

相关研究文献

PubMedSmall (Weinheim an der Bergstrasse, Germany)2026-09-10

Manipulating the Buried Interfacial Dipole: The Role of Pyridine Acetate-Hydrochloride Isomers in Carbon-Based Perovskite Solar Cells Prepared in Air.

Shi Yifei Y, Gong Jianwen J, Wang Xu X, Hu Shuming S et al.

The buried interface between tin oxide and perovskite is the key factor for non-radiative recombination and energy level mismatch, which limits the performance and stability of perovskite solar cells. This work explores a simple interfacial dipole engineering strategy, where three pyridine acetate-hydrochloride (PAH) isomer molecules (2-PAH, 3-PAH, and 4-PAH) are used to modify the SnO2 electron transport layer. The 3-PAH-modified layer can control the work function of tin oxide, achieve the best energy level alignment, and improve the crystallization quality of the perovskite film, thereby effectively suppressing interface recombination and promoting electron extraction. All the devices are prepared in air, and the device optimized by 3-PAH achieved a champion energy conversion efficiency of 14.31% and demonstrated stability. Subsequent to an 800 h placement in an N2 glove box or a 340 h exposure to an air environment, the unencapsulated target devices that were modified by 3-PAH maintained 80.7% and 81.3% of their initial efficiency.

PMID 42717680
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PubMedAAPS PharmSciTech2026-09-10

Ethosomal Gel-Based Topical Delivery of Albendazole Hydrochloride for Psoriasis: In Vitro and In Vivo Evaluation.

Rençber Seda S, Karpuz Merve M, Ünlü Çakıcı Büşra B, Karayıldırım Çinel Köksal ÇK et al.

This study aimed to develop an albendazole hydrochloride (ALB)-loaded ethosomal gel for topical psoriasis treatment. ALB-loaded ethosomes were prepared and characterized to select the optimal formulation, which was subsequently incorporated into an HPMC-based hydrogel. The ethosomal gel was evaluated through physicochemical, in vitro and in vivo studies. The optimized ethosomal formulation prepared by the film hydration method exhibited a mean vesicle size of 490.00 ± 0.14 nm, polydispersity index of 0.31 ± 0.14, zeta potential of -22.85 ± 2.28 mV and encapsulation efficiency of 23.90 ± 1.43%. After incorporation into the hydrogel matrix, the Gel4-E3/ALB formulation demonstrated appropriate mechanical properties (hardness 8.42 ± 0.70 mN, adhesiveness - 16.85 ± 1.50 mN·s, elasticity 0.89 ± 0.07, cohesiveness 1.14 ± 0.09) and shear-thinning behavior, ensuring ease of application and skin retention. A controlled release pattern was observed, consistent with the controlled-release behavior expected from ethosomal hydrogel systems. Radiolabeling studies demonstrated high labeling efficiency (> 95%). In vitro cytotoxicity evaluation indicated that the optimized ethosomal gel formulation was non-toxic. In vivo studies performed in an imiquimod (IMQ)-induced psoriatic mouse model revealed significant therapeutic improvement in the Gel4-E3/ALB-treated group compared with the IMQ control, with visible reduction in erythema, scaling, and skin thickening after the fifth day of treatment. Hematological analysis showed no adverse effects associated with the formulation. Histopathological evaluation confirmed the reduction in epidermal hyperplasia and inflammatory cell infiltration in the treated group. The developed ALB-loaded ethosomal gel represents a safe and promising topical therapeutic system for psoriasis management.

PMID 42717176
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PubMedFrontiers in pharmacology2026-09-10

Spatial inequalities and contextual correlates of methylphenidate dispensing in Jiangsu Province, China.

Sun Yao Y, Lu Miao M, Zhang Yong Y, Xu Jin J et al.

Understanding geographic inequalities in psychotropic medication dispensing is important for improving health equity and informing place-based pharmaceutical management. This study characterized the spatiotemporal distribution of methylphenidate hydrochloride extended-release tablet dispensing in Jiangsu Province, China, from 2019 to 2023 and examined its socioeconomic and education-related correlates. Annual county-level dispensed tablet volumes were analyzed using Getis-Ord Gi* hot-spot analysis, standard deviational ellipses, and weighted-centroid analysis. Prefecture-level contextual correlates were examined using annual Lasso models interpreted with SHAP. The proportion of county-level units with zero recorded dispensing decreased from approximately 52%-36%, while the proportion with annual volumes exceeding 20,000 tablets increased from 7% to 20%. Southern Jiangsu consistently exhibited higher dispensing volumes than Northern Jiangsu, with Central Jiangsu generally occupying an intermediate position. Getis-Ord Gi* identified localized high-value concentrations mainly in Southern and parts of Central Jiangsu. The standard deviational ellipse area increased by 23.1%, while the weighted centroid remained in south-central Jiangsu. Within the annual Lasso models, predictive importance was allocated mainly to economic-demographic indicators in 2019-2020 and more strongly to education-related indicators in 2021-2023. The findings support geographically differentiated monitoring of medication access, dispensing patterns, and prescribing quality.

PMID 42718491
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PubMedThe AAPS journal2026-09-10

Dissolution Enhancement by Binding Agents: A Potential Shortcut to Improving Bioavailability?

Chronowska Maja M, Dressman Jennifer J

The poor water solubility of many drugs and drug candidates is a limiting factor to their bioavailability after oral administration. Although dissolution enhancing approaches, e.g. amorphous solid dispersions, are often used to make enabling formulations, these are usually associated with high development and manufacturing costs. This study focuses on the potential of using pharmaceutical excipients (binders) in simple tablet formulations to improve drug release and thus bioavailability. Loperamide hydrochloride, fenofibrate, compound c0 (a drug candidate) and carvedilol were chosen for this study as poorly water-soluble model compounds. Their solubility in the absence and presence of three polymeric binders, polyvinylpyrrolidone (PVP) K90, hydroxypropyl methylcellulose (HPMC) E4M and E15, and methylcellulose (MC) was tested in FaSSIF-V1 buffer and biorelevant media. Additionally, after wet granulation using PVP K90 or HPMC E15 as binders and tablet compression, the dissolution of the model compounds was tested in FaSSIF-V1 buffer and biorelevant media. Although solubilities and dissolution profiles of the model compounds were mostly improved by the binders, correlation between solubility in buffers and dissolution from the tablets in biorelevant FaSSIF-V1 was poor, indicating that dissolution experiments may be a better screening tool than solubility experiments. An important conclusion of these studies is that it is possible to increase the rate, and in some cases, the extent of dissolution of four poorly soluble drugs using wet granulation with polymeric binders, followed by tablet compression - a simple and cost-effective approach to improving drug performance.

PMID 42717179
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PubMedJournal of the International Society of Sports Nutrition2026-09-10

Creatine formulations and repeated sprint training: effects on physical and physiological adaptations in soccer players during the short-term preparation phase.

Duan Changyuan C, Wang Zaitao Z, Wang Qianjin Q

This research examined the impact of various creatine (Cr) supplementation formulations during a 4-week preparatory phase on the efficacy of repeated sprint training (RST) and on improvements in physical and physiological performance in male soccer athletes. A total of forty collegiate young soccer players volunteered for the study. They were randomly divided into four groups: creatine monohydrate (Cr-Mon, n = 10), creatine ethyl ester (Cr-Ee, n = 10), creatine hydrochloride (Cr-Hcl, n = 10), and placebo (PL, n = 10). All athletes engaged in a 4-week training intervention, three times a week (i.e. 12 sessions), and physical (countermovement vertical jump [CMVJ], 20-m sprint, and L-run) and physiological (Wingate anaerobic power and incremental exercise tests) performance were assessed both before and after the training period. All training groups improved physical and physiological performance following the 4-week intervention period (p < 0.05). Additionally, the groups receiving the Cr supplement exhibited significantly greater changes (p = 0.001) in physical performance, peak power output, and fatigue index compared to the PL group. However, no significant differences were found among the groups regarding mean power output and VO2max. Notably, the Ee and Hcl forms of Cr showed superior gains (p < 0.05) in physical performance and peak power compared to the Mon form after the 4-week intervention. The results underscore the importance of Cr ingestion in enhancing adaptations for short-term physical performance tasks, highlighting the effectiveness of the Ee and Hcl forms in further improving the CMVJ, 20-m sprint, L-run, and peak power among soccer players during the short-term preparation phase.

PMID 42720250
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PubMedFrontiers in veterinary science2026-09-10

Dietary Echinacea purpurea polysaccharide supplementation improves antioxidative status, intestinal immune, and structure of cecal microbiota in Mahuang chickens.

Peng Su S, Zhang Zhiying Z, Huang Xiaojie X, Xiao Yaqi Y et al.

Echinacea purpurea polysaccharide (EPP), a key bioactive constituent of the natural immunostimulant E. purpurea, shows potential as a poultry feed additive. This study evaluated EPP's impact on growth performance, serum biochemistry indices, organ index, antioxidant capacity, immunity, intestinal health, and microbiota in Mahuang chickens. A total of 180 one-day-old Mahuang chicks (initial average body weight 39.10 ± 0.51 g) were randomly divided into six groups (six replicates, five chicks per replicate): a basal diet with 0 (CON), 0.1 g/kg levamisole hydrochloride (LMS), 100 mg/kg EPP (EPP100), 200 mg/kg EPP (EPP200), 400 mg/kg EPP (EPP400), and 800 mg/kg EPP (EPP800) for 42 days. The results showed that EPP did not affect serum biochemical indices and organ index, but significantly improved growth performance by increasing body weight gain (d 21) (p < 0.05). Additionally, EPP improved intestinal (duodenum, jejunum, and ileum) morphology by increasing villus height and villus height-to-crypt depth ratio, and decreasing crypt depth (d 21 and d 42) (p < 0.05). Com-pared to the CON and LMS groups, EPP significantly increased superoxide dismutase activity (p = 0.011) and total antioxidant capacity activity (p = 0.001) (d 21), elevated the levels of immunoglobulin (Ig) M (p < 0.001) and secretory IgA (p = 0.038) (d 21), and upregulated intestinal barrier-related genes (d 21 and d 42) (p < 0.05). 16S rRNA gene sequencing revealed that EPP treatment increased the Bacteroidetes/Firmicutes ratio. EPP also elevated the relative abundances of Bacteroides, Lactobacillus, Ruminococcus, Butyricicoccus, Oscillospira, and Akkermansia, while decreasing the relative abundance of Streptococcus (p < 0.05). Overall, the EPP groups outperformed the CON and LMS groups, with the high-dose groups (EPP400, EPP800) showing superior effects to the low-dose groups (EPP100, EPP200). In summary, this study confirmed that supplementing with EPP could boost growth performance, antioxidant capacity, immunity, intestinal barrier function, and cecal microbial community in Mahuang chickens without adverse effects, and the 400-800 mg/kg EPP appears to be optimal. This highlights the potential of EPP as a safe and effective alternative to synthetic immunostimulants in poultry production.

PMID 42718682
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