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Hypidone hydrochloride(YL-0919)ameliorates functional deficits after traumatic brain injury in mice by activating the sigma-1 receptor for antioxidation
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作者 Yafan Bai Hui Ma +5 位作者 Yue Zhang Jinfeng Li Xiaojuan Hou Yixin Yang Guyan Wang Yunfeng Li 《Neural Regeneration Research》 SCIE CAS 2025年第8期2325-2336,共12页
Traumatic brain injury involves complex pathophysiological mechanisms,among which oxidative stress significantly contributes to the occurrence of secondary injury.In this study,we evaluated hypidone hydrochloride(YL-0... Traumatic brain injury involves complex pathophysiological mechanisms,among which oxidative stress significantly contributes to the occurrence of secondary injury.In this study,we evaluated hypidone hydrochloride(YL-0919),a self-developed antidepressant with selective sigma-1 receptor agonist properties,and its associated mechanisms and targets in traumatic brain injury.Behavioral experiments to assess functional deficits were followed by assessment of neuronal damage through histological analyses and examination of blood-brain barrier permeability and brain edema.Next,we investigated the antioxidative effects of YL-0919 by assessing the levels of traditional markers of oxidative stress in vivo in mice and in vitro in HT22 cells.Finally,the targeted action of YL-0919 was verified by employing a sigma-1 receptor antagonist(BD-1047).Our findings demonstrated that YL-0919 markedly improved deficits in motor function and spatial cognition on day 3 post traumatic brain injury,while also decreasing neuronal mortality and reversing blood-brain barrier disruption and brain edema.Furthermore,YL-0919 effectively combated oxidative stress both in vivo and in vitro.The protective effects of YL-0919 were partially inhibited by BD-1047.These results indicated that YL-0919 relieved impairments in motor and spatial cognition by restraining oxidative stress,a neuroprotective effect that was partially reversed by the sigma-1 receptor antagonist BD-1047.YL-0919 may have potential as a new treatment for traumatic brain injury. 展开更多
关键词 antidepressant drug blood-brain barrier cognitive function hypidone hydrochloride(YL-0919) neurological function nuclear factor-erythroid 2 related factor 2 oxidative stress sigma-1 receptor superoxide dismutase traumatic brain injury
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In situ modifed screen printed and carbon paste ion selective electrodes for potentiometric determination of naphazoline hydrochloride in its formulation
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作者 Gehad G.Mohamed F.A.Nour El-Dien +1 位作者 Eman Y.Z.Frag Marwa El-Badry Mohamed 《Journal of Pharmaceutical Analysis》 SCIE CAS 2013年第5期367-375,共9页
The construction and performance characteristics of new sensitive and selective in situ modified screen printed (ISPE) and carbon paste (ICPE) electrodes for determination of naphazoline hydrochloride (NPZ-HC1) ... The construction and performance characteristics of new sensitive and selective in situ modified screen printed (ISPE) and carbon paste (ICPE) electrodes for determination of naphazoline hydrochloride (NPZ-HC1) have been developed. The electrodes under investigation show potentiometric response for NPZ-HC1 in the concentration range from 7.0 x 10-7 to 1.0 x 10-2 M at 25 ~C and the electrode response is independent of pH in the range of 3.1-7.9. These sensors have slope values of 59.7+0.6 and 59.2+0.2 mV decade-l with detection limit values of 5.6 ~ 10-7 and 5.9 x 10-7 M NPZ- HC1 using ISPE and ICPE, respectively. These electrodes show fast response time of 4-7 s and 5-8 s and exhibits lifetimes of 28 and 30 days for ISPE and ICPE, respectively. Selectivity for NPZ-HC1 with respect to a number of interfering materials was also investigated. It was found that there is no interference from the investigated inorganic cations, anions, sugars and other pharmaceutical excipients. The proposed sensors were applied for the determination of NPZ-HC1 in pharmaceutical formulation using the direct potentiometric method. It showed a mean average recovery of 100.2% and 102.6% for ISPE and ICPE, respectively. The obtained results using the proposed sensors were in good agreement with those obtained using the official method. The proposed sensors show significantly high selectivity, response time, accuracy, precision, limit of detection (LOD)and limit of quantification (LOQ) compared with other proposed methods. 展开更多
关键词 ISPE and ICPE POTENTIOMETRY naphazoline hydrochloride Eye drops
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Design and optimization of a greener sinomenine hydrochloride preparation process considering variations among different batches of the medicinal herb 被引量:1
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作者 Dandan Ren Jiale Xie +2 位作者 Tianle Chen Haibin Qu Xingchu Gong 《Chinese Journal of Chemical Engineering》 SCIE EI CAS CSCD 2024年第7期77-90,共14页
The current methods used to industrially produce sinomenine hydrochloride involve several issues,including high solvent toxicity,long process flow,and low atomic utilization efficiency,and the greenness scores of the ... The current methods used to industrially produce sinomenine hydrochloride involve several issues,including high solvent toxicity,long process flow,and low atomic utilization efficiency,and the greenness scores of the processes are below 65 points.To solve these problems,a new process using anisole as the extractant was proposed.Anisole exhibits high selectivity for sinomenine and can be connected to the subsequent water-washing steps.After alkalization of the medicinal material,heating extraction,water washing,and acidification crystallization were carried out.The process was modeled and optimized.The design space was constructed.The recommended operating ranges for the critical process parameters were 3.0–4.0 h for alkalization time,60.0–80.0℃ for extraction temperature,2.0–3.0(volume ratio)for washing solution amount,and 2.0–2.4 mol·L^(-1) for hydrochloric acid concentration.The new process shows good robustness because different batches of medicinal materials did not greatly impact crystal purity or sinomenine transfer rate.The sinomenine transfer rate was about 20%higher than that of industrial processes.The greenness score increased to 90 points since the novel process proposed in this research solves the problems of long process flow,high solvent toxicity,and poor atomic economy,better aligning with the concept of green chemistry. 展开更多
关键词 Sinomenine hydrochloride Process optimization ANISOLE
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Carbon-doped CuFe_(2)O_(4) with C-O-M channels for enhanced Fenton-like degradation of tetracycline hydrochloride: From construction to mechanism 被引量:1
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作者 Hong Qin Yangzhuo He +9 位作者 Piao Xu Yuan Zhu Han Wang Ziwei Wang Yin Zhao Haijiao Xie Quyang Tian Changlin Wang Ying Zeng Yicheng Li 《Green Energy & Environment》 SCIE EI CAS CSCD 2024年第4期732-747,共16页
Carbon-doped copper ferrite(C–CuFe_(2)O_(4))was synthesized by a simple two-step hydrothermal method,which showed enhanced tetracycline hydrochloride(TCH)removal efficiency as compared to the pure CuFe_(2)O_(4) in Fe... Carbon-doped copper ferrite(C–CuFe_(2)O_(4))was synthesized by a simple two-step hydrothermal method,which showed enhanced tetracycline hydrochloride(TCH)removal efficiency as compared to the pure CuFe_(2)O_(4) in Fenton-like reaction.A removal efficiency of 94%was achieved with 0.2 g L^(-1) catalyst and 20 mmol L^(-1) H_(2)O_(2) within 90 min.We demonstrated that 5%C–CuFe_(2)O_(4) catalyst in the presence of H_(2)O_(2) was significantly efficient for TCH degradation under the near-neutral pH(5–9)without buffer.Multiple techniques,including SEM,TEM,XRD,FTIR,Raman,XPS M€ossbauer and so on,were conducted to investigate the structures,morphologies and electronic properties of as-prepared samples.The introduction of carbon can effectively accelerate electron transfer by cooperating with Cu and Fe to activate H_(2)O_(2) to generate·OH and·O_(2)^(-).Particularly,theoretical calculations display that the p,p,d orbital hybridization of C,O,Cu and Fe can form C–O–Cu and C–O–Fe bonds,and the electrons on carbon can transfer to metal Cu and Fe along the C–O–Fe and C–O–Cu channels,thus forming electron-rich reactive centers around Fe and Cu.This work provides lightful reference for the modification of spinel ferrites in Fenton-like application. 展开更多
关键词 Fenton-like reaction CuFe_(2)O_(4) Tetracycline hydrochloride degradation
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Benzydamine hydrochloride ameliorates ethanol-induced inflammation in RAW 264.7 macrophages by stabilizing redox homeostasis
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作者 Tiasha Dasgupta Venkatraman Manickam 《Asian Pacific Journal of Tropical Biomedicine》 SCIE CAS 2024年第2期73-81,I0006-I0009,共13页
Objective:To evaluate the protective effect of benzydamine hydrochloride against ethanol-induced oxidative stress and inflammation in RAW 264.7 macrophages.Methods:RAW 264.7 macrophages were treated with ethanol(100 m... Objective:To evaluate the protective effect of benzydamine hydrochloride against ethanol-induced oxidative stress and inflammation in RAW 264.7 macrophages.Methods:RAW 264.7 macrophages were treated with ethanol(100 mM)and benzydamine hydrochloride(7.5μM).The imflammatory status was confirmed by measuring pro-(TNF-αand IL-6)and anti-inflammatory(IL-10)cytokines through ELISA and RT-PCR assays.Reactive oxygen species generation and mitochondrial membrane potential were investigated to study the protective role of benzydamine hydrochloride against ethanol-induced oxidative stress.Apoptosis detection was also investigated using flow cytometry and acridine orange/ethidium bromide staining.Results:Benzydamine hydrochloride significantly decreased the secretion of TNF-αand IL-6,as well as the generation of reactive oxygen species inside the cells,thereby stabilizing the mitochondrial membrane potential and reducing DNA fragmentation.The ethanol-induced cellular necrosis was also reversed by the administration of benzydamine hydrochloride.Conclusions:Benzydamine hydrochloride ameliorates ethanol-induced cell apoptosis and inflammation in RAW macrophages. 展开更多
关键词 ALCOHOL Benzydamine hydrochloride INFLAMMATION Oxidative stress Apoptosis
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Method Verification and Validation of Hydralazine Hydrochloride: Spectrophotometric Analysis in Pure and Pharmaceutical Formulations
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作者 Laila Abdullah Alshatti 《American Journal of Analytical Chemistry》 CAS 2024年第7期219-228,共10页
The new method proposed is based on the formation of hydralazine-Bromophenol blue ion pair simply and without further extraction or heating. The ion pair was prepared in the presence of pH 3 citrate buffer forming a y... The new method proposed is based on the formation of hydralazine-Bromophenol blue ion pair simply and without further extraction or heating. The ion pair was prepared in the presence of pH 3 citrate buffer forming a yellow-colored chromogen. A new maximum UV-visible band formed at 416 nm. The color was stable for more than 10 hours and obeyed Beer’s Law over the concentration range of 10 - 50 µg/mL. The calculated molar absorptivity and Sandell’s sensitivity were 1.01 × 104 L∙mol−1∙cm−1 and 0.0514 µg/mL, respectively. The elements of method validation stipulated by The International Conference on Harmonization [Q2 (R1)] were applied for hydralazine hydrochloride assay in pure and pharmaceutical tablet formulation. The average recoveries of the pure solution and the pharmaceutical formulation were 98.94% and 99.50%, respectively. The results were statistically compared by F-test, which indicates that the method can be precise and repeatable for both pure and pharmaceutical solutions. The method was found to be accurate, reproducible, and cost-effective, and validated for the assay of hydralazine in terms of the routine quality control. 展开更多
关键词 SPECTROPHOTOMETRY Validation Hydralazine hydrochloride International Conference on Harmonization Q2 (R1)
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Clinical effect of acupuncture at ghost points combined with fluoxetine hydrochloride on mild-to-moderate depression
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作者 Yi Wang Qun Lu +5 位作者 Ittipalanukul Penpat Juan Wu Dilinuer Abulikemu Fei-Cui Zeng Jia-Ying Huang Zhi-Hai Hu 《World Journal of Psychiatry》 SCIE 2024年第6期848-856,共9页
BACKGROUND Depression is a common,chronic,and recurrent mood disorder that has become a worldwide health hazard.Fluoxetine hydrochloride,a common treatment method,can inhibit 5-hydroxytryptamine(5-HT)recycling in the ... BACKGROUND Depression is a common,chronic,and recurrent mood disorder that has become a worldwide health hazard.Fluoxetine hydrochloride,a common treatment method,can inhibit 5-hydroxytryptamine(5-HT)recycling in the presynaptic membrane;however,the efficacy of a single drug is inadequate.At present,mildto-moderate depression can be treated with acupuncture of ghost caves,but the clinical curative effect of combined therapy with fluoxetine hydrochloride has not been sufficiently reported.AIM To evaluate the clinical effect of acupuncture at ghost points combined with fluoxetine hydrochloride in the treatment of mild-to-moderate depression.METHODS This retrospective study included 160 patients with mild-to-moderate depression who were admitted to Shanghai Hospital of Integrated Traditional Chinese and Western Medicine,Affiliated to Shanghai University of Traditional Chinese Medicine,between January 2022 and June 2023.Patients were separated into a single-agent group(fluoxetine hydrochloride treatment,n=80)and a coalition group(fluoxetine hydrochloride treatment combined with acupuncture at ghost points,n=80).Pre-treatment symptoms were recorded,and the clinical curative effect and adverse reactions[Asberg Antidepressant Side Effects Scale(SERS)]were assessed.Depression before and after treatment[Hamilton Depression Scale(HAMD)-24],neurotransmitter levels[5-HT,norepinephrine(NE),dopamine(DA)],oxidative stress indicators[superoxide dismutase(SOD),malondialdehyde(MDA)],and sleep quality[Pittsburgh Sleep Quality Index(PSQI)]were compared.RESULTS The total efficacy rate was 97.50%in the coalition group and 86.25%in the single-agent group(P<0.05).After 2,4,6,and 8 wk of treatment,the HAMD,self-rating depression scale,and SERS scores of the coalition and single-agent groups decreased compared with pre-treatment,and the decrease was more significant in the coalition group(P<0.05).After 8 wk of treatment,the levels of NE,DA,5-HT,and SOD in the coalition and single-agent groups increased,while the levels of MDA decreased;the increases and decrease in the coalition group were more significant(P<0.05).The PSQI scores of the coalition and single-agent groups decreased,and the decrease was more significant in the coalition group(P<0.05).CONCLUSION Acupuncture at ghost points combined with paroxetine tablets can safely improve depressive symptoms and sleep disorders,regulate neurotransmitter levels,and reduce stress responses in patients with mild-to-moderate depression. 展开更多
关键词 DEPRESSION PRICK Fluoxetine hydrochloride Curative effect Depressive symptoms Oxidative stress index
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Analysis of the Efficacy of Atomoxetine Hydrochloride Combined with Psycho-Behavioral Modification Therapy in the Treatment of ADHD in Children
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作者 Nan Li 《Journal of Clinical and Nursing Research》 2024年第4期137-142,共6页
Objective: To evaluate the therapeutic efficacy of atomoxetine hydrochloride (ATX) combined with psychological-behavioral modification therapy for attention-deficit/hyperactivity disorder (ADHD) in children. Methods: ... Objective: To evaluate the therapeutic efficacy of atomoxetine hydrochloride (ATX) combined with psychological-behavioral modification therapy for attention-deficit/hyperactivity disorder (ADHD) in children. Methods: A total of 60 cases of ADHD children admitted to our hospital between November 2021 and November 2022 were selected and randomly grouped into Group I and Group II. There were 30 cases in Group I who were treated with ATX combined with psychological-behavioral modification therapy. There were 30 cases in Group II who were treated with ATX monotherapy, and the therapeutic effects were compared. Results: Before treatment, there was no difference in the behavioral problem scores and cognitive function indexes of the two groups (P>0.05). After treatment, the behavioral problem scores of Group I were lower than those of Group II, and the cognitive function indicators of Group I were lower than those of Group II (P < 0.05). The adverse reaction rate of Group I was lower than that of Group II, and the total effective rate was higher than that of Group II (P < 0.05). Conclusion: ATX combined with psychological-behavioral modification therapy improved the behavioral problems of ADHD children, enhanced their cognitive function, and reduced the adverse reactions to drug treatment. 展开更多
关键词 Atomoxetine hydrochloride Psycho-behavioral modification therapy ADHD in children
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Clinical Study on the Treatment of Senile Alzheimer’s Dementia with Sodium Oligomannate Combined with Memantine Hydrochloride
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作者 Jian Zhao Xi Li +1 位作者 Xuelian Jia Ganke Gao 《Journal of Clinical and Nursing Research》 2024年第10期208-217,共10页
Objective:To analyze the clinical effects of sodium oligomannate combined with memantine hydrochloride in the treatment of senile Alzheimer’s dementia.Methods:Sixty-eight cases of Alzheimer’s dementia treated at the... Objective:To analyze the clinical effects of sodium oligomannate combined with memantine hydrochloride in the treatment of senile Alzheimer’s dementia.Methods:Sixty-eight cases of Alzheimer’s dementia treated at the Second People’s Hospital of Fujian University of Traditional Chinese Medicine from March 2020 to March 2022 were selected as the study subjects.The patients were divided into two groups based on different treatment methods:the control group(treated with memantine hydrochloride,34 cases)and the treatment group(treated with sodium oligomannate+memantine hydrochloride,34 cases).Cognitive function,activities of daily living,neurotransmitters,serum intestinal flora metabolic markers,inflammatory factors,neurotrophic factors,and adverse reactions were compared between the two groups.Results:The treatment group showed better cognitive function,quality of life scores,and levels of relevant metabolic markers in the body compared to the control group,with statistically significant differences(P<0.05).The incidence of adverse reactions between the two groups(treatment group:2%;control group:4%)was not statistically significant(χ^(2)=0.731,P=0.393).Conclusion:Sodium oligomannate combined with memantine hydrochloride has better efficacy than the control group for treating senile Alzheimer’s dementia.It significantly improves and restores cognitive function and daily living abilities,benefits neurotransmitter secretion and internal regulation,upregulates the expression of neurotrophic factors,and has fewer adverse reactions,making it a treatment worthy of further clinical promotion and application. 展开更多
关键词 Senile Alzheimer’s dementia Sodium oligomannate Memantine hydrochloride Cognitive function TREATMENT
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Fluoxetine Hydrochloride的NMR数据解析 被引量:1
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作者 吴鸣建 赵天增 张海艳 《波谱学杂志》 CAS CSCD 北大核心 2007年第3期297-301,共5页
由美国Lilly公司开发的第二代抗抑郁症药物盐酸氟西汀(Fluoxetine hydrochloride),属于选择性5-羟色胺再摄取抑制剂(SSRI),除了用于治疗各类抑郁症,包括轻性或重性抑郁症,尤宜用于老年性抑郁症之外,对于强迫症、惊恐发作、贪食症、经前... 由美国Lilly公司开发的第二代抗抑郁症药物盐酸氟西汀(Fluoxetine hydrochloride),属于选择性5-羟色胺再摄取抑制剂(SSRI),除了用于治疗各类抑郁症,包括轻性或重性抑郁症,尤宜用于老年性抑郁症之外,对于强迫症、惊恐发作、贪食症、经前期焦虑等亦有很好疗效.Fluoxetine hydrochloride是一种双环化合物,与传统的三环类、杂环类或单胺氧化酶抑制剂抗抑郁药相比,具有疗效好、不良反应轻而少,安全性高、耐受性好等特点,目前已作为一线的抗抑郁药得到广泛应用.本文对Fluoxetine hydrochloride进行了1H NMR和13C NMR检测,并通过DEPT和1H-1HCOSY、HMBC、HSQC等2D NMR技术对其1H NMR和13C NMR数据进行了较为详细的解析和比文献[1]更为全面的NMR归属,为以后的分析鉴定提供更完善的依据. 展开更多
关键词 NMR 归属 2D NMR FLUOXETINE hydrochloride
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Development of Prolonged Release Microspheres of Metformin Hydrochloride Using Ion Exchange Resins 被引量:1
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作者 刘宏飞 苏显英 +3 位作者 李想 赵欣 臧蕾 潘卫三 《Journal of Chinese Pharmaceutical Sciences》 CAS 2006年第3期155-161,共7页
Aim To prepare the prolonged-released microspheres of mefformin hydrochloride. Methods Ion-exchange resin-drug mefformin hydrochloride complexes were prepared as core materials, and followed by coating using ethylcell... Aim To prepare the prolonged-released microspheres of mefformin hydrochloride. Methods Ion-exchange resin-drug mefformin hydrochloride complexes were prepared as core materials, and followed by coating using ethylcellulose (EC) by the emulsion solvent diffusion technique. The release rate of mefformin from the microcapsules was highly dependent on the encapsulating formulation, thus being used as an index for formulation screening. Orthogonal experiments were performed to optimize the coating formulation. Results The final chosen formulation for coating of mefformin microcapsules were as follows: ( 1 ) the ratio of EC (20cps) to EC (45cps) was 50:50; (2) the ratio of plasticizer to coating materials was 20% ;and (3) the ratio of resin-mefformin complexes to coating materials was 5 : 1. Conclusion The prolonged release microspheres of mefformin hydrochloride were successfully prepared. 展开更多
关键词 metformin hydrochloride ion exchange resin emulsion solvent diffusion technique sustained-release microcapsule
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Influence of pH Environment on Nasal Absorption of Meptazinol Hydrochloride 被引量:1
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作者 史振祺 蒋新国 《Journal of Chinese Pharmaceutical Sciences》 CAS 2004年第1期32-36,共5页
Aim To investigate the relationship between pH environment of meptazinolhydrochloride (MEP) and its nasal absorption. Methods In situ nasal peifusion was performed to studythe effect of pH environment on the nasal abs... Aim To investigate the relationship between pH environment of meptazinolhydrochloride (MEP) and its nasal absorption. Methods In situ nasal peifusion was performed to studythe effect of pH environment on the nasal absorption. Its effect on the transport from nose tobrain was further researched by in vivo experiment. Results In in situ perfusion experiment, thenasal absorption of MEP in basic environment was significantly higher than that in acid condition,but the difference was not observed in in vivo experiment. Conclusion The pH environment ofmeptazinol hydrocloride in formulation cannot be regarded as an important factor influencing nasalabsorption and transport from nose to brain. 展开更多
关键词 nasal absorption pH environment lipophilic drug meptazinol hydrochloride
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The Study of Dipivefrin Hydrochloride Ophthalmic Gel 被引量:1
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作者 王丽茹 张强 《Journal of Chinese Pharmaceutical Sciences》 CAS 2001年第3期128-132,共5页
Dipivefrin hydrochloride ophthalmic gel was prepared and the release test and the isolated cornea permeation test of the formulation in vitro were investigated. The release test of the formulation was studied by using... Dipivefrin hydrochloride ophthalmic gel was prepared and the release test and the isolated cornea permeation test of the formulation in vitro were investigated. The release test of the formulation was studied by using permeable membrane. The content and the release amount of Dipivefrin hydrochloride from the gel base were measured by high performance liquid chromatography. The cornea permeation test of the formulation was studied by using isolated rabbit corneas. The formulation release behavior in vitro followed the first-order kinetic equation. The release amount of Dipivefrin hydrochloride raised significantly with less polymer in the formulation. The cornea permeation behavior of the drug in vitro followed the first-order kinetic equation. The eye irritancy of Dipivefrin hydrochloride gel is lower than that of eyedrops. 展开更多
关键词 Dipivefrin hydrochloride GEL HPMC Release in vitro HPLC Isolated cornea per-meation.
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治疗睡眠障碍新药——盐酸达利雷生(daridorexant hydrochloride) 被引量:5
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作者 陈本川 《医药导报》 CAS 北大核心 2022年第9期1401-1406,I0001,共7页
治疗睡眠障碍新药盐酸达利雷生片(daridorexant hydrochloride tablets,简称达利雷生)于20世纪90年代末由强生制药(J.&J.)有限公司并购的瑞士Actelion生物制药公司开始研发,2017年6月Actelion生物制药公司将新药发现和药物的早期临... 治疗睡眠障碍新药盐酸达利雷生片(daridorexant hydrochloride tablets,简称达利雷生)于20世纪90年代末由强生制药(J.&J.)有限公司并购的瑞士Actelion生物制药公司开始研发,2017年6月Actelion生物制药公司将新药发现和药物的早期临床开发资产从强生制药有限公司剥离,注入新成立的瑞士Idorsia生物制药公司;2019年12月,Idorsia生物制药公司与日本持田制药公司签订独家协议,将共同开发、营销和供应达利雷生片。达利雷生是双重食欲素受体拮抗药,通过阻断食欲素受体与促觉醒神经肽食欲素的结合,抑制过度活跃的不眠状态。临床试验受试者包含多种形式睡眠障碍,如入睡困难、早醒、睡眠维持困难、睡眠质量下降、睡眠结构紊乱等。结果表明,达利雷生治疗组患者进入持续性睡眠所需时间(LPS)和入睡后觉醒(WASO)的变化均优于安慰药组。达利雷生能显著改善患者入睡和睡眠维持的客观指标,以及患者报告的总睡眠时间(sTST);并能减少患者次日嗜睡情况。2020年8月,Idorsia生物制药公司与美国跨国合同研究组织(Syneos Health)在美国的商业化签订营销协议Actelion生物制药公司与日本持田制药公司于2021年8月联合向美国食品药品管理局(FDA)提出新药上市申请。FDA于2022年1月7日批准其上市,商品名为QUVIVIQ^(■)。该文对治疗睡眠障碍新药达利雷生片的非临床和临床药理毒理学、临床研究、不良反应、适应证、剂量与用法、用药注意事项及知识产权状态和国内外研究进展等进行介绍。 展开更多
关键词 达利雷生 盐酸 daridorexant hydrochloride 双重食欲素受体拮抗药 睡眠障碍 失眠症
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Study of Sustained Release Phenylpropanolamine Hydrochloride Hydrophilic Matrix Tablets Containing Hydroxypropylmethylcellulose K100M and Carbopol 971P 被引量:1
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作者 吕丹 裴元英 《Journal of Chinese Pharmaceutical Sciences》 CAS 2000年第4期185-190,共6页
选用HPMC K100M和卡波普971P为骨架材料,粉末直接压片法制备骨架片,考察释放度,反相高效液相色谱法检测盐酸苯丙醇胺(PPA·HCl)的浓度。释药曲线均符合Higuchi方程(R>0.98,P<0.01)。运用正交设计法,以美国市场的PPA&#... 选用HPMC K100M和卡波普971P为骨架材料,粉末直接压片法制备骨架片,考察释放度,反相高效液相色谱法检测盐酸苯丙醇胺(PPA·HCl)的浓度。释药曲线均符合Higuchi方程(R>0.98,P<0.01)。运用正交设计法,以美国市场的PPA·HCl缓释片Acutrim^R为对照,相似因子f2值为指标,筛选获得了最优处方。其工艺重现性合格。研制片在0.1mol·L^-1 HCl,H2O(pH6.5),磷酸盐缓冲液(PBS)pH5.0,6.8和7.4的介质中,以及在0.1mol·L^-1HCl中释放2h,转移至PBS6.8中释放10h,相对于对照品的f2值为63-74,表明在各介质中两制剂的释药曲线相似。释药影响因素的考察结果表明:在本实验考察的范围内,骨架片在水中的释药速率与HPMC K100M和卡波普971P的用量呈负相关。HPMC K100M和卡波普971P的比例(保持聚合物总用量相同),硬脂酸镁量和骨架片硬度对释药速率无显著性影响。 展开更多
关键词 Hydroxypropylmethylcellulose(HPMC K100M) Carbopol 971P Phenylpropanolamine hydrochloride Hydrophilic sustained release matrix tablets Similarity factor
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Development and Validation of an HPLC Method for the Determination of Bupropion Hydrochloride in Tablets
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作者 齐美玲 王鹏 +2 位作者 耿颖姝 顾峻岭 傅若农 《Journal of Chinese Pharmaceutical Sciences》 CAS 2002年第1期16-18,共3页
A rapid, accurate and sensitive HPLC method for the determination of bupropion hydrochloride in a new tablet formulation is described. Chromatographic separation of bupropion hydrochloride is achieved using a mobile p... A rapid, accurate and sensitive HPLC method for the determination of bupropion hydrochloride in a new tablet formulation is described. Chromatographic separation of bupropion hydrochloride is achieved using a mobile phase consisting of methanol -0.01 mol·L -1 ammonium dihydrogen phosphate (80:20, v/v, pH 4.8) at a flow rate of 1.0 mL·min -1 on a Hypersil BDS C18 column. Absorbance is monitored at 251 nm where bupropion hydrochloride has maximum absorption in the mobile phase. The linear range of determination for bupropion hydrochloride is between 2.12 and 21.2 μg·mL -1. The proposed method was validated with respect to accuracy, precision, limits of detection and quantification and robustness, etc. 展开更多
关键词 HPLC Bupropion hydrochloride TABLETS
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Simultaneous Determination of Ticlopidine Hydrochloride and Nitrendipine in a New Tablet Formulation by HPLC
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作者 齐美玲 王鹏 顾峻岭 《Journal of Beijing Institute of Technology》 EI CAS 2002年第4期378-382,共5页
An accurate, simple and sensitive high performance liquid chromarographic (HPLC) method for simultaneous determination of ticlopidine hydrochloride and nitrendipine in a new tablet formulation is described. Chromatogr... An accurate, simple and sensitive high performance liquid chromarographic (HPLC) method for simultaneous determination of ticlopidine hydrochloride and nitrendipine in a new tablet formulation is described. Chromatographic separation of ticlopidine hydrochloride and nitrendipine was achieved on a Hypersil BDS C18 column using a mobile phase consisting of acetonitrile-methanol-10 mmol/L ammonium acetate (60∶10∶30(V/V), pH 6.5) at a flow rate of 1.0 mL/min. Absorbance was monitored at 236 nm where both drugs have significant absorption. The proposed method was validated with respect to linearity, selectivity, accuracy, precision, and limits of detection and quantitation. The linear ranges for ticlopidine hydrochloride and nitrendipine were found to be 75-750 μg/mL and 1-10 μg/mL, respectively. The mean recoveries were 100.1%(S R=0.6%,n=9) for ticlopidine hydrochloride and 99.9%(S R=0.7%,n=9) for nitrendipine. The within-day precision and between-day precision for ticlopidine hydrochloride and nitrendipine were 0.63% and 0.89%, and 0.74% and 1.0%, respectively. The proposed HPLC method can be used for the simultaneous determination of both drugs in pharmaceutical preparations. 展开更多
关键词 HPLC DETERMINATION ticlopidine hydrochloride NITRENDIPINE
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Determination of penehyclidine hydrochloride in beagle dog plasma by liquid chromatography-electrospray ionization mass spectrometry and the pharmacokinetic study
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作者 崔彦 尹海林 +3 位作者 包旭 熊梅瑾 陈聪 叶利明 《Journal of Chinese Pharmaceutical Sciences》 CAS 2008年第2期122-128,共7页
To develop a fast and sensitive liquid chromatography-mass spectrometry method for the determination of penehyclidine hydrochloride (PH) in beagle dog plasma. PH and diphenhydramine hydrochloride (internal standard... To develop a fast and sensitive liquid chromatography-mass spectrometry method for the determination of penehyclidine hydrochloride (PH) in beagle dog plasma. PH and diphenhydramine hydrochloride (internal standard, IS) were extracted with a solvent mixture of petroleum ether-ethyl ether (7:3). Chromatographic separation was achieved on a reversed-phase Eclipse XDB-C18 column (4.6 mm × 150 mm, 5 um) using the eluent of methanol-water (5 mmol/L ammonium acetate) (90:10, v/v, pH 5.8) as mobile phase. The electrospray ionization source was set at the positive multiple reaction monitoring (MRM) mode. This method involved the use of the [M+H]^+ ions of PH and diphenhydramine hydrochloride at m/z 316.4- 128.2 and m/z 256.4-167.2. The calibration curve was linear in the range of 1-1000 ng/mL with a correlation coefficient of 0.9988. The lower limit of quantification was 0.05 ng/mL. The precision, accuracy and recovery of the method were acceptable. Following intravenous injection admires' tration at doses of 0.5, 1 and 5 mg/kg PH, the main pharmacokinetic parameters were as the followings, t1/2a 0.33 h, t1/2β 2.44 1% tmax 0.058 1% AUC and Cmax exhibited a linear increase along with the increase of dose. The two-compartment model fit the three dose groups. This method was sensitive, accurate and fast for the determination of concentration of PH in beagle dog plasma. It could be used in pharmacokinetic studies of PH. 展开更多
关键词 Liquid chromatography-mass spectrometry-mass spectrometry Penehyclidine hydrochloride Eleetrospray ionization PHARMACOKINETICS
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治疗儿童和青少年注意力缺陷多动症--盐酸维洛沙嗪(viloxazine hydrochloride)缓释胶囊 被引量:2
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作者 陈本川 《医药导报》 CAS 北大核心 2021年第12期1785-1792,I0001,共9页
盐酸维洛沙嗪(viloxazine hydrochloride)是去甲肾上腺素再摄取抑制药,作为治疗儿童和青少年注意力缺陷多动障碍(ADHD)的非兴奋药,由美国专门从事中枢神经系统疾病治疗药物的Supernus制药公司自主研发。20世纪60—70年代,Supernus制药... 盐酸维洛沙嗪(viloxazine hydrochloride)是去甲肾上腺素再摄取抑制药,作为治疗儿童和青少年注意力缺陷多动障碍(ADHD)的非兴奋药,由美国专门从事中枢神经系统疾病治疗药物的Supernus制药公司自主研发。20世纪60—70年代,Supernus制药公司将盐酸维洛沙嗪研制成速释胶囊,用于治疗抑郁症,在英国和欧洲其他几个国家上市销售,因治疗服药剂量大,疗效难于与同类药物相似,撤出市场。Supernus制药公司转为开发新的缓释胶囊剂,主攻治疗儿童和青少年ADHD,经多批次Ⅲ期临床试验,取得良好疗效,均达到治疗终点,且有广泛的安全性。Supernus制药公司原订计划于2010年1月向美国FDA提交盐酸维洛沙嗪缓释胶囊用于治疗6~17岁儿童和青少年ADHD适应证新药上市申请(NDA),因该公司内部药物分析部门搬迁新址,分析数据未能满足NDA申请要求,收到FDA完整回函(CRL)。经协商,研发公司于2021年2月2日重新补充全部申报资料。美国食品药品管理局(FDA)于2021年4月2日正式批准盐酸维洛沙嗪缓释胶囊上市,商品名为Qelbree。这是近十年来FDA批准的首个针对ADHD的新型非刺激性疗法。而盐酸维洛沙嗪缓释胶囊在ADHD成人中进行的Ⅲ期临床试验研究也于2020年12月取得积极结果,按计划Supernus公司将于2021年下半年递交针对成人ADHD的补充NDA。该文对盐酸维洛沙嗪缓释胶囊的非临床和临床药理毒理学、临床研究、不良反应、适应证、剂量与用法、用药注意事项及知识产权状态和国内外研究进展等进行介绍。 展开更多
关键词 盐酸维洛沙嗪 viloxazine hydrochloride 缓释胶囊 注意力缺陷多动症 注意力缺陷多动障碍/儿童和青少年
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Electrodeposition of aluminium and aluminium-copper alloys from a room temperature ionic liquid electrolyte containing aluminium chloride and triethylamine hydrochloride 被引量:10
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作者 P.V. Suneesh T.G. Satheesh Babu T. Ramachandran 《International Journal of Minerals,Metallurgy and Materials》 SCIE EI CAS CSCD 2013年第9期909-916,共8页
The electrodeposition of A1 and A1-Cu binary alloys on to gold substrates from a room temperature ionic liquid electrolyte containing A1C13-EtaNHC1 was studied. The electrochemical behavior of the electrolyte and the ... The electrodeposition of A1 and A1-Cu binary alloys on to gold substrates from a room temperature ionic liquid electrolyte containing A1C13-EtaNHC1 was studied. The electrochemical behavior of the electrolyte and the mechanism of deposition were investigated through cyclic voltammetry (CV), and the properties of deposits obtained were assessed by scanning electron microscopy with energy dispersive X-ray spectroscopy (SEM-EDS) and X-ray diffraction (XRD). A1 of 70μm in thickness and an A1-Cu alloy of 30μm in thickness with 8at% copper were deposited from the electrolyte. SEM images of the deposits indicate that the A1 deposit was smooth and uniform, whereas the Al-Cu deposit was nodular. The average crystalline size, as determined by XRD patterns, was found to be (30±5) and (29±5) nm, respectively, for A1 and A1-Cu alloys. Potentiodynamic polarization (Tafel plots) and electrochemical impedance spectroscopic (EIS) measurements showed that Al-Cu alloys are more corrosion resistant than Al. 展开更多
关键词 ELECTRODEPOSITION aluminium copper alloys ionic liquids triethylamine hydrochloride copper acetylacetonate
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