盐酸丁卡因滴眼液的稳定性研究

目的 :考察 1 %盐酸丁卡因滴眼液的稳定性 ,确定其有效贮存期。方法 :采用经典恒温法预测其有效期。结果 :经典恒温法[1 ] 预测室温贮存期约为 2 0d ,冰箱贮存期约为 1 1 0d。结论 :该制剂对热不稳定 ,应冷藏。     

The depressing effect of tetracaine and ryanodine on the slow outward current correlated with that of contraction in voltage-clamped frog muscle fibres

The effects of tetracaine (10–50 M) and ryanodine (0.1–10 M) were tested on the slow outward K⁺ current (I _so) and the mechanical tension of isolated frog muscle fibres in a voltage-clamp device (double mannitol-gap) connected to a mechanoelectric transducer. In the concentration range tested, both drugs induced a simultaneous inhibition of tension and current. In all cases the effect on tension was twice that on current. The tetracaine-induced current and tension blocks were fully reversible and dose-dependent. In contrast the ryanodine effects on current and tension were not reversible and did not exhibit a dose dependence except for the delay before the onset of the response, which was shortened when the concentration was raised. Linear regression analysis of the time-dependent and dose-dependent effects of both drugs indicated a strong correlation between the decreases in tension and current. It is concluded that the slow outward current is partly under the control of the Ca²⁺ release from sarcoplasmic reticulum during contraction.     

反相高效液相色谱法同时测定盐酸丁卡因胶浆中2组分的含量

目的:建立以反相高效液相色谱法同时测定盐酸丁卡因胶浆中盐酸丁卡因和羟苯乙酯含量的方法。方法:色谱柱为C8,流动相为甲醇-无水乙醇-水-三乙胺(70∶15∶15∶0.05) ,检测波长为280nm。结果:盐酸丁卡因与羟苯乙酯的检测浓度线性范围分别为10～50μg/ml(r=0. 9997)、2～10μg/ml(r=0 .9999) ;平均回收率分别为100.82 %、100.16 %。结论:本方法简便、快速、准确,适用于盐酸丁卡因胶浆的质量控制。     

Biodegradable poly(DL-lactic-co-glycolic acid) microspheres containing tetracaine hydrochloride. In-vitro release profile

Tetracaine does not result in effective treatment of intractable pain caused by trigeminal neuralgiabecause of its short duration of effect. In asustained release system a controlled delivery of the drug at the site of administration, would avoid successive administrations. Tetracaine hydrochloride (HCl) has been encapsulated using a technique based on the evaporation of solvent from an O/O emulsion, using poly(dl-lactic-co-glycolic acid) (PLGA) 50:50. Microspheres were separated into three fractions: 106-212, 212-300 and 300-425mum. The effects of two variables of the manufacturing method (volume of the inner phase of the emulsion and volume of surfactant added to the external phase) on the drug loading into microspheres, dissolution profiles and SEM characterization of the microspheres were evaluated. Microspheres containing tetracaine hydrochloride (up to94% referred tothe theoretical) released the drug, in-vitro, over 35 days. Tetracaine HCl was delivered according to zero order kinetics from day 5 until the end of the release assay. The rate of drug release depended mainly on the viscosity of the discontinuous phase and on the size of microparticles. Microsphere size resulted more homogeneous when using the highest volume of the surfactant, being almost 80% of microparticles within the range 212-300mum.     

国产盐酸丁卡因凝胶用于介入治疗动脉插管术前皮肤局部麻醉作用的临床研究

目的 研究盐酸丁卡因凝胶用于介入治疗动脉插管术前的麻醉效果及临床安全性。方法 选取需行动脉穿刺插管病人40例。采用单盲随机平行对照观察方法分为两组。其中试验组和对照组各20例。用药后穿刺右股动脉，观察局部麻醉作用、插管时瞬间疼痛及不良反应。结果 两组病人局部麻醉作用显效率分别为85％、90％，有效率均为100％。插管时瞬间疼痛比较镇痛有效率分别为95％、100％。两组均未出现不良反应。结论 盐酸丁卡因凝胶麻醉效果好，操作简单，无创伤无痛苦，临床安全性好，无明显不良反应，可用于介入治疗动脉插管术前的局部麻醉。     

2％盐酸丁卡因溶液的稳定性预测及影响因素考察

目的研究2%盐酸丁卡因溶液的稳定性及影响因素。方法采用初均速法测定其在20℃时、含量下降5%的贮存期;并将成品在避光与室内光、低温与常温条件下进行留样观察,定期测定含量。结果2%盐酸丁卡因溶液在20℃、含量下降5%时的贮存期为13个月。在避光条件下贮存,其含量下降较室内光缓慢;在低温(8℃±1℃)条件下贮存,其含量下降较常温缓慢。结论2%盐酸丁卡因溶液的有效期可定为一年,以低温、避光贮存为宜。     

正交函数光谱法测定复方普鲁卡因注射液的含量

目的：测定复方普鲁卡因注射液中普鲁卡因的含量。方法：使用正交函数分光光度法。结果：盐酸普鲁卡因的平均回收率为１００．０４％,ＲＳＤ为０．１５％（ｎ＝６）。结论：样品不经分离直接测定,结果准确,可用于普鲁卡因制剂的快速质量检验。     

不同浓度罗哌卡因对幼兔脊髓和脊神经的毒性作用

目的 探讨不同浓度罗哌卡因对幼兔脊髓和脊神经的毒性作用.方法 日本大耳白幼兔120只,随机分为5组(n=24):0.9%生理盐水阴性对照组(S组)、2%丁卡因阳性对照组(T组)和0.25%、0.5%、0.75%罗哌卡因组(R1～3组).行L6,7穿刺后,各组于20 s内鞘内注人生理盐水、2%丁卡因或不同浓度罗哌卡因各0.2 ml.分别于鞘内给药后3、6 h、7 d时各取8只动物,行运动阻滞程度评估后处死,其中6只动物切取L5,6段脊髓,HE染色后光镜下观察脊髓病理学结果;TUNEL法检测细胞凋亡情况,计算细胞凋亡指数(AI);免疫组化法测定Bax蛋白和Bcl-2蛋白的表达水平.另2只动物切取L5,6段脊髓后角组织及神经根,透射电镜下观察脊髓和脊神经超微结构.结果 R3组可见神经胶质细胞核轻度固缩,T组脊髓出现典型凋亡细胞,其余各组脊髓和脊神经超微结构基本正常.与T组比较,R1～3>组运动阻滞显效时间延长(P<0.05);与R1组比较,R2,3组运动阻滞显效时间缩短(P<0.05). R<1～3>组与S组AI、Bax蛋白和Bcl-2蛋白表达水平差异无统计学意义(P>0.05);与T组比较,其余各组AI降低,Bax蛋白和Bcl-2蛋白表达下调(P<0.05).结论 0.25%～0.75%罗哌卡因对幼兔脊髓和脊神经无毒性作用;Bax蛋白和Bcl-2蛋白表达上调可能参与了脊髓和脊神经毒性作用的发生.     

曙红Y-盐酸丁卡因体系的同步荧光猝灭反应及其分析应用

目的在pH3.0的弱酸性介质中,盐酸丁卡因（TA.HCl）与曙红Y（EY）形成1∶1的离子缔合物,导致曙红Y溶液在521 nm处同步荧光猝灭（Δλ=25nm）。荧光猝灭值（ΔF）与TA.HCl浓度在0.18-3.0μg.mL^-1范围呈良好的线性关系。该方法灵敏度高,检出限为0.055μg.mL^-1。考察了共存物质的影响,表明方法有良好的选择性。据此发展了一种高灵敏、简便快速测定微量TA.HCl的新荧光分光光度法。该法用于人血清及尿样中盐酸丁卡的含量测定,结果满意。     

毛细管区带电泳法测定复方西吡氯铵含片中两组分的含量

目的　用毛细管区带电泳法测定复方西吡氯铵含片中氯化十六烷基吡啶和维生素C的含量。方法　用 30mmol·L-1硼砂 (pH 6 .5 ) -乙睛 (70∶30 )为运行缓冲液 ,以咖啡因为内标 ,分离电压 2 5kV ,在 2 5 4nm处检测氯化十六烷基吡啶 ,在 2 6 6nm处测定维生素C。结果　样品中各组分完全分离且呈良好线性关系 ,氯化十六烷基吡啶回收率为 99.14 % ,RSD =1.4 % (n =5 ) ,维生素C回收率为 99.2 1% ,RSD =1.5 % (n =5 )。结论　该法能消除大量辅料对测定的干扰 ,简单 ,分析时间短 ,结果准确