薄层色谱法检查注射用盐酸丁卡因中的有关物质的研究

目的 检查新药注射用盐酸丁卡因的有关物质。方法 现版中国药典与美国药典均采用TLC法。结果 强光照射试验后中国药典法未检出杂斑点而美国药典法能检出杂斑点。结论 采用美国药典法适用于注射用盐酸丁卡因有关物质的检出。     

丁卡因胶浆对全身麻醉拔管期血流动力学的影响

目的 研究丁卡因胶浆对全身麻醉拔管期血流动力学的影响.方法 将100例择期气管插管全身麻醉患者按随机数字表法分为对照组和试验组,每组50例.对照组在气管导管表面均匀涂抹无菌液态石蜡油,试验组于相同部位均匀涂抹丁卡因胶浆.记录麻醉诱导前（T1）、手术结束停止输注药物后5 min（T2）、拔管后1 min（T3）、拔管后3 min（T4）、拔管后5 min （T5）的收缩压、舒张压和心率,患者术后清醒时耐管效果,术后24h发生咽喉痛、声音嘶哑的例数.结果 两组T1、T2收缩压、舒张压、心率比较差异均无统计学意义（P＞0.05）;试验组T3 ～T5收缩压、舒张压、心率明显低于对照组[收缩压：（122.3±11.3）,（120.0±9.8）,（112.0±6.3） mmHg（1 mmHg =0.133 kPa）比（158.3±15.0）,（142.5±13.5）,（133.0±14.5） mmHg;舒张压：（75.0±13.5）,（75.8±10.5）,（58.3±4.2） mmHg比（111.0±20.3）,（106.5±12.8）,（63.8±15.8） mmHg;心率：（81.9±13.7）,（83.6±13.4）,（60.7±3.5）次/min比（113.5±19.4）,（117.5±21.7）,（71.8±14.6）次/min],差异均有统计学意义（P＜0.05）.试验组耐管总有效率明显高于对照组[96％（48/50）比56％（28/50）],咽喉痛和声音嘶哑发生率明显低于对照组[6％（3/50）比48％（24/50）和4％（2/50）比36％（18/50）],差异均有统计学意义（P＜0.05）.结论 丁卡因胶浆可以减轻全身麻醉患者拔管期血流动力学的剧烈波动,能增强患者对气管导管的耐受性,有效降低全身麻醉气管插管所引起的咽喉痛和声音嘶哑的发生率.     

丁卡因胶浆在经直肠前列腺穿刺活检中的临床应用价值

目的 比较患者在行经直肠前列腺穿刺活检术时,在直肠内及肛周使用丁卡因胶浆或单纯润滑剂,患者所经历的疼痛情况.方法 回顾性分析2011年1月至2013年1月120例行经直肠前列腺穿刺患者的临床资料.其中术中采用单纯性润滑剂患者60例（组Ⅰ）,采用丁卡因胶浆患者60例（组2）.采用水平视觉疼痛评分法评估患者经历的疼痛程度.结果 通过组间比较,两组患者疼痛程度与患者年龄、PSA水平、DRE是否异常、穿刺数目及术后并发症发生等均无统计学意义（P＞0.05）,当穿刺器械进入肛门时患者疼痛不适评分组1为2.8±1.8分,组2为1.3±1.6分（P=0.000＜0.05）,当行前列腺穿刺活检术时患者疼痛不适评分组1为5.5±1.7分,组2为3.3±1.5分（P=0.211 ＞0.05）.结论 麻药制剂并不能增加经直肠前列腺穿刺活检术的安全性,但采用麻药制剂（如丁卡因胶浆）后可明显减轻穿刺所带给患者的疼痛不适.     

丁卡因口腔粘附片的研制

目的:研制丁卡因口腔粘附片。考察不同辅料的体外膨胀行为及释药性能。方法:采用聚维酮(PVP)、羟丙甲纤维素(HPMC)、羟丙纤维素(L-HPC)及卡波姆934(CP_(934))为生物粘附材料,以不同配比制备丁卡因口腔粘附片,桨板法测定其释放度。结果:采用CP/HPC、CP/HPMC配比作为粘附材料取得良好效果。     

pH影响丁卡因麻醉作用实验研究

不同pH丁卡因溶液抑制离体坐骨神经动作电位和对家兔鼻粘膜、角膜的麻醉作用。pH7.4和4.8丁卡因溶液抑制离体坐骨神经动作电位IC50分别为0.34mg/ml和0.67mg/ml。对鼻粘膜麻醉作用ED50分别为0.39±0.03mg和1.1±0.15mg。对角膜麻醉作用ED50分别为0.45±0.05mg和1.2±0.18mg。上述三种实验均有非常显著差别。无论pH7.4还是4.8丁卡因溶液鼻粘膜给药1/5LD50后60min内血压、呼吸和心率均无显著影响     

丁卡因口腔粘附片的研制

目的：研制丁卡因口腔粘附片。考察不同辅料的体外膨胀行为及释药性能。方法：采用聚维酮（PVP），羟丙甲纤维素（HPMC），羟丙纤维素（L-HPC）及卡波姆934（CP934）为生物粘附材料，以不同配比制备丁卡因口腔粘附片，桨板法测定其释放度。结果：采用CP/HPC，CP/HPMC配比作为粘附材料取得良好效果。     

Solid lipid nanoparticles (SLN) for controlled drug delivery II. drug incorporation and physicochemical characterization

Solid lipid nanoparticles (SLN) are a colloidal carrier system for controlled drug delivery. The lipophilic model drugs tetracaine and etomidate were incorporated to study the maximum drug loading, entrapment efficacy, effect of drug incorporation on SLN size, zeta potential (charge) and long-term physical stability. Drug loads of up to 10% could be achieved whilst simultaneously maintaining a physically stable nanoparticle dispersion. Incorporation of drugs showed no or little effect on particle size and zeta potential compared to drug-free SLN. The optimized production parameters previously established for drug-free SLN dispersions can therefore be transferred to drug-loaded systems to facilitate product development.     

丁卡因与布比卡因分别联合芬太尼及氟哌利多在硬膜外术后镇痛中的效果观察

目的探讨丁卡因联合布比卡因与芬太尼及氟哌利多在硬膜外术后镇痛（PCEA）的临床效果。方法将80例行硬膜外手术患者随机分为试验组（丁卡因组,其药物组成成分：1%丁卡因12.5 mL、0.7 mg芬太尼、5 mg氟哌利多）和对照组（布比卡因组和其药物组成成分：0.75%布比卡因16.7 mL、5 mg氟哌利多、0.7 mg芬太尼）。两组自控硬膜外镇痛（PCEA）,两组总容量为100 mg,持续计量为2 mL/h,每15分钟为一次锁定时间,每1小时最大输出量2 mL,在术后72 h内停止镇痛。记录术后6 h、24 h镇痛效果、镇静评分、副作用（尿潴留、恶心、呕吐、眩晕）、下肢运动阻滞程度。结果两组镇痛效果和镇静评分差异无统计学意义（P〉0.05）。两组的双下肢运动阻滞程度差异无统计学意义（P〉0.05）。结论低浓度（0.125%）丁卡因用于临床硬膜外术后镇痛有效,安全,经济适用,值得临床推广。     

不同pH值丁卡因咽喉部表面麻醉药代动力学实验研究

本文研究了不同ｐＨ值丁卡因溶液咽喉部给药后药代动力学。１２只家兔随机分为ｐＨ７．４组或４．７组，咽喉部粘膜表面分别喷雾ｐＨ７．４或４．７丁卡因溶液，５ｍｇ／ｋｇ．高效液相色谱法测定丁卡因血药浓度。ｐＨ７．４与４．７丁卡因溶液药代动力学参数分别为３．１８±３．０４和１．２９±０．７４ｍｉｎ；Ｃｍａｘ分别为３１８．２９±１７５．５９和８７８．８１±３４７．２９ｎｇ／ｍｌ；Ｔｐｅａｋ分别为２．５２±１．１２和１．７９±０．４０ｍｉｎ：Ｖｄ分别为１３．６０±７．４０和４．３０±２．００ｍｌ／ｋｇ；Ｃｌｓ分别为３０２．５６６±１６４．２５和１５３．８７±８４．２２ｎｇ．ｍｌ－１／ｍｉｎ，组间均有显著差异（Ｐ＜０．０５或＜０．０１）。小鼠肠肌组织中ｐＨ值７．４和４．７丁卡因含量分别为６．３７±３．２和１．３８±１．２０ｍｇ／ｇ（Ｐ＜０．０１）。结果表明ｐＨ值７．４丁卡因溶液分布到血液中速度慢，血药浓度低，组织浓度高，代谢快，不易发生中毒。     

Reinforcement of spinal anesthesia by epidural injection of saline: a comparison of hyperbaric and isobaric tetracaine

Purpose. An epidural injection of saline was reported to extend spinal anesthesia because of a volume effect. The aim of this study was to evaluate the influence of the baricity of spinal local anesthetics upon the extension of spinal anesthesia by epidural injection of saline. Methods. Forty patients undergoing elective lower-limb surgery were randomly allocated to four groups of 10 patients each. Group A received no epidural injection after the spinal administration of hyperbaric tetracaine (dissolved in 10% glucose). Group B received an epidural injection of 8 ml of physiological saline 20 min after spinal hyperbaric tetracaine. Group C received no epidural injection after spinal isobaric tetracaine (dissolved in physiological saline). Group D received an epidural injection of 8 ml of saline 20 min after spinal isobaric tetracaine. The level of analgesia was examined by the pinprick method at 5-min intervals. Results. The levels of analgesia 20 min after spinal anesthesia were significantly higher in hyperbaric groups than in isobaric groups [T5 (T2–L2) vs. T7 (T3–12)]. After epidural injection of saline, the levels of analgesia in groups B and D were significantly higher than in groups A and C. The segmental increases after epidural saline injection were 2 (0–3) in group B and 2 (1–7) in group D. Sensation in the sacral area remained 20 min after spinal block in one patient in group D; however, it disappeared after epidural saline injection. Conclusion. In this study, 8 ml of epidural saline extended spinal analgesia. However, there was no difference between the augmenting effect in isobaric and hyperbaric spinal anesthesia. We conclude that the reinforcement of spinal anesthesia by epidural injection of saline is not affected by the baricity of the spinal anesthetic solution used. Received for publication on March 11, 1999; accepted on December 13, 1999