HPLC法同时测定丁氯麻滴眼液中三组分的含量

目的：建立高效液相色谱法同时测定丁氯麻滴眼液中盐酸麻黄碱、盐酸丁卡因、氯霉素三种成分的含量。方法：采用Kromasil C18柱（250mm×4．6mm，5μm），流动相为甲醇-水-三乙胺-冰醋酸（40：60：0．5：0．5），流速1ml·min^-1，检测波长为254nm，柱温为30℃。结果：盐酸麻黄碱进样量在0．51-2．56μg范围内线性关系良好（r=0．9998），平均回收率为97．6％，RSD为1．6％。盐酸丁卡因进样量在0．47—2．34μg范围内线性关系良好（r=0．9998），平均回收率为99．2％，RSD为1．9％。氯霉素进样量在0．26-1．13μg范围内线性关系良好（r=0．9989），平均回收率为97.0％，RSD为1．9％。结论：该法准确，重现性好，效率高，操作简便，是丁氯麻滴眼液质量控制的有效方法。     

HPLC法测定复方地塞米松丁卡因乳膏中醋酸地塞米松和盐酸丁卡因的含量

建立复方地塞米松丁卡因乳膏中醋酸地塞米松、盐酸丁卡因含量的HPLC测定方法。色谱柱为SUNTEK Kromasil C18;流动相为甲醇-水-三乙胺(75∶25∶0.04),流速为1.0mL.min-1,检测波长为240 nm,线性范围:醋酸地塞米松2.5~20μg.mL-1,盐酸丁卡因100~800μg.mL-1,r=0.9999。平均回收率:醋酸地塞米松为100.12%,RSD为0.89%;盐酸丁卡因为98.63%,RSD为0.97%。方法准确可靠,简单易行,可用于复方地塞米松丁卡因乳膏中醋酸地塞米松、盐酸丁卡因的含量测定。     

永停滴定法测定盐酸丁卡因含量

目的：建立永停滴定法测定盐酸丁卡因的含量，并与药典方法相比较。方法：永停滴定法滴定条件为以极化电压为50mv、电流计的灵敏度为10^-9A、门限制为60格，以亚硝酸钠滴定液（0．05mol·L^-1）滴定盐酸丁卡因，用永停法指示滴定终点，从而计算出盐酸丁卡因的含量；药典方法为非水滴定法。以t检验法对两种测定方法的结果进行分析。结果：永停滴定法测得的平均回收率为99．65％（RSD=0．66％，n=5），其测定结果与非水滴定法的测定结果基本一致。结论：本方法操作简便、快速、准确、重现性好，可用于盐酸丁卡因含量测定。     

高效液相色谱法同时测定复方甲硝唑散中甲硝唑、盐酸丁卡因及醋酸地塞米松的含量

目的:建立以高效液相色谱法同时测定复方甲硝唑散中甲硝唑、盐酸丁卡因及醋酸地塞米松含量的方法。方法:色谱柱为C18,流动相为甲醇-水-三乙胺(65∶35∶0.36),检测波长甲硝唑、盐酸丁卡因为310nm,醋酸地塞米松为240nm,流速为1ml/min,柱温为25℃。结果:甲硝唑、盐酸丁卡因、醋酸地塞米松进样量分别在0.412μg~2.06μg(r=0.9999)、0.191μg~0.956μg(r=0.9999)、0.121μg~0.604μg(r=0.9998)范围内线性关系良好;平均回收率分别为100.69%(RSD=1.28%)、101.37%(RSD=0.23%)、102.40%(RSD=0.89%)。结论:本方法简便、准确,重现性好,可用于复方甲硝唑散的质量控制。     

Tetracaine oral gel in patients treated with radiotherapy for head-and-neck cancer: final results of a phase II study

PURPOSE: We performed a phase II study to assess feasibility, pain relief, and toxicity of a tetracaine-based oral gel in the treatment of radiotherapy (RT)-induced mucositis. METHODS and MATERIALS: Fifty patients treated with RT for head-and-neck cancer with clinical evidence of acute oral mucositis of grade>or=2 were scheduled to receive the tetracaine gel. A questionnaire evaluating the effect of the gel was given to all subjects. RESULTS: In 38 patients (79.2%), a reduction in oral cavity pain was reported. Thirty-four patients (82.9%) reported no side effect. Seventy-one percent of patients had no difficulties in gel application. Unpleasant taste of the gel and interference with food taste were noticed in 5 (12%) and 16 patients (39%), respectively. Planned RT course was interrupted less frequently in patients who reported benefit from gel application than in patients who did not (p=0.014). None of the patients who experienced pain relief needed a nasogastric tube, opposite to the patients who did not report any benefit from gel application (p=0.001). CONCLUSION: Tetracaine oral gel administration seemed feasible and safe while reducing RT-induced mucositis-related oral pain in a sizeable proportion of treated head-and-neck cancer patients. A trial designed to compare efficacy of this gel vs. standard treatment is warranted.     

Prevention of guanine nucleotide-induced reductions in muscarinic agonist binding to rabbit ileal submucosal membranes by lidamidine and tetracaine

Summary The effects of low concentrations (< = 1 mM) of the anti-diarrhoeal drug lidamidine and sub-anaesthetic concentrations (< = 1 M) of tetracaine on the binding of the muscarinic antagonist [³H] N-methylscopolamine ([³H]NMS) and the high affinity muscarinic agonist, [³H] oxotremorine-M ([³H]oxo-M) to broken cell preparations of rabbit ileal submucosal membranes were investigated. High affinity [3H]NMS binding (K _D = 0.79 ± 0.05 nM, B _max = 1.75 ± 0.13 pmoles · mg^–1) was unaffected by either lidamidine or tetracaine. Inhibition of NMS binding by the muscarinic agonist carbachol was reduced by the nonhydrolyzable analogue of GTP, GppNHp. This effect of GppNHp was partially prevented by lidamidine. Analysis of equilibrium binding of the muscarinic agonist [³H] oxotremorine-M revealed that the binding of oxotremorine-M could be best described by the presence of the least two populations of sites with affinities of 0.9 ± 0.2 and 27.7 ± 0.9 nM respectively. High affinity [³H] oxotremorine-M binding was markedly reduced by GppNHp, GDPS and fluoride (5 mM). Neither lidamidine, nor tetracaine had any effect on the binding of oxotremorine-M when added alone. However, lidamidine and tetracaine prevented GppNHp, GDPS and fluoride-induced reductions in oxotremorine-M binding. The present findings are consistent with an allosteric interaction between lidamidine or tetracaine and GppNHp-induced reductions in oxotremorine-M binding to submucosal muscarinic receptors. These effects are discussed in relation to the observed action of lidamidine in potentiating presynaptic inhibition of acetylcholine release by muscarinic agonists. Send offprint requests to D. Bleakman     

肌松药对丁卡因引起的离体家兔宫颈环肌条松弛作用的影响

本文就肌松药对丁卡因引起的离体家兔宫颈环肌条松驰的作用进行实验，结果表明：１．丁卡因本身对离体家兔宫颈环肌条的松弛作用不明显。２．预先注入肾上腺素后，使离体家兔宫颈环肌条处于收缩状态下，丁卡因可使肾上腺素的收缩曲线明显下降，且呈剂量依赖性。３．丁卡因在肾上腺素作用下，与肌松药合用，其离体家兔宫颈环肌条的松弛作用明显增强。提示：临床应用丁卡因可与肌松药合用，以减少丁卡因用药量提高麻醉效果。     

3种绝经后妇女宫内节育器取出术的疗效比较

目的：探讨3种不同绝经后妇女宫内节育器取出术的疗效。方法：选择绝经后妇女317例,随机分成3组。A组（104例）口服补佳乐（2 mg）,连服5 d,术前3 h于阴道后穹窿放置米索前列醇400 μg。手术开始后使用丁卡因胶浆3 g进行表面麻醉。B组（112例）使用米索前列醇及丁卡因联合,方法及剂量同A组。C组（101例）手术开始后单纯使用丁卡因胶浆。记录3组节育器取出术中患者的疼痛程度、术后阴道出血时间及取器成功率。结果：3组一次性取出节育器成功率比较差异有统计学意义（χ2=15.585,P＜0.05）。3组节育器取出术中疼痛程度、术后阴道出血时间比较差异有统计学意义（H 分别为144.366和31.567,P＜0.05）。结论：在绝经后妇女宫内节育器取出术前应用补佳乐、米索前列醇及术中配伍丁卡因,能减轻患者的痛苦,增加取器的一次成功率,减少术后阴道出血时间。     

盐酸丁卡因脂质体凝胶剂的经皮渗透性

目的:比较盐酸丁卡因脂质体凝胶与盐酸丁卡因游离药物凝胶的离体皮肤渗透性,探讨脂质体作为盐酸丁卡因的载体对皮肤渗透的影响.方法:采用体外双室渗透池作为离体皮肤的渗透试验装置,测定盐酸丁卡因在接受液内的累计透过百分率和在皮肤内的滞留百分率.结果:盐酸丁卡因脂质体凝胶和游离药物凝胶相比,药物透过皮肤的速度明显减慢,累计透过百分率与时间之间均符合Hihuchi方程;以卡波普为基质的盐酸丁卡因脂质体凝胶涂于皮肤24 h后,在皮肤内滞留量为36.7%,而游离药物凝胶皮肤内滞留量为9. 7%.结论:脂质体有促进药物进入皮肤的能力,而药物进入接受液中的量并不增加.     

达克罗宁与丁卡因复合麻醉在纤维喉镜诊断与治疗中的应用

目的探讨达克罗宁与丁卡因复合麻醉在纤维喉镜检查和治疗中的临床效果。方法对90例接受纤维喉镜诊治的病人,随机分成达克罗宁组、丁卡因组、达克罗宁与丁卡因复合麻醉组,每组30例,观察其麻醉效果。结果达克罗宁与丁卡因复合麻醉组、达克罗宁组及丁卡因组均取得了满意的麻醉效果,总有效率分别为96.7%、93.3%、90%,其中达克罗宁与丁卡因复合麻醉显效率为90%,明显优于达克罗宁组60%和丁卡因组63.3%,三组经χ2检验,差异有统计学意义。结论纤维喉镜检查与治疗前选用达克罗宁与丁卡因复合黏膜麻醉,可提高麻醉的安全性和可控性,能减少病人痛苦,病人更易于接受。