靶控输注法对丙泊酚复合不同浓度芬太尼的临床观察

目的观察靶控输注丙泊酚和不同浓度芬太尼的临床效应。方法38例行下腹部手术的患者,随机分为2组,靶控输注丙泊酚3mg.mL-1分别复合芬太尼2ng.mL-1(A组)及4ng.mL-1(B组)。观察2组病人在麻醉前、气管插管后、切皮后的平均动脉压(MAP)、心率(HR)、心率变异性指数(LF/HF),并于气管插管后、切皮后、手术30,60,90及120min,观察2组病人的脑电双频指数(BIS)变化。结果A组病人在气管插管后,MAP、LF/HF均显著高于麻醉前;切皮后MAP、HR、LF/HF与麻醉前比较无显著性差异(P>0.05)。B组各指标在气管插管、切皮后与麻醉前比较,均无显著性差异(P>0.05)。2组各时间点的BIS值在35~58,组间比较无显著性差异。结论靶控输注丙泊酚3mg.mL-1伍用芬太尼4ng.mL-1,可以有效抑制气管插管和切皮反应,并可获得满意的麻醉深度;而伍用芬太尼2ng.mL-1可以有效抑制切皮反应,但不能抑制气管插管反应。     

中药经皮给药脂质体的研究与展望

中药经皮给药有悠久的应用历史,脂质体作为新型载体用于中药活性成分的经皮给药可以提升药物在局部的皮内滞留或（和）透皮吸收效果,从而显著改善药效。该文从皮肤屏障的特点、中药经皮给药概况、脂质体促进经皮吸收的机制与影响因素、中药经皮给药脂质体的皮内滞留、中药经皮给药脂质体的透皮吸收等5个方面对相关研究进展进行了综述,涉及常规脂质体以及传递体、醇质体、萜质体、甘油体、表面修饰脂质体等新型脂质体的应用,并提出了坚持正确的研究方向、提升制剂技术水平和提高研究技术水平三方面的展望。      

Constant voltage ‘Iron’tophoresis

The objective of this study was to investigate the feasibility of rapid administration of iron via transdermal route as an alternative to parenteral route of administration. In vitro drug delivery studies were carried out using porcine epidermis mounted on Franz diffusion cells. The effect of chemical permeation enhancers and physical techniques (constant voltage iontophoresis, electroporation and combination of electroporation with iontophoresis) on the transport of ferric pyrophosphate (FPP) was studied. Transepidermal water loss (TEWL) and electrical resistance were measured in order to see the effect of these techniques on the skin barrier function. The amount of FPP permeated was not enhanced significantly with the use of any of the enhancers (P?>?0.05). It was found that constant voltage iontophoresis (0.5, 2 or 4?V) for about 30?min across electroporated epidermis (120?V, 100 pulses, 10?ms at 5 Hz) enhanced the delivery of FPP over control in the range of 2- to 42-fold. Hence, a therapeutically required dose of iron could be delivered by transdermal route using electrically-mediated techniques.     

Development of drug-in-adhesive transdermal patch for α-asarone and in vivo pharmacokinetics and efficacy evaluation

A transdermal drug delivery system has been reported that can increase the bioavailability, reduce the administration duration, and maintain the concentration of drug in blood. In the present study, drug-in-adhesive transdermal patches of α-asarone using Eudragit E100 as pressure-sensitive adhesives and oleic acid plus isopropyl myristate as penetration co-enhancers were developed. In vitro permeation, in vivo pharmacokinetics in rabbits, and efficacy in asthmatic rats were evaluated. The results showed that co-enhancers could induce a synergistic effect on α-asarone permeability. In vivo study suggested that the patch can keep a relatively certain blood level of drug within 10–30?h in rabbits. Furthermore, the patch with the size of 4?cm² containing drug 3?mg/cm² showed a noticeable treating effect on asthmatic rats which is equivalent to the effect of dexamethasone, while avoiding the side-effect induced by the corticorsteroid. This suggests that the drug-in-adhesive transdermal patch is a promising delivery system containing α-asarone to be used for asthma treatment.     

Transdermal Clonidine Therapy and Blood Pressure Nocturnal Fall in Mild Hypertensive Male Subjects

Treatment of mild hypertension with an antihypertensive drug administered by means of a transdermal therapeutic system (TTS) could produce favorable results, when compared with a traditional oral regimen. Purpose: Using 24-h ambulatory blood pressure (BP) monitoring (ABPM) in mild hypertensive male subjects, to analyze three aspects which have not been completely clarified: a) whether a latency in the antihypertensive effect may be present, recording BP already from the first day of application of the patch, b) the eventual hazardous enhancement of circadian nocturnal fall in BP values in treated mild hypertensive patients and, c) the possible overlapping of antihypertensive effect between the administration of two consecutive patches. Subjects and methods: In 12 caucasian male outpatients (yrs 55 ± 3 SEM) with uncomplicated essential mild hypertension, a patch containing placebo was applied for the first week (T 0 period). At the end of the T 0 period, a 5 mg TTS-2 clonidine patch was applied for one week, and, subsequently, a new patch of 5 mg TTS-2 clonidine was kept for another week. ABPM was performed on the last day of the placebo period (T 0) and on the 1st day (T1), the 7th day (T2) and the 14th day (T3) of transdermal clonidine therapy. Results: Both systolic and diastolic BP (24 h mean, day-night-time) decreased on the 1st, 7th and 14th day, when compared with T0. However, no significant differences were documented between the BP levels on the 1st and the 7th day of treatment. The incidence of nocturnal fall in systolic and diastolic BP was evaluated and no significant differences were found, when compared with night-time reference values. Conclusions: When compared with the placebo period, TTS-2 clonidine lowers SBP and DBP within the first 24 hours of application. The antihypertensive effect persists at the end of the first week, as well as after 14 days. The lowest values of systolic-diastolic BP documented were not below the levels reported in normotensive men. Therefore, TTS-2 clonidine seems to act as an antihypertensive agent rather than a hypotensive drug since it normalizes BP without lowering it below physiological levels.     

地佐辛应用于瑞芬太尼静脉麻醉后患者的痛觉过敏观察

目的探析地佐辛对瑞芬太尼静脉麻醉术后患者疼痛过敏的影响，评价其镇痛的安全性以及有效性。方法选择腹腔镜下手术患者60例为研究对象，回顾性分析其临床资料。结果观察组患者要求进行镇痛距手术结束时间明显比对照组长（P〈0．05）；观察组患者在T1、T2、T3时点Ramsay评分明显优于对照组（P〈0．05），T3时点观察组VAS评分明显优于对照组（P〈0．05）；苏醒和拔管的时间、呼吸抑制、恶习呕吐等差异不具有统计学意义（P〉0．05）。结论地佐辛能有效的得到控制或者改善疼痛过敏，有效地减轻患者术后的疼痛感，安全性高。     

纳米微针透皮技术联合郑氏新伤软膏贴敷治疗急性踝关节扭伤的临床研究

目的:探讨纳米微针透皮技术联合郑氏新伤软膏贴敷治疗急性踝关节扭伤的临床疗效和安全性。方法:将80例急性踝关节扭伤患者随机分为2组,每组40例。软膏贴敷组采用郑氏新伤软膏贴敷治疗,每晚贴敷8~10h,共2周;联合治疗组在贴敷郑氏新伤软膏前先采用纳米微针透皮技术治疗,每晚1次,每次3min,共2周。分别于治疗前、治疗结束后记录并比较2组患者足踝部周径、踝部疼痛视觉模拟量表(visual analogue scale,VAS)评分及Kofoed踝关节评分,并观察并发症发生情况。结果:①足踝部周径。治疗前2组患者足踝部周径比较,差异无统计学意义[(35.08±2.39)cm,(34.93±2.44)cm,t=0.278,P=0.782];治疗结束后,联合治疗组患者足踝部周径小于软膏贴敷组[(28.63±1.40)cm,(30.18±1.60)cm,t=-4.626,P=0.000],2组患者足踝部周径均小于治疗前(t=17.338,P=0.000;t=14.162,P=0.000)。②踝部疼痛VAS评分。治疗前2组患者踝部疼痛VAS评分比较,差异无统计学意义[(7.08±1.14)分,(7.05.±1.13)分,t=-0.308,P=0.758];治疗结束后,联合治疗组患者踝部疼痛VAS评分低于软膏贴敷组[(2.03±0.73)分,(3.10±1.17)分,t=-4.467,P=0.000],2组患者踝部疼痛VAS评分均低于治疗前(t=-5.591,P=0.000;t=-5.690,P=0.000)。③Kofoed踝关节评分。治疗前2组患者Kofoed踝关节评分比较,差异无统计学意义[(50.18±5.49)分,(50.23±5.26)分,t=-0.042,P=0.967];治疗结束后,联合治疗组患者Kofoed踝关节评分高于软膏贴敷组[(89.95±1.74)分,(82.18±1.88)分,t=19.205,P=0.000],2组患者Kofoed踝关节评分均高于治疗前(t=-40.124,P=0.000;t=-37.709,P=0.000)。④综合疗效。治疗结束后,联合治疗组优15例、良18例、及格6例、差1例,软膏贴敷组优9例、良16例、及格11例、差4例;联合治疗组的综合疗效优于软膏贴敷组(Z=-2.100,P=0.036)。⑤并发症发生情况。2组患者均未出现药物过敏反应;联合治疗组2例遗留踝关节轻微疼痛,软膏贴敷组7例遗留踝关节轻微疼痛,因不影响日常生活,均未给予特殊处理。2组并发症发生率比较,差异无统计学意义(χ²=2.003,P=0.157)。结论:纳米微针透皮技术联合郑氏新伤软膏贴敷治疗急性踝关节扭伤,能缓解疼痛、减轻肿胀和改善关节功能,其疗效优于单纯郑氏新伤软膏贴敷治疗,但两者安全性相当。     

三联麻醉法在混合痔手术中的应用

目的:评价丙泊酚、芬太尼静脉基础麻醉联合局麻即三联麻醉法在混合痔手术中的麻醉效果及安全性。方法:将60例混合痔患者随机分为联合组和对照组,每组30例,联合组病人麻醉方式采用丙泊酚、芬太尼做基础麻醉,辅以肛周局部神经阻滞麻醉;对照组单纯采用肛周局部神经阻滞麻醉。观察并记录术中病人HR、MBP、SpO2、手术肌松程度、患者满意度、术后不良反应和尿潴留情况。结果:两组患者基础心率无差异,术中10min、20min、手术结束时心率联合组慢于对照组,P<0.05;两组患者在SpO2、MBP方面差异无统计学意义,P>0.05。联合组的肌松满意度、患者满意度均优于对照组,P<0.05;两组在尿潴留、不良反应方面差异无统计学意义,P>0.05。结论:三联麻醉法安全性较好,麻醉效果理想,患者易于接受。     

Fabrication and design of transdermal fluconazole spray

The objective of the present study was to formulate fluconazole transdermal spray for obtaining modified drug transport using eutectic mixture, ethyl cellulose, polyethylene oxide and alcohol. The formulated products were characterized. The selection of the optimized batch was done considering the results of drug transport in the first hour, the time required for 90% drug transport, viscosity and spray angle of the formulations. The inclusion of eutectic mixture, consisting of equal parts of camphor and menthol, showed improved drug transport through rat skin. The optimized batch exhibited larger mean zone of inhibition (antifungal activity), efficient in vivo activity and short term stability.     

Skin permeation behavior of elastic liposomes: role of formulation ingredients

Introduction: With the incorporation of edge activators into the lipid bilayer structure, elasticity properties are given to liposomes. Regardless of the debate over the precise permeation mechanism of elastic liposomes, these vesicles have been proven to enhance drug permeation into or through skin in most cases.

Areas covered: This article provides an overview of the formulation ingredients of elastic liposomes and their relationship with skin permeation behavior. The ingredients are divided into two categories of basic and optional ingredients. The effect of stability on permeation behavior of the vesicles is highlighted.

Expert opinion: More attention should be paid to the stability of elastic liposomes. The different stability properties of the elastic liposomes following administration can induce different skin permeation behaviors of the vesicles. It is necessary to select the optimum composition of the elastic liposomes in order to control the stability and permeation behavior of the vesicles into or through the skin. Moreover, for the development of elastic liposomes, particular attention should also be paid to the drug leakage from the vesicles during long-term storage. The application of optional ingredients to improve the stability and/or elasticity of the elastic liposomes is becoming a new trend.