乙氧苯柳胺软膏工艺改变前后透皮实验研究

目的建立检测乙氧苯柳胺软膏不同工艺下透皮接收介质中乙氧苯柳胺含量的高效液相色谱法。方法利用40%乙醇/pH 7.4的磷酸溶液作为接收介质,通过不同时间点取样;高效液相色谱法（Agilent1200高效液相色谱仪）,甲醇：水(67：33)用磷酸调pH至2.6为流动相进行测定。结果对同一样品分析6次,其面积RSD均＜1.0%;标准曲线r为0.999 8。结论该法可有效对乙氧苯柳胺软膏透皮接收介质中乙氧苯柳胺含量进行测定,并对乙氧苯柳胺软膏工艺改变前后透皮效果进行比较。     

乙氧苯柳胺软膏治疗慢性湿疹的随机对照临床试验

目的：研究乙氧苯柳胺软膏治疗慢性湿疹的疗效和安全性。方法：６０ 例慢性湿疹病人,３０ 例（ 男性２３ 例,女性７ 例;年龄５０ ａ ±ｓ １５ ａ） 用乙氧苯柳胺软膏均匀涂布患处,ｔｉｄ , ４ ｗｋ 为一个疗程;另３０例（ 男性２４ 例,女性６ 例,年龄４４ ａ ±１４ ａ） 采用乙氧苯柳胺软膏基质（ 基质） 均匀涂敷患处,ｔｉｄ ,４ ｗｋ 为一个疗程。结果：乙氧苯柳胺胺膏２ ｗ ｋ 和４ ｗｋ 时的总有效率分别为２０ ％ 和６３ ％ ,基质的总有效率分别为１０ ％ 和１４ ％ 。乙氧苯柳胺软膏的不良反应发生率为７ ％ ,基质为３ ％ 。结论：乙氧苯柳胺软膏治疗慢性湿疹有效,不良反应发生率与基质无明显差异。     

局部用咪喹莫特泡囊凝胶剂的制备、表征及皮内滞留效应

目的:制备并表征局部用咪喹莫特泡囊凝胶剂,考察药物皮内滞留效应。方法:制备并表征咪喹莫特泡囊凝胶剂,离体鼠皮透皮实验考察药物皮内滞留量和透过量,切片观察药物皮内分布。结果:泡囊的平均粒径197.2 nm,Zeta电位-42.97 m V,包封率27.44%;泡囊凝胶剂体外释放t1/2与泡囊相似,但为凝胶剂的4.94倍和市售乳膏的3.83倍,12 h透过药量均比凝胶剂和市售乳膏小一半,单位面积皮内药物滞留量约为它们的2倍,切片显示药库效应显著。结论:泡囊凝胶剂具缓释作用和药库效应,可增加皮内滞留,减少角质层拦截和透过皮肤的药量,将有利于皮肤病的治疗,并可降低局部刺激性和全身毒性的风险。     

高效液相色谱法测定环吡酮胺乳膏中药物的含量及其体外透皮释放量

目的采用高效液相色谱（HPLC）法测定环吡酮胺乳膏的含量及体外透皮量.方法色谱柱为Intersil ODS 3 C18柱（4.6 mm×200 mm,5 μm）,流动相为乙腈 0.1%乙二胺四醋酸二钠溶液（70：30）,检测波长304 nm.体外透皮释放实验采用单室Franz扩散池,大鼠皮肤,自制乳膏与市售乳膏的透皮结果对比.结果环吡酮胺在20～180 μg&;#8226;mL 1范围内,线性关系良好（r＝0.999 8）,平均回收率为99.7%,RSD为0.69%.体外透皮释放量与时间呈良好的线性关系,相关因素为0.967 9.自制乳膏与市售乳膏的透皮结果差异无显著性.结论该法测定环吡酮胺乳膏药物含量及体外透皮释放量操作简便,快速准确.软膏基质和皮肤中成分对测定无干扰.     

丹皮酚凝胶处方优选及结晶行为研究

目的：优选丹皮酚凝胶处方并考察其结晶行为。方法：摇瓶法测定丹皮酚在不同乳化剂及助乳化剂中的饱和溶解度；结合凝胶外观及药物结晶情况，分别优选凝胶处方中的乳化剂、助乳化剂及凝胶材料；采用Franz扩散池法考察丹皮酚凝胶及软膏在离体小鼠皮肤的渗透及滞留；比较丹皮酚凝胶及软膏在放置过程中的结晶行为。结果：丹皮酚在不同乳化剂及助乳化剂中的溶解度均显著优于纯水；以10%丙二醇单辛酸酯为乳化剂、5%甘油为助乳化剂、1%卡波姆934为凝胶材料制得的丹皮酚凝胶较稳定，其小鼠离体皮肤透过率及滞留量均优于市售软膏，且放置1个月未观察到与软膏类似的结晶行为。结论：所得丹皮酚凝胶的透皮性能及结晶稳定性均优于软膏。     

姜黄二酮醇质体凝胶的制备与经皮渗透性研究

摘要：目的:采用醇质体凝胶装载药物改善姜黄二酮透皮性能。方法:分别制备姜黄二酮醇质体凝胶、普通凝胶、乳膏选取小鼠腹部皮肤进行Franz体外扩散试验用HPLC法测定姜黄二酮的浓度。以透皮量、皮肤储滞留量和透皮速率为指标,评价三者透皮性能。结果:姜黄二酮醇质体凝胶中姜黄二酮的稳态透皮速率为64.24μg·cm-2·h-1,分别达普通凝胶的3.29倍、乳膏的1.21倍;皮肤滞留量为369.35μg·cm-2,分别为普通凝胶的5.11倍、乳膏的3.36倍。结论:姜黄二酮醇质体凝胶的透皮性能良好具有新药开发的前景。     

姜黄素醇质体体外透皮及其稳定性研究

目的：对姜黄素醇质体体外透皮及其稳定性进行考察方法：采用透皮扩散仪进行体外透皮实验,比较姜黄素醇质体、溶液、脂质体经小鼠离体皮肤的累积渗透量及皮肤滞留量;并将姜黄素醇质体4℃条件下冷藏,考察其稳定性。结果：姜黄素醇质体12h内单位面积皮肤的累计渗透量和皮肤滞留量是其溶液（含0．5％吐温-80）的2．71倍和2．81倍;但与其脂质体无显著差异。姜黄素醇质体4℃条件下冷藏1个月,其外观、包封率、粒径及多分散指数（PDI）变化较小。结论：醇质体作为透皮给药载体能促进姜黄素的透皮吸收,并能增加皮肤中的滞留量;姜黄素醇质体具有一定的稳定性。     

乙氧苯柳胺软膏治疗面部皮炎疗效观察

乙氧苯柳胺软膏为非甾体抗炎抗过敏药物,主要用于治疗慢性湿疹及神经性皮炎。我科于2009年2月～2010年4月使用乙氧苯柳胺软膏治疗成人面部皮炎,取得了良好效果,现报道如下。     

水包油(O/W)型乙氧苯柳胺软膏的体外溶出及稳定性实验

本文设计了不含氮酮(azone)和含不同浓度氮酮的3种O/W型软膏基质并制备了乙氧苯柳胺软膏。体外溶出实验结果表明,各软膏中药物的溶出均符合单指数模型。不含氮酮软膏的溶出速度明显大于含氮酮软膏(P相似文献   

薄荷脑和樟脑对复方苯海拉明乳膏透皮作用的影响

目的研究薄荷脑和樟脑对复方苯海拉明乳膏中盐酸苯海拉明和苯佐卡因透皮作用的影响。方法采用改良Franz直立式扩散池,以离体乳猪皮肤为渗透屏障进行体外透皮扩散试验,以盐酸苯海拉明和苯佐卡因的累积渗透量、稳态流量及皮肤滞留量为指标,考察薄荷脑和樟脑在处方中的透皮调节作用。结果薄荷脑和樟脑对盐酸苯海拉明的累积渗透量、稳态流量及皮肤滞留量均无显著影响(P>0.05);对苯佐卡因的累积渗透量、稳态流量有显著抑制作用(P<0.01),并能提高其12 h皮肤滞留量(P<0.05)。结论薄荷脑和樟脑在复方苯海拉明乳膏中除发挥其药理活性外,还能调节药物的透皮吸收,其对苯佐卡因经皮渗透的抑制及皮肤滞留量的增加可能更有利于复方苯海拉明乳膏发挥局部治疗作用。     

氟尿嘧啶泡囊凝胶剂的体外透皮试验

目的:研究氟尿嘧啶泡囊凝胶剂的体外透皮扩散率及皮内滞留率。方法:建立用分光光度法测定氟尿嘧啶的方法,通过离体鼠皮透皮扩散试验,测定氟尿嘧啶泡囊凝胶的透皮扩散率及皮外残留率,并与氟尿嘧啶凝胶剂和医院制剂乳膏等作对照。结果:氟尿嘧啶泡囊凝胶剂的12 h的透皮累积扩散率仅为乳膏的10%,但皮内滞留率却增加2倍以上。结论:氟尿嘧啶泡囊凝胶剂可大大减少透过皮肤进入全身的药量,显著增加局部浓度,利于提高对皮肤病的疗效和降低全身毒性。     

派瑞松乳膏中3种药物透皮特性的研究

目的:评价派瑞松乳膏中曲安奈德(TACA)、苯甲酸(BEN)、硝酸益康唑(ECN)3种药物的透皮特性.方法:采用Franz扩散池法,考察药物经完整皮肤和去角质层皮肤的体外透皮能力,并采用了胶带剥离、皮肤萃取法分别获取了皮肤角质层、去角质层皮肤样本,用HPLC法测定了样本中的药物含量.结果:经过24 h透皮吸收,TACA和BEN的去角质层皮肤渗透量分别为完整皮肤的1.5和1.3倍,ECN的渗透量基本为零.8h透皮实验,TACA高、中、低3个浓度角质层中药物含量基本相同,真皮层则存在浓度依赖现象;ECN在皮肤各层和接受室均检测不到;BEN在角质层和真皮层中的分布与TACA相似,但透过量比TACA大.结论:角质层是皮肤渗透的重要屏障,派瑞松乳膏应用于皮肤溃疡、受损或者婴幼儿皮肤仍需谨慎.     

盐酸特比萘芬乳膏的透皮吸收和含量测定

目的:建立盐酸特比萘芬乳膏HPLC分析方法,并使用该方法进行自制乳膏和原研制剂的透皮吸收考察和自制乳膏的含量测定.方法:采用Kromasil C₁₈柱(4.6 mm×250 mm,5 μm),甲醇-乙腈-pH 7.5的醋酸三乙胺缓冲液(55:35:10)为流动相,流速1 ml·min^-1,检测波长282 nm.体外透皮实验采用Franz智能透皮吸收仪,以实验用离体乳猪皮为透皮屏障,通过累计渗透量和皮肤滞留量评价自制乳膏与原研制剂的透皮相似性.结果:盐酸特比萘芬质量浓度在4~150 ng·ml^-1、20~400 μg·ml^-1范围内线性关系良好(r=0.999 6,r=0.999 8),盐酸特比萘芬溶液平均回收率为98.88%,制剂加样平均回收率为100.4%.3批自制乳膏的平均含量为97.2%,累计渗透量和24 h皮肤滞留量与原研制剂差异无显著性(P >0.05).结论:所建立HPLC方法快速、准确,可同时用于盐酸特比萘芬乳膏的透皮吸收考察和含量测定.自制乳膏的透皮吸收特性与原研制剂相似,含量达到要求.     

Local anesthetic cream prepared from lidocaine-tetracaine eutectic mixture

Local anesthetic creams for the clinical treatment of conditions such as postherpetic neuralgia were prepared as an in-house formulation from the eutectic mixture of lidocaine-tetracaine (LT cream) using two eutectic mixtures of local anesthetic (EMLA) type bases. The LT formulation was compared with a lidocaine-prilocaine (LP cream) eutectic mixture formulated using the same base as EMLA. The chemical stability of lidocaine was examined in advance and was found to be stable for more than 3 months either in LT cream or in LP cream. The release rate of lidocaine from the formulated creams was examined using a cellulose ester membrane. The release rate of lidocaine from LT cream was similar to that from LP cream. The release rate of tetracaine was slightly slower than that of lidocaine in LT cream reflecting the larger molecular size of tetracaine. The penetration rate was examined in vitro using a Yucatan micropig skin. The penetration rate of lidocaine was similar between LT and LP creams. Infiltration anesthesia action examined in guinea pigs indicated that the difference between the two creams was statistically insignificant. The present study suggests the equivalence of the LT and LP creams as a local anesthetic and the potential of LT cream for clinical use either in the easy formulation or in the low-cost formulation.     

Biochemical and clinical study of calcium pantetheine-S-sulfonate

Calcium pantetheine-S-sulfonate (PaSSO3Ca) is one of the pantothenic acid derivatives. We examined PaSSO3Ca inhibition capacity of tyrosinase activity in vitro. For the safety evaluation when it will be applied to the human skin, we tested PaSSO3Ca creams to the fifty one patients with skin diseases by 48 hours closed patch test method. And clinical evaluation of PaSSO3Ca creams were performed in fifty patients with chloasma by half side method. Results were as follow: 1, PaSSO3Ca was proved to inhibit the tyrosinase activity in vitro. 2, PaSSO3Ca cream was shown to be safe to human skin. 3, 10% PaSSO3Ca cream lightened the skin hyperpigmentation.     

Enhanced Transdermal Delivery of Diazepam by Submicron Emulsion (SME) Creams

Diazepam, a lipophilic drug with CNS activity, serves here as a model to investigate the efficacy of SubMicron Emulsion (SME) as a novel transdermal vehicle. Diazepam was formulated in various topical regular creams and SubMicron Emulsion creams of different compositions. The different formulations were applied topically and protection against Pentamethylenetetrazole induced convulsive effects in mice was monitored. The efficacy of Diazepam applied topically in emulsion creams strongly depends on the oil droplet size and to a lesser degree - on the formulation composition and the oil type. Processing medium-chain-triglyceride (MCT) emulsion with a high-pressure homogenizer causes a drastic reduction in the droplet size, thereby significantly increasing the transdermal activity of Diazepam. In this case both the high-pressure homogenization and the presence of lecithin, an efficient dispersant, contribute to the effective droplet size reduction of below 1 micron, usually between 100–300 nm. The SubMicron Emulsions as vehicles for transdermal delivery of Diazepam generate significant systemic activity of the drug as compared with regular creams or ointments. Transdermal delivery of Diazepam via SME formulations is very effective, and the activity may reach the range of parenteral delivery. A single application of Diazepam in SME cream to mice skin provides pronounced transdermal drug delivery and prolonged protective activity up to 6 hours.     

复方利多卡因乳膏联合芬太尼透皮贴剂治疗老年患者带状疱疹后遗神经痛的临床观察

目的：观察复方利多卡因乳膏联合芬太尼透皮贴剂治疗带状疱疹后遗神经痛的疗效。方法60例临床诊断为带状疱疹后遗神经痛患者随机分为三组（复方利多卡因组、芬太尼透皮贴剂组和复方利多卡因联合芬太尼透皮贴剂组）,利多卡因乳膏组：在最痛的皮肤区涂抹复方利多卡因乳膏,根据皮肤大小涂抹,保留时间最大不超过12 h,每次间隔时间大于12 h,每天涂抹次数不超过3次;芬太尼透皮贴剂组：使用芬太尼初始剂量为12．5μg·h－1,如疼痛控制不满意,逐渐增加剂量（每72 h增加12．5μg·h－1）;利多卡因乳膏联合芬太尼透皮贴剂组：使用芬太尼初始剂量为12．5μg·h－1,如疼痛控制不满意,在最痛的皮肤区涂抹复方利多卡因乳膏。观察并记录治疗前三组的VAS（视觉模拟尺）评分及治疗4周后三组的VAS评分、统计三组中的芬太尼及利多卡因用量、并发症。结果三组患者疼痛均获得了明显缓解（P＜0．05）,利多卡因乳膏联合芬太尼透皮贴剂组的治疗满意度与芬太尼透皮贴剂组及利多卡因乳膏组相比,有统计学差异（P＜0．05）。结论复方利多卡因乳膏联合芬太尼透皮贴剂治疗带状疱疹后遗神经痛取得了较好的疗效,值得临床推广。     

Relationship between in vivo skin blanching and in vitro release rate for betamethasone valerate creams.

Betamethasone valerate creams from two firms were evaluated using the skin blanching procedure. In both studies, the same cream formulation exhibited significantly higher blanching compared to the other product. An in vitro release rate was determined for these betamethasone valerate cream products using a diffusion cell system, with a cellulose acetate membrane and a 60% ethanol:water receptor medium. The release rate (flux) of betamethasone valerate was higher for the higher blanching formulation and was statistically different from the other product. The integrity of the cellulose acetate membrane in 60% ethanol:water mixture was ascertained using hydrocortisone cream product. The in vitro drug release method, using a diffusion cell system and a synthetic membrane, can serve as a good quality control test method for topical creams.     

雷公藤甲素微乳凝胶的制备及体外透皮性能考察

目的：制备雷公藤甲素微乳凝胶并考察其理化性质及体外透皮扩散特性。方法：以混合乳化剂Tween80/Labrasol 1：4,助乳化剂无水乙醇,油相：油酸/Gemseal402：3,水相,泊洛沙姆407制备雷公藤甲素微乳凝胶。测定微乳的外观形态、粒径分布、pH、稳定性等理化性质。采用改良的Franz扩散池法,比较雷公藤甲素微乳凝胶和乳膏的经皮渗透特性。结果：制备的微乳澄清透明,呈现轮廓分明分布均匀的球形,平均粒径（27.8±0.3） nm,且PdI（0.2±0.004）,稳定性等理化性质均较好。雷公藤甲素微乳凝胶和雷公藤甲素乳膏24h单位面积累积渗透量分别为（4.33±0.17）、（7.07±0.16） μg·cm^-2,2种剂型中雷公藤甲素的渗透行为均符合Higuchi方程,透皮速率分别为1.9871,0.9149 μg·cm^-2·h^-1。结论：雷公藤甲素微乳凝胶和乳膏均具有缓释释药效果。雷公藤甲素微乳凝胶显著提高了雷公藤甲素的经皮渗透量及透过速率,且较乳膏强,可为雷公藤甲素经皮给药制剂选择提供参考。     

维A酸贴剂的体外透皮扩散研究

目的:研究自制的维A酸贴剂的体外透皮扩散率及在皮肤内的蓄积量。方法:按《中国药典》2005年版规定测定含量均匀度,以酸性异丙醇为溶剂,在波长352nm处测定维A酸,用透皮扩散仪测定透皮贴剂与市售维A酸乳膏对小鼠皮的扩散率及皮肤内的蓄积量。结果:贴剂的含量均匀度合格;测定的平均回收率为97.99%。测得含量为9.73mg/片,为标示量的97.3%;贴剂的扩散率虽低于乳膏,但皮肤内的蓄积量明显高于乳膏。结论:该贴剂能使药物蓄积于皮肤内,有利于提高对皮肤病的疗效和降低毒性,值得进一步开发。