盐酸川芎嗪透皮贴剂体外透皮速率测定和体外释放研究

目的研究盐酸川芎嗪透皮贴剂的经皮吸收的可行性。方法采用高效液相色谱法测定透皮接受液和释放接受液中盐酸川芎嗪的浓度。结果体外透皮实验和体外释放实验结果表明：盐酸川芎嗪在24h内以一定的速率（0．1014mg／cm^2h^1恒速渗透,其释放符合Higuchi方程。此外,该贴剂的体外释放速率为0．1332mg／cm^2h^1/2。结论盐酸川芎嗪透皮贴剂为皮肤限速型的骨架控释透皮给药系统。     

双氯芬酸钠贴片的制备及体外释放、透皮吸收测定分析

目的探讨双氯芬酸钠贴片的制备方法,分析其体外释放与透皮吸收能力。方法制备以聚丙烯酸酯为骨架的双氯芬酸钠贴片,进行体外透皮与释放度试验、制备DCF标准曲线、进行DCF贴片释放度试验,用蛇皮进行体外经皮渗透试验,以改进Franz扩散池检验药物的经皮渗透性能。结果成功制作了以聚丙烯酸酯为骨架的双氯芬酸钠贴片,测定显示,双氯芬酸钠贴片的体外释放速率为21.98μg/(cm2 h1/2),体外透皮速率为17.97μg/(cm2 h1/2)。结论本次研究制定的双氯芬酸钠贴片的释放度曲线与24h累计渗透量与Higuchi方程相符合,是一种新型的缓释型外用制剂。     

酮洛芬贴片体外透皮释放方法学研究

目的:建立酮洛芬贴片体外透皮释放方法学。方法 :采用HPLC法测定释放液中酮洛芬的含量,测定条件:DiamonsilC18色谱柱(150 mm×4.6 mm,5μm),流动相为pH 3.5磷酸盐缓冲液-乙腈-水(2∶53∶45),检测波长为253 nm,流速为1.0mL.min-1,柱温25℃。以裸鼠皮肤为实验皮肤,采用Frans扩散池方法进行三批酮洛芬贴片样品的体外透皮实验。结果:在该HPLC条件下,酮洛芬与其他杂质分离良好,进样量在0.509~40.72μg.mL-1时,酮洛芬浓度与峰面积呈良好的线性关系(r=0.999 9),回收率为101.09%,RSD为1.23%。三批酮洛芬贴片样品的透皮释放速率分别为18.157,17.973,20.001μg.cm-2.h-1,药物透皮释放符合零级动力学过程。结论:本文建立的酮洛芬贴片体外透皮释放方法简便,重现性好,可以用于控制产品质量。     

双氯芬酸钠贴片的制备及体外释放、透皮吸收测定

目的:制备双氯芬酸钠贴片,研究其体外释放、透皮吸收性能.方法:制备以聚丙烯酸酯为骨架的双氯芬酸钠贴片,以蛇皮为模型,采用改进Franz扩散池考察药物经皮渗透性能,并按中国药典方法考察了贴片的体外释放性能.结果:双氯芬酸钠贴片体外释放速率为21.98μg·cm-2·h1/2,体外透皮速率为17.97 μg·cm-2·h-1/2.结论:双氯芬酸钠贴片释放度曲线及24 h累计渗透量均符合Higuchi方程,是一种新颖的缓释型外用制剂.     

咳喘穴位贴片体外透皮速率和体外释放规律研究

目的:研究咳喘穴位贴片体外透皮速率和体外释放规律。方法:采用高效液相色谱法测定透皮接受液和释放液中指标成分盐酸麻黄碱的浓度,计算其渗透速率和体外释药速率。结果:麻黄碱以6.4679μg.cm-2.h-1/2的速率恒速渗透,其体外释药速率为21.382μg.cm-2.h-1/2,其释放过程符合Higuchi方程。结论:咳喘穴位贴片可研制为皮肤限速型的骨架控释系统。     

麝香壮骨膏中不同极性药物的体外释放与透皮对比

摘要：目的:考察麝香壮骨膏中盐酸苯海拉明、水杨酸甲酯的体外释放和透皮规律。方法:采用垂直式Franz扩散池进行体外释放和透皮试验,HPLC法测定释放液和透皮接受液中盐酸苯海拉明、水杨酸甲酯含量,计算单位面积累积释放率和累积透过率。结果:麝香壮骨膏中盐酸苯海拉明、水杨酸甲酯24h单位面积累积释放率均值分别为19.75%,73.50%,释放过程均符合Higuchi模型;单位面积累积透过率分别为12.48%,45.62%,透皮过程均符合零级模型;麝香壮骨膏样品中水杨酸甲酯单位面积平均累积释放率、累积透过率显著高于盐酸苯海拉明（P＜0.05）。结论:麝香壮骨膏中,脂溶性药物较水溶性药物具有更高的体外释放和经皮渗透性能。     

磷酸川芎嗪缓释透皮贴剂的制备及体外释放度测定

目的制备磷酸川芎嗪缓释透皮贴剂并优化其处方。方法通过正交实验,筛选缓释透皮贴剂的处方组成。结果采用聚丙烯酸树脂EUDRAGITE100为控释骨架和压敏胶材料,1.0%氮酮作为渗透促进剂制备胶粘剂骨架型经皮给药系统,药物从胶粘剂骨架/药物储库(压敏胶层)中恒速释放,体外释放度表明,贴剂的释放符合零级方程。结论所研制的磷酸川芎嗪缓释透皮贴剂具有理想的释药特性。     

司来吉兰贴片的制备及其体外透皮释放量的研究

 目的：制备司来吉兰贴片,研究其体外释放行为。方法：以丙烯酸酯压敏胶为骨架材料,氮酮为促渗剂,用离体豚鼠皮和Franz立式扩散池作为体外经皮释药模型,HPLC法测定司来吉兰贴片体外透皮量。结果：司来吉兰贴片中的药物经皮渗透符合零级动力学。结论：该贴片制备工艺简单,所制备的贴片具有良好的体外释放行为。     

氮酮促进盐酸川芎嗪透皮吸收的考察

考察了氮酮对盐酸川芎嗪透皮吸收的影响。结果含氮酮 0 ,0 .5 % ,1 .0 % ,2 .0 %的盐酸川芎嗪软膏 2 4h透皮吸收率分别为 4 0 .9% ,4 1 .1 % ,5 0 .0 % ,4 1 .2 %。唯含氮酮 1 .0 %的盐酸川芎嗪软膏促透作用明显     

莫索尼定贴片的制备及体外释放、透皮吸收研究

研究了莫索尼定贴片的制备、释放度及体外透皮吸收过程。该贴片释放度曲线符合Higuchi方程 ;莫索尼定从贴片中缓慢释放 ,72h累积透皮量符合Q～t方程     

Physicochemical characterization and evaluation of buccal adhesive patches containing propranolol hydrochloride

Buccal adhesive patches containing 20 mg of propranolol hydrochloride were prepared using solvent casting method. Chitosan was used as a natural bioadhesive polymer. Patches were prepared at different ratios of PVP K-30 and evaluated for various physicochemical characteristics such as weight variation, drug content uniformity, folding endurance, surface pH, ex-vivo mucoadhesive strength, ex-vivo residence time, in vitro drug release and in vitro buccal permeation study. Patches exhibited sustained release over a period of 7 hours. The mechanism of drug release was found to be Non-Fickian diffusion. Addition of PVP K-30 generally enhanced the releasing rate. The ex-vivo mucoadhesive strength was performed using sheep buccal mucosa on modified physical balance. Optimized patches (batch F4) showed satisfactory bioadhesive strength (9.6 degrees 2.0 gram) and ex vivo residence time (272 degrees 0.25 minutes). Swelling index was proportional to PVP K-30. The surface pH of all batches was within satisfactory limit (7.0+/-1.5) and hence patches would not cause irritation in the buccal cavity. Good correlation was observed between in vitro drug release and in vitro drug permeation with correlation coefficient of 0.9364. Stability of optimized patches was performed in natural human saliva showed that both drug and dosage forms were stable in human saliva.     

Novel biomaterial for transdermal application: in vitro and in vivo characterization

The objective of the present study was to evaluate a novel film forming biomaterial for its potential application in the preparation of unilaminate transdermal adhesive matrix systems. The biomaterial, Damar Batu (DB), was tried alone and in combination with Eudragit RL100 as a matrixing agent in the preparation of transdermal patches. Developed transdermal patches of Diltiazem hydrochloride (DH) were evaluated for thickness uniformity, weight uniformity, folding endurance and drug content. USP dissolution apparatus V was used for in vitro drug release studies. Modified Franz diffusion cell used for permeation study using excised human cadaver skin. Total 6 formulations were developed and on the basis of in vitro drug release and in vitro skin permeation profile F5 composed of DB: Eudragit RL100 (60:40) and carrying 20 %w/w DH was selected as an optimized formulation for in vivo study. The in vivo study results showed that F5 achieved the Cmax of about 269.76 ± 1.52 ng/mL in 6 h and sustained the release of the drug till 24 h. The skin irritation study results proved that the novel biomaterial is non-sensitizing and non-irritating. Drug-polymer interaction study carried out to check the compatibility of drug and polymer showed the intactness of the drug in the formulation proving the compatibility of the polymer. It can be proposed from the outcome of the present study that by applying suitable adhesive layer and backing membrane, DB: Eudragit RL100 (60:40) transdermal patches can be of potential therapeutic use.     

盐酸川芎嗪眼用原位温敏凝胶的制备及体外释药特性研究

目的：制备盐酸川芎嗪眼用原位温敏凝胶并对其体外释药特性进行考察。方法采用泊洛沙姆407和泊洛沙姆188为温敏基质制备眼用温敏凝胶,采用无膜溶出模型,研究药物在某一时间的累积释放百分率与时间的变化,对曲线进行拟合分析,研究川芎嗪的体外释放特性。结果所制得凝胶为均匀稍带黏性的澄清溶液,该制剂的体外释放行为遵循零级动力学方程（r ＝0．9887）,由 Ritger －Peppas 方程拟合的 n 值为0．7533。结论盐酸川芎嗪眼用温敏凝胶体外释药是由药物扩散和凝胶溶蚀双重机制控制。     

Drug in adhesive type transdermal matrix systems of ondansetron hydrochloride: optimization of permeation pattern using response surface methodology

The present investigation aims at development of pressure sensitive adhesive (PSA) based drug in adhesive type transdermal systems of ondansetron hydrochloride with higher permeation flux. The effect of mixture of two chemical permeation enhancers (oleic acid and lauric acid diethanolamide); and drug loading dose on the ex vivo human cadaver skin permeation from the transdermal patches has been investigated using a d-optimal combined mixture design. Incorporation of chemical permeation enhancers significantly improved the permeability parameters and it was also found that blend of permeation enhancers is more effective than either permeation enhancer. Criterion of desirability was employed to numerically optimize the transdermal system. Optimized formulation was achieved with 67.5% lauric acid diethanolamide, 32.5% oleic acid and 10% drug loading in an acrylate based PSA matrix. Optimized formulation was found to be nonirritating and safe for dermatological application.     

盐酸地匹福林眼用凝胶剂的研究

目的：研制了盐酸地匹福林眼用凝胶剂,进行了体外释放、体外渗透以及眼部刺激性实验。方法：建立了高效液相色谱法测定制剂的含量及体外释药量的方法,采用透析膜扩散法进行处方的体外释药实验,采用离体角膜进行体外渗透实验。结果：亲水凝胶材料含量越小,盐酸地匹福林从凝胶基质中释放越快,凝胶剂体外释药符合一级释放动力学方程。凝胶剂离体角膜渗透行为符合一级释放规律。盐酸地匹福林凝胶剂具有较低的眼部刺激性。结论：盐酸地匹福林眼用凝胶剂有较好的缓释行为,可以明显降低眼部刺激。     

克仑特罗透皮给药系统的研究

对丙烯酸酯共聚物制备的胶粘带型长效克仑特罗透皮制剂的研究表明,其体外释放符合 Higuchi方程,体外皮肤渗透呈零级速率过程。其皮肤渗透的主要屏障是角质层。在共聚物中,加入少量肉桂氮(艹卓)酮、司盘85等,可明显提高该透皮制剂的体外释放和皮肤渗透速率。     

<Emphasis Type="Italic">In vitro</Emphasis> Percutaneous absorption of ondansetron hydrochloride from pressure-sensitive adhesive matrices through hairless mouse skin

To investigate the feasibility of developing a new ondansetron transdermal system, the effects of vehicles and penetration enhancers on the in vitro permeation of ondansetron hydrochloride (OS) from a pressure-sensitive adhesive (PSA) matrices across dorsal hairless mouse skin were studied. Vehicles employed in this study consisted of various ratios of propylene glycol monocaprylate (PGMC)-diethylene glycol monoethyl ether (DGME) co-solvents and PGMC-propylene glycol (PG) co-solvents with 3% oleic acid. Duro-Tak 87-2100 and Duro-Tak 87-2196 were used as PSAs. The concentration of DGME in PGMC-DGME co-solvent system affected the release rate; as the concentration of DGME increased, the release rate decreased. The cumulative release amount of OS increased as the ratio of PSA to drug solution decreased. The permeation flux was also primarily affected by the amount of PSAs; as the amount decreased, the permeation flux increased. The overall fluxes from matrix formulations were significantly lower when compared to those obtained from solution formulations. The ratio of PG to PGMC did not affect permeation flux, while the lag time decreased significantly from 5.14 +/- 3.31 to 0.31 +/- 0.12 h as the PG increased from 40% to 60%.     

盐酸丁螺环酮口腔粘附片的制备及释药机理初步研究

口腔粘附制剂是指将药物与适宜的生物粘附剂等辅料经加工制成的制剂 ,使用时将制剂粘附于口腔粘膜上 ,恒定释放药物。口腔粘附制剂不仅能够局部治疗口腔疾病 ,而且药物可以透过口腔粘膜吸收 ,进入血液循环 ,起到全身治疗作用。药物经口腔粘膜吸收时 ,避免了胃肠道及肝脏的首过作用 ,因此对于易受胃肠道酸和酶降解的蛋白质、肽类及其他大分子药物 ,以及受肝脏首过代谢作用严重的药物 ,通过口腔粘膜给药可以提高生物利用度[1] 。本文选择的药物盐酸丁螺环酮 (ｂｕｓｐｉｒｏｎｅｈｙｄｒｏｃｈｌｏｒｉｄｅ)是一个新型的非苯二氮类抗焦虑症…     

Design and Evaluation of a Monolithic Drug-in-Adhesive Patch for Testosterone Based on Styrene–Isoprene–Styrene Block Copolymer

The purpose of the present study was to design and evaluate a monolithic drug-in-adhesive patch with a novel pressure-sensitive adhesive (PSA) matrix based on styrene–isoprene-styrene (SIS) block copolymer. Testosterone was selected as the model drug. The orthogonal array design for ternary mixtures was employed to optimize the amounts of SIS, C-5 hydrocarbon resin, and liquid paraffin. The drug release percentage, water vapor permeability, adhesive properties were chosen as response variables. The patch formulation was optimized by investigating the effects of the drug loading capacity, the type, and amount of permeation enhancer on the adhesive properties and skin permeation. The compositions of the optimal matrix were: 120 g of SIS copolymer, 120 g of C-5 hydrocarbon resin, 60 g of liquid paraffin. An optimized formulation with maximum skin permeation and acceptable adhesive properties was developed incorporating 2% testosterone and 6% isopropyl myristate. No significant differences for in vitro release, skin permeation, and in vivo absorption were observed between the optimal formulation and Testopatch®. The stability evaluation showed that the patches were stable at 25°C/60% relative humidity for 6 months. The result indicated that SIS copolymer was a suitable and compatible polymer for the development of PSA. © 2013 Wiley Periodicals, Inc. and the American Pharmacists Association J Pharm Sci 102:2221–2234, 2013     

薄荷醇酯衍生物对压敏胶分散型贴剂中非甾体抗炎药体外经皮渗透性的影响

制备了含不同非甾体抗炎药(酮洛芬、吲哚美辛和双氯芬酸)及促透剂[月桂氮酮、薄荷醇、庚酸薄荷醇酯(M-HEP)或油酸薄荷醇酯(M-OA)]的压敏胶分散型贴剂。采用双室扩散池,以离体大鼠皮肤为屏障进行体外渗透试验,考察了压敏胶和促透剂的种类对贴剂中药物渗透行为的影响。结果表明,用Duro-TAK 87-4098型压敏胶制备的贴剂中酮洛芬的稳态渗透速率和24 h累积透过量显著高于用其他两种压敏胶(Duro-TAK 87-2677和87-2852)制备的贴剂。各促透剂对酮洛芬促渗透作用依序为:M-HEP>M-OA>薄荷醇>月桂氮酮;对吲哚美辛的促渗透作用依序为:M-HEP>M-OA>月桂氮酮≈薄荷醇;M-OA和月桂氮酮对双氯芬酸有显著的促渗透效果,前者的促渗效果较强,而薄荷醇及M-HEP无促渗透作用。