呋喃妥因透皮吸收作用的研究

采用简单小室法,初步研究了呋喃妥因软膏体外透皮吸收情况。结果表明,０．５％的氨酮对呋喃肥因无透皮促进作用,含２％氮酮的呋喃肥因软膏在各时间下的透皮吸收量比不含氮酮者均提高１倍以上;含２％与１％呋喃妥因的软膏之间,含两种透皮促进剂与一种透皮促进剂的软膏之间,呋喃妥因的透皮吸收在数量统计学上无显著差异。     

诺氟沙星软膏的透皮吸收试验

不同浓度氮酮（Ａｚｏｎｅ）及不同浓度Ｎ－甲基－２－砒咯烷酮（ＮＰ）对诺氟沙星（Ｎｏｒ）体外透皮吸收试验结果表明,１％－５％（质量分数）的Ａｚｏｎｅ对Ｎｏｒ透皮吸收均有一定促进作用,但在统计学上无显著差异,Ｎｏｒ累积透皮释药量与时间呈良好的线性关系,符合零级动力学过程;ＮＰ对Ｎｏｒ无透皮促渗透作用。     

中药软膏剂体外透皮效果研究

为评价复方中药软膏剂中不同浓度的透皮剂药物氮酮对马属动物的透皮效果,首先利用中药复方水提醇沉浓缩液制备中药软膏剂,然后在软膏剂中分别加入2%、4%、5.5%、7%的透皮剂药物氮酮,以软膏剂中的淫羊藿苷成分作为标记物,利用酶标仪法测定经智能药物透皮仪处理后的马皮肤透过液中的标记物含量。结果表明,在中药软膏剂中加入5.5%的氮酮作为促渗剂,所获得的药物渗透效果最佳。该研究为马属动物中药软膏剂中透皮剂药物的选择提供了理论依据,也为复方中药透皮给药系统的研究提供了更为安全、有效、稳定的给药途径。     

洛美沙星（Lomefloxacin）透皮吸收搽剂中氮酮的最佳浓度

应用洛美沙星搽剂作为模型药物，采用离体鼠皮，研究了氮酮（Azone)在0%，1%，3%，5%，7%浓度时对洛美沙星透皮吸收的影响。试验结果表明，氮酮在洛美沙星透皮吸收搽剂中最佳浓度为4.01%。     

我国中草药透皮吸收研究现状

透皮给药系统是药剂学中一个诱人而具有挑战性的新兴领域，硝酸甘油贴片自８０年代问世以来，一直是世界上最畅销的５０种药物之一犤１犦，随着透皮给药系统的深入研究，越来越多的药物有望制成透皮制剂。中草药作为祖国传统药物，与化学药品相比，具有低毒、低残留、不易产生耐药性等优点。近年来，我国科研工作者在中草药透皮吸收研究方面做了大量的工作。本篇文章中，我们将对国内中草药透皮吸收的研究状况进行综述。１传统医药透皮吸收治疗体系（transdermaltherapeuticsys－temTTS）理论属于近代新兴的研究理论，而祖国医学自古以来…     

利福平透皮溶液的经皮渗透研究

本实验采用Franz扩散池，研究了利福平（Rifampin）透皮溶液的体外透皮吸收情况。实验结果表明，透皮溶液中的药物能透过离体小白鼠皮肤，且透皮渗透促进剂能明显促进药物的透皮吸收。     

促渗剂促进药物透皮吸收机理的研究进展

综述了促渗剂促进药物透皮吸收机理的研究概况,着重介绍了氮酮、油酸和萜烯等常用促渗剂的促渗机理研究进展,并提出透皮吸收机理研究发展趋势,为该领域进一步深入研究提供参考.     

新型外用透皮杀虫剂的研究

通过对几种杀虫剂进行透皮吸收剂型的研究,筛选出高效、低毒、稳定透皮吸收效果好的最佳剂型,命名为“虱螨灵”。通过临床试验有效率达95％以上,从而解决了在干旱、缺水、寒冷季节防治羊外寄生虫的问题,并可减少杀虫剂对环境造成的污染。     

药物透皮吸收理论研究进展

由于透皮吸收制剂有着超越一般给药方法的独特优点 ,并且可有效避免肝首过效应 ,维持平衡血药浓度 ,已引起药学人士的普遍关注。近年来 ,人们对药物的透皮吸收进行了广泛深入的研究 ,尤其在透皮吸收理论方面的研究取得很大的进展。1　透皮给药过程的动力学药物透皮吸收不同其它途径的吸收。药物从给药部位进入体循环要经过一系列动态过程 ,因此其动力学描述也不同于一般给药途径。Ｇｕｙ等提出局部作用的多隔室模型 ,并用此模型解释了多剂量透皮吸收后尿药的变化 ,以此模型建立的数学公式为 :Ｘ尿 =ＦＸ0 Ｋ1Ｋ2 Ｋ4[1 /(Ｋ1αβ) -ｅ-1Ｋ/…     

The effects of equine skin preparation on transdermal drug penetration in vitro

An increasing number of formulations are applied to equine skin, yet variable penetration can affect efficacy, or the incidence of adverse effects, or both. To investigate the effects of common methods of skin preparation on transdermal drug penetration in vitro, we clipped, harvested, and froze skin samples from 5 Thoroughbred geldings. Thawed samples were prepared as follows: control (no preparation); cleaned with aqueous chlorhexidine (Aq-C, 0.1% w/v); cleaned with alcoholic chlorhexidine (Al-C, 0.5% w/v); shaved (Sh); or tape-stripped (Ta) with the use of adhesive tape. The samples were then placed in diffusion cells, and 2 g of methylsalicylate (MeSa) gel (Dencorub) was applied to the stratum corneum side. The penetration of MeSa and its analyte, salicylate (Sa), through the skin samples was measured over 10 h. Compared with control skin, significantly more MeSa penetrated through skin prepared with Al-C or Sh (P < 0.01) or with Aq-C or Ta (P < 0.05), and significantly more Sa was recovered in the receptor phase from skin prepared with Aq-C, Al-C, or Sh (P < 0.05) or with Ta (P < 0.01). A significantly higher rate of penetration and shorter lag time were also noted for MeSa with all the prepared skin samples, compared with the control samples. The results show that clinical techniques routinely used to clean or prepare skin can significantly affect the rate and extent of penetration of a topically applied drug. This may result in greater systemic availability of active drug, which could lead to enhanced efficacy and, possibly, a higher incidence of adverse effects.     

The effects of skin disease on the penetration kinetics of hydrocortisone through canine skin in vitro

This study investigated the effects of allergic skin disease on the penetration kinetics of hydrocortisone through canine skin in vitro. Full-thickness lesional and nonlesional (normal) skin was removed from the dorsal lumbosacral and dorsocaudal thoracic regions, respectively, of five canine cadavers. The dogs were suspected of having flea allergy dermatitis based on their distribution and types of skin lesions. Nonlesional skin was confirmed to be histologically normal, and the histopathology of the lesional skin was consistent with allergic dermatitis. Excised skin was clipped, mounted in Franz-type diffusion cells, and the transdermal penetration of a saturated, radiolabelled hydrocortisone solution was measured over 30 h. When the penetration data for all five dogs were pooled, a restricted (or residual) maximal likelihood mixed model predicted that the permeability coefficient and pseudosteady-state flux of hydrocortisone was more than twice as great (95% confidence interval 1.55-2.71 times as great; P < 0.0001) through lesional compared with nonlesional skin. There was no significant difference in the lag time for hydrocortisone penetration through lesional compared with nonlesional skin of the dogs. This study has confirmed that the transdermal penetration of hydrocortisone may be altered, typically increased twofold, but could be as high as 10-fold, through lesional compared with nonlesional skin of dogs with suspected flea allergy dermatitis. This is likely to be affected by variables such as disease severity, concurrent infections and interindividual differences in skin characteristics.     

Effects of eight vehicles on transdermal lidocaine penetration in sheep skin in vitro

This study investigated the effects of vehicles on penetration and retention of lidocaine applied to sheep skin in vitro. Thoracic skin from two sheep was clipped of wool and stored at −20 °C, until used. Skin samples were defrosted and mounted in Franz‐type diffusion cells, and then one of the following formulations, each saturated with lidocaine, was added: sodium lauryl sulphate (SLS) 0.5% in water, SLS 1% in water, dimethyl sulphoxide (DMSO) 50% in water (wt/wt), DMSO 100%, isopropyl myristate 100% (IPM), water alone, diethylene glycol monoethyl ether (DGME) 50% in water (wt/wt) and DGME 100%. The penetration of lidocaine in each skin sample was measured over 8 h. Significantly greater lidocaine skin concentrations and flux (J_SS) were achieved with the nonaqueous vehicles, DMSO 100% (P < 0.00001 and P < 0.01, respectively), followed by DGME 100% and IPM (P < 0.00001 and P < 0.01, respectively). The lag time (t_lag) for lidocaine penetration in the DMSO 100% vehicle was significantly shorter (P < 0.01) compared with all other vehicles except water. Improved transdermal penetration of lidocaine in the DMSO 100% vehicle was likely due to skin barrier disruption, as determined by differences in pre‐ and post‐treatment transepidermal water loss (TEWL). This study has shown that nonaqueous vehicles enhanced penetration of lidocaine in sheep skin to a greater extent than aqueous vehicles, which has implications for topically applied local anaesthesia in sheep.     

Regional differences in the in vitro penetration of methylsalicylate through equine skin

Commercial formulations of non-steroidal anti-inflammatory drugs (NSAIDs) are developed for human use but the extent to which they will pass through equine skin is unknown. Skin was harvested from five Thoroughbred geldings from the thorax, groin and leg (dorsal metacarpal) regions and frozen (-20 degrees C) until required. Two grams of methylsalicylate (MeSa) gel was applied to defrosted full-thickness samples in diffusion cells and the penetration of MeSa and its active metabolite, salicylate (Sa), through skin samples were measured over 24 h. Significantly higher (P < or = 0.02) total salicylate (AUC; MeSa + Sa) penetrated through skin from the leg region (5491.3 h mg/L), compared to thorax (3710.7 h mg/L) and groin (3571.5 h mg/L). In addition, there was a significantly higher (P0.01) rate of penetration of total Sa through leg skin in the first 6h after application. It was concluded that the commercial formulation of MeSa would achieve therapeutic levels of total salicylate beneath sites of topical application, with a faster and more pronounced response through the leg region, compared to the upper body.     

Regional differences in the in vitro penetration of hydrocortisone through equine skin

Little is known about the transdermal penetration of hydrocortisone in the horse and, although commercial formulations containing hydrocortisone are registered for topical use in the horse, there have been no studies investigating the movement of this glucocorticoid through different regions of equine skin. Skin was harvested from the thorax, groin and leg (dorsal metacarpal) regions of five Thoroughbred geldings and frozen (-20 degrees C) until required. Defrosted skin was placed in Franz-type diffusion cells and the amount of radiolabelled ((3)H) hydrocortisone, in a saturated solution of unlabelled hydrocortisone in 50% ethanol (w/w), which penetrated through and remained within skin samples was measured over 24 h. Significantly higher (P < 0.001) maximum flux (J(max); mol/cm(2)/h) was measured when hydrocortisone was applied to skin from the leg, compared to thorax and groin, although significantly less hydrocortisone (P < 0.001) was retained within skin from the leg at 24 h. Topical application of hydrocortisone in a vehicle containing ethanol would penetrate faster through leg skin from the lower leg when compared with the thorax or groin, which depending on cutaneous blood flow, may result in higher systemic drug concentrations or greater efficiency in treating local inflamed tissue.     

The effects of vehicle and region of application on in vitro penetration of testosterone through canine skin

The effects of the vehicles phosphate-buffered saline (PBS), ethanol (EtOH; 50% in PBS w/w) and propylene glycol (PG; 50% in PBS w/w) and the region of administration on in vitro transdermal penetration of testosterone was investigated in the dog. Skin was harvested from the thorax, neck (dorsal part) and groin regions of greyhounds after euthanasia and stored at -20 degrees C until required. The skin was then de-frosted and placed into Franz-type diffusion cells which were maintained at approximately 32 degrees C by a water-bath. Saturated solutions of testosterone, containing trace amounts of radiolabelled (14C) testosterone, in each vehicle were applied to the outer (stratum corneum) surface of each skin sample and aliquots of receptor fluid were collected at 0, 2, 4, 8, 16, 20, 22 and 24h and analysed for testosterone by scintillation counting. The maximum flux (J(max)) of testosterone was significantly higher for all sites when dissolved in a vehicle containing 50% EtOH or 50% PG, compared to PBS. In contrast, higher residues of testosterone were found remaining within the skin when PBS was used as a vehicle. This study shows that variability in percutaneous penetration of testosterone could be expected with formulation design and site of application.     

八味中药提取物的体外抑菌试验

随着抗生素类药物的不断被发现和在临床上的滥用,细菌以及其他微生物的抗药性问题日趋严重,给临床治疗带来了一定的困难.     

Effect of solute lipophilicity on penetration through canine skin

OBJECTIVE: To investigate the effect of lipophilicity on the percutaneous penetration of a homologous series of alcohols through canine skin. DESIGN: Skin harvested from Greyhound thorax was placed in Franz-type diffusion cells and the in vitro passage of radiolabelled (14C) alcohols (ethanol, butanol, hexanol and octanol (Log P 0.19-3.0)) through separate skin sections was measured in replicates of five. Permeability coefficient (kP, cm/h), maximum flux (Jmax, mol/cm2/h) and residue remaining within the skin were determined. RESULTS: The kP increased with increasing lipophilicity (6.2 x 10(-4) +/- 1.6 x 10(-4) cm/h for ethanol to 1.8 x 10(-2) +/- 3.6 x 10(-3) cm/h for octanol). Alcohol residues remaining within each skin sample followed a similar pattern. An exponential decrease in Jmax with increasing lipophilicity was observed. CONCLUSION: Changes in canine skin permeability occur with increasing alcohol lipophilicity. This finding has practical consequences for the design of topical formulations and optimisation of drug delivery through animal skin.     

Clinical study on the effect of biotin on skin conditions in dogs

In a collaborative study with small-animal veterinary surgeons, dogs with fur and skin conditions were treated with biotin (approximately 5 mg biotin/10 kg body weight/day) for 3 to 5 weeks. In total 119 cases could be treated which were reported to show symptoms such as dull coat, brittle hair, loss of hair, scaly skin, pruritus or dermatitis. Cases requiring other treatments with e.g. glucocorticoids, were excluded from the study. In 60% of the cases all symptoms were reported to be cured after the biotin treatment and in a further 31% an improvement was noted; in only 9% no effect was recorded. All breeds responded but to a variable extent: e.g. in Poodles the response was lower (no response in 6 out of 11 cases) than in Alsatians where all improved and 14 out of 29 were completely cured. The results confirm the favourable effect of biotin for treatment of fur and skin conditions in dogs.