溶液载体和用药部位对甲硝唑在犬中透皮吸收的影响

研究不同的溶液载体（PBS，5％薄荷醇和5％氮酮）和不同部位的皮肤对甲硝唑在犬中体外透皮吸收和皮内摄取的影响。取下北京犬颈部、胸部以及腹部皮肤，-20℃保存。使用时，皮肤解冻固定在改良Franz透皮扩散仪上，保持恒速（200±1）r／min，恒温（35±0．5）℃。在扩散池中的皮肤角质层上加入2mL溶液载体（含甲硝唑58．4μmol），以20％乙醇为溶剂溶解薄荷醇和氮酮，在预定时间点取样1mL，采用HPLC方法测定各接受液中的药物量和皮肤中摄取的药物量。结果显示，与PBS相比，薄荷醇和氮酮能增加所有部位甲硝唑的透皮吸收量和皮内摄取量（P〈0．05）。同一溶液载体在不同部位的渗透性存在差异，腹部〉颈部〉胸部，不同部位的皮内摄取量也存在差异，颈部〉胸部〉腹部。说明甲硝唑在不同溶液载体和不同部位皮肤的渗透性存在差异。     

溶液载体和用药部位对甲硝唑在犬中透皮吸引的影响

研究不同的溶液载体(PBS,5%薄荷醇和5%氮酮)和不同部位的皮肤对甲硝唑在犬中体外透皮吸收和皮内摄取的影响.取下北京犬颈部、胸部以及腹部皮肤,-20℃保存.使用时,皮肤解冻固定在改良Franz透皮扩散仪上,保持恒速(200±1)r/min,恒温(35±0.5)℃.在扩散池中的皮肤角质层上加入2 mL溶液载体(含甲硝唑58.4 μmol),以20%乙醇为溶剂溶解薄荷醇和氮酮,在预定时间点取样1 mL,采用HPLC方法测定各接受液中的药物量和皮肤中摄取的药物量.结果显示,与PBS相比,薄荷醇和氮酮能增加所有部位甲硝唑的透皮吸收量和皮内摄取量(P<0.05).同一溶液载体在不同部位的渗透性存在差异,腹部>颈部>胸部,不同部位的皮内摄取量也存在差异,颈部>胸部>腹部.说明甲硝唑在不同溶液载体和不同部位皮肤的渗透性存在差异.     

三组药物对离体猪皮不同部位透皮效果的研究

采用ZRS－4型智能溶出仪为体外透皮装置，用紫外分光光度计检测3组药物（黄连＋冰片、黄连＋冰片＋氮酮、黄连＋蒽诺沙星＋氮酮）对仔猪不同部位（腰背部、腹侧部、腹底部）离体皮肤的透过率。结果，相同药物在不同部位的透皮率差异显著（P＜0．05）；3组药物在相同部位的透皮率无显著差异（P＞0．05）。表明，机体用药部位的选择对皮治疗的效果具有重要意义。     

不同浓度促透剂对绿原酸体外透皮吸收的影响

目的:通过小鼠体外透皮实验,探讨不同促透剂对绿原酸巴布剂药贴体外透皮吸收的影响,确定最佳促透剂及其浓度,为研制绿原酸透皮吸收制剂奠定良好的基础。方法:采用改良Franz扩散池法,以离体小鼠皮肤为透皮屏障,加入不同浓度促透剂制备绿原酸巴布剂药贴,以HPLC法考察绿原酸不同时间透过量,以绿原酸为定量指标进行体外透皮吸收检测。结果:单一促透剂中以1%氮酮效果最佳,5%油酸效果次之。结论:常用促透剂氮酮、油酸均可以使巴布剂中的绿原酸透过皮肤,且以1%氮酮促透效果最佳。     

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。     

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。     

氮酮促进洛美沙星仔猪皮肤吸收机理的研究

选用10～12日龄同品种仔猪,随机分组,于仔猪腹部皮肤涂搽含氮酮的洛美沙星透皮吸收剂, 分别于涂药前、涂药后2、4、6、12、24、48和72 h 在体取皮,应用透射电镜观察皮肤表皮结构变化,探讨氮酮促进洛美沙星透皮吸收的作用机理.结果表明,氮酮通过以下途径促进药物透皮吸收:(1)作用于表皮角质层细胞间脂质,使角质层变得疏松,细胞间距增大,外角质层细胞易于脱落,降低了皮肤对药物的屏障作用;(2)氮酮进入角质细胞内,与细胞内基质相作用,引起基底角质层肿胀,增加了角质细胞水化程度和药物存储空间.研究还发现,氮酮在体对仔猪皮肤的作用可维持72 h 以上;由氮酮引起皮肤结构的改变是一非损伤可复性过程.     

复方酮康唑纳米乳的研制及其体外经皮吸收

本研究研制出一种以纳米乳为载体的质量稳定,高效的药物传递系统.通过伪三元相图法筛选配方,找到最佳配比;通过HPLC法及稳定性试验考察复方酮康唑纳米乳的稳定性;用大鼠皮肤及透皮扩散仪进行透皮试验,考察其体外透皮性能.复方酮康唑纳米乳是由EL-40,乙醇,2-苯乙醇,乙酸乙酯,酮康唑,丙酸氯倍他索,丁香酚,水构成的淡黄色澄清透明的液体,稳定性良好;其透皮速率与2.5％氮酮组相当,优于混悬液及复方酮康唑软膏.复方酮康唑纳米乳是一种质量稳定、高效的药物传递系统.     

新曹药氯氰碘柳胺钠透皮溶液含量方法学研究

透皮溶液（Pour—onSolution,PS）是指使药物透过皮肤由毛细血管进人全身血液循环达到有效血药浓度,并在各组织或病变部位起治疗或预防疾病作用的外用溶液剂型。透皮给药系统fTransdermalTherapeuticSystem,yrs）是指经皮肤给药而起全身治疗作用的控释制剂。     

冰片、薄荷醇及氮酮对乳炎清凉巴布剂透皮吸收的影响

目的:考察冰片、薄荷醇、氮酮3种促渗剂联合应用对乳炎清凉巴布剂体外透皮吸收的影响,确定其最优组合。方法:利用ZTY-型透皮扩散仪,以乳牛皮肤为材料,采用三因素三水平正交试验设计,以HPLC法检测乳炎清凉巴布剂主要成分绿原酸在不同时间的透皮含量,计算各组透皮吸收速率、累积渗透量等。结果:9个试验组均有绿原酸透皮吸收,组间有显著性差异,其中A1B1C2(冰片∶薄荷醇∶氮酮为1%∶1%∶3%)为最优组合。结论:冰片、薄荷醇、氮酮3种促渗剂按1%、1%、3%联合应用能显著促进乳炎清凉巴布剂中绿原酸的透皮吸收。     

Effects of vehicle and region of application on absorption of hydrocortisone through canine skin

OBJECTIVE: To determine the effects of various vehicles on the penetration and retention of hydrocortisone applied to canine skin. SAMPLE POPULATION: 20 canine skin samples obtained from the thorax, neck, and groin regions of 5 Greyhounds. PROCEDURE: Skin was harvested from dogs after euthanasia and stored at -20 degrees C until required.The skin was then defrosted and placed into diffusion cells, which were maintained at approximately 32 degrees C by a water bath. Saturated solutions of hydrocortisone that contained trace amounts of radiolabelled [14C]-hydrocortisone in each vehicle (ie, PBS solution [PBSS] alone, 50% ethanol [EtOH] in PBSS [wt/wt], and 50% propylene glycol in PBSS [wt/wt]) were applied to the outer (stratum corneum) surface of each skin sample, and aliquots of receptor fluid were collected for 24 hours and analyzed for hydrocortisone. RESULTS: The maximum flux of hydrocortisone was significantly higher for all sites when dissolved in a vehicle containing 50% EtOH, compared with PBSS alone or 50% propylene glycol, with differences more prominent in skin from the neck region. In contrast, higher residues of hydrocortisone were found remaining within the skin when PBSS alone was used as a vehicle, particularly in skin from the thorax and neck. CONCLUSIONS AND CLINICAL RELEVANCE: Penetration of topically applied hydrocortisone is enhanced when EtOH is used in vehicle formulation. Significant regional differences (ie, among the thorax, neck, and groin areas) are also found in the transdermal penetration and skin retention of hydrocortisone. Variability in clinical response to hydrocortisone can be expected in relation to formulation design and site of application.     

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.     

Vehicle Effects on the <Emphasis Type="Italic">In Vitro</Emphasis> Penetration of Testosterone through Equine Skin

The effects of three vehicles, phosphate-buffered saline (PBS), ethanol (50% in PBS w/w) and propylene glycol (50% in PBS w/w) on in vitro transdermal penetration of testosterone was investigated in the horse. Skin was harvested from the thorax of five Thoroughbred horses after euthanasia and stored at −20^°C until required. The skin was then defrosted and placed into Franz-type diffusion cells, which were maintained at approximately 32^°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 24 h and analysed for testosterone by scintillation counting. The maximum flux (J _max) of testosterone was significantly higher for all sites when testosterone was dissolved in a vehicle containing 50% ethanol or 50% propylene glycol, 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 clinical response to testosterone could be expected with formulation design.     

促渗剂对鹿茸多肽透皮吸收的影响及鹿茸多肽免疫活性检测

通过探讨不同质量浓度促渗剂月桂氮卓酮和冰片对鹿茸多肽透皮吸收的影响,优化出鹿茸多肽的给药方式,即通过口腔黏膜服用,为鹿茸运用于创伤、烧伤和美容提供依据。通过脾细胞增殖试验,检测鹿茸多肽的免疫活性。结果表明：（1）SDS-PAGE显示鹿茸酸粗提取物中含有不等量的蛋白质和多肽等,且多为大分子量多肽,但醇提多肽多为10000左右的某些小分子量多肽。（2）含5％月桂氮卓酮的醇提鹿茸多肽和含0．12％冰片的醇提鹿茸多肽比只含醇提鹿茸多肽溶液的累积透皮透过量多,说明促渗剂月桂氮卓酮和冰片能明显的增加醇提鹿茸多肽的透皮扩散速度和扩散的总量,而且0．12％冰片的促渗效率比5％月桂氮卓酮的促渗效果要高。（3）鹿茸多肽具有促进脾细胞增殖的活性,并存在剂量依赖性：醇提鹿茸多肽质量浓度从10mg／L上升到40mg／L时,对促进脾细胞增殖呈上升趋势,当质量浓度超过40mg／L时,增殖率增加不显著。     

The examination of biophysical parameters of skin (transepidermal water loss, skin hydration and pH value) in different body regions of normal cats of both sexes

The purpose of this study was to evaluate transepidermal water loss (TEWL), skin hydration and skin pH in normal cats. Twenty shorthaired European cats of both sexes were examined in the study. Measurements were taken from five different sites: the lumbar region, the axillary fossa, the inguinal region, the ventral abdominal region and the left thoracic region. In each of the regions, TEWL, skin hydration and skin pH were measured. The highest TEWL value was observed in the axillary fossa (18.22g/h/m(2)) and the lowest in the lumbar region (10.53g/h/m(2)). The highest skin hydration was found in the inguinal region (18.29CU) and the lowest in the lumbar region (4.62CU). The highest skin pH was observed in the inguinal region (6.64) and the lowest in the lumbar region (6.39). Statistically significant differences in TEWL were observed between the lumbar region and the left side of the thorax region (P=0.016), the axillary fossa (P=0.0004), the ventral region (P=0.005), and the inguinal region (P=0.009). There were significant differences in skin hydration between the lumbar region and the left thorax (P=0.000003), the axillary fossa (P=0.002), the ventral abdomen (P=0.03), and the inguinal region (P=0.0003) as well as between the thorax and the ventral abdomen (P=0.005). TEWL was higher in females (15g/h/m(2)) than in males (4.57g/h/m(2)). Skin hydration was higher in females (13.89CU) than in males (12.28CU). Significant differences were not found between males and females for TEWL and skin hydration. Skin pH was higher in males (6.94) than in females (6.54), which was significant (P=0.004).     

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。     

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 transdermal penetration of fentanyl through equine skin

The rate and regional differences for the penetration of fentanyl through equine skin was investigated in vitro using a commercial transdermal therapeutic system (TTS) or ‘patch’. Skin collected from the thorax, groin and leg (dorsal metacarpal) regions of five horses was placed in diffusion cells and a fentanyl TTS applied to each skin sample. Drug penetration through each skin sample over 48 h measured using high performance liquid chromatography (HPLC). Cumulative penetration (μg/cm²) was plotted against time (h) and used to regress the steady state flux (μg/cm²/h) of fentanyl through each skin site. Results showed similar fluxes for both the thorax (2.32 ± 0.17 μg/cm²/h and groin (2.21 ± 0.11 (μg/cm²/h) regions, but significantly lower flux (P = < 0.05) for the leg region (1.56 ± 0.120 μg/cm²/h. Interestingly, there was a significantly longer lag time for the penetration of fentanyl through the groin region (7.87 ± 0.51 h) compared to the other two sites (5.66 ± 0.97 h and 5.75 ± 0.43 h for the thorax and leg regions respectively). The results suggest that a fentanyl TTS applied to the leg region may have a small but significantly lower amount of fentanyl available systemically, compared to patches applied to the thorax or groin regions, which may affect the level of analgesia subsequently achieved in the horse.     

The effect of region of application on absorption of ethanol and hexanol through canine skin

The effect of region of application on the percutaneous penetration of solutes with differing lipophilicity was investigated in canine skin. Skin from the thorax, neck, back, groin, and axilla regions was harvested from Greyhound dogs and placed in Franz-type diffusion cells. Radiolabelled (14C) ethanol (Log P 0.19) or hexanol (Log P 1.94) was applied to each skin section for a total of 5h. The permeability coefficient (kP, cm h(-1)) and residue of alcohol remaining in the skin were significantly (P=0.001) higher for hexanol compared to ethanol. In contrast, ethanol had a far greater maximum flux (Jmax, mol (cm2)(-1) h(-1)) than hexanol (P=0.001). A comparison of regional differences shows the kP and Jmax for ethanol in the groin was significantly lower (P=0.035) than the back. The kP and Jmax for hexanol were significantly higher (P=0.001) in the axilla than the other four skin sites. An understanding of factors influencing percutaneous drug movement is important when formulating topical preparations for the dog.     

中国穿山甲体征及内脏器官解剖学观察

对中国穿山甲的体征及其内脏器官进行解剖和解剖学观察。结果表明：中国穿山甲体重（2.73±0.77）kg,体全长（805±74.61）mm,尾长（356±39.27）mm。身体狭长,头呈圆锥形,吻端尖,耳小,耳长（11±1.17）mm,无齿,舌细长可伸缩;尾扁平,背稍微隆起;头、颈、背、体侧、尾和四肢外侧均被以覆瓦状排列...