氮酮对鬼臼毒素固体脂质纳米粒透皮性的影响

目的 考察氮酮对鬼臼毒素固体脂质纳米粒透皮性的影响。方法 以大鼠腹部皮肤为屏障，考察氮酮浓度（体积比）对鬼臼毒素固体脂质纳米粒表现透皮系数的影响。结果 当氯酮浓度分别为0，1％，2％，3％。4％，5％，6％时，鬼臼毒素脂质纳誊粒的表观透皮系数（x10^5）分别为24．82，53．05，55．14，43．92，20．57，25．86，23，30。结论 在有效浓度范围内，氮酮可增加鬼臼毒索固体脂质纳米粒的透皮吸收，含不同浓度氮酮的鬼臼毒素固体脂质纳米粒的透皮能力有差异。     

Role of Appendages in Skin Resistance and lontophoretic Peptide Flux: Human Versus Snake Skin

Purpose. 1. The assessment of the role of hair follicles and sweat glands in skin resistance and percutaneous iontophoretic flux of 9-desglycinamide, 8-arginine vasopressin (DGAVP) by comparing two skin species: human stratum corneum which contained hair follicles, sweat and sebaceous glands, and shed snake skin which lacked all appendages. 2. The effect of l-dodecylazacycloheptan-2-one (dodecyl-Azone, a lipid perturbing agent) on the iontophoretic DGAVP flux. Methods. Iontophoresis in vitro was performed in a transport cell (0.79 cm² area available for percutaneous transport) by 8-hours application of a pulsed constant current of 100 Hz, 50% duty cycle and 0.26 mA.cm^–2 current density delivered by a pair of Ag/AgCl electrodes, of which the anode was facing the anatomical surface of the skin samples. Results. The initial resistances of human stratum corneum and shed snake skin samples were of the same order of magnitude (20–24 k.cm²) and both skin species showed a comparable resistance-decrease profile during 8-hours iontophoresis, indicating that the resistances were mainly determined by the stratum corneum and not greatly influenced by the appendageal structures. The initial resistances of the skin samples pretreated with dodecyl-azone were less than 50% of the values of untreated samples. Because dodecyl-azone is known to perturb the ordering of the intercellular lipids, the effect of azone on the resistance confirms that the resistance mainly resides within the intercellular lipids of the stratum corneum. No correlation was found between the iontophoretic DGAVP-flux and the conductance of human skin. For shed snake skin, however, a good correlation was found, indicating that the iontophoretic permeability of human skin in vitro for a peptide such as DGAVP is, unlike shed snake skin, not related to its overall permeability to ions. While the initial resistances of both human and snake skin were in the same order of magnitude and showed the same declining profile during iontophoresis, the steady state iontophoretic DGAVP flux across human stratum corneum was approximately 140 times larger than through shed snake skin. These findings suggest that small ions follow pathways common to both skin types, presumably the intercellular route, while the peptide on the other hand is transported differently: across snake skin presumably along intercellular pathways only, but across human stratum corneum along additional pathways (most likely of appendageal origin) as well. This interpretation is supported by the observations made of the effects of dodecyl-azone on DGAVP-iontophoresis. Pretreatment with dodecyl-azone did not significantly change steady state fluxes and lag times of DGAVP-iontophoresis across human stratum corneum, but resulted in a significant 3-fold lag time decrease and a 3-fold flux increase of DGAVP-iontophoresis across snake skin. Conclusions. The results of these in vitro studies emphasize the importance of the appendageal pathway for iontophoretic peptide transport across human stratum corneum.     

透皮促进剂预处理皮肤对环孢素A经皮渗透的影响

目的：考察透皮促进剂对环孢素Ａ经皮渗透的影响。方法：用透皮促进剂预处理离体小鼠皮肤,以改良的Ｆｒａｎｚ扩散装置进行体外渗透实验。结果：环孢素Ａ经皮渗透符合零级动力学过程,几种透皮促进剂的促渗作用大小依次为月桂氮Ｚｈｕｏ酮－丙二醇（１：１）〉月桂氮Ｚｈｕｏ酮〉水溶性月桂氮Ｚｈｕｏ酮〉二甲基亚砜〉Ｎ－甲基吡咯烷酮〉薄荷油。结论：体外实验证明,透皮促进剂可增加环孢素Ａ的透皮吸收。     

风湿宁贴片中透皮吸收促进剂的筛选研究

目的 :对风湿宁贴片中的透皮吸收促进剂进行筛选研究。方法 :应用均匀设计法从氮酮、丙二醇、油酸中选择风湿宁贴片的透皮吸收促进剂及最佳配比。结果 :氮酮、丙二醇、油酸的含量配比为 6 %∶10 %∶0 %时 ,风湿宁贴片中的青藤碱有最大的透皮速率常数。结论 :氮酮—丙二醇 (6 %∶10 % )是风湿宁贴片较理想的透皮吸收促进剂。     

氮酮用量对马尼地平乳膏离体透皮吸收影响的研究

目的研究经皮吸收促进剂氮酮用量对马尼地平乳膏体外经皮渗透作用的影响,并拟定氮酮的最佳用量。方法分别取含0%、1%、3%、5%氨酮的马尼地平乳膏各约1 g,以1%十二烷基磺酸钠溶液为接受液,小鼠离体皮肤为屏障,采用Franz扩散池进行体外渗透实验,HPLC法测定接受液中马尼地平的含量。结果 24 h内,不同浓度的氮酮对马尼地平乳膏透皮吸收均有一定的促进作用,其促渗作用大小顺序为：3%氮酮〉5%氮酮〉1%氮酮。结论氮酮对马尼地平乳膏的透皮吸收具有一定的促渗作用,但促渗作用不因氮酮的浓度增高而增高,其最佳浓度是3%。     

吲哚美辛巴布剂小鼠离体皮肤透皮吸收实验研究

目的：以吲哚美辛为检测指标,研究氮酮对吲哚美辛巴布剂体外透皮吸收的影响及将该制剂与其市售乳膏剂的体外透皮速率进行比较,为巴布剂的进一步深入研究提供参考。方法：采用改良Franz扩散池进行体外透皮试验,HPLC测定接受液中吲哚美辛含量。结果：含有氮酮的巴布剂较不含氮酮的巴布剂及市售乳膏剂的体外透皮速率明显增大。     

桂氮酮合成中主要杂质的分离与鉴定

报道了以己内酰胺和1-溴代正十二烷为原料，采用液-液相转移催化法合成新型皮肤渗透促进剂桂氮酮产品中主要杂质的分离与鉴定．结果表明，产品中的主要杂质为未反应的原料己内酰胺和副产物6-氨基己酸正十二烷基酯与正十二醚．     

以经皮微渗析技术研究芍药苷大鼠经皮吸收

目的:研究芍药苷的经皮渗透性,并考察透皮渗透促进剂氮酮(azone)对经皮渗透性的影响。方法:以Wistar大鼠为实验动物,采用经皮微渗析技术进行经皮渗透性研究。以浓差法测定探针的体外回收率,以反向渗析法测定探针的在体回收率。结果:氮酮可以显著提高药物透过性,1%,3%,5%azone经皮传递率分别为0.906 9,1.887 8,1.272 8μg.h-1。结论:azone是芍药苷经皮吸收优良的渗透促进剂,且促渗效果与浓度不成线性。经皮微渗析技术是在体研究药物经皮渗透性的有效手段。     

驻极体利多卡因贴剂的透皮促渗作用

目的:研究驻极体对利多卡因透皮吸收的促渗作用。方法:利用Franz扩散池和高效液相色谱法测定利多卡因贴剂、含不同浓度氮酮利多卡因贴剂、正/负极性驻极体利多卡因贴剂和含不同浓度氮酮的正/负极性驻极体利多卡因贴剂在10 h内的体外大鼠皮肤累积渗透量,研究驻极体对利多卡因的透皮促渗作用。结果:(1)含1%、3%和5%氮酮的利多卡因贴剂的10 h药物累积渗透量分别是利多卡因贴剂的1.06、1.10、1.66倍(5%氮酮组有统计学差异,P＜0.05)。(2)含1%、3%和5%氮酮的负极性驻极体利多卡因贴剂与相应的含化学促渗剂利多卡因贴剂具有类似的促渗效果。(3)含1%、3%和5%氮酮的正极性驻极体利多卡因贴剂与相应的化学促渗剂利多卡因贴剂相比,具有更大的增渗倍数(P＜0.05 或P<0.01),且5%氮酮与正极性驻极体对利多卡因的透皮吸收有联合促渗作用。结论:正极性驻极体对利多卡因贴剂有更好的促渗效果,氮酮与正极性驻极体对利多卡因透皮吸收有联合促渗作用,并与氮酮的浓度有关。     

丹参氮酮助渗液对瘢痕治疗作用的探讨

目的　观察 5 %丹参氮酮助渗液对瘢痕的治疗效果并探讨其作用机理。方法　进行离体大鼠皮肤、活体及离体人皮肤对 5 %丹参氮酮助渗液的通透效果测定。并将应用硅膜弹力布贴膏治疗的 30 1例增生性瘢痕患者分成治疗组和对照组 ,治疗组使用含 5 %丹参氮酮助渗液的布贴膏 ,对照组则不含 ,对两组进行临床疗效观察比较。结果　离体大鼠皮肤通透试验经Poisson级数差别检验 ,差异有非常显著性意义 (χ2 =84 6 32 98,P <0 0 1) ;活体及离体人皮肤的通透效果测定 ,差异有非常显著性意义 (χ2 =15 9,P <0 0 1) ,说明 5 %丹参氮酮助渗液透皮效果良好 ;临床观察治疗组总有效率为 91 4 % ,对照组总有效率为 71 3% ,治疗组明显优于对照组。结论　 5 %丹参氮酮助渗液可以渗入皮肤 ,能显著降低皮肤电阻值 ,增加皮肤通透性 ,与硅膜弹力布贴膏合用对瘢痕有着良好的治疗效果。