Enhancement of Nasal Salmon Calcitonin Absorption by Lauroylcarnitine Chloride in Rats

Purpose. We investigated optimum formulation characteristics in the nasal absorption of salmon calcitonin (sCT) by incorporation of acylcarnitines. Methods. Nasal sCT formulations were administered to anesthetized rats. Plasma calcium level was measured and pharmacological bioavailability (P.bioav) was calculated. Results. Nasal sCT absorption was significantly enhanced by carnitines with acyl groups of 12 or more carbon atoms. Enhancement by lauroylcarnitine chloride (LCC) was observed at its critical micelle concentration and reached a plateau at the concentration of 0.1%. Optimal absorption was achieved at a molar ratio of LCC to sCT of 5:1. Enhancement was not influenced by osmolarity and maximum enhancement was obtained at pHs 3.1 and 4.0. Conclusions. The 12-carbon LCC was the strongest enhancer among acylcarnitines. Micelle formation played a key role in this enhancement effect.     

The Relative Effect of Azone® and Transcutol® on Permeant Diffusivity and Solubility in Human Stratum Corneum

Purpose. The purpose of this work was to analyse the mechanism of the enhancement of percutaneous penetration demonstrated by the known enhancers Azone^® and Transcutol^®. Methods. Enhancer induced changes in the diffusivity and solubility of a model permeant (4-cyanophenol) in human stratum corneum were monitored (in-vitro) using Attenuated total reflectance Fourier transform infra-red (ATR-FTIR) spectroscopy and compared to the gross effects of the enhancers on flux as measured using simple Franz-type diffusion cells. Results. It has been shown by both the well-established Franz diffusion cell technique and the use of ATR-FTIR spectroscopy that the enhancers studied both increase the flux of cyanophenol across human skin in-vitro by a factor of approximately two. Furthermore, it has been demonstrated by ATR-FTIR that these enhancers are likely to exert their effects by different mechanisms. It is probable that Azone reduces the diffusional resistance of the stratum corneum and that Transcutol increases the solubility of the penetrant in this barrier. Conclusions. There is increasing interest in the apparently synergistic nature in which certain enhancers appear to work. The exact nature of these multiplicative and/or additive effects is not known although there are numerous suggestions in the current literature. The application of ATR-FTIR spectroscopy to such enhancing systems will allow the mechanisms of the observed enhancements to be probed in greater depth.     

3种环糊精对姜黄素角膜渗透性影响研究

目的研究β-环糊精(β-CD)、羟丙基-β-环糊精(HP-β-CD)和磺丁基醚-β-环糊精(SBE-β-CD)对姜黄素离体角膜渗透作用的影响。方法采用改良Franz扩散池,以离体角膜扩散实验考察不同质量分数的3种环糊精对姜黄素角膜渗透性的影响。结果β-CD质量分数为0.02%、0.04%、0.06%、0.08%时,姜黄素的角膜表观渗透系数分别增加了1.06、1.03、1.00、0.95倍,同质量分数的HP-β-CD分别增加了1.16、1.19、1.17、1.12倍,质量分数为0.04%、0.06%时,与对照组相比有显著差异(P0.05);同质量分数的SBE-β-CD分别增加了1.06、1.23、1.08、0.90倍,质量分数为0.04%时,与对照组相比有显著差异(P0.05)。以质量分数为0.06%的SBE-β-CD作为促渗剂,姜黄素释放曲线符合零级释放方程(r=0.997 8);角膜水化平均为81.7%。结论 HP-β-CD质量分数为0.04%、0.06%,分别增加表观渗透系数1.19、1.17倍(P0.05);SBE-β-CD为0.04%时,增加1.23倍(P0.05)。SBE-β-CD作为眼用促渗剂使药物的释放过程更加安全有效;3种环糊精促渗剂对角膜无刺激。     

Advances in understanding the molecular basis of the first steps in color vision

Serving as one of our primary environmental inputs, vision is the most sophisticated sensory system in humans. Here, we present recent findings derived from energetics, genetics and physiology that provide a more advanced understanding of color perception in mammals. Energetics of cis–trans isomerization of 11-cis-retinal accounts for color perception in the narrow region of the electromagnetic spectrum and how human eyes can absorb light in the near infrared (IR) range. Structural homology models of visual pigments reveal complex interactions of the protein moieties with the light sensitive chromophore 11-cis-retinal and that certain color blinding mutations impair secondary structural elements of these G protein-coupled receptors (GPCRs). Finally, we identify unsolved critical aspects of color tuning that require future investigation.     

促进剂对复方脚癣灵搽剂中小檗碱和黄芩苷体外经皮吸收及其皮内滞留量的影响

目的研究复方脚癣灵的体外经皮渗透特征,确定最佳促进剂及浓度。方法以自制双室水平扩散池和离体鼠皮进行体外渗透实验,采用HPLC法同时测定盐酸小檗碱和黄芩苷的皮内含量。结果促进剂为丙二醇和薄荷醇,最佳质量分数均为3%时,复方脚癣灵中2种成分的皮内蓄积量有显著的提高。结论应用促进剂后,制剂中小檗碱与黄芩苷在离体鼠皮内有较强的蓄积作用。     

中药巴布剂的研究进展及展望

目的:解巴布剂的研究现状及其发展前景。方法:本文介绍国内巴布剂的最新研究进展,分别对现阶段巴布剂的基质原料及配比研究、透皮吸收促进剂研究、制备工艺、质量评价标准、药理毒理、临床研究进行综述。结果:巴布剂在现阶段疼痛性疾病的临床治疗中已展现出良好疗效,与其它外用制剂相比具有不可替代的优势。结论:提高其质量可控性和稳定性并将其推向规模化生产是巴布剂今后研究的主要方向,巴布剂必将有良好的市场前景。     

小檗碱对3T3-L1前脂肪细胞增殖及分化相关基因PPARγ、C/EBPα mRNA和蛋白表达的影响

目的 探讨小檗碱对脂肪细胞增殖、分化的影响及其机制。     

复方甲巯咪唑软膏中甲巯咪唑及氢化可的松体外透皮释药研究

 目的：测定不同基质、不同主药浓度、不同渗透促进剂的各种软膏中他巴唑及氢化可的松的体外透皮释药率，评价各因素对主药经皮渗透的影响。方法：用改良Franz垂直扩散池，HPLC测定。结果：A型、B型基质软膏中，他巴唑的透皮释药率分别为49.10%，29.83%(P＜0.05);氢化可的松的透皮释药率分别为3.17%,1.59%(P＜0.05)。有或无月桂氮酮的软膏中，他巴唑的透皮释药率分别为49.10%,54.14%(P＞0.05),氢化可的松的透皮释药率分别为3.17%,1.61%(P＜0.05)。结论：o/w型基质较w/o型基质更有利于他巴唑及氢化可的松的经皮渗透。月桂氮酮对他巴唑无明显的促进渗透作用，但可提高氢化可的松的经皮渗透率1.92倍。