胰岛素鼻黏膜给药系统的研究进展

目的综述胰岛素近年来鼻黏膜给药的相关信息。方法查阅国内外相关文献36篇,进行相关分析、归纳和总结。结果综述出鼻黏膜给药的特点以及提高鼻黏膜生物利用度的诸多方法。在胰岛素制剂中加入安全高效的吸收促进剂或水不溶性粉末将会很大程度上提高其生物利用度。结论胰岛素鼻黏膜给药在药学领域将会有广阔的发展前景。     

基于微透析技术的花椒挥发油在体经皮促透作用研究

该文拟采用经皮微透析技术测定花椒挥发油对不同脂溶性中药成分皮肤药动学行为的影响,评价其在体经皮促透特征。选择川芎嗪和葛根素作为亲脂性和亲水性模型药物,采用浓差法考察微透析探针体外回收率与传递率,采用反向渗析法测定药物探针在体回收率;以常用化学促透剂氮酮为阳性对照,测定不同浓度花椒挥发油对川芎嗪和葛根素的皮肤药动学行力影响。结果显示,2种模型药物探针回收率与传递率相等,药物在渗析膜间无相互作用,川芎嗪和葛根素的在体相对回收率分别为59.17%,19.85%。在体经皮试验表明花椒挥发油对川芎嗪具良好促透效果,且呈浓度依赖性关系,5%花椒挥发油的在体促透倍数(ER)为98.64,比氮酮最佳浓度的促透效果更好(3%氮酮,ER=89.11);同时,花椒挥发油也可显著增加葛根素的在体经皮吸收,也表现出浓度依赖性关系。因此,该研究进一步证实花椒挥发油作为经皮促透剂的良好促透性能,为其在中药外用制剂中的应用提供了数据支持。     

Scientific evidence for traditional claim of anti-obesity activity of Tecomella undulata bark

Ethnopharmacological relevance

The bark of Tecomella undulata is traditionally claimed in the treatment of various disease ailments including obesity and cancer. Till now there are no studies about anti-obesity activity of Tecomella undulata bark.

Aim of the study

The present study was aimed to establish a scientific evidence for anti-obesity efficiency of ethyl acetate extract of Tecomella undulata bark (EATUB). Further to standardize the active fractions of EATUB using different biomarkers.

Materials and methods

We investigated activity of EATUB fractions (F1–F7) using 3T3-L1 fibroblasts. Further, F1-mediated effects were characterized by determining mRNA and protein levels of SIRT1, one of the key targets for the treatment of obesity, using semi-quantitative RT-PCR (sqRT-PCR) and western blot analysis. The consequences of modulation of SIRT1 on mRNA and protein levels of various adipogenesis mediators like PPARγ, C/EBPα, E2F1, leptin, adiponectin and LPL were also studied. In vivo studies were performed using High Fat Diet (HFD) obese mice.

Results

Our data showed that compared to controls, preadipocytes and adipocytes incubated with F1 exhibited a significant decrease in adipogenesis and lipogenesis. In addition, sqRT-PCR and western blot analysis showed significant increase in SIRT1 and adiponectin levels and decrease in PPARγ, C/EBPα, E2F1, leptin and LPL levels in preadipocytes and adipocytes. In vivo studies of F1 in HFD induced obese mice showed significant improvement in lipid profile and glucose levels. The bioactive fraction (F1) was determined to possess 4.95% of ferulic acid.

Conclusion

Thus, our findings signified the beneficial effects of Tecomella undulata bark in pharmacologic interventions related to obesity and metabolic disorders. Ferulic acid and rutin are being reported and quantified for the first time from the bark of Tecomella undulata.     

中药透皮吸收促进剂的研究进展

中药透皮吸收促进剂具有起效快、效果好、副作用小、无污染等优点,总结近年来常用中药透皮吸收促进剂的研究进展,中药透皮吸收促进剂主要包括单一中药透皮吸收促进剂和含中药PE多元透皮吸收促进剂,并对存在的问题及今后的研究前景进行了思考和展望。     

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。     

萜烯类经皮渗透促进剂的研究与应用进展

透皮给药系统可有效避免肝脏首过效应及胃肠道降解，调控释药速率和血药浓度，降低不良反应及用药频率，提高患者顺应性。但角质层的屏障作用和药物的低渗透量，使其应用受到限制。萜烯类经皮渗透促进剂具有毒性低，促透能力强，可改善皮肤通透性，对亲水、亲脂药物均有促渗作用，低浓度高促透性的特点，在透皮给药系统中日益发挥着重要作用，显示出良好的应用前景。对其来源、分类、促透机制、实际应用、选择评价及应用前景进行综述。     

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.