Enhancing Mechanism of Enhancers as a Basis for Delivery of Bioactive Peptides

当利多卡因溶解在水凝胶中时，药物被很好地吸收，当针头穿过皮肤注射人类生长激素时，疼痛减轻。虽然地尔硫卓可以很好地通过胃肠道吸收，但由于地尔硫卓通过口腔黏膜的吸收效率不高，因此需要能够通过口腔黏膜快速吸收药物的配方。由于药物在口腔中的快速溶解，需要在口腔中产生高浓度，以增加口腔的吸收，并在血液中提供足够的浓度。两性霉素B分子量为924，是一种大分子，不易被胃肠道吸收。为了以可预测的方式吸收药物，必须对配方进行一些修改。测量了成人和儿童血液中的药物浓度，两者的浓度都很低。以壳聚糖为代表，研究了其对亲水性药物鼻腔吸收的影响。水溶性在高分子量壳聚糖中受到限制，中等可溶性壳聚糖样品进行了检测。磷酸核黄素因其亲水性和易于测定而被用作多肽模型。从几家公司获得了壳聚糖样品，采用了四种高水溶性样品进行研究。研究了壳聚糖对家兔鼻黏膜吸收核黄素的影响。由于其他样品比壳聚糖C-9更难溶于水，因此研究了壳聚糖浓度对增强磷酸核黄素吸收的影响。在0.5%、1%和2%中，最大增强效果为0.5%。壳聚糖可提高胰岛素的生物利用度。等值素，一种阿苏烯的衍生物，能有效地提高胰岛素和鲑鱼降钙素的生物利用度。

When lidocaine is dissolved in an aqueous gel, the drug is absorbed well, and decreased pain when a needle is inserted through the skin for injection of human growth hormone.Al though diltiazem is absorbed through the gastrointestinal tract well, formulations which enable to absorb the drug fast through oral mucosa is required since absorption of diltiazem through the oral mucosa is not very efficient. High concentrations in the mouth caused by fast dissolution of the drug in the mouth are required to increase absorption from the mouth and to give enough concentrations in the blood.Amphotericin B with molecular weight of 924 is a large molecule and is poorly absorbed from the gastrointestinal tracts. In order to absorb the drug in a predictable fashion, some modification in formulation is necessary. Concentrations of the drug in the blood were measured both in adults and children and low in both.Effect of chitosan, a polysaccaride with amino groups, on nasal absorption of hydrophilic drugs was studied as a representative of basic polymers. Aqueous solubility is limited in high molecular weight chitosan, and moderately soluble chitosan samples weer examined. Riboflavin phosphate was used as a model of peptides because of its hydrophilic nature and its easy assay. Chitosan samples were obtained from several companies and four samples with high aqueous solubility were employed in the study. Effect of chitosan on absorption of riboflavin phosphate through nasal mucosa in rabbits was studied. Effect of concentrations of chitosan on enhancing absorption of riboflavin phosphate was studied in Chitosan C-9 because other samples were less soluble than this in water. Maximal enhancing effect was noted at 0.5% among 0.5,1, and 2%. Bioavailability of insulin was increased by chitosan.Egualen, a delivative of azulene was effective in increasing bioavailability of insulin and salmon calcitonin.