生物粘附材料的研究进展

目的系统地了解生物粘附材料的类别和性质 ,生物粘附的机理 ,影响生物粘附的因素 ,生物粘附性的实验研究方法 ,生物粘附材料在制剂中的应用及存在的问题。方法对近期的文献进行检索、分类和整理。结果对生物粘附传递系统的研究比较活跃 ,但性能优良的生物粘附材料的品种较少 ,生物粘附的机理尚不完全清楚 ,生物粘附性的实验研究方法有待于完善。结论生物粘附传递系统将具有较好的应用前景。     

生物粘附给药系统研究进展

本文收集了国内近年来有关生物粘附给药系统研究状况的文献,对生物粘附给药系统的作用机理、常用粘附材料、生物粘附制剂技术的应用等进行了综述,表明生物粘附给药系统具有较高的生物利用度,应用前景广阔。     

生物黏附制剂的黏附机制及其新剂型的发展近况

随着具有优良粘附性、稳定性及生物相容性的生物粘附聚合物的发展,新的粘附制剂将不断出现。现就生物粘附制剂的粘附机制及其新剂型的发展近况作一综述。     

口腔粘附制剂的研究与应用

从口腔中附制剂的特点、芗的口腔吸收的机制、生物粘附产选择、口腔粘附制剂的应用及展望等几个方面介绍了国外对口腔粘附制剂的研究概况。指出：口腔粘附制剂在局部治疗口腔疾病人有缓释、定位的优点,在进行全身治疗时也因避免了药物在胃肠道降解和肝首过效应,提高了生物利用度。所以,口腔粘附制剂具有广阔的发展前景。     

生物粘附给药系统进展概况

目的：介绍生物粘附给药系统国内的研究状况。方法：收集国内近年来有关文献，内容包括生物粘附给药系统的作用机理、常用粘附剂的制剂、质量评价、测定方法等。结果：生物粘附给药系统作用机理比较明确，不同部位不同作用特点的粘膜制剂已有较多的报道和应用。结论：生物粘附给药系统具有较高的生物利用度，应用前景较好。     

颊粘膜给药系统的研究概述

颊粘膜给药是生物粘附性制剂中的一种。生物粘附性制剂近年来发展很快 ,该制剂在控制药物释放、提高药物生物利用度和靶向给药等方面具有明显优势。在颊粘膜给药系统中 ,药物通过颊粘膜可以直接入血 ,避免肝首过作用及胃肠的代谢 ,故对于肝首过作用显著和口服利用度低的药物有开发价值。此外 ,颊粘膜给药既能迅速发挥药效 ,又能长时间维持药效 ,因而具有缓释的作用 ,较只有迅速显效作用的舌下给药有更广泛的应用范围。现将近年来国内外有关颊粘膜给药系统的研究状况 ,概述如下 :1　生物粘附1 1　生物粘附机制[1]生物粘附 (ｂｉｏａｄｈｅｓ…     

生物粘附性给药系统的研究

生物粘附性给药系统是年年来药剂学的研究热点,它以特有的缓、控释优势而成为很有前途的剂型。本文对生物粘附作用原理、生物粘附性制剂的给药特点、剂型及发展趋向等进行综述。     

生物粘附性聚丙烯酸类高分子在药剂中的应用

介绍了几种具有生物粘附性的丙烯酸类高分子的结构、粘附机制、影响粘附性因素及其在生物粘附制剂中的应用。     

生物粘附性微粒在黏膜给药中的应用进展

生物粘附性微粒是生物粘附给药系统的重要组成部分，将生物粘附特性与微球制剂结合的给药载体的研究近年来广受关注。生物粘附性微粒制剂结合了生物粘附和微粒两种载体的优点，可通过各种黏膜吸收控制药物释放、达到靶向给药。该文介绍了生物粘附性载体的特点、影响因素、材料和应用的最新进展。     

第二代胃肠道生物粘附材料——凝集素及其应用

近20年来 ,人们发现很多聚合物与机体组织粘膜可产生较长时间的粘着力 ,即生物粘附作用 (bioadhesion) ,这些生物粘附聚合物被广泛研究用于药物传递 ,从而形成了生物粘附制剂(bioadhesivedrugdeliverysystem)。生物粘附制剂 ,特别是口服生物制剂 ,具有很多的优点 ,可延长制剂在胃肠道的停留时间 ,增加药物吸收总量 ,提高药物吸收速率 ,还可用于结肠定位给药 ,保护在胃肠道不稳定的药物及发挥局部治疗作用。但是 ,普通的粘附材料有一个共同的缺点 ,即它们对相应的底物没有特异性 ,特别是在胃肠道给药中 ,这可能引起药物的过早失活 ,限制药物…     

凝集素介导的生物黏附微粒制剂研发趋势

阐述了第二代生物黏附微粒制剂的概念及黏附机制，介绍了影响凝集素黏附性能的因素和凝集素的类型，并对该系统的应用及发展趋势进行了概述。生物黏附释药系统作为一种新颖的药物释放系统，以特有的靶向性，缓、控释等优势成为很有前途的给药系统。其中凝集素介导的第二代生物黏附给药系统具有特异靶向性，微粒制剂又在提高药物稳定性、控制药物释放等方面具有优势。     

生物黏附制剂的研究进展

目的对生物黏附制剂研究进展进行综述。方法参考近几年国内外文献30余篇,介绍利用生物黏附材料作为制剂载体,以给药途径的不同阐述生物黏附新剂型的研究进展。结果目前生物黏附制剂给药途径一般分为口腔给药、眼部给药、鼻黏膜给药、胃肠道给药和阴道盆腔给药。利用各种具有生物黏附功能的辅料,制备不同剂型的制剂,给药后黏附于特定给药部位,可以控制释药速率,提高靶部位药物浓度,进而提高疗效。结论归纳总结国内外生物黏附制剂最新研究进展,生物黏附制剂具有良好的缓、控释释药及靶向给药等优势,具有较高的市场开发潜力。     

小檗碱生物黏附缓释片的制备及体外评价

目的 测定小檗碱生物黏附缓释片和大鼠离体胃组织的黏附力,探究其体外释药作用,制备小檗碱生物黏附缓释片。方法 以羟丙基甲基纤维素(HPMC)和卡波姆(carbopol,CP)为生物黏附材料,通过正交试验对辅料用量进行优化。测定生物黏附缓释片的释放度,溶出介质为人工胃液(pH=1.2)。通过自制黏附力测定装置测定、比较小檗碱生物黏附缓释片和盐酸小檗碱片对大鼠离体胃组织的黏附力。结果 每片生物黏附缓释片中974P/971P为1/3,卡波姆用量为20 mg,羟丙基甲基纤维素为15 mg。生物黏附缓释片的体外释放达到缓释制剂要求,与普通片剂相比其对大鼠离体胃组织的黏附力更大。结论 小檗碱生物黏附缓释片的处方和工艺能够达到设计要求。     

In-vitro evaluation of bioadhesion in particulate systems and possible improvement using interactive mixtures

The bioadhesion of tablet components was tested using the fracture method (maximum tensile stress in detaching the sample from mucus membrane) and comparing traditional tablet specimens with powder monolayers. Both nonadhesive excipients and established mucoadhesive materials were investigated. Some nonadhesive materials showed unexpectedly good adhesive properties when tested as tablets but not as powders. Conversely, some bioadhesive materials had unexpectedly low adhesive properties when tested as tablets. Thus, powder specimens of some materials appear to give more realistic results than tablet specimens in this respect. The use of powder specimens seems particularly applicable for testing dispersible tablets intended for transmucosal absorption. Potential for increasing the bioadhesive properties of coarse, nonadhesive carrier particles by coating them with fine particles of bioadhesive materials during dry mixing (forming interactive mixtures) was also studied. The tensile strength of the adhesive bond between the mucosa and the nonadhesive excipients was improved when fine cross-linked carboxymethyl cellulose sodium (Ac-Di-Sol) particles were added. The addition of increased proportions of Ac-Di-Sol initially improved the bioadhesive properties until a plateau was reached. A standardised test of bioadhesive capacity could therefore involve the addition of fine bioadhesive powders to coarse carriers in proportions close to those providing monoparticulate surface coverage. Interactive mixtures such as these may also offer potential as a tool for use in the development of bioadhesive drug formulations.     

Comparison of salivary miconazole concentrations after administration of a bioadhesive slow-release buccal tablet and an oral gel

Summary The salivary miconazole concentrations after administration of a bioadhesive slow-release buccal tablet and an oral gel have been compared. The bioadhesive tablet consisted of a mixture of thermally modified starch and 5% polyacrylic acid.Although the amount of drug administered via the bioadhesive tablet was sixfold lower than when the gel was used, the salivary miconazole levels were higher and remained above the MIC value ofCandida albicans for more than 10 hours. The mean adhesion time of the tablet was 586 min.The bioadhesive tablet appears to be a promising drug delivery system for the buccal administration of drugs for local therapy.     

Bioadhesive delivery of metformin using prosopis gum with antidiabetic potential

The antidiabetic properties of prosopis gum alone and as a bioadhesive base for the delivery of metformin are presented. The bioadhesive value of the gum was commensurate with those of Carbopol 974-P and sodium carboxymethyl cellulose (NaCMC). The release of the drug was higher from prosopis gum based bioadhesive formulations than from NaCMC and Carbopol 974-P products. This was shown by the shorter time required to reach t(50) (the time required for 50% of the drug to be released) or t(20) (time required for 20% of the drug to be released) for the release of metformin. The gum showed moderate antidiabetic properties when used alone. In combination with metformin in a bioadhesive form, the glucose lowering effect was found to be synergistic. The areas under the plasma drug concentration vs. time curves (AUCs) for the bioadhesive combinations were similar to those of the drugs alone in an aqueous system. This shows that the gum did not interfere with absorption of the incorporated drug. However, the areas under the effect vs. time curves (AUECs) were much higher when combined in a bioadhesive form than with the drug alone. The AUCs obtained with NaCMC based bioadhesive formulations were relatively smaller than those of metformin in an aqueous system and the combinations of metformin and prosopis gum.     

法莫替丁生物黏附缓释片的体外释放研究

目的:评价法莫替丁生物黏附缓释片的体外释放特性。方法:建立法莫替丁生物黏附缓释片释放度的高效液相色谱测定法,运用Higuchi方程、Ritger-Peppas方程拟合其释放过程,采用Peppas修正式分析释放过程中不同机制的释药比例。结果:Ritger-Peppas方程更能拟合法莫替丁生物黏附缓释片的释放,凝胶骨架溶蚀机制在法莫替丁生物黏附缓释片的释放评价中占有更重要的地位。结论:Peas修正式可定量评价法莫替丁生物黏附缓释片的体外释放。     

Formulation and evaluation of controlled release Eudragit buccal patches

Controlled release buccal patches were fabricated using Eudragit NE40D and studied. Various bioadhesive polymers, namely hydroxypropylmethyl cellulose, sodium carboxymethyl cellulose and Carbopol of different grades, were incorporated into the patches, to modify their bioadhesive properties as well as the rate of drug release, using metoprolol tartrate as the model drug. The in-vitro drug release was determined using the USP 23 dissolution test apparatus 5 with slight modification, while the bioadhesive properties were evaluated using texture analyzer equipment with chicken pouch as the model tissue. The incorporation of hydrophilic polymers was found to affect the drug release as well as enhance the bioadhesiveness. Although high viscosity polymers can enhance the bioadhesiveness of the patches, they also tend to cause non-homogeneous distribution of the polymers and drug, resulting in non-predictable drug-release rates. Of the various bioadhesive polymers studied, Cekol 700 appeared to be most satisfactory in terms of modifying the drug release and enhancement of the bioadhesive properties.     

中心复合设计法优化维生素C阴道生物黏附缓释片处方

目的：制备维生素C阴道生物黏附缓释片,考察其释放和黏附性能的影响因素,并运用中心复合设计法优化处方。方法：选用羟丙甲纤维素和卡波普分别作为骨架材料及生物黏附材料制备缓释片,采用自制装置测定缓释片的生物黏附力,应用相似因子法评价不同处方工艺制备的缓释片释放行为;以缓释片的生物黏附力和释放度综合评分为评价指标,对羟丙甲纤维素和卡波普的用量进行多元线性回归和二项式拟合,预测最优处方。结果：经预测分析,获得最优处方,且由此优化处方制备的缓释片各评价指标的实验值与预测值很接近。结论：应用中心复合设计法优化维生素C阴道生物黏附缓释片处方,切实可行。