口腔黏膜黏附制剂的研究概况

口腔黏膜黏附制剂是一种新的药物释放系统,系利用生物黏附材料与口腔黏膜间的生物黏附力,延长制剂在口腔中的滞留时间,控制药物的释放速度和释药量,使制剂产生最佳疗效.该文作者就口腔黏膜黏附制剂的特点、生物黏附材料的选择及近年来的口腔黏膜黏附制剂的研究概况作一综述,并展望了其发展前景.     

口腔黏膜黏附制剂研究概况

口腔黏膜黏附制剂是一种新的药物释放系统,系利用生物黏附材料与口腔黏膜间的生物黏附力,延长制剂在口腔中的滞留时间、控制药物的释放速度和释药量,使制剂产生最佳疗效.本文就口腔黏膜黏附制剂的特点、生物黏附材料的选择及近年来口腔黏膜黏附制剂的研究概况作一综述,并展望了其发展前景.     

中药口腔生物黏附制剂的研究进展

目的对近年来中药口腔生物黏附制剂的研究概况作一综述。方法根据国内外文献资料进行整理归纳。结果中药口腔生物黏附制剂是一种新型的药物释放系统,是以生物黏附材料为药物载体,通过生物黏附作用,长时间黏附于黏膜而发挥疗效,从而延长制剂在口腔中的滞留时间,控制药物的释放速度和释药量,使制剂产生最佳疗效。结论中药口腔生物黏附制剂对于治疗口腔局部病变方面有重要意义。     

口腔黏膜黏附制剂的研究进展

口腔黏膜黏附制剂是以生物黏附材料为药物载体,通过生物黏附作用长时间黏附于黏膜而发挥疗效的药物制剂。该文就口腔黏附制剂的特点、药物口腔黏膜吸收的影响因素及近年来口腔黏附制剂的研究应用进行了综述。     

漂浮-生物黏附协同作用制剂的研究进展

目的介绍漂浮-生物黏附协同作用制剂研究进展。方法对漂浮-生物黏附协同作用制剂的作用特点、制备方法及体外评价方法进行综述。结果该制剂可以延长药物在胃内的滞留时间,提高生物利用度。结论随着研究的深入,漂浮-生物黏附制剂将逐步受到重视,成为常用的药物新剂型之一。     

生物黏附给药系统新剂型

系统查阅国内外有关生物黏附给药系统及生物黏附制剂的相关文献,进行归纳总结。生物黏附制剂可黏附于特定部位来控制药物释放速率,提高药物浓度,减少不良反应,增加疗效。其开发积极推动了制剂现代化的发展。     

阴道生物黏附缓释制剂的研究进展

综述了近年来国内外阴道生物黏附缓释新型制剂的进展,包括生物黏附性缓释乳膏、生物黏附阴道片、缓释凝胶剂等.     

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。     

胃肠道生物黏附给药系统研究进展

胃肠道生物黏附给药系统(GBDDS)是指利用聚合物与胃、肠黏膜黏液层/上层细胞表面之间的生物黏附,延长药物制剂在胃肠道停留时间或特定部位作用时间的给药系统,在缓控释给药系统中占重要地位.现对胃肠道生物黏附作用的机制、影响因素、生物黏附材料的种类和生物黏附制剂的体内外评价方法进行综述,旨在为研究开发新型口服给药系统提供新的思路和方法.     

生物黏附给药新剂型的发展近况

生物黏附给药系统(bioadhesive drug delivery system,BDDS)是现代给药剂型中一个新兴分支。生物黏附制剂是一类以生物黏附材料为药物载体,通过生物黏附作用长时间黏附于黏膜而发挥疗效的药物制剂。与其他给药剂型相比,生物黏附制剂有以下主要优点:①载体多由具有生物黏附材料所组成,对黏膜都有不同程度的黏附作用,可以延长释药     

生物黏附凝胶剂的研究与开发

生物黏附凝胶剂具有药效持久、稳定性好、制备简单、应用方便等众多优点。本文从药物品种、处方设计、制备工艺等方面综述生物黏附凝胶剂的研究与开发近况。     

Studies on bioadhesive PLGA nanoparticles: A promising gene delivery system for efficient gene therapy to lung cancer

The study aimed to design novel bioadhesive PLGA nanoparticles for efficient gene delivery to lung cancer cells. The bioadhesive agent and stabilizer, Carbopol 940 was chosen to establish bioadhesive PLGA nanoparticles and Pluronic F68, Pluronic F127 stabilized PLGA nanoparticles were formulated as control. The effects of different surfactants on the physicochemical and biological characterizations of PLGA nanoparticles were compared. All the obtained nanoparticles showed negative surface charge, similar spherical morphology, a relatively narrow particle size distribution, and lower cytotoxicity to A549 cells comparing with Lipofectamine 2000. Carbopol stabilized nanoparticles hold advantages in DNA-binding efficiency (>80%) at an optimal Carbopol concentration, DNA protection from enzymatic degradation in vitro release and better buffering capacity. Most importantly, higher transfection efficiency in A549 cells was observed comparing to Pluronics stabilized nanoparticles or naked DNA, similar to that of Lipofectamine 2000. These results revealed that the bioadhesive PLGA nanoparticles formulated with Carbopol might be a very attractive candidate as a non-viral vector for lung cancer gene therapy and might alleviate the drawbacks of the conventional cationic vectors/DNA complexes for gene delivery in vivo.     

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。     

Efficacy of a new ketoconazole bioadhesive vaginal tablet on Candida albicans

To develop more effective treatment for vaginal candidasis, ketoconazole (KTZ) was formulated in bioadhesive tablet formulations that increase the time of contact of drug with the vaginal mucosa. The bioadhesive vaginal tablets delivery of KTZ was prepared by direct compression of sodium carboxymethyl cellulose or polyvinylpyrrolidone or hydroxypropylmethyl cellulose (HPMC-E(50)). Dissolution studies of bioadhesive tablets and commercial ovules were carried out with a new basket method (horizontal rotating basket). In vitro, a good sustained release action was obtained with bioadhesive tablets containing 1:1 and 1:2 drug/polymer ratio using HPMC-E(50). These bioadhesive tablets containing 400 mg of KTZ showed a zero-order drug release kinetic. KTZ solutions at increasing concentrations (0.16, 0.33, 0.5 and 0.66 mg/ml) were prepared for microbiological trials. These concentrations correspond to 25%, 50%, 75% and 100% of KTZ released from bioadhesive tablets, respectively. Yeast mixture was mixed with each concentration of KTZ at ratio of 1:10. One hundred microliters of this mixture was transferred in 900 microl liquid Sabouraud medium after a certain time interval for each concentration of KTZ and incubation at 37 degrees C for 24 h. Then this culture streaked onto Sabouraud-dextrose-agar plates, which were incubated at 37 degrees C for 48 h. The 0.16 and 0.33 mg/ml concentrations of KTZ showed fungistatic effect in 120 min. The 0.5 mg/ml concentration of KTZ was fungistatic in 90 and 120 min; and the 0.66 mg/ml concentration of the drug was fungistatic in 120 min as well as in 180 min. It was found that, in vitro antifungal activity of KTZ was dependent on its concentration and contact time with yeast cells. These results indicated that a new bioadhesive vaginal tablet formulations might be further developed for safe convenient and effective treatment of vaginal candidasis.     

In Vitro-In Vivo Evaluation of a Controlled Release Buccal Bioadhesive Device for Oral Drug Delivery

Purpose. To investigate the use of buccal bioadhesive device in targeting controlled drug delivery to the gastrointestinal tract. Methods. A three-leg crossover study was designed to evaluate the application of buccal bioadhesive device for providing controlled drug delivery to the gastrointestinal tract of a model drug cyanocobalamin in four healthy adult male beagle dogs. Results. In vitro dissolution studies using deionized water as the medium indicated that 100% of the drug was released within 15 min from a immediate release oral capsule formulation, whereas 90% of the drug was released within a period of 18 hrs from a buccal bioadhesive device formulation. Drug release from the buccal bioadhesive devices appeared to follow Higuchi's square root of time dependent model. The terminal half-life of the drug following I.V. administration in four dogs was found to be 16.4 ± 2.4 hrs. Following immediate release oral capsule administration of the drug C_max, t_max and bioavailability were 2333 ± 1469 ng/L, 2.5± 1.0 hrs and 14.1 ± 7.9%, respectively. Following buccal bioadhesive device administration of the drug C_max, t_max and bioavailability were 4154 ± 1096 ng/L, 11 ± 1.2 hrs and 35.8 ± 4.1%, respectively. Significantly higher bioavailability of the drug was observed with the buccal bioadhesive device administration when compared to the immediate release oral capsule. Conclusions. The buccal bioadhesive device appears to improve the oral bioavailability of cyanocobalamin by providing controlled delivery of the drug to the gastrointestinal tract.     

乙酰螺旋霉素口腔贴片的研制及体外释药的考察

目的:研制乙酰螺旋霉素口腔贴片。方法:以卡波姆934P和HPMC(K4M)作为黏附材料,制备口腔贴片,并对其生物黏附力及体外释放度进行了考察,采用一阶导数光谱法测定乙酰螺旋霉素的含量。结果:卡波姆934P的生物黏附性优于HPMC,体外释放均符合Higuchi方程,HPMC的缓释效果优于卡波姆934P。结论:处方中以卡波姆934P与HPMC配比为1:1时为最优处方。     

盐酸索他洛尔生物粘附微球的制备及体外释药特性研究

目的：制备盐酸索他洛尔生物粘附微球,考察其体外释药特性并评价其粘附性能。方法：应用正交试验筛选盐酸索他洛尔生物粘附微球的最佳处方,采用高效液相色谱法测定盐酸索他洛尔生物粘附微球的含量与释放度,选用滞留率为指标考察微球的粘附特性。结果：盐酸索他洛尔生物粘附微球的最佳处方为盐酸索他洛尔投药量占处方组成的30％．分散相与连续相比为70％,司盘80用量为9．0g;体外释药试验结果表明盐酸索他洛尔生物粘附微球30min累积释药百分率达30％,4h释药达90％;离体法与在体法测得微球胃黏膜上的滞留率分别为（87．6±2．8）％与（60．2±9．8）％。结论：盐酸索他洛尔生物粘附微球处方设计合理,制备工艺简单,与盐酸索他洛尔普通片相比,盐酸索他洛尔生物粘附微球具有一定缓释特性,且其在离体与在体模型中粘附性能良好。     

绿原酸生物黏附微球的制备及其体外释放特性的研究

目的制备绿原酸生物黏附微球,并考察其体外释放规律和黏附性。方法采用液中干燥法制备绿原酸生物黏附微球,结合微球的释放行为,单因素筛选最佳处方和工艺;用HPLC法考察其体外释放性质,采用滞留率作为考察其黏附性的指标。结果绿原酸生物黏附微球在最佳处方条件下的平均载药量为17.25%,平均包封率为57.25%;微球在体外12 h可释放92.07%,体外释药符合Weibull模型:ln[ln[1/(1-Q)]]=0.6376lnt-0.4373(r=0.9819);体外黏膜平均滞留率为78.54%,体内黏膜平均滞留率为30.23%。结论所用制备工艺稳定可行,所制微球具有明显的缓释效果。     

Pressure-sensitive mucoadhesive polymer-based dental patches to treat periodontal diseases: an in vitro study

Abstract

Local drug delivery for periodontal diseases is still a challenge due to very short residence time, involuntary swallowing and salivary wash-out. Present study is, therefore, an attempt to develop pressure-sensitive adhesive polymers-based mucoadhesive dental patches to ensure satisfactory prolonged release of drugs, to treat periodontal diseases locally. Polymers such as duro-tak® 387-2516 and duro-tak® 387, ethylcellulose, polyvinylpyrrolidone, polyvinyl alcohol along with drugs amoxicillin trihydrate and diclofenac sodium were used to develop the experimental patches. The patches were characterized for mass variation, thickness, area, moisture-content and moisture-uptake, folding endurance, structural integrity in simulated saliva, bioadhesive strength, surface pH, scanning electron microscopy, cellular morphology, in vitro drug release and temperature-dependant stability study as per ICH guideline. Incorporation of release enhancers in the patches improved drug release. Drugs released in a sustained manner due to the formation of physical bonds between the polymers (as assessed by FTIR study) which might alter the length of drug diffusion pathways. The formulation F3 with tween 80 as release enhancer provided best drug release profile over the period of 8?h, thus it could be a successful attempt for the management of oral pathogens and dental pain.     

大蒜油口腔黏附片的研究

目的 研制大蒜油口腔黏附片,并考察其生物黏附性及释药性能.方法 采用羟丙基甲基纤维素(HPMC)和卡波姆(Carbopol 934P)为黏附材料,制备不同处方配比的大蒜油口腔黏附片,测定其体外溶胀百分率、黏附力和黏附时间,并采用浆法测定释放度.结果 以HPMC: Carbopol 934P为3:1的处方制得的口腔黏附片较好.结论 成功制备了大蒜油口腔黏附片.