丁卡因口腔粘附片的研制

目的：研制丁卡因口腔粘附片。考察不同辅料的体外膨胀行为及释药性能。方法：采用聚维酮（PVP），羟丙甲纤维素（HPMC），羟丙纤维素（L-HPC）及卡波姆934（CP934）为生物粘附材料，以不同配比制备丁卡因口腔粘附片，桨板法测定其释放度。结果：采用CP/HPC，CP/HPMC配比作为粘附材料取得良好效果。     

丁卡因口腔粘附片的研制

目的:研制丁卡因口腔粘附片。考察不同辅料的体外膨胀行为及释药性能。方法:采用聚维酮(PVP)、羟丙甲纤维素(HPMC)、羟丙纤维素(L-HPC)及卡波姆934(CP_(934))为生物粘附材料,以不同配比制备丁卡因口腔粘附片,桨板法测定其释放度。结果:采用CP/HPC、CP/HPMC配比作为粘附材料取得良好效果。     

胰岛素口腔粘附片粘附力的考察

目的：考察胰岛素口腔粘附片生物粘附性。方法：测定以卡波姆（CP）和羟丙基甲基纤维素（HPMC）为粘附材料和缓释骨架,制备不同处方配比的胰岛素口腔粘附片,并测定其粘附力、粘附时间、溶胀百分比和表面pH值。结果：不同处方配比制备的粘附片生物粘附性差异较大,以CP：HPMC为1：1的处方制备的粘附片效果较好,粘附力为79.20±3.51g.cm^-2,粘附时间为4.0±0.63h,溶胀百分率达25%以上。结论：CP：HPMC为1：1的处方制备的口腔粘附片生物粘附性符合要求,可进一步进行体内、外研究。     

制霉菌素口腔粘附片的研制及粘附性考察

目的:研制制霉菌素口腔粘附片,并考察其生物粘附性。方法:以卡波姆(CP)、羟丙基甲基纤维素(HPMC)为粘附材料和缓释骨架制备不同处方配比的制霉菌素口腔粘附片,测定其粘附力、粘附时间、溶胀百分比和表面pH值。结果:不同处方配比制备的粘附片生物粘附性差异较大,以CP∶HPMC为1∶1的处方制备的粘附片效果较好。结论:成功制备了制霉菌素口腔粘附片,其可用于进一步的体内、外研究。     

口腔粘膜粘附制剂的开发

口腔粘膜粘附制剂作为一种新颖的药物释放系统,利用生物粘附聚合物与口腔粘膜间的生物粘附力,延长制剂在口腔内的滞留时间,提高与口腔粘膜的亲合程度,控制制剂中药物的释放速度和释药量。使制剂产生最佳治疗效果。本文阐述了粘膜粘附机理,并对近年来口腔粘膜粘附制剂,如粘附片,半固体剂型等的开发及其发展前景人作一概述。     

影响卡波姆-羟丙基甲基纤维素粘附片粘附性质的因素考察

目的：研究影响卡波姆（Carbopol)-羟丙基甲基纤维素（HPMC）粘附片粘附性质的各种因素。方法：测定Carbopol,HPMC及其不同比例混合物制备粘附片的粘附力，溶胀速率和粘附时间。结果：Carbopol与HPMC以一定比例混合后制成粘附片的粘附力和溶胀速率随HPMC含量增加而下降，而粘附时间与二者比例有关。结论：当Carbopol与HPMC的比例为1：1或1：2时，制备的粘附片具有较大的粘附力，适宜的溶胀速率和较长的粘附时间。     

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。     

甲硝唑口腔粘附片的粘附时间与释药动态研究

甲硝唑口腔粘附片的粘附时间与释药动态研究△ＡＤＨＥＳＩＶＥＴＩＭＥＡＮＤＲＥＬＥＡＳＥＯＦＯＲＡＬＭＵＣＯＳＡＬＡＤＨＥＳＩＶＥＴＡＢＬＥＴＳＯＦＭＥＴＲＯＮＩＤＡＺＯＬＥ陈庆才邵志高余末一陆敏ａ张明玉ａ王为民ａ（南京医科大学，南京２１００２９；ａ泰...     

替硝唑口腔粘附片的制备及质量控制

目的：研究一种持续时间较长,不良反应少的替硝唑口腔粘附剂,方法：以替硝唑为主药,卡波姆940,HPMCK4M为辅料,采用正交设计筛选出最优处方,对其含量测定方法,溶出度,剥离力进行了考察,同时还进行了体内释药实验。结果：该制剂工艺简单,含量测定方法可靠,剥离力为7．8N,体内释药符合Higuchi方程,r=0.9720,T0.5=2.39h,T0.9=6.97h,体外释药亦符合Higuchi方程,r=0.9885,Kh=0.6077.h^-1,可缓慢释放3h以上,结论：本制剂工艺可行,具有维持时间较长的特点。     

紫外分光光度法测定甲硝唑口颊片的含量

目的：测定甲硝唑口颊片中甲硝唑的含量。方法：采用紫外分光光度法,在277nm波长处测定,空白辅料无干扰。结果：甲硝唑浓度在5～15μg/mL范围内与吸光度有良好的线性关系（r=0．9999）,平均回收率为100．4％,RSD=0,51％。结论：该方法简便、灵敏、准确,可供甲硝唑口颊片的含量测定。     

Effect of polymer type on characteristics of buccal tablets using factorial design

A two factor three level factorial design was used to investigate the effects of carbopol and cationic hydrophilic polymers which have a common use in buccal drug formulations. Statistical models with interaction terms were derived to evaluate influence of carbopol (X1) and chitosan (X2) on tablet disintegration (Y1) and dissolution (Y2), mechanical properties (Y3), swelling (Y4). Tablet disintegration studies were carried out using two different pH environments within buccal region pH limits and also two different commonly used dissolution methods for buccal tablets were also investigated to compare the effect of polymer type on dissolution. Polymer type and ratio affect the characteristics of the buccal tablets due to their different physicochemical behavior at buccal pH. Also significant variances between dissolution profiles for buccal tablets, using either USP Paddle or flow through cell methods were found. These results indicate that both polymer type and ratio as well as combination of them effects the drug behavior in different ways.     

In vivo bioavailability studies of sumatriptan succinate buccal tablets

Back ground and the purpose of study

Sumatriptan succinate is a Serotonin 5- HT1 receptor agonist, used in treatment of migraine. It is absorbed rapidly but incompletely when given orally and undergoes first-pass metabolism, resulting in a low absolute bioavailability of about 15%. The aim of this work was to design mucoadhesive bilayered buccal tablets of sumatriptan succinate to improve its bioavailability.

Methods

Mucoadhesive polymers carbopol 934 (Carbopol), HPMC K4M, HPMC K15M along with ethyl cellulose as an impermeable backing layer were used for the preparation of mucoadhesive bilayered tablets. In vivo bioavailability studies was also conducted in rabbits for optimized formulation using oral solution of sumatriptan succinate as standard.

Results

Bilayered buccal tablets (BBT) containing the mixture of Carbopol and HPMC K4M in the ratio 1:1 (T1) had the maximum percentage of in vitro drug release within 6 hrs. The optimized formulation (T1) followed non-Fickian release mechanism. The percentage relative bioavailability of sumatriptan succinate from selected bilayered buccal tablets (T1) was found to be 140.78%.

Conclusions

Bilayered buccal tablets of sumatriptan succinate was successfully prepared with improved bioavailability.     

Design and evaluation of buccal adhesive hydrocortisone acetate (HCA) tablets

Many studies have shown that topical buccal therapy with steroid anti-inflammatory drugs is useful in controlling ulcerative and inflammatory mucosal diseases. This local treatment is based on the concept that a high activity of steroids can be produced at the site of administration and, at the same time, the degree of systemic side effects can be minimized or avoided. In this study we developed a new formulation consisting of a mucoadhesive tablet formulation for buccal administration of hydrocortisone acetate (HCA). Three types of tablet were developed containing three mucoadhesive components: hydroxypropylmethyl cellulose (Methocel K4M), carboxyvinyl polymer (Carbopol 974P), and polycarbophyl (Noveon AA1); the first polymer is a cellulose derivative, the others are both polyacrylic acid derivatives. For each of those, three tablet batches were produced changing the quantity of the mucoadhesive component (10, 20, and 30%), resulting in 9 different formulations. The compatibility of HCA with all excipients using Differential Scanning Calorimetry (DSC) was assessed. Tablets were manufactured by wet granulation followed by compression. Technological controls on granulates (Hausner index, Carr index, granulometry and Karl-Fischer percentage humidity) and tablets (thickness, diameter, friability, hardness, uniformity of content, weigh uniformity and dissolution kinetic) were carried out. Mucoadhesion properties, ex vivo permeability through porcine buccal mucosa, in vivo behavior and compliance were evaluated. Technological controls have demonstrated that the increase in the (percentage) of mucoadhesive causes an increase in granulometry followed by a reduction in the granulate flowability, however all the tablets have given satisfactory technological results and conformed to the 3rd Ed. European Pharmacopoeia specifications. Mucoadhesion, ex vivo permeability and in vivo behavior results notably differed among tablets, depending on the quality and quantity of the mucoadhesive component. An overall comparison of results showed the tablets containing Carbopol 20% resulted to be the best formulation among those developed.     

磷酸氯喹口腔黏附片的研制与质量控制

目的:研究磷酸氯喹口腔黏附片的制备及质量控制。方法:采用羧甲基淀粉钠和聚丙烯酸酯Ⅲ等为辅料,用正交设计筛选出最佳处方。用紫外分光光度法测定磷酸氯喹口腔黏附片的含量。结果:含量测定平均回收率为99%,RSD为0.24%(n=5)。结论:本制剂制备容易,质量稳定,控制方法快速淮确。     

咪康唑颊贴缓释片的黏附性能测试方法的建立及处方优化

目的建立咪康唑颊贴缓释片的黏附性能测试方法并优化处方。方法采用自制黏附力测定装置,运用正交试验法,考察乳蛋白和卡波姆974的比例,乳蛋白和卡波姆974的总量,HPMC的用量三个主要影响因素,对咪康唑颊贴缓释片的黏附力和溶胀速率的影响。结果当乳蛋白∶卡波姆974=2∶1,乳蛋白和卡波姆974总量为30 mg,HPMC的量为20 mg时,咪康唑颊贴片的黏附性能最好,可以满足口腔颊贴缓释片的要求。结论自制的黏附力测定装置可以用于咪康唑颊贴缓释片的黏附性能测试。     

乙酰螺旋霉素片的工艺研究

目的：筛选乙酰螺旋霉素片最佳处方。方法：考察预胶化淀粉、低取代羟丙基纤维素和吐温－８０对乙酰螺旋霉素片的质量影响,并与２种市售乙酰螺旋霉素片作溶出度比较。结果：筛选的最佳处方制备的乙酰螺旋霉素片,体外溶出度大为提高。结论：本法处方合理,工艺简单,适用于工业化生产。