放线菌素D阴道生物黏附片的研制

目的：研制一种持续作用时间长，毒副作用小的放线菌素D阴道生物黏附片。方法：以放线菌素D为主药，卡波姆934（CP934）、羟丙基纤维素（HPC）、乳糖、酸碱产气系统（碳酸氢钠和枸橼酸）为辅料。采用正交设计试验制备了不同处方的放线菌素D阴道生物黏附片。同时用自制黏附力测定装置测定了黏附片的黏附力；用桨法测定了体外释药速率。结果：最优处方为CP934：HPC=2：3，乳糖用量20％，酸碱产气系统用量5％。结论：本制剂工艺简单、可行，可通过调节处方配比，获得生物黏附力和体外释药均较理想的处方。     

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.     

格列齐特生物黏附缓释片的研制及体外评价

目的制备格列齐特生物黏附性缓释片,考察其体外释药行为,并测定其与家兔离体胃、小肠组织的黏附力.方法以羟丙基甲基纤维素(HPMCK15M)和卡波姆(carbopol,CP)为生物黏附材料和骨架材料,乳糖为稀释剂制备生物黏附性缓释片.以磷酸盐缓冲液(pH 8.6)400 mL为溶剂,转篮法(转速150 r·min-1)测定2、12、20 h时的释放度.以自制黏附力测定装置测定、比较格列齐特生物黏附性缓释片及格列齐特(Ⅱ)片对家兔离体胃、肠组织的黏附力.结果生物黏附性缓释片体外释放符合缓释制剂要求,其与家兔离体胃、肠组织的黏附力明显大于普通片剂,且与肠的黏附力大于与胃的黏附力.结论格列齐特生物黏附缓释片的处方、工艺基本能够满足设计要求.     

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。     

野菊花总黄酮口腔生物黏附双层贴片成型工艺优化

目的:研究野菊花总黄酮口腔生物黏附双层片的成型工艺。方法:采用Franz扩散法优选可阻止有效成分渗透的保护层;以黏附力和释放度为指标,采用单因素试验筛选生物黏附材料,以正交试验优选载药量、黏附材料的比例及填充剂用量。结果:该贴片的黏附层为卡波普934P和羟丙基纤维素1:2混合物,占75.8%,总黄酮20%,乳糖4%,微粉硅胶0.2%,以乙基纤维素作为黏附片的保护层。结论:该成型处方制成的野菊花生物黏附双层片具有较好的生物黏附性,背衬层可阻滞药物释放。     

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。     

盐酸黄连素生物黏附包衣片的制备及性质研究

目的:制备盐酸黄连素生物黏附包衣片并研究其性质。方法:采用正交设计法,确定生物黏附材料羟丙基甲基纤维素、卡波姆934P的用量及配比与制剂体外释放度及黏附力的关系,并对释放度进行释药动力学模拟,根据各模型拟合的残差平方和(Re)、赤池信息准则计算值(AIC)和拟合度(r)值来研究其释药规律。根据Peppas方程特征参数判断其释药机制。结果:羟丙基甲基纤维素与卡波姆对阻滞药物的释放及黏附力影响较大,且卡波姆的效果强于羟丙基甲基纤维素。生物黏附包衣片以Hixson-Crowell方程拟合最佳,药物释放机制为非Fick扩散。结论:盐酸黄连素生物黏附包衣片具有良好的黏附性能和pH依赖性。     

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。     

锡类散贴片制备工艺及稳定性、黏附性和释放性能的研究

目的:制备锡类散贴片并研究其配方比例、稳定性、黏附性及释放度。方法:通过测定锡类散贴片的稳定性、黏附性和释放性能.确定其配比和工艺。结果:最佳配比为羧甲基纤维素钠(CMC-Na):低取代羟丙基纤维素(L-HPC):锡类散=1:1.1:0.94,此时贴片具有较好的药物黏附性能且性质稳定,并具有缓释作用。结论:按该配比制备的贴片既有良好的黏附作用又可定位释放,延长了药物与病灶部位的作用时间,提高了疗效。     

氟尿嘧啶-羟丙基-β-环糊精包合物温敏凝胶生物黏附力及溶出度研究

目的：考察不同生物黏附材料对氟尿嘧啶-羟丙基-β-环糊精包合物温敏凝胶剂粘附性及溶出度的影响。方法：以羟丙基甲基纤维素（HPMC）、海藻酸钠、透明质酸钠、卡波姆、聚卡波菲为生物黏附材料制备氟尿嘧啶-羟丙基-β-环糊精包合物温敏凝胶剂,测定各处方的黏附力,并在溶出介质p H 7.2磷酸盐缓冲液中,用透析袋法进行体外释药试验。结果：以0.2%聚卡波菲为生物黏附材料的处方黏附力为32.3 g·ml^-1,药物释放时间延长至8 h,采用不同的生物黏附材料对制剂溶出行为没有显著影响。结论：以0.2%聚卡波菲为生物黏附材料,制备氟尿嘧啶-羟丙基-β-环糊精包合物温敏凝胶剂黏附力高,且具有良好的缓释效果。     

尼索地平口腔黏附片的制备及影响因素考察

目的：考察尼索地平口腔黏附片处方工艺对体外释放度和生物黏附力的影响。方法：测定各处方工艺条件下黏附片的释放度及黏附力。结果：保护层用量〉41．66％时，可保证药物的单向释放；含药层中卡波姆比例增加、乳糖比例减少及硬度的增大会使释药速度减慢；黏附力随卡波姆比例增加而增大，随乳糖增加而减少，硬度为5kg时黏附力较大。结论：处方中卡波姆比例、乳糖用量、黏附片硬度对体外释药速度和黏附力有显著影响。     

影响葛根总黄酮生物粘附片体外释放度的因素研究

目的 :探讨影响葛根总黄酮生物粘附片释放度的主要因素。方法 :以羟丙基甲基纤维素 (HPMC)与卡波姆 (CP)为生物粘附材料和骨架材料、乳糖为致孔剂制备葛根总黄酮生物粘附片 ;采用转篮法测定释放度 ,以0 1mol/LHCl为溶出介质 ,转速为100r/min ,测定累积释放度 ,同时考察HPMC用量、CP用量、致孔剂种类、乳糖用量、压片颗粒大小、介质 pH等因素对释放度的影响。结果与结论 :HPMC用量、CP用量、致孔剂种类、乳糖用量、压片时颗粒大小、介质 pH等因素对生物粘附片溶出均有明显影响     

Dissolution properties and bioavailability of ground mixture of N,N-dimethylcarbamoylmethyl alpha, 2-dimethyl-5H-[1]benzopyrano[2,3-b]-pyridine-7-acetate with various pharmaceutical ingredients

Ground mixture of N,N-dimethylcarbamoylmethyl alpha, 2-dimethyl-5H-[1]benzopyrano-[2,3-b]pyridine-7-acetate (1) with various pharmaceutical ingredients were prepared in order to investigate their dissolution behaviors and bioavailability. Taking into account the weakly basic property of 1, the dissolution rate was determined in the 2nd fluid (pH 6.8) of disintegration test, JP XI. Dissolution rates of the ground mixtures (1 : 1, w/w) of 1 with hydroxypropylcellulose-L (HPC-L), low substituted hydroxypropylcellulose (L-HPC) or lactose respectively, showed a significant increase compared with compound 1 alone. Three kinds of experimental fine granules were prepared; type A: produced from ground mixture of 1, HPC-L, L-HPC and lactose; type B: produced from physical mixture having the same composition as type A; type C: produced 1, L-HPC and lactose. In these fine granules, only type A exhibited pH-independent dissolution profiles. Bioavailability study was carried out in beagle dogs whose gastric acidity was controlled in advance to low levels by administration of omeprazole. The test was conducted in a cross over design. Reflecting their dissolution characteristics, type A granules showed better bioavailability than the others. These results suggest that grinding is useful for the improvement of the dissolution property and bioavailability of 1, a weakly basic compound.     

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。     

头孢氨苄生物黏附缓释片的制备及体外评价

目的：制备头孢氨苄生物黏附缓释片,并对其体外黏附性能及释药特性进行评价。方法：以单因素考察法确定制备头孢氨苄生物黏附缓释片的最优处方,以自制黏附力测定装置测定优化处方所制缓释片的黏附力,以转篮法（转速100r·min^-1）测定其在1、2、4、8小时时的释放度,并对其释药过程进行动力学方程拟合以判断释药机制。结果：最优处方采用羟丙甲纤维素（HPMC K15M,6mg）为骨架材料,卡波姆（CP971P,20mg）为黏附材料,乳糖（18mg）为填充剂,头孢氨苄和硬脂酸镁分别为52.6mg和0.5mg。按优化处方所制的缓释片的黏附力为54.7g;在0.1mol·L^-1的盐酸溶液中1、2、4、8小时的释放度分别为30%、50%、70%和90%以上;体外释药符合Higuchi方程,释放机制为扩散和骨架溶蚀的协同作用。结论：该头孢氨苄生物黏附缓释片的处方工艺基本满足设计要求。     

The distribution of components in the different size fractions of granules prepared from binary mixtures

Boric acid, sulphanilamide and citric acid have been mixed separately with lactose and then granulated by massing and screening. The granules have been fractionated by sieving and each fraction has been analysed for lactose content. The effect of premixing time, massing time, binder volume and ratio of components on the distribution of lactose between size fractions of granules prepared from lactose: boric acid mixtures has been investigated. Uneven distribution of lactose has been found for all blends examined. There is a premixing time and massing time that gives the optimum distribution of lactose for any given blend and binder volume. Increased binder volume in some cases improves granule uniformity. The proportion of lactose in the blend has a major effect on the distribution of this component in the granules, as does the particle size of the lactose. Granules prepared from blends of lactose with sulphanilamide and with citric acid were also examined for lactose distribution.     

The distribution of components in the different size fractions of granules prepared from binary mixtures.

Boric acid, sulphanilamide and citric acid have been mixed separately with lactose and then granulated by massing and screening. The granules have been fractionated by sieving and each fraction has been analysed for lactose content. The effect of premixing time, massing time, binder volume and ratio of components on the distribution of lactose between size fractions of granules prepared from lactose: boric acid mixtures has been investigated. Uneven distribution of lactose has been found for all blends examined. There is a premixing time and massing time that gives the optimum distribution of lactose for any given blend and binder volume. Increased binder volume in some cases improves granule uniformity. The proportion of lactose in the blend has a major effect on the distribution of this component in the granules, as does the particle size of the lactose. Granules prepared from blends of lactose with sulphanilamide and with citric acid were also examined for lactose distribution.