重组幽门螺杆菌尿素酶B亚单位疫苗鼻腔免疫的实验研究

目的:探讨基因工程疫苗Hp重组尿素酶B亚单位(rUreB)鼻腔接种的免疫效果。方法:以rUreB不同剂量或加不同佐剂滴鼻免疫BALB/c小鼠。末次免疫7 d后,收集血清及胃黏膜、小肠黏膜、鼻黏膜及气管黏膜冲洗液,用ELISA法检测抗rUreB特异性抗体。结果:rUreB鼻腔免疫后各实验组血清特异性IgG及各黏膜冲洗液中特异性IgA的水平均明显增高,与对照组相比较差异显著(P<0.01)。20μg剂量组与10μg剂量组相比较,仅血清特异性IgG水平增高,其它黏膜特异性IgA的水平未见增高。大肠杆菌不耐热肠毒素B亚单位(LTB)的佐剂效果较霍乱毒素B亚单位(CTB)强,卡泊波可增强鼻腔接种疫苗在胃黏膜洗液中的抗体应答水平。结论:CTB、LTB、卡泊波均可作为rUreB鼻腔黏膜接种的佐剂。HprUreB鼻黏膜接种,不仅可诱导血清特异性抗体反应,而且能引起多个黏膜部位的免疫应答,是一种方便、有效、廉价的免疫途径。     

QbD-based carbopol transgel formulation: characterization,pharmacokinetic assessment and therapeutic efficacy in diabetes

In order to develop transdermal drug delivery system that facilitates the skin permeation of Pioglitazone (PZ) encapsulated in carbopol-based transgel system (proniosomes/niosome). The developed formulations were optimized using quality by design (QbD) approach and particle size, percentage entrapment and transdermal flux were determined. It was found to be more efficient delivery carriers with high encapsulation and enhanced flux value demonstrated that the permeation of PZ through skin was significantly increased with developed formulation. The transdermal enhancement from proniosome was 3.16 times higher than that of PZ from control formulation (ethanol buffer formulation, 3:7), which was further confirmed by confocal laser scanning microscopy. In vivo pharmacokinetic study of carbopol transgel showed a significant increase in bioavailability (2.26 times) compared with tablet formulation. It also showed better antidiabetic activity in comparison to marketed tablet, so our results suggest that carbopol-based transgel are an efficient carrier for delivery of pioglitazone through skin.     

Enhanced transdermal delivery of luteolin via non-ionic surfactant-based vesicle: quality evaluation and anti-arthritic assessment

Luteolin (LUT) is a promising molecule with potential anti-arthritic activity. This investigation presents formulation and evaluation of niosomal transgel for enhanced transdermal delivery of LUT. Different non-ionic surfactants and vesicle compositions were employed for preparation of niosomes. The vesicle size analysis showed that all vesicles were in the range from 534.58 to 810.22?nm which favoured efficient transdermal delivery. The entrapment of LUT in vesicle was found to be higher in all surfactant. The developed formulation was proved significantly superior in terms of amount of drug permeation with an enhancement ratio of 2.66 when compared to a control formulation. The in vivo bioactivity studies revealed that the prepared niotransgel formulation of LUT was able to provide good anti-arthritic activity and the results were comparable to standard (diclofenac gel for anti-arthritic and analgesic). Finally, the results were confirmed through radiological analysis which proved that the prepared niotransgel was effectively able to treat arthritis and results were comparable with the standard formulation.     

盐酸利多卡因凝胶-口服液的研制及质量控制

目的筛选盐酸利多卡因凝胶-口服液处方,制备适合电子胃镜检查的辅助制剂。方法以卡波姆-940为基质、二甲基硅油为消泡剂制备盐酸利多卡因凝胶-口服液,详细考察其性状均匀性、消泡能力、含量、pH,确定最优处方,并通过高温、低温及离心试验考察样品的初步稳定性。结果2%盐酸利多卡因凝胶-口服液主要成分的最优处方为卡波姆-9400.3%,甘油15%,三乙醇胺0.8%,二甲基硅油2%。除高温下会使样品主药含量略有下降外,其他性质均稳定。结论2%盐酸利多卡因凝胶-口服液的制备工艺简便,质地细腻均匀,室温下稳定性好,消泡能力强,符合临床应用要求。     

Effect of Different Polymer Concentration on Drug Release Rate and Physicochemical Properties of Mucoadhesive Gastroretentive Tablets

Mucoadhesive tablets have emerged as potential candidates for gastroretentive drug delivery providing controlled release along with prolonged gastric residence time. Gastroretentive mucoadhesive tablets could result in increased bioavailability due to prolonged gastric residence time. A hydrophilic matrix system was developed as mucoadhesion is achievable on appropriate wetting and swelling of the polymers used. The polymers were so chosen so as to provide a balance between swelling, mucoadhesion and drug release. The polymers chosen were hydroxypropyl methylcellulose K4M, chitosan, and Carbopol 934. The concentrations of these polymers used has a great impact on the physicochemical properties of the resulting formulation. The tablets were formulated using wet granulation method and tranexamic acid was used as the model drug. The prepared tablets were characterized for size, shape, appearance, hardness, friability, weight variation, swelling, mucoadhesion and in vitro drug release. Several batches of tablets were prepared by varying the ratio of hydroxypropyl methylcellulose K4M and Chitosan. The batches having a greater ratio of chitosan showed higher rate of swelling, greater erosion, less mucoadhesion and faster release rate of the drug whereas the batches having greater ratio of hydroxypropyl methylcellulose K4M showed lesser rate of swelling, less erosion, better mucoadhesion and a smaller drug release rate. The level of carbopol was kept constant in all the batches.     

口腔缓释粘附膜剂与粘附片剂的比较

目的　对口腔缓释粘附片剂与粘附膜剂进行比较。方法　分别对制成的粘附膜剂与粘附片剂进行有关质量的检测及临床观察对比。结果　粘附片剂的粘附力、溶出度、口腔内粘附试验及临床疗效均比粘附膜剂优越。粘附片剂吸水膨胀后可粘附于口腔溃疡的创面上 ,既可起到治疗作用 ,又可保护创面 ,维持较长的药效。结论　口腔粘附缓释片剂的性能优越 ,疗效显著 ,但制备复杂 ,而膜剂简单     

复方苯甲酸凝胶的研制

目的研制外用抗真菌药复方苯甲酸凝胶,并对制剂稳定性进行观察。方法以卡波姆-940为基质,用常规方法制备凝胶。结果制剂稳定性较好,对黏膜无刺激作用。结论该制剂的制备工艺简单、检测方便、制剂稳定、安全。     

黄芩滴眼剂的制备与临床应用

目的研究黄芩滴眼剂的制备方法。方法以0．05％卡波姆为基质制备滴眼剂，建立质量控制标准，并观察对结膜炎、角膜炎等50例患者的治疗效果。结果该制剂制备工艺、质量控制方法可行，质量稳定，疗效确切。结论黄芩滴眼剂治疗结膜炎、角膜炎等眼部疾患有较好效果，可应用于临床。