右旋布洛芬缓释胶囊的初步稳定性试验

目的:考察右旋布洛芬缓释胶囊的初步稳定性考察。方法:通过光照试验、加速试验和长期试验,对右旋布洛芬缓释胶囊的外观性状、色泽、溶出度、含量和有关物质等指标进行考察,并预测其有效期。结果:在各受试条件下各样品外观无显著变化,含量和溶出度无明显差异,有关物质量稍有增加。结论:本品较稳定,各时间检测样品与0时比较无明显差异,可以对制定右旋布洛芬缓释胶囊的有效期提供参考。     

黄芩苷缓释胶囊的研制

制备黄芩苷缓释胶囊,并通过体外释放度对其处方进行优化.以黄芩苷为原料药,羟丙甲纤维素(HPMC)、微晶纤维素(MCC)、乳糖、聚维酮(PVP)的乙醇溶液为辅料制备缓释胶囊,考察不同因素对释放度的影响,通过正交试验优化制备处方.优化后的黄芩苷缓释胶囊的处方为黄芩苷0.5 g,HPMC 0.25 g,MCC 0.2 g,PVP的乙醇溶液浓度为6%,乳糖0.25 g.研究方法简便、快速,体外释放度显示黄芩苷缓释胶囊处方设计比较合理,可进一步研发.     

复方奥硝唑茶多酚口腔温敏型凝胶的制备及其体外释放度测定

目的：制备复方奥硝唑茶多酚口腔温敏型凝胶并对其体外释药进行考察。方法：以奥硝唑和茶多酚为主药,以泊洛沙姆P407、泊洛沙姆P188及聚乙二醇400的用量为考察因素,胶凝温度为考察指标进行正交试验筛选处方,以磷酸盐缓冲液为释放介质,按桨法测定主药的体外释放度。结果：最佳处方为泊洛沙姆P407为16％,泊洛沙姆P188为2％,聚乙二醇400为12％,胶凝温度为36．4℃,药物的释放时间可达4 d以上。结论：该处方设计合理,制备工艺简单,质量可靠,所得复方奥硝唑茶多酚口腔温敏型凝胶缓释性能良好。     

西地碘口腔黏附片的研制

研制一种局部使用的用于治疗口腔溃疡的缓释西地碘口腔黏附片,并考察其对体外释放度和生物黏附性的影响.采用羧甲基纤维素钠(CMC-Na)和卡波姆(CP)为生物黏附材料,用直接粉末压片法制备的包括保护层和含药层的双层口腔黏附片.通过对不同处方黏附片的生物黏附力,体外黏附时间和溶胀速率进行测定,确定黏附剂的组成及用量,得到最佳的处方.含药层中黏附剂比例增加、乳糖比例减少及硬度的增大都会使释药速度减慢,硬度为4 kg左右时黏附力和释药比较好.处方中卡波姆比例用量、乳糖用量、黏附片硬度均对体外释药速度和黏附力有影响.     

苦参素脂质体的体外释放度研究

目的：研究苦参素脂质体的体外释放特性。方法：以乙醇注入法制备苦参素脂质体,以透析法分离游离的苦参素和苦参素脂质体,按照中国药典（2010版）溶出度第三法考察释放度,对脂质体释放规律进行研究。结果：以磷酸盐缓冲溶液（PBS）7.4作为释放介质的透析法适用于体外释放度的测定。所制备的苦参素脂质体体外释放行为符合Higuchi方程。结论：苦参素脂质体在体外具有良好的缓释作用。     

阿司匹林脉冲控释片的研制

以阿司匹林为模型药物制备脉冲片,并考察各处方因素对脉冲片释放度的影响.以主药和崩解剂为片芯,乙基纤维素(EC)为包衣材料,聚乙二醇6000(PEG6000)为致孔剂,羟丙甲基纤维素(HPMC)为增塑剂,采用压制包衣法制备含阿司匹林50 mg的脉冲控释片.各辅料的比例及包衣层厚度对阿司匹林片的脉冲释放均有影响.通过对处方的优化,得最终处方为主药50 mg、崩解剂30 mg,EC 180 mg,PEG6000 60 mg,HPMC 30 mg的阿司匹林脉冲控释片.通过选择片芯中的崩解剂、调整包衣层组成和厚度,可以用压制包衣的方法得到不同时间脉冲释药的阿司匹林片剂.     

依托度酸双层渗透泵控释片的制备

目的:制备依托度酸双层渗透泵控释片.方法:采用单因素法考察依托度酸渗透泵控释片体外释药行为的影响.结果:最佳片剂处方组成为:包衣膜增重为15%,聚氧乙烯(PEO)65%,CMS-Na 56 mg,HPMCK100M 45 mg,CP971NF 11.6 mg,PVPK30 22 mg,NaCl 32.5 mg.控释片批间重复性良好.结论:自制依托度酸双层渗透泵控释片工艺稳定,零级释药特征明显,24 h内释药完全.     

pH值敏感水凝胶的合成及药物缓释性能研究

聚乙二醇(PEG)与丙烯酰氯反应合成聚乙二醇双丙烯酸酯(PEGDA)，然后以PEGDA、N—乙烯基—2—此咯烷酮(NVP)及丙烯酸为主要原料，N，N^ —亚甲基双丙烯酰胺(BIS)为交联剂，偶氮二异丁腈(AIBN)为引发剂，采用自由基聚合法合成了对pH值变化敏感的N—乙烯基—2—吡咯烷酮—丙烯酸—聚乙二醇双丙烯酸酯交联共聚物(po1y[NVP-AA-PEGDA])水凝胶．利用该共聚物为载体对抗癌药5—氟脲密啶(5—FU)进行包埋，并在SIF及SGF缓冲溶液中于37℃进行体外释药研究．结果表明，在pH值较小的缓释介质中药物释放曲线较平缓，释药周期较长，同时最终的平衡释药百分数也较小；随着样品中PEGDA量的减少，释药曲线趋于平缓，释药周期变长，最终的平衡释药百分数成小．     

钩藤总碱凝胶骨架片的研制及释放度考察

以羟丙甲基纤维素(HPMC)为骨架材料，采用湿法制粒，制备钩藤总碱缓释片。以体外释放度实验研究了缓释片的释药机理及其影响因素。结果表明：钩藤总碱凝胶骨架片的释放符合Higuchi方程，其释放速度受多种因素的影响，如HPMC、乳糖、微晶纤维素的用量，附加剂的调节和控制。     

二氧化钛改性纳米材料对三磷酸腺苷的吸附与缓释特性

以固相反应法所合成的硼、硫掺杂二氧化钛纳米材料为载体,探讨三磷酸腺苷在载体表面上的吸附与缓释行为.结果表明,在相同的条件下,以二氧化钛为基体的纳米粉体材料对ATP有良好的吸附作用.40 min内,S-B-TiO2、B-TiO2、S-TiO2及TiO2纳米粉体对ATP的吸附率分别为94.7％、83.4％、71.3％和66.0％.其中S-B-TiO2纳米粉体的载药量比纯TiO2提高了28.7％;TiO2及其改性纳米材料对ATP的释放起到一定的调控作用,5h内其释药百分比分别为43.5％、47.9％、25.1％和37.0％.其中S-TiO2对ATP的缓释速率比纯TiO2明显减缓.ATP的缓释过程符合非Fick扩散机理和Korsmeyer-Peppas模型.     

膜过滤实验装置及过滤特性初步研究

自行研制了油田含油污水膜过滤实验装置,并对该实验装置的可靠性进行了验证。以去离子水作为料液,初步研究了各种因素对改性聚四氟乙烯膜组件过滤性能的影响。     

卵磷脂修饰改性聚乳酸微球的制备及表征

采用氨解结合乳化及热致相分离的技术来制备改性聚乳酸微球,通过浸泡法让卵磷脂包裹在改性微球上,进一步提高改性微球的亲水性。探讨了卵磷脂溶液的浓度、浸泡时间对改性微球形貌和亲水性能的影响。实验结果表明,卵磷脂修饰改性微球的最佳制备工艺条件为:卵磷脂溶液的浓度为1%,浸泡时间为5h,在此条件下制备的微球卵磷脂包裹均匀且亲水性得到了改善。通过红外光谱,X射线光电子能谱表征微球,结果表明卵磷脂已经成功接枝到改性微球上,通过水接触角测试,卵磷脂修饰后的改性微球亲水性得到了进一步提高。     

Effect of small bowel preparation with simethicone on capsule endoscopy

Background: Capsule endoscopy is a novel non-invasive method for visualization of the entire small bowel. The diagnostic yield of capsule endoscopy depends on the quality of visualization of the small bowel mucosa and its complete passage through the small bowel. To date, there is no standardized protocol for bowel preparation before capsule endoscopy. The addition ofsimethicone in the bowel preparation for the purpose of reducing air bubbles in the intestinal lumen had only been studied by a few investigators. Methods: Sixty-four participants were randomly divided into two groups to receive a bowel preparation of polyethylene glycol (PEG) solution (Group 1) and both PEG solution and simethicone (Group 2). The PEG solution and sime-thicone were taken the night before and 20 min prior to capsule endoscopy, respectively. Frames taken in the small intestine were examined and scored for luminal bubbles by two professional capsule endoscopists. Gastric emptying time and small bowel transit time were also recorded. Results: Simethicone significantly reduced luminal bubbles both in the proximal and distal small intes-tines. The mean time proportions with slight bubbles in the proximal and distal intestines in Group 2 were 97.1% and 99.0%, respectively, compared with 67.2% (P<0.001) and 68.8% (P<0.001) in Group 1. Simethicone had no effect on mean gastric emptying time, 32.08 min in Group 2 compared with 30.88 min in Group 1 (P=0.868), but it did increase mean small intestinal transit time from 227.28 to 281.84 min (P=0.003). Conclusion: Bowel preparation with both PEG and simethicone significantly reduced bubbles in the intestinal lumen and improved the visualization of the small bowel by capsule endoscopy without any side effects observed.     

A simple and inexpensive enteric-coated capsule for delivery of acid-labile macromolecules to the small intestine

Understanding the ecology of the gastrointestinal tract and the impact of the contents on the host mucosa is emerging as an important area for defining both wellness and susceptibility to disease. Targeted delivery of drugs to treat specific small intestinal disorders such as small bowel bacterial overgrowth and targeting molecules to interrogate or to deliver vaccines to the remote regions of the small intestine has proven difficult. There is an unmet need for methodologies to release probes/drugs to remote regions of the gastrointestinal tract in furthering our understanding of gut health and pathogenesis. In order to address this concern, we need to know how the regional delivery of a surrogate labeled test compound is handled and in turn, if delivered locally as a liquid or powder, the dynamics of its subsequent handling and metabolism. In the studies we report on in this paper, we chose ¹³C sodium acetate (¹³C-acetate), which is a stable isotope probe that once absorbed in the small intestine can be readily measured non-invasively by collection and analysis of ¹³CO₂ in the breath. This would provide information of gastric emptying rates and an indication of the site of release and absorptive capacity. In a series of in vitro and in vivo pig experiments, we assessed the enteric-protective properties of a commercially available polymer EUDRAGIT®L100-55 on gelatin capsules and also on DRcaps®. Test results demonstrated that DRcaps®coated with EUDRAGIT®L100-55 possessed enhanced enteric-protective properties, particularly in vivo. These studies add to the body of knowledge regarding gastric emptying in pigs and also begin the process of gathering specifications for the design of a simple and cost-effective enteric-coated capsule for delivery of acid-labile macromolecules to the small intestine.     

Fe(bpy)_3~(2 )在Pan/Ben修饰电极上的循环伏安行为研究

研究了Pan/Ben(聚苯胺 /膨润土 )修饰电极对Fe(bpy) 2 3 (铁联吡啶 )电活性的影响 ,发现修饰电极中Pan含量越大 ,Fe(bpy) 2 3 的电响应相应地增大 .扭厚度与其峰电流值无关     

乌索酸滴丸的制备工艺研究

目的:经过筛选处方和优化工艺,将乌索酸制成滴丸剂,同时考察其体外溶出度,评价其质量.方法:采用滴制法制备乌索酸滴丸.以滴丸的圆整度、重量差异及硬度等作为综合评定指标,优选出滴丸的最佳处方和成型工艺,采用RP-HPLC法测定含量.结果:筛选出了最佳的处方和成型工艺,合理可行,制备的乌索酸滴丸质量稳定,质控方法准确可靠.结论:制备的乌索酸滴丸外观性状好,丸重差异小,含量准确,溶出度得到了显著提高,75m in内乌索酸滴丸的体外溶出度比片剂提高232.8%,比乌索酸胶囊提高12.5%.     

Inhibition of mitochondria responsible for the anti-apoptotic effects of melatonin during ischemia-reperfusion

Objective： To investigate a possible mechanism responsible for anti-apoptotic effects of melatonin and provide theoretical evidences for clinical therapy. Methods： lschemia-reperfusion mediated neuronal cell injury model was constructed in cerebellar granule neurons （CGNs） by deprivation of glucose, serum and oxygen in media. After ischemia, melatonin was added to the test groups to reach differential concentration during reperfusion. DNA fragmentation, mitochondrial transmembrane potential, mitochondrial cytochrome c release and caspase-3 activity were observed after subjecting cerebellar granule neurons to oxygen-glucose deprivation （OGD）. Results： The results showed that OGD induced typical cell apoptosis change, DNA ladder and apoptosis-related alterations in mitochondrial functions including depression of mitochondrial transmembrane potential （its maximal protection ratio was 73.26%） and release of cytochrome c （its maximal inhibition ratio was 42.52%） and the subsequent activation of caspase-3 （its maximal protection ratio was 59.32%） in cytoplasm. Melatonin reduced DNA damage and inhibited release of mitochondrial cytochrome c and activation of caspase-3. Melatonin can strongly prevent the OGD-induced loss of the mitochondria membrane potential. Conclusion： Our findings suggested that the direct inhibition of mitochondrial pathway might essentially contribute to its anti-apoptotic effects in neuronal ischemia-reperfiusion.     

Review: Adjuvant effects of saponins on animal immune responses

Vaccines require optimal adjuvants including immunopotentiator and delivery systems to offer long term protection from infectious diseases in animals and man. Initially it was believed that adjuvants are responsible for promoting strong and sustainable antibody responses. Now it has been shown that adjuvants influence the isotype and avidity of antibody and also affect the properties of cell-mediated immunity. Mostly oil emulsions, lipopolysaccharides, polymers, saponins, liposomes, cytokines,ISCOMs (immunostimulating complexes), Freund's complete adjuvant, Freund's incomplete adjuvant, alums, bacterial toxins etc.,are common adjuvants under investigation. Saponin based adjuvants have the ability to stimulate the cell mediated immune system as well as to enhance antibody production and have the advantage that only a low dose is needed for adjuvant activity. In the present study the importance of adjuvants, their role and the effect of saponin in immune system is reviewed.     

Adjuvant effects of saponins on animal immune responses

Vaccines require optimal adjuvants including immunopotentiator and delivery systems to offer long term protection from infectious diseases in animals and man. Initially it was believed that adjuvants are responsible for promoting strong and sustainable antibody responses. Now it has been shown that adjuvants influence the isotype and avidity of antibody and also affect the properties of cell-mediated immunity. Mostly oil emulsions, lipopolysaccharides, polymers, saponins, liposomes, cytokines, ISCOMs (immunostimulating complexes), Freund’s complete adjuvant, Freund’s incomplete adjuvant, alums, bacterial toxins etc., are common adjuvants under investigation. Saponin based adjuvants have the ability to stimulate the cell mediated immune system as well as to enhance antibody production and have the advantage that only a low dose is needed for adjuvant activity. In the present study the importance of adjuvants, their role and the effect of saponin in immune system is reviewed.     

多索茶碱冻干粉针的制备及质量控制

目的:制备多索茶碱冻干粉针并对其进行质量检查.方法:制备工艺采用脱炭、过滤、细菌内毒素检查和冷冻干燥,并对其有关物质和含量等项目进行了检测.结果:最佳处方为每100支用多索荼碱10.5 g,甘露醇30.0 g;本品在5%葡萄糖注射液和0.9%NaCl注射液中室温放王4 h稳定性良好;有关物质及多索荼碱含量符合规定.结论:本研究表明多索茶碱冻干粉针的制备工艺稳定,质量可控.