雷公藤胃漂浮缓释片的制备和质量评价

目的研制雷公藤胃漂浮缓释片,考察其漂浮和释药性能。方法采用粉末直接压片法制备雷公藤胃漂浮缓释片,以漂浮性能、雷公藤总二萜内酯的释放度为考察指标,进行处方筛选,并采用正交设计实验对处方进行优化。结果以羟丙基甲基纤维素(HPMCK4M)为骨架材料,十六醇为助漂剂,碳酸氢钠为产气剂,聚维酮为致孔剂,制备了一天给药两次的胃内漂浮型缓释片。该制剂在人工胃液中立即起漂,2h释放约30%,6h释放约60%,12h释放90%以上,满足12h释放要求,体外释药规律符合Higuchi方程,说明本缓释片属于药物扩散和骨架溶蚀混合控释机制。结论研制的雷公藤胃漂浮缓释片具有良好的漂浮性能和释药特性

基于多组分评价的雷公藤提取物固体分散体的制备及体外表征

目的制备雷公藤提取物(ETW)固体分散体(ETW-SD),提高其体外溶出度。方法通过溶剂-熔融法,以聚乙二醇6000(PEG 6000)、泊洛沙姆188(F68)为载体制备ETW-SD。以雷公藤甲素、雷公藤内酯酮、雷公藤次碱、雷公藤红素以及雷公藤内酯甲为评价指标,通过体外溶出度、电子扫描电镜(SEM)、差示热量扫描(DSC)和X-射线衍射(XRD)对ETW-SD进行表征。结果 ETW-SD的最优处方为ETW-PEG 6000-F68(1∶2∶1)。与原料药相比,在60 min内雷公藤内酯酮、雷公藤甲素的溶出度分别提高了3.32倍,雷公藤次碱提高了2倍,而雷公藤红素和雷公藤内酯甲的溶出度均达到83%以上。福州总医院院立课题(2016L02);;福建省科技计划重大项目(2012I1001

Advance in research of water-proof liquid band-aid

创可贴是人们生活中最常用的外科用药。传统的创可贴即是一长形胶布,中间附以浸过药物的纱布,从而起保护伤口,暂时止血的作用。传统创可贴适合创伤较为表浅,伤口整齐干净、出血不多而又不需要缝合的小伤口使用。本文所要讲述的液体创可贴可用于大部分的外伤伤口,能够及时止血及防止病原微生物的感染。本文主要讲述了近些年刚刚出现的防水型液体创可贴,包括其主要的作用,材料组成及相关临床研究。Band-aid is the most commonly used surgical medication. The traditional band-aid is a longshaped adhesive,and the intermediate layer accompanied by soaking medicine gauze,thereby used for the wound and temporary hemostasis. The traditional band-aid is suitable for shallow trauma,small wound,clean and tidy wound,less bleeding and the wound that needs no suture. In this article we introduced a liquid band-aid that can be used for most of the traumatic wound,can timely stop bleeding and prevent microbial infection. We mainly described the waterproof liquid band-aid appeared in recent years,including its main effects,material composition and related clinical research

痤疮发病机制及其药物治疗的研究进展

目的：了解痤疮的发病机制及其药物治疗的研究进展,为其临床治疗提供参考。方法：查阅近年来国内外相关文献,就痤疮的发病机制及其药物治疗的研究进展进行归纳和总结。结果：痤疮的发病机制主要为雄激素分泌异常、痤疮丙酸杆菌的大量繁殖、炎症损害和免疫失常及毛囊皮脂腺导管角化异常等。痤疮的局部治疗药物中维A酸类药物与抗菌药物可联用于治疗轻、中度痤疮,其中全反式维A酸、阿达帕林与他扎罗汀是治疗轻度痤疮的首选药物,全反式维A酸常联合外用抗菌药物治疗中度痤疮,阿达帕林和克林霉素分别与过氧化苯甲酰联用、果酸参与的联合给药方案也用于治疗痤疮。口服治疗药物中维A酸类药物主要用于重度痤疮,第一代的异维A酸较第二代疗效更好,但均有致畸作用;口服抗菌药物适用于中、重度痤疮患者,多西环素与米诺环素是首选药物,米诺环素联用过氧化苯甲酰疗效好;大环内酯类抗菌药物口服后不良反应较多,故常作为外用药;口服激素类药物中的抗雄激素类药物用于女性患者,但长期使用会引发高胰岛素血症;螺内酯有潜在的安全问题,西咪替丁抗雄激素效果较弱,不作为治疗痤疮的常用药物;糖皮质激素类药物常用于暴发性痤疮或聚合性痤疮的治疗,使用剂量须严格控制。结论：痤疮的治疗应根据痤疮的发生原因和严重程度选择合理的用药方案,增加疗效并减少不良反应的发生,并注意药物相互作用,提高用药安全性。军队医疗机构制剂标准提高科研专项课题（No.14ZJZ17

Development and stability test of compound ketoconazole ointment

目的 制备复方酮康唑软膏并考察其稳定性。方法 以酮康唑、莫匹罗星和糠酸莫米松为主药，以聚乙二醇（PEG）为基质制备软膏；利用影响因素试验考察软膏中药物的稳定性。结果 PEG400和PEG3350的比例为2：1时，软膏的黏度最佳，易于涂展。制成软膏后，高温下糠酸莫米松和莫匹罗星稳定性良好；酮康唑有少许分解，加入0.5%的抗坏血酸棕榈酸酯（L-A）后，酮康唑的含量明显提高。加速试验发现，放置6个月后软膏的颜色无变化，3种药物的含量均在98%以上。结论 本实验成功制备了新型复方酮康唑软膏，药物稳定性良好。Objective To prepare compound ketoconazole ointment and perform the stability study.Methods Ketoconazole, mupirocin and mometasone furoate were used as active pharmaceutical ingredients （API）. PEG mixture was used as matrix to prepare the ointment.Stability of the API in the ointment was evaluated by the stress tests.Results The optimal ratio of PEG400 to PEG3350 for the ointment matrix was 2：1. Mometasone furoate and mupirocin in the ointment were stable to the high temperature（40℃）while ketoconazole had some degradation. The stability of the API was improved by addition of 0.5% of L-A. During the accelerate test, the ointment had no color change and the API percentages were above 98%. Conclusion The novel compound ketoconazole ointment was successfully prepared and the formulation stability was excellent.福建省自然科学基金项目（2010J01218

Mechanism of nanostructured lipid carriers in promotion of absorption of poorly soluble drugs

纳米结构脂质载体(nlC)是药剂学备受关注的研究领域,作为一种性能优良的新型药物传递系统,能促进难溶性药物的口服吸收。探讨并总结纳米结构脂质载体促进难溶性药物口服吸收的机制。Objective Nano-structured lipid carriers(NLC) is a concerned research area in pharmaceutics,which as a novel drug delivery system to promote oral absorption of poorly soluble drugs.The literatures were reviewed to explore and summarize the mechanism that nano-structured lipid carriers in promotion of the absorption of poorly soluble drugs

放疗与化疗所致口腔黏膜损伤防治药物研究进展

综述近年来防治放化疗所致口腔黏膜损伤的药物,拟为开发新制剂提供参考。通过检索国内外相关文献,从作用机制角度对防治药物进行归纳和总结。发现已有较多化学药物与传统中药复方应用于防治口腔黏膜损伤。因此,开发有效的防治放化疗所致口腔黏膜损伤制剂的相关研究需要进一步地深入

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中药是我国传统医学的重要组成部分,但部分中药存在成分复杂、水溶性差等问题,给临床前研究,尤其是体外药效学研究带来困扰。本文就目前体外药效学研究中难溶性中药或中药成分增溶方法或技术进行综述,探讨其可行性及对中药药效行为的影响。福建省自然科学基金项目（2015J01491

水飞蓟素固体分散体的制备及5种成分的溶出度

目的制备水飞蓟素固体分散体,并评价5种成分的溶出度。方法以F68与PVPk30为联合载体,溶剂熔融法制备固体分散体。再考察联合载体比例、药物-载体比例对水飞蓟宾、异水飞蓟宾、水飞蓟宁、水飞蓟亭、花旗松素溶出度的影响。结果最佳条件为联合载体比例1∶3,药物-载体比例1∶5。固体分散体中5种成分的溶出度显著高于原料药和物理混合物(水飞蓟素-载体)中。结论固体分散体可显著提高水飞蓟素中有效成分的溶出度。福建省自然科学基金项目(2015J01491

Spectrum-effect relationship of immunosuppressive activity of Leigongteng Duogan Tablet based on partial least squares regression analysis

目的初步探讨雷公藤多苷片免疫抑制作用及其HPlC指纹图谱间的相关性。方法采用HPlC建立7个厂家生产的雷公藤多苷片醋酸乙酯提取物的指纹图谱,选择刀豆蛋白A(COn A)刺激的小鼠脾淋巴细胞模型进行免疫抑制药效学研究,分别考察雷公藤多苷片对小鼠脾淋巴细胞增殖以及细胞因子γ干扰素(Ifn-γ)分泌的影响;采用偏最小二乘回归分析法分析谱效关系。结果建立了7个厂家生产的雷公藤多苷片的HPlC指纹图谱,从HPlC指纹图谱中提取出18个能够表征差异的特征峰。药效研究结果显示不同厂家生产的雷公藤多苷片均可显著抑制COn A诱导的小鼠脾淋巴细胞增殖和Ifn-γ的分泌(P<0.05)。偏最小二乘回归法分析结果显示,以抑制小鼠脾淋巴细胞增殖IC50值为药效指标时第1、2、6、7、17、18号峰为药效峰;以Ifn-γ分泌抑制率为指标时,第1、2、6、7、8、9、12、13号峰为药效峰。结论第1、2、6、7、8、9、12、13、17、18号峰所代表的化合物可能为雷公藤多苷片中发挥免疫抑制主要有效成分。Objective To investigate the immunosuppressive components in Leigongteng Duogan Tablet(LDT).Methods High performance liquid chromatography(HPLC) was applied to establish the fingerprint for LDT from seven manufactures.The immunosuppressive effect of LDT was observed on Con A-induced mice spleen cells, and the cell proliferation and contents of IFN-γ were recorded.Then the partial least squares regression(PLSR) analysis was used to investigate its spectrum-effect relationship.Results The HPLC fingerprint for LDT from seven manufactures was established, and 18 characteristic peaks were confirmed.The in vitro cell experimental results showed that the proliferation of mice spleen cells and secretion of IFN-γ were inhibited by all LDT significantly compared with the control group.According to the results of PLSR, No.1, 2, 6, 7, 17, and 18 peaks were strongly related to the proliferation inhibition of mice spleen cells and No.1, 2, 6, 7, 8, 9, 12, and 13 peaks were related to the secretion of IFN-γ.Conclusion The No.1, 2, 6, 7, 8, 9, 12, 13, 17, and 18 peaks are the principal immunosuppressive substances in LDT.福建省科技计划重大项目(2012I1001