琥珀酸美托洛尔HPMC骨架片释放影响因素研究

以羟丙基甲基纤维素（HPMC）为骨架材料，乙基纤维素（EC）为阻滞剂，采用湿颗粒压片法制备琥珀酸美托洛尔亲水凝胶骨架片，考察HPMC用量、HPMC黏度、EC用量、制备方法、压片压力、释放介质及转速对琥珀酸美托洛尔（MS）骨架片体外释药的影响。结果表明，MS骨架片体外释药符合Higuchi方程，药物释放机制是骨架溶蚀和药物扩散的综合效应；HPMC用量与黏度、阻滞剂用量、制备方法、压片压力对释放速率均有显著性影响；释放介质的pH值及转速对释放速率无显著性影响。     

丙戊酸镁缓释片体外释药特性及体内相对生物利用度的研究

目的:研制丙戊酸镁缓释片,并评价其体外释药特性及体内生物等效性。方法:以释放度为主要指标筛选片剂处方及制备工艺,并对12名健康男性受试者进行体内生物利用度研究。结果:以优选的处方,工艺制备的片剂,体外释药性能良好,符合Higuchi方程,持续释药达8h以上。且释药性能稳定,不受溶出介质pH值的影响。其体内药代动力学参数为:Cmax,30.0±4.6ug·ml-1;Tmax,11.5±4.8h;T1/2。17.8±4.6h;F,95±8％。结论:丙戊酸镁缓释片与普通片相比具有缓释特性。相对生物利用度为95±8％。     

氨酚氯雷伪麻双层片的处方设计

目的 研究亲水凝胶型骨架片氨酚氯雷伪麻双层缓释片的处方工艺,并对缓释片制备过程中的几点影响因素进行了初步探讨.方法 以氯雷他定的含量均匀度为考察指标,通过正交试验筛选出最佳处方工艺,并考察羟丙甲基纤维素(HPMC)用量对氨酚氯雷伪麻缓释片体外释放度的影响.结果 按最佳处方制备的氨酚氯雷伪麻缓释片,对乙酰氨基酚和硫酸伪麻黄碱释放度达到要求,氯雷他定含量均匀度符合要求.结论 按优化处方制备的氨酚氯雷伪麻缓释片符合相关规定.     

单硝酸异山梨酯脉冲控释微丸的制备及体外释药影响因素的研究

制备单硝酸异山梨酯脉冲控释微丸并对影响释药的因素进行考察.采用挤出滚圆法制备载药丸芯,以水溶胀性材料为内包衣溶胀层,乙基纤维素水分散体为外包衣控释层制备脉冲控释微丸,并考察溶胀层材料类型、溶胀层和控释层包衣增重、介质pH值等对药物释放的影响.结果表明,该包衣微丸可脉冲释药,药物释放情况不受pH值的影响,低取代羟丙基纤维素与羟丙基甲基纤维素以一定比例混合作为内包衣层,乙基纤维素水分散体为外包衣层制备的脉冲控释微丸,当内包衣层增重为15%和外包衣层增重为13%时,达到了时滞为5 h、时滞后1.5 h累积释药80%以上的脉冲释药效果.     

长效避孕皮下埋植剂体外缓释行为研究

本文对以加成型硅橡胶为基质的左旋18—甲基炔诺酮长效避孕埋植剂的体外释放行为及对可能影响其释放量的诸因素,进行了观察与研究,结果表明:此长效避孕皮下埋植剂的体外释药行为,符合零级释药动力学规律。释药量受控释膜厚度,控释膜交联密度及释药面积的影响。体外释放药物曲线无明显爆破峰。     

盐酸多柔比星缓释植入剂体外释药与体外降解的研究

以聚（乳酸-羟基乙酸）共聚物（PLGA）为载体制备盐酸多柔比星缓释植入剂,测定植入剂的释放度和PLGA失重率,结果表明PLGA体外降解曲线呈＂S＂形,起初的迟缓期后降解速率加快,5周时失重率达80%。植入剂表现出趋于零级的药物释放模式（r=0.9880）,在0~25 d日均释放度达3.26%,35 d时累积释放度达90%以上。植入剂可持续释药1个月,释药速率主要取决于PLGA降解速率,通过调节PLGA降解速率可以很好地控制药物的释放度。     

盐酸表阿霉素纳米靶向制剂的缓释效应

背景：盐酸表阿霉素是一种广谱抗生素,目前临床使用的不足多为药物释放快、目标组织药物浓度低,静脉给药后广泛分布于体内各种组织器官,不良反应明显。 目的：针对盐酸表阿霉素临床应用的不足,制备盐酸表阿霉素纳米靶向注射制剂。 方法：以叶酸偶联牛血清白蛋白为载体,采用乳化-高压匀质法,制备盐酸表阿霉素纳米靶向注射制剂,以激光粒度分析仪测定纳米颗粒的粒径大小、粒径分布及Zeta电位,扫描电镜观察纳米颗粒的表面形态,高效液相色谱法分析白蛋白负载盐酸表阿霉素纳米制剂的包封率、载药量和释药性能。 结果与结论：制备的盐酸表阿霉素纳米粒外观呈均匀球型,粒径分布较窄,平均粒径为(157.73±     0.40) nm,平均 Zeta 电位为(-30.85±0.43) mV,载药量 22.78%,包封率可达96.24%。体外模拟释药结果表明药物释放曲线分为两个阶段,突释阶段微球释药量在24 h内达42.6%,缓释阶段纳米粒释药持续时间长,在112 h 时释药量达 84.1%,载药纳米粒的药物释放速率持续稳定。结果表明乳化结合高压匀质法制备的盐酸表阿霉素纳米靶向制剂粒径均匀,粒径范围分布窄,载药量和包封率高,具有一定的缓释作用。     

磁性聚乳酸-羟基乙酸氧化苦参碱纳米粒的制备及其特性

目的研究磁性聚乳酸-羟基乙酸氧化苦参碱纳米粒(M-PLGA-OM-NP)的制备工艺,并对纳米粒子进行评价。方法运用复乳法制备M-PLGA-OM-NP,通过透射电子显微镜观察纳米粒形态,并对纳米粒的平均粒径、载药量、包封率、体外释药情况等进行评价。结果纳米粒外观呈规则球形,其平均粒径为146.5 nm,载药量为7.61%,包封率为44.8%。突释后至第72小时,纳米粒维持较稳定的释药速度,累积释放达52.9%。72～240 h,药物释放缓慢,累计释放约为16.6%,体外释放符合Ritger peppas方程lny=1.280 6+lnt。氧化苦参碱药性不受温度影响。结论获得了较满意的M-PLGA-OM-NP制备工艺,其过程简单,粒子性状符合要求。     

羧甲基壳聚糖作为植入可降解缓释微球辅料的实验研究

羧甲基壳聚糖作为一种高分子材料 ,具有良好的组织相容性和生物可降解性。本实验试图利用羧甲基壳聚糖作为植入环丙沙星微球的缓释辅料 ,并探索这一剂型的制备工艺、结构形态和体外释药特性。首先我们采用乳化交联技术制备微球 ;然后用扫描电子显微镜、红外光谱、及示差热分析等方法研究微球的结构和形态 ;建立体外持续流动释放系统初步检测微球的体外释放特性。实验结果发现 :微球的结构和形态受制备工艺条件如温度、离子强度、搅拌速度等因素的影响 ;一定工艺条件下制备的环丙沙星微球的体外释放时间可达 7d以上 ,释放行为符合 Higuchi方程。因此 ,我们认为 :羧甲基壳聚糖可作为环丙沙星可降解植入微球的缓释辅料 ;乳化交联技术是制备这一微球的有效方法 ,工艺简单、稳定     

载异烟肼利福平聚乳酸纳米粒的制备及体外释药**

背景：微载体药物因具有靶向性、控释性、稳定性、更好的安全性备受关注。 目的：观察载异烟肼利福平两种抗结核药于同一聚乳酸纳米粒的给药系统及体外释放特性。 方法：采用改良的自乳化二元溶剂扩散法制备载异烟肼和利福平纳米粒,亚微粒径分析仪测定纳米粒粒径及分布,透射电镜观察其形态;高效液相色谱仪建立测定异烟肼、利福平的载药量和包封率;以磷酸盐缓冲液为释放介质,观察载异烟肼和利福平纳米粒的体外释药特性。 结果与结论：载利福平和异烟肼纳米粒表面完整光滑,无明显粘连现象,纳米粒均匀度好。亚微粒径分析仪测定纳米粒平均粒径80.4 nm。异烟肼载药量为(15.95±1.34)%,包封率为(5.01±0.17)%;利福平载药量为(4.66±0.97)%,包封率为(4.05±0.18)%。体外释药结果显示纳米粒的体外释药过程较平稳。突释期纳米粒中异烟肼释放度为15.22%,到3 d累积释放度可达95.6%;利福平释放度为9.26%,到3 d累积释放度可达90.3%。提示采用改良的自乳化二元溶剂扩散法制备载异烟肼和利福平纳米粒,所得载药纳米粒的粒径小且较均匀。纳米粒体外释药过程较平稳,无明显突释现象。关键词：聚乳酸;异烟肼;利福平;纳米粒;体外释药 doi:10.3969/j.issn.1673-8225.2012.16.014     

盐酸吗啡缓释片联合低剂量阿米替林治疗中重度癌性骨痛的疗效观察

目的 探讨盐酸吗啡缓释片联合低剂量阿米替林治疗中重度癌性骨痛的疗效及安全性。方法 选择2015年1~12月在自贡市第四人民医院接受盐酸吗啡缓释片联合低剂量阿米替林镇痛治疗的中重度癌性骨痛患者,共47例,观察并记录患者镇痛有效率、生活质量评分及副反应。结果 治疗14 d后患者疼痛缓解总有效率为89.36%。治疗后生活质量评分较治疗前有改善[（18.22±4.53）分vs（12.92±5.41）]分,P＜0.05;主要不良反应为恶心、呕吐、便秘、嗜睡及口干。结论 盐酸吗啡缓释片联合低剂量阿米替林治疗中重度癌性骨痛安全有效,不良反应少。     

Preparation and characterization of TAM-loaded HPMC/PAN composite fibers for improving drug-release profiles

The present paper reports the preparation and characterization of composite hydroxypropyl methylcellulose/polyacrylonitrile (HPMC/PAN)-medicated fibers via a wet spinning technique. Tamoxifen (TAM) was selected as a model drug. Numerous analyses were conducted to characterize the mechanical, structure and morphology properties of the composite fibers. The drug content and in vitro dissolution behavior were also investigated. SEM images showed that the TAM-loaded HPMC/PAN composite fibers had a finger-like outer skin and a porous structure. FT-IR spectra demonstrated that there was a good compatibility between polymer and drug. Results from X-ray diffraction and DSC suggested that most of the incorporated TAM was evenly distributed in the fiber matrix in an amorphous state, except for a minority that aggregated on the surface of fibers. The drug content in the fibers was lower than that in the spinning solution and about 10% of TAM was lost during spinning process. In vitro dissolution results indicated that, compared to TAM-PAN fibers, HPMC/PAN composite systems had weaker initial burst release effects and more drug-loading. The combination of hydrophilic polymer HPMC with PAN could improve the performance of polymer matrix composite fibers in regulating the drug-release profiles.     

盐酸羟考酮缓释片对急性放射性黏膜炎所致疼痛的应用效果评价

目的 探讨应用盐酸羟考酮缓释片处理急性放射性黏膜炎所致疼痛的效果。方法 选择2014年12月~2018年9月我院肿瘤内科收治106例鼻咽癌放化疗患者,随机分为对照组和实验组,每组53例;对照组常规行口腔护理、雾化治疗、非甾体类止痛药物治疗、抗炎治疗及营养支持治疗,实验组在对照组基础上应用盐酸羟考酮缓释片替代非甾体类止痛药物,比较两组患者在放疗期间及结束时止痛效果、睡眠状态、体重变化、口腔黏膜损伤恢复情况及治疗过程中药物不良反应发生情况。结果 实验组镇痛总有效率为88.68%,高于对照组的15.09%,差异有统计学意义（P＜0.05）;实验组治疗前后体重变化低于对照组,差异有统计学意义（P＜0.05）。实验组中应用羟考酮缓释片期间15.09%的患者出现便秘,5.66%的患者有轻度的恶心头晕,副反应小可耐受。结论 应用小剂量盐酸羟考酮缓释片对减轻急性放射性黏膜炎所致疼痛效果显著,药物不良反应小,无成瘾性,改善患者生活质量及治疗依从性,影响预后。     

盐酸坦洛新缓释胶囊治疗输尿管结石的临床疗效分析

目的：探析采用盐酸坦洛新缓释胶囊治疗输尿管结石的临床效果。方法：选取我院2013年3月至2015年3月收治的输尿管结石患者312例,均行体外冲击波碎石治疗,术后随机分为甲、乙、丙组各104例开展药物辅助排石治疗。甲组采取加味结石汤、双氯芬酸钠栓联合硝苯地平片,乙组在此基础上给予盐酸坦洛新缓释胶囊,丙组在此基础上应用盐酸坦索罗辛缓释胶囊。观察并比较三组患者的结石排净率、肾绞痛发生率及疼痛程度等情况。结果：乙组与丙组患者治疗后3 d、1周、2周与4周的结石排净率均显著高于甲组,同时,两组患者治疗后肾绞痛发生率与视觉模拟量表(visual analogue scale,VAS)疼痛评分均显著好于甲组,具有统计学意义(P<0.05)。而乙组患者治疗后3 d的结石排净率与治疗后肾绞痛发生率均显著好于丙组,具有统计学意义(P<0.05)。三组患者治疗后不良反应发生率比较差异均无统计学意义(P>0.05)。结论：输尿管结石患者术后采用盐酸坦洛新缓释胶囊与盐酸坦索罗辛缓释胶囊治疗均可获得良好的治愈效果,但盐酸坦洛新缓释胶囊的起效更为迅速,对肾绞痛的抑制效果更为显著,且具有较高临床安全性。     

苏州吴江区社区医院2017年降压药使用情况分析

目的 通过收集2017年各类降压药销售金额和患者购买情况,分析各类降压药使用情况,以便进一步优化社区降压药的销售品种。方法 采用回顾性分析的方法,收集社区2017年全年门诊降压药的使用数据。计算各类药物的销售金额、用药频度（DDDs）、药物日均费用（DDDc）,并通过各药的DDDs排序（A）和用药金额排序（B）,计算比值（B/A）。结果 苯磺酸左旋氨氯地平片、厄贝沙坦片、盐酸贝那普利（洛汀新）、缬沙坦分散片（达乐）、非洛地平缓释片（波依定）DDDs值较高,临床对该类药的选择倾向性大,使用频率高。苯磺酸左旋氨氯地平片的B/A值为1.00、尼莫地平胶囊、琥珀酸美托洛尔缓释片、盐酸贝那普利（洛汀新）以及利尿剂的B/A值接近1,这些药同步性较好,药品的价格与患者的接受程度相一致。结论 门诊高血压患者最常用的降压药物是钙拮抗剂,其次为ACEI和ARB,应用最少的是利尿剂。我院降压药的使用情况基本合理,随着医疗卫生体制改革的变化,降压药的使用结构会越发合理。     

Preparation and Characterization of TAM-Loaded HPMC/PAN Composite Fibers for Improving Drug-Release Profiles

The present paper reports the preparation and characterization of composite hydroxypropyl methylcellulose/polyacrylonitrile (HPMC/PAN)-medicated fibers via a wet spinning technique. Tamoxifen (TAM) was selected as a model drug. Numerous analyses were conducted to characterize the mechanical, structure and morphology properties of the composite fibers. The drug content and in vitro dissolution behavior were also investigated. SEM images showed that the TAM-loaded HPMC/PAN composite fibers had a finger-like outer skin and a porous structure. FT-IR spectra demonstrated that there was a good compatibility between polymer and drug. Results from X-ray diffraction and DSC suggested that most of the incorporated TAM was evenly distributed in the fiber matrix in an amorphous state, except for a minority that aggregated on the surface of fibers. The drug content in the fibers was lower than that in the spinning solution and about 10% of TAM was lost during spinning process. In vitro dissolution results indicated that, compared to TAM–PAN fibers, HPMC/PAN composite systems had weaker initial burst release effects and more drug-loading. The combination of hydrophilic polymer HPMC with PAN could improve the performance of polymer matrix composite fibers in regulating the drug-release profiles.     

Sustained release of a model macromolecule from preparations with erodible core

A series of sustained release tablets were prepared which consisted of a water-soluble core and a highly hydrophobic coat. Release of a macromolecule, Spectrum Orange, from this preparation was studied. It was found that release was controlled by the coat composition and coating solution viscosity. SEM and optical microscopy of the tablets indicated that the coats contained pores on the surface which penetrated in towards the centre of the core. It was deduced that the almost zero order release of macromolecules from these tablets was basically through these pores and not by diffusion through the polymer matrix.     

非洛地平缓释片在中国高血压患者治疗中的应用

BACKGROUND: Felodipine sustained-release tablets are taken orally once daily, which not only exhibit a flat plasma-concentration curve, but also have characteristics of stable effect-acting, good absorption in vivo, high bioavailability and good compliance. OBJECTIVE: To introduce the application status of felodipine sustained-release tablets in the hypertensive treatment of China. METHODS: A computer-based research of CNKI database was performed for literatures published from January 1, 2005 to July 1, 2016. Using the keywords of “felodipine sustained-release tablets, hepertension”, 174 articles were retrieved; and when retrieving “felodipine sustained-release tablets, materials”, 22 were obtained. Thirty literatures were enrolled finally for analysis according to the exclusion criteria. RESULTS AND CONCLUSION: Felodipine sustained-release tablets have been popularized to the hypertensive treatment in our country, and obtain satisfactory treatment outcomes for mild and moderate spontaneous hepertension, which are similar with those of the nifedipine sustained-release tablets, metoprolol sustained-release tablets and benazepril hydrochloride tablets. Felodipine sustained-release tablets also induce slight adverse reactions, such as headache, flush, palpation and swelling of ankles. For patients with hypertension cannot be alleviated through single use of felodipine sustained-release tablets, combination with other types of antihypertensive drugs including beta blockers, angiotensin converting enzyme inhibitors and diuretics is advisable. Compound felodipine sustained-release tablets have been used in clinic, and numerous multicenter, double-blind, randomized control trials have proved its effectiveness and safety. Therefore, compound felodipine sustained-release tablets are another choice when single treatment shows no improvement on patients with spontaneous hypertension.