双波长一元线性回归分光光度法同时测定复方磺胺甲噁唑片中两组分含量

本文采用双波长一元线性回归分光光度法同时测定了复方磺胺甲噁唑片中SMZ和TMP的含量,分析结果表明:平均回收率SMZ为99.9%,TMP为100.2%,变异系数SMZ为0.25%,TMP为0.76%。     

中和法测定复方新诺明片中SMZ的含量

复方新诺明片中的SMZ的含量测定有双波长紫外分光光度法和亚硝酸钠法。本文根据SMZ酸性较强的特点,采用中和法测定其含量,结果满意。 1 仪器与试药     

测定复方磺胺甲蘸唑片剂含量的简易方法

根据复方磺胺甲噁唑片磺胺甲噁唑(SMZ)分子结构中磺酰胺基-SO2NH-的酸性,我们参考了文献:多数酸性较强的磺胺类药物可用标准碱液直接滴定以测定含量的原理,采用酸量法不经分离测定SMZ含量;用简便分离法以单光束分光光度计测定TMP含量,可在2h内完成复方磺胺甲噁唑片剂的含量测定.较药典法配制对照品精称干燥恒重步骤简捷,同样准确,现介绍如下.     

同时测定复方磺胺药各组分的卡尔曼滤波紫外分光光度法

研究了卡尔曼滤波紫外分光光度法测定复方新诺明片和增效联磺片中各组分的实验条件,结果复方新诺明片平均回收率分别为100.4±0.2%(SMZ)和100.4±0.5%(TMP);增效联磺片平均回收率分别为99.5±0.7%(SMZ)、100.8±0.6%(SD)和99.2±0.6%(TMP)。     

近红外光谱—偏最小二乘方法同时测定复方磺胺甲唑片的两种有效成分

目的建立复方磺胺甲口恶唑片的两种有效成分磺胺甲口恶唑(SMZ)和甲氧苄啶(TMP)的快速同时测定方法。方法基于近红外漫反射光谱技术,利用偏最小二乘方法建立该复方中SMZ和TMP的定量分析多元校正模型。结果对于所建立的SMZ与TMP模型,相关系数分别为:100.00%与100.00%;校正集残差分别为:0.0163与0.008 36;预测均方差分别为:0.156与0.0815。结论本方法在样品不经任何预处理的情况下,实现了该制剂的两种有效成分SMZ和TMP的简单、快速、两组分同时准确测定。     

复方磺胺二甲噁唑和复方磺胺甲异噁唑在正常受试者药物动力学的比较

复方磺胺甲异噁唑(Co-trimoxazole,复方SMZ)是由SMZ和TMP组成,体外试验表明,在最佳浓度比(1:10～1:40)时,两药可发生协同作用。但研究表明,使用复方SMZ后,尿液、支气管吸出液和脑脊液中两药浓度并不能达到最佳比例。最近又引进了     

联立方程组的新解法用于复方磺胺甲(口恶)唑片二组分的测定

在分光光度法中,用解联立方程组法分析复方制剂中两组分含量时,需求测吸收系数,测定受仪器性能等的影响,带入的误差较大,笔者采用联立方程组新解法,以吸收度比代替吸收系数的测定,分析复方磺胺甲(?)唑片剂中 SMZ、TMP 二组分含量,得到较满意的结果。与药典方法比较,方法简便,相对误差不大于1.5%(SMZ)、2.0%(TMP)。1 方法原理设复方制剂中互相干扰的两组分为 a、b,则(?)     

流动注射分析法测定片剂磺胺甲基异恶唑含量的研究

复方磺胺甲基异恶唑片中磺胺甲基异恶唑(SMZ)含量《中国药典》1985年版采用亚硝酸钠法(永停滴定),方法繁琐、费时。笔者利用SMZ与对二甲胺基苯甲醛反应,生成颜色的薛夫氏碱,以流动注射分析法(FIA)在波长452nm处测定其吸收度,对测定制剂中SMZ的含量进行研究,在国内尚未见到报道。本法特点灵敏、快速,用样品量少,重现性好,回收率为99.36～100.61     

复方新诺明有效成分的晶体结构及共晶研究

目的 研究复方新诺明中有效成分磺胺甲噁唑(SMZ)的单晶结构,研究其与甲氧苄啶(TMP)的共晶现象,为开发共晶新剂型提供实验支持.方法 采用加溶剂研磨法制备SMZ和TMP的共晶粉末,利用反射法测定红外光谱,采用差示扫描量热法(DSC)测定熔点,通过粉末X射线衍射(PXRD)研究晶型.通过溶剂挥发法得到SMZ的单晶,利用X射线单晶衍射仪测定其晶体结构.结果 SMZ的单晶属于单斜晶系,空间点群为C2/c,晶胞参数a=1.6209(10)nm,b=0.5527(3)nm,c=2.5955(16)nm,每个晶胞中有8个分子.共晶粉末的熔点为187.78℃,介于SMZ的熔点170.92℃和TMP的熔点201.96℃之间.与单独组分相比较,红外图谱的指纹区发生明显变化,PXRD产生新的X射线粉末衍射峰.结论 SMZ的单晶属于E型结构,SMZ和TMP通过研磨可以形成共晶,共晶现象引起红外、熔点和衍射峰的明显变化,研究结果为开发药物共晶新剂型提供实验基础.     

差示分光光度法测定复方磺胺合剂中两种磺胺的含量

本文建立了以差示分光光度法在254nm,318nm处分别测定复方磺胺合剂中两种磺胺(SMZ、SD)含量的方法,方法简便、快速、准确。     

陈香露白露薄膜衣片的研制

目的:制备陈香露白露薄膜衣片,提高药物稳定性。方法:选用不同的粘合剂制备片芯,再选用不同的包衣材料进行包衣,比较陈香露白露薄膜衣片与糖衣片的稳定性。结果:采用10%聚乙烯吡咯烷酮乙醇液为粘合剂制备片芯,用隔离材料玉米阮将片芯保护,采用上海卡乐康公司的黄色或红棕色胃溶性包衣粉制备的陈香露白露薄膜衣片在外观质量上优于其它材料制备的成品,尤其是防渗油和防潮性方面优势明显;薄膜衣片稳定性优于糖衣片。结论:陈香露白露薄膜衣片质量稳定,制备工艺简单。     

Delivery of prazosin hydrochloride from osmotic pump system prepared by coating the core tablet with an indentation

The preparation of an osmotic pump tablet was simplified by elimination of laser drilling using prazosin hydrochloride as the model drug. The osmotic pump system was obtained by coating the indented core tablet compressed by the punch with a needle. A multiple regression equation was achieved with the experimental data of core tablet formulations, and then the formulation was optimized. The influences of the indentation size of the core tablet, environmental media, and agitation rate on drug release profile were investigated. The optimal osmotic pump tablet was found to deliver prazosin hydrochloride at an approximately constant rate up to 24 hr, and independent on both release media and agitation rate. Indentation size of core tablet hardly affected drug release in the range of 0.80-1.15 mm. The method that is simplified by elimination of laser drilling may be promising for preparation of an osmotic pump tablet.     

Delivery of Prazosin Hydrochloride from Osmotic Pump System Prepared by Coating the Core Tablet with an Indentation

The preparation of an osmotic pump tablet was simplified by elimination of laser drilling using prazosin hydrochloride as the model drug. The osmotic pump system was obtained by coating the indented core tablet compressed by the punch with a needle. A multiple regression equation was achieved with the experimental data of core tablet formulations, and then the formulation was optimized. The influences of the indentation size of the core tablet, environmental media, and agitation rate on drug release profile were investigated. The optimal osmotic pump tablet was found to deliver prazosin hydrochloride at an approximately constant rate up to 24 hr, and independent on both release media and agitation rate. Indentation size of core tablet hardly affected drug release in the range of 0.80–1.15 mm. The method that is simplified by elimination of laser drilling may be promising for preparation of an osmotic pump tablet.     

替硝唑片粘合剂的筛选

目的筛选替硝唑片的粘合剂。方法分别采用8%聚乙烯吡咯烷酮(PVP-K30)、10%淀粉浆、40%糖浆和2.0%羟丙基甲基纤维素K4(HPMC-K4),50%乙醇作为替硝唑片的粘合剂,制成不同粘合剂配方的药片,观察素片的外观以及包衣后外观的变化,测定其硬度、脆碎度、崩解时限和溶出度。结果PVP-K30制成的片有光泽,测定脆碎度后有少许崩边缺角现象,包衣后片表面粗糙;淀粉浆制成的片有光泽,测定脆碎度后无崩边缺角现象,包衣后药片完整;糖浆制成的片较脆,测定脆碎度后有崩边、顶裂现象,包衣后片表面粗糙且有顶裂倾向;羟丙基甲基纤维素制成的片有光泽,振摇无崩边缺角现象,包衣后完整,外观好。结论用2.0%HPMC-K4、50%乙醇为粘合剂制备的药片外观好,在包薄膜衣过程中,不易出现崩边、缺角现象,包衣后片面美观,硬度、崩解度和溶出度也优于用其它粘合剂制成的片子。     

复方盐酸曲马多分散片处方及制剂工艺

目的:制备以盐酸曲马多和对乙酰氨基酚为主药的分散片.方法:选用直接粉末压片技术,建立反相高效液相色谱法测定该制剂中盐酸曲马多和紫外分光光度法测定对乙酰氨基酚.结果:工艺简便,分散快,5min累积释放度达到80%,质量稳定.结论:该处方工艺制成的分散片符合中国药典的要求.     

Preparation of monolithic osmotic pump system by coating the indented core tablet.

A method for the preparation of monolithic osmotic pump tablet was obtained by coating the indented core tablet compressed by the punch with a needle. Atenolol was used as the model drug, sodium chloride as osmotic agent and polyethylene oxide as suspending agent. Ethyl cellulose was employed as semipermeable membrane containing polyethylene glycol 400 as plasticizer for controlling membrane permeability. The formulation of atenolol osmotic pump tablet was optimized by orthogonal design and evaluated by similarity factor (f2). The optimal formulation was evaluated in various release media and agitation rates. Indentation size of core tablet hardly affected drug release in the range of (1.00-1.14) mm. The optimal osmotic tablet was found to be able to deliver atenolol at an approximately constant rate up to 24h, independent of both release media and agitation rate. The method that is simplified by coating the indented core tablet with the elimination of laser drilling may be promising in the field of the preparation of osmotic pump tablet.     

甲花片薄膜包衣的生产工艺优化

目的：改进甲花片的制备工艺,将甲花片改为薄膜包衣片。方法：采用正交设计对甲花片处方工艺进行优化。结果：以2％羟丙甲基纤维素（70％乙醇溶液）为粘合剂取代淀粉浆,搅拌时间15min,颗粒水分为2％-4％,片芯硬度在3～4kg·mm^-2,制成的包衣片合格率高,且崩解时限符合规定。结论：采用新处方工艺生产的甲花薄膜包衣片质量稳定,薄膜包衣合格率可达95％以上。     

The effect of buffering of acetylsalicylic acid on dissolution,absorption, gastric pH and faecal blood loss

A high-buffered experimental acetylsalicylic acid (ASA) tablet designed to be swallowed intact and a conventional low-buffered ASA tablet were compared in vitro with regard to dissolution and buffering and in vivo with regard to absorption, intragastric buffering and tendency to cause gastrointestinal bleeding.high-buffered tablet was dissolved in vitro within 3 min. In vivo the tablet raised the intragastric pH to a minimum value of 7 and reached a maximal plasma concentration after 20–30 min. The low-buffered tablet dissolved more slowly and did not raise the pH in vitro above 2. In vivo the tablet raised the intragastric pH to 4.5 and a maximal plasma concentration of salicylate was obtained after 90 min. The high-buffered tablet reduced the daily faecal blood loss by 50% compared to the low-buffered tablet.It can be concluded that the high-buffered tablet was more rapidly dissolved and faster absorbed than the low-buffered tablet. The reduced gastrointestinal bleeding found with the high-buffered tablet is probably due to an adequate in vivo buffering.     

Food effects on tablet disintegration.

The aims of the present study was to investigate if food components, as represented by a multi-component nutritional drink for tube feeding, could affect tablet disintegration of standard tablets in vitro as well as in vivo and propose a mechanism for potential food effects on tablet disintegration. The tablet disintegration was delayed between 5 min and more than 1h in the simulated gastric fed medium compared to a simple buffer. This effect was dependent on the tablet composition. A similar delay in tablet disintegration was also found in vivo after administration of the nutritional drink to three Labradors as observed by removing the tablet from the stomach at different times through a gastric fistula. The delay in tablet disintegration appeared to be caused by precipitation of a film, mainly consisting of protein, on the tablet surface as indicated by disintegration studies with pure nutrients, identification by IR spectroscopy of contents of precipitates obtained in a model study were the nutrients were incubated with different tablet excipients and visual observations of tablets exposed to the simulated fed medium. The drug dissolution of a soluble compound, metoprolol tartrate, from a standard tablet was also strongly delayed in the simulated fed medium. In conclusion, food, could significantly delay tablet disintegration and drug dissolution in the stomach by formation of a film around the tablets. This effect could be monitored by a simple in vitro disintegration test using a test medium based on a nutritional drink. More studies are needed to investigate the significance of the slow tablet disintegrations on bioavailability and for which types of food the present effect occurs.     

氟伐他汀钠分散片的制备

目的制备氟伐他汀钠分散片。方法以崩解时间为指标,采用正交设计试验,对氟伐他汀钠分散片处方进行筛选。结果乳糖、微晶纤维素(MCC)各40%为填充剂,MCC、羧甲基淀粉钠(CMS-Na)5%和低取代羟丙基纤维素(LS-HPC)10%为崩解剂,湿法制粒制备分散片。进行了溶出度实验。符合中国药典中有关分散片的要求。结论所制分散片处方合理,崩解快、溶出快而完全。