乙酰螺旋霉素片的工艺研究

目的：筛选乙酰螺旋霉素片最佳处方。方法：考察预胶化淀粉、低取代羟丙基纤维素和吐温－８０对乙酰螺旋霉素片的质量影响,并与２种市售乙酰螺旋霉素片作溶出度比较。结果：筛选的最佳处方制备的乙酰螺旋霉素片,体外溶出度大为提高。结论：本法处方合理,工艺简单,适用于工业化生产。     

提高乙酰螺旋霉素片溶出度的研究

目的:研究乙酰螺旋霉素片的处方,提高溶出速度。方法:采用正交试验的方法进行试验。结果:找出生产工艺的最佳工艺参数。结论:表面活性剂的用量、粘合剂用量、湿混合时间是影响乙酰螺旋霉素片溶出度的重要因素。     

提高尼美舒利片溶出度的工艺研究

目的:筛选尼美舒利片的最佳处方工艺,提高其溶出度.方法:考察粘合剂浓度、研磨时间、压片力对尼美舒利片溶出度的影响.结果:按照筛选的最佳处方工艺制备的尼美舒利片溶出度大为改善,符合药典标准.结论:该方法处方合理,工艺简单,适合于工厂化生产的要求.     

阿莫西林克拉维酸钾(7∶1)片处方、工艺研究及溶出度考察

目的:研究阿莫西林克拉维酸钾片处方及工艺,并考察其溶出度.方法:通过吸湿性试验、处方及工艺优化确定制备工艺,制备了阿莫西林克拉维酸钾片,用高效液相色谱法测定其溶出度并与进口薄膜衣片进行比较.结果:本制剂必须采用干法制粒压片工艺,制备环境湿度控制在33%以下,自制片与进口片溶出相当.结论:阿莫西林克拉维酸钾片处方工艺合理.     

西咪替丁片的制备工艺及对溶出度的影响

目的:寻求制备西咪替丁片的最佳工艺.方法:考察L-HPC、吐温-80的选择与用量,粘合剂的种类及润滑剂对西咪替丁片溶出度的影响.结果:所选处方和工艺制备的西咪替丁片硬度较好,脆碎度合格,外观光洁,溶出度可达98%以上.结论:本法处方合理,工艺简单.     

乙酰螺旋霉素的质量评价

摘 要 目的：评价乙酰螺旋霉素的质量现状及存在的问题。方法: 依据中国药典2015年版二部标准,对乙酰螺旋霉素及其制剂进行检验,分析国内乙酰螺旋霉素的质量总体水平;并对其有关物质、组分及溶出度开展探索性研究,进一步分析其质量状况。结果: 在 258批次的制剂中,仅有1批乙酰螺旋霉素片溶出度不合格,合格率为99.6%。探索性研究结果表明,合成工艺决定原料杂质,国内外制剂杂质谱差异较大;国产制剂在4种介质中的溶出行为与原研制剂均不相似。结论:目前国产乙酰螺旋霉素质量状况较好;有关物质研究为今后目标杂质的控制提供了参考,溶出度的一致性评价为乙酰螺旋霉素片的处方工艺改进和临床应用提供参考。     

改善桂利嗪片溶出度的制备工艺研究

目的 解决桂利嗪片溶出度不稳定的问题.方法 通过正交优化选择处方,达到最佳制备工艺. 结果桂利嗪片溶出度符合规定.结论 制备工艺可行.     

头孢呋辛酯片溶出度的研究分析

目的研究适宜头孢呋辛酯片的处方与制备工艺,以提高其溶出度。方法设计不同辅料的处方,从不同处方中筛选出最适宜的辅料,并通过研究微晶纤维素的硬度、用量及含水量,以选出头孢呋辛酯片的最佳处方与制备工艺,提高其溶出度。结果当微晶纤维素的硬度为4~6kg,用量为主药的60%,水分为2%时,所制备的头孢呋辛酯片溶出度为90%,符合规定标准。结论运用适宜的辅料及制备工艺,可有效提高头孢呋辛酯片的溶出度,增强药物利用率。     

富马酸比索洛尔片制备工艺与质量控制研究

目的:制备富马酸比索洛尔片,并测定其含量均匀度和溶出度。方法:利用含量测定、溶出度测定等方法,结合药物性质,筛选制剂处方、工艺,并进行质量研究。结果:确定了处方、制备工艺,建立了质量标准。结论:所制富马酸比索洛尔片符合《中华人民共和国药典》2000年版二部附录ⅠA所规定的片剂质量标准。     

吡罗昔康片处方工艺的改进研究

目的　通过对吡罗昔康片处方及工艺的改进提高其溶出度。方法　采用正交实验设计方法 ,以溶出度测定结果为指标进行处方筛选。结果　筛选后的处方可达到中国药典 2 0 0 0年版对溶出度的要求。结论　该片剂处方合理 ,制备工艺简单易行 ,适合工业化生产。     

乙酰螺旋霉素片剂和胶囊剂的抗菌作用比较

目的比较乙酰螺旋霉素片剂和胶囊剂的体外抗菌作用。方法将乙酰螺旋霉素随机分为片剂组和胶囊组,2组均进行药物体外抗菌实验,测定其对大肠杆菌、金黄色葡萄球菌、枯草芽孢杆菌及绿脓杆菌的最小抑菌浓度（MIC）和最小杀菌浓度（MBC）,对2组的抗菌作用进行比较。结果片剂组MIC及MBC值均高于胶囊组,差异均有统计学意义（P〈0.05）。结论乙酰螺旋霉素片剂抗菌效果优于胶囊剂,可将片剂作为抗菌作用的最佳剂型。     

丹参酮口腔速溶片工艺及理化性质的研究

目的：探讨丹参酮速溶片的制备工艺。方法：采用正交设计法，以粉粒流动性、崩解时限、体外溶出度为指标，对丹参酮速溶片处方进行筛选。结果：速溶片在30s内完全崩解，体外溶出度明显优于普通片。结论：制备的丹参酮速溶片工艺成熟，质量稳定。     

Use of Glancing Angle X-Ray Powder Diffractometry to Depth-Profile Phase Transformations During Dissolution of Indomethacin and Theophylline Tablets

PURPOSE: The purpose of this study was (i) to develop glancing angle x-ray powder diffractometry (XRD) as a method for profiling phase transformations as a function of tablet depth; and (ii) to apply this technique to (a) study indomethacin crystallization during dissolution of partially amorphous indomethacin tablets and to (b) profile anhydrate --> hydrate transformations during dissolution of theophylline tablets. METHODS: The intrinsic dissolution rates of indomethacin and theophylline were determined after different pharmaceutical processing steps. Phase transformations during dissolution were evaluated by various techniques. Transformation in the bulk and on the tablet surface was characterized by conventional XRD and scanning electron microscopy, respectively. Glancing angle XRD enabled us to profile these transformations as a function of depth from the tablet surface. RESULTS: Pharmaceutical processing resulted in a decrease in crystallinity of both indomethacin and theophylline. When placed in contact with the dissolution medium, while indomethacin recrystallized, theophylline anhydrate rapidly converted to theophylline monohydrate. Due to intimate contact with the dissolution medium, drug transformation occurred to a greater extent at or near the tablet surface. Glancing angle XRD enabled us to depth profile the extent of phase transformations as a function of the distance from the tablet surface. The processed sample (both indomethacin and theophylline) transformed more rapidly than did the corresponding unprocessed drug. Several challenges associated with the glancing angle technique, that is, the effects of sorbed water, phase transformations during the experimental timescale, and the influence of phase transformation on penetration depth, were addressed. CONCLUSIONS: Increased solubility, and consequently dissolution rate, is one of the potential advantages of metastable phases. This advantage is negated if, during dissolution, the metastable to stable transformation rate > dissolution rate. Glancing angle XRD enabled us to quantify and thereby profile phase transformations as a function of compact depth. The technique has potential utility in monitoring surface reactions, both chemical decomposition and physical transformations, in pharmaceutical systems.     

Fast-dissolving tablets of glyburide based on ternary solid dispersions with PEG 6000 and surfactants

Marketed glyburide tablets present unsatisfying dissolution profiles that give rise to variable bioavailability. With the purpose of developing a fast-dissolving tablet formulation able to assure a complete drug dissolution, we investigated the effect of the addition to a reference tablet formulation of different types (anionic and nonionic) and amounts of hydrophilic surfactants, as well as the use of a new technique, based on ternary solid dispersions of the drug with an hydrophilic carrier (polyethylene glycol [PEG] 6000) and a surfactant. Tablets were prepared by direct compression or previous wet granulation of suitable formulations containing the drug with each surfactant or drug:PEG:surfactant ternary dispersions at different PEG:surfactant w/w ratios. The presence of surfactants significantly increased (p<0.01) the drug dissolution rate, but complete drug dissolution was never achieved. On the contrary, in all cases tablets containing ternary solid dispersions achieved 100% dissolved drug within 60 min. The best product was the 10:80:10 w/w ternary dispersion with PEG 6000 and sodium laurylsulphate, showing a dissolution efficiency 5.5-fold greater than the reference tablet formulation and 100% drug dissolution after only 20 min.     

卡马西平片体外溶出度与体内吸收相关性

目的：考察卡马西平（ＣＢＺ）片溶出度与体内吸收的相关性。方法：应用ＺＲＳ－４溶出度仪测定卡马西平片的溶出度。４名男性健康志愿性ｐｏ单剂量２００ｍｇＣＢＺ用ＴＤｘ分析仪测定血药浓度，并按照Ｗａｇｎｅｒ－Ｎｅｌｓｏｎ公式计算药物吸收分数。结果：体外溶出度与体内药物吸收分数的相关系数ｒ＝０．９２６１，体外溶出度与体内药物吸收分数的相关系数ｒ＝０．９９７７。结论：ＣＢＺ片体外溶出度与体内吸收有较好的相关性     

甲磺酸酚妥拉明分散片溶出度测定的研究

目的：对甲磺酸酚妥拉明分散片进行了体外溶出度试验。方法：选用转篮法,溶出量采用紫外分光光度法测定。结果：本品3批3min平均溶出量均超过标示量的80%。结论：本方法用于甲磺酸酚妥拉明分散片的溶出度测定快速简便,结果满意。     

片剂溶出度影响因素分析

目的:考察片剂溶出度的影响因素,提高片剂溶出度,从而提高产品质量。方法:通过实验,研究各种参数对片剂溶出度的影响,选择出最佳工艺条件,如改进处方、控制颗粒硬度和大小、控制压力等工艺参数,用于指导大型生产,提高片剂溶出度。结论:崩解剂及润滑剂的用量对片剂溶出度影响较大,颗粒的硬度及大小、粘合剂的温度,压片压力对片剂的溶出度亦有影响;片剂直径大小对片剂溶出度影响不大。     

一阶导数光谱法测定卡托普利片溶出度

目的:建立卡托普利片溶出度实验方法;方法:小杯法,60r·min;介质:水,用一阶导数光谱法测定卡托普利的溶出度;结果:30min时的溶出度量不少于75％;结论:本方法准确可用于卡托普利片溶出度的测定。     

卡维地洛片溶出度的研究

目的：测定卡维地洛片的溶出度。方法：按要求根据中华人民共和国药典1995年版二部“转篮法”测定其百分含量。结果：卡维地洛片在30min内累积溶出百分率＞90％,回收率＞95％,RSD＜1％。结论：通过对卡维地洛片溶出百分率的测定,表明卡维地洛片处方设计合理。     

布洛芬微晶体在口腔崩解片中的应用

目的：改善口腔崩解片干粉压片工艺中药物的可压性、流动性、黏冲性，提高崩解片的崩解速度。方法：以布洛芬为模型药物，利用溶剂-非溶剂法改变其结晶形态，获得5种不同的微晶体，并用扫描电镜（SEM）和X衍射仪（XRD）表征。通过各晶体的压片工艺性能测试及压片后的崩解实验，优选出性能良好的晶体，并对其压制的崩解片进行了体外洛出性能的测定。结果：优选出的微晶体具有良好的可压性、流动性和抗黏冲性能，压片后崩解时限大大缩短，溶出度也有一定的提高。结论：优选出的布洛芬微晶体改善了口腔崩解片的整体性能。