粉体弹性恢复对缓释片释放度的影响

目的：考查盐酸安非他酮缓释片压片后强度的变化对释放度的影响。方法：压片后1、2和4d测定片剂抗张强度、弹性恢复率和释放度，与压片当日测定结果进行比较。结果：2d内片剂抗张强度降低10．58％、弹性恢复率0．4596％、释放速度变快2％～3％。结论：经过弹性恢复期片剂强度有所下降，主药在各时间点的释放度增大，提示在缓释片处方设计及生产过程中有必要考查弹性恢复对释放度的影响。     

粉末X-射线衍射法测定阿托伐他汀钙片剂中晶型Ⅰ的含量

目的 应用粉末X-射线衍射技术对片剂中阿托伐他汀钙的晶型Ⅰ含量进行定量分析。方法 采用缩短扫描范围,降低扫描速度,提高步进扫描时间的精细扫描方法,建立了晶型Ⅰ含量测定的线性方程y=3179.3x-304.56（r=0.992 3）,并经方法学验证。结果 对2个规格6个批号片剂的晶型Ⅰ含量进行了测定,结果发现片剂中晶型Ⅰ含量有一定的变化。结论 本法操作简单,在辅料没有干扰的情况下可用于片剂中阿托伐他汀钙晶型Ⅰ含量的定量分析。     

格列本脲(优降糖)片剂的生物利用度

对四种格列本脲(Glibenclamide)商品片剂A、B、C、D 及两种对照片E、F,进行体外溶出速度试验,并测定E、F 片剂的体内生物利用度。E、F 的处方及制备方法与商品片剂相同,仅微粒大小不同,E 为未微粉化片剂,F 则为微粉化片剂。以上片剂每片格列本脲含量均为5mg。体外试验,分别对6种片剂进行硬度、含量均匀度、解集速率及溶出速度试验。溶出速度分别在两种不同     

盐酸四环素片剂的某些性质与稳定性

四环素类片剂在贮藏中,常因产生降解产物(脱水四环素,4-差向脱水四环素)而变色,使毒性增大。因而,贮藏期的稳定性是四环素类片剂的主要质量指标。此外,片剂的崩解度和主药溶出速度对于保证片剂的生     

片剂分装后的质量调查

片剂分装是医院药房较普通的一项工作,可加快处方调配速度,提高药房工作效率。但是片剂分装后,在使用和存放过程中,总有一定数量的药品发生不同程度的质量变化。为此笔者于1998年两次对我院药房的分装片剂进行了调查分析。1　调查11　材料与方法:分层随机抽样法,调查本院西药房的分装片剂,即在一年中选择有代表性的两个时间段,然后分别从其中随机抽取某一时刻的分装片剂为样品,进行普查。12　分装片剂质量变化评定主要从外观等物理指标评定,即凡有变色、粘片、发霉、松片、潮解等,定为质量变化。2　调查结果第一次,1998年7月10日,室温28℃,…     

口服补液盐稳定性实验

以恒温恒湿加速实验研究了温度与湿度对口服补液盐（ＯＲＳ）散剂稳定性影响，结果揭示ＯＲＳ稳定性受温度、湿度影响显著。ＯＲＳ变色速度快于ＯＲＳ中葡萄糖分解速度。     

克霉唑乳膏成分检测及稳定性分析

目的:探讨克霉唑乳膏不同贮存条件下主成分的稳定性.方法:通过HPLC法检测克霉唑乳膏不同贮存条件下存放不同时间段主成分克霉唑的含量,并对结果进行分析比较.结果:克霉唑乳膏的贮存温度超出标准温度越高,含量下降越快,贮存时间越长,下降越多.结论:贮存条件会对克霉唑乳膏的稳定性产生影响,存放温度越高,主成分分解下降速度越快.     

氟罗沙星注射液与维生素C配伍的稳定性

目的研究在不同温度(25℃、38℃)条件下,氟罗沙星注射液与维生素C注射液配伍的稳定性.方法用紫外分光光度法测定供试液中氟罗沙星和维生素C的含量,并观察外观、pH值的变化.结果配伍液在两种温度下外观、pH值、紫外吸收图谱无显著变化.两药含量呈下降趋势,温度越高含量下降越快,特别是维生素C在38℃下2 h含量已降至95%.结论可以配伍使用.     

盐酸氟安定片剂的研究

盐酸氟安定(Flurazepam Hydrochlo-ride)是一种较好的镇静催眠药。由于该药对光、热、湿的稳定性较差,目前市售仅有胶囊剂型,尚未见片剂。为提高其稳定性,便于片剂生产,选择了最佳片剂处方及制备工艺;测定了主药含量均匀度、药物溶出速率;预测了稳定性,并测定了室温放置二年的含量变化。     

温度、溶媒及稳定剂对过氧乙酸稳定性的影响

目的:观察温度、溶媒及稳定剂对过氧乙酸稳定性的影响.方法:测定过氧乙酸在不同温度,不同电导率的水(自来水、纯净水、蒸馏水)作为稀释溶媒,及用不同稳定剂(3 g·L-1枸椽酸、2 g·L-1水杨酸、2.5 g·L-1苯甲酸、70%乙醇、4 g·L-1磷酸)时的含量变化.结果:稀过氧乙酸比浓过氧乙酸更易分解,且贮存温度越高,分解越快.用不同电导率的水(自来水、纯净水、蒸馏水)稀释后,其下降速度常数k值分别为1.690,1.009,0.630.分别加入5种稳定剂后过氧乙酸的下降速度常数分别为0.132,0.139,0.147,0.176,0.165.结论:过氧乙酸溶液应贮存在阴凉处,以减少其分解.稀释溶媒的电导率越大,分解越快.5种稳定剂对过氧乙酸稳定性结果为枸椽酸＞水杨酸＞苯甲酸＞磷酸＞乙醇.     

The effect of moisture content on the energies involved in the compaction of ibuprofen

The influence of moisture content and compression speed on the ejection force, plastic and elastic energies of ibuprofen was measured. It was found that moisture can significantly reduce the force required to initiate ejection by the breaking of tablet/die-wall adhesions. At all compression speeds, an increase in moisture content resulted in a marked reduction in the ejection force of ibuprofen compacts. The plastic energy was found to increase with moisture content up to 2.5% w/w, ascribed to an increase in particle-particle interactions. Subsequent decrease in plastic energy at higher moisture contents was probably due to a decrease in particle interaction due to the moisture separation of the particles of ibuprofen. The elastic energy was found to decrease with increasing moisture content up to about 2.5% w/w. This is believed to be due to the strong bonding of particles, brought about by moisture facilitating the formation of interparticle hydrogen bonding and so reducing the interparticle separation. Subsequent increase of elastic energy with increasing amount of moisture beyond 2.5% w/w was thought to be due to the formation of multilayers of water at the surfaces of the particles. This excess moisture increased the elastic energy, by decreasing particle-particle interaction.     

Impact of Different Elastomer Formulations on Moisture Permeation through Stoppers Used for Lyophilized Products Stored under Humid Conditions

The purpose of this study was to evaluate the effect of moisture permeability of different elastomer formulation stoppers, which had different moisture absorption abilities, on the increase of moisture content inside lyophilized vials during long-term storage under humid conditions. Two different elastomer formulation stoppers (high-moisture and low-moisture uptake stoppers) were compared. The increased amount of moisture content inside lyophilized vials fitted with high-moisture stoppers was higher than those fitted with low-moisture stoppers during the early stage of storage. However, this trend was reversed during the later stage of storage. Our data show that the moisture increase inside the lyophilized vials at the early stage was caused by moisture transfer from the stoppers, whereas the later moisture increase was caused by external moisture permeation through the stoppers. Results indicate that the difference in the moisture uptake profile inside the lyophilized vials at each period of storage was caused by the moisture absorption ability and moisture permeation ability of the two elastomer formulation stoppers. In terms of long-term storage stability under humid conditions, our data indicate that external moisture permeating through the stopper into the lyophilized vial during the late stage was the more important factor. In addition, the increase in moisture content at the early stage was controlled by stopper drying time. Furthermore, stopper drying time did not have an effect on moisture permeation at the late stage. Moisture permeation during the storage period appears to be dependent on the different elastomer formulations of the stoppers. The moisture permeation of different elastomer stoppers was an important factor in terms of the increased moisture content inside the lyophilized vials during the late stage of long-term storage under humid conditions. For lyophilized products stored at room temperature, the moisture permeation ability of the stopper is one of the most important factors for long-term storage stability.     

番泻叶提取物的吸湿性及辅料对其影响的研究

目的:研究番泻叶提取物的吸湿性,探讨辅料对番泻叶提取物吸湿性的影响。方法:采用粉末吸湿法,测定样品的吸湿率;以平均吸湿速度、吸湿加速度、吸湿初速度、临界相对湿度等吸湿参数为指标,考察番泻叶提取物的吸湿性及辅料对其的影响。结果:辅料均不同程度地降低了番泻叶提取物的平均吸湿速度,其中乳糖的作用最强;但乳糖对番泻叶提取物的临界相对湿度几乎没有影响。结论:辅料的合理使用可以改善番泻叶提取物的吸湿性。     

药用全蝎含水量、含盐量的测定

目的:对市售全蝎含水量、含盐量进行测定.方法:用烘干法测定全蝎含水量和银量法测定全蝎含盐量.结果:市售全蝎含水量、含盐量最高分别这40.16%、38.75%.结论:建议<中国药典>增加全蝎的含水量、含盐量限度标准,以确保全蝎的质量.     

Determination of fluidized bed granulation end point using near-infrared spectroscopy and phenomenological analysis

Simultaneous real-time monitoring of particle size and moisture content by near-infrared spectroscopy through a window into the bed of a fluidized bed granulator is used to determine the granulation end point. The moisture content and particle size determined by the near-infrared monitor correlates well with off-line moisture content and particle size measurements. The measured particle size is modeled using a population balance approach, and the moisture content is shown to follow accepted models during drying. Given a known formulation, with predefined parameters for peak moisture content, final moisture content, and final granule size, the near-infrared monitoring system can be used to control a fluidized bed granulation by determining when binder addition should be stopped and when drying of the granules is complete.     

Moisture sorption behavior of selected bulking agents used in lyophilized products

To develop a rational approach for the formulation of lyophilized products, six bulking agents commonly used in freeze-dried formulations were lyophilized under identical conditions, and their moisture sorption behavior, before and after lyophilization, were determined as a function of relative humidity at 25 degrees C. The bulking agents evaluated were mannitol, anhydrous lactose, sucrose, D(+)-trehalose, dextran 40 and povidone (PVP K24). The materials were also characterized for their crystal and thermal properties by powder X-ray diffraction, DSC and TG after exposure to various relative humidity conditions. Mannitol was crystalline and non-hygroscopic both before and after lyophilization with total moisture contents of 0.1 to 0.3% w/w between 10 and 60% RH. Anhydrous lactose, sucrose and trehalose were crystalline prior to lyophilization with moisture contents of 0.86, 0.15 and 9.2%, respectively, and the crystalline materials were relatively non-hygroscopic. Upon lyophilization, they converted to the amorphous form and had moisture contents of 1.6, 2.5 and 1.2%, respectively. The amorphous materials sorbed moisture rapidly upon exposure to increasing relative humidity conditions. The amorphous lactose converted to its crystalline hydrate form at 55% RH after sorption of an additional 10% moisture. This conversion to the crystalline hydrate form was accompanied by desorption of practically all the moisture sorbed by the amorphous form. Similarly, lyophilized sucrose converted to its crystalline form after the sorption of additional 4.5% moisture at 50% RH, and the lyophilized trehalose sorbed additional 10% moisture prior to its conversion to a crystalline hydrate form at 50% RH. Dextran and povidone were amorphous and hygroscopic both before and after lyophilization and they sorbed as much as 10-20% moisture at 50% RH. It is well established that different drugs, especially proteins, need different levels of moisture for optimal stability. The results of the present study show that moisture contents of lyophilized cakes may be varied and optimized by the selection of suitable excipients.     

Moisture sorption profiles and tensile strength of tableted phenobarbitone formulations

The tensile strength of tablets made from phenobarbitone and sodium phenobarbitone formulations after storage at increasing ambient relative humidity has been investigated. The moisture sorption and desorption profiles of the formulations were analysed for three locations of moisture: monolayer adsorbed moisture, normally condensed moisture and absorbed moisture. Maxima in tensile strength occur at moisture distributions determined by the disintegrant used. The changes in tensile strength have been explained in terms of changes produced in the interparticle separation, the range of the interparticle forces and changes in the ratio of the binding to diffusional forces, acting on the water molecules which are on the particles' surface.     

Analysis of moisture sorption hysteresis in hard gelatin capsules,maize starch,and maize starch: drug powder mixtures

Moisture sorption and desorption isotherms at 25°C for hard gelatin capsules, maize starch and 50:50 mixes of maize starch: barbitone and maize starch: sodium barbitone have been measured. The sorption hysteresis observed in all four systems studied has been analysed according to the hypothesis of Young & Nelson (1967a) which distinguishes three locations for moisture—monolayer adsorbed moisture, normally condensed moisture and absorbed moisture. Hysteresis is explained by a separation of absorption and desorption isotherms for absorbed moisture and different patterns of moisture distribution are demonstrated in the four systems examined.     

The Effect of Moisture on the Heckel and Energy Analysis of Hydroxypropylmethylcellulose 2208 (HPMC K4M)

The influence of moisture content on the Heckel analysis, energy analysis and strain-rate sensivity of hydroxyproplymethylcellulose 2208 (HPMC K4M) has been evaluated. An increase in moisture content from 0 to 14.9% w/w decreased the mean yield pressure, probably due to a plasticizing effect of moisture which reduced the resistance of particles to deformation. For each moisture content (0, 2.2, 3.8, 5.9, 9.6 and 14.9% w/w), the initial relative density and the extrapolated density from the linear portion of the Heckel plot, tended to decrease with increasing compression speed. Minor changes were observed in the initial relative density due to changes in the moisture content. The strain-rate sensitivity increased from 21.6 to 50.7% as the moisture content increased from 0 to 14.9% w/w, indicating that the plasticity of HPMC increased with increase in moisture content, whereas increase in moisture content from 0 to 14.9% w/w decreased the plastic energy. Increase in compression force or speed of compaction increased both the plastic and elastic energies. An increase in moisture content from 0 to 5.9% w/w slightly reduced the elastic energy but above 5.9% moisture content the elastic energy was unaffected by the moisture content.