影响片剂脆碎度的因素分析

目的优化片剂脆碎度。方法对生产过程中影响脆碎度的因素进行逐一对比分析。结果与结论生产过程中人员、设备、物料、方法、环境对脆碎度均有影响。     

片剂脆碎度不合格问题的探讨

片剂脆碎度检查法是《中华人民共和国药典》2000年版二部新增订的内容,本法用于检查非包衣片的脆碎情况及其它物理强度,如压碎强度等。片剂脆碎度检查法执行起来在生产中遇到了许多困难,本文对可能造成片剂脆碎度不合格的诸多因素及解决办法进行了探讨。1 影响因素1.1 主药的影响主药的性状、理化性质,如晶型、结晶水、粘度等及主药的稳定性对片剂的脆碎度有较大影响,但其     

优化去痛片脆碎度工艺的研究

目的:研究去痛片脆碎度的工艺优化问题。方法:采用正交实验的方法进行实验。结果:找出生产工艺的最佳参数。结论:粘合剂的用量和浓度、喷浆速度、原料细度均是影响去痛片脆碎度的重要因素。     

完善依苏工艺优化脆碎度的研究

马来酸依那普利片 (依苏 5mg、10mg)对治疗心血管病、血压、血脂过高有良好的治疗效果。因其独特的疗效和优良的质量 ,在市场上一直十分畅销。脆碎度是衡量片剂质量的重要指标。为了满足市场的需求 ,本着降低成本、保证产品质量、增加市场竞争力 ,寻找最佳生产工艺流程 ,优化其脆碎度。本文研究了依苏脆碎度的影响因素 ,获得了理想的效果。仪器与药品脆碎度测定仪 (WG - 2 0 0 2 -XB) ;马来酸依那普利 :符合WS - 335 (X - 2 5 9) - 93马来酸依那普利项下的规定 ;淀粉 :符合《中国药典》 2 0 0 0年版二部(P780 )淀粉项下的规定 ;乳糖 :符…     

对乙酰氨基酚片脆碎度的研究

目的研究解决对乙酰氨基酚片的脆碎度问题。方法以脆碎度、崩解度、溶出度为指标,通过处方筛选确定优化的生产工艺。结果预胶化淀粉对对乙酰氨基酚片脆碎度的改善明显优于微晶纤维素、麦芽糊精。结论优化处方的预胶化淀粉能保证对乙酰氨基酚片的脆碎度等相关质量要求。     

优化吡拉西坦片工艺,提高其崩解时限及脆碎度

目的:提高其崩解时限及脆碎度,确保产品质量。方法:通过正交实验,确定影响吡拉西坦片崩解时限及脆碎度的三个因素,即粘合剂的浓度,温度,湿混时间,从而确定最后工艺。选用两种辅料,进口羧甲基淀粉钠和羟丙纤维素进行对比实验,确定最后辅料的使用。通过辅料的添加形式进行对比实验,确定辅料的最后添加形式。结果:通过以上3种方法及相应的措施,来确定是否能提高吡拉西坦片的崩解时限及脆碎度。吡拉西坦片崩解时限提高到7．1min,脆碎度提高到0．148％。结论:添加4％的羟丙纤维素,吡拉西坦片崩解时限及脆碎度数据最好,因此确定辅料的使用为4％的羟丙纤维素。羟丙纤维素内外各加2％效果最好。     

片剂脆碎度——片剂质控的又一重要手段

片剂脆碎度—片剂质控的又一重要手段任重远王平刘铁锁（卫生部药典委员会１０００５０）片剂脆碎度（Ｆｒｉａｂｉｌｉｔｙ）是反映片剂生产工艺水平、控制片剂质量的一项重要指标，直接影响片剂的生产、包装、运输和使用。正确反映和测试片剂脆碎度，对于片剂的生产和科...     

葡萄糖酸钙片脆碎度与产品质量的相关性

目的：考察葡萄糖酸钙片的脆碎度情况。方法：采用《中国药典》2015年版四部片剂脆碎度检查法,对2017年国家药品评价品种葡萄糖酸钙片抽样样品进行测定并判定。结果：涉及16家生产企业的306批样品中,不合格8批,不合格率2.6% ,不合格涉及4家企业。结论：脆碎度可反映非包衣片的质量,建议将其纳入到各论项下作为检查项目。     

正交实验法优选酚氨咖敏片制粒目数

目的优选酚氨咖敏片制粒目数,使之符合生产需要。方法采用正交实验法进行优选。结果采用优选后的制粒目数,可提高酚氨咖敏片脆碎度的合格率。合格率由86%提高为95%。结论优化制粒目数后的酚氨咖敏片,可确保脆碎度稳定且不影响其片重差异,从而保证产品质量。     

关于明胶空心胶囊标准中脆碎度检查的建议

目的:对明胶空心胶囊标准中的脆碎度检查项目提出修改建议。方法:对明胶空心胶囊的脆碎度检查的历版标准(1989～2010年,共5版)内容进行比较、分析并辅以实际试验进行佐证。结果:经比较分析及实际试验操作发现,历版标准中明胶空心胶囊的脆碎度检查存在相对湿度控制不量化、硝酸镁饱和溶液制备无依据、检验器具不明确等方面的不足。结论:建议相关部门重视并最终确定明胶空心胶囊的脆碎度检查的各项条件,使之更具可操作性,使建立的标准发挥应有的指导作用。     

Assessment of Tablet Surface Hardness by Laser Ablation and Its Correlation With the Erosion Tendency of Core Tablets

Surface erosion of uncoated tablets results in processing problems such as dusting and defects during coating and is governed by the strength of particle bonding on tablet surface. In this study, the correlation between dusting tendency of tablets in a coating pan with friability and laser ablation surface hardness was assessed using tablets containing different concentrations of magnesium stearate and tartaric acid. Surface erosion propensity of different batches was evaluated by assessing their dusting tendency in the coating pan. In addition, all tablets were analyzed for crushing strength, friability, modified friability test using baffles in the friability apparatus, and weight loss after laser ablation. Tablets with similar crushing strength showed differences in their surface erosion and dusting tendency when rotated in a coating pan. These differences did not correlate well with tablet crushing strength or friability but did show reasonably good correlation with mass loss after laser ablation. These results suggest that tablet surface mass loss by laser ablation can be used as a minipiloting (small-scale) tool to assess tablet surface properties during early stages of drug product development to assess the risk of potential large-scale manufacturing issues.     

Influence of disintegrant type and proportion on the properties of tablets produced from mixtures of pellets

The influence of the composition and properties of pellets on the properties of the tablets prepared from their mixtures has been evaluated. Three types of pellets were prepared, (a) those containing a model drug readily identifiable by colour, to evaluate tablet consistency; (b) those containing a deformable material, glyceryl monostearate, to provide pressure absorbing and binding properties, and (c) those containing an inorganic disintegrating agent. Tablets from various mixtures of these pellets, in a statistical designed manner, were prepared at a known compression force and their weight uniformity, friability, diametral breaking load and disintegration times were measured. The uniformity of composition of selected tablets was also determined. Analysis of variance established that the disintegrant type, the proportion of drug pellets and the proportion of disintegrant pellets influenced the breaking load and the disintegration time of the tablets. The proportion of drug and disintegrant pellets influenced the tablet friability whereas the type of disintegrant did not. Canonical analysis failed to establish an exact relationship between pellet properties and tablet properties. However some conclusions can be drawn from this analysis. First, an increase in either the amount of drug pellets or disintegrant pellets decreases the tablet breaking load, and the disintegration times are reduced. Secondly, disintegration times are increased with disintegrants of a high density. Thirdly, larger amounts of drug and disintegrant pellets increase the tablet friability.     

Box-Behnken设计-效应面法优选四逆泡腾片干法制粒工艺

目的:优选四逆泡腾片干法制粒工艺。方法:以颗粒得率和颗粒脆碎度为评价指标,以轧轮压力、轧轮转速、浸膏粉含水量为考察因素,采用单因素试验考察各因素对指标的影响程度;采用Box-Behnken设计考察各因素对评价指标总评OD值的影响,并采用效应面法预测、分析、选取最佳工艺。结果:最佳干法制粒工艺为浸膏粉含水量为2.1%,轧轮转速为8.8 Hz,轧轮压力为2.3 MPa。结论:所选工艺稳定、可行、重现性好,可用于四逆泡腾片的制粒。     

格列喹酮片的分剂量评价

目的 评价单面带刻痕的格列喹酮片的分剂量药学特性。方法 分别采用切药器和手工对自研品和参比制剂进行分割,以分割前后质量损失为评价指标,考察自研品和参比制剂的可分割性;取在硬度上限（8 kg）和下限（4 kg）处的自研格列喹酮片分别用切药器分割后,考察分割质量损失;按照《中国药典》2020年版片剂脆碎度检查法研究分割后的片剂脆碎度;参考《欧洲药典》,随机取30片,分割后检测单一半片占半片平均片质量百分比;高效液相色谱法测定格列喹酮整片、半片在pH 8.5磷酸盐缓冲液中的溶出曲线;参照《中国药典》含量均匀度检查法（通则0941）,对切药器分割后的30片自研品进行含量均匀度测定。结果 质量损失结果表明手工分割和切药器分割无显著性差异;硬度上限与下限时片剂分割后的脆碎度和质量损失均符合要求;分割后片剂质量差异、脆碎度和含量均匀度均符合药典要求;自研品与参比制剂的半片溶出行为一致;与整片溶出量相比,分割后的自研品60 min溶出量为51.46%,参比制剂为49.12%。结论 自研品和参比制剂分割后的药学特性相同。     

Practical Limitations of Tableting Indices

The purpose of this study was to utilize tableting indices to distinguish between materials with varying degrees of compactibility by establishing a quantitative relationship between indices and compactibility. Compactibility in this study is restricted to tablet strength and friability alone. Nine mixtures with varying degrees of compactibility were tableted and the tensile strength and friability of the tablets were determined. The tableting indices of these mixtures were determined using an Instron® Universal testing machine. An artificial neural network program was used to establish a quantitative relationship between indices and tablet strength and friability. Six new powders were used to validate the models describing the relationship between indices and tablet strength and friability. These powders were compressed into tablets and their strength and friability were determined. Their indices were also determined. The established models were used to predict tablet strength and friability from index values. The predicted values were compared with the experimentally determined values. There was little correlation between the predicted and experimentally determined values for tablet strength and friability. It was also found that materials or mixtures having almost similar indices had remarkably different compactibilites. It was concluded that models created to predict compactibility using one set of materials may not be able to successfully predict the compactibility of a new material. This calls into question the practicality of indices.     

Practical limitations of tableting indices.

The purpose of this study was to utilize tableting indices to distinguish between materials with varying degrees of compactibility by establishing a quantitative relationship between indices and compactibility. Compactibility in this study is restricted to tablet strength and friability alone. Nine mixtures with varying degrees of compactibility were tableted and the tensile strength and friability of the tablets were determined. The tableting indices of these mixtures were determined using an Instron Universal testing machine. An artificial neural network program was used to establish a quantitative relationship between indices and tablet strength and friability. Six new powders were used to validate the models describing the relationship between indices and tablet strength and friability. These powders were compressed into tablets and their strength and friability were determined. Their indices were also determined. The established models were used to predict tablet strength and friability from index values. The predicted values were compared with the experimentally determined values. There was little correlation between the predicted and experimentally determined values for tablet strength and friability. It was also found that materials or mixtures having almost similar indices had remarkably different compactibilities. It was concluded that models created to predict compactibility using one set of materials may not be able to successfully predict the compactibility of a new material. This calls into question the practicality of indices.     

克拉霉素分散片的处方工艺改进

目的 :研究制备克拉霉素分散片的最佳处方工艺 ,以解决原处方生产的片剂易缺角、烂边的问题。方法 :内加低取代羟丙基纤维素 (LS -HPC) ,通过处方筛选以确定制备处方工艺。结果 :用LS -HPC取代原处方的淀粉较为理想 ,增加了片剂的硬度 ,改善了脆碎度 ,解决了原片剂的缺角、烂边问题。结论 :改进后的处方工艺有利于提高本品的质量     

Formulation and In Vitro Evaluation of Ofloxacin Tablets using Natural Gums as Binders

Natural gums are economical, easily available, and useful as tablet binders. In the present investigation, an attempt was made to formulate Ofloxacin tablets using three natural binders, namely Acacia arabica, Hibiscus esculentus, and xanthan gum. Such six batches of Ofloxacin tablets were prepared by using different types and amounts of the natural binders by the wet granulation method. The tablets were analyzed for their hardness, friability, and weight variation, and in vitro release was performed in a phosphate buffer at pH 6.8. The prepared tablets were also evaluated for their various release kinetics and similarity factors f₂. The physical properties of the tablets containing the natural binders showed sufficient hardness, desirable disintegration time, and low friability. Their better percentage of drug release was observed as compared to the marketed formulation showing more than 85% drug release within 45 minutes. The in vitro release data was well-fitted into zero-order and the values of release exponent ‘n’ were between 0.303 and 0.514. The high similarity factor f₂ of 64.50 was achieved with the best batch in comparison to the marketed tablets. The results obtained indicated that the gum Acacia arabica performed as well as gelatin compared to the other binders for the Ofloxacin tablet formulation.     

聚维酮K30、S630对尼美舒利分散片分散性能的影响

目的:比较2种聚维酮类亲水性黏合剂对尼美舒利分散片分散性能的影响。方法:分别选择聚维酮S630和K30的5%乙醇溶液及5%水溶液作为亲水性黏合剂制备尼美舒利分散片,通过检测各组分散片的脆碎度、硬度和分散性比较二者对分散片性能的影响。结果:从分散片的脆碎度、硬度和分散性等方面考察,聚维酮S630的乙醇溶液或水溶液与K30的乙醇溶液或水溶液比较性能相同甚至在分散性方面前者更好。结论:聚维酮S630可以作为K30的替代物用作分散片的亲水性黏合剂。     

Punch geometry and formulation considerations in reducing tablet friability and their effect on in vitro dissolution.

The tablet friability resulting from formulation variations was studied under controlled granulation moisture content and tablet crushing strength. Tablets made with lactose were more friable than tablets made with microcrystalline cellulose. Replacement of 0.5% magnesium stearate with 0.5% stearic acid in the formula reduced tablet friability, whereas the combination of 0.5% stearic acid and up to 0.25% magnesium stearate did not increase tablet friability, decrease drug dissolution rate, or increase tablet-to-tablet variability in dissolution. Tablets compressed with extra deep concave punches resulted in lower friability compared with tablets compressed with standard concave or deep concave punches. The friabilities of the standard convex and deep convex tablets were similar, indicating that a critical level of punch tip curvature was important in reducing tablet friability. The dissolution rate was not affected by the punch tip geometry, but the tablet-to-tablet dissolution variability at the 0.5% stearic acid level for the extra deep convex tablets was higher compared with the standard convex tablets.