新型直压辅料的粉体学性质评价

目的:考察新型直压辅料的粉体学性质,为粉末直接压片技术中辅料的筛选提供参考。方法:以新型直压辅料的粒径分布、吸湿性、润湿性、流动性、可压性和润滑敏感度等为考察指标,初步评价7种新型直压辅料(直压型微晶纤维素AvicelPH101、AvicelPH102,喷雾干燥乳糖FastFlo316、Flowlac100,预混辅料LubriToseSD、Cellactose80,预胶化淀粉)的粉体学性质、稀释潜力及在粉末直接压片中的应用情况。结果:Cellactose80的粒径分布、流动性较好,抗张强度最大;Flowlac100的流动性最大;FastFlo316的流动性大,吸湿性小,润滑敏感度低,但出片力大;AvicelPH101、AvicelPH102可压性好,流动性不及喷雾干燥乳糖,且润滑敏感度高,不宜单独作为直接压片的辅料;LubriToseSD具有极好的流动性、可压性以及较好的自润滑能力;预胶化淀粉可压性较差,但流动性好,适合于黏性大、崩解时间长的物料的压片。结论:新型直压辅料具有很好的流动性和可压性,扩大了粉末直接压片辅料筛选范围,增加了粉末直接压片技术应用的可行性。     

乳糖粉体学性质的初步探讨

测定5种型号乳糖产品的粒度分布、松密度、摇实密度、休止角、流速及成形性，确定何种乳糖适合用作直接压片辅料。以双氯芬酸钾为模型药物，用各型号乳糖为填充剂直接压片，制得双氯芬酸钾片，测定所得片子的硬度、脆碎度和片重差异。结果显示：粒度以GranuLac200最细，其他几种差不多；流动性以GranuLac200最差，GranuLac70次之，其他三种相关不大，成形性以Cellactosc 80最好，Tablettose70次之，CapsuLac80最差。综合各项粉体学性质，Cellactose80和Tablettose70较适合用作直接压片的辅料。用以上各型号乳糖作填充剂直接压片制得双氯芬酸钾片，其压片结果与上述测定结果基本相符，显示粉体学指标的测定对辅料的选择确有一定的指导作用。     

药用辅料学教学方法探索

药用辅料学是中药学、药学、制药工程、药物制剂等相关专业的专业课,对于学生学习和掌握药物辅料起着重要作用。经过7年的教学实践,根据学科发展和药学人才培养的趋势,结合这门课程自身的特点,需要不断进行教学方法的探索,加强应用性、实用性研究,达到有效提高教学质量的目的,以取得良好的教学效果。     

乳糖粉体学性质的初步探讨

测定5种型号乳糖产品的粒度分布、松密度、摇实密度、休止角、流速及成形性,确定何种乳糖适合用作直接压片辅料.以双氯芬酸钾为模型药物,用各型号乳糖为填充剂直接压片,制得双氯芬酸钾片,测定所得片子的硬度、脆碎度和片重差异.结果显示:粒度以GranuLac 200最细,其他几种差不多;流动性以GranuLac 200最差,GranuLac 70次之,其他三种相差不大,成形性以Cellactosc 80最好,Tablettose 70次之,CapsuLac 80最差.综合各项粉体学性质,Cellactose 80和Tablettose 70较适合用作直接压片的辅料.用以上各型号乳糖作填充剂直接压片制得双氯芬酸钾片,其压片结果与上述测定结果基本相符,显示粉体学指标的测定对辅料的选择确有一定的指导作用.     

乳糖粉体学性质的初步探讨

测定 5种型号乳糖产品的粒度分布、松密度、摇实密度、休止角、流速及成形性 ,确定何种乳糖适合用作直接压片辅料。以双氯芬酸钾为模型药物 ,用各型号乳糖为填充剂直接压片 ,制得双氯芬酸钾片 ,测定所得片子的硬度、脆碎度和片重差异。结果显示 :粒度以GranuLac 2 0 0最细 ,其他几种差不多 ;流动性以GranuLac 2 0 0最差 ,GranuLac 70次之 ,其他三种相差不大 ,成形性以Cellactosc 80最好 ,Tablettose70次之 ,CapsuLac 80最差。综合各项粉体学性质 ,Cellactose80和Tablettose 70较适合用作直接压片的辅料。用以上各型号乳糖作填充剂直接压片制得双氯芬酸钾片 ,其压片结果与上述测定结果基本相符 ,显示粉体学指标的测定对辅料的选择确有一定的指导作用     

填充剂对环孢素A固体分散体颗粒粉体学性质的影响

环孢素A(cyclosporin A,1)是由11个氨基酸组成的亲脂性环状多肽,难溶于水,口服生物利用度低.Gelucire 50/13(聚乙二醇脂肪酸甘油酯)为一种亲水性的载体材料,与1制成固体分散体后,45min体外累积释放率较原药提高了7倍,但其本身熔点较低,流动性欠佳.     

预混辅料直接压片的性质考察

目的考察几种预混辅料的性质。方法以粒度分布、休止角、堆密度为指标,考察预混辅料的粉体学性质,并将预混辅料应用于粉末直接压片工艺中。结果与普通辅料淀粉、微晶纤维素相比,预混辅料直压淀粉、直压微晶纤维素的休止角、压缩度小,流动性好。结论预混辅料的粉体学性质优于普通辅料,且粉末直接压片法所得片剂质量良好。     

超微粉碎对牡蛎壳粉体学性质和溶出度的影响

目的:考察超微粉碎对牡蛎壳粉体学性质和溶出度的影响,为牡蛎壳综合开发利用提供实验依据。方法:牡蛎壳以粉碎机制备成普通粉,再将普通粉以超微粉碎机制备成微粉Ⅰ(粉碎5 min)和微粉Ⅱ(粉碎10 min)。从粉体粒径分布、比表面积、孔隙度、休止角、堆密度、吸湿率等方面考察牡蛎壳超微粉碎前后的粉体学差异,采用扫描电镜、傅里叶变换红外光谱(FTIR)和X射线衍射(XRD)等分析其形态特征和化学结构的变化情况,并考察其溶出度。结果:与普通粉比较,微粉Ⅰ和微粉Ⅱ粒径小且分布均匀,但粒子易黏附聚集,比表面积、孔隙度及休止角增大,堆密度减少,吸湿性增强;FTIR和XRD图谱显示牡蛎壳超微粉碎后化学结构无明显变化。微粉Ⅱ和微粉Ⅰ在10 min时溶出度分别为18.5%和10.3%,普通粉在60 min时溶出度只有6.4%。结论:与普通粉比较,牡蛎壳超微粉碎后的粉体学性质呈现出明显差异,粉体溶出度增加,化学结构未发生明显变化。     

几种常用崩解剂的理化性能和应用效果

目的考察市面常用崩解剂的理化性能和应用效果。方法采用显微镜观察崩解剂的微观形态,采用马尔文激光粒度仪测定粒径及分布;以吸水膨胀为评价指标,研究其吸水性、流动性和可压性;以磷酸氢钙为模型药物,研究崩解剂种类和用量对崩解时间的影响。结果低取代羟丙基纤维素为长纤维状粉末,粒径范围广,相对而言流动性较差,可压性较好,具有较大的表面积,使片剂易于成型,加大片剂崩解后的分散度;羧甲基淀粉钠为类椭球状粉末,粒径分布较均匀,吸水性和流动性很好,能够显著加快片剂的崩解。结论在选择崩解剂时,不仅要考虑崩解剂的种类,还要选择崩解剂的型号、用量、来源。     

直接压片辅料LubriTose AN的粉体学评价

本文考察评价了LubriTose AN的粉体学性能,为其进行直接压片工艺提供初步的理论基础。从流动性、可压性、润滑性及稀释能力等角度考察,测定了LubriTose AN粉体的休止角、卡氏指数、流出速度、抗张强度、弹性复原率、屈服压力和出片力等指标,并选择模型药物考察了LubriTose AN的稀释潜能,评价了其在粉末直接压片工艺中的应用。LubriTose AN的流动性要优于其相应的物理混合物。LubriTose AN和无水乳糖具有相同的形变机制,主要是脆性形变。在中低压力条件下LubriTose AN的可压性和压实性要优于物理混合物。LubriTose AN对大部分疏水性药物的稀释潜能良好。LubriTose AN具有良好的润滑能力。结果表明,LubriTose AN是一种优良的预混辅料,对促进和提高片剂的粉末直压工艺有重要意义。     

微粉硅胶在制剂中作为粉末抗静电剂的探讨性研究

目的探讨微粉硅胶作为粉末抗静电剂在制备微粒中的应用。方法使用流化床制备微粒时会遇到粉末静电吸附现象,严重影响制粒过程,针对该问题,本实验采用PVC粉作为实验模型药物,用接触式静电探头法测定在加入微粉硅胶前后的粉末静电电量和表面电阻率。结果在加入质量分数为0.8%微粉硅胶后,静电电量与表面电阻率明显降低,粉末静电吸附现象消失。结论适量的微粉硅胶对粉末静电有明显的消除作用,对流化床制备微粒有着重要意义。     

制剂企业药用辅料内控质量标准的研究

药用辅料是药物制剂的重要组成成分,药用辅料质量与成品质量息息相关,本文结合国内外药典收载情况及作者自己工作经验,浅谈药用辅料内控质量标准的制定,为药品制剂企业药用辅料内控质量标准的建立提供参考。     

Study of talcs as antisticking agents in the production of tablets

Talc is defined as a crystalline structure characteristic of lamellar structures. Antisticking power varies according to the talc considered. Besides chemical properties, it is necessary to assess physical properties related to functionality. It is difficult to define the physical properties of talc implicated in its antisticking power. In this work, we characterized different talcs and then evaluated their performances in reducing sticking in tablet manufacturing. We compared talcs before and after delamination which is a way to obtain talcs with different physical characteristics. Granulometric analysis was carried out by laser diffractometry using a method which made it possible to assess the mean thickness of the lamellar particles. We defined a functionality assay on a single punch press to assess the antisticking power of talcs. The different talcs tested possess a very variable antisticking power towards Avicel PH 102. They present different basal dimensions and particle thickness. The force necessary to detach tablets from the punch surface varies according to the functioning time of the tablet machine, the percentage of talc and the basal dimension of talc.     

Relation between structural characteristics of talc and its properties as an antisticking agent in the production of tablets

Antisticking power varies according to the talc considered. Besides its chemical properties, it is necessary to assess its physical properties related to functionality. It is difficult to define the physical properties of talc implicated in its antisticking power. In this work, different talcs were characterised and their performance in reducing sticking in tablet manufacturing was evaluated. The following parameters were studied: apparent density, morphogranulometry, roughness, and the specific surface through the adsorption–desorption of argon. Next, the relationship between the characteristics of talcs and their antisticking power was considered. Talc before and after delamination—which is a way to obtain talcs with different physical characteristics—was compared. Antisticking power appeared to be dependent on the basal dimensions of talc, and on the ratio value of the external specific surface measured by diffractometry to the total specific surface by the BET method. Models to express the effect of textural factors of talc particles on antisticking power were defined.     

基于多元数据分析的固体分散体粉体学性质及其与重结晶过程中相对结晶度的相关性研究

目的 研究固体分散体(solid dispersion,SD)粉体学性质与SD重结晶过程中相对结晶度(relative crystallinity,RC)的相关性。方法 以穿心莲内酯作为模型药,聚乙烯吡咯烷酮、聚乙二醇8000、泊洛沙姆188、Soluplus^®为载体材料,采用3种制备工艺获得了12种穿心莲内酯SD粉体,测定了SD的粉体学性质,并通过主成分分析法、偏最小二乘法等数据分析手段,研究SD粉体学性质与SD重结晶过程中RC的相关性。结果 通过偏最小二乘法成功建立了SD粉体学性质与RC之间的相关性模型。其中,粒径参数D(0.5)的VIP值>1.2,说明SD粉体学性质中粉体粒径是影响SD重结晶的关键因素。结论 在实际工作中,可以通过不同的制备方法,或者通过调整选定制备方法的工艺参数,获得具有不同粒径参数的SD粉体,以提高SD的重结晶稳定性。     

药用辅料中人工合成着色剂的标准体系现状分析

对药用辅料中人工合成着色剂的标准体系现状进行梳理,对存在问题进行分析,为加强药用辅料中人工合成着色剂监管提供技术参考。通过对人工合成着色剂产品标准的颁布年限、发布部门、标准范围、重金属等有害物质的控制情况进行比较,结合现行的法律法规体系,分析人工合成着色剂作为药用辅料在实际监管工作中存在的问题。建设药用辅料中人工合成着色剂标准体系,对科学监管具有重要的现实意义。     

Theoretical and Experimental Evaluation of Flow Pattern of Pharmaceutical Powder Blends Discharged From Intermediate Bulk Containers (IBCs)

The purpose of this study is to assess the prevalence of funnel flow pattern for common pharmaceutical powder blends, upon discharging from modern intermediate bulk containers (IBCs) in drug product manufacturing. The estimation was built upon Jenike’s original radial stress field theory. It was modified to account for the stress-dependence of wall friction angle commonly observed in pharmaceutical powders. A total of 260 flow pattern estimations, based on 20 real-life IBCs and 13 investigational powder blends, were made. The estimated results showed that the mass flow pattern is present in less than 5% of all cases. Funnel flow pattern is clearly prevalent among pharmaceutical powder blends. The prevalence of funnel flow stems from several factors: 1) relatively shallow hopper section shared by all IBCs, 2) the common transition-type geometry, leading to even shallower hopper inclination at the edge of the hopper section, and 3) relatively high wall friction angles resulting from low wall normal stresses. This conclusion was verified through at-scale experiments, by discharging multiple pharmaceutical powder blends from a representative IBC. In general, our study suggests that, unless the powder wall friction can be substantially reduced, pharmaceutical powders are likely to discharge under funnel flow from modern IBCs.     

冰硼散合蒙脱石散佐治小儿疱疹性咽峡炎95例临床观察

目的 观察冰硼散合蒙脱石散佐治小儿疱疹性咽峡炎的临床疗效。方法 将190例疱疹性咽峡炎患儿随机分为2组,对照组95例采用利巴韦林治疗,治疗组95例在利巴韦林治疗的基础上,予冰硼散和蒙脱石1∶1的混合剂外敷咽部疱疹、溃疡处,早、中、晚各1次,观察热退、咽痛流涎、疱疹溃疡愈合时间及临床疗效。结果 在利巴韦林治疗基础上,加用冰硼散合蒙脱石散治疗小儿疱疹性咽峡炎疗效较好,可迅速缓解症状,缩短病程,减少患儿痛苦,且未发现明显不良反应。结论 冰硼散合蒙脱石散佐治小儿疱疹性咽峡炎临床疗效显著,不良反应少。     

The Wall Friction Properties of Pharmaceutical Powders,Blends, and Granulations

Data from wall friction testing and physical property characterization of over 100 pharmaceutical powders, blends, and granulations have been analyzed. The analyses focused on data for stainless steel surfaces with the most common finishes for pharmaceutical powder processing equipment, either a 2B cold rolled mill finish or an electropolished 2B surface. Active pharmaceutical ingredients exhibited the highest friction against these surfaces, whereas active granulations exhibited the least friction. The typical (median) wall friction angle for an active blend on 2B stainless steel was 22° versus 18° for an active granulation. Typical wall friction values on electropolished 2B surfaces were about 17° and 12° for active blends and granulations, respectively. Blends typically exhibited larger wall friction angles than the granulations suggesting that simple blends will usually require hoppers or bins with steeper walls to achieve mass flow. Lower wall friction angles were consistently observed against the smoother electropolished 2B surface, and, thus, the wall surface finish should be considered when designing bins and hoppers for use with pharmaceutical powders. The wall friction angles of blends and granulations did not show any definite trend as the percentage of active pharmaceutical ingredient increased.     

精制橄榄油细菌内毒素检查的可行性研究

目的对精制橄榄油进行凝胶法干扰试验,建立精制橄榄油细菌内毒素的检查方法。方法按2010年版《中国药典》(二部)"细菌内毒素检查法",用不同厂家的鲎试剂对不同批号的精制橄榄油分别进行干扰试验。结果精制橄榄油稀释至浓度83.4mg/mL或以下稀释浓度的溶液对细菌内毒素检查法无干扰作用。结论精制橄榄油注射液进行细菌内毒素检查是可行的。