球晶造粒法制备硝苯地平缓释微球

目的考察硝苯地平缓释微球的制备工艺及其体外释放度。方法以邻苯二甲酸羟丙甲纤维素酯(HP55)为载体材料,采用球晶造粒技术制备硝苯地平缓释微球。考察硝苯地平微球的粒径、形态、载药量、包封率及体外释放度。结果所得微球外观圆整度好,粒径分布在70~150μm,载药量为18.91%,包封率为94.95%。结论该法可用于硝苯地平缓释微球的制备。     

齐酞酸钠肠溶固体分散剂对免疫性肝炎小鼠模型的保护作用

齐酞酸钠(Oleanolic and 3β-phthalic monoester disodiumsah,OAPES)是对天然药物齐墩果酸(Oleanolicand,OA)进行结构修饰得到的一个新化合物。齐墩果酸是我国20世纪80年代临床上用于治疗急慢性肝炎的五环三萜类化学物，其缺点为溶解性差、生物利用度低。而齐酞酸钠的水溶性和保肝作用比齐墩果酸有显著改善。在病毒感染中，免疫病     

齐酞酸钠肠溶片溶出度研究

对齐墩果酸的前体药物制剂——齐酞酸钠肠溶片的溶出度作了研究，结果表明６０ｍｉｎ内齐酞酸钠溶出９０％以上，Ｔ５０为２０～３０ｍｉｎ，比齐墩果酸有显著改善。溶出速率试验数据用对数正态分布模型进行拟合，获得各溶出参数     

胰岛素肠溶微球口服的实验研究

目的 :研制一种可供口服的胰岛素肠溶微球。方法 :采用相分离法制备胰岛素丙烯酸树脂微球 ;建立放射性免疫法测定微球包封率 ;利用体外实验法考察微球的抗酸及肠溶能力 ;将不同处方的微球给大鼠灌胃 ,测定其血糖变化。结果 :制得微球粒径分布在 2～ 7μm ;包封率 95 .17% ;在人工胃液中 2h有少于 14%的胰岛素释放 ;在人工肠液中 1h内胰岛素的释放度达 96 % ;微球可使大鼠产生明显的降血糖效果。结论 :胰岛素口服肠溶微球是一类具有发展前景的制剂。     

促肝细胞生长素口服肠溶微球的制备

以促肝细胞生长素为多肽大分子模型药物，利用能在结肠ｐＨ值较高的环境下溶解的邻苯二甲酸醋酸纤维素为材料，经优化工艺制备口服结肠释放微球。粒径５～１５μｍ者占总数７７．８％，平均粒径１２．７μｍ，建立了微球中载药量的测定方法，测得为２９．７±２．５％。微球在人工胃液中２ｈ释药未超过１０％，而在ｐＨ７．２的磷酸盐缓冲液中１ｈ释药达９８％。     

喷雾干燥法制备麦冬皂苷肠溶微球的影响因素

以丙烯酸树脂Ⅱ为囊材、微粉硅胶为抗黏剂、蓖麻油为增塑剂、95%乙醇为溶剂,采用喷雾干燥法制得麦冬皂苷肠溶微球.以外观形态、粒径、包封率、释放度等为指标,对进风温度、雾化速度、增塑剂种类、药物与囊材比例、囊材浓度等因素进行考察.结果表明,按优化条件制得的微球表面光滑,平均粒径(20.6±5.2)μm,包封率(94.8±2.7)%,载药量(54.8±2.1) mg/g.在pH 6.8磷酸盐缓冲液中的释放度较好.     

球晶造粒技术制备药用可直压微粒的研究进展

球晶造粒技术使微粒晶型在结晶或反应过程中直接转变为球形聚集体,从而改善微粒的第二性质,如流动性和可压性,使其可以直接用于压片。本文介绍球晶造粒技术制备药用可直压微粒的研究进展情况。     

球晶制粒技术制备水飞蓟宾缓释微球

目的提高水飞蓟宾的生物利用度。方法采用固体分散载体和阻滞性高分子材料,使用固体分散与球晶制粒相结合的技术制备水飞蓟宾缓释微球。运用差示热分析及X-射线粉末衍射检测水飞蓟宾在微球中分散状态,采用扫描电子显微镜观察微球的形态、表面结构和内部结构,并对微球的特性如平均粒径、粒径分布、松密度进行评价。结果研制微球的大小可由搅拌速度来控制,水飞蓟宾从缓释微球中的释放速度随分散剂的量的增加而增加,阻滞剂可延缓药物的释放。微球中药物的释放速度能够通过调节分散剂和阻滞剂的比例来控制。X射线衍射与差示热分析结果表明:水飞蓟宾以无定型高度分散在微球中。在40℃,相对湿度75%条件下,加速三个月,药物释放与含量不会改变。结论水飞蓟宾缓释微球可通过采用固体分散与球晶制粒相结合的技术一步制成。该制备过程简便、重现性好、成本低,是水不溶性药物制备缓释微球的有效方法。     

HPLC指纹图谱对五味子肠溶微球的质量评价

目的:建立五味子肠溶微球HPLC指纹图谱,以此作为该制剂质量评价的指标。方法:采用DIKMA Platisil ODS(4.6mm×250 mm,5μm)色谱柱,流动相为乙腈-水,梯度洗脱(0→20→25→55→70 min,48%→48%→65%→65%→48%乙腈),流速0.8 mL.min-1,二极管阵列检测器(DAD),检测波长254 nm,柱温40℃,进样量40μL。以五味子醇甲为参照物建立五味子肠溶微球的HPLC指纹图谱。结果:图谱中有21个共有峰,确定为其指纹峰。采用国家药典委员会中药色谱指纹图谱相似度评价系统(2004A版)自动处理,10批样品的相似度均大于0.99。结论:该方法简便、稳定,重现性好,适于作为五味子肠溶微球质量评价的指标。     

齐酞酸钠固体分散物的制备和体外溶出度研究

目的采用固体分散技术提高齐酞酸钠口服制剂的溶出速度和稳定性。方法以肠溶性材料聚丙烯酸树脂Ⅲ为载体,制备药物与载体不同比例的固体分散物及物理混合物,采用X-射线衍射方法、差热分析和红外光谱分析鉴别分散状态,并测定体外溶出速度。结果齐酞酸钠以无定形态分散在载体中,主要在碱性溶液中溶出,形成肠溶性固体分散物,溶出速率高于物理混合物。结论齐酞酸钠与载体适当比例的肠溶性固体分散物可明显提高体外溶出速率,并可防止药物的水解。     

用球形结晶技术改善甲苯磺丁脲的溶出速率

用球形结晶技术将难溶性药物甲苯磺丁脲在羧甲基纤维素钠(CMC—Na)的溶液中制成球形结晶聚集体(简称球晶)。用扫描电镜法观察到原药结晶为棱状结晶,而球形结晶为小片状及小梭状结晶的聚集体。用粉末X线衍射谱检测了球晶与原晶,发现衍射峰有不同之处,说明有部分晶型发生改变。其球晶的溶解过程由Hixson—Crowll方程式描述,溶解比原药快。     

Preparation of microparticles of naproxen with Eudragit RS and Talc by spherical crystallization technique

Microparticles of naproxen with Eudragit RS and talc were prepared by the spherical crystallization technique, i.e. quasi-emulsion solvent diffusion method. The obtained microparticles were evaluated by micromeritic properties, yield, encapsulation efficiency, drug physical state and dissolution rate of drug. The influence of formulation factors and preparation condition (drug: polymer ratio, talc: polymer ratio, SLS concentration, stirring speed) on the properties of the microparticles were also examined. The resultant microparticles were finely spherical and uniform with high incorporation efficiency and yield. Greater encapsulation efficiency was obtained by increasing the drug: polymer ratio and talc: polymer ratio and by reducing the SLS %. The dissolution rate of naproxen from microparticles was enhanced significantly with increasing the ratio of drug: polymer and stirring rate, and sustained by increasing SLS % in crystallization medium. The results of X-ray diffraction and differential scanning calorimeter analysis indicated that naproxen was highly dispersed in microparticles, so as amorphous state. Studies carried out to characterize the micromeritic properties of formulations, such as flowability and packability showed that microparticles were suitable for further pharmaceutical manipulation (e.g. capsule filling). Hence, the spherical crystallization technique can be successfully used for obtaining spherical microparticles, generating a heterogeneous matrix system and providing sustained drug release.     

Enhanced dissolution rate of simvastatin using spherical crystallization technique

Simvastatin is a hypocholestrolemic drug that is insoluble in water. Its low water solubility rate limits the pharmacological effects. The aim of this study was to improve the dissolution rate of simvastatin using spherical crystallization method. The drug was dissolved in boiling dichloromethane as the good solvent. This solution was added to 5°C water as the non-solvent. After sedimentation, isopropyl acetate was added as the bridging solvent. At the end the crystals were collected and dried for 12?h in a 50°C oven. The FTIR and DSC results showed no change in the drug after crystallization process. XRPD studies showed the sharp peaks are present in the diffractograms of spherical crystals with minor reduction in height of the peaks. The particle size of spherical aggregates was about 37 μm and the dissolution efficiency of simvastatin up to 60?min increased to about 2-fold in phosphate buffer solution containing 0.5% sodium dodecyl sulfate (pH 7) using the rotating paddle method. Spherical crystals showed enhanced solubility than untreated powder possibly due to partial conversion to amorphous form. Their dissolution rate at 60?min was still 4-fold of untreated powder when stored at 25°C and 84% relative humidity for one month.     

球晶造粒技术制备可直压乙基纤维素及适应性研究

目的 评价进口、国产乙基纤维素(EC)及球晶技术自制EC聚集体对药物的适应性.方法 分别以阿司匹林含量为10%～90%与进口、国产乙基纤维素(EC)及自制EC聚集体混合后直接压片,测定混合物粉体学性质如休止角,流出速度,卡氏指数及压片后的片重差异、脆碎度、硬度,以考察聚集体对药物的稀释潜力.结果 与国产及进口乙基纤...     

球晶技术制备可直压乙基纤维素的粉体学性能评价

目的:评价进口、国产乙基纤维素(EC)及球晶技术自制EC聚集体的粉体学性能。方法:分别测定3种EC的表面形态、粒度分布、休止角、卡氏指数、川北方程、Heckel方程参数等各项粉体学性能及与药物压片后的各项指标。结果:自制聚集体呈球形,表面光滑,休止角最小,川北方程及Heckel方程均显示其有最好的填充性和可压性,制备后片剂各项指标均优良。结论:球晶造粒技术通过改变国产辅料的形态、孔隙率、松密度等各项物理性质而改善流动性及填充性,性能优于进口辅料,操作设备、工艺简单。     

高效液相色谱法测定三两半药酒中齐墩果酸的含量

目的：建立三两半药酒中齐墩果酸含量,测定方法。方法：HPLC法,以Hypersil(4.6*250mm,5um)为色谱柱,甲醇－水（90：10）为流动相,检测波长为220nm。结果：齐墩果酸测定线性范围为9.6-48.0ug/ml(r=0.9998),平均回收率为98．5％,结论：该法简便,可用于测定三两半药酒中齐墩果酸的含量。     

吲达帕胺肠溶微球的制备及影响因素考察

目的制备吲达帕胺肠溶微球及影响因素考察。方法以羟丙甲纤维素酞酸酯(HPMCP)为肠溶载体材料,采用乳化溶剂扩散法制备吲达帕胺肠溶微球,对影响微球的成型性、收率、载药量、包封率及其释药性能等因素进行了考察。结果微球形态圆整,架桥剂和乳化剂是其成型主要影响因素;载药量14.85%,包封率76.30%,药物在模拟肠液中累计释放度符合要求,载体材料用量控制药物释放速度。结论本方法适宜制备吲达帕胺肠溶微球,工艺简单,体外肠溶释放性良好。     

齐酞酸钠在大鼠肠道吸收动力学研究

目的:研究齐酞酸钠(OAHDPS)在大鼠肠道内的吸收特性.方法:采用大鼠在体小肠吸收实验方法,测定OAHDPS在不同剂量(100,50,25μg·mL-1)下结扎和不结扎胆管条件下的小肠吸收量和吸收速率常数(Ke),并比较各个肠段的吸收.结果:研究表明,OAHDPS在肠道内的吸收机制是被动扩散方式,且在小肠的吸收不受胆汁等分泌物的影响;在肠道正常pH值情况下,平均Ke为(0.162±0.012)h-1;各个肠段对OAHDPS均有吸收且Ke无显著差异.结论:在OAHDPS口服剂型设计时应首先考虑肠溶缓释制剂.     

Preparation and in vitro characterization of piroxicam enteric coated pellets using powder layering technique

The objective of this study was to develop piroxicam enteric coated pellets using nonpareil seeds by powder layering technique to minimize its gastrointestinal adverse effects. Inert seeds were prepared by incorporating sugar, Avicel PH 101 and lactose. The obtained cores were then treated by PVP 10 w/v % solution using centrifugal granulator (CF-granulator) and then coated with micronized piroxicam using HPMC solution (8 w/v %) as binder. The piroxicam pellets were finally coated with different polymers (Eudragit L30D-55, Eudragit L100, Eudragit NE30D, Acryleze, or mixture of Eudragits L30D-55 and NE30D) and plasticizers (triethyl citrate and polyethylene glycol 6000). Results showed that Eudragit L30D-55 with 3% weight gain accompanied with TEC produced suitable enteric coated pellets.     

高效液相色谱法测定枇杷叶中熊果酸和齐墩果酸含量

目的建立高效液相色谱法同时测定枇杷叶中熊果酸和齐墩果酸含量.方法Lichrospher C18(250 mm×4.6 mm,5μm)为色谱柱,甲醇水冰醋酸-三乙胺(90100.030.06)为流动相,流速为0.8 mL·min-1,检测波长为215 nm.结果熊果酸、齐墩果酸能达到基线分离(Rs＞1.65),两者在0.4～4.0μg范围内线性关系良好.结论此方法简便、准确、重现性好.