正交试验法筛选口服去氢骆驼蓬毫微粒制备工艺

目的对骆驼蓬毫微粒的制备工艺进行研究,优选最佳制备工艺。方法以可生物将解的聚氰基丙烯酸正丁脂为聚合材料,采用乳化聚合法制备(HM-PBCA-NP),紫外分光光度法测定骆驼蓬含量,L9(34)正交试验设计处方工艺。结果按优化工艺条件,制得载药毫微粒:平均粒径69nm,分布范围28～110nm。结论经过优化筛选的组方工艺制备的骆驼蓬毫微粒粒,为最佳制备工艺。     

肝靶向氧化苦参碱毫微粒制备工艺研究

目的 优选出肝靶向氧化苦参碱毫微粒的制备工艺。方法采用乳化聚合法制备,以毫微粒的包封率作为考察指标,系统观察法筛选出最佳制备工艺。结果 得到的毫微粒粒子均匀圆整,平均粒径100-200nm之间。包封率较高,平均为87.06％。结论 工艺先进可行,可作为生产工艺的参考。     

眼用诺氟沙星毫微粒制备工艺的初选及优化

目的:寻找眼用诺氟沙星毫微粒最佳的处方和制备工艺。方法:选择氰基丙烯酸正丁酯为载体材料,用乳化聚合法制备NFLXPBCANP,通过单因素试验初选、均匀设计优化处方和制备工艺。结果:在优化条件下制备的NFLXPBCANP为乳白色胶体溶液,毫微粒外形圆整光滑、分布均匀、不粘连,平均粒径553nm,包封率90.14%,载药量22.70%。结论:该优化条件可作为眼用诺氟沙星毫微粒最佳的处方和制备工艺。     

草参固金胶囊生产工艺研究

目的:确定草参固金胶囊醇提、成型的最佳工艺.方法:分别以干膏量、总皂苷等为考察指标以正交试验法确定草参固金胶囊的最佳制备工艺.结果:最佳工艺为蝙蝠蛾拟青霉菌粉以净粉量投料,其余西洋参、淫羊藿、绞股蓝用70％乙醇回流提取2次,每次加10倍量溶剂,每次2小时,制成干膏粉备用.蝙蝠蛾拟青霉菌粉与上述干膏粉混合均匀后用70％乙醇制成软材制粒.结论:本法为草参固金胶囊的制备工艺提供实验依据.     

复方杨桃颗粒的成型工艺研究

目的 优选复方杨桃颗粒的成型工艺.方法 以吸湿率、成型率、溶化性因素为考察指标,筛选最佳辅料与配比,确定复方杨桃颗粒的成型工艺.结果 最佳成型工艺条件为:干浸膏:可溶性淀粉:糊精=1:1:0.2,90％乙醇为润湿剂,按照该成型工艺制备3批颗粒并作评价.颗粒的成型率可达80％以上,粒度检查、水分测定和溶化性均符合规定,颗...     

原位聚合法制备脲醛树脂微囊的处方工艺研究

目的 确定制备脲醛树脂微囊的最佳处方和工艺,特别是包括抗微囊粘连效果最佳的抗黏剂和添加剂.方法 采用原位聚合一步法制备微囊,考察系统稳定剂种类及用量、多种抗粘剂及添加剂对成囊过程及囊粒粒径的影响.结果 以1.5％PVA作为系统稳定剂,在pH值为3.5、搅拌速度为700r/min的工艺条件下,制备的微囊粒径均匀、不粘连.反应结束后调节系统pH值为7,加入固化剂间苯二酚和增稠剂黄原胶,具有良好抗粘连效果.结论 系统稳定剂的作用是使芯材形成稳定油滴,促使囊材包覆其表面上,最佳的系统稳定剂可降低囊材自身成核的几率.     

磷酸卡维地洛缓释微丸的制备及生物等效性研究

目的 制备与参比制剂生物等效的磷酸卡维地洛缓释微丸.方法 采用流化床制备磷酸卡维地洛载药微丸,进一步制备缓释微丸,采用正交实验优化处方工艺.结果 载药微丸的最佳处方为:丸芯粒径0.35～0.5 mm,崩解剂用量15％,黏合剂用量10％,增溶剂用量15％;缓释微丸的最佳处方为:包衣增重7％,包衣液浓度50％,致孔剂用量5％,二氧化硅用量10％.结论 自研制剂与参比制剂生物等效.     

滋肝益肾膏制备工艺研究

目的:优选滋肝益肾膏制备工艺的最佳条件参数.方法:以岀膏率为指标,以加水倍数、煎煮时间、提取次数为三因素,用L9(34)正交表进行试验,优选出滋肝益肾膏的最佳工艺参数.结果:经优选的制备工艺条件为加水5 倍,每次煎煮1.5h,提取3次.结论:该制备工艺参数可行,质量符合要求,是制备滋肝益肾膏的最佳工艺.     

草乌甲素可溶性微针的制备、质量评价及体外透皮性能研究

目的 为克服草乌甲素现有给药方式的不足,开展草乌甲素可溶性微针的制备工艺、质量评价及体外透皮性能研究.方法 采用分层浇筑法制备草乌甲素可溶性微针,通过正交法优选最佳处方及制备工艺,并对微针进行质量评价,如微针表观、机械强度、载药量、透皮释放等.结果 草乌甲素可溶性微针的最佳处方及制备工艺为:以35％乙醇溶液作为溶剂,0...     

薄荷油β-环糊精包合物制备工艺的研究

目的:研究薄荷油-β-环糊精包合物的最佳制备工艺.方法:采用单因素实验法和正交试验法,以包合率及收得率测定为评价指标,对影响薄荷油-β-环糊精包合物制备工艺因素进行研究,寻找出最佳制备工艺,并用TLC、红外光谱扫描法对包合物进行验证.结果:最佳的制备工艺为薄荷油与β-环糊精的比例:1∶7;β-环糊精与水的比例:1∶7;搅拌时间75分钟;包合温度40℃.挥发油与β环糊精的比例:1∶7;B环糊精与水的比例:1∶7;搅拌时间75分钟;包合温度40℃,为薄荷油包合物最佳制备条件.结论:优选出来的工艺简便、稳定,包合物产率较高,为薄荷油包合物制备工艺提供了最佳制备条件.     

5-氨基水杨酸pH依赖型控释微丸的制备及质量评价

目的:制备5-氨基水杨酸(美沙拉嗪)pH依赖型控释微丸,考察影响载药丸芯制备和微丸控释的因素.方法:以圆整度、粒度分布和收率、脆碎度和流动性为指标,采用正交设计法筛选丸芯的处方和工艺以及包衣的增重和老化条件.结果:最佳处方工艺为载药量80％、粘合剂用量40mL/100 g、挤出速度30 Hz、滚圆速度30 r·min-1;包衣增重8％,老化条件为60℃、24 h.结论:制备了适合流化床包衣的美沙拉嗪载药丸芯,以尤特奇水分散体包衣得到了pH依赖型控释微丸.     

Formation of size-controlled nano carrier systems by self-assembly

Nano carrier systems were prepared by forming self-assembled liposomes having a size distribution in the nano range through use of an ultrasonic homogenizer. Phosphatidylcholine and cholesterol were utilized as an amphiphilic compound and a shape stabilizer, respectively. The size of prepared samples was decreased (up to 150 nm) by elevating ratio of lecithin and extending homogenization time (2 ～ 6 min). After secondary coating with alginic acid (0.1, 0.3 and 0.5%, W/V), size was remarkably changed in the range of ±30 nm and zeta-potential was altered (only chitosan coating (molecular weight: 30 000 Da, 0.2%, W/V): 10.3 mV, Alginic acid coating (0.5%, W/V) after the chitosan coating: ?21.8 mV). The low molecular weight chitosan (0.1%, W/V)-coated nano-liposomes had a lower absolute value of zeta-potential than the high molecular weight chitosan (0.1%, W/V)-coated nano-liposomes. The encapsulation efficiency was measured by gas chromatography. The efficiency was decreased slightly by elevating chitosan concentration (0.1 ～ 0.5%, W/V).     

盐酸罗沙替丁醋酸酯脉冲控释微丸的研制

目的:制备盐酸罗沙替丁脉冲控释微丸(ROXPCP)。方法:取空白丸芯分别以含药层、溶胀层(含交联羧甲基纤维素钠)和控释层(含乙基纤维素水分散体)顺序包衣制备ROXPCP,通过考察不同类型空白丸芯、溶胀层材料及溶胀层与控释层的不同包衣增重对药物释放的影响来优选工艺,并进行处方验证试验。结果:各考察因素均对药物的释放影响显著。优选工艺结果为:空白丸芯采用蔗糖型,溶胀层材料采用交联羧甲基纤维素钠,溶胀层和控释层包衣增重分别为15%、24%。以此制备的微丸时滞时间为4h左右,时滞后4h内累积释药百分率达到80%。结论:所制备的ROXPCP具有体外脉冲控释作用。     

阿莫西林脉冲释药微丸的研制

目的:制备阿莫西林脉冲释药微丸。方法:取空白丸芯分别以含药层、溶胀层(羧甲基淀粉钠)和控释层(乙基纤维素水分散体)顺序依次进行包衣制备阿莫西林脉冲释药微丸。采用紫外法和篮法考察溶胀层(12%、16%、20%)和控释层包衣增重(24%、28%、32%)及不同介质(水、盐酸、pH6.8磷酸盐缓冲液)对药物释放的影响。结果:溶胀层和控释层包衣增重对脉冲控释微丸的释药时滞和释放速率具有显著影响,药物释放情况不受介质pH值的影响;溶胀层和控释层包衣增重分别为16%、28%时制备的微丸时滞时间约为4h,时滞后4h累积释药率达到80%。结论:所制备的阿莫西林脉冲释药微丸具有体外脉冲释放作用。     

The effect of some formulation and process variables on the surface roughness of film-coated tablets

The effect of some formulation and process variables on the surface appearance of film-coated tablets has been examined by measuring the arithmetic mean roughness, Ra, values across the faces of tablets before and after they were coated with hydroxypropyl methyl-cellulose. For all tablet cores except those that were very porous, film coating resulted in an increasing surface roughness; for very porous cores a decrease was found. Tablets with rough surfaces were produced by coating with low molecular weight grades of the polymer; increaseing the polymer molecular weight resulted in a smoother finish with a minimum roughness at intermediate molecular weight grades. Increasing the polymer concentration above 2% w/v caused an increase in roughness as did increasing film thickness to 140 μm. There was a minimum in roughness at film thicknesses of 20 μm. The addition of pigment in low concentrations (0–25% v/v) caused a marginal increase in surface roughness but at concentrations above the critical pigment volume concentration, the surfaces were very rough. The results illustrate the potential of the method in the optimization of film formulations and process conditions during product development.     

The effect of some formulation and process variables on the surface roughness of film-coated tablets.

The effect of some formulation and process variables on the surface appearance of film-coated tablets has been examined by measuring the arithmetic mean roughness, Ra, values across the faces of tablets before and after they were coated with hydroxypropyl methyl-cellulose. For all tablet cores except those that were very porous, film coating resulted in an increasing surface roughness; for very porous cores a decrease was found. Tablets with rough surfaces were produced by coating with low molecular weight grades of the polymer; increasing the polymer molecular weight resulted in a smoother finish with a minimum roughness at intermediate molecular weight grades. Increasing the polymer concentration above 2% w/v caused an increase in roughness as did increasing film thickness to 140 micrometer. There was a minimum in roughness at film thickness of 20 micrometer. The addition of pigment in low concentrations (0--25% v/v) caused a marginal increase in surface roughness but at concentrations above the critical pigment volume concentration, the surfaces were very rough. The results illustrate the potential of the method in the optimization of film formulations and process conditions during product development.     

曲尼司特巴布剂的研制及释放度测定

目的:制备曲尼司特巴布剂并研究其体外释药性能.方法:以水溶性高分子材料为主要基质,以巴布剂基质的成型时间为指标,考察影响巴布剂物理性状和影响因素;进行体外释放度的测定,研究巴布剂的透皮释放行为.结果:巴布剂最佳处方为:曲尼司特 0.5 g,聚乙烯醇 6 g,水溶性高分子材料 25 g,甘油 5 g,丙二醇 5 g,氮酮 5 g,蒸馏水加至 150 g;4天药物释放率大于80%.结论:曲尼司特巴布剂含水量高,皮肤水合效果好,无刺激性;符合皮肤缓释型透皮给药系统的要求.     

2015年版《国家药包材标准》药用铝箔黏合剂涂布量差异试验的探讨

摘要 目的：对2015年版《国家药包材标准》药用铝箔中溶剂型丙烯酸酯类黏合剂涂布量差异试验进行探讨。方法：分别用乙酸乙酯、丙酮及乙醇逐次擦去药用铝箔上的黏合剂,计算每组5片平均涂布量及涂布量差异,摸索试验最佳的擦拭溶剂及擦拭程度。结果：对于涂布溶剂型丙烯酸酯类胶黏剂涂布量差异的检测,采用丙酮比乙酸乙酯,具有更好的擦拭效率,乙醇不能作为擦拭溶剂进行试验。结论：本试验摸索的条件可靠、准确,适用于涂布溶剂型丙烯酸酯类黏合剂涂布量差异的测定。     

定制设计法在盐酸丁咯地尔缓释片处方设计中的应用

目的应用定制设计法优化盐酸丁咯地尔缓释片的处方。方法以片芯中乙基纤维素和氯化钠比例的变化、包衣增重为考察因素,以不同时间点的累积释放量为优化指标,应用定制设计法筛选最佳处方,并对优化处方进行验证。结果最优处方组成为,盐酸丁咯地尔600 mg、乙基纤维素90 mg、氯化钠10 mg、包衣增量为3%,12 h累积释放量为80%以上,体外释放曲线平稳。结论采用定制设计法得到了盐酸丁咯地尔缓释片的处方优化模型,应用优化处方制备缓释片所得的实测值与预测值无明显差异,实现了处方优化。     

Methylmethacrylate sulfopropylmethacrylate copolymer nanoparticles for drug delivery. Part I: Preparation and physicochemical characterization

Methylmethacrylate (MMA) sulfopropylmethacrylate (SPM) copolymer nanoparticles were prepared by free radical polymerization. The conditions of preparation were varied with regard to the concentration of initiator and monomer, and copolymer composition. Nanoparticles with a yield greater than 80% were produced. The particles were characterized in terms of particle size, size distribution, particle charge (zetapotential) and molecular weight. The data were compared to pure polymethylmethacrylate (PMMA) nanoparticles. The copolymer composition was shown to influence particle size and particle charge. The influence of the total monomer amount in the polymerization medium on the particle size was characteristic up to a concentration of 2% depending on the solubility of MMA in water at the temperature of reaction. An increasing amount of total monomer led to particle sizes of 60–130 nm for low monomer concentrations (0.5%), depending on the proportion of SPM (0–10%), to 120–280 nm for higher total monomer concentrations (greater than 2%). Surface charge as well as particle size were influenced mainly by the proportion of the comonomer SPM in the copolymer. The negative surface charge increased from - 52 mV for pure PMMA nanoparticles to − 80mV for the copolymer particles with an SPM content of 10%. In the same range of 0–10%), SPM of the total monomer, the particle sizes decreased from 187 to 100 run. The concentration of the initiator up to a concentration of 0.3% showed no effect on the particle size of the resulting nanoparticle suspension. Higher concentrations led to intolerably large variability in the polymerization process.