微滤联用微波真空干燥技术在三七三醇皂苷生产中的应用

目的采用微滤与微波真空干燥联用技术,研究提高三七三醇皂苷(PTS)质量和产量的工业化生产。方法以静态饱和吸附量、PTS纯度、收率、有效成分转移率与指纹图谱为主要评价指标,考察了微滤对PTS与大孔吸附树脂的影响,进行微滤工艺L9(34)正交试验,经多批次验证与评价,确定微滤技术的可行性;以干燥PTS纯度、水分、损耗率、有效成分转移率和指纹图谱为评价指标,对干燥工艺进行筛选,进行L9(34)正交试验,经多批次验证与评价,确定微波真空干燥的可行性。结果微滤工艺,可改善产物性状、提高PTS纯度、延长树脂的再生周期、提高卫生学质量,指纹图谱相似度可大于0.99(n=5);微波真空干燥使PTS损耗率由4%～5%降低至0.2%～0.5%,指纹图谱相似度可大于0.99(n=5)。结论采用微滤与微波真空干燥联用技术能大幅度提高PTS工业化生产的质量及产量,工艺稳定,重复性好。     

Comparison of α-tocopherol microparticles produced with different wall materials: pea protein a new interesting alternative

α-Tocopherol is a radical chain breaking antioxidant that can protect the integrity of tissues and play an important role in life process. Microparticles containing α-tocopherol were produced by spray drying technique using pea protein (PP), carboxymethylcellulose(CMC) and mixtures of these materials with maltodextrin (PP-M and CMC-M) as wall materials. The microparticles produced were characterised as regards the core retention (high performance liquid chromatography), the morphology (scanning electron microscopy) and size distribution (laser diffraction). The retention of α-tocopherol within all microparticles was above 77%. They showed a spherical shape and roughness at varied degrees. Their mean particles size remained below 7?µm, and the smallest sizes were found in PP and CMC-M microparticles. The results obtained in this work show that the pea protein use for α-tocopherol microencapsulation is a promising system for further application in food.     

不同工艺干燥的玄参中桃叶珊瑚苷含量比较

目的 建立测定玄参中桃叶珊瑚苷含量的高效液相色谱法,探讨不同干燥工艺对玄参质量的影响.方法 分别对鲜玄参进行自然晾晒干燥、烘箱干燥和微波真空干燥;采用Kromasil C18柱(250 mm×4.6 mm,5μm),流动相为乙腈-水(5:95),检测波长为206 nm,柱温为30℃,流速为1.0 mL/min.结果 桃叶珊瑚苷进样量在0.11～1.81 μg与峰面积呈良好线性关系(r=0.999 7,n=6);采用微波真空干燥和自然晾晒干燥的玄参中桃叶珊瑚苷含量远高于烘箱干燥的玄参.结论 高效液相色谱法测定玄参中桃叶珊瑚苷含量,方法专属性好、准确、稳定可靠.微波真空技术用于中药玄参的干燥,不仅工艺简单、干燥时间短,而且能较好地保留桃叶珊瑚苷等有效成分.     

元胡止痛滴丸的成型工艺及晾丸工艺研究

目的:探讨元胡止痛滴丸成型工艺及晾丸工艺的优化。方法:采用正交试验法,以滴丸的圆整度、丸重差异及成型率为考察指标,优化滴距、滴速、冷凝温度及料温等滴制工艺参数;应用低温真空干燥技术晾丸,并以滴丸含水量为考察指标,对干燥温度、压力和时间等晾丸工艺参数进行优化。结果:优选基质为PEG 6000,中药提取物与基质配比为1.0∶2.0;最佳滴制工艺:滴距为3 cm,滴速为45滴/min,冷凝温度为10℃,料温为85℃;最佳晾丸工艺:干燥温度为35℃,压力为-0.05 Mpa,时间为18 h。结论:该优化工艺合理、可行,极大提高了滴丸的生产效率,且重现性良好。     

喷雾干燥法制备丹酚酸壳聚糖微囊

目的以壳聚糖为载体制备丹酚酸微囊,并对其体外释药模式进行研究。方法以收率和载药量为指标,考察处方及工艺因素对微囊的影响,并对处方和工艺进行优化。结果壳聚糖质量浓度1.5%,丹酚酸与壳聚糖的质量比1∶3,进风温度190℃,蠕动泵速度300mL.h-1,所制得的微囊表面圆整,载药量为25.99%,收率为51.88%,包封率为86.21%,平均粒径为105.6nm。体外具有一定的缓释特性,在0～240min内拟合一级释药模型方程ln(1-Q)=-0.236 9 t+4.591 7,r=0.920 3。结论采用喷雾干燥法制得的丹酚酸微囊,收率和载药量较高,制备工艺简单,可望成为实现中药微球工业化的有效方法。     

不同干燥工艺的六味地黄提取物的粉体学性能评价

目的考察不同干燥工艺对六味地黄提取物物理性质与粉体学性质的影响。方法选用六味地黄提取物考察了真空干燥、喷雾干燥及冷冻干燥对六味地黄提取物物理性质与粉体学性质的差异。结果六味地黄喷雾干燥所得浸膏粉的黏性较小,所得粉粒较细小、圆整,且压缩度、抗张强度、吸湿速率及平衡吸湿量均比真空干燥的大。冷冻干燥所得浸膏粉的比表面积、孔容均比真空干燥的大。结论干燥方式及原理的不同导致了干燥产物物理性质与粉体学性质的差异,应根据不同制备的需求选择不同的制备工艺。     

多指标综合评分法优选荆芥饮片的干燥工艺

目的 研究并确定荆芥饮片的最佳干燥工艺条件.方法 通过GC-MS法,考察了不同干燥温度、时间、初始含水率对干燥品含水率、胡薄荷酮和薄荷酮含量的影响作用.在单因素试验结果的基础上,以含水率、胡薄荷酮和薄荷酮含量为指标,采用多指标综合评分法选择正交试验的因素水平,最后通过L9(34)正交试验,确定荆芥饮片的最佳干燥工艺.结果与结论 本试验初步确定荆芥饮片最佳干燥工艺为风温60℃,干燥4h,初始含水率为197.62％d.b.     

Development of a spray-drying method for the formulation of respirable microparticles containing ofloxacin–palladium complex

The purpose of this study was to produce low-releasing spray-dried polymeric microparticles (MP) useful to target alveolar macrophages in tuberculosis (TB) inhalation therapy.     

Manufacturing of solid dispersions of poorly water soluble drugs by spray drying: Formulation and process considerations

Spray drying is an efficient technology for solid dispersion manufacturing since it allows extreme rapid solvent evaporation leading to fast transformation of an API-carrier solution to solid API-carrier particles. Solvent evaporation kinetics certainly contribute to formation of amorphous solid dispersions, but also other factors like the interplay between the API, carrier and solvent, the solution state of the API, formulation parameters (e.g. feed concentration or solvent type) and process parameters (e.g. drying gas flow rate or solution spray rate) will influence the final physical structure of the obtained solid dispersion particles. This review presents an overview of the interplay between manufacturing process, formulation parameters, physical structure, and performance of the solid dispersions with respect to stability and drug release characteristics.     

An approach to a cold chain free oral cholera vaccine: in vitro and in vivo characterization of Vibrio cholerae gastro-resistant microparticles

The present work describes the formulation of Eudragit^® L30 D-55 microparticles (MP) alone or with mucoadhesive agents, alginate or Carbopol^®, as an approach for the development of an oral cholera vaccine. In the first part, a spray drying technique was optimized for microparticle elaboration, obtaining a microparticle size ranging from 7 to 9 μm with high encapsulation efficiencies. Moreover, gastro resistant properties and Vibrio cholerae (VC) antigenicity were maintained, but for Eudragit^®-Carbopol^® microparticles which showed low antigenicity values, ≈25%. Next, a stability study was performed following ICH Q1 A (R2) guidelines, i.e. 25 °C-60% relative humidity (RH) for 12 months, and 30 °C-65% RH and 40 °C-75% RH for 6 months. Upon storage, microparticle size changed slightly, 1 μm for Eudragit^®-alginate MPs and 0.36 μm for Eudragit^®MP. However, gastro resistance and antigenicity values were kept in an acceptance range. In the third stage of this work, in vivo experiments were performed. The immune response evoked was measured by means of vibriocidal titer quantification, observing that Eudragit^®-alginate MPs were able to induce stronger immune responses, comparable to the free VC. Therefore, microencapsulation of VC by spray drying could be proposed as an approach to a cold chain free and effective oral cholera vaccine.