中药液体制剂研究中的药用辅料及其应用技术

药用辅料是制剂处方设计时,为解决制剂的成型、有效、稳定及安全性能而加入处方中的,除主药以外的一切药用物料的统称.正确、合理地应用药用辅料对保障药物制剂质量起着十分重要的作用.本文简要介绍了中药液体制剂研究中的药用辅料及其应用技术,可供从事现代中药液体制剂研究、生产者参考.     

磷脂等乳化剂在花生冰淇淋中的应用

对磷脂等乳化剂在花生冰淇淋中的作用机理研究表明 ,磷脂与冰淇淋中蛋白质、油脂和水形成了一定强度的多分子吸附膜 ,从而使冰淇淋晶粒细小 ,质地光滑 ;磷脂不仅能提高花生冰淇淋的营养价值 ,而且乳化性还优于单甘酯 .正交实验获得了最佳乳化剂配方 :磷脂 0 .1 7% ,蔗糖酯0 .1 % ,单甘酯 0 .1 % .     

Preparation of Highly Charged,Monodisperse Nanospheres

A two‐stage shot growth emulsifier‐free polymerization was applied to prepare styrene(St)/sodium styrenesulfonate (NaSS) latices. The latex particles prepared in the pure water medium were monodisperse and highly charged spheres, but their particle diameters were all higher than 120 nm. By using the two‐stage shot growth copolymerization at 70°C in the mixed reaction medium of water and acetone, we successfully prepared monodisperse, highly charged nanospheres with the smallest particle diameter of 89 nm. As the acetone content in the mixed reaction medium was increased to an acetone/H₂O ratio of around 0.125, the particle diameter decreased to minimum, and then the particle diameters increased with increasing acetone content in the mixed reaction medium. The conversion‐time curves for the first stage emulsifier‐free copolymerization of St/NaSS in the mixed reaction medium with varied acetone contents show that the polymerization rate first increased with increasing acetone content, and then decreased. The enhanced rate of polymerization in the lower acetone content results from the increase in the number of primary particle in the reaction medium. As the acetone content was further increased, the solubility of St in the reaction medium further increased, making the copolymerization somewhat like the dispersion polymerization and thus causing increased particle size.     

In vitro testing of tensides employing monolayer cultures: a comparison with results of patch tests on human volunteers

Evaluation of the irritant potential of new products or ingredients prior to human testing is generally performed in vivo on animals. However, according to the 6th amendment and following updates of the European Community directive on cosmetic products (93/35/EEC), animal testing will be banned when suitable substitutes will be available. To know whether in vitro tests for assessment of skin irritancy provide results approaching human conditions, comparisons have to be made between data deriving from in vitro tests and skin response in humans. The aim of our study was to assess the validity of the monolayer culture system of normal human keratinocytes as a model for the evaluation of the irritant effects of detergents, by comparing in vitro cell culture data to in vivo acute skin irritancy effects of cocamidopropyl betaine (CAPB), an amphoteric compound, Tween 20 (TW20) (polysorbate 20) and Tween 80 (TW80) (polysorbate 80), representing nonionic compounds, applied to the skin of 24 healthy volunteers at a concentration similar to that employed in commercial products. As parameters for cytotoxicity, cell proliferation, cell membrane integrity and cell metabolism were assessed by cell counts, thymidine incorporation, MTT conversion, and Neutral Red uptake. In order to increase the sensitivity of the in vivo evaluation, bioengineering methods for assessment of the effects of test products on the skin were employed. Whereas all 4 in vitro methods ranked the tensides according to their toxicity in the following order: CAPB>SLS>TW20>TW80, both in vivo methods agreed in identifying SLS as the most irritating substance. Moreover, as compared with the irritation potential on human skin, all 4 in vitro tests overestimated the toxicity of CAPB. This suggests that the keratinocyte monolayer cell culture technique cannot directly replace in vivo methods, and that data obtained by this method should be interpreted cautiously.     

OP乳化剂荧光猝灭法测定甲壳素胶囊中壳聚糖的含量

目的:建立甲壳素胶囊中壳聚糖含量的测定方法。方法:采用OP(聚乙二醇辛基苯基醚)乳化剂荧光猝灭法。在pH4.5的B-R缓冲溶液中,波长为λex/λem=226/304nm时,考察壳聚糖对OP乳化剂的荧光猝灭作用。结果:壳聚糖检测浓度在0.20～2.00mg.L-1范围内与OP乳化剂的荧光猝灭程度呈线性关系(r=0.9993),检出限为0.039mg.L-1;平均加样回收率为96.90%,RSD=3.25%(n=6)。结论:该法简便、快速、准确可靠,可用于较为复杂样品中微量壳聚糖的含量测定。     

混合表面活性剂分光光度法测定痕量锌

目的：在曲拉通-100（TritonX-100）和乳化剂（OP）存在下,基于Zn（Ⅱ）与2-（5-溴吡啶-2-偶氮）-5-二乙氨基苯酚（5-Br-PADAP）溶液的显色反应,建立了分光光度法测定痕量锌的新方法,同时为反应机理做一些基础实验。方法：通过添加TritonX-100-OP进入Zn（Ⅱ）-5-Br-PADAP体系提高灵敏度来测量锌含量。结果：体系最大吸收波长为575nm,表观摩尔吸光系数为ε=1.90×105 L.mol-1.cm-1,Zn（Ⅱ）含量在0.026～12.0μg/25mL范围内服从比尔定律,线性回归方程为A=0.3365C（μg/25mL）＋0.1006r,=0.9992,干扰离子较少。结论：已用于人发中锌含量的测定,结果令人满意。     

两种双亲性聚合物自组装胶束复合水溶液的乳化性能

以苯乙烯(St)、含香豆素光敏单体(VM)、丙烯酸(AA)为单体,偶氮二异丁腈（AIBN）为引发剂引发自由基共聚,合成了双亲性光敏无规共聚物P(St-co-VM-co-AA)(简称PSVA);又以St及甲基丙烯酸二甲胺乙酯(DMAEMA)为单体,AIBN为引发剂引发自由基共聚,制得二元双亲性无规共聚物P(St-co-DM)(简称PSDM)。用凝胶渗透色谱及核磁共振氢谱对聚合物进行了表征;双亲性聚合物PSVA以及PSDM分别在选择性溶剂N,N-二甲基甲酰胺水中自组装形成阴离子PSVA胶束和阳离子PSDM胶束,通过激光粒度分析仪和Zeta电位仪研究了两种胶束按不同质量配比复配所得复合胶束的粒径及电位;以不同复合配比所得复合胶束作为颗粒乳化剂,制备甲苯-水乳液,用数码照片和光学显微镜表征乳状液以及乳液滴形貌。结果表明：水相体系中,阴离子PSVA和阳离子PSDM胶束按不同质量配比复合可得到不同的复合胶束PSVAPSDM溶液,改善了单一体系的乳化性,且当w(PSDM)=24.2%时复合胶束达到等电点,当w(PSDM)=33.3%时乳化效果最好;紫外光交联得到的交联PSVA胶束（CL-PSVA）,与PSDM复配后的复合胶束CL-PSVA-PSDM可作为乳化剂改善PSVA-PSDM复合胶束所制备乳液的稳定性。     

乳化剂对聚硅氧烷乳液稳定性的影响

研究了乳化剂烷基酚聚氧乙烯醚(OP)、烷基聚氧乙烯醚和烷基季铵盐对聚硅氧烷乳液聚合的影响。采用复合乳化剂可以提高乳液稳定性。结果表明：①在以D4、N-β-氨乙基-γ-氨丙基甲基二甲氧基硅烷为原料的乳液聚合中。当非离子型乳化剂烷基聚氧乙烯醚和离子型乳化剂烷基季铵盐复合使用时，二者性能互补，产生协同效应，可使聚合物乳液具有很大的稳定性。②在实验选定的乳化剂中，非离子型烷基聚氧乙烯醚乳化剂用量为80mL(含量为0．05g／mL)、离子型烷基季铵盐乳化剂为60mL(浓度为0．05g／mL)时。其乳液的电解质稳定性、pH稳定性、冻融高温稳定性和离心稳定性等较好。