朝鲜蓟提取物颗粒剂的制备工艺研究

以单因素试验为基础，采用正交实验设计优化制备朝鲜蓟(Cynara scolymus)提取物颗粒剂的最佳工艺条件。以原料与辅料配比、原料药比例、乙醇浓度及干燥温度为考察因素，以颗粒合格率、溶化时间作为评价指标，采用L₉(3⁴)正交试验分别对颗粒合格率、溶化时间进行直观分析及方差分析。结果表明，最佳成型工艺为乳糖:糊精=3:1，乙醇浓度60%，原料药比例7.0%，干燥温度50 ℃。按此方案进行验证实验，颗粒性状良好，颗粒合格率为91.45%，含水量4.90%，减失重量不超过2.0%，溶解时间85.67 s，均符合2020年中国药典有关规定。通过正交试验优选的颗粒剂制备工艺稳定、简便易行，为朝鲜蓟提取物的剂型开发及工业化生产颗粒剂提供理论依据。     

Suitable fusion of N-terminal heptad repeats to achieve covalently stabilized potent N-peptide inhibitors of HIV-1 infection

N-terminal heptad repeat (NHR)-derived peptide (N-peptide) fusion inhibitors, which are derived from human immunodeficiency virus (HIV) envelope glycoprotein 41 (gp41), are limited by aggregation and unstable trimer conformation. However, they could function as potent inhibitors of viral infection by forming a coiled-coil structure covalently stabilized by interchain disulfide bonds. We previously synthesized N-peptides with potent anti-HIV-1 activity and high stability by coiled-coil fusion and covalent stabilization. Here, we attempted to study the effects of NHRs of chimeric N-peptides by fusing de novo coiled-coil isopeptide bridge-tethered T21 peptides of different NHR lengths. Peptides (T21N23)₃ and (T21N36)₃ was a more potent HIV-1 fusion inhibitor than (T21N17)₃. The site of isopeptide bond formation was precisely controlled and had little influence on N-peptide properties. The N-peptide (T21N36)₃, which had a similar conformation as the NHR trimer and interacted well with the C34 peptide, may be useful for screening other C-peptides and small-molecule fusion inhibitors, and for studying the interactions between the NHR trimer and C-terminal heptad repeats.     

Systematic designs for experiments with mixtures

In this paper systematic designs for experiments with mixtures are developed. The plan of analysis of the experiment is discussed for a quadratic model of SCHEFF É (1958) for q-component mixture with orthogonal polynomials of third degree describing the time trends.     

Systematic and comparative anatomy of Cymbidieae (Orchidaceae)

Cymbideae comprise an assemblage of 28 genera nearly all of which are represented in this study. Their anatomy is relatively homogenous with the exception of Govenia , in which roots lack velamen and pseudobulb vascular bundles lack sclerenchyma, conditions that do not obtain in other genera. Marginal fibre bundles in leaves of Grammatophyllum and Porphyroglottis consist of clusters of thicker-walled, narrower, epidermis-facing fibres as well as thinner-walled, wider, mesophyll-facing fibres. This feature also occurs in some species of Maxillaria . Baculate tilosomes appear in the roots of a majority of genera in Cymbidieae, as they do in species of Maxillaria , confirming DNA analyses showing a close relationship between tribes Cymbidieae and Maxillarieae. Govenia is singled out both on anatomical and molecular grounds as being ill-placed in Cymbidieae. Cladistic analysis produces only a few tentative hypotheses of phylogenetic relationships among the 28 genera, showing that anatomical characters are of limited value in assessing affinities within this tribe. © 2002 The Linnean Society of London, Botanical Journal of the Linnean Society , 2002, 139 , 1–27.