Effect of drug-loading methods on drug load, encapsulation efficiency and release properties of alginate/poly-L-arginine/chitosan ternary complex microcapsules

The drug-loaded alginate/poly-L-arginine/chitosan ternary complex microcapsules were prepared by mixing method, absorption method and the combined method of mixing and absorption, respectively. The effect of drug-loading methods on drug load, the encapsulation efficiency and the release properties of the complex microcapsules were investigated. The results showed that the absorption process is a dominating factor to greatly increase the drug load of Hb into microcapsules. Upon loading Hb into microcapsules by combined method of mixing and absorption, the drug load (19.9%) is up to the maximum value, and the encapsulation efficiency is 93.8%. Moreover, the drug release is a zero-order kinetics process for the ternary complex microcapsules made by mixing. For the complex microcapsules made by absorption, the drug release is a first-order kinetics. However, for the complex microcapsules made by combining the mixing and the absorption, the drug release obeys a first-order kinetics during the first eighteen hours, changing afterwards to a zero-order kinetics process. Effect of drug-loading methods on drug load and encapsulation efficiency of alginate/poly-L-arginine/chitosan ternary complex microcapsules.     

相转移催化合成增塑剂BBP和水杨醛的研究

相转移催化合成增塑剂ＢＢＰ和水杨醛的研究郭锡坤，高文华，曾东宇（汕头大学化学系，汕头５１５０６３）关键词相转移催化，季铵盐，聚乙二醇，邻苯二甲酸丁苄酯，水杨醛，增塑剂邻苯二甲酸丁苄酯（增塑剂ＢＢＰ）是一种优良的增塑剂．邻羟基苯甲醛（水杨醛）不仅是重要...     

Acetylation and molecular mass effects on barrier and mechanical properties of shortfin squid chitosan membranes

Chitosan samples with different N-deacetylation levels were obtained from β-chitin under heterogeneous alkali conditions. Oxidative depolymerisation was performed to attain low-acetylated chitosan samples with different molecular mass. Water vapour permeability, membrane swelling and tensile mechanical properties were analysed in plasticized self-supporting chitosan membranes. The main purpose was to describe unambigously the effect of the biopolymer molecular mass and acetylation degree on these properties. Commercially available chitosan samples derived from α-chitin were also studied for comparison. The equilibrium degree of swelling in water and the water vapour permeability increase by increasing the molecular mass or the degree of acetylation. Regarding the effect on the mechanical properties, generally harder and tougher membranes were obtained for chitosans with higher molecular mass or lower acetylation degree. These observations are tentatively explained based on the different structural characteristics of the polymer and can lead to a better understanding of the tools necessary to tailor a specific type of chitosan membrane.     

2-羟丙基三甲基氯化铵壳聚糖的制备及其性能研究

以脱乙酰度为95.37%的壳聚糖(CTS)为原料,异丙醇为溶剂,2,3-环氧丙基三甲基氯化铵为改性剂,于80℃反应12 h合成了水溶性季铵盐2-羟丙基三甲基氯化铵壳聚糖(HACC)。HACC的吸水保水性是CTS的2倍～3倍,加入化妆品中培养2周后菌落总数少于100 CFU.g-1。     

固体超强酸催化剂SO_4~(2-)/TiO_2-WO_3的制备及其催化性能研究

制备了固体超强酸催化剂SO2 -4/TiO2 WO3 ,并以丁酸丁酯的合成作为探针反应 ,系统考察了WO3 的含量、硫酸浸渍浓度、焙烧温度等制备条件对SO2 -4/TiO2 WO3 催化活性的影响 .实验表明 :制备催化剂的适宜条件为m(H2 WO4) =12 5 % ,硫酸浸渍浓度为 1 0mol·L-1,焙烧温度为 5 80℃ ,活化时间 3h .利用优化条件下制备的催化剂SO2 -4/TiO2 WO3 催化合成缩醛 (酮 ) ,在醛 /酮与二元醇 (乙二醇 ,1,2 丙二醇 )的投料摩尔比为 1∶1 5 ,催化剂的用量占反应物总投料质量的 0 5 % ,反应时间为 1h条件下 ,2 甲基 2 乙氧羰甲基 1,3 二氧环戊烷的收率为 78 7% ,2 ,4 二甲基 2 乙氧羰甲基 1,3 二氧环戊烷的收率为 83 0 % ,环己酮 -乙二醇缩酮的收率为 85 9% ,环己酮 1,2 丙二醇缩酮的收率为 84 6% ,丁酮 -乙二醇缩酮的收率为70 7% ,丁酮 1,2 丙二醇缩酮的收率为 88 3 % ,2 丙基 1,3 二氧环戊烷的收率为 80 6% ,4 甲基 2 丙基 1,3 二氧环戊烷的收率为 79 6% ,2 异丙基 1,3 二氧环戊烷的收率为 64 2 % ,4 甲基 2 异丙基 1,3 二氧环戊烷的收率为 83 3 % ,2 苯基 1,3 二氧环戊烷的收率为 75 3 % ,4 甲基 2 苯基 1,3 二氧环戊烷的收率为 95 1% .     

Swelling kinetics and release characteristic of crosslinked chitosan: Polyether polymer network (semi-IPN) hydrogels

The aqueous swelling kinetics of a series of crosslinked chitosan (cr-CS) with glutaraldehyde (GA) interpenetrating polyether hydrogels have been studied as functions of pH, the N-deacetylation degree of chitosan, the amount of crosslinking agent, the electrolyte composition in solution, temperature, and gel composition. Based on these results, the swelling mechanism of the hydrogels was discussed. The release profiles of chlorhexidini acetas from the semi-IPN were also investigated. © 1994 John Wiley & Sons, Inc.     

Comparison of reactivities of 1- and 4-oxotetrahydrocarbazoles in reactions with nucleophilic and electrophilic reagents

The half-wave potentials of polarographic reduction of the carbonyl group in unsubstituted and N-methyl- and N-phenylsulfonyl-substituted 1- and 4-oxotetrahydrocarbazoles and their reactivities in reactions with nucleophilic (NaBH₄, malonodinitrile, and cyanoacetamide) and electrophilic (DMF dimethyl acetal) reagents were compared. 4-Oxotetrahydrocarbazoles are much less reactive than 1-oxotetrahydrocarbazoles. __________ Published in Russian in Izvestiya Akademii Nauk. Seriya Khimicheskaya, No. 8, pp. 1832–1836, August, 2005.     

SYNTHESIS OF BLOCK COPOLYMER FROM 5,6 -BENZO-2-METHYLENE-1,3-DIOXEPANE AND METHYL ACRYLATE VIA ATOM TRANSFER RADICAL POLYMERIZATION

Poly(methyl acrylate)-b-poly(5,6-benzo-2-methylene-1, 3-dioxepane) (PMA-b-PBMDO) was synthesized by two-step atom transfer radical polymerization (ATRP). Firstly, ATRP of methyl acrylate (MA) was realized using ethyl α-bromobutyrate (EBrB) as initiator in the presence of CuBr/2,2'-bipyridine. After isolation, poly(methyl acrylate) withterminal bromine (PMA-Br) was synthesized. Secondly, the resulting PMA-Br was used as a macromolecular initiator in theATRP of BMDO. The Structure of block copolymer was characterized by ~1H-NMR spectroscopy. Molecular weight andmolecular weight distribution were determined on a gel permeation chromatograph (GPC).     

丁酸壳聚糖液晶的临界行为研究

用偏光显微镜法测定了丁酸壳聚糖在四种酸性溶剂中的临界浓度值．发现临界浓度值（ｖ／ｖ％）与溶剂的酸性无关，都是１６％～１７％．在以二氯乙酸为溶剂时，不同丁酰化程度的丁酸壳聚糖有相同的临界浓度．用ＤＳＣ法测定了丁酸壳聚糖／二氯乙酸体系的临界温度，并绘制了相图．结果表明，浓度达６０％（ｗ／ｗ％）后，临界温度基本不再变化，稳定在３９℃左右．     

Stereoselective routes to substituted β-amino carbonyl compounds via heterodiene [4π+2π] cycloadditions of auxiliary-based C2 symmetric ketene acetals

Heterodiene [4π+2π] cycloadditions of (S,S)-4,5-diaryl-2-methylene-1,3-dioxolanes 1 to a series of β-amido-α,β-unsaturated carbonyl compounds are diastereoselective (d.r.≥4:1). The products can be purified by trituration or crystallisation and hydrolysed with acid to generate the corresponding β-amido carbonyl compounds, the overall sequence effecting an auxiliary-based enantioselective conjugate addition of an acetate enolate, leading to β-aminoacid derivatives.