Novel strategy for encapsulation and targeted delivery of poorly water-soluble active substances

Carriers for targeted delivery and controlled release of poorly water-soluble active substances (PWSAS) are facing three challenges: (a) the encapsulation issues, (b) limitations of PWSAS water solubility, and (c) burst drug release which can be pharmacologically dangerous and economically inefficient. The present study brings a novel strategy for encapsulation and controlled release of PWSAS—caffeine in concentrations which are higher than its maximal water solubility without the possibility of burst effect. The modification of hydrophilic carrier based on poly(methacylic acid) was done using casein and liposomes. To further increase the maximal caffeine loading inside the carrier nicotinamide was used. The release study of the encapsulated PWSAS was elaborated with respect to morphology of the carriers and interactions that could be established between its structural components. The carriers swelling and the release of caffeine and nicotinamide were also investigated depending on caffeine concentration, the presence of different liposomal formulations and the volume ratio of liposomal formulation, in three media with different pH simulating the path of the carrier through the human gastrointestinal tract. The synthesized carriers are promising candidates for encapsulation of PWSAS in concentrations which are higher than its maximal water solubility and for the targeted delivery of those dosages.     

含葡萄糖基水溶性硫化黑的合成

本文以C.I.硫化黑1为原料,经葡萄糖还原成隐色体后,再与葡萄糖缩合,合成出含葡萄糖基水溶性硫化黑。合成方法分别采用了焙烘法和水介质中合成。结果表明,水介质中合成的含葡萄糖基水溶性硫化黑溶解度好于焙烘法。     

纤维素的辐射裂解及其化学性质

纤维素经高能射线辐照,能产生一系列的化学和物理性质的变化。本文报道在不同剂量的~(60)Coγ射线辐照下,稻草中的水溶性糖、易水解糖、难水解糖,以及氨基酸、蛋白质等物质的化学变化;用辐射与加泡涨剂相结合的方法处理稻草,可以降低剂量、提高效应。     

Structure, properties and application to water-soluble coatings of complex antimicrobial agent Ag-carboxymethyl chitosan-thiabendazole

The structure, properties and application to water-soluble coatings of a new complex antimicrobial agent Ag-carboxylmethyl citosan-thiabendazole （Ag-CMCTS-TBZ） prepared from different materiel ratios were reported. The silver ions were preferably coordinated with the free-NH2 groups and the -OH groups of secondary alcohol and carboxyl in CMCTS. TBZ preferably bonded to carboxyl group in CMCTS by electrostatic force and hydrogen bonding. Increase in silver ions content in the complex agent improved to some limited extent the antibacterial activity, but enhanced coloring and cost of the complex agent. Increase in TBZ content resulted in increase of antifungal activity, but decrease of water solubility of the complex agent. The antimicrobial MICs of the complex agent to Esherichia coil, Staphylococcus aureus, Candida albicans, Aspergillus niger, Mucor sp. were 20 -80, 15 -60, 20 - 55, 40 - 250, and 400 - 1700 mg/kg, respectively. Addition of 0.1% of this complex agent to acrylic emulsion paint made the paint without substantial change in color, luster, viscosity, odor or pH value, but with an excellent and chronically persisting broad-spectra antimicrobial activity.     

气体硬化水溶性砂芯的性能研究

以电熔刚玉为骨料、氢氧化钡为粘结剂、铝粉为添加剂的型芯混合料在吹入CO_2气体后即可实现硬化。本文研究了这种型芯的硬化工艺和常温特性,并采用X射线衍射分析、失重—示差热分析等方法,结合粘结膜的扫描电镜照片,对型芯的受热物理化学变化、高温强度、水溶性等行为进行了实验研究。     

乙酸酐对魔芋葡甘聚糖的改性

研究了乙酸酐对魔芋葡甘聚糖的改性,制备了魔芋葡甘聚糖醋酸酯,优化了制备工艺条件,得出了酸性催化剂条件下,乙酰化魔芋葡甘聚糖的最佳改性工艺条件为:n(乙酸酐)∶n(魔芋葡甘聚糖)=4 8∶1,反应温度50℃,反应时间4h,催化剂c(H2SO4)=0 038mol/L,取代度DS=0 662。物化性能测试表明,取代度超过0 270时,魔芋葡甘聚糖醋酸酯在水中溶解;60℃时最大溶解度为w(魔芋葡甘聚糖醋酸酯)=12%,取代度超过0 469时,魔芋葡甘聚糖醋酸酯能制成均匀的薄膜,膜厚10～30μm。     

Reaction products of ammonium nitrate phosphate fertilizers of varying water-soluble phosphorus content in different Indian soils

Studies were undertaken on the isolation and identification of reaction products of ammonium nitrate phosphate (ANP) fertilizers containing 30, 50 and 70 per cent water-soluble phosphorus (WSP) of total phosphorus in representative soils of the vertisol, oxisol, alfisol, entisol, mollisol and aridisol groups of India. ANP fertilizers were applied in solid form to soil, and reaction products formed at and around the site of ANP fertilizer placement were identified after six weeks incubation in moist soils by X-ray diffraction technique. DCPD (dicalcium phosphate dihydrate- CaHPO₄ · 2H₂O) was the major reaction product of ANP fertilizers containing 30 and 50 per cent WSP in vertisol, entisol, aridisol, mollisol, oxisol and alfisol, and of ANP containing 70 per cent WSP in vertisol, entisol, alfisol, aridisol and mollisol. DCP (dicalcium phosphate-CaHPO₄) was detected with ANP of 30 and 50 per cent WSP in the vertisol, alfisol, entisol, mollisol and aridisol groups of soils. In addition to DCPD, FePO₄ · 2H₂O (metastrengite) and AlPO₄ · 2H₂ O-monoclinic (metavariscite) were formed in alfisol and oxisol soils with ANP of 30 and 50 per cent WSP. FePO₄ · 2H₂O and AlPO₄ · 2H₂O (metavariscite) were identified in alfisol and oxisol soils while AlPO₄ · 2H₂O-orthorhombic (variscite) was formed in alfisol soils with ANP of 70 per cent WSP.     

PAA·2HC1—RH体系引发DMDAAC—AM共聚合的动力学研究

合成了二甲基二烯丙基氯化铵—丙烯酰胺共聚物 ,测定了水溶性偶氮化合物 -RH引发体系 (PAA·2HCl-RH)和过硫酸钾 -RH引发体系 (KPS -RH)引发共聚反应时单体DM和AM的竞聚率 ,以及PAA·2HCl-RH体系用于DM -AM共聚时的活化能。结果表明 :PAA·2HCl-RH引发DM -AM共聚时 ,DM和AM的竞聚率分别为 0 .174和 6 .8,活化能为 33.2 5kJ/mol;而KPS -RH引发DM -AM共聚时 ,DM和AM的竞聚率分别为 0 .0 76和 7.1。     

金属注射成型用水溶性粘结剂的研究

介绍了一种金属注射成型用水溶性粘结剂的制备方法，该粘结剂使用方便且安全无毒，用于金属注射成型时可用水作溶剂脱除，从而使成本大大降低。     

Water-soluble Copolymers of N-vinylpyrrolidone and Vinyl Acetate: Synthesis, Characterization, and Monomer Reactivity at High Conversions

Homogeneous copolymers of N-vinylpyrrolidone (VP) and vinyl acetate (VA) which form clear aqueous solutions were prepared by free radical polymerization in a solution of isopropanol alcohol, using 2,2-azobisisobutyronitrile as an initiator. They were characterized by FTIR, ¹H-NMR, and element analysis studies. The reactivity ratios of the monomer were computed by the Extended Kelen–Tüdós method at high conversions, using data from both ¹H-NMR and elemental analysis studies. The reactivity ratios of VP and VA in a homogenous copolymer were observed to be very different from that of a heterogeneous copolymer. Additional information was obtained by finding out the sequence length distribution for copolymers.