Snyman D, Govender T, Kotzé A F
Department of Pharmaceutics, School of Pharmacy, Faculty of Health Sciences, Potchefstroom University for Christian Higher Education, Potchefstroom, South Africa.
Pharmazie. 2003 Oct;58(10):705-8.
For a better understanding of the behaviour of macromolecules in vitro and in vivo, their structural and chemical properties that may be influential as experimental variables need to be characterised. N-Trimethyl chitosan chloride and N-triethyl chitosan chloride have been synthesised from chitosan to increase the solubility range of these polymers. However, little is known about the effect of the degree of quaternisation, molecular weight, viscosity and different substitution groups on the polymer's ability to enhance the transport of large hydrophilic compounds, such as peptide and protein drugs, across intestinal and nasal epithelia and on their toxicity profile. This study describes the synthesis of various quaternised chitosan polymers from low and medium molecular weight chitosan. These polymers were characterised to determine if any relationships between their degree of quaternisation, molecular weight and viscosity could be found which will determine their behaviour as absorption enhancers in future studies.
为了更好地理解大分子在体外和体内的行为,需要对其可能作为实验变量产生影响的结构和化学性质进行表征。已从壳聚糖合成了N-三甲基氯化铵壳聚糖和N-三乙基氯化铵壳聚糖,以扩大这些聚合物的溶解度范围。然而,关于季铵化程度、分子量、粘度和不同取代基对聚合物增强大型亲水性化合物(如肽和蛋白质药物)跨肠上皮和鼻上皮转运能力及其毒性特征的影响,人们了解甚少。本研究描述了由低分子量和中分子量壳聚糖合成各种季铵化壳聚糖聚合物的过程。对这些聚合物进行了表征,以确定能否找到它们的季铵化程度、分子量和粘度之间的任何关系,这将决定它们在未来研究中作为吸收促进剂的行为。