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为探讨中药制剂过程常用辅料对神经氨酸酶(Neuraminidase,NA)活性的影响,避免中药制剂对抗病毒物质药效的干扰,为生产工艺中各种辅料的使用提供借鉴依据。分别将各种受试物对NA进行干预,研究各类物质对NA活性的影响。各类辅料对神经氨酸酶活性作用不同,其中,乙酸、聚山梨酯-20、二甲基亚砜和聚乙二醇-4 000对NA活性具有较强抑制作用,IC_(50)均小于5%;Trition-X-100和乙酸乙酯较以上物质抑制作用弱,IC_(50)分别为26.7%,30.7%;乙醇与正丁醇的抑制作用较弱,难以计算其IC_(50)值,而聚乙二醇-6000则呈现出对NA活性一定的激活作用等。不同制剂辅料对NA活性影响不同,在抗流感药物的生产工艺中应高度重视各类辅料的合理应用,严格规范用量,设计合理工艺,尽量减少各类辅料在药物应用和再研究过程中对药效的干扰。
In order to explore the effect of common excipients on the activity of Neuraminidase (NA) and to avoid the interference of traditional Chinese medicine (TCM) preparations against the efficacy of anti-virus agents, this study provides references for the use of various excipients in the production process. A variety of subjects were interfered with NA to study the impact of various substances on NA activity. Various kinds of excipients had different effects on the activity of neuraminidase, among which acetic acid, polysorbate-20, dimethylsulfoxide and polyethylene glycol-4000 had a strong inhibitory effect on NA activity, with IC 50 being less than 5%. The inhibitory effects of Trition-X-100 and ethyl acetate were weaker than those of the above substances with IC 50 of 26.7% and 30.7% respectively. The inhibitory effect of ethanol and n-butanol was weak, , While polyethylene glycol -6000 showed a certain activation of NA activity and so on. Different preparations have different effects on NA activity. In the production process of anti-influenza drugs, we should attach great importance to the rational application of various excipients, strictly regulate the dosage, design a reasonable process to minimize the various types of excipients in the drug application and re-study process of the drug Effective interference.