星点设计最终版
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星点设计—效应面法优选制巴戟天炮制工艺目的优选制巴戟天的最佳炮制工艺。
方法以巴戟肉为原料,通过单因素试验,选取加甘草汁量、煮制时间、闷润时间为自变量,以甲基异茜草素-1-甲醚、耐斯糖、水晶兰苷、甘草苷、甘草酸含量的综合评分为因变量,采用星点设计-效应面法优选制巴戟天最佳炮制工艺。
结果制巴戟天的最佳炮制工艺为:加甘草汁量1.5倍,闷润时间4 h,煮制时间25 min。
实际测量值与OD预测值的偏差为1.39%。
结论采用星点设计-效应面法优选的制巴戟天炮制工艺稳定可行且预测性良好,可为制巴戟天的规范化生产提供依据。
Abstract:Objective To optimize the licorice-processing technology of Morinda officinalis How. Methods Morinda officinalis How was selected as raw materials. Single-factor experiment was used to select licorice-juice amount,boiling time and moistening time as independent variables,the comprehensive scores of contents of rubiadin-1-methylether,nystose,monotropein,liquiritin,glycyrrhizinate as the dependent variables. The central composite design and response surface methodology was employed to optimize processing technology of Morinda officinalis How. Results The optimized processing parameters consisted of 1.5 times the amount of licorice juice,moistening 4 h,boiling 25 min. The deviation between real measured value and predicted value of OD was 1.39%. Conclusion The central composite design and response surface methodology for optimizing licorice-processing technology of Morinda officinalis How is stable,feasible and highly predictable,which can provide references for standardizing production of Morinda officinalis How.Key words:Morinda officinalis How;central composite design and response surface methodology;processing technology巴戟天系茜草科巴戟属多年生攀援木质藤本植物巴戟天Morinda officinalis How的干燥根,为著名的“四大南药”之一,具有补肾阳、强筋骨、祛风湿功效[1],临床用于治疗阳痿遗精、宫冷不孕、月经不调、少腹冷痛、风湿痹痛、筋骨痿软等症。
第22卷第1 2期2020年12月这宁中医药大学学报JOURNAL OF LIAONING UNIVERSITY OF TCMVol. 22 No. 12D ec., 2020方药纵横D01:10.13194/j.iss n.1673-842x.2020.12.013星点设计-效应面法伉化PFV修饰紫杉醇和青蒿琥酯胶束处方研究王为1,李学涛\孔亮1,姜爽2,罗一夫2,王晓波w(1.辽宁中医药大学,辽宁大连116600;2.中国人民解放军联勤保障部队第九六七医院,辽宁大连116011)摘要:目的制备细胞穿膜肽(P F V Y L1,P F V)修饰紫杉醇和青蒿琥酯股束,采用星点设计-效应面法优化胶束 处方,提高难溶性药物紫杉醇的包封率方法薄膜水化法制备不同处方胶束,高效液相色谱法(H ig h Perfo n m ncre L iq u id C h r o m a t o g r a p h y,H P L C)测定肢束中紫杉醇含量,并计算包封率用星点设计-效应面法对S o lu p lu s/紫杉醇 (质量比)、水化时间、水化温度进行处方优选:结果制备胶束的最佳处方为S o lu p lm/紫杉醇=120:1 (质量比);水 化时间:11111丨11;水化温度:35^:。
胶束的平均包封率为91.32%±1.27%(/1=3)。
结论建立的14丨)1^法对紫杉醇的 含量测定准确,简便,可用于计算胶束中紫杉醇的包封率:,星点设计-效应面法优化出最佳胶束处方,紫杉醇的包 封率符合要求,所建模型具有较高的显著性,适合制备P F V修饰紫杉醇和青蒿琥酯胶束为开发新的抗肿瘤靶向制 剂奠定基础关键词:星点设计-效应面法;胶束;紫杉醇;青蒿琥酯;处方优化中图分类号:R284.2 文献标志码:A文章编号:1673-842X(2020) 12-0056-05P re sc rip tio n O p tim iz a tio n o f PF V M odified P aclitaxel a n d A rte su n a te M icellesby C e n tra l C o m p o site D esign—R esponse S u rface M ethodologyW ANG W ei',LI Xuetao1,KONG Liang1,JIA N G Shuang2,LUO Yifu2,W ANG Xiaobo1,2(1 .College of Pharm acy,Liaoning University of Traditional Chinese M edicine,Dalian 1 16600, Liaoning,C hina; 2.The967 Hospital of the Logistic1Support Forceof the Chinese People's Liberation A rm y,Dalian 1 1601 1 ,Liaoning,China )A b s tr a c t: O bjective PFV mcxlifiefl paclitaxel ancl artesunate m icelles were preparer!,which wereojilim ized by central c omposite design—response surface methodology.M ethods Different prescription m icelles were prepared by membrane hyrhation,tlie HPLC method was adopted to determine the content of parlitaxel in m icelles and the enrapsulation rate of paclitaxel was c alrulated.Soluplus/parlitaxel (mass ratio ),hydration tim e,and hydration temperature were optimized hy central composite design—response sui*fare melhodology.Results As a result,the〇|)timum formulation was as follows:Soluplus/parIitaxel=120 •1(mass ratio ).Hydration tim e: 1 1m in;Hydration temperature: 35^ .Under the optimum ronrlitions,the entrapment effic iency was ( 91.32%± 1.27% ) (,口3 )•Coiic/usioii The HPLC rnethcxl for the determination of paclitaxel content is accurate,sim ple and ran he used to ralrulate the encapsulation rate of paclitaxel in m icelles.T h ere fo re,central com posite design and response surface methodology can precisely and effectively optimize the preparation of PFV modified parlitaxel and artesunate m icelles.It lays a foundation for the rlevelopment of new targeted antitumor agents.K e y w o rd s:central composite design—response surface metli〇(lology;m icelles;parlitaxel;artesunate;prescription optimization紫杉醇(Paclitaxel )具有较高抗癌活性,可以抑制微管蛋白的解聚,使细胞的有丝分裂停滞和凋亡,在临床中用于多种癌症的治疗。
星点设计-效应面法优化波生坦渗透泵片处方夏美华;张婧;李翔;刘亚丽;罗晓健【摘要】目的:运用星点设计-效应面法优化处方,制备波生坦单层渗透泵片。
方法:通过单因素考察结果,以片芯中氯化钠、聚氧乙烯(PEO N80)含量、包衣增重为自变量,以24h的累积释放量(Y_1)、药物释放曲线的相关系数(Y_2)、综合评价(Y_3)为考察指标,利用星点设计-效应面法优化处方并验证。
结果:优化处方为波生坦125mg,氯化钠78mg,PEO N80 371mg,硬脂酸镁1.44mg,衣膜处方CA 77.6mg,PEG4000 8.6mg,包衣液组成为丙酮:水=97∶3(v∶v),包衣液CA固含量为3%,包衣增重15%。
以优化处方制备的渗透泵片具有较好释药行为,24h的累积释放量为90.47%,释放曲线相关系数为0.9880,考察最优处方释放曲线实际值与预测值接近。
结论:星点设计-效应面法可用于波生坦单层渗透泵片的处方优化,所建模型具有良好的预测能力。
【期刊名称】《江西中医药大学学报》【年(卷),期】2016(028)005【总页数】5页(P83-87)【关键词】渗透泵片;星点设计-效应面法;波生坦【作者】夏美华;张婧;李翔;刘亚丽;罗晓健【作者单位】[1]江西中医药大学中药固体制剂制造技术国家工程研究中心,南昌330006;[2]江西中医药大学现代中药制剂教育部重点实验室,南昌330004【正文语种】中文【中图分类】R283.6渗透泵给药系统具有零级释放特点,相对其他缓释制剂能较长时间地维持匀速释放,且释药不受环境pH、胃肠道蠕动的影响。
对于难溶性药物,由于其自身不能产生足够的渗透压,且容易在片芯发生沉淀而致释药不完全,因此常被制作成双层片和高分子单层片。
双层片工艺较为复杂,而由于片重限制,大剂量难溶性药物的辅料调节范围较小[1-4],所以在制备大剂量难溶性药物渗透泵片时也有一定难度。
波生坦(bosentan)(普通薄膜衣片,商品名全可利,加拿大Patheon Inc.)为非选择性的内皮素受体拮抗剂,薄膜衣起到隔潮的作用,在临床上主要用于治疗WHOⅢ期和Ⅳ期原发性肺高压,或硬皮病引起的肺高压,已被美国心脏病学会基金会/美国心脏学会(ACCF/AHA)推荐为低风险肺动脉高压患者的一线治疗药物[5-8]。