共查询到19条相似文献,搜索用时 109 毫秒
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苦参总碱贴片体内药物动力学研究 总被引:14,自引:0,他引:14
本文应用Wistar大鼠研究了苦参总碱贴片经皮给药后的体内药物动力学,由于其它生物碱含量过低,故以测定血中苦参碱和氧化苦参碱浓度之和代表苦参总碱,计算出药动学参数。结果表明苦参总碱在体内为二室模型一级吸收过程,Tp为8.44,Cm为6.559ug/ml,t1/2α为5679h,t1/2β为19.572h,t1/2Ka为2.831h。 相似文献
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高速逆流层析分离中药苦参和洋金花总碱 总被引:1,自引:0,他引:1
本文应用我国创制的89-A型HSCCC,以氯仿一磷酸钠缓冲液为溶剂系统,上相为固定相,下相为流动相。从苦参总碱分离苦参碱(Ⅰ)和氧化苦参碱(Ⅱ)等;从洋金花总碱分离东茛菪碱(A)和茛菪碱(B)等。检测手段为UV、TLC和PPC分离效果满意,溶剂用量少,操作简便省时。 相似文献
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苦参总碱注射液的药动学的研究 总被引:17,自引:0,他引:17
目的 建立了兔血浆中苦参类生物碱的毛细管电泳分离测定法。方法 在血浆中加入内标西咪替丁后 ,用甲醇进行蛋白沉淀 ,高速离心后 ,直接进样测定。运行缓冲液为 0 .2mol·L-1Tris 4 0mmol·L-1磷酸二氢钠溶液 2 0 %异丙醇 ,用磷酸调pH至 5 .5 ,检测波长为 2 0 5nm。 结果 本测定方法的提取回率为 94 .6 4 %~ 98.78% ,对血浆中氧化槐果碱的最低检测浓度为 0 .2 μg·L-1,氧化苦参碱的最低检测浓度为 1.0 μg·L-1,氧化槐果碱和氧化苦参碱的线性范围分别为 0 .4 1~ 72 .5 μg·L-1和 1.95~ 2 6 8.5 μg·L-1,相关系数分别为 0 .9992和 0 .9994。兔静注 10 0mg·kg-1苦参总碱注射液后 ,用本法测定了兔血浆中氧化槐果碱和氧化苦参碱的浓度经时变化过程 ,并对其药动学参数进行估算。结论 用本法同时测定兔血浆中的氧化槐果碱和氧化苦参碱 ,结果满意 ,氧化槐果碱和氧化苦参碱在体内符合开放式二室模型 相似文献
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[目的]通过对苦参提取工艺的研究,寻找适合于提取苦参总碱的方法。[方法]对几种从苦参中提取生物碱的主要方法进行比较,选择树脂法为本次工艺研究的实验方法。[结果]苦参总碱的收率在4~7之间,平均值为5.87。氧化苦参碱的含量也在75%~80%之间,平均值为76.38%。[结论]用树脂法提取以氧化苦参碱为主的苦参总碱,提高了其产品的收率和含量。为企业大批量生产提供了有效数据。 相似文献
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苦参总生物碱提取纯化工艺研究 总被引:1,自引:4,他引:1
目的:研究苦参总碱的提取纯化工艺。方法:以总生物碱提取率为指标考察冷浸、渗漉、水煎煮三种提取工艺;以总生物碱及氧化苦参碱含量为指标,优选纯化工艺路线及阳离子树脂纯化工艺的技术参数,包括树脂用量,流速,解吸附方法等。结果:最佳提取工艺为:1%醋酸水溶液冷浸3次,以1/3(生药重)量的阳离子树脂纯化,5%氨水乙醇回流解吸附。提取物中苦参总生物碱含量可达95%以上,总生物碱的提取纯化转移率可达80%左右。结论:工艺简单,周期短,成本低,提取物中总碱转移率及纯度均高。 相似文献
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HPLC法测定苦参软膏中苦参碱、槐定碱和氧化苦参碱 总被引:2,自引:0,他引:2
目的 建立苦参软膏(苦参总碱等)中苦参碱、槐定碱和氧化苦参碱的定量测定方法.方法 采用RP-HPLC法,以Inertsil ODS-3的色谱柱(5μm,0.46 cm×15 cm)分离,乙腈-0.1%磷酸溶液(18∶82,v/v)(三乙胺调节pH值至8.0)为流动相洗脱,体积流量1.0 mL/min,检测波长220 nm.结果 苦参碱、槐定碱和氧化苦参碱分别在0.078 08~ 7.808 μg、0.0996-9.96 μg和0.02004 -2.004 μg范围内进样量与峰面积呈良好的线性关系,相关系数均为1.0000,平均回收率分别为97.7%(RSD为1.8%,n=9)、99.9%(RSD为1.8%,n=9)、97.8%(RSD为2.2%,n=9).结论 本法重复性好、灵敏度高、定量准确,可作为苦参软膏质量控制方法之一. 相似文献
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??OBJECTIVE To prepare amoxicillin enteric-coated tablets and study the in vitro release properties. METHODS The drug-containing pellets were prepared by extrusion-spheronization process. Taking the cumulative release at 15 min as the response value, the optimization test was performed using the common rotation combination design and the optimal formulation was validated. The drug-containing pellets were coated with Eudragit L30D-55 to prepare enteric-coated pellets. The effects of different coating weight gains on the release characteristics of enteric-coated pellets, different amounts of plasticizer on the release characteristics of enteric-coated pellets and tablets, and different hardness of tablets on the release characteristics of enteric-coated tablets were investigated by single factor method. RESULTS The optimal formulation of the drug-containing pellets determined by response surface analysis method included 5% of croscarmellose sodium, 1.2% of polyoxyethylene 35 castor oil and 1% hydroxypropyl cellulose. The predictive value of the cumulative release at 15 min was close to the measured value. The coating weight gain of Eudragit L30D-55 should be about 20%, the amount of plasticizer should be 30% of solid content of Eudragit L30D-55, and the hardness of tablets was (130??20)N. CONCLUSION It is reasonable and reliable to optimize the formulation of drug-containing pellets by response surface analysis method. The enteric-coated tablets have good delayed release effect, and this product has the feasibility of industrial production. 相似文献
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Li-ping Liang Hong-lang Chen Shu-ming Zhao Wen-feng Chen Li-jun Song Wen-chang Zhao 《中草药(英文版)》2016,8(1):44-52
Objective To deliver multiple component drugs to colon site and sustain a synchronous release for better therapeutic effect. For achieving this purpose, colon specific pellet containing total alkaloids of Sophora alopecuroides(TASA) was prepared. Methods The pellet was prepared by extrasion-spheronizing and subsequently coated with three layers of two polymers. Results The pellet core consisted of 40% TASA, 1:2 in ratio of Bletilla striata polysaccharide(BSP), an enzyme-degradable material, to microcrystalline cellulose(MCC), filler, and 1% CMC-Na solution as binder by optimization. Concerning of the three coated layers, the outer layer was coated with Eudragit RS30 D for controlling drug release in colon, the intermediate layer and the inner layer were coated with same polymer, Eudragit S100, for preventing drug release in upper gastrointestinal tract, which required 23.2%, 21.7%, and 9.3% weigh gain, respectively. The coated pellets released 1.20% of sophoridine and 1.98% of matrine in media mimicking the stomach condition for 2 h, and 23.88% of sophoridine and 22.91% of matrine in media mimicking the intestine for 3 h and finally 90.25% of sophoridine and 89.94% of matrine in colonic conditions within 24 h. And the similarity factor f2 of sophoridine and matrine of release curve for investigated formulation was internal in(50-100) and 80, demonstrating that sophoridine and matrine in formulation achieved a synchronous release. Conclusion The coated pellets achieve a certain colon-specific release and synchronous release. 相似文献
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目的研制黄葵缓释片,并考察其体外释放度。方法采用混合骨架材料制备黄葵缓释片,以人工胃液为溶出介质,采用紫外分光光度法考察缓释片体外释放度。结果筛选得到缓释片最佳处方为:TFA25%,HPMC(K4M)55%,EC 5%,Lactose 15%,Mg stearate 1%。结论黄葵缓释片的制备工艺较简单稳定、重现性好,制得的缓释骨架片具有较理想的缓释作用。 相似文献
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HPLC法测定不同产地苦参中苦参碱和氧化苦参碱的含量 总被引:2,自引:0,他引:2
目的:HPLC法测定不同产地苦参中苦参碱和氧化苦参碱的含量。方法:HPLC条件:Waters Spherisorb 5μm NH24.6mm×250mm;流动相:乙腈-无水乙醇-3%磷酸溶液(80∶10∶10),流速1.0ml.min-1;检测波长220nm。结论:不同产地苦参中苦参碱、氧化苦参碱含量及其比例存在明显差异,可为评价不同产地苦参质量提供依据。 相似文献
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pH敏感型苦参结肠靶向微丸的处方筛选及其释药性能评价 总被引:2,自引:2,他引:0
目的:筛选确定pH敏感型苦参结肠靶向微丸的制剂处方,评价其释药性能。方法:采用挤出-滚圆法制备丸芯,以圆整度、脆碎度、得率、粒度分布、溶出度为评价指标,对丸芯处方进行筛选。采用流化床包衣技术,以释药性能为评价指标,对pH敏感包衣处方进行筛选,以浆法对包衣微丸的体外释药性能进行评价。结果:以主药4倍量的微晶纤维素为稀释剂,加入6%羧甲基淀粉钠混匀,加入28%水润湿,制软材,挤出滚圆得丸芯;以Eudragit S100为膜控材料,加入25%滑石粉,20%柠檬酸三乙酯,以95%乙醇为溶剂,配制包衣液,包衣使丸芯增重30%,得包衣微丸。该微丸在人工胃液、小肠液中苦参碱、氧化苦参碱的累积泄漏率为21.6%,结肠液中累积释放率达95.3%。结论:拟定了苦参结肠靶向微丸的制剂处方,制备得微丸质量稳定,具有良好结肠靶向释药性能。 相似文献
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苦参制剂对体外血清胆碱酯酶和转氨酶活性的影响 总被引:1,自引:0,他引:1
目的探讨临床常用苦参制剂(肝炎灵、苦参碱和苦参素)对血清胆碱酯酶和转氨酶活性的影响。方法采用体外药物与血清共育方式,分别于药物与血清共育10min和24h后,用全自动生化分析仪检测血清胆碱酯酶和转氨酶的活性。结果只有苦参碱对血清胆碱酯酶和转氨酶活性有直接抑制作用,苦参素和肝炎灵对血清胆碱酯酶和转氨酶活性均无直接抑制作用。结论苦参碱能直接抑制血清胆碱酯酶和转氨酶活性;肝炎灵和苦参素对体外血清胆碱酯酶和转氨酶活性无直接抑制作用,其体内用药致血清胆碱酯酶活性下降的原因是其在体内经过代谢转化成为苦参碱或其他具有强力抑制胆碱酯酶活性的代谢产物或转化产物。 相似文献