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1.
贝诺酯片剂的研制及生物利用度研究   总被引:1,自引:0,他引:1  
陈俊  屠锡德 《药学学报》1994,29(9):707-712
通过减小药物粒径,提高贝诺酯片剂的生物利用度。在市售片以A(500mg)基础上研制了新处方片剂B(400mg)。建立贝诺酯片剂体外溶出度试验方法,即以表面活性剂溶液作溶出介质,以浆法进行溶出度测定。用HPLC法测定贝诺酯在体内的水解产物水杨酸和扑热息痛的血药浓度。结果表明药物研磨粉碎前后体外溶出速度常数分别为0.0152min-1及0.0337min-1(P<0.001)。A及B体外平均溶出时间分别为42.25min及15.77min(P<0.001)。体内研究表明A及B水杨酸的Cmax,Tp,AUC之间均无显著性差异(P>0.1)(A,B的服用量分别为4.5g及3.6g),B的相对生物利用度为125.59%。  相似文献   

2.
目的 建立昆仙胶囊多指标成分的溶出度测定方法,以有效控制其内在质量。方法 采用Agilent Zorbax SB-C18色谱柱(250 mm×4.6 mm,5 μm),以乙腈-0.1%磷酸水溶液为流动相进行梯度洗脱,流速为0.8 mL·min–1,柱温33℃,检测波长270 nm。采用篮法,以900 mL pH 6.8的磷酸盐缓冲液为溶出介质,转速100 r·min–1,测定昆仙胶囊中朝藿定A、朝藿定B、朝藿定C及淫羊藿苷的溶出度,并通过相似因子(f2)法对不同批次样品的溶出曲线进行相似性比较。结果 朝藿定A、朝藿定B、朝藿定C及淫羊藿苷在各自范围内线性关系良好(r=0.999 9),平均回收率分别为100.9%(RSD=1.29%),102.1%(RSD=1.18%),100.8%(RSD=1.30%)及99.9%(RSD=0.92%),不同批次昆仙胶囊中4种成分的溶出曲线相似度较高,相似因子f2均>67。结论 该法简便、准确、可行,专属性良好,可为昆仙胶囊的质量评价提供实验依据。  相似文献   

3.
目的 开展体内外相关性试验以探讨国内生产的呋塞米片的药物溶出度试验是否可以替代生物等效性试验。方法 选择呋塞米片受试与对照制剂,按照中国药典要求和光纤药物溶出度实时测定仪测试方法,监测呋塞米累积溶出百分率并计算f2相似因子,测定2种制剂的体内血药浓度并计算药动学参数,测算其体内吸收分数、生物利用度和生物等效性,分析呋塞米片体内外试验的相关性。结果f2相似因子方法评估,受试与对照制剂的呋塞米溶出曲线相似,2种制剂的主要药动学参数tmaxCmax、AUC0-24和AUC0-∞、生物利用度和生物等效性均差异明显,其体内百分吸收系数和体内外试验的相关性较差。结论 国内生产的呋塞米片的药物溶出度试验尚不能替代生物等效性试验。  相似文献   

4.
目的研究阿昔莫司缓释片在家犬体内单剂量和多剂量的药代动力学和生物等效性。方法测定6只家犬单剂量和多剂量口服缓释片和普通胶囊后的血药浓度。结果阿昔莫司的药-时曲线符合非隔室模型。单剂量给药后,缓释片和普通胶囊的AUC分别为(158±30)和(147±37) μg·h·mL-1Tmax分别为(4.3±0.8)和(2.6±1.3) h;Cmax分别为(29±6)和(42±10) μg·mL-1T1/2分别为(2.3±0.7)和(1.60±0.10) h;MRT分别为(6.0±0.8)和(3.9±0.7) h;Fr为(108±16)%。多剂量给药后,缓释片和普通胶囊的AUC分别为(209±23)和(195±26) μg·h·mL-1Tmax分别为(6.3±0.8)和(3.4±1.5) h;Cmax分别为(27±4)和(36±5) μg·mL-1Cmin分别为(2.2±1.0)和(0.20±0.20) μg·mL-1Cav分别为(8.7±1.0)和(8.1±1.1) μg·mL-1;FI分别为(293±73)%和(448±91)%;Fr为(114±19)%。结论单剂量实验的双单侧检验结果表明:缓释片和普通胶囊生物等效;缓释片具有良好的缓释效果。多剂量实验结果表明:缓释片和普通胶囊生物等效;缓释片的波动系数优于普通胶囊。  相似文献   

5.
目的:药物透过血脑屏障是药代动力学的重要过程,H2受体拮抗剂是作用于神经外周的抗溃疡药物,为避免该类药物透过血脑屏障损伤中枢神经,产生毒副作用,指导该类药物的设计与合成。方法和结果:选择了不依赖于实验参数的比较分子力场分析(CoMFA)方法和最近发展的本征值(EVA)方法,建立了有关的三维药代动力学性质(3D-QSPR)模型。CoMFA模型的统计参数为:交叉验证系数r2cv=0.625,相关系数r2=0.893,F3,17=47.270,标准偏差SE=0.254;EVA模型的统计参数为:交叉验证系数r2cv=0.697,相关系数r2=0.922,F3,17=67.766,标准偏差SE=0.203。结论:两种方法都能建立三维定量构效模型,EVA模型有更高的预测能力。  相似文献   

6.
目的 建立考察苯丙氨酯片溶出过程的方法,比较不同厂家的生产工艺及质量。方法 以对照品法,利用FODT-601FX光纤药物溶出度实时测定仪实时监测苯丙氨酯片的溶出过程,并采用相似因子(f2)对溶出曲线进行一致性评价。结果 选择0.5 mm探头,260 nm为测定波长,苯丙氨酯浓度在20~130 μg/mL与吸光度具有良好的线性关系,r=0.999 9。考察了市售的5个厂家(A~E厂)11个批次的苯丙氨酯产品在水中的溶出曲线,除D厂外各批次苯丙氨酯片的溶出度检查结果均符合日本橙皮书的规定,但各厂家苯丙氨酯片的溶出曲线存在一定差异,选取样品C1作为参比制剂,有A、C2、C3、E样品的溶出曲线与C1相似(50≤f2≤100),而B、D厂样品的溶出曲线与C1明显不同(f2<50)。结论 光纤法溶出度能客观反映苯丙氨酯片溶出全过程,监测的5个厂家生产的苯丙氨酯片存在药品溶出过程不相似以及部分厂家内在质量差异较大的问题。  相似文献   

7.
目的 考察喷液处方对硝苯地平喷雾干燥分散体(spray dried dispersion,SDD)的表征和非漏槽条件下溶出度的影响。方法 采用minitab DOE(design of experiment)中的田口设计(Taguchi design)方法,以120 min以内的溶出度曲线下面积(AUC0~120 min)及120 min时的溶出浓度和最大浓度的比值(C120/Cmax)为评价指标,考察载体材料的种类和用量及喷雾溶液的固含量对硝苯地平SDD的药物存在状态和体外溶出度的影响。结果 硝苯地平与聚合物的比例对固体分散体中药物的存在状态和体外溶出度均有显著影响,固含量对结果影响较小。以共聚维酮为载体材料时,可以获得比醋酸羟丙甲基纤维素琥珀酸酯(HPMCAS)更高的最大溶出浓度(Cmax),但是HPMCAS的抑制药物重结晶的效果明显优于共聚维酮,其中药物-HPMCAS LG 1∶4时可以获得最大的Cmax和AUC0~120 min结论 硝苯地平与HPMCAS LG按照1∶4的比例配成固含量10%的溶液进行喷雾干燥,可以制得溶出度显著改善的SDD。  相似文献   

8.
目的:通过对二氟尼柳胶囊溶出速率的评价,以期得到一个有较好溶出特性的胶囊剂。方法:参照USP23版二氟尼柳片剂的溶出度测定方法,用紫外分光光度仪测定溶出度。结果:二氟尼柳胶囊溶出度的方法回收率为100.27% ,RSD为0.62% ,重现性与均一性都较好。胶囊较原料的溶出度明显加快;与片剂相比,胶囊5min时的溶出有一滞后时间,但T80 两者无显著差异(胶囊T80=1 2 .80min ,片剂T80=13.04min)。结论:二氟尼柳胶囊所选择的赋形剂能明显提高其溶出速率,胶囊与片剂均符合USP2 3版所规定的溶出限度  相似文献   

9.
拟人参皂苷F11在大鼠体内的药物代谢研究   总被引:8,自引:1,他引:7  
王金辉  李铣 《药学学报》2001,36(6):427-431
目的探讨拟人参皂苷F11在大鼠体内的药物代谢产物及其过程.方法ip拟人参皂苷F11后,应用TLC分析排泄物中的代谢产物,并利用制备薄层分离制备代谢产物,通过波谱解析(MS,1HNMR,13CNMR,1H-1HCOSY)确定其结构.结果从粪便中分离鉴定了3种代谢产物,分别为拟人参皂苷RT5,ocotillol和1个新的代谢产物F-3-1,并确定其结构为6-O-α-L-吡喃鼠李糖基(1-2)-β-D-吡喃葡糖基-(20S,23S,24R)-达玛-20(24)-环氧-3β,6α,12β,23,25-五醇(6-O-α-L-rhamnopyranosyl-(1-2)-β-D-glucopyranosyl-(20S,23S,24R)-dammar-20(24)-epoxy-3-β,6α,12β,23,25-pentanol).但在尿液和胆汁中并未发现任何代谢产物.结论拟人参皂苷F11不被肝脏代谢,但胆汁排泄物可在肠道被代谢为水解和氧化产物.  相似文献   

10.
目的 比较3个药厂生产的地氯雷他定片的体外溶出度。方法 采用紫外分光光度法测定地氯雷他定片的含量,用溶出度测定第三法(中国药典)测定体外溶出度,根据Weibull分布求得溶出参数(T50,Td,m) ,并对参数进行方差分析。结果 3个药厂产品的含量和含量均匀度均符合国家药品监督管理局颁发的规定标准,但是3个药厂产品的溶出参数有统计学差异(P<0.01或P<0.05 )。结论 由于生产工艺和制剂处方不同,各厂家产品的体外溶出度有统计学差异。  相似文献   

11.
目的:采用光纤化学传感技术实时、在位监测固体制剂体外溶出度的测定并与2000年版中国药典方法比较。方法:应用光纤原位药物溶出度/释放度试验仪,将分支光纤一端连接光源,公共端部探头浸入溶出液;另一端连接检测器,计算机记录并处理数据。结果:本法监测药物溶出的全过程,显示药物实时溶出曲线图,直接提取相关参数,与药典方法比较,无统计学差异(P>0.05)。结论:光纤化学溶出度过程监测法能够有效地测定固体药物的体外溶出度,并能真实地反映药物溶出的全过程。  相似文献   

12.
The aim of this study was to investigate pharmaceutical potentialities of a polymeric microparticulate drug delivery system for modulating the drug profile of poorly water-soluble quercetin. In this research work two cost effective polymers sodium alginate and chitosan were used for entrapping the model drug quercetin through ionic cross linking method. In vitro drug release, swelling index, drug entrapment efficiency, Fourier Transforms Infrared Spectroscopy (FTIR), Scanning Electron Microscopy (SEM), X-ray Diffraction (XRD) and Differential Scanning Calorimetric (DSC) studies were also done for physicochemical characterization of the formulations. Swelling index and drug release study were done at a pH of 1.2, 6.8 and 7.4 to evaluate the GI mimetic action which entails that the swelling and release of the all the Formulation1 (F1), Formulation2 (F2) and Formulation3 (F3) at pH 1.2 were minimal confirming the prevention of drug release in the acidic environment of stomach. Comparatively more sustained release was seen from the formulations F2 & F3 at pH 6.8 and pH 7.4 after 7 h of drug release profiling. Drug entrapment efficiency of the formulations shows in F1 (D:C:A = 2:5:30) was approximately 70% whereas the increase in chitosan concentration in F2 (D:C:A = 2:10:30) has shown an entrapment efficiency of 81%. But the comparative further increase of chitosan concentration in F3 (D:C:A = 2:15:30) has shown a entrapment of 80% which is not having any remarkable difference from F2. The FTIR analysis of drug, polymers and the formulations indicated the compatibility of the drug with the polymers. The smoothness of microspheres in F2 & F3 was confirmed by Scanning Electron Microscopy (SEM). However F1 microsphere has shown more irregular shape comparatively. The DSC studies indicated the absence of drug-polymer interaction in the microspheres. Our XRD studies have revealed that when pure drug exhibits crystalline structure with less dissolution profile, formulated microparticles can help us to obtain amorphous form of the same drug that is likely to have more dissolution property. The findings of the study suggest that the microsphere formulations were a promising carrier for quercetin delivery and can be considered as a favorable oral controlled release dosage form for hydrophobic drug quercetin.  相似文献   

13.
Microdialysis is a non-equilibrium dynamic sampling method in which the analytes diffuse across a semipermeable membrane due to a concentration gradient and are carried away by the constantly pumping perfusion medium for on-line analysis. A BAS, Inc. microinfusion pump/injector and an on-line LC system were interfaced with a dissolution apparatus to automate dissolution testing of tablets. A DL-5 microdialysis loop probe was suspended in the dissolution medium for sampling. The automated system was used reproducibly (RSD <2%) to measure the dissolution of acetaminophen and Sulfatrim tablets. Drug recovery from the microdialysis probe was a function of the perfusion rate at constant temperature. However, microdialysis recovery was independent of drug concentration over the linear ranges of the assays for the analytes of interest. Dissolution profiles determined by microdialysis sampling were compared with manual sampling. Identical profiles were obtained for acetaminophen tablets in water at 37°C and 50 rpm by both sampling methods. Dissolution of Sulfatrim tablets was determined in 0.1 M hydrochloride acid at 37°C and 75 rpm. Microdialysis sampling permitted the use of a specially designed perfusion medium to buffer the acidic samples before injecting onto the LC column. Dissolution profiles of sulphamethoxazole were comparable for both sampling methods; however, microdialysis sampling indicated slightly higher release of trimethoprim from the Sulfatrim tablets, which was attributed to release of adsorbed drug from the connecting tubing.  相似文献   

14.
目的研究一种实时、在位监测药物固体制剂体外溶出度的测定方法———光纤化学药物溶出度过程实验法,考察本方法与《中国药典》2000版溶出度测定方法的差异。方法将双分支光纤分别连接光源和检测器,光纤公共端部直接插入溶出杯中,检测药物溶出度,通过改变药典规定吡嗪酰胺的测试波长,实现溶出度过程分析。结果方法学考察吡嗪酰胺在310nm处,浓度在60.00~280.00mg·L-1范围内吸收度与浓度成线性,r=0.9999,日内日间精密度为0.8%和1.1%(n=6),平均回收率97.8%,实现检测吡嗪酰胺溶出度,可直接从溶出曲线上提取相关参数,与《中国药典》2000版溶出度测定方法比较,两种测定方法无统计学意义(P>0.05)。结论光纤化学药物溶出度过程实验法通过改变吡嗪酰胺测试波长,不经过滤稀释,获得药物在体外的溶出曲线,数据信息完整。  相似文献   

15.
过程分析比较不同剂型头孢羟氨苄溶出度   总被引:1,自引:0,他引:1       下载免费PDF全文
目的制备并评价利福平-羟丙基-β-环糊精包合物。方法采用研磨法制备利福平-羟丙基-β-环糊精包合物,以差示扫描量热法、红外分光光度法对包合物进行鉴定,采用紫外分光光度法、相溶解度法验证利福平β-环糊精包合物的形成。体外肉汤稀释试验测定包合物对金葡菌和大肠埃希菌的抑制作用。结果利福平能够与羟丙基-β-环糊精形成物质的量比为1∶1的包合物,包合物改善了药物的溶解性能。包合物对金葡菌和大肠埃希菌的最低抑菌浓度分别为0.125μg.mL-1和32.0μg.mL-1。结论羟丙基-β-环糊精可以包合利福平并改善其溶解性能。包合物对革兰氏阳性菌和阴性菌均有明显的抑制作用。  相似文献   

16.
杜宁  王玉  蔡美明  狄斌 《中国药师》2010,13(6):828-829
目的:采用光纤化学传感技术,实时、在位监测米非司酮片的溶出度.方法:运用E1%/1cm值法监测米非司酮片的溶出全过程.结果:本法监测的溶出过程曲线与〈中国药典〉2005年版方法手动取样测定所拟合的曲线基本一致.结论:光纤药物溶出度监测仪可以准确测定固体药物的体外溶出度,真实地反映药物溶出的全过程.  相似文献   

17.
18.
A novel method for investigating drug release in a dynamic manner from nanoparticles including, but not limited to, biodegradable poly(lactic acid) (PLA) is reported. The PLA nanoparticles were prepared by the nanoprecipitation method. Two poorly soluble drugs, beclomethasone dipropionate (BDP) and indomethacin, were encapsulated into PLA nanoparticles, and their dissolution from the nanoparticles were followed in a dynamic way. The on-line method comprised a short column (vessel) packed with the PLA nanoparticles, on-line connected to an analytical liquid chromatographic column via a multiport switching valve equipped with two loops. The system allowed monitoring of the drug release profiles in real time, and the conditions for the drug release could be precisely controlled and easily changed. The effects of solvent composition and temperature on the rate of dissolution of the drugs from the PLA nanoparticles were investigated. The system proved to be linear for the drugs tested over the concentration range 10–3000 ng (n = 6, R2 = 0.999 and 0.997 for indomethacin and beclomethasone, respectively) and repeatable (RSD of peak areas <0.5%). The recoveries of the dissolution study were quantitative (120 and 103% for indomethacin and beclomethasone, respectively).  相似文献   

19.
Currently recommended compendial dissolution methods for quality control of orally administered solid dosage forms of rifampicin containing formulations are not found to be able to forecast the in vivo performance. A recently proposed dissolution method of 0.01 N HCl at 50 rpm using paddle apparatus for screening was found to be more appropriate and able to predict the in vivo performance of those formulations. The objective of this investigation was to validate the new method of dissolution testing for solid dosage forms of rifampicin containing formulations using a basket apparatus and to compare it with the frequently recommended pharmacopeial method. In the present study the newly proposed dissolution condition (0.01 N HCl) was validated using six formulations of two, three and four drug combinations from two different manufacturers by basket method and compared with the widely recommended compendial medium. In this investigation, the appropriateness of the proposed methodology was confirmed by the dissolution results of the two FDC formulations (a two-drug and a four-drug combinations) that had previously passed the bioequivalence tests. It was found that the recommended dissolution medium of 0.01 N HCl can be used for screening of rifampicin containing formulations using both paddle and basket dissolution apparatus at 50 rpm and 100 rpm, respectively.  相似文献   

20.
The aim of this study was to investigate the solubility of mefenamic acid (MA), a highly cohesive, poorly water-soluble drug in a copolymer of polyoxyethylene–polyoxypropylene (Lutrol F68®), and to understand the effect drug polymer solubility has on in vitro dissolution of MA. Solid dispersions (SD) of MA were prepared by a hot melt method, using Lutrol F68® as a thermoplastic polymeric platform. High-speed differential scanning calorimetry (Hyper-DSC), Raman spectroscopy, powder X-ray diffractometry (PXRD) and hot-stage/fluorescence microscopy were used to assess the solubility of the drug in molten and solid polymer. Drug dissolution studies were subsequently conducted on single-phase solid solutions and biphasic SD using phosphate buffer pH 6.8 as dissolution media. Solubility investigations using Hyper-DSC, Raman spectroscopy and hot-stage microscopy suggested MA was soluble in molten Lutrol F68® up to a concentration of 35% (w/w). Conversely, the solubility in the solid-state matrix was limited to <15% (w/w); determined by Raman spectroscopy, PXRD and fluorescence microscopy. As expected the dissolution properties of MA were significantly influenced by the solubility of the drug in the polymer matrix. At a concentration of 10% (w/w) MA (a single phase solid solution) dissolution of MA in phosphate buffer 6.8 was rapid, whereas at a concentration of 50% (w/w) MA (biphasic SD) dissolution was significantly slower. This study has clearly demonstrated the complexity of drug–polymer binary blends and in particular defining the solubility of a drug within a polymeric platform. Moreover, this investigation has demonstrated the significant effect drug solubility within a polymeric matrix has upon the in vitro dissolution properties of solid polymer/drug binary blends. © 2009 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 98:4545–4556, 2009  相似文献   

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