复方烟酸双层缓释片与市售烟酸缓释片的生物等效性研究

目的:研究复方烟酸双层缓释片和市售烟酸缓释片的生物等效性。方法:采用双周期自身交叉给药,6只家犬单剂量灌胃复方烟酸双层缓释片与市售烟酸缓释片(均含烟酸500 mg)后,采用高效液相色谱法测定给药后12 h内的烟酸血药浓度,以3p97软件计算烟酸药动学参数和相对生物利用度。结果:家犬口服复方烟酸双层缓释片和市售烟酸缓释片后,烟酸的药动学特征符合一室模型;其主要药动学参数tmax分别为(5.2±1.4)、(5.0±1.6)h,cmax分别为(77.3±10.8)、(76.3±7.3)μg/ml,t1/2分别为(1.5±0.2)、(1.4±0.2)h,AUC0-∞分别为(416.6±60.5)、(377.5±50.7)μg·h/ml;双层缓释片的相对生物利用度为(111.1±14.8)%,双层缓释片cmax、AUC0-∞的90%置信区间分别为87.0%¹19.0%、101.0%119.0%、101.0%¹20.0%。结论:两种缓释片的cmax、AUC0-∞比较差异无统计学意义,具有生物等效性。     

心脏副交感神经正电子显像剂的研究进展

心脏副交感神经正电子显像剂的研发在评估心血管疾病中起着不可估量的作用,正电子发射断层显像能够高灵敏地反映心脏副交感神经的变化。本文旨在介绍烟碱类、毒蕈碱类和乙酰胆碱酯酶类三种心脏副交感神经显像剂的研究新进展。2-18F-氟-3-(2(S)-甲氧基氮杂环丁烷基)吡啶(2-18F-F-A-85380)、(R, S)-N-11C-甲基-二苯乙醇酸-3-奎宁环酯(11C-MQNB)和4-18F-氟苄基-右苄替米特(4-18F-FDEX)为烟碱类和毒蕈碱类副交感神经显像剂,11C-多奈哌齐(11C-DNP)和N-[11C]甲基-3[[(二甲氨基)羰基]氧基]-2-(2', 2'-二苯基丙氧基甲基)吡啶(11C-MDDP)为乙酰胆碱酯酶类副交感神经显像剂。其中11C-MQNB、2-18F-F-A-85380研究较为深入,而11C-DNP、11C-MDDP、4-18F-FDEX是具有良好临床应用潜质的显像剂。      

左乙拉西坦pH敏感鼻用凝胶在大鼠体内的药代动力学研究

目的 研究左乙拉西坦(LEV)pH敏感鼻用凝胶在大鼠体内的药代动力学.方法 用高效液相色谱法测定大鼠血中LEV的浓度.色谱柱为Wondasil C18柱(250.0 mm×4.6 mm,5.0μm),流动相为乙腈-水(11:89),检测波长为205 nm,内标为甲硝唑.按照体质量将大鼠随机分为实验组和对照组,每组6只....     

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??OBJECTIVE To prepare a nasal gel of risperidone (RIS) and evaluate its in vitro quality. METHODS The formulation and preparation process of RIS nasal gel were optimized with orthogonal test using appearance,spreading ability and in vitro release as main evaluation indexes. The quality items of the optimized RIS nasal gel such as appearance,pH value,contents of RIS and preservative,in vitro release and related substances were then evaluated. RESULTS The optimal formulation of the RIS nasal gel consisted of 0.5% RIS,0.35% carbopol 940,0.5% chlorobutanol,20% propanediol and 15% DM-??-CD and appropriate amount of purified water. Its ideal pH value was about 6.0. Furthermore,the quality items such as the appearance,pH value,contents of RIS and preservative,in vitro release and related substances of the preparation all conformed to the relevant quality requirements in China Pharmacopiea (2010). CONCLUSION The RIS nasal gel will be a promising new preparation for nasal administration due to its reasonable formulation,simple preparation process and controllable quality.     

pH值对富马酸比索洛尔化学稳定性及油水分配系数的影响

目的:研究pH值对富马酸比索洛尔(bisoprolol fumarate,BF)的化学稳定性及油水分配系数(P)的影响,为研制BF的粘膜给药液体制剂奠定基础。方法:采用HPLC法测定BF的浓度;在不同pH值下,分别测定BF在80℃下的降解百分率以及在25℃下正辛醇-水/缓冲液系统中的P值。结果:在所考察pH值范围内,随着pH的增加,BF的降解百分率逐渐减小,在pH大于4.0时,BF的降解速率趋于零。BF在正辛醇-水系统中的P值为0.23;在正辛醇-缓冲液系统中,pH为2.0～7.0范围时,药物的P值均小于1,在pH大于7.0时,P值显著增大。结论:pH值对BF的化学稳定性以及P值均有明显影响。选择适宜的pH值,对研制BF的粘膜给药液体制剂极其重要。     

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??OBJECTIVE To study the pharmacokinetics of risperidone (RIS) nasal gel and its brain targeting effect and related mechanisms in rats. METHODS The concentrations of RIS in rat plasma and brain tissues were determined by HPLC method. The pharmacokinetics and relative bioavailability to oral RIS preparation of RIS nasal gel and the drug distribution in various brain tissues such as olfactory bulb (OB), olfactory tract (OT), cerebellum (CL) and cerebrum (CR) were investigated in rats. RESULTS The main pharmacokinetic parameters of RIS following nasal and oral administration such as t_max and ??_max were 5 and 20 min, 9.89 and 1.93 ??g??mL^-1, respectively. The relative bioavailability of nasally administered RIS was up to 4 730%. Furthermore, the AUC values of RIS nasal gel for different brain tissues such as OB, OT, CL and CR were found to be 45.3,9.9,1.5 and 1.1 folds of those of oral drug suspension, respectively. CONCLUSION The in vivo absorption rate and bioavailability of RIS following nasal administration are obviously increased and improved. Additionally, the significant brain targeting characteristics of the drug nasal gel is also confirmed.     

氢溴酸西酞普兰鼻用温敏凝胶的处方优化及体外性质评价

目的优化氢溴酸西酞普兰(citalopram hydrobromide,CTH)鼻用温敏凝胶的处方并对其体外性质进行评价。方法以泊洛沙姆407(F127)和卡波姆940(CP940)作为凝胶基质材料,胶凝温度与胶凝时间为观察指标,采用星点设计-效应面法和单因素实验法优化凝胶基质处方;同时,以离体羊鼻黏膜为模型,采用Franz透皮扩散池法筛选药物透皮吸收促渗剂,最后采用冷法制备CTH鼻用温敏凝胶并进行体外性质评价;采用无膜溶出法测定制剂的体外溶蚀率及体外释放率;采用透析膜法测定其体外释放度。同时,考察温度及pH对该制剂黏度的影响。结果CTH鼻用温敏凝胶最优处方组成为:CTH 8.0%、F12720.27%、CP9400.17%、DM-β-003.0%、尼泊金乙酯0.05%及适量水。该制剂的胶凝温度为32.5℃,胶凝时间为42s,PH值为5.0,55 min时体外累积溶蚀率与药物累积释放率均大于90%,且二者具有良好线性相关性(r^2=0.9986);该制剂在8 h内体外累积释药为92%,其释药过程符合Higuchi动力学方程。温度及pH对该制剂的黏度均有不同程度的影响。结论采用星点设计-效应面法和单因素法优化处方所制备CTH鼻用温敏凝胶其肢凝温度、胶凝时间及pH值适宜,符合鼻用制剂要求,其体外释药具明显缓释特征。     

假龙胆属植物研究进展＊

近年来,假龙胆属植物的研究逐步深入,该属植物有着相似的化学成分与药理作用。本研究通过对近20年的相关文献进行检索,对假龙胆属植物的化学结构与药理活性进行归纳整理,旨在为假龙胆属植物的进一步研究与发展提供参考。