固相微萃取-HPLC测定生物样品中异丙酚含量

目的 采用固相微萃取（solid phase microextraction,SPME）-HPLC联用技术测定生物样品中异丙酚的含量。方法 采用Oasis HLB固相微萃取小柱对样品进行前处理,Shim-pack VP-ODS色谱柱（250 mm×4.6 mm,5 μm）,乙腈-水（1%三氟乙酸调pH值至4.00）（70：30）为流动相,流速1.0 mL·min^-1,激发波长276 nm,发射波长301 nm,柱温40℃。结果 异丙酚和卡马西平分离度良好。异丙酚在1.2~21.0 mg·L^-1内线性关系良好（r=0.999 7）,平均方法回收率为98%~104%,RSD<5%;日内、日间精密度RSD均<5%。结论 该方法简便、专属性好,能有效消除部分内源性物质的干扰,适用于异丙酚的血药浓度监测和临床药动学研究。     

PVC/PE/PVDC固体药用复合硬片PVDC涂布量测定

目的 建立一种测定聚氯乙烯/聚乙烯/聚偏二氯乙烯（PVC/PE/PVDC）固体药用复合硬片PVDC涂布量的方法。方法 裁取10 cm×10 cm的样品5片,将样品先在丙酮中浸泡,分离得到PVC层和PE/PVDC复合层。将PE/PVDC复合层于80℃中干燥2 h后,于23℃放置4 h,精密称定。再将PE/PVDC复合层在四氢呋喃中浸泡,使PVDC层溶解在四氢呋喃溶液中,得到PE膜层,于80℃中干燥2 h后,于23℃放置4 h,精密称定,前后2次差值即为PVDV质量（g）。最后计算PVDC涂布量（以g·m^-2表示）。结果 5批样品PVDC涂布量测定结果与标示涂布量均一致,且偏差均在±5%之内。结论 该方法准确、灵敏,适用于PVC/PE/PVDC固体药用复合硬片PVDC涂布量的测定。     

多指标综合评分法优化痛风巴布剂的醇提工艺

目的 优选痛风巴布剂的最佳提取工艺。方法 以青藤碱、总生物碱的含量和干浸膏得率为评价指标,采用正交设计试验,考察乙醇浓度、乙醇用量、提取时间和提取次数对提取结果的影响,确定痛风巴布剂处方药材的最佳提取工艺。结果 痛风巴布剂的最佳提取工艺为65%乙醇,提取3次,每次6倍量溶剂,提取总时间为1.5 h,在该工艺条件下得到的青藤碱含量、总生物碱含量和干浸膏得率分别为2.79 mg·g^-1、1.22%和13.06%。结论 优选的醇提工艺稳定、可行。     

药品自动请领模块的改进与应用效果分析

目的 进一步提高药品自动请领模块的运行效率,降低各药房药品请领后的拒收药品品种数和药品配送过程中的催送药品品种数。方法 分析汇总原有药品自动请领模块的不足之处,改进药品请领数量的计算公式,在根据药品销量请领的基础上又增加了根据药品警戒库存请领窗口和短缺药品优先出库窗口。结果 改进后的药品自动请领模块与之前相比,由于药品自动请领量过大而导致的拒收药品品种数门诊药房由5.70±1.89下降到1.10±0.74,住院药房由1.90±0.99下降到0.30±0.48;药品配送过程中的催送药品品种数门诊药房由1.50±1.08下降到0.20±0.42,住院药房由0.40±0.52下降到0;药房药师对药品自动请领模块的满意度在门诊药房由（85.0±3.39）分上升到（96.8±2.39）分,在住院药房由（85.2±6.38）分上升到（97.6±2.30）分。结论 药品自动请领模块改进后,有效减少了2个药房由于药品自动请模块功能不完善而导致的拒收药品品种数和催送药品品种数,提高了2个药房对药品自动请领模块的满意度。     

反向离子对色谱法测定氨甲苯酸片的含量

目的:建立反向离子对色谱法测定氨甲苯酸片中氨甲苯酸含量的方法。方法:采用Agilent 5TC-C18 150mm×4.6μm色谱柱,用甲醇-0.005mol?L-1的十二烷基硫酸钠溶液（用磷酸调节pH值至3.0）=55:45为流动相,流速1.0mL?min-1,柱温30℃,检测波长226nm。结果:氨甲苯酸在约1.0～0.02mg?mL-1的浓度范围内线性关系良好（r=0.9999）;平均回收率为99.96%,RSD为0.15%（n=9）,样品测定误差<0.1%。结论:本法经方法学验证,可用于氨甲苯酸片的质量控制。     

Triterpenoids with antioxidant activities from Myricaria squamosa

A new triterpenoid, namely myricarin C (compound 1), together with three known compounds myricarin A (compound 2) and myricarin B (compound 3), 3α-hydroxy-D-friedoolean-14-en-28-oic acid (compound 4), was isolated from the overground part of Myricaria squamosa. Compound 2 and compound 3 existed in the solution by the form of cis-trans isomers. Their structures were elucidated by means of extensive spectroscopic methods, including 1D-NMR, 2D-NMR, and HR-ESI-MS. The antioxidant properties of all compounds were calculated based on the DPPH radical scavenging activities. Results showed that myricarin A and myricarin C had general antioxidant activities with EC₅₀ values of 40.90 μg/ml, 42.22 μg/ml, respectively, compared to the control, rutin (5.17 μg/ml). The EC₅₀ values of myricarin B was 195.81 μg/ml. Compound 4 had no antioxidant activities.     

Doxorubicin-conjugated D-glucosamine- and folate- bi-functionalised InP/ZnS quantum dots for cancer cells imaging and therapy

Nanoscaled quantum dots (QDs), with unique optical properties have been used for the development of theranostics. Here, InP/ZnS QDs were synthesised and functionalised with folate (QD-FA), D-glucosamine (QD-GA) or both (QD-FA-GA). The bi-functionalised QDs were further conjugated with doxorubicin (QD-FA-GA-DOX). Optimum Indium to fatty acid (In:MA) ratio was 1:3.5. Transmission electron microscopy (TEM) micrographs revealed spherical morphology for the QDs (11?nm). Energy-dispersive spectroscopy (EDS) spectrum confirmed the chemical composition of the QDs. MTT analysis in the OVCAR-3 cells treated with bare QDs, QD-FA, QD-GA, QD-FA-GA and QD-FA-GA-DOX (0.2?mg/mL of QDs) after 24?h indicated low toxicity for the bare QDs and functionalised QDs (about 80–90% cell viability). QD-FA-GA-DOX nanoparticles elicited toxicity in the cells. Cellular uptake of the engineered QDs were investigated in both folate receptor (FR)-positive OVCAR-3 cells and FR-negative A549 cells using fluorescence microscopy and FACS flow cytometry. The FA-functionalised QDs showed significantly higher uptake in the FR-positive OVCAR-3 cells, nonetheless the GA-functionalised QDs resulted in an indiscriminate uptake in both cell lines. In conclusion, our findings indicated that DOX-conjugated FA-armed QDs can be used as theranostics for simultaneous imaging and therapy of cancer.     

Optimization and evaluation of lyophilized fenofibrate nanoparticles with enhanced oral bioavailability and efficacy

Abstract

The objective of this study was to enhance physiochemical properties as well as oral bioavailability of the poorly water soluble drug fenofibrate (FB), through preparation of amorphous solid dispersions (ASDs). ASDs were prepared via freeze drying using polyvinylpyrrolidone (PVP) K30 and poloxamer 188 as hydrophilic carriers. Formulations were optimized by 3² full factorial design (FFD) with PVP-K30 level (X₁) and poloxamer 188 level (X₂) as independent variables and particle size (Y₁), zeta potential (Y₂), drug content (Y₃) and dissolution rate (T90, [Y₄]) as dependent variables. Optimized FB nanoparticles were physicochemically evaluated and formulated into lyophilized sublingual tablets. Pharmacokinetic, pharmacodynamics and histological finding of optimized formulation were performed on rabbits. Y₁ and Y₄ were significantly affected by independent variables while Y₂ and Y₃ were not affected. Physicochemical characterization showed the drug was in amorphous state, nanometer range and pharmacophore of FB was preserved. Administration of optimized FB tablets to rabbits with fatty liver led to significant reduction (p?<?0.001) in serum lipids. Moreover, histological analysis of liver specimens confirmed the improved efficacy in animals with fatty liver. In this study, we confirmed that ASDs of FB had beneficial effects on managing fatty liver and serum lipids level in hyperlipidemic rabbits.     

Zero-order release and bioavailability enhancement of poorly water soluble Vinpocetine from self-nanoemulsifying osmotic pump tablet

Abstract

Solid self-nanoemulsifying (S-SNEDDS) asymmetrically coated osmotic tablets of the poorly water-soluble drug Vinpocetine (VNP) were designed. The aim was to control the release of VNP by the osmotic technology taking advantage of the solubility and bioavailability-enhancing capacity of S-SNEDDS. Liquid SNEDDS loaded with 2.5?mg VNP composed of Maisine? 35-1, Transcutol^® HP, and Cremophor^® EL was adsorbed on the solid carrier Aeroperl^®. S-SNEDDS was mixed with the osmotic tablet excipients (sodium chloride, Avicel^®, HPMC-K4M, PVP-K30, and Lubripharm^®), then directly compressed to form the core tablet. The tablets were dip coated and mechanically drilled. A 3²*2¹ full factorial design was adopted. The independent variables were: type of coating material (X₁), concentration of coating solution (X₂), and number of drills (X₃). The dependent variables included % release at 2?h (Y₁), at 4?h (Y₂), and at 8?h (Y₃). The in vivo performance of the optimum formula was assessed in rabbits. Zero-order VNP release was obtained by the single drilled 1.5% Opadry^® CA coated osmotic tablets and twofold increase in VNP bioavailability was achieved. The combination of SNEDDS and osmotic pump tablet system was successful in enhancing the solubility and absorption of VNP as well as controlling its release.     

Targeted delivery of hyaluronic acid-coated solid lipid nanoparticles for rheumatoid arthritis therapy

Rheumatoid arthritis (RA) is a chronic, systemic inflammatory disease. Long-term, high-dose glucocorticoid therapy can be used to treat the disease, but the fact that the drug distributes systemically can give rise to severe adverse effects. Here we develop a targeted system for treating RA in which the glucocorticoid prednisolone (PD) is encapsulated within solid lipid nanoparticles (SLNs) coated with hyaluronic acid (HA), giving rise to HA-SLNs/PD. HA binds to hyaluronic receptor CD44, which is over-expressed on the surface of synovial lymphocytes, macrophages and fibroblasts in inflamed joints in RA. As predicted, HA-SLNs/PD particles accumulated in affected joint tissue after intravenous injection into mice with collagen-induced arthritis (CIA), and HA-SLNs/PD persisted longer in circulation and preserved bone and cartilage better than free drug or drug encapsulated in SLNs without HA. HA-SLNs/PD reduced joint swelling, bone erosion and levels of inflammatory cytokines in serum. These results suggest that encapsulating glucocorticoids such as PD in HA-coated SLNs may render them safe and effective for treating inflammatory disorders.