Plasticizing effect of ibuprofen induced an alteration of drug released from Kollidon SR matrices produced by direct compression

The objectives of this study were to investigate the effect of storage temperature on drug release from matrices containing 10, 40 and 70% w/w ibuprofen in Kollidon® SR (KSR). The matrix tablets were produced by direct compression and then kept at 30 and 45?°C for 3 months. Drug release from the matrix tablets was examined after storage for 0, 1, 4 and 12 weeks. Scanning electron microscope was used to reveal physical appearance of the tablet surface at the respective time intervals. In addition, differential scanning calorimeter was used to investigate glass transition temperature (T_g) of ibuprofen in KSR at 0–100% w/w based on the principle of Gordon–Taylor equation. At 45?°C, the dissolution of ibuprofen in KSR as well as the coalescence of polymer particles were observed to be higher than those of storage at 30?°C. The physical state of ibuprofen dispersed in the polymeric matrix and degree of polymer coalescence led to the variation of drug release. The coalescence of polymer particles was a result of the polymer transition from glassy to rubbery state according to water absorption of KSR and plasticizing effect of ibuprofen. The reduction of the T_g of ibuprofen blended with KSR could be better described by the Kwei equation, a modified version of Gordon–Taylor equation.     

羟乙基纤维素接枝聚丙烯酸纳米颗粒的制备及药物缓释

羟乙基纤维素接枝聚丙烯酸共聚物(HEC g PAA)在选择性溶剂中进行自组装,制备了具有良好分散稳定性的纳米颗粒,用动态激光光散射和透射电子显微镜对纳米颗粒大小分布和形态进行了表征.以生物可降解的HEC g PAA接枝共聚物负载模型药物布洛芬(Ibuprofen),制备载药纳米颗粒(Ib HEC g PAA).在37℃于不同pH的缓冲溶液中进行了体外释放研究.药物释放速率的测定结果表明,以HEC g PAA作为布洛芬的载体,可以在选择性条件下实现药物可控释放的目的.     

芳基取代羧酸离子液体结构与摩擦学性能的构效关系研究

目的研究芳基取代羧酸离子液体的分子结构与其摩擦学性能、物理化学性质之间的构效关系。方法分别以4-甲基苯乙酸(4-Me-PA)、4-叔丁基苯乙酸(4-tBu-PA)、4-苯基丁酸(PB)、异丁基苯丙酸钠(布洛芬钠,Ibu)作为阴离子源,以四丁基氢氧化铵(N4444OH)、四丁基氯化铵(N4444Cl)、1-丁基-3-甲基咪唑氯盐(C4mim)、1-辛基-3-甲基咪唑氯盐(C8mim)为阳离子源,通过酸碱中和反应和离子交换反应合成了七种芳基取代羧酸离子液体。以市售合成润滑油聚α-烯烃(PAO10)和传统离子液体1-丁基-3-甲基咪唑四氟硼酸盐(L-B104)为对照样,对其分子结构与摩擦学性能、物理化学性质之间的构效关系进行了系统研究。结果芳基取代羧酸离子液体的热分解温度在161~217℃之间,水解反应的p H值保持不变,具有较高的水解稳定性和热稳定性,对金属基底材料无腐蚀,作为润滑剂使用时,在钢/钢、钢/铜、钢/铝三种摩擦副上的平均摩擦系数f和平均磨损体积V分别为f钢/钢=0.081,f钢/铜=0.067,f钢/铝=0.080,V钢/钢=3.24×10-3 mm3,V钢/铜=22.04×10-3 mm3,V钢/铝=22.35×10-3 mm3,均具有良好的减摩抗磨性能,它们的分子结构对其摩擦学性能和物理化学性质均具有较明显的影响。结论芳基取代羧酸离子液体中,阳离子上取代烷基链越长,其热分解温度越高,运动黏度和黏度指数也越大;阴离子的空间体积越大,相应离子液体的黏度指数越大;它们在钢/钢、钢/铜、钢/铝摩擦副上均表现出良好的润滑作用。这主要是因为在摩擦过程中离子液体在摩擦副表面形成了稳定的吸附膜,在这层吸附膜中,阴阳离子的影响作用不同,阳离子对其减摩作用的影响较大,阴离子对其抗磨作用的影响较大;这层吸附膜的润滑性能还受到黏度的影响,具有适中运动黏度和较大黏度指数的离子液体作为润滑剂,摩擦学性能更加优异。     

Granulation of ibuprofen/isonicotinamide co-crystals by continuous spray granulator (CTS-SGR)

The importance of granulation is paramount for tablet manufacturing, and is based on the fact that granulated powders are characterized by improved flowability, compressibility, segregation, and dust reduction. The aim of this study was to prepare and characterize continuous granules of high drug content by using a continuous-spray granulator (CTS-SGR). Ibuprofen (IBU), a drug of low-flowability, was selected as the model drug. As IBU has a low melting point and cannot easily granulate on its own, we employed isonicotinamide (INA) as a coformer that would allow us to prepare co-crystal granules containing 60 % IBU. The results of the undertaken differential scanning calorimetry and powder X-ray diffraction revealed that the IBU and the INA in the granules formed co-crystals. The granulation conditions affected the particle size and the yield of the granules; in fact, a low air supply temperature, a low atomizing air rate, and a high solution flow rate ensured a high granulation efficiency. Moreover, continuous granulation increased the yields of the formulations compared to those obtained through a short-run granulation, and high yields were obtained after applying a low atomizing air rate. The circularity of the granules exceeded 90 %, and their flowability improved when compared to that of the IBU bulk. The undertaking of dissolution studies revealed no change in the elution amount of IBU as a result of the co-crystallization. Our study shows that it is possible to produce high-content IBU granules in a direct and continuous manner through the co-crystallization of IBU and the use of a CTS-SGR.     

碳气凝胶阴极用于电化学-臭氧体系去除布洛芬的机理试验研究

以天然棉花为前驱物,通过直接一步热解法制备了新型碳纤维气凝胶(CFA)阴极,用于电化学-臭氧技术(E-O3-CFA),通过SEM、BET、XPS等方法对CFA进行成分和结构分析,系统地研究了E-O3-CFA体系对水中布洛芬(IBP)的去除情况,考察了阴极材料、臭氧浓度、电流强度和初始pH值等因素的影响,分析该体系去除I...