口感是口腔给药系统(oral drug delivery system,ODDS)制剂处方研究设计的重要内容。传统的感官评价结果严重受制于受试者的个体差异,重现性较差,难以客观量化。鉴于此,介绍了其他学科领域口感评价的一些新技术、新方法,重点对药物在口...口感是口腔给药系统(oral drug delivery system,ODDS)制剂处方研究设计的重要内容。传统的感官评价结果严重受制于受试者的个体差异,重现性较差,难以客观量化。鉴于此,介绍了其他学科领域口感评价的一些新技术、新方法,重点对药物在口腔中的味觉、黏附性、黏膜刺激性、沙砾感等新型评价方法进行了评述,以期为中药ODDS的质量评价及开发利用提供方法学借鉴。展开更多
口腔黏膜给药(oral transmucosal drug delivery)指药物经过口腔黏膜吸收进入体循环而发挥药效,具有生物利用度高、起效快等优势。本文介绍了口腔黏膜的生理特点,详细分析了影响口腔黏膜给药系统药物动力学性质的因素,如口腔生理屏障、...口腔黏膜给药(oral transmucosal drug delivery)指药物经过口腔黏膜吸收进入体循环而发挥药效,具有生物利用度高、起效快等优势。本文介绍了口腔黏膜的生理特点,详细分析了影响口腔黏膜给药系统药物动力学性质的因素,如口腔生理屏障、不同给药部位、药物理化性质、剂型因素和处方因素,阐述了体外渗透性、在体口腔吸收、体内药物动力学以及生理药代动力学模型等研究在口腔黏膜给药系统药物动力学研究中的应用,为口腔黏膜给药系统开发提供方法和借鉴。展开更多
Increasing the degree of supersaturation of drugs and maintaining their proper stability are very important in improving the oral bioavailability of poorly soluble drugs by a supersaturated drug delivery system(SDDS)....Increasing the degree of supersaturation of drugs and maintaining their proper stability are very important in improving the oral bioavailability of poorly soluble drugs by a supersaturated drug delivery system(SDDS). In this study, we reported a complex system of Soluplus–Copovidone(Soluplus–PVPVA)loaded with the model drug silybin(SLB) that could not only maintain the stability of a supersaturated solution but also effectively promote oral absorption. The antiprecipitation effect of the polymers on SLB was observed using the solvent-shift method. In addition, the effects of the polymers on absorption were detected by cellular uptake and transport experiments. The mechanisms by which the Soluplus–PVPVA complex promotes oral absorption were explored by dynamic light scattering, transmission electron microscopy, fluorescence spectra and isothermal titration calorimetry analyses. Furthermore, a pharmacokinetic study in rats was used to demonstrate the advantages of the Soluplus–PVPVA complex. The results showed that Soluplus and PVPVA spontaneously formed complexes in aqueous solution via the adsorption of PVPVA on the hydrophilichydrophobic interface of the Soluplus micelle, and the Soluplus–PVPVA complex significantly increased the absorption of SLB. In conclusion, the Soluplus–PVPVA complex is a potential SDDS for improving the bioavailability of hydrophobic drugs.展开更多
文摘口感是口腔给药系统(oral drug delivery system,ODDS)制剂处方研究设计的重要内容。传统的感官评价结果严重受制于受试者的个体差异,重现性较差,难以客观量化。鉴于此,介绍了其他学科领域口感评价的一些新技术、新方法,重点对药物在口腔中的味觉、黏附性、黏膜刺激性、沙砾感等新型评价方法进行了评述,以期为中药ODDS的质量评价及开发利用提供方法学借鉴。
文摘口腔黏膜给药(oral transmucosal drug delivery)指药物经过口腔黏膜吸收进入体循环而发挥药效,具有生物利用度高、起效快等优势。本文介绍了口腔黏膜的生理特点,详细分析了影响口腔黏膜给药系统药物动力学性质的因素,如口腔生理屏障、不同给药部位、药物理化性质、剂型因素和处方因素,阐述了体外渗透性、在体口腔吸收、体内药物动力学以及生理药代动力学模型等研究在口腔黏膜给药系统药物动力学研究中的应用,为口腔黏膜给药系统开发提供方法和借鉴。
基金supported by the National Natural Science Foundation of China (grant Nos. 81573378 and 81773651)the Shanghai Science and Technology Innovation Action Plan for Basic Research, China (No. 17430741500)
文摘Increasing the degree of supersaturation of drugs and maintaining their proper stability are very important in improving the oral bioavailability of poorly soluble drugs by a supersaturated drug delivery system(SDDS). In this study, we reported a complex system of Soluplus–Copovidone(Soluplus–PVPVA)loaded with the model drug silybin(SLB) that could not only maintain the stability of a supersaturated solution but also effectively promote oral absorption. The antiprecipitation effect of the polymers on SLB was observed using the solvent-shift method. In addition, the effects of the polymers on absorption were detected by cellular uptake and transport experiments. The mechanisms by which the Soluplus–PVPVA complex promotes oral absorption were explored by dynamic light scattering, transmission electron microscopy, fluorescence spectra and isothermal titration calorimetry analyses. Furthermore, a pharmacokinetic study in rats was used to demonstrate the advantages of the Soluplus–PVPVA complex. The results showed that Soluplus and PVPVA spontaneously formed complexes in aqueous solution via the adsorption of PVPVA on the hydrophilichydrophobic interface of the Soluplus micelle, and the Soluplus–PVPVA complex significantly increased the absorption of SLB. In conclusion, the Soluplus–PVPVA complex is a potential SDDS for improving the bioavailability of hydrophobic drugs.
