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| 1 | Investigating the molecular dissolution process of binary solid dispersions by molecular dynamics simulations显示文摘Dissolution molecular mechanism of solid dispersions still remains unclear despite thousands of reports about this technique. The aim of current research was to investigate the molecular dissolution mechanism of solid dispersions by molecular dynamics simulations. The formation of ibuprofen/polymer solid dispersions was modeled by the simulated annealing method. After that, the models of solid dispersions were immersed into the water box with 25–30 ? thicknesses and 50–100 ns MD simulations were performed to all systems.Simulation results showed various dissolution behaviors in different particle sizes and various polymers of solid dispersions. Small-sized particles of solid dispersions dissolved quickly in the water, while the large particles of PEG or PVP-containing solid dispersions gradually swelled in the dissolution process and drug molecules may aggregate together. In the dissolution process, the carboxylic groups of ibuprofen molecules turned its direction from polymer molecules to external water box and then the drug molecules left the polymer coils.At the same time, polymer coils gradually relaxed and became free polymer chains in the solution. In addition, solid dispersion with poloxamer could prevent the precipitate of drug molecules in the dissolution process, which is different from those of PEG or PVPcontaining systems. This research provided us clear images of dissolution process of solid dispersions at the molecular level. | TengIan Chan Defang Ouyang | 2018 | Asian Journal of Pharmaceutical Sciences2018，13，3： | 1 |
| 2 | Hot melt extrusion: An application for enhancing drug solubility显示文摘Low aqueous solubility of API is a problem of drug product development.There are several methods to enhance drug solubility.Although drugs can increase solubility using many chemical and physical modifications,the few methods are able to enhance drug solubility for industrial scale[1].Hot-melt extrusion is one reliable process for enhancing drug solubility in a large scale production.It has been recognized as a one step process with several advantages.It can not only increase solubility of drug,but can also be used as a process to prepare controlled release dosage forms.Using a biodegradable polymer with hot-melt extrusion,the drug release of up to 1–6 months can be achieved[2]. | Duangratana Shuwisitkul | 2016 | Asian Journal of Pharmaceutical Sciences2016，11，1： | 0 |
| 3 | Development and characterization of nifedipine-amino methacrylate copolymer solid dispersion powders with various adsorbents显示文摘Solid dispersions of nifedipine(NDP), a poorly water-soluble drug, and amino methacrylate copolymer(AMCP) with aid of adsorbent, that is, fumed silica, talcum, calcium carbonate,titanium dioxide, and mesoporous silica from rice husks(SRH), were prepared by solvent method. The physicochemical properties of solid dispersions, compared to their physical mixtures, were determined using powder X-ray diffractometry(PXRD) and differential scanning calorimetry(DSC). The surface morphology of the prepared solid dispersions was examined by scanning electron microscopy(SEM). The dissolution of NDP from solid dispersions was compared to NDP powders. The effect of adsorbent type on NDP dissolution was also examined. The dissolution of NDP increased with the ratio of NDP:AMCP:adsorbent of 1:4:1 when compared to the other formulations. As indicated from PXRD patterns, DSC thermograms and SEM images, NDP was molecularly dispersed within polymer carrier or in an amorphous form, which confirmed the better dissolution of solid dispersions. Solid dispersions containing SRH provided the highest NDP dissolution, due to a porous nature of SRH, allowing dissolved drug to fill in the pores and consequently dissolve in the medium.The results suggested that solid dispersions containing adsorbents(SRH in particular) demonstrated improved dissolution of poorly water-soluble drug when compared to NDP powder. | Yotsanan Weerapol Sontaya Limmatvapirat Jurairat Nunthanid Srisuda Konthong Supakij Suttiruengwong Pornsak Sriamornsak | 2017 | Asian Journal of Pharmaceutical Sciences2017，12，4： | 0 |
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