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共研磨不仅降低粒度,同时引起分子性质的变化如多晶形的相变换、固相的结晶度及化学反应速率的变化。将结晶药物与微晶纤维素、甲壳素及脱乙酰甲壳素、环糊精、明胶、PVP及甲基纤维素共研磨,难溶药物变无定形,其溶解度和生物利用度显著提高。本文报道萘普生难溶于水,它与β环糊精(β-CD)的固态反应可由X线衍射及红外光谱确定。萘普生与β-CD(1:1克分子)球磨机研磨20分钟即得,在37℃pH1.2的缓冲液中其溶解速率比萘普生或萘普生与β-CD物理混合物大大提高。萘普生80~120分钟溶出
Co-grinding not only reduces particle size, but also causes changes in molecular properties such as polymorphic phase transformation, solid phase crystallinity and chemical reaction rate changes. Crystallization drugs and microcrystalline cellulose, chitin and chitosan, cyclodextrin, gelatin, PVP and methyl cellulose co-grinding, insoluble drugs become amorphous, the solubility and bioavailability significantly increased. This article reports that naproxen is poorly soluble in water and its solid state reaction with β-cyclodextrin (β-CD) can be determined by X-ray diffraction and infrared spectroscopy. Naproxen and [beta] -CD (1: 1 molar) ball mills for 20 minutes resulted in a much greater rate of dissolution than Naproxen or Naproxen and [beta] -CD in 37 [deg.] C buffer at pH 1.2 . Naproxen 80 ~ 120 minutes dissolution