目的 基于凝膠材料的吸水膨脹、溶蝕及凝膠對藥物擴(kuò)散的阻滯等影響親水凝膠骨架片藥物釋放的關(guān)鍵因素,對國產(chǎn)和進(jìn)口羥丙甲纖維素進(jìn)行系統(tǒng)的比較研究。方法 采用稱重法,考察不同來源羥丙甲纖維素的吸水膨脹、溶蝕等特性的異同;以鹽酸二甲雙胍、托拉塞米、布洛芬為模型藥物,考察不同來源羥丙甲纖維素在不同濃度下對藥物擴(kuò)散所起的阻滯作用的差異。結(jié)果 國產(chǎn)羥丙甲纖維素吸水膨脹速率大于進(jìn)口羥丙甲纖維素,而溶蝕速率小于進(jìn)口羥丙甲纖維素;羥丙甲纖維素溶液對藥物擴(kuò)散的阻滯作用與溶液中羥丙甲纖維素濃度呈正相關(guān),在較低濃度(5 mg/mL)時,國產(chǎn)羥丙甲纖維素與進(jìn)口羥丙甲纖維素對3種模型藥物的阻滯率相當(dāng),而在中等濃度(15 mg/mL)及高濃度(25 mg/mL)時,進(jìn)口羥丙甲纖維素對3種模型藥物的阻滯作用均小于國產(chǎn)羥丙甲纖維素。結(jié)論 相同型號的國產(chǎn)和進(jìn)口羥丙甲纖維素的吸水膨脹、溶蝕及對藥物擴(kuò)散的阻滯等性質(zhì)并不完全一致。

Objective To investigate the water absorption, swelling, erosion of the gel material, and the blocking effect of it on drug diffusion, domestic and imported hydroxypropyl methyl cellulose (HPMC) were systematically compared by the key factor of affecting hydrophilic matrix tablets drug release. Methods A gravimetric method was employed for studying their swelling, erosion, and other characteristics of different sources of HPMC. Metformin hydrochloride, torasemide, and ibuprofen were used as representative drugs to investigate the blocking effect of different HPMC on drug diffusion under different concentration. Results The water absorption and swelling rate of domestic HPMC were more than those of imports HPMC, while the erosion rate of it was less than imports HPMC; The blocking effect of HPMC on drug diffusion was positively correlated with the concentration of HPMC, in addition, the blocking effect of domestic and imports HPMC on three model drugs was basically the same at low concentration (5 mg/mL),while the blocking effect of imports HPMC on three model drugs was lower at a moderate concentration (15 mg/mL) and a high concentration (25 mg/mL). Conclusion The water absorption, swelling, and erosion of HPMC with different models are not entirely consistent, the same as the blocking effect of them on drug diffusion.