本文關(guān)鍵詞： 布洛芬 乳化法 納米微粉 表征 透皮　出處：《中國藥房》2017年01期 　論文類型：期刊論文

【摘要】：目的:制備布洛芬納米微粉并對其進(jìn)行表征,考察其體外透皮作用。方法:采用乳化法,以氯仿-乙醇(7∶3,V/V)為有機(jī)相、超純水為水相、聚山梨酯80為表面活性劑制備布洛芬納米微粉。利用激光粒度分析方法、掃描電鏡、傅里葉變換紅外光譜、X射線衍射、差示掃描對制備的布洛芬納米微粉進(jìn)行表征。比較布洛芬納米微粉與原料藥的飽和溶解度、體外溶出度和體外透皮率。結(jié)果:確定的處方及制備工藝為聚山梨酯80 5 mg/m L、水相-有機(jī)相體積比40∶1、布洛芬質(zhì)量濃度250 mg/m L、勻漿速度5000 r/min、勻漿時(shí)間2 min。所制布洛芬納米微粉為多孔疏松珊瑚狀,其化學(xué)結(jié)構(gòu)未改變,由原來的晶體態(tài)變?yōu)闊o定形態(tài),粒徑為179.6 nm,載藥量為8.99%;其飽和溶解度、溶出度和透皮率分別是原料藥的148、1.23、4.08倍。結(jié)論:所制布洛芬納米微粉具有良好的水溶性和體外透皮性。
[Abstract]:Objective: to prepare and characterize ibuprofen nano-powder and investigate its transdermal effect in vitro. Methods: the emulsification method was used with chloroform-ethanol 7: 3 V / V) as organic phase and ultrapure water as aqueous phase. The ibuprofen nano-powder was prepared by using polysorbate 80 as surfactant. Laser particle size analysis, scanning electron microscope, Fourier transform infrared spectroscopy (FTIR) and X-ray diffraction (FTIR) were used to prepare ibuprofen nanocrystalline powder. The prepared ibuprofen nano-powder was characterized by differential scanning and the saturation solubility of ibuprofen nano-powder and raw material was compared. Results: the formulation and preparation process were determined as follows: the polysorbate 805 mg/m / L, the volume ratio of aqueous phase to organic phase 40: 1. The ibuprofen nanocrystalline powder prepared by ibuprofen concentration 250 mg/m / L, homogenate speed 5000rmin, homogenate time 2 mins, is porous and loose coral, and its chemical structure remains unchanged. From the original crystal state to the amorphous form, the particle size is 179.6 nm, and the drug load is 8.99 nm; The saturated solubility, dissolution and transdermal rate of ibuprofen were 1.234.08 times of that of the raw drug, respectively. Conclusion: the prepared ibuprofen nano-powder has good water solubility and in vitro transdermal properties.
【作者單位】： 東北林業(yè)大學(xué)森林植物生態(tài)學(xué)教育部重點(diǎn)實(shí)驗(yàn)室;
【基金】：國家自然科學(xué)基金資助項(xiàng)目(No.21473023)
【分類號】：R943
【正文快照】： 布洛芬(異丁苯丙醇,Ibuprofen)是一類非甾體抗炎藥,具有抗炎、鎮(zhèn)痛、解熱作用。臨床上用于輕到中度的偏頭痛發(fā)作期治療和預(yù)防性治療,及各類關(guān)節(jié)和肌肉病變,同時(shí)也用于軀體疼痛、手術(shù)及外傷后的鎮(zhèn)痛[1-3]。但是,由于布洛芬水溶性差,而且口服時(shí)會(huì)引起潰瘍、出血等胃腸道反應(yīng)[4-6

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1 李丹;肖學(xué)成;陳鳳;李金;;過氧化苯甲酰凝膠體外透皮吸收量測定[A];2013年全國醫(yī)藥學(xué)術(shù)交流會(huì)暨臨床藥學(xué)與藥學(xué)服務(wù)研究進(jìn)展培訓(xùn)班論文集[C];2013年

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