盐酸地芬尼多双层渗透泵片的制备及体外释放研究
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摘要
目的:制备盐酸地芬尼多双层渗透泵片并研究其体外释放特性。方法:采用双层压片技术和薄膜包衣工艺制备盐酸地芬尼多双层渗透泵片,比较其与市售盐酸地芬尼多普通片、自制盐酸地芬尼多单层渗透泵片的体外释放度。结果:盐酸地芬尼多双层渗透泵片处方为盐酸地芬尼多75 mg、氯化钠10 mg、低分子量聚氧乙烯15 mg、5%聚乙烯吡咯烷酮K30乙醇溶液适量;助推层为高分子量聚氧乙烯60 mg、氯化钠20 mg、聚乙烯吡咯烷酮K30 6 mg、硬脂酸镁适量。所制双层渗透泵片12 h累积释放度(Q)达80%,且释放符合零级动力学方程;盐酸地芬尼多普通片的Q15 min达90%,盐酸地芬尼多单层渗透泵片的Q12 h仅为51.14%。结论:所制盐酸地芬尼多双层渗透泵片具有缓释作用,且较单层渗透泵片12 h内释药更完全。
OBJECTIVE:To prepare Diphenidol hydrochloride double-layer osmotic pump tablets,and study its in vitro release characteristics. METHODS:Double-layer compressing technique and film coating technology were conducted to prepare Diphenidol hydrochloride double-layer osmotic pump tablets. The in vitro releases of it,Difenidol hydrochloride tablets in market,self-made Difenidol hydrochloride single-layer osmotic pump tablets were compared. RESULTS:The formulation was as follow as diphenidol hydrochloride 75 mg,sodium chloride 10 mg,low-molecular-weight polyoxyethylene 15 mg and right amounts of 5% PVP K30 ethanol solution. Booster layer was high-molecular-weight polyoxyethylene 60 mg,sodium chloride 20 mg,PVP K30 6 mg,right amounts of magnesium stearate. 12 h cumulative release(Q)of prepared double-layer osmotic pump tablets reached 80%,and the release was in line with zero-order kinetic equation. Q15 minof Difenidol hydrochloride tablets had reached 90%;Q12 hof Difenidol hydrochloride single-layer osmotic pump tablets was only 51.14%. CONCLUSIONS:The prepared Difenidol hydrochloride doublelayer osmotic pump tablets have sustained release effect,with more complete drug release within 12 h than single-layer one.
OBJECTIVE:To prepare Diphenidol hydrochloride double-layer osmotic pump tablets,and study its in vitro release characteristics. METHODS:Double-layer compressing technique and film coating technology were conducted to prepare Diphenidol hydrochloride double-layer osmotic pump tablets. The in vitro releases of it,Difenidol hydrochloride tablets in market,self-made Difenidol hydrochloride single-layer osmotic pump tablets were compared. RESULTS:The formulation was as follow as diphenidol hydrochloride 75 mg,sodium chloride 10 mg,low-molecular-weight polyoxyethylene 15 mg and right amounts of 5% PVP K30 ethanol solution. Booster layer was high-molecular-weight polyoxyethylene 60 mg,sodium chloride 20 mg,PVP K30 6 mg,right amounts of magnesium stearate. 12 h cumulative release(Q)of prepared double-layer osmotic pump tablets reached 80%,and the release was in line with zero-order kinetic equation. Q15 minof Difenidol hydrochloride tablets had reached 90%;Q12 hof Difenidol hydrochloride single-layer osmotic pump tablets was only 51.14%. CONCLUSIONS:The prepared Difenidol hydrochloride doublelayer osmotic pump tablets have sustained release effect,with more complete drug release within 12 h than single-layer one.
引文
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[6]张冠男,白靖,曹德英.尼莫地平双层渗透泵片的制备及其体外释放度考察[J].中国药房,2012,23(29):2740-2743.
[7]Enkhtogtokh B,吴正红,陈钦,等.硝苯地平双层渗透泵片的制备及家兔体内药动学研究[J].药学与临床研究,2011,19(4):302-305.
[8]曹凤习.HPLC法测定盐酸地芬尼多片中杂质的含量[J].中国药师,2011,14(2):203-205.
[9]国家药典委员会.中华人民共和国药典:四部[S].2015年版.北京:中国医药科技出版社,2015:121-124.
[10]曾媛,郑露露,刘辉.盐酸苯环壬酯控释片释放度研究方法的建立[J].中国药师,2015,18(1):11-13.
[11]谢沐风.如何科学、客观地制订溶出度试验质量标准[J].中国医药工业杂志,2012,43(3):243-252.
[2]Murakami K,Inoue N,Fuchikami C,et al.Blockade of voltage-gated calcium channel Cav1.2 and alpha1-adrenoceptors increases vertebral artery blood flow induced by the antivertigo agent difenidol[J].Eur J Pharmacol,2012,689(1/2/3):165-171.
[3]Chen YW,Tzeng JI,Liu KS,et al.Systemic diphenidol reduces neuropathic allodynia and TNF-alpha overexpression in rats after chronic constriction injury[J].Neurosci Lett,2013,doi:10.1016/j.neulet.2013.07.030.
[4]Zhao Z,Wu C,Zhao Y,et al.Development of an oral push-pull osmotic pump of fenofibrate-loaded mesoporous silica nanoparticles[J].Int J Nanomedicine,2015,doi:10.2147/IJN.S76755.
[5]马磊.渗透泵给药系统的研究进展[J].中国药科大学学报,2014,45(6):726-730.
[6]张冠男,白靖,曹德英.尼莫地平双层渗透泵片的制备及其体外释放度考察[J].中国药房,2012,23(29):2740-2743.
[7]Enkhtogtokh B,吴正红,陈钦,等.硝苯地平双层渗透泵片的制备及家兔体内药动学研究[J].药学与临床研究,2011,19(4):302-305.
[8]曹凤习.HPLC法测定盐酸地芬尼多片中杂质的含量[J].中国药师,2011,14(2):203-205.
[9]国家药典委员会.中华人民共和国药典:四部[S].2015年版.北京:中国医药科技出版社,2015:121-124.
[10]曾媛,郑露露,刘辉.盐酸苯环壬酯控释片释放度研究方法的建立[J].中国药师,2015,18(1):11-13.
[11]谢沐风.如何科学、客观地制订溶出度试验质量标准[J].中国医药工业杂志,2012,43(3):243-252.