克拉霉素掩味颗粒的制备及评价
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摘要
制备克拉霉素掩味颗粒并对其进行评价。通过流化床包衣和造粒工艺制备克拉霉素掩味颗粒。对样品在不同pH溶出介质的溶出度进行分析,通过傅里叶红外光谱、热分析、扫描电镜及X-射线粉末衍射对样品和物理混合物(克拉霉素+卡波姆+邻苯二甲酸羟丙甲基纤维素酯)进行分析,比较两者差异,通过志愿者对掩味效果进行评价。通过该工艺制备的克拉霉素颗粒体外释放度良好,掩味效果优异。制备的克拉霉素掩味颗粒的耐酸性较好,与美国市售制剂相比溶出度相似性较高,并且该工艺能应用于工业化生产。
Clarithromycin taste masked granules were prepared and evaluated.Clarithromycin taste masked granules were prepared by combination of fluid-bed coating procedure with palletization. The final products were evaluated by dissolution in different solution,FT-IR( KBr),DSC,SEM,X-Ray diffraction,and taste evaluation. The Clarithromycin granules prepared by this process has good dissolution and excellent masking effect.Clarithromycin masked granules have good resistance and high similarity for the in vitro dissolution compared with the commercial preparations in United States,and the process can be applied to industrial production.
Clarithromycin taste masked granules were prepared and evaluated.Clarithromycin taste masked granules were prepared by combination of fluid-bed coating procedure with palletization. The final products were evaluated by dissolution in different solution,FT-IR( KBr),DSC,SEM,X-Ray diffraction,and taste evaluation. The Clarithromycin granules prepared by this process has good dissolution and excellent masking effect.Clarithromycin masked granules have good resistance and high similarity for the in vitro dissolution compared with the commercial preparations in United States,and the process can be applied to industrial production.
引文
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[9]ALEKSANDRA A,MARTA S,PATRYCJA C,et al.Characterization and taste masking evaluation of microparticles with cetirizine dihydrochloride and methacrylate-based copolymer obtained by spray drying[J]. Acta Pharm.,2017,67(1):113-124.
[10]DIONYSIOS D D,ANDREAS G,SILKE S.Development and evaluation of cetirizine HCl taste-masked oral disintegrating tablets[J]. AAPS Pharm. Sci. Tech.,2011,12(1):141-151.
[11]ZHANG T,WANG C R,SHEN S.Preparation and evaluation of enteric-coated and taste masking clarithromycin granules[J]. Acta Pharm. Sin. B,2011,46(12):1 520-1 525.
[12]MOHAMMED M,JOSHUA S B,BABUR Z C,et al. A review on the taste masking of bitter APIs:hot-melt extrusion(HME)evaluation[J]. Drug. Dev. Ind. Pharm.,2014,40(2):1-12.
[13]JOSEPH T M,MANJEET P,JUN-BOM P.The effects of screw configuration and polymeric carriers on hot-melt extruded taste-masked formulations incorporated into orally disintegrating tablets[J]. J. Pharm. Sci.,2015,104(1):124-134.
[14]HU L D,LIU W,LI L,et al.Preparation and in vitro,in vivo evaluation of clarithromycin microcapsules[J]. J.Basic Clin.Pharm.,2011,2(1):1-9.
[2]INUKAI K,TAKIYAMA K,NOGUCHI S,et al.Effect of gel formation on the dissolution behavior of clarithromycin tablets[J].Int.J.Pharm.,2017,521(1-2):33-39.
[3]ETSUO Y,SHINICHI K,SHUEI M,et al.Physicochemical properties of amorphous clarithromycin obtained by grinding and spray drying[J].Eur. J. Pharm. Sci.,1999,7(4):331-338.
[4]MOHD N M,MICHELLE D P,VALERIE B,et al.Acidcatalyzed degradation of clarithromycin and erythromycin B:a comparative study using NMR spectroscopy[J]. J.Med.Chem.,2000,43(3):467-474.
[5]KIRAN B,SHAFI S,DIVYAKUMAR B.Taste mask,design and evaluation of an oral formulation using ion exchange resin as drug carrier[J]. AAPS Pharm. Sci. Tech.,2008,9(2):557-562.
[6]GUPTA M M,NIRAJ G,BHUPENDRA S C,et al. Fast disintegrating combination tablet of taste masked levocetrizine dihydrochloride and montelukast sodium:formulation design,development and characterization[J]. J.Pharm.,2014,2 014:1-15.
[7]MURALIDHAR N,CHANDRA S R G,PRABHAKAR R V. Formulation and evaluation of gastroretentive dosage forms of clarithromycin[J].AAPS Pharm.Sci.Tech.,2008,9(1):231-237.
[8]DIVYAKUMAR B,PRIYANKA B,KIRAN B.Taste masking by spray drying technique[J]. AAPS Pharm. Sci.Tech.,2008,9(4):1 159-1 164.
[9]ALEKSANDRA A,MARTA S,PATRYCJA C,et al.Characterization and taste masking evaluation of microparticles with cetirizine dihydrochloride and methacrylate-based copolymer obtained by spray drying[J]. Acta Pharm.,2017,67(1):113-124.
[10]DIONYSIOS D D,ANDREAS G,SILKE S.Development and evaluation of cetirizine HCl taste-masked oral disintegrating tablets[J]. AAPS Pharm. Sci. Tech.,2011,12(1):141-151.
[11]ZHANG T,WANG C R,SHEN S.Preparation and evaluation of enteric-coated and taste masking clarithromycin granules[J]. Acta Pharm. Sin. B,2011,46(12):1 520-1 525.
[12]MOHAMMED M,JOSHUA S B,BABUR Z C,et al. A review on the taste masking of bitter APIs:hot-melt extrusion(HME)evaluation[J]. Drug. Dev. Ind. Pharm.,2014,40(2):1-12.
[13]JOSEPH T M,MANJEET P,JUN-BOM P.The effects of screw configuration and polymeric carriers on hot-melt extruded taste-masked formulations incorporated into orally disintegrating tablets[J]. J. Pharm. Sci.,2015,104(1):124-134.
[14]HU L D,LIU W,LI L,et al.Preparation and in vitro,in vivo evaluation of clarithromycin microcapsules[J]. J.Basic Clin.Pharm.,2011,2(1):1-9.