Three new alkyl substituted anthraquinone derivatives, trivially named as symploquinones A-C(Compounds 1-3) were isolated from Symplocos racemosa. The structures of these compounds were determined on the basis of exte...Three new alkyl substituted anthraquinone derivatives, trivially named as symploquinones A-C(Compounds 1-3) were isolated from Symplocos racemosa. The structures of these compounds were determined on the basis of extensive spectroscopic analyses(UV, IR, Mass, ~1 H-and ^(13)C-NMR, and two-dimensional(2D) NMR techniques). The resulting data were also compared with the reported literature. These compounds were then subjected to antibacterial or antibiofilm testing. Compounds 1 and 3 exhibited good antibacterial activity in the concentration range of 160-83 μg·m L^(-1) against Streptococcus mutans, methicillin resistant Staphylococcus aureus and Proteus mirabilis. Both compounds were further screened for anti-biofilm activity, which revealed promising activities at sub-MIC concentrations. None of the compounds were found to be active against Klebsiella pneumoniae.展开更多
This study involves mathematical simulation model such as in vitro-in vivo correlation(IVIVC) development for various extended release formulations of nimesulide loaded hydroxypropylmethylcellulose(HPMC) microparticle...This study involves mathematical simulation model such as in vitro-in vivo correlation(IVIVC) development for various extended release formulations of nimesulide loaded hydroxypropylmethylcellulose(HPMC) microparticles(M1,M2 and M3 containing 1,2,and 3 g HPMC,respectively and 1 g drug in each) having variable release characteristics.In vitro dissolution data of these formulations were correlated to their relevant in vivo absorption profiles followed by predictability worth analysis of these Level A IVIVC.Nimaran was used as control formulation to validate developed formulations and their respective models.The regression coefficients of IVIVC plots for M1,M2,M3 and Nimaran were 0.834 9,0.831 2,0.927 2 and 0.898 1,respectively.The internal prediction error for all formulations was within limits,i.e.,<10%.A good IVIVC was found for controlled release nimesulide loaded HPMC floating M3 microparticles.In other words,this mathematical simulation model is best fit for biowaiver studies which involves study parameters as those adopted for M3 because the value of its IVIVC regression coefficient is the closest to 1 as compared to M1 and M2.展开更多
基金supported by Higher Education Commission(HEC)of Pakistan for financial support under NRPU programme(No.20-2003/NRPU)COMSATS Abbottabad for financial support
文摘Three new alkyl substituted anthraquinone derivatives, trivially named as symploquinones A-C(Compounds 1-3) were isolated from Symplocos racemosa. The structures of these compounds were determined on the basis of extensive spectroscopic analyses(UV, IR, Mass, ~1 H-and ^(13)C-NMR, and two-dimensional(2D) NMR techniques). The resulting data were also compared with the reported literature. These compounds were then subjected to antibacterial or antibiofilm testing. Compounds 1 and 3 exhibited good antibacterial activity in the concentration range of 160-83 μg·m L^(-1) against Streptococcus mutans, methicillin resistant Staphylococcus aureus and Proteus mirabilis. Both compounds were further screened for anti-biofilm activity, which revealed promising activities at sub-MIC concentrations. None of the compounds were found to be active against Klebsiella pneumoniae.
基金Higher Education Commission of Pakistan for proving financial support for research.
文摘This study involves mathematical simulation model such as in vitro-in vivo correlation(IVIVC) development for various extended release formulations of nimesulide loaded hydroxypropylmethylcellulose(HPMC) microparticles(M1,M2 and M3 containing 1,2,and 3 g HPMC,respectively and 1 g drug in each) having variable release characteristics.In vitro dissolution data of these formulations were correlated to their relevant in vivo absorption profiles followed by predictability worth analysis of these Level A IVIVC.Nimaran was used as control formulation to validate developed formulations and their respective models.The regression coefficients of IVIVC plots for M1,M2,M3 and Nimaran were 0.834 9,0.831 2,0.927 2 and 0.898 1,respectively.The internal prediction error for all formulations was within limits,i.e.,<10%.A good IVIVC was found for controlled release nimesulide loaded HPMC floating M3 microparticles.In other words,this mathematical simulation model is best fit for biowaiver studies which involves study parameters as those adopted for M3 because the value of its IVIVC regression coefficient is the closest to 1 as compared to M1 and M2.
