Aim In this study, compound metformin/glipizide bilayer extended release tablets were formulated with hydroxypropyl methylcellulose （HPMC） by wet granulation technique in order to tackle the problems associated with...Aim In this study, compound metformin/glipizide bilayer extended release tablets were formulated with hydroxypropyl methylcellulose （HPMC） by wet granulation technique in order to tackle the problems associated with the muhidrug therapy of non-insulin dependent diabetes mellitus. Me^ls High-dose metformin is difficult to formulate into a tablet dosage form due to its poor compressibility and compactibility. In this study, the way to overcome the difficulty was to utilize stearic alcohol to prepare the tablet formulation. The influences of viscosity, amount of HPMC, and weight of fillers were investigated. The optimal formulation had acceptable physicochemical properties and released metformin and glipizide over 10 h. Results The data of metformin obtained from in vitro release fitted Higuchi kinetics best, while the release of glipizide in vitro was found to follow zero kinetics. Conclusion Compound metformin/glipizide bilayer extended release tablets have been successfully developed.展开更多
A tablet matrix system was developed for ibuprofen and the influence of the polymer blend and concentration on the release rate of the drug was evaluated.Tablets containing different concentrations of calcium silicate...A tablet matrix system was developed for ibuprofen and the influence of the polymer blend and concentration on the release rate of the drug was evaluated.Tablets containing different concentrations of calcium silicate and PVP(polyvinyl pyrrolidone)were prepared using direct compression and the weight uniformity,crushing strength,friability,drug content uniformity,dissolution profile,and in vitro release kinetics were examined.Formulated tablets were found to be within the official acceptable limits of physical and chemical parameters except for the thickness test that was below the conformation of extended-release tablets.The crushing strength of the tablets was in the range of 2.5 to 5.6 kg/f,the weight variations of the tablets of all the formulation was less than±5%.The friability of all the formulations was in the range of 0.6%to 1.83%.Tablet thickness and diameter was in range of 3.18 mm to 4.48 mm and 12.53 mm to 12.64 mm respectively.Absolute drug contents of all the formulations were found to be in range of 83.50%to 98%.The release kinetic of F3 containing 20 mg of calcium silicate,40 mg of PVP as matrix formers showed the best linearity(r^2=0.6975)with%drug release of 96 showing that combination of the two polymers(20 mg calcium silicate and 40 mg PVP)for use as a matrix former is best for extended-release formulation of ibuprofen.展开更多
We hypothesize that a cylinder implant made of multilayer Poly-lactic-co-glycolic-acid (PLGA) membrane can be a method for controlled and extended drug release. We fashioned a multilayer cylindrical implant termed STI...We hypothesize that a cylinder implant made of multilayer Poly-lactic-co-glycolic-acid (PLGA) membrane can be a method for controlled and extended drug release. We fashioned a multilayer cylindrical implant termed STID100 that released doxorubicin for 3 weeks in an orthotopic 4T1 breast cancer model in Balb/C mice. This implant starts as a thin doxorubicin-embedded PLGA membrane, and is then rolled into a cylinder containing an air gap between the membrane layers. Its controlled sustained release delivered 2× the amount of the intravenous (IV) equivalent of doxorubicin, inhibited the primary tumor, and prevented lung metastasis. Importantly it did not cause weight loss, splenomegaly, or cardiac toxicity vs systemically administrated doxorubicin. This favorable safety profile is further substantiated by the finding of no detectable plasma doxorubicin in multiple time points during the 3-week period, and low tumor doxorubicin concentration. The implant system delivered to the specification of an ideal pharmacological paradigm might offer a better coverage of the local tumor, significantly preventing metastatic spread with less drug toxicity to many vital organs, compared to the traditional pharmacology of IV route. The profile of STID made it an attractive therapeutic alternative in metastatic tumor prevention, pain management and many other diverse clinical scenarios.展开更多
文摘Aim In this study, compound metformin/glipizide bilayer extended release tablets were formulated with hydroxypropyl methylcellulose （HPMC） by wet granulation technique in order to tackle the problems associated with the muhidrug therapy of non-insulin dependent diabetes mellitus. Me^ls High-dose metformin is difficult to formulate into a tablet dosage form due to its poor compressibility and compactibility. In this study, the way to overcome the difficulty was to utilize stearic alcohol to prepare the tablet formulation. The influences of viscosity, amount of HPMC, and weight of fillers were investigated. The optimal formulation had acceptable physicochemical properties and released metformin and glipizide over 10 h. Results The data of metformin obtained from in vitro release fitted Higuchi kinetics best, while the release of glipizide in vitro was found to follow zero kinetics. Conclusion Compound metformin/glipizide bilayer extended release tablets have been successfully developed.
文摘A tablet matrix system was developed for ibuprofen and the influence of the polymer blend and concentration on the release rate of the drug was evaluated.Tablets containing different concentrations of calcium silicate and PVP(polyvinyl pyrrolidone)were prepared using direct compression and the weight uniformity,crushing strength,friability,drug content uniformity,dissolution profile,and in vitro release kinetics were examined.Formulated tablets were found to be within the official acceptable limits of physical and chemical parameters except for the thickness test that was below the conformation of extended-release tablets.The crushing strength of the tablets was in the range of 2.5 to 5.6 kg/f,the weight variations of the tablets of all the formulation was less than±5%.The friability of all the formulations was in the range of 0.6%to 1.83%.Tablet thickness and diameter was in range of 3.18 mm to 4.48 mm and 12.53 mm to 12.64 mm respectively.Absolute drug contents of all the formulations were found to be in range of 83.50%to 98%.The release kinetic of F3 containing 20 mg of calcium silicate,40 mg of PVP as matrix formers showed the best linearity(r^2=0.6975)with%drug release of 96 showing that combination of the two polymers(20 mg calcium silicate and 40 mg PVP)for use as a matrix former is best for extended-release formulation of ibuprofen.
文摘We hypothesize that a cylinder implant made of multilayer Poly-lactic-co-glycolic-acid (PLGA) membrane can be a method for controlled and extended drug release. We fashioned a multilayer cylindrical implant termed STID100 that released doxorubicin for 3 weeks in an orthotopic 4T1 breast cancer model in Balb/C mice. This implant starts as a thin doxorubicin-embedded PLGA membrane, and is then rolled into a cylinder containing an air gap between the membrane layers. Its controlled sustained release delivered 2× the amount of the intravenous (IV) equivalent of doxorubicin, inhibited the primary tumor, and prevented lung metastasis. Importantly it did not cause weight loss, splenomegaly, or cardiac toxicity vs systemically administrated doxorubicin. This favorable safety profile is further substantiated by the finding of no detectable plasma doxorubicin in multiple time points during the 3-week period, and low tumor doxorubicin concentration. The implant system delivered to the specification of an ideal pharmacological paradigm might offer a better coverage of the local tumor, significantly preventing metastatic spread with less drug toxicity to many vital organs, compared to the traditional pharmacology of IV route. The profile of STID made it an attractive therapeutic alternative in metastatic tumor prevention, pain management and many other diverse clinical scenarios.
