The objective of this study is to investigate the feasibility of using chitosanesodium alginate(CSeSA)based matrix tablets for extended-release of highly water-soluble drugs by changing formulation variables.Using tri...The objective of this study is to investigate the feasibility of using chitosanesodium alginate(CSeSA)based matrix tablets for extended-release of highly water-soluble drugs by changing formulation variables.Using trimetazidine hydrochloride(TH)as a water-soluble model drug,influence of dissolution medium,the amount of CSeSA,the CS:SA ratio,the type of SA,the type and amount of diluents,on in vitro drug release from CSeSA based matrix tablets were studied.Drug release kinetics and release mechanisms were elucidated.In vitro release experiments were conducted in simulated gastric fluid(SGF)followed by simulated intestinal fluid(SIF).Drug release rate decreased with the increase of CSeSA amount.CS:SA ratio had only slight effect on drug release and no influence of SA type on drug release was found.On the other hand,a large amount of water-soluble diluents could modify drug release profiles.It was found that drug release kinetics showed the best fit to Higuchi equation with Fickian diffusion as the main release mechanism.In conclusion,this study demonstrated that it is possible to design extended-release tablets of watersoluble drugs using CSeSA as the matrix by optimizing formulation components,and provide better understanding about drug release from CSeSA matrix tablets.展开更多
The scientific concept of probiotics has been widely accepted throughout the last decades; consequently, its industrial production and commercialization have been increased. This is only the beginning since a recent g...The scientific concept of probiotics has been widely accepted throughout the last decades; consequently, its industrial production and commercialization have been increased. This is only the beginning since a recent global probiotic market analysis estimated an annual growth, boosted mainly by a rising request from the Asian and European consumer in the next 5 years. So the pharmaceutical industry needs to develop new dosage forms containing probiotic microorganisms in order to offer consumers a variety of products. Different kinds of matrix tablets with Lactobacillus coryniformis CECT 5711 were designed to protect this strain from the technological process and harsh gastrointestinal conditions up until their arrival in the gut, as well as environmental conditions during their storage. With this aim, various retarding polymers were combined so as to get controlled release tablets. All formulations were evaluated in terms of technological processability, bacterial viability and stability. Finally, an optimal formulation with Methocel K-15 M EP, Eudragit L-100 and alginate sodium, which contain Lactobacillus coryniformis CECT 5711, was selected due to the fact that it assured an excellent survival of the microorganisms after their exposition to all conditions mentioned above, besides it will be able to improve human＇s health.展开更多
A novel floating osmotic pump controlled release system （FOP） and traditional matrix sustained release tablets （MT） of dipyridamole （DIP） were characterized in terms of pharmacokinetics, drug release, and in vit...A novel floating osmotic pump controlled release system （FOP） and traditional matrix sustained release tablets （MT） of dipyridamole （DIP） were characterized in terms of pharmacokinetics, drug release, and in vitro-in vivo correlation. In vivo study was performed by a three-crossover study in six beagle dogs relative to the conventional tablet （CT）. A HPLC method for the determination of DIP in the plasma was developed. Cumulative percent of absorption fraction was compared to that of in vitro cumulative release. Both FOP and MT displayed obvious extended release characteristic in vivo while FOP showed a better extended release behavior. The bioavailability of FOP was higher than that of MT and a zero-order release linear correlation of DIP between fraction absorbed in vivo and fraction dissolved in vitro was established for FOP while not for MT. The results indicated the existence of an absorption window in upper part of the GI track of DIP, which meant that floating system could be excellent for the drug delivery. In addition, the in vitro model was a good choice for depicting in vivo absorption and for optimization of the formulation of FOP if it is needed to be bio-equivalent to MT.展开更多
基金supported by Liaoning Institutions excellent talents support plan(No.LR2013047).
文摘The objective of this study is to investigate the feasibility of using chitosanesodium alginate(CSeSA)based matrix tablets for extended-release of highly water-soluble drugs by changing formulation variables.Using trimetazidine hydrochloride(TH)as a water-soluble model drug,influence of dissolution medium,the amount of CSeSA,the CS:SA ratio,the type of SA,the type and amount of diluents,on in vitro drug release from CSeSA based matrix tablets were studied.Drug release kinetics and release mechanisms were elucidated.In vitro release experiments were conducted in simulated gastric fluid(SGF)followed by simulated intestinal fluid(SIF).Drug release rate decreased with the increase of CSeSA amount.CS:SA ratio had only slight effect on drug release and no influence of SA type on drug release was found.On the other hand,a large amount of water-soluble diluents could modify drug release profiles.It was found that drug release kinetics showed the best fit to Higuchi equation with Fickian diffusion as the main release mechanism.In conclusion,this study demonstrated that it is possible to design extended-release tablets of watersoluble drugs using CSeSA as the matrix by optimizing formulation components,and provide better understanding about drug release from CSeSA matrix tablets.
文摘The scientific concept of probiotics has been widely accepted throughout the last decades; consequently, its industrial production and commercialization have been increased. This is only the beginning since a recent global probiotic market analysis estimated an annual growth, boosted mainly by a rising request from the Asian and European consumer in the next 5 years. So the pharmaceutical industry needs to develop new dosage forms containing probiotic microorganisms in order to offer consumers a variety of products. Different kinds of matrix tablets with Lactobacillus coryniformis CECT 5711 were designed to protect this strain from the technological process and harsh gastrointestinal conditions up until their arrival in the gut, as well as environmental conditions during their storage. With this aim, various retarding polymers were combined so as to get controlled release tablets. All formulations were evaluated in terms of technological processability, bacterial viability and stability. Finally, an optimal formulation with Methocel K-15 M EP, Eudragit L-100 and alginate sodium, which contain Lactobacillus coryniformis CECT 5711, was selected due to the fact that it assured an excellent survival of the microorganisms after their exposition to all conditions mentioned above, besides it will be able to improve human＇s health.
文摘A novel floating osmotic pump controlled release system （FOP） and traditional matrix sustained release tablets （MT） of dipyridamole （DIP） were characterized in terms of pharmacokinetics, drug release, and in vitro-in vivo correlation. In vivo study was performed by a three-crossover study in six beagle dogs relative to the conventional tablet （CT）. A HPLC method for the determination of DIP in the plasma was developed. Cumulative percent of absorption fraction was compared to that of in vitro cumulative release. Both FOP and MT displayed obvious extended release characteristic in vivo while FOP showed a better extended release behavior. The bioavailability of FOP was higher than that of MT and a zero-order release linear correlation of DIP between fraction absorbed in vivo and fraction dissolved in vitro was established for FOP while not for MT. The results indicated the existence of an absorption window in upper part of the GI track of DIP, which meant that floating system could be excellent for the drug delivery. In addition, the in vitro model was a good choice for depicting in vivo absorption and for optimization of the formulation of FOP if it is needed to be bio-equivalent to MT.
