Gastro-retentive drug delivery system(GRDDS) has gained immense popularity in the field of oral drug delivery recently. It is a widely employed approach to retain the dosage form in the stomach for an extended period ...Gastro-retentive drug delivery system(GRDDS) has gained immense popularity in the field of oral drug delivery recently. It is a widely employed approach to retain the dosage form in the stomach for an extended period of time and release the drug slowly that can address many challenges associated with conventional oral delivery, including poor bioavailability.Different innovative approaches like magnetic field assisted gastro-retention, plug type swelling system, muco-adhesion technique, floating system with or without effervescence are being applied to fabricate GRDDS. Apart from in vitro characterization, successful GRDDS development demands well designed in vivo study to establish enhanced gastro-retention and prolonged drug release. Gama scintigraphy and MRI are popular techniques to evaluate in vivo gastric residence time. However, checking of their overall in-vivo efficacy still remains a major challenge for this kind of dosage form, especially in small animals like mice or rat.Reported in vivo studies with beagle dogs, rabbits, and human subjects are only a handful in spite of a large number of encouraging in vitro results. In spite of the many advantages,high subject variations in gastrointestinal physiological condition, effect of food, and variable rate of gastric emptying time are the challenges that limit the number of available GRDDS in the market. This review article highlights the in vivo works of GRDDS carried out in the recent past, including their limitations and challenges that need to be overcome in the near future.展开更多
Management of cardiovascular risk factors in diabetes demands special attention due to their co-existence. Pioglitazone （PIO） and telmisartan （TLM） combination can be beneficial in effective control of cardiovascu...Management of cardiovascular risk factors in diabetes demands special attention due to their co-existence. Pioglitazone （PIO） and telmisartan （TLM） combination can be beneficial in effective control of cardiovascular complication in diabetes. In this research, we developed and validated a high throughput LC-MS/MS method for simultaneous quantitation of PIO and TLM in rat plasma. This developed method is more sensitive and can quantitate the analytes in relatively shorter period of time compared to the previously reported methods for their individual quantification. Moreover, till date, there is no bioanalytical method available to simultaneously quantitate PIO and TLM in a single run. The method was validated according to the USFDA guidelines for bioanalytical method validation. A linear response of the analytes was observed over the range of 0.005-10 pg/mL with satisfactory precision and accuracy. Accuracy at four quality control levels was within 94.27%-106.10%. The inlxa- and inter-day precision ranged from 2.32% to 10.14% and 5.02% to 8.12%, respectively. The method was reproducible and sensitive enough to quantitate PIO and TLM in rat plasma samples of a preclinical pharmacokinetic study. Due to the potential of PIO-TLM combination to be therapeutically explored, this method is expected to have significant usefulness in future.展开更多
The methods used for flow characterization of a powder mass include the angle of repose （AOR）, Carr index （CI）, and powder flow tester （PFT）. The use of nanosilica as a flow modifier （glidant） is very common i...The methods used for flow characterization of a powder mass include the angle of repose （AOR）, Carr index （CI）, and powder flow tester （PFT）. The use of nanosilica as a flow modifier （glidant） is very common in industry. This study aims to compare the glidant effect of hydrophobic and hydrophilic silica on a poorly flowable active pharmaceutical ingredient （ibuprofen） by different flow characterization techniques. Different percentages （0.5, 1.0, and 2.0 wt%） of both types of mixed silica–ibuprofen powders were evaluated by the AOR, CI, bulk density, and PFT. The flow factor, effective angle of friction, and cohesion were determined to explain the bulk powder properties. The results show that different types of silica show different levels of flow property improvement, but the techniques do not equally discriminate the differences. Hydrophobic silica results in better improvement of the flow property than hydrophilic silica, probably because of its better surface coverage of silica on the host particles. Change of the bulk density with applied pressure was significant for the different powders. This study demonstrates that combining several characterization methods provides a better understanding of bulk powder flow properties with respect to powder–process relationships than a single flow indicator.展开更多
文摘Gastro-retentive drug delivery system(GRDDS) has gained immense popularity in the field of oral drug delivery recently. It is a widely employed approach to retain the dosage form in the stomach for an extended period of time and release the drug slowly that can address many challenges associated with conventional oral delivery, including poor bioavailability.Different innovative approaches like magnetic field assisted gastro-retention, plug type swelling system, muco-adhesion technique, floating system with or without effervescence are being applied to fabricate GRDDS. Apart from in vitro characterization, successful GRDDS development demands well designed in vivo study to establish enhanced gastro-retention and prolonged drug release. Gama scintigraphy and MRI are popular techniques to evaluate in vivo gastric residence time. However, checking of their overall in-vivo efficacy still remains a major challenge for this kind of dosage form, especially in small animals like mice or rat.Reported in vivo studies with beagle dogs, rabbits, and human subjects are only a handful in spite of a large number of encouraging in vitro results. In spite of the many advantages,high subject variations in gastrointestinal physiological condition, effect of food, and variable rate of gastric emptying time are the challenges that limit the number of available GRDDS in the market. This review article highlights the in vivo works of GRDDS carried out in the recent past, including their limitations and challenges that need to be overcome in the near future.
文摘Management of cardiovascular risk factors in diabetes demands special attention due to their co-existence. Pioglitazone （PIO） and telmisartan （TLM） combination can be beneficial in effective control of cardiovascular complication in diabetes. In this research, we developed and validated a high throughput LC-MS/MS method for simultaneous quantitation of PIO and TLM in rat plasma. This developed method is more sensitive and can quantitate the analytes in relatively shorter period of time compared to the previously reported methods for their individual quantification. Moreover, till date, there is no bioanalytical method available to simultaneously quantitate PIO and TLM in a single run. The method was validated according to the USFDA guidelines for bioanalytical method validation. A linear response of the analytes was observed over the range of 0.005-10 pg/mL with satisfactory precision and accuracy. Accuracy at four quality control levels was within 94.27%-106.10%. The inlxa- and inter-day precision ranged from 2.32% to 10.14% and 5.02% to 8.12%, respectively. The method was reproducible and sensitive enough to quantitate PIO and TLM in rat plasma samples of a preclinical pharmacokinetic study. Due to the potential of PIO-TLM combination to be therapeutically explored, this method is expected to have significant usefulness in future.
文摘The methods used for flow characterization of a powder mass include the angle of repose （AOR）, Carr index （CI）, and powder flow tester （PFT）. The use of nanosilica as a flow modifier （glidant） is very common in industry. This study aims to compare the glidant effect of hydrophobic and hydrophilic silica on a poorly flowable active pharmaceutical ingredient （ibuprofen） by different flow characterization techniques. Different percentages （0.5, 1.0, and 2.0 wt%） of both types of mixed silica–ibuprofen powders were evaluated by the AOR, CI, bulk density, and PFT. The flow factor, effective angle of friction, and cohesion were determined to explain the bulk powder properties. The results show that different types of silica show different levels of flow property improvement, but the techniques do not equally discriminate the differences. Hydrophobic silica results in better improvement of the flow property than hydrophilic silica, probably because of its better surface coverage of silica on the host particles. Change of the bulk density with applied pressure was significant for the different powders. This study demonstrates that combining several characterization methods provides a better understanding of bulk powder flow properties with respect to powder–process relationships than a single flow indicator.
