Aim Polylactic acid (PLA) or polylactide-co-glycolide (PLGA) was used asbiodegradable and biocom-patible carriers to achieve sustained release ofestradial-PLGA/PLA-Microspheres (E_2-PLGA/PLA-MS). THF was added in the ...Aim Polylactic acid (PLA) or polylactide-co-glycolide (PLGA) was used asbiodegradable and biocom-patible carriers to achieve sustained release ofestradial-PLGA/PLA-Microspheres (E_2-PLGA/PLA-MS). THF was added in the organic phase to study itseffects on the properties of MS. Methods MS were formed by an emulsification-solvent extractionmethod with mixture of ethyl acetate (EtoAc) and tetrahydrofuran (THF) as the organic solvents, andthen the properties and in vitro drug release behavior were examined. Results The results indicatedthat the drug loading efficiency decreased when THF added, but when the ratio of EtoAc was more than50% , there was no obvious effect of THF ratio, but the particle size increased accordingly. Thecarriers' properties and the drug contents were the main factors influencing the in vitro drugrelease. Conclusions By controlling the technology and formulation, we can get sustained-release E_2biodegradable microsperes with proper particle size, drug content and low burst-release, althoughTHF with readily solubility in water was used in the organic phase.展开更多
In the present study,an extended-release(ER)suspension of guanfacine hydrochloride(GFN)was successfully formulated using a self-synthesized cation-exchange resin characterized by a narrow particle size distribution.Th...In the present study,an extended-release(ER)suspension of guanfacine hydrochloride(GFN)was successfully formulated using a self-synthesized cation-exchange resin characterized by a narrow particle size distribution.The drug-resin complex was prepared through a static adsorption method,employing the resin as a pharmaceutical carrier.Subsequently,guanfacine hydrochloride-coated microcapsules(GFN-CM)were fabricated via an emulsion solvent evaporation technique to achieve sustained-release functionality.Characterization revealed that the in-house resin exhibited a smoother surface and a narrower size distribution(Span value:0.74)compared to the commercial counterpart,Amberlite®IRP69.In vitro release studies demonstrated that the GFN-CM followed a zero-order kinetic model over 10 h,with a cumulative drug release of 81.88%observed at 12 h.Furthermore,pharmacokinetic evaluation in New Zealand rabbits showed that the mean residence time(MRT0–24)of the GFN suspension extended from 7.619 to 8.336 h,displaying a more stable plasma concentration-time profile and an average relative bioavailability(Fr)of 111.36% compared to marketed ER GFN tablets.These findings highlighted the successful development of a novel cation exchange resin-based delivery system,offering a promising strategy for enhancing the performance of ER pharmaceutical formulations.展开更多
文摘Aim Polylactic acid (PLA) or polylactide-co-glycolide (PLGA) was used asbiodegradable and biocom-patible carriers to achieve sustained release ofestradial-PLGA/PLA-Microspheres (E_2-PLGA/PLA-MS). THF was added in the organic phase to study itseffects on the properties of MS. Methods MS were formed by an emulsification-solvent extractionmethod with mixture of ethyl acetate (EtoAc) and tetrahydrofuran (THF) as the organic solvents, andthen the properties and in vitro drug release behavior were examined. Results The results indicatedthat the drug loading efficiency decreased when THF added, but when the ratio of EtoAc was more than50% , there was no obvious effect of THF ratio, but the particle size increased accordingly. Thecarriers' properties and the drug contents were the main factors influencing the in vitro drugrelease. Conclusions By controlling the technology and formulation, we can get sustained-release E_2biodegradable microsperes with proper particle size, drug content and low burst-release, althoughTHF with readily solubility in water was used in the organic phase.
基金The Postgraduate Research&Practice Innovation Program of Jiangsu Province(Grant No.SJCX24-2440)the 2021 Zhenjiang sixth“169 project”scientific research projectthe 2023 Qinglan Project of Jiangsu Province,China。
文摘In the present study,an extended-release(ER)suspension of guanfacine hydrochloride(GFN)was successfully formulated using a self-synthesized cation-exchange resin characterized by a narrow particle size distribution.The drug-resin complex was prepared through a static adsorption method,employing the resin as a pharmaceutical carrier.Subsequently,guanfacine hydrochloride-coated microcapsules(GFN-CM)were fabricated via an emulsion solvent evaporation technique to achieve sustained-release functionality.Characterization revealed that the in-house resin exhibited a smoother surface and a narrower size distribution(Span value:0.74)compared to the commercial counterpart,Amberlite®IRP69.In vitro release studies demonstrated that the GFN-CM followed a zero-order kinetic model over 10 h,with a cumulative drug release of 81.88%observed at 12 h.Furthermore,pharmacokinetic evaluation in New Zealand rabbits showed that the mean residence time(MRT0–24)of the GFN suspension extended from 7.619 to 8.336 h,displaying a more stable plasma concentration-time profile and an average relative bioavailability(Fr)of 111.36% compared to marketed ER GFN tablets.These findings highlighted the successful development of a novel cation exchange resin-based delivery system,offering a promising strategy for enhancing the performance of ER pharmaceutical formulations.
