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Zhang Z.-B.,Beijing University of Chemical Technology | Zhang Z.-B.,Beijing Winsunny Pharmaceutical Co. | Xie M.-L.,Beijing Winsunny Pharmaceutical Co. | Kuang Y.-Y.,Beijing University of Chemical Technology | And 4 more authors.
Chemical Engineering and Processing: Process Intensification | Year: 2016

For many water insoluble acidic or alkaline drugs, amorphization and nanonization represent an effective bioavailability enhancement strategy. Cefixime (CFX) was chosen as a model drug, and amorphous nanoparticles were prepared via a typical process intensification technology: high-gravity reactive precipitation (HGRP). The effects of temperature, rotating speed, overall flow rate, and drug concentration on the particle size and size distribution were investigated. Under the optimum conditions, spherical nanoparticles with a mean size of 45 nm could be precipitated. After filtration, redispersion and spray-drying processes, the obtained CFX nano-powder showed a good stability and exhibited a tremendously enhanced saturation solubility, reaching ~11 times higher than that of raw CFX. Furthermore, CFX nano-powder achieved 100% drug dissolution within 2 min while raw CFX did not dissolve completely after 45 min. Since the production capacity of lab-scale RPB reached 2.3 kg/h, HGRP method might offer a general platform for mass production of drug nanoparticles without the use of organic solvents and pharmaceutical additives. © 2016 Elsevier B.V.


Kuang Y.-Y.,Beijing University of Chemical Technology | Kuang Y.-Y.,Beijing Winsunny Pharmaceutical Co. | Zhang Z.-B.,Beijing Winsunny Pharmaceutical Co. | Xie M.-L.,Beijing Winsunny Pharmaceutical Co. | And 3 more authors.
Industrial and Engineering Chemistry Research | Year: 2015

To enhance the solubility and dissolution rate, and thus potentially improve the oral bioavailability of cefixime (CFX), amorphous CFX nanoparticles were prepared via high-gravity antisolvent precipitation (HGAP) without the aid of any pharmaceutical additives in a rotating packed bed (RPB). The effects of operating variables on particle size and distribution were investigated. Compared to raw CFX, the mean size of prepared nanoparticles decreased greatly from about 2.1 μm to 57 nm, and the saturation solubility increased tremendously from 0.289 to 0.951 mg/mL. CFX nanoparticles showed good stability and were capable of generating a maximum supersaturation level, reaching up to ∼22.8 times of raw CFX's saturation solubility. Further, CFX nanoparticles achieved 100% drug dissolution within 2 min, while the raw drug did not dissolve completely after 45 min, suggesting that the solubility and dissolution properties of CFX nanoparticles were significantly improved. Since the drug recovery ratio achieved 99.9%, and the production capacity of lab-scale RPB with a continuous operation reached 1.8 kg/h, the HGAP method might offer a general and facile platform for mass production of CFX nanoparticles. © 2015 American Chemical Society.


Yan Z.,Shenyang Pharmaceutical University | Yan Z.,Beijing Winsunny Pharmaceutical Co. | Sun J.,Shenyang Pharmaceutical University | Chang Y.,Shenyang Pharmaceutical University | And 11 more authors.
Molecular Pharmaceutics | Year: 2011

Five peptidomimetic prodrugs of didanosine (DDI) were synthesized and designed to improve bioavailability of DDI following oral administration via targeting intestinal oligopeptide transporter (PepT1) and enhancing chemical stability. The permeability of prodrugs was screened in Caco-2 cells grown on permeable supports. 5′-O-l-Valyl ester prodrug of DDI (compound 4a) demonstrated the highest membrane permeability and was selected as the optimal target prodrug for further studies. The uptake of glycylsarcosine (Gly-Sar, a typical substrate of PepT1) by Caco-2 cells could be inhibited by compound 4a in a concentration-dependent manner. The Caco-2 cells were treated with 0.2 nM leptin for enhanced PepT1 expression. The uptake of compound 4a was markedly increased in the leptin-treated Caco-2 cells compared with the control Caco-2 cells, both of which were obviously inhibited by 20 mM Gly-Sar. The K m and Vmax values of kinetic study of compound 4a transported by PepT1 in Caco-2 cells were 0.91 mM and 11.94 nmol/mg of protein/10 min, respectively. The chemical stability studies were performed in simulated gastric fluid (SGF), phosphate buffers under various pH conditions, rat tissue homogenates and plasma at 37°C. The concentrations of DDI could not be detected in the two minutes in SGF. But compound 4a could significantly increase DDI acidic stability, and its t1/2 was extended to as long as 36 min in SGF. Compound 4a was stable in pH 6.0 phosphate buffer but could be quickly transformed into DDI in plasma and tissue homogenates. The oral absolute bioavailability of DDI was 47.2% and 7.9% after compound 4a and DDI were orally administered to rats at a dose of 15 mg/kg, respectively. The coadministration with antiacid agent could also suggest that compound 4a was more stable under harsh acidic conditions compared with DDI. Compound 4a bioavailability in rats was reduced to 33.9% when orally coadministrated with Gly-Sar (100 mg/kg). The In Vivo bioactivation mechanism of compound 4a was investigated by comparing the levels of DDI and compound 4a in the jugular and portal veins in rats. The plasma concentration of intact compound 4a was very low in portal veins and could hardly be detected in the jugular vein. In conclusion, compound 4a could significantly improve the oral bioavailability of DDI in rats through PepT1-mediated absorption and enhanced acidic stability, followed by rapid and mostly intracellular bioactivation, the majority in the intestinal cells but the minority in the liver. Additionally, the prodrug strategy targeted to intestinal PepT1 could offer a promising strategy to improve oral bioavailability of poorly absorbed didanosine. © 2011 American Chemical Society.


Patent
Beijing Winsunny Pharmaceutical Co. | Date: 2010-04-14

An oxygen humidification and delivery device includes a case (1), humidification material (2), a seal film or seal plate (3), and an oxygen delivery tube (4). The humidification material (2) is disposed within the case (1). At least two protuberant air ports (6) are provided on the top of the case (1), one of which is air inlet, and the other is air outlet. The seal film or seal plate (3) is adapted to seal the case (1) accommodating the humidification material (2). The air ports are connected to the oxygen delivery tube (4).

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