Mesoporous silica cocoon materials(MSNCs) and MgO doped mesoporous silica cocoons(MgO-MSNCs) with the cocoon-like hierarchical morphology and different alkalinities were synthesized as carriers for acidic drugs. Indom...Mesoporous silica cocoon materials(MSNCs) and MgO doped mesoporous silica cocoons(MgO-MSNCs) with the cocoon-like hierarchical morphology and different alkalinities were synthesized as carriers for acidic drugs. Indomethacin(IMC) was selected as a model drug and loaded into carriers. All materials and the drug-loaded samples were characterized by nitrogen adsorption, FTIR spectroscopy, transmission electron microscopy(TEM), powder X-Ray diffraction(XRD) and differential scanning calorimetry(DSC). The effect of the Mg/Si molar ratio on the kinetics and equilibrium of IMC adsorption on MgO-MSNCs was thoroughly examined, and it was found that the increase in the Mg/Si molar ratio resulted in an increasing IMC adsorption rate due to the increased affinity between alkaline MgO-MSNCs and weak acid IMC. The adsorption kinetics fitted a pseudo second-order model well. The Freundlich isotherm showed a better fit, indicating that the coverage of IMC on the surface of MgO-MSNCs was heterogeneous. The maximum adsorption capacity of adsorbent was calculated by the Langmuir isotherm equation. The Temkin equation provided further support that the IMC adsorption on MgO-MSNCs was dominated by a chemisorption process. MgO-MSNCs also have the advantage of allowing an adjustment of the drug release rate of weak acid drug. The cytotoxicity assay indicated good biocompatibility of MgO-MSNCs. Our research on MgO-MSNCs carriers demonstrated their potential therapeutic benefit for safe and effective management of IMC adsorption and in vitro release.展开更多
Background Acute gout is an intensely painful, inflammatory arthritis. Although the non-steroidal anti-inflammatory drugs （NSAIDs） are widely used for this condition, the efficacy is based on only a few studies, par...Background Acute gout is an intensely painful, inflammatory arthritis. Although the non-steroidal anti-inflammatory drugs （NSAIDs） are widely used for this condition, the efficacy is based on only a few studies, particularly in China. We tried to assess the safety and efficacy of etoricoxib in the treatment of acute gouty arthritis in China. Methods A randomized, double-blind, active comparator study was conducted at 10 sites in China. Patients （n=178; 〉18 years of age） with acute gouty attack （〈48 hours） were treated for 5 days with etoricoxib （120 mg/d; n=89） or indometacin （75 mg twice daily; n=89）. The primary efficacy end point was self-assessed pain in the affected joint （0-4 point Likert scale） from days 2-5. Secondary end points included investigator assessments of tenderness and swelling, patient/ investigator global assessments of response to therapy, and patients discontinuing treatment. Safety was assessed by adverse events （AEs）. Results Etoricoxib and indometacin had comparable primary and secondary end points. Mean change difference from baseline from days 2-5 was 0.03 （95% confidence interval （CI） -0.19 to 0.25; P=0.6364）, which fell within the prespecifled comparative bounds of -0.5 to 0.5. No severe AEs were associated with etoricoxib use. Non-severe AEs were mainly digestive and general, and most （73.7%） were mild, although they caused withdrawal of two subjects in the etoricoxib group, due to bilateral renal calculi and uronephrosis of the left kidney （unrelated to etoricoxib） and fever and chills （potentially etoricoxib-related）. Overall, AEs were similar, although the absolute number of AEs in the etoricoxib group （n=31） was less than the indometacin group （n=34）. Conclusions Etoricoxib （120 mg once daily） is effective in treating acute gout, is generally safe and well-tolerated, and is comparable in efficacy to indometacin （75 mg twice daily）.展开更多
基金supported by the National Basic Research Pro-gram of China(973 Program)(No.2015CB932100)National Natural Science Foundation of China(No.81473165)Liaoning Provincial Key Laboratory of Drug Preparation De-sign&Evaluation of Liaoning Provincial Education Depart-ment(No.LZ2015068)
文摘Mesoporous silica cocoon materials(MSNCs) and MgO doped mesoporous silica cocoons(MgO-MSNCs) with the cocoon-like hierarchical morphology and different alkalinities were synthesized as carriers for acidic drugs. Indomethacin(IMC) was selected as a model drug and loaded into carriers. All materials and the drug-loaded samples were characterized by nitrogen adsorption, FTIR spectroscopy, transmission electron microscopy(TEM), powder X-Ray diffraction(XRD) and differential scanning calorimetry(DSC). The effect of the Mg/Si molar ratio on the kinetics and equilibrium of IMC adsorption on MgO-MSNCs was thoroughly examined, and it was found that the increase in the Mg/Si molar ratio resulted in an increasing IMC adsorption rate due to the increased affinity between alkaline MgO-MSNCs and weak acid IMC. The adsorption kinetics fitted a pseudo second-order model well. The Freundlich isotherm showed a better fit, indicating that the coverage of IMC on the surface of MgO-MSNCs was heterogeneous. The maximum adsorption capacity of adsorbent was calculated by the Langmuir isotherm equation. The Temkin equation provided further support that the IMC adsorption on MgO-MSNCs was dominated by a chemisorption process. MgO-MSNCs also have the advantage of allowing an adjustment of the drug release rate of weak acid drug. The cytotoxicity assay indicated good biocompatibility of MgO-MSNCs. Our research on MgO-MSNCs carriers demonstrated their potential therapeutic benefit for safe and effective management of IMC adsorption and in vitro release.
文摘Background Acute gout is an intensely painful, inflammatory arthritis. Although the non-steroidal anti-inflammatory drugs （NSAIDs） are widely used for this condition, the efficacy is based on only a few studies, particularly in China. We tried to assess the safety and efficacy of etoricoxib in the treatment of acute gouty arthritis in China. Methods A randomized, double-blind, active comparator study was conducted at 10 sites in China. Patients （n=178; 〉18 years of age） with acute gouty attack （〈48 hours） were treated for 5 days with etoricoxib （120 mg/d; n=89） or indometacin （75 mg twice daily; n=89）. The primary efficacy end point was self-assessed pain in the affected joint （0-4 point Likert scale） from days 2-5. Secondary end points included investigator assessments of tenderness and swelling, patient/ investigator global assessments of response to therapy, and patients discontinuing treatment. Safety was assessed by adverse events （AEs）. Results Etoricoxib and indometacin had comparable primary and secondary end points. Mean change difference from baseline from days 2-5 was 0.03 （95% confidence interval （CI） -0.19 to 0.25; P=0.6364）, which fell within the prespecifled comparative bounds of -0.5 to 0.5. No severe AEs were associated with etoricoxib use. Non-severe AEs were mainly digestive and general, and most （73.7%） were mild, although they caused withdrawal of two subjects in the etoricoxib group, due to bilateral renal calculi and uronephrosis of the left kidney （unrelated to etoricoxib） and fever and chills （potentially etoricoxib-related）. Overall, AEs were similar, although the absolute number of AEs in the etoricoxib group （n=31） was less than the indometacin group （n=34）. Conclusions Etoricoxib （120 mg once daily） is effective in treating acute gout, is generally safe and well-tolerated, and is comparable in efficacy to indometacin （75 mg twice daily）.
