A biodegradable poly(lactic-co-glycolic acid) loading atorvastatin calcium(AC) nanoparticles(AC-PLGA-NPs) were prepared by probe ultrasonication and evaporation method aiming at improving the oral bioavailability of A...A biodegradable poly(lactic-co-glycolic acid) loading atorvastatin calcium(AC) nanoparticles(AC-PLGA-NPs) were prepared by probe ultrasonication and evaporation method aiming at improving the oral bioavailability of AC. The effects of experimental parameters, including stabilizer species, stabilizer concentration and pH of aqueous phase, on particle size were also evaluated. The resultant nanoparticles were in spherical shape with an average diameter of 174.7 nm and a narrow particle size distribution. And the drug loading and encapsulation efficiency were about 8% and 71%, respectively. The particle size and polydispersion were almost unchanged in 10 days. The release curves of AC-PLGA-NPs in vitro displaying sustained release characteristics indicated that its release mechanisms were matrix erosion and diffusion. The pharmacokinetic study in vivo revealed that the Cmax and AUC0-∞ of AC-PLGA-NPs in rats were nearly 3.7-fold and 4.7-fold higher than that of pure atorvastatin calcium suspension. Our results demonstrated that the delivery of AC-PLGANPs could be a promising approach for the oral delivery of AC for enhanced bioavailability.展开更多
Due to low solubility and bioavailability, atorvastatin calcium is confronted with challenge in conceiving appropriate formulation. Solid dispersion of atorvastatin calcium was prepared through the solvent evaporation...Due to low solubility and bioavailability, atorvastatin calcium is confronted with challenge in conceiving appropriate formulation. Solid dispersion of atorvastatin calcium was prepared through the solvent evaporation method, with Poloxamer 188 as hydrophilic carriers. This formulation was then characterized by scanning electron microscopy, differential scanning calorimetry, powder X-ray diffraction and fourier transform infrared spectroscopy. Moreover, all these studies suggested the conversion of crystalline atorvastatin calcium. In addition, the drug solubility studies as well as dissolution rates compared with bulk drug and market tablets Lipitor were also examined. Furthermore, the study investigated the pharmacokinetics after oral administration of Lipitor and solid dispersion. And the AUC 0–8 h and C max increased after taking ATC-P188 solid dispersion orally compared with that of Lipitor. All these could be demonstrated that ATC-P188 solid dispersions would be prospective means for enhancing higher oral bioavailability of ATC.展开更多
目的:探讨口服磷酸钠盐导致的急性磷酸盐肾病(APN)患者的临床病理特征及预后。方法:回顾分析2010年1月至2022年11月国家肾脏疾病临床医学研究中心行肾活检诊断为APN的患者,分析其临床表现、病理特点、治疗及预后。结果:共纳入APN患者9例...目的:探讨口服磷酸钠盐导致的急性磷酸盐肾病(APN)患者的临床病理特征及预后。方法:回顾分析2010年1月至2022年11月国家肾脏疾病临床医学研究中心行肾活检诊断为APN的患者,分析其临床表现、病理特点、治疗及预后。结果:共纳入APN患者9例,其中男性7例,肾活检时年龄60.1±9.1岁。患者均因需行结肠镜检查口服磷酸钠盐,服药前血清肌酐(SCr)水平均在正常范围,1例无高危因素,其余8例存在2~4种高危因素(中位3种)。诊断急性肾损伤(AKI)时,SCr为257.24±63.65μmol/L;除1例血磷升高,余患者血钙、血磷水平均在正常范围。尿检无红细胞,仅2例出现少量蛋白尿。肾活检光镜下主要表现为肾小管间质损伤,肾小管上皮细胞、管腔和间质中均观察到多处偏振光无折光性的嗜碱性钙盐沉积(全片共25~58处)。6例患者接受泼尼松(15~30 mg/d)治疗。中位随访14月,7例患者肾功能改善,但SCr均未恢复至正常范围,末次随访SCr为175.92±45.05μmol/L,估算的肾小球滤过率(e GFR)为36.33±12.83 m L/(min·1.73m^(2))。结论:口服磷酸钠盐导致的APN通常起病较为隐匿,肾活检有助于明确诊断。对于存在高危因素的患者应慎用磷酸盐洗肠液,并密切监测肾功能变化,以提早识别和处理。展开更多
基金financially supported by the Science and Technology Research Project of Liaoning Provincial Education Department L2013390
文摘A biodegradable poly(lactic-co-glycolic acid) loading atorvastatin calcium(AC) nanoparticles(AC-PLGA-NPs) were prepared by probe ultrasonication and evaporation method aiming at improving the oral bioavailability of AC. The effects of experimental parameters, including stabilizer species, stabilizer concentration and pH of aqueous phase, on particle size were also evaluated. The resultant nanoparticles were in spherical shape with an average diameter of 174.7 nm and a narrow particle size distribution. And the drug loading and encapsulation efficiency were about 8% and 71%, respectively. The particle size and polydispersion were almost unchanged in 10 days. The release curves of AC-PLGA-NPs in vitro displaying sustained release characteristics indicated that its release mechanisms were matrix erosion and diffusion. The pharmacokinetic study in vivo revealed that the Cmax and AUC0-∞ of AC-PLGA-NPs in rats were nearly 3.7-fold and 4.7-fold higher than that of pure atorvastatin calcium suspension. Our results demonstrated that the delivery of AC-PLGANPs could be a promising approach for the oral delivery of AC for enhanced bioavailability.
文摘Due to low solubility and bioavailability, atorvastatin calcium is confronted with challenge in conceiving appropriate formulation. Solid dispersion of atorvastatin calcium was prepared through the solvent evaporation method, with Poloxamer 188 as hydrophilic carriers. This formulation was then characterized by scanning electron microscopy, differential scanning calorimetry, powder X-ray diffraction and fourier transform infrared spectroscopy. Moreover, all these studies suggested the conversion of crystalline atorvastatin calcium. In addition, the drug solubility studies as well as dissolution rates compared with bulk drug and market tablets Lipitor were also examined. Furthermore, the study investigated the pharmacokinetics after oral administration of Lipitor and solid dispersion. And the AUC 0–8 h and C max increased after taking ATC-P188 solid dispersion orally compared with that of Lipitor. All these could be demonstrated that ATC-P188 solid dispersions would be prospective means for enhancing higher oral bioavailability of ATC.
文摘目的:探讨口服磷酸钠盐导致的急性磷酸盐肾病(APN)患者的临床病理特征及预后。方法:回顾分析2010年1月至2022年11月国家肾脏疾病临床医学研究中心行肾活检诊断为APN的患者,分析其临床表现、病理特点、治疗及预后。结果:共纳入APN患者9例,其中男性7例,肾活检时年龄60.1±9.1岁。患者均因需行结肠镜检查口服磷酸钠盐,服药前血清肌酐(SCr)水平均在正常范围,1例无高危因素,其余8例存在2~4种高危因素(中位3种)。诊断急性肾损伤(AKI)时,SCr为257.24±63.65μmol/L;除1例血磷升高,余患者血钙、血磷水平均在正常范围。尿检无红细胞,仅2例出现少量蛋白尿。肾活检光镜下主要表现为肾小管间质损伤,肾小管上皮细胞、管腔和间质中均观察到多处偏振光无折光性的嗜碱性钙盐沉积(全片共25~58处)。6例患者接受泼尼松(15~30 mg/d)治疗。中位随访14月,7例患者肾功能改善,但SCr均未恢复至正常范围,末次随访SCr为175.92±45.05μmol/L,估算的肾小球滤过率(e GFR)为36.33±12.83 m L/(min·1.73m^(2))。结论:口服磷酸钠盐导致的APN通常起病较为隐匿,肾活检有助于明确诊断。对于存在高危因素的患者应慎用磷酸盐洗肠液,并密切监测肾功能变化,以提早识别和处理。
