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
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
The study carried out here was focused on developing conventional monolithic controlled release matrix tablet of Atorvastatin calcium using carbomer as release controlling polymer. This system ensures the drug release...The study carried out here was focused on developing conventional monolithic controlled release matrix tablet of Atorvastatin calcium using carbomer as release controlling polymer. This system ensures the drug release at the alkaline pH region where the drug has got maximum solubility. Further the study was concentrated on comparing the impact of gelling agent polyvinyl pyrrolidone on drug release. Quality by design tools were considered during formulation development and the polymer concentrations were optimized adopting the statistical tool, design of experiments (DoE). The optimized formulation of present study exhibited desired controlled drug release characteristics in the alkaline pH conditions and at acidic environment the drug dissolution was minimal as intended.展开更多
Background Hypertension combined with dyslipidemia is the main cause of cerebrovascular and cardiovascular accidents in elderly patients,and actively controlling blood pressure and lipid levels is the best way to redu...Background Hypertension combined with dyslipidemia is the main cause of cerebrovascular and cardiovascular accidents in elderly patients,and actively controlling blood pressure and lipid levels is the best way to reduce the risk of cardiovascular accidents and death.This study focused on the clinical pharmaceutical analysis of combined therapy with amlodipine benzenesulfonate and atorvastatin calcium for elderly patients with hypertension and dyslipidemia.Methods A total of 292 elderly patients with hypertension and dyslipidemia from August 2022 to February 2023 were selected and grouped according to random number table method,and evenly assigned to control group(n=146)and observation group(n=146).Control group was treated with amlodipine besylate,and observation group was treated with combined therapy with amlodipine benzenesulfonate and atorvastatin calcium.The effects and adverse reactions of the two groups were compared,and the changes of blood pressure and lipid indexes before and after treatment were also compared.Results The total effective rate of observation group was higher than that of control group,the difference was significant(P<0.05).There was no significant difference in the incidence of adverse reactions between the two groups(P>0.05).No significant differences were found in systolic blood pressure,diastolic blood pressure,total cholesterol and triglyceride between the two groups before treatment(P>0.05).While after treatment,the level of systolic blood pressure,diastolic blood pressure,total cholesterol and triglyceride in the observation group were lower than those in the control group(P<0.05).Conclusions The combination therapy with amlodipine benzenesulfonate and atorvastatin calcium is effective and safe,improving blood pressure and lipid levels in patients with hypertension and dyslipidemia,and can be widely applied to elderly patients with hypertension and dyslipidemia.[S Chin J Cardiol 2024;25(1):38-43].展开更多
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.
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The study carried out here was focused on developing conventional monolithic controlled release matrix tablet of Atorvastatin calcium using carbomer as release controlling polymer. This system ensures the drug release at the alkaline pH region where the drug has got maximum solubility. Further the study was concentrated on comparing the impact of gelling agent polyvinyl pyrrolidone on drug release. Quality by design tools were considered during formulation development and the polymer concentrations were optimized adopting the statistical tool, design of experiments (DoE). The optimized formulation of present study exhibited desired controlled drug release characteristics in the alkaline pH conditions and at acidic environment the drug dissolution was minimal as intended.
文摘Background Hypertension combined with dyslipidemia is the main cause of cerebrovascular and cardiovascular accidents in elderly patients,and actively controlling blood pressure and lipid levels is the best way to reduce the risk of cardiovascular accidents and death.This study focused on the clinical pharmaceutical analysis of combined therapy with amlodipine benzenesulfonate and atorvastatin calcium for elderly patients with hypertension and dyslipidemia.Methods A total of 292 elderly patients with hypertension and dyslipidemia from August 2022 to February 2023 were selected and grouped according to random number table method,and evenly assigned to control group(n=146)and observation group(n=146).Control group was treated with amlodipine besylate,and observation group was treated with combined therapy with amlodipine benzenesulfonate and atorvastatin calcium.The effects and adverse reactions of the two groups were compared,and the changes of blood pressure and lipid indexes before and after treatment were also compared.Results The total effective rate of observation group was higher than that of control group,the difference was significant(P<0.05).There was no significant difference in the incidence of adverse reactions between the two groups(P>0.05).No significant differences were found in systolic blood pressure,diastolic blood pressure,total cholesterol and triglyceride between the two groups before treatment(P>0.05).While after treatment,the level of systolic blood pressure,diastolic blood pressure,total cholesterol and triglyceride in the observation group were lower than those in the control group(P<0.05).Conclusions The combination therapy with amlodipine benzenesulfonate and atorvastatin calcium is effective and safe,improving blood pressure and lipid levels in patients with hypertension and dyslipidemia,and can be widely applied to elderly patients with hypertension and dyslipidemia.[S Chin J Cardiol 2024;25(1):38-43].
