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
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
Objective:To study the effects of Atorvastatin calcium combined with Aspirin on serum levels of homocysteine (Hcy), neuron-specific enolase (NSE), uric acid (UA), high sensitity C-reactive protein (hs-CRP) and inflamm...Objective:To study the effects of Atorvastatin calcium combined with Aspirin on serum levels of homocysteine (Hcy), neuron-specific enolase (NSE), uric acid (UA), high sensitity C-reactive protein (hs-CRP) and inflammatory factors of patients with cerebral infarction. Methods:100 cases of patients with cerebral infarction from March 2014 to May 2016 were treated in the Department of Neurology of our hospital and affiliated to Huazhong University of Science and Technology of traditional Chinese medicine and Western Medicine. The subjects were divided into the control group (n=50) and the treatment group (n=50) randomly. The control group was treated with Aspirin, the treatment group were treated with Atorvastatin calcium combined with Aspirin. The two groups were treated for 28 d. The serum levels of Hcy, NSE, UA, hs-CRP, interleukin-6 (IL-6), interleukin-8 (IL-8) and tumor necrosis factor-α(TNF-α) of the two groups before and after treatment were compared. Results:There were no significantly differences of the serum levels of the Hcy, NSE, UA and hs-CRP of the two groups before treatment (P>0.05). After treatment, the serum levels of the Hcy, NSE, UA and hs-CRP of the two groups were significantly lower than before treatment, and that of the treatment group were significantly lower than the control group (P<0.05). There were no significantly differences of the serum levels of the IL-6, IL-8 and TNF-αof the two groups before treatment (P>0.05). After treatment, the serum levels of the IL-6, IL-8 and TNF-αof the two groups were significantly lower than before treatment, and that of the treatment group were significantly lower than the control group (P<0.05). Conclusions:Atorvastatin calcium combined with Aspirin can significantly reduce the serum levels of Hcy, NSE, UA, hs-CRP, IL-6, IL-8 and TNF-αof the patients with cerebral infarction.展开更多
Objective:To explore the effect of atorvastatin calcium on the carotid atherosclerotic plaque, serum lipid level, and cerebral hemodynamic indicators in patients with transient ischemic attack (TIA).Methods:A total of...Objective:To explore the effect of atorvastatin calcium on the carotid atherosclerotic plaque, serum lipid level, and cerebral hemodynamic indicators in patients with transient ischemic attack (TIA).Methods:A total of 80 patients with TIA and carotid atherosclerotic plaque who were admitted in our hospital and confirmed by the ultrasound were included in the study and randomized into the treatment group and the control group (n = 40). The patients in the two groups were given TIA routine treatments and aspirin. On this basis, the patients in the treatment group were given atorvastatin calcium. The carotid ultrasound before treatment and 6 months after treatment in the two groups was performed to compare the atherosclerotic plaque area and IMT. The serum lipid level and cerebral hemodynamic parameters were detected. Results:IMT and carotid plaque area after treatment in the treatment group were significantly reduced when compared with before treatment (P<0.05). IMT and carotid plaque area after treatment in the treatment group were significantly lower than those in the control group (P<0.05). The comparison of TC, TG, LDL, and HDL levels before treatment between the two groups was not statistically significant (P>0.05). TC, TG, and LDL levels after treatment were significantly reduced when compared with before treatment (P<0.05), while HDL level was significantly elevated when compared with before treatment (P<0.05). TC, TG, and LDL levels after treatment in the treatment group were significantly lower than those in the control group (P<0.05), while HDL level was significantly higher than that in the control group (P<0.05). The average blood velocity and average blood flow volume of cerebral circulation after treatment in the treatment group were significantly higher than those in the control group (P<0.05), while the cerebrovascular characteristic resistance and peripheral resistance were significantly lower than those in the control group (P<0.05).Conclusions:Atorvastatin calcium in the treatment of TIA can significantly reduce the serum lipid level, alleviate or stabilize the carotid atherosclerotic plaque, and improve the cerebral hemodynamic indicators, with a significant efficacy.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Objective:To study the effects of Atorvastatin calcium combined with Aspirin on serum levels of homocysteine (Hcy), neuron-specific enolase (NSE), uric acid (UA), high sensitity C-reactive protein (hs-CRP) and inflammatory factors of patients with cerebral infarction. Methods:100 cases of patients with cerebral infarction from March 2014 to May 2016 were treated in the Department of Neurology of our hospital and affiliated to Huazhong University of Science and Technology of traditional Chinese medicine and Western Medicine. The subjects were divided into the control group (n=50) and the treatment group (n=50) randomly. The control group was treated with Aspirin, the treatment group were treated with Atorvastatin calcium combined with Aspirin. The two groups were treated for 28 d. The serum levels of Hcy, NSE, UA, hs-CRP, interleukin-6 (IL-6), interleukin-8 (IL-8) and tumor necrosis factor-α(TNF-α) of the two groups before and after treatment were compared. Results:There were no significantly differences of the serum levels of the Hcy, NSE, UA and hs-CRP of the two groups before treatment (P>0.05). After treatment, the serum levels of the Hcy, NSE, UA and hs-CRP of the two groups were significantly lower than before treatment, and that of the treatment group were significantly lower than the control group (P<0.05). There were no significantly differences of the serum levels of the IL-6, IL-8 and TNF-αof the two groups before treatment (P>0.05). After treatment, the serum levels of the IL-6, IL-8 and TNF-αof the two groups were significantly lower than before treatment, and that of the treatment group were significantly lower than the control group (P<0.05). Conclusions:Atorvastatin calcium combined with Aspirin can significantly reduce the serum levels of Hcy, NSE, UA, hs-CRP, IL-6, IL-8 and TNF-αof the patients with cerebral infarction.
文摘Objective:To explore the effect of atorvastatin calcium on the carotid atherosclerotic plaque, serum lipid level, and cerebral hemodynamic indicators in patients with transient ischemic attack (TIA).Methods:A total of 80 patients with TIA and carotid atherosclerotic plaque who were admitted in our hospital and confirmed by the ultrasound were included in the study and randomized into the treatment group and the control group (n = 40). The patients in the two groups were given TIA routine treatments and aspirin. On this basis, the patients in the treatment group were given atorvastatin calcium. The carotid ultrasound before treatment and 6 months after treatment in the two groups was performed to compare the atherosclerotic plaque area and IMT. The serum lipid level and cerebral hemodynamic parameters were detected. Results:IMT and carotid plaque area after treatment in the treatment group were significantly reduced when compared with before treatment (P<0.05). IMT and carotid plaque area after treatment in the treatment group were significantly lower than those in the control group (P<0.05). The comparison of TC, TG, LDL, and HDL levels before treatment between the two groups was not statistically significant (P>0.05). TC, TG, and LDL levels after treatment were significantly reduced when compared with before treatment (P<0.05), while HDL level was significantly elevated when compared with before treatment (P<0.05). TC, TG, and LDL levels after treatment in the treatment group were significantly lower than those in the control group (P<0.05), while HDL level was significantly higher than that in the control group (P<0.05). The average blood velocity and average blood flow volume of cerebral circulation after treatment in the treatment group were significantly higher than those in the control group (P<0.05), while the cerebrovascular characteristic resistance and peripheral resistance were significantly lower than those in the control group (P<0.05).Conclusions:Atorvastatin calcium in the treatment of TIA can significantly reduce the serum lipid level, alleviate or stabilize the carotid atherosclerotic plaque, and improve the cerebral hemodynamic indicators, with a significant efficacy.