Idiopathic pulmonary fibrosis（IPF） is characterized by progressive lung scarring, reduced median survival, poor prognosis and limited therapeutic options, leading to great need for new pharmacologic therapies. In re...Idiopathic pulmonary fibrosis（IPF） is characterized by progressive lung scarring, reduced median survival, poor prognosis and limited therapeutic options, leading to great need for new pharmacologic therapies. In recent years, researchers have found that Rho-ROCK signaling pathway may be a new drug target in the prevention of IPF. This article reviewed the role of Rho-ROCK pathway in pulmonary fibrosis and the application of ROCK inhibitors in experimental models of IPF. Multiple lines of evidence therefore indicated that ROCK inhibition has great potential to be a powerful therapeutic tool in the prevention and treatment of IPF in clinic.展开更多
In the present study, we aimed to prepare poloxamer 403/407 mixed micelles in order to improve the solubility and oral bioavailability of genistein. Genistein was incorporated in the mixed poloxamer micelles by thin-f...In the present study, we aimed to prepare poloxamer 403/407 mixed micelles in order to improve the solubility and oral bioavailability of genistein. Genistein was incorporated in the mixed poloxamer micelles by thin-film hydration method, and its physicochemical properties, including particle size, zeta potential, entrapment efficiency and drug loading, were investigated. In vitro release of genistein from the mixed micelles was monitored by dialysis method, and pharmacokinetic study of genistein loaded mixed micelles was carried out in rats. We found that the particle size and zeta potential of mixed micelles were（20.31±0.43） nm and（–8.94±0.35） m V, with encapsulation efficiency 90.59%±0.67% and drug loading 7.74%±0.05%. Solubility of genistein in mixed micelles reached 3.80 mg/m L, which was about 130 times higher than that in water. Genistein-loaded mixed micelles showed sustained release characteristics in vitro with no burst release phenomenon, but it was faster than suspension. The AUC0–t and AUC0–∞ of mixed micelles were 196.74% and 204.62% greater than that of genisein suspension, respectively. Consequently, poloxamer 403/407 mixed micelles significantly improved the solubility and oral bioavailability of genistein, which could be used as an effective drug delivery system for oral administration of poorly soluble drugs.展开更多
In the present study, we aimed to assess the preparation method of sterile lansoprazole powder for injection, as well as its quality and stability. By cryodesiccation technology in combination with the control of its ...In the present study, we aimed to assess the preparation method of sterile lansoprazole powder for injection, as well as its quality and stability. By cryodesiccation technology in combination with the control of its quality and stability, the optimal formulation and preparation route were screened. Through small-scale and pilot-scale production validation, the formulation and preparation route were confirmed, in which mannitol was used as skeletal matter, meglumine was used as solubilizer and p H stabilizer, and sodium hydroxide was used as p H regulator. The formulation and preparation route were reasonable, showing good quality control and stability and fitting the pharmaceutical and clinical need.展开更多
基金Zhejiang Provincial Natural Science Foundation of China(Grant No.LQ15H280007)National Natural Science Foundation of China(Grant No.81202977)project of Traditional Chinese Medicine Science of Zhejiang province(Grant No.2013ZA026 and 2016ZA042)
文摘Idiopathic pulmonary fibrosis（IPF） is characterized by progressive lung scarring, reduced median survival, poor prognosis and limited therapeutic options, leading to great need for new pharmacologic therapies. In recent years, researchers have found that Rho-ROCK signaling pathway may be a new drug target in the prevention of IPF. This article reviewed the role of Rho-ROCK pathway in pulmonary fibrosis and the application of ROCK inhibitors in experimental models of IPF. Multiple lines of evidence therefore indicated that ROCK inhibition has great potential to be a powerful therapeutic tool in the prevention and treatment of IPF in clinic.
基金The Zhejiang Public Welfare Technology Application Research Project(Grant No.2015C31100)the Ningbo Science and Technology Innovation Team Project(Grant No.2015C110027)
文摘In the present study, we aimed to prepare poloxamer 403/407 mixed micelles in order to improve the solubility and oral bioavailability of genistein. Genistein was incorporated in the mixed poloxamer micelles by thin-film hydration method, and its physicochemical properties, including particle size, zeta potential, entrapment efficiency and drug loading, were investigated. In vitro release of genistein from the mixed micelles was monitored by dialysis method, and pharmacokinetic study of genistein loaded mixed micelles was carried out in rats. We found that the particle size and zeta potential of mixed micelles were（20.31±0.43） nm and（–8.94±0.35） m V, with encapsulation efficiency 90.59%±0.67% and drug loading 7.74%±0.05%. Solubility of genistein in mixed micelles reached 3.80 mg/m L, which was about 130 times higher than that in water. Genistein-loaded mixed micelles showed sustained release characteristics in vitro with no burst release phenomenon, but it was faster than suspension. The AUC0–t and AUC0–∞ of mixed micelles were 196.74% and 204.62% greater than that of genisein suspension, respectively. Consequently, poloxamer 403/407 mixed micelles significantly improved the solubility and oral bioavailability of genistein, which could be used as an effective drug delivery system for oral administration of poorly soluble drugs.
文摘In the present study, we aimed to assess the preparation method of sterile lansoprazole powder for injection, as well as its quality and stability. By cryodesiccation technology in combination with the control of its quality and stability, the optimal formulation and preparation route were screened. Through small-scale and pilot-scale production validation, the formulation and preparation route were confirmed, in which mannitol was used as skeletal matter, meglumine was used as solubilizer and p H stabilizer, and sodium hydroxide was used as p H regulator. The formulation and preparation route were reasonable, showing good quality control and stability and fitting the pharmaceutical and clinical need.
