Herpetospermum caudigerum lignans(HTL), one of the potential drugs with anti-hepatitis B virus and hepatoprotective effects, has limited clinical applications because of poor aqueous solubility and low bioavailability...Herpetospermum caudigerum lignans(HTL), one of the potential drugs with anti-hepatitis B virus and hepatoprotective effects, has limited clinical applications because of poor aqueous solubility and low bioavailability. Both herpetrione(HPE) and herpetin(HPN) are the most abundant ingredients in HTL and exhibit weak acidity. The purpose of the present study was to produce dried preparations of HTL(composed of HPE and HPN) nanosuspensions(HTL-NS) with high redispersibility using lyophilization technology. The HTL-NS was prepared by utilizing precipitation-combined homogenization technology based on acid-base neutralization reactions, and critical formulation and process parameters affecting the characteristics of HTL-NS were optimized. The resultant products were characterized by particle size analysis, SEM, XRD, stability, solubility, dissolution and in vivo bioavailability. HTL-NS showed near-spherical-shaped morphology and the size was 243 nm with a narrow PDI value of 0.187. The dried preparations with a relatively large particle size of 286 nm and a PDI of 0.215 were achieved by using 4%(W/V) mannitol as cryoprotectants, and had a better stability at 4 or 25 oC for 2 months, compared to HTL-NS. In the in vitro test, the dried preparations showed markedly increased solubility and dissolution velocity. Besides, in the in vivo evaluation, it exhibited significant increases in AUC0–t, C_(max), MRT and a decrease in T_(max), compared to the raw drug.. In conclusion, our results provide a basis for the development of a drug delivery system for poorly water-soluble ingredients with p H-dependent solubility.展开更多
Let G be a finite group and F a saturated formation of finite groups.Then G is a quasi-F-group if for every F-eccentric chief factor H/K of G and every x∈G,x induces an inner automorphism on H/K.In this article,we ob...Let G be a finite group and F a saturated formation of finite groups.Then G is a quasi-F-group if for every F-eccentric chief factor H/K of G and every x∈G,x induces an inner automorphism on H/K.In this article,we obtain some results about the quasi-F-groups and use them to give the conditions under which a group is quasisupersoluble.展开更多
基金supported by the National Key New Drugs Innovation Foundation(No.2015ZX09101025)the National Science Foundation of China(No.81503169)the New Drugs Development Special Foundation of Beijing City of China(No.Z141100002214007)
文摘Herpetospermum caudigerum lignans(HTL), one of the potential drugs with anti-hepatitis B virus and hepatoprotective effects, has limited clinical applications because of poor aqueous solubility and low bioavailability. Both herpetrione(HPE) and herpetin(HPN) are the most abundant ingredients in HTL and exhibit weak acidity. The purpose of the present study was to produce dried preparations of HTL(composed of HPE and HPN) nanosuspensions(HTL-NS) with high redispersibility using lyophilization technology. The HTL-NS was prepared by utilizing precipitation-combined homogenization technology based on acid-base neutralization reactions, and critical formulation and process parameters affecting the characteristics of HTL-NS were optimized. The resultant products were characterized by particle size analysis, SEM, XRD, stability, solubility, dissolution and in vivo bioavailability. HTL-NS showed near-spherical-shaped morphology and the size was 243 nm with a narrow PDI value of 0.187. The dried preparations with a relatively large particle size of 286 nm and a PDI of 0.215 were achieved by using 4%(W/V) mannitol as cryoprotectants, and had a better stability at 4 or 25 oC for 2 months, compared to HTL-NS. In the in vitro test, the dried preparations showed markedly increased solubility and dissolution velocity. Besides, in the in vivo evaluation, it exhibited significant increases in AUC0–t, C_(max), MRT and a decrease in T_(max), compared to the raw drug.. In conclusion, our results provide a basis for the development of a drug delivery system for poorly water-soluble ingredients with p H-dependent solubility.
基金supported by the grant of NSFC(Grant#11701223,11271016,11501235)the Key Natural Science Foundation of Anhui Education Commission(KJ2017A569)Research project of China West Normal University(17E091).
文摘Let G be a finite group and F a saturated formation of finite groups.Then G is a quasi-F-group if for every F-eccentric chief factor H/K of G and every x∈G,x induces an inner automorphism on H/K.In this article,we obtain some results about the quasi-F-groups and use them to give the conditions under which a group is quasisupersoluble.
