检索结果-南通市图书馆

Formulation of dried lignans nanosuspension with high redispersibility to enhance stability,dissolution,and oral bioavailability

引用

Chinese Journal of Natural Medicines 2016年第10期14卷 757-768页

作者： SHEN Gang CHENG Ling WANG Li-Qiang ZHANG Li-Hong SHEN Bao-De LIAO Wei-Bo LI Juan-Juan ZHENG Juan XU Rong YUAN Hai-Long Department of Pharmacy Air Force General Hospital of PLABeijing 100142China Pharmacy College Chengdu University of Traditional Chinese MedicineChengdu 611137China School of Biomedical Sciences Huaqiao UniversityQuanzhou 362021China

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.

关键词： Herpetospermum caudigerum lignans Nanosuspensions Acid-base neutralization saturation solubility Dissolution Oral bioavailability

来源：

维普期刊数据库

同方期刊数据库评论

在线全文

学校读者我要写书评

暂无评论

Nanosuspensions of Poorly Water Soluble Drugs Prepared by Precipitation-Combined Homogenization Technology based on Acid-Base Neutralization Reactions

Nanosuspensions of Poorly Water Soluble Drugs Prepared by Pr...

引用

2015年中国药学大会暨第十五届中国药师周

作者： Gang Shen Ling Cheng Lihong Zhang Baode shen Juanjuan Li Juan Zhen Rong Xu Hailong Yuan Pharmacy College Chengdu University of Traditional Chinese Medicine Department of Pharmacy Air Force General Hospital of PLA

Herpetospermum caudigerum lignans（HTL）, one of the potential drugs with the treatment of anti-hepatitis B virus and hepatoprotective effects, have been limited in clinical applications because of poor saturation solubility, resulting in low bioavailability. Both herpetrione（HPE） and herpetin（HPN） are considered as the most abundant ingredient in HTL and exhibit weak acidity. The purpose of this study was to produce dried preparations of HTL（composed of HPE and HPN） nosuspensions with high redispersibility using lyophilization. The HTL-NS was prepared by utilizing precipitation-combined homogenization technology based on acid-base neutralization reactions, and variously critical formulation and process parameters affecting the characteristics of HTL-NS were optimized. The resultant products were characterized by particle size analysis, SEM, XRD, physical stability, solubility, dissolution and bioavailability. The dried preparations with a mean redispersed particle size of 286 nm was produced by using 4%（w/v） mannitol as cryoprotectants and possessed good physical stability at 4 oC or 25 oC for two months. Meanwhile, in vitro evaluation showed dried preparations could significantly increase saturation solubility and dissolution rate along with improving in vivo oral bioavailability, when compared with raw drug. This study provides a feasible drug delivery system for poorly water-soluble ingredients with pH-dependent solubility.

关键词： Herpetospermum caudigerum lignans nanosuspensions acid–base neutralization saturation solubility dissolution oral bioavailability

来源： cnki会议评论

在线全文

cnki会议

学校读者我要写书评

暂无评论

欢迎您,

建议与咨询留下您的常用邮箱和电话号码，以便我们向您反馈解决方案和替代方法

时间限定

文献类型

馆藏选择

核心期刊

语言

文献类型

帮助

文字说明：

检索规则说明：

检索范例：

分类表

所选分类

限定检索结果

文献类型

馆藏范围

日期分布

学科分类号

主题

机构

作者

语言

在线全文

在线全文

请选择保存的检索档案：

请选择收藏分类：

通借通还

欢迎您,

建议与咨询 留下您的常用邮箱和电话号码，以便我们向您反馈解决方案和替代方法

时间限定

文献类型

馆藏选择

核心期刊

语言

文献类型

帮助

文字说明：

检索规则说明：

检索范例：

分类表

所选分类

限定检索结果

文献类型

馆藏范围

日期分布

学科分类号

主题

机构

作者

语言

在线全文

在线全文

请选择保存的检索档案： 新增检索档案 确定 取消

请选择收藏分类： 新增自定义分类 确定 取消

通借通还

建议与咨询留下您的常用邮箱和电话号码，以便我们向您反馈解决方案和替代方法

请选择保存的检索档案：

请选择收藏分类：