Development and bioavailability assessment of ramipril nanoemulsion formulation

被引:571
作者
Shafiq, Sheikh [1 ]
Shakeel, Faiyaz [1 ]
Talegaonkar, Sushma [1 ]
Ahmad, Farhan J. [1 ]
Khar, Roop K. [1 ]
Ali, Mushir [1 ]
机构
[1] Jamia Hamdard, Dept Pharmaceut, Fac Pharm, New Delhi 110062, India
关键词
nanoemulsion; ramipril; bioavailability; SNEDDS; phase diagrams; solubility; Sefsol; 218;
D O I
10.1016/j.ejpb.2006.10.014
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The objective of our investigation was to design a thermodynamically stable and dilutable nanoemulsion formulation of Ramipril, with minimum surfactant concentration that could improve its solubility, stability and oral bioavai lability. Formulations were taken from the o/w nanoemulsion region of phase diagrams, which were subjected to thermodynamic stability and dispersibility tests. The composition of optimized formulation was Sefsol 218 (20% w/w), Tween 80 (18% w/w), Carbitol (18% w/w) and standard buffer solution pH 5 (44% w/w) as oil, surfactant, cosurfactant and aqueous phase, respectively, containing 5 mg of ramipril showing drug release (95%), droplet size (80.9 nm), polydispersity (0.271), viscosity (10.68 cP), and infinite dilution capability. In vitro drug release of the nanoemulsion formulations was highly significant (p < 0.01) as compared to marketed capsule formulation and drug suspension. The relative bioavailability of ramipril nanoemulsion to that of conventional capsule form was found to be 229.62% whereas to that of drug suspension was 539.49%. The present study revealed that ramipril nanoemulsion could be used as a liquid formulation for pediatric and geriatric patients and can be formulated as self-nanoemulsifying drug delivery system (SNEDDS) as a unit dosage form. (C) 2006 Elsevier B.V. All rights reserved.
引用
收藏
页码:227 / 243
页数:17
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