In-Vitro, Ex-Vivo Characterization of Furosemide Bounded Pharmacosomes for Improvement of Solubility and Permeability

Vivekanand K.Chatap,Savita D Patil,Prashant L Patil

doi:10.13189/app.2014.020501

Abstract

The design of the present investigation was to prepare furosemide bounded pharmacosomes to enhance solubility and permeability drug by simple reproducible solvent evaporation technique and further investigated. Furosemide bounded pharmacosomes formulation (PMC1 & PMC2) was taken and compared with pure drug by way of enhanced solubility 5.4 fold in the water, 3.33, 4.76 fold in pH 7.4 and pH 5.8 respectively, increases permeability of furosemide bounded pharmacosomes 28.28% when compared with pure drug, drug content showed 94.83, N-octanol/water partition coefficient from 2.33 to 5.15 and in-vitro release profile exhibits excellent sustained drug release properties. Prepared furosemide bounded Pharmacosomes were confirmed from differential scanning calorimetry (DSC), X-ray diffraction (XRD) and FT-IR. The pharmacosomes reported amphiphilic nature may responsible for the improvement of solubility and permeability leads to enhancement of oral bioavailability. From this study it can be concluded that, this formulation strategy becomes important for drug belongs to the BCS class- II & IV.

Highlights

More than 40% active pharmaceutical ingredients developed over the year in the pharmaceutical industry are having poor bioavailability, and the formulation development of poorly soluble as well as poorly permeable substances for oral delivery present great challenges to researchers in the pharmaceutical industry[1].In the case of biopharmaceutical classification system (BCS) class IV drug, drug dissolution permeation is the rate limiting step in the process of drug absorption[1].Furosemide (FRMD) is 5-(aminosulphonyl) -4-chloro-2-[(2-fuanyl-methyl) amino] benzoic acid, a potent high ceiling diuretic, mainly used in the treatment of hypertension
The objective of this research is that a) furosemide-phospholipid complex was prepared by simple method; b) the physicochemical characters of furosemide bounded pharmacosomes were evaluated, such as Differential Scanning Calorimetry (DSC), X-ray diffraction (XRD) and Fourier Transforms Infrared (FT-IR)
Results and Discussion nature of the Pharmacosomes and a polar group of furosemide were masked by phospholipids

Summary

Introduction

More than 40% active pharmaceutical ingredients developed over the year in the pharmaceutical industry are having poor bioavailability, and the formulation development of poorly soluble as well as poorly permeable substances for oral delivery present great challenges to researchers in the pharmaceutical industry[1].In the case of BCS class IV drug, drug dissolution permeation is the rate limiting step in the process of drug absorption[1].Furosemide (FRMD) (fig. 1) is 5-(aminosulphonyl) -4-chloro-2-[(2-fuanyl-methyl) amino] benzoic acid, a potent high ceiling (loop) diuretic, mainly used in the treatment of hypertension. More than 40% active pharmaceutical ingredients developed over the year in the pharmaceutical industry are having poor bioavailability, and the formulation development of poorly soluble as well as poorly permeable substances for oral delivery present great challenges to researchers in the pharmaceutical industry[1].In the case of BCS class IV drug, drug dissolution permeation is the rate limiting step in the process of drug absorption[1]. 1) is 5-(aminosulphonyl) -4-chloro-2-[(2-fuanyl-methyl) amino] benzoic acid, a potent high ceiling (loop) diuretic, mainly used in the treatment of hypertension. It is a BCS class IV drug that is of low solubility (6 mg/L in urine) and low permeability (log P o/w 1.4)[2, 3].

Objectives

Results

Conclusion