Formulation, characterization and in vivo evaluation of novel edible dosage form containing nebivolol HCl

Pujari Vijayanand,Manda Venkata Reddy,Jagadevappa Patil

doi:10.1590/s1984-82502016000100020

Abstract

ABSTRACT The objective of this investigation was to develop a novel oral edible gel dosage form for nebivolol hydrochloride, with suitable rheological characteristics that can provide a means of administering the drug to dysphagic and geriatric patients. Edible gels were prepared using low acetylated gellan gum and sodium citrate in different concentrations. The effect of concentration of the solution on gelation time, viscosity, and drug release was studied. Optimized formulation had "spoon thick" consistency that is considered suitable for dysphagic patients as suggested by National Dysphagia Diet Task Force. The optimized formulation containing gellan gum (0.4 % w/v) and sodium citrate (0.3 % w/v) showed more than 95% drug release in 20 minutes. This formulation also showed significantly better pharmacokinetic profile when compared to marketed conventional tablets in New Zealand white rabbits (n = 3). Optimized formulation was found stable for 6 months when stored at 25 °C ± 0.2 °C/60 ± 5% RH. From this study, it can be concluded that the novel edible gel dosage form containing nebivolol hydrochloride may prove to be more efficacious in the treatment of hypertension in dysphagic patients.

Highlights

Oral administration of drugs is most preferred because of its ease of ingestion, no pain and improved patient compliance
There is clearly a need for a suitable dosage form that can address the low bioavailability of Nebivolol HCl (NEB) and eases the administration of drugs to dysphagic patients
Nebivolol HCl was obtained as gift sample from Aurobindo Pharma, Hyderabad, India

Summary

INTRODUCTION

Oral administration of drugs is most preferred because of its ease of ingestion, no pain and improved patient compliance. Nebivolol HCl (NEB) is a cardio selective third generation β-receptor blocking agent, used orally in the treatment of hypertension (Bystolic, 2007). After oral administration, it reaches peak plasma concentration within 0.5-2 h. There exists some white space for the development of edible dosage forms for elderly patients suffering from dysphagia coupled with other chronic diseases like hypertension. There is clearly a need for a suitable dosage form that can address the low bioavailability of NEB and eases the administration of drugs to dysphagic patients. This study tries to address the same by formulating NEB into novel oral edible gel (OEG) dosage form. We formulated the OEG using gellan gum as polymer and assessed the in-vitro and in-vivo performance of the same

MATERIAL AND METHODS

Methods

RESULTS AND DISCUSSION

Evaluation parameters

CONCLUSION