FORMULATION AND IN VITRO–IN VIVO PHARMACOKINETIC EVALUATION OF CARDIOVASCULAR DRUG-LOADED PULSATILE DRUG DELIVERY SYSTEMS

Kumar Babu Pasupuleti,Venkatachalam A,Bhaskar Reddy Kesavan

doi:10.22159/ijap.2021v13i6.42607

Kumar Babu Pasupuleti, Venkatachalam A + Show 1 more

Open Access

https://doi.org/10.22159/ijap.2021v13i6.42607

Copy DOI

Abstract

Objective: This study is to formulate Nebivolol into a Pulsatile liquid, solid composite compression coated tablet, which will delay the release of the drug in early morning hypertension conditions. Methods: The liquid, solid composite tablet was formulated and compressed with the ethylcellulose coating polymer. The percent in vitro drug release of the liquid solid composite compressed tablet was tested. Based on disintegration time and wetting time, the LCS2, LCS3, LSC6, LCS7 and LCS12 formulations were found to be the optimized solid-liquid compacts fast-dissolving core tablet formulations, which may be excellent candidates for further coating with polymer to transfer into press coated pulsatile tablet formulations. Coating the core tablet with varying ethyl cellulose concentrations resulted in five different formulations of the pulsatile press-coated tablet (CT1, CT2, CT3, CT4, CT5). In vitro drug release, in vitro release, kinetic studies, in vivo pharmacokinetic and stability tests were all performed for the prepared pulsatile press coated tablet. Results: CT3 tablets are coated with ethyl cellulose polymer, which shows maximum controlled drug release from the core tablet i.e. 96.34±1.2% at 8th h. It shows there was an efficient delay in drug release form core tablet i.e. up to 3 h, followed by the maximum amount of drug release of 96.34±2.4 at 8h. Which shows the core drug will be more efficiently protected from the gastric acid environment 1.2 pH, duodenal environment 4.0 pH and release drug only in the small intestine. Conclusion: According to the findings, CT3 Pulsatile press-coated tablet increased the bioavailability of Nebivolol by 3.11 percent.

Highlights

Cos of the patient compliance and cost involved in therapy paves the oral route act as the most popular way for medications to be consumed among the many routes of drug administration
Pulsatile drug delivery systems (PDDS) are better for treating such disorders since they are characterized by a slow initial release of the drug, followed by a rapid and full release of the drug after a brief lag time
CT3 tablets are coated with ethyl cellulose polymer, which shown maximum and well-controlled drug release from the core tablet i.e., concentration 96.34±1.2% at 8thh time interval

Summary

Introduction

Cos of the patient compliance and cost involved in therapy paves the oral route act as the most popular way for medications to be consumed among the many routes of drug administration. Knowing the exact fate of medications following oral delivery in the body necessitates knowledge of gastrointestinal physiology (GIT). Pulsatile drug delivery systems (PDDS) are better for treating such disorders since they are characterized by a slow initial release of the drug, followed by a rapid and full release of the drug after a brief lag time. The majority of PDDS are reservoir systems with a barrier layer that dissolves, erodes, or ruptures with time, allowing for rapid drug release from the reservoir. Traditional PDDS, on the other hand, release the medication after 5-6 h and in physiological settings, typically in the large intestine. We generated timed-release pulsatile formulations for several medications using tablet and capsule technology [6, 7]

Methods

Results

Conclusion