Drug-Excipient Interaction during Formulation Development, in vitro andin vivo Evaluation of Gastroretentive Drug Delivery System for Nizatidine

Abstract

The present investigation dealswith the development and evaluation of floating tablets of nizatidine to prolong the gastric residence time, increase local delivery of drug to the H2-receptor of the parietal cell wall to reduce stomach acid secretion. The drug-excipient compatibility studies were conducted by using FTIR, DSC and visual observations. Citric acid inclusion in formulations resulted in incompatibility and the composition was modified to eliminate the problem of incompatibility. Floating matrix tablets of nizatidine were developed by direct compression method using hydroxypropyl methylcellulose (HPMC K4M) and polyox WSR 1105 alone as release retardants and sodium bicarbonate as a gas-generating agent. Alleleven formulations exhibited satisfactory physicochemical characteristics andin vitro buoyancy. Formulations F6 and F10 exhibited controlled and prolonged drug release for 10 h with zero order release. Formulation (F10) was selected as optimized formulation based on physicochemical properties and in vitro drug release and was used inradiographic studies by incorporating BaSO4. The radiographic studies were conducted in comparison with plain controlled release tablets. These studies revealed that gastric retention time of floating and plain controlled release tablets in fasting state were 2 ± 0.86 h and ≤ 0.5 h respectively in human volunteers. Gastric retention time of floating and plain controlled release tablets in fed state were 5.33 ± 0.57 h and 1.66 ± 0.28 h respectively in human volunteers. In conclusion, optimal floating matrix tablet for nizatidine with desired in vitro buoyancy, in vivo gastric retention time and prolonged release could be prepare

Development and Evaluation of Gastric Floating Tablets of Riboflavin Using Box-Behnken Design

“…The way drugs and excipients can physically or chemically interact with each other may affect how the drug and dosage form perform in terms of bioavailability, efficacy, stability, and safety [17]. As a result, FTIR studies were conducted to determine the chemical compatibility of riboflavin and the excipients used in the study.…”

“…The integrity of riboflavin seems to be maintained in the formulation as the major functional groups are unaltered. However, minor shifts or changes in weaker peaks that were not detected could still point to some degree of interaction [28]. More sensitive techniques may be needed to fully rule out any incompatibility.…”