Formulation and in vitro Evaluation of pH Dependent Colon Targeted Controlled Release Tablet of Mesalamine Containing Cyamopsis tetragonoloba Gum and Sodium Alginate

Abstract

Curiosity in colon-specific drug delivery has increased recently due to an increasing number of colonic ailments, such as diverticulosis, polyps, Irritable Bowel Syndrome (IBS), Ulcerative Colitis (UC), local bacterial infections, colorectal cancer, Crohn's Disease (CD), intestinal wound healing, and fistula. 3 By utilizing a variety of techniques, such as incorporating tablets with pH-sensitive polymers, prodrugs, pressure-control systems, osmotic pumps, and gastrointestinal tablets, one can target drug delivery not only for localized colonic diseases but also for protein and peptide delivery. 4 The existence of microbial flora in the colon ABSTRACT Objectives: The goal of the study was to treat ulcerative colitis by targeting drug delivery to the colon via the novel ingredient's guar gum and pH-dependent polymer sodium alginate. The drug was released at a high pH in the colon due to the sodium alginates. Guar gum was a novel ingredient that was used as a release retarder, binder, and swelling agent. The galactomannan enzyme naturally degrades the guar gum. Because this enzyme is only found in the human body's GIT colon, the tablet colon is naturally target-specific. Materials and Methods: The tablet was prepared through wet granulation using an IPA solution. The formed granules subjected to the pre-formulation studies had free flow ability and a uniform size or shape. After the pre-formulations, the tablets were formed using the ZP-17 machine, and post-compression studies such as the hardness test, friability test, weight variation test, and thickness or diameter test were performed. Results: The precompression and post-compression studies, including the hardness test, friability test, weight variation test, and thickness or diameter test, were in the specification. The disintegration test was performed on the tablets, but due to the swelling nature of guar gum, they did not disintegrate. The dissolution studies were performed for 24 hr using acidic and basic buffers. The drug releases at a basic pH of 7.4 in the presence of the galactomannose enzyme, which shows its pH dependence and colon targeting. The various kinetic models were used to release kinetic models. According to the kinetic release studies, the R 2 explained that formulations were controlled releases and followed the zero order, which is independent of drug concentration.

Fabrication and in-vitro characterization of mucoadhesive tablet using a natural biocompatible polymer containing metformin HCl

“…Carr's Index/Compressibility Index After weighing the ingredients, move them into a measuring cylinder. Determine the bulk volume (VB) without tapping, then tap until it reaches a constant volume, record the tapped volume (Vt), and use Carr's equation to calculate the compressibility index (Mustafa et al, 2023a). The following formula may be used to determine Carr's index.…”

“…Record the initial volume of the drug in the cylinder. Using a USP bulk density apparatus, tap the measuring cylinder 50 times (Mustafa et al, 2023a). Use the following formulas to determine the bulk density and tap density:…”

“…The fixed funnel was utilized at a height of 2.5cm (H) above a level surface, and paper was placed beneath. After pouring the powder through the inverted funnel, the diameter was found (Mustafa et al, 2023a). The angle of repose is determined through the following formula.…”

“…The temperature remained constant at 37°C. The time it took for the tablets to dissolve was recorded, and any remaining tablets were examined to ensure no fragments remained (Mustafa et al, 2023a).…”