Abstract

PREPARATION OF CONTROLLED RELEASE TABLETS: A MINI REVIEW

R. Baskar*, J. Priyananga and S. Dharmarajsanthosam

.

Abstract

The current study uses 32 full factorial designs to show how the concentration of PEG 6000 as a melt binder and the ratio of HPMC K4M: PVP affect the formulations of Zolpidem tartrate controlledrelease tablets. Drug release at 1 hour (Q1), 4 hours (Q4), and 8 hours (Q8), diffusion coefficient (n), and release rate constant (K) were chosen as dependent factors. The ratio of HPMC K4M and PVP K30 (X1) and the concentration of melt binder (X2) were chosen as independent variables. By using the melt granulation process, tablets were created. The distribution of a medicine at a predetermined rate and/or to a specific place for a predetermined amount of time is referred to as controlled drug delivery. In addition to extending the time of drug delivery, which is comparable to the goal of sustained release and prolonged release, the term "controlled release drug administration" also suggests the predictability and reproducibility of drug release kinetics. An oral controlled release drug delivery device delivers medications continuously orally for a predetermined amount of time during GI transit at predictable and reproducible kinetics. To create once-a-day (OAD) pregabalin tablets, brand-new three-layered (TL) tablet systems were contrasted with both monolithic matrix (MM) formulations and a commercial immediate-release (IR) capsule. The pharmacokinetic parameters of the TL tablet were compared with those of an IR capsule in beagles and humans, as well as the physical characteristics of the TL tablets, including dissolving and swelling rates, with those of the MM tablets. Our findings showed that regardless of the tablet geometry, formulations containing the same quantity of a hydrophilic polymer at 12 h had comparable dissolving patterns. However, the extent of tablet swelling varied, with tablets that contained more polymer exhibiting a greater degree of swelling. Additionally, TL pills swelled quicker than MM tablets. The beagles showed absorption findings for the TL tablet that were comparable to those of an IR capsule, however the humans showed low overall absorption compared to an IR capsule. The findings of the beagle investigation were consistent with the highest plasma concentration of 6 hours in the fed condition of humans. The objective of this study was to increase the pace at which aceclofenac dissolves and to regulate its release throughout a 24-hour period. Hydrophilic polymers (HPMC/guar gum) were used in the direct compression method to create matrix tablets. Wet granulation was used to create matrix tablets utilising a variety of hydrophilic polymers (HPMC/guar gum). The purpose of the current study was to develop and assess ramipril sustained release tablets using xanthan gum, as well as to examine the effectiveness of these tablets in vitro and in vivo using rabbits as animal models. Ramipril sustained release tablets were created using the direct compression method. The current study's objective was to formulate and assess controlled release polymeric tablets of diclofenac potassium using the wet granulation method for the drug's release rate, pattern, and mechanism. Wet granulation was used to compress the formulations with various drug to polymer ratios (10:3, 10:1) and three grades of Ethocel (7P, 7FP, 10P, 10FP, 100P, 100FP). Co-excipients were introduced to a few particular formulations to see whether they would have an impact on how quickly drugs would release in vitro. To determine the drug release rate and patterns, in vitro drug dissolution tests using controlled release matrices for miglitol 25 mg were carried out in the current investigation. As rate-regulating polymers, hydroxypropyl methyl cellulose, hydroxypropyl cellulose, and hydroxyethyl cellulose were employed. In order to study the effects of adding hydroxypropylcellulose and hydroxyethylcellulose on in-vitro drug dissolution, hydroxypropylmethylcellulose was employed as the main rate-controlling polymer. Tablets were created with a total polymer content of 30, 35, and 40%, a standard hydroxypropyl methylcellulose polymer content of 20% across all batches, and a range of hydroxypropyl cellulose and hydroxyethyl cellulose concentrations between 10, 15 and 20%. Using USP Type II at 50 rpm in 900 ml of an acidic dissolving medium (pH 1.2) for two hours, then 900 ml of an alkaline dissolution medium (pH 7.4) for up to twelve hours, in-vitro drug release was performed. To ascertain the kinetics of drug release, various kinetic models were used to the dissolution profiles. The goal of the current endeavour was to create aspirin pills with controlled release. All of these formulations were created using the direct compression method. Levosulpiride is a commonly used gastroprokinetic medication that is used to treat a variety of stomach diseases, but due to its short half-life and higher dosage frequency, it is not often taken as prescribed, which might have unfavourable effects. The main goal of the current study was to create a Levosulpiride formulation with bioresorbable cellulose derivatives for prolonged release. Levosulpiride sustained-release formulations were created through direct compression employing a variety of cellulose derivatives as release-modifying polymers, including CMC sodium, HPC, and HPMC in various polymer-to-drug weight ratios. The outcomes also indicated that formulation F9, which exhibited sustained release behaviour, was the best formulation among those that had been developed. The goal of the current study is to create and assess Milnacipran HCL controlled release tablets using several grades of HPMC polymers, including HPMC K100M, HPMC K15M, and HPMC K4M. In order to create the controlled release tablets, direct compression was used. Studying the impact of polymers on the sustained release of captopril from tablets was the goal of the current investigation. DSC and Fourier transform infrared spectroscopy were used to investigate compatibility. Xanthan gum and ethyl cellulose were used in the direct compression procedure to create the tablets. The HPMC K4M and HPMC K100M polymers were used in the direct compression procedure to create the cisapride SR tablets. The formulation was improved using 32 full factorial designs with drug release kinetic analysis, compatibility studies (FTIR), and stability studies after various assessment tests, such as in vitro disintegration and dissolution. To determine the drug release rate and patterns, in vitro drug dissolution investigations were carried out on controlled release matrices containing 200 mg of mefenamic acid. Methocel was utilised as a polymer that controlled pace. During in vitro dissolution investigations, the impact of several co-excipients on the drug release rates was also examined. Methocel was manufactured with the medication at 4 distinct D:P ratios and employed as a rate-controlling polymer. Using the PharmaTest dissolving apparatus, phosphate buffer with a pH of 7.2 was employed as the dissolution media. The primary goal of the current effort was to create troxipide sustained release matrix tablets using hydroxypropyl methyl cellulose (HPMC). Different drug to polymer ratios, including 1:0.5, 1:1, 1:1.5, 1:2, 1:2.5, and 1:3, were chosen for the investigation. After adjusting the medication to polymer ratio, the drug release could be regulated for the desired amount of time. The in vitro release investigation was carried out in 0.1N HCl pH 1.2 for 2 hours and in phosphate buffer pH 6.8 for up to 12 hours following the examination of the tablet's physical qualities. It was found that the drug release from matrix tablets, which had a drug:polymer ratio of 1:2, was successfully sustained for up to 12 hours. Out of all the formulations, formulation F4's release profile was the best at releasing the medication according to zero order kinetics via swelling, diffusion, and erosion. Troxipide was found to be stable in the matrix tablets after three months of stability experiments (40°C/75%RH). There was no chemical interaction between the medication and excipients, according to the FTIR research. Dextromethorphan Hydrobromide Sustained Release (SR) Matrix Tablets were made by wet granulating hydrox-ypropyl methyl cellulose (HPMC-K-100 CR), a hydrophilic rate-controlling polymer. On the in vitro drug release rate, the impact of the polymer concentration and various fillers was investigated. The research showed that altering the concentration of the polymer and fillers could modify the medication release. On six healthy male volunteers, a thorough crossover bioavailability analysis of the developed sustained tablets and the commercialised immediate release tablets was conducted. Because of the SR tablets' longer half-life and lower clearance rate compared to commercial dextromethorphan hydrobromide tablets, there was a significantly higher degree of drug absorption.

Keywords: Tablets, Controlled release, Melt granulation, Solid dispersion, Direct compression.