Controlled Release Matrix Tablets Research Articles

Formulation and characterization: Metoprolol succinate controlled release matrix tablets

Metoprolol succinate-controlled release matrix tablets were made utilizing the wet granulation process with various ratio of Hydroxypropyl methyl cellulose (HPMC K4M). Isopropyl alcohol is used as a granulating agent in the Povidone (PVP K30) solution. In addition to being utilised as diluents to raise the weight of the tablets, magnesium stearate and talc were added to enhance the granules' flow ability during tablet compression. The crushed tablets underwent physicochemical characteristics, in-vitro and kinetic tests, and the micromeritic properties of the generated granules were evaluated. In every formulation, results were nearly satisfactory, with M4 being the best among the others. All of the formulations showed good correlation. The drug diffusion kinetics from matrix tablets appeared to be zero order, and the release mechanism was diffusion regulated.

Scaling up and evaluation of Dyphylline controlled release matrix tablets

The aim of the current study was to scale up controlled release matrix tablets of Dyphylline, used for the management of various respiratory conditions such as asthma, cardiac dyspnea, chronic bronchitis, and emphysema. The tablets were scaled up to 3500 tablets scale then the optimized formulations were further scaled up to 35000 tablets. Tablets were manufactured using direct compression, wet granulation, and hot melt methods. The prepared tablets were evaluated for Hardness, Friability, content uniformity, in-vitro drug release, and stability study. The results obtained showed that the ten prepared tablets showed accepted values for the hardness, friability, and content uniformity tests. The formulations showed controlled drug release profiles with high similarity to our target release profile (f values ranged from 63.9 to 84.9). The release profiles showed a better fit to zero order than diffusion model. The Exponent n of Korsmeyer-Peppas model ranged from 0.67 to 0.692 indicating non-Fickian diffusion. The stability study indicating good stability of the selected formulation. All these results concluded that formulation prepared by wet granulation can be manufactured on large scale perfectly.

Preparation and in-vitro evaluation of dyphylline controlled release matrix tablets

Preparation and in-vitro evaluation of dyphylline controlled release matrix tablets

Formulation development and evaluation of controlled release matrix tablets of glibenclamide

The present study aimed to formulate and evaluate the controlled-release matrix tablets of Glibenclamide which is an antidiabetic drug that belongs to the second-generation oral hypoglycemics. Matrix tablets were prepared by three different polymers as sustained-release agents, using Glibenclamide as a model drug. Three polymers were selected for this study- HPMC K 15, HPMC K 100, and EC in different drug: polymer ratios. The drug was identified by FTIR spectroscopic method. The pre-compression and post-compression parameters of all formulations were found to be within acceptable limits. The release rate of Glibenclamide from matrix tablets was studied using the USP Dissolution Testing Apparatus type-I (Basket method). The formulation F6 which contained EC 50mg showed a maximum release of 99.28% in 24 hrs and revealed that EC was more effective in sustaining the drug release therefore formulation F6 was selected as the optimized formulation. The in-vitro release data of optimized formulation was fit into various kinetic models, among the different model's data of in-vitro release of best fit into Zero order kinetic model. The formulation best fit the Higuchi model and showed that drug release from the prepared matrix tablets occurs via a diffusion process.

Physicochemical and Pharmacokinetic Studies of Metformin for Development of Controlled Release Matrix Tablet: Formulation Optimization Using in silico Tools

Metformin, taken by nearly 120 million people across the world as a treatment for type 2 diabetes, has a relatively short plasma half-life and low absolute bioavailability. In this study, physicochemical and pharmacokinetics properties of metformin have been thoroughly assayed using ADMETLab, SwissADME, SmartCYP, LigandScout web-servers and software to evaluate the effectiveness of its formulation as controlledrelease matrix tablets. The objective of the present work was to develop a formulation of an oral controlled-release (CR) metformin tablet, using hydrophilic hydroxylpropylmethylcellulose (HPMC) grades K4M and K100M polymers at different concentrations utilizing computational simulatory tools. Intestinal membrane permeability of the drug has been assayed using 2 hours simulation run with MembranePlus Software. Simulated environment generated for in silico dissolution study, using DDDPlus software, of the prepared formulations used USP Apparatus Type 2 rotating at 100 rpm. The simulation run was for 2 hours using 0.1N HCl phase followed by 8 hours with 6.8 USP Phosphate buffer phase. The results showed that drug release from the higher viscosity grade, K100M was slower as compared to the lower viscosity grade K4M at a fixed polymer concentration level. Furthermore, plasma concentration-time curves for the formulations have been generated using GastroPlus software. Dhaka Univ. J. Pharm. Sci. 22(1): 29-42, 2023 (June)

Development of controlled-release matrix tablets of anti-diabetic agent using natural and synthetic polymers

The aim of this study was to develop and produce natural polymer-based controlled-release matrix tablets of metformin hydrochloride. The formulations were manufactured from a mixture of natural and synthetic polymers, including gum copal, gum damar, gum olibanum, xanthum gum, and hydroxypropyl methylcellulose (HPMC) K15M. The granules were characterized by Fourier transform infrared spectroscopy (FTIR). The kinetics of drug release from the formulations was determined by zero-order kinetic analysis. The formulas were found to be in the following ranges: 4.20.054 to 5.10.58 ​kg/cm2, 844.86.84 to 852.64.13 ​mg, 0.230.002 to 0.670.048 percent, and 99.450.15 to 101.930.16 percent, respectively. For all formulations, it was found that Carr's index, Hausner's ratio, bulk density, tapped density, and angle of repose were less than 15% and 1.18, respectively, indicating that the generated tablets had acceptable flow properties. Formulations F3, F4, and F5, which contained varying amounts of gum copal, showed respective drug release rates of 91.21 percent, 85.69 percent, or 99.87 percent after 12 ​h. For formulations F11, F12, and F13, which included varying quantities of olibazine gum, after 10, 10, and 9.5 ​h, it generated 100% drug release after 10, 10.5, and 10 ​h. Formulation F5 which included gum copal, and the HPMC showed sufficient release to exert the necessary therapeutic effect in under 12 ​h, whereas the other formulations showed anomalous or non-Fickian diffusion. This study suggests that matrix tablets for continuous controlled release can be made.

Study the effect of polymers on the release rate of propranolol hydrochloride from controlled release matrix tablets

Study the effect of polymers on the release rate of propranolol hydrochloride from controlled release matrix tablets

Influence of formulation and process variables on physical characteristics and dissolution behavior of controlled release matrix tablets

Influence of formulation and process variables on physical characteristics and dissolution behavior of controlled release matrix tablets

Formulation and Evaluation of Controlled Release Tablet of Irbesartan

The main aim of present work was to formulate and evaluate controlled release matrix tablets of Irbesartan. It releases drugs at fixed and expected rate in a controlled manner either by dissolution and diffusion control mechanism. The matrix tablet was prepared by wet granulation method using by various concentration of HPMC and ethyl cellulose with combination of various release retardant polymer. The powder mixtures were subjected to various pre- compression parameters such as angle of repose, bulk density, tapped density and Carr’s index shows satisfactory result and the compressed tablets are evaluated for post- compression parameters such as weight variation, thickness, hardness, friability, drug content and in- vitro dissolution studies. In- vitro dissolution studies were carried out for 24 hours using 0.1N HCL for first 2 hours and ph 6.8 phosphate buffers for 24 hours and the result showed that formulations F3 and F4 show good dissolution profile to control the drug release respectively. The drug content of the formulation was determined by using 0.1 N HCL at 262nm. The drug content was maximum with formulation F5 and minimum with formulation F3.

Geometry in Pharmaceutical Systems

The aim of the paper is to brief out geometry in pharmaceutical systems, i.e., influence of tablet surface area/volume (SA/Vol) on drug release from controlled-release matrix tablets containing hydroxyl propyl methyl cellulose (HPMC) and describes a situation where the erosion rates of the tablet are different in the radial and axial directions, 3D printing technologies available for the manufacture of modern medicines and so on.

Preparation of Losartan Potassium Controlled Release Matrices and In-Vitro Investigation Using Rate Controlling Agents.

Controlled release matrices have predictable drug release kinetics, provide drugs for an extended period of time, and reduce dosing frequency with improved patient compliance as compared with conventional tablet dosage forms. In the current research work, losartan potassium controlled release matrix tablets were fabricated and prepared with rate altering agents; that is, Ethocel grade 100 combined with Carbopol 934PNF. Various drug to polymer ratios were used. HPMC, CMC, and starch were incorporated in some of the matrices by replacing some amount of filler (5%). The direct compression method was adopted for the preparation of matrices. In phosphate buffer (pH 6.8), the dissolution study was conducted by adopting the USP method-I as the specified method. Drug release kinetics was determined and dissolution profiles were also compared with the reference standard. Prolonged release was observed for all matrices, but those with Ethocel 100FP Premium showed more extended release. The co-excipient (HPMC, CMC, and starch) exhibited enhancement in the drug release rates, while all controlled release matrices released the drug by anamolous non-Fickian diffusion mechanism. This combination of polymers (Ethocel grade 100 with Carbopol 934PNF) efficiently extended the drug release rates up to 24 h. It is suggested that these matrix tablets can be given in once a day dosage, which might improve patient compliance, and the polymeric blend of Ethocel grade 100 with Carbopol 934PNF might be used in the development of prolonged release matrices of other water-soluble drugs.

Assessment of Once Daily Controlled-release Ibuprofen Matrix Tablets Prepared using Eudragit ®E100/Carbopol® 971P NF Polymers and their Salt Combinations.

Hydrophilic polymers that swell or dissolve in aqueous media can have the potential to prepare controlled/sustained dosage forms for weakly acidic and poorly soluble drugs. The main objective of this study is to utilize Eudragit®E100 (EE) and Carbopol®971P NF (Cp) polymers and their salt forms for the preparation of a once-daily controlled-release matrix tablet for model drug, Ibuprofen (IB). Combinations of the polymers in their base forms (EE)/(Cp) or in their salt forms (EEHCl/ CpNa) were compressed with (IB) into single layer matrix tablets, or otherwise into bilayer tablets. Dissolution profiles were constructed using three different consecutive stages (pH 1.2, 4.8 and 6.8). It was found that the incorporation of (EEHCl) modified the release rates of (IB) from (Cp) based matrix tablets. However, a major enhancement of (IB) release rates occurred when the polymers were combined in their salt forms in a 1:1 ratio by weight. In addition, a bilayer tablet was prepared wherein a relatively rapidly disintegrating layer composed of polymers salts (EEHCl and CpNa), and a second layer containing only (Cp) polymer in its base form in a 1:2 weight ratio possessed excellent release properties and mechanical strength. It was concluded that the prepared bilayer tablet could be promising for controlling the release rates of (IB) in an extended manner to allow once-daily administration with an improved pH-independent release behavior.

Controlled Release Formulation of Tofacitinib Citrate Tablets Evaluated Using Quality by Design (QBD) Approach

The goal of the project is to use the quality-by-design (QbD) method to create and optimise Tofacitinib citrate matrix tablets with controlled release excipients. The drug's physicochemical parameters, reference product characterisation, QTPP (Quality Target Product Profile), and CQAs were used to start product development (Critical Quality Attributes). Hypromellose (Methocel K100 premium LV CR), Polyethylene Oxide (SentryPolyox WSR N80 LEO), and Magnesium Stearate were used as formulation variables and were optimised together. The complete factorial design of experiment (DOE) with three centre points was used to investigate traditional monolithic controlled release matrix tablets. Using Design-expert12 programme, dissolution was assessed as CQA. At acidic pH, hypromellose with a higher viscosity grade provides a regulated release pattern by retaining the integrity of the medication and preventing rapid drug release. Due to the nonionic nature of the polymer, drug release from the polymer matrices is pH independent. Present monolithic controlled release matrix system the extensive degradation of Tofacitinib Citrate in the acidic condition can be avoided with desired in-vitro drug release.

Formulation and Evaluation of Controlled Release Matrix Tablets of Cefixime Trihydrate

Abstract: The main objective of the present work was to develop sustained release matrix tablets of Cefixime Trihydrate were prepared by direct compression techniques and evaluates the effect of formulation variables such as lubricant, binder, polymer content and viscosity grades of HPMC on the behavior of Cefixime Trihydrate release. The prepared tablets were evaluated for various physico-chemical parameters. In vitro release profile was check to evaluate the sustained release matrix tablet of Cefixime Trihydrate. The drug release from the optimized formulation was found to follow zero order kinetics. Thus the phenomenon of drug release showed that the release of optimized formulation is controlled by diffusion. Administration of Cefixime Trihydrate in a sustained release dosage would be more desirable for bacterial infections effects by maintaining the plasma concentrations of the drug well above the therapeutic concentration. From In vitro dissolution profile, Formulation S3 was prepared with Hydroxypropyl methylcellulose (K15M) combination where drug release was about 99.14% at the end of 24 hrs and followed zero order with non-Fickian diffusion method. It is selected as the best formulation.

Physiologically relevant model to establish the in vivo-in vitro correlation for etamsylate controlled release matrix tablets

BackgroundIn vivo-in vitro correlation (IVIVC) are used during product development for optimization of drug formulations and can serve as a surrogate for bioequivalence studies. AimThis research was performed to investigate the in vitro dissolution and in vivo pharmacokinetics of different etamsylate immediate release (IR), and two controlled release (CR) matrix tablets with different dissolution rates; CRfast and CRslow. Also, to develop a simple physiological model to establish the IVIVC for etamsylate CR tablets. MethodThree different formulations containing 500 mg etamsylate were developed; IR, CRfast, and CRslow tablets. The in vitro dissolution of the IR tablets was examined at different pHs, while the in vitro dissolution of the CR tablets was performed by the buffer transition method, where the pH of the dissolution medium was changed throughout the 12-h dissolution experiment. A group of eight healthy volunteers received one tablet of each formulation, in a three-way cross-over experimental design, with one-week wash-out period between treatments. The pharmacokinetic parameters of etamsylate after the three treatments were estimated. A model that utilized the in vitro dissolution data, the estimated pharmacokinetic parameters after the IR tablets was developed to establish the IVIVC for the CR tablets. ResultsThe in vitro dissolution of the IR tablets showed a pH-dependent dissolution. The plasma concentration-time profile after administration of etamsylate IR tablet followed one-compartment model with first-order absorption and elimination. The maximum concentrations were 7.52 ± 2.1, 3.93 ± 0.96, and 3.13 ± 0.27 mg/L, and the time to achieve the maximum concentration was 5, 8, and 10 h, and the area under the curves were 80.2 ± 13.73, 69.4 ± 12.97, and 61.1 ± 0.44 mg-h/L for the IR, CRfast and CRslow tablets, respectively. There was a good agreement between the model-predicted concentration-time profile and the experimentally observed drug profile after administration of the two CR formulations. The model predicted Cmax and AUC were within 10% of the observed Cmax and AUC. Also, there was very good correlation between the time-scaled % in vivo absorption and the % in vitro dissolution for the two CR matrix tablets, indicating validity of the model. ConclusionThe use of the buffer transition method was appropriate in predicting the in vivo dissolution of the developed CR matrix tablets. The developed model was valid in the establishment of the IVIVC for etamsylate CR tablets.

An Updated Overview on Mucoadhesive Buccal Drug Delivery System

Among the various routes of drug delivery, the oral route is an attractive site for the delivery of drugs. The main advantages of these formulations are: drug targeting, sustained release, increased permanence time in the buccal mucosa, increased bioavailability, and decreased potential adverse effects and maintains constant blood levels for extended period of time. The buccal cavity was found to be the most suitable and easily accessible site for the delivery of therapeutic agents for both local and systemic delivery. Buccal mucosa has a tremendous availability, which leads to direct access to systemic circulation through the internal jugular vein bypasses the drug from hepatic first pass metabolism. The main disadvantage of this route is Limited absorption area- the total surface area of the membranes of the oral cavity available for drug absorption is 170 cm2 of which ~50 cm2 represents non-keratinized tissues, including buccal membrane, the barrier function of the skin changes from one site to the other and from one person to other person with age and large dose of drug are difficult to be administered. Melt granulation is emerging technique and this technique used to increase the dissolution rate of poorly water-soluble drugs. Tablet molding technique: Tablets produced by the molding technique are easier to scale up for industrial manufacture than lyophilisation technique. Hot melt extrusion of film method: Hot melt extrusion has been used for the manufacture of controlled release matrix tablets, pellets and granules, as well as oral disintegrating films.

FORMULATION DEVELOPMENT AND EVALUATION OF HIGHLY WATER-SOLUBLE DRUG-LOADED CONTROLLED RELEASE MATRIX TABLETS

Formulation of controlled release matrix tablets of Itopride hydrochloride (ITP) was done using direct compression method. Different polymers were used to evaluate the influence of different types (HPM, EC, Kollidon® SR), concentration (20-40%) and viscosity grade (HPMC-4000 cps, HPMC-100000 cps, EC-10 cps and Kollidon SR) on drug release. Twelve different tablet formulations were designed with constant amount of ITP in each tablet formulation (150 mg). The dissolution studies of CR matrix formulations were carried out in acidic buffer (pH 1.2) and phosphate buffer (pH 6.8). Drug release kinetics was studied for first order, Zero-order, Higuchi, Korsmeyer-Peppas and Weibull models using DD Solver (an add-in software for MS Excel). Formulation ECF7, ECF8 and ECF9 containing EC (20-40%) greatly controlled the release rate of drug over an extended period of 12 hr. However, drug release from tablets formulations K4F3, K100F5 and ECF8, followed zero-order kinetics with regression coefficient of 0.966-0.999. The release mechanism of tablets formulations K4F2, KK4F3, K4F4, ECF7, KSRF10, KSRF11 and KSRF12 were non-fickian diffusion, whereas the release mechanism from formulations K4F1, K100F5, K100F6, ECF8 and ECF9 were super case-II transport mechanism. It was concluded that HPMC and ethylcellulose (EC-10cps) in the percentage range of 20-30% were excellent release controlling polymers for itopride HCl.

A Detailed Review on Oral Controlled Release Matrix Tablets

A Detailed Review on Oral Controlled Release Matrix Tablets

Starch-based controlled release matrix tablets: Impact of the type of starch

Different types of starches were used to prepare controlled release tablets loaded with diprophylline by direct compression. The impact of the natural origin of the starch, potential chemical modifications (e.g., cross-linking with phosphate or adipate, hydroxypropylation, acetylation to different degrees, partial hydrolysis) and type of pre-gelatinization process (laboratory scale with ethanol and oven drying versus industrial scale drum drying) on the resulting drug release kinetics were studied. Texture analysis of the hydrogels created upon exposure to the release medium, optical and scanning electron microscopy as well as X-ray powder diffraction measurements were used to better understand the observations. Also, a “quick test” using a texture analyzer to rapidly estimate the capacity of a specific starch type to control the resulting drug release rate was proposed. Two types of hydroxypropyl methylcellulose (HPMC K100 M and K100 LV) were studied for reasons of comparison. Interestingly, the “quick test” allowed to detect differences in the mechanical strength of the hydrogels formed upon contact with aqueous fluids, which correlated well with the observed drug release patterns from tablets when measured using a USP III (“Bio’-Dis”) apparatus at 30 rpm. However, diprophylline release was not very much affected by the investigated starch types when using a USP basket apparatus at 75 rpm. This can be attributed to the much lower mechanical stress experienced by the hydrogels under these conditions. Furthermore, caution must be paid when studying starch types, which are pre-gelatinized at the laboratory scale using ethanol precipitation and oven drying. The obtained starch granules can have significantly different key properties compared to granules obtained by industrial scale drum drying, resulting in substantially different drug release patterns.

Design and In Vitro Evaluation Of Controlled Release Matrix Tablets Of Prazosin

Design and In Vitro Evaluation Of Controlled Release Matrix Tablets Of Prazosin