Sustained Release Matrix Tablets Research Articles

Clinical Investigation of Valsartan Sustained-Release Matrix Tablets: Formulation Design and Performance Evaluation

The primary objective of this main study is to develop and assess the sustained-release matrix tablets containing Valsartan, an angiotensin II receptor type 1 antagonist. The powder mixtures underwent a thorough examination of pre-compression parameters and observed angle of repose, bulk density, tapped density, and Carr’s index, all of which exhibited satisfactory results. Following compression, the tablets were subjected to post-compression evaluations, including weight variation, thickness, hardness, friability, drug content, in-vitro dissolution, and stability studies. In-vitro dissolution investigations are conducted over 24 hours, employing 0.1 N HCL for the initial 2 hours and pH 6.8 phosphate buffer for the subsequent 24 hours. Notably, formulations F4 and F7 demonstrated promising dissolution profiles, effectively controlling the release of the drug. These formulations, enriched with higher concentrations of chitosan and sodium alginate in addition to other polymers, successfully sustained the drug release for the entire 24-hour duration. The compatibility of the drug, polymers, and other excipients was meticulously assessed using FT-IR Spectroscopy, affirming the harmonious interaction among these components. Further analysis involved fitting the release data to various mathematical models, including Zero-order, First-order, Higuchi equation, and Korsmeyer-Peppas model, to ascertain the kinetics and mechanisms governing drug release. Results indicated that the drug release adhered to first-order kinetics, with a non-Fickian mechanism prevailing. Stability studies conducted for 3 months provided reassurance regarding the stability of the selected formulations (F4 and F7), bolstering confidence in their potential for sustained release of Valsartan.

Preparation and Evaluation of Sustained Release Matrix Tablets of Acelofenac and Comparision of Formulated and Marketed Product

The aim of performing this study is to develop matrix tablet to improve the dissolution rate of aceclofenac and release the drug in a controlled manner over a period of 24 hours. Matrix tablets of aceclofenac, using various viscosity of hydrophilic polymer HPMC in two different proportions, hydrophobic polymer ethyl cellulose and Guar gum were prepared by wet granulation method and subjected to in vitro drug release studies. Tablets were evaluated for in vitro drug release profile in phosphate buffer with pH 7.5. The thickness and hardness of prepared tablets were 3.8 ± 0.2 to 3.9 ±0.2 mm and 4 ± 3 to 5 ± 3 kg/cm2, respectively. The friability was within the acceptable limits of pharmacopeial specifications (0.31 to 0.71%), which indicates the good mechanical strength of the tablets. The in vitro drug release from the proposed system was best explained by Higuchi’s model, indicating that drug release from tablets displayed a diffusion-controlled mechanism. Based on the study results, formulation F7 was selected as the best formulation.

Design and Characterization of Mangiferin Sustained-Release Tablets

Background: Mangiferin is a natural bioactive compound used for various pharmacological activities like antidiabetic, anticancer, and anti-inflammatory. Objective: The development of unique sustained-release matrix tablets of mangiferin is the purpose of the work that is being presented here. Method: In this study, an effort is made to formulate mangiferin sustained-release matrix tablets by combining the sustained-release polymers HPMC K100M, Kollidone@SR, Keltone LVCR. Mangiferin matrix tablets have been synthesized by wet granulation utilizing the lactose works as the diluent. Systems were developed with different polymer percentages. Results: Refine the design based on observed differences in weight, hardness, thickness, percent friability, percent drug content, and in-vitro drug release. In-vitro release trials conducted by utilizing a USP type II device utilizing a 6.8 pH phosphate buffer as the separation medium revealed that the most successful F2 formulation, which included 20% polymer, was capable of supporting the mangiferin release for a time of 12 hours period. This sample showed the greatest coefficient (R) value in the Hixson-Crowell model, and release kinetics studies showed that this sample exhibited an erosion process and followed zero-order kinetics. Conclusion: We can conclude that Kollidone@Sr can be used to prepare sustained-release mangiferin.

Formulation and Evaluation of Sustained Release Matrix Tablet of Valsartan

The aim of this study was to develop antihypertensive matrix tablets with sustained release of valsartan, an angiotensin type II receptor antagonist, using hydroxypropyl methylcellulose and combination of ethyl cellulose material as matrix in different proportions by wet granulation. The granules are evaluated by tapped density, bulk density, angle of repose and compressibility index. The tablets are tested for friability, hardness, weight variation and in vitro release. The granules showed good flow properties and compressibility properties and all tablet formulations showed pharmaceutical properties. The result of dissolution study indicate that the formulation prepared by combination of high grade HPMC K100M and ethyl cellulose showed maximum drug release for 12hrs and high drug release around 98.56% i.e., Formulation F8 is the best formulation.

Formulation and Evaluation of Miglitol Sustained Release Matrix Tablets Using Moringa Oleifera Gum

Formulation and Evaluation of Miglitol Sustained Release Matrix Tablets Using Moringa Oleifera Gum

Formulation and Evaluation of Propranolol Hydrochloride Sustained Release Matrix Tablets Using Different Grades of HPMC and MCC

Formulation and Evaluation of Propranolol Hydrochloride Sustained Release Matrix Tablets Using Different Grades of HPMC and MCC

Formulation and Evaluation of Cola acuminata Gum-based Mucoadhesive Sustained-release Matrix Tablets of Diclofenac Sodium.

This study aimed to evaluate Cola acuminata gum (CAG) for the formulation of mucoadhesive sustained-release matrix tablets of diclofenac sodium. Different batches of granules containing CAG and 100 mg of DS in ratios 0.5:1, 1:1, 2:1, and 3:1 were prepared, compressed into tablets, and evaluated for mucoadhesive strength, swelling index, and drug release in SGF (pH 1.2) and SIF (pH 7.4). Swelling indices and mucoadhesive strengths of the tablets were pH-dependent. Swelling indices of 56 ± 2.03 to 121 ± 2.19% and mucoadhesive strengths of 7.25 ± 1.45 to 15.43 ± 2.71 g/cm2 obtained at pH 7.4 were significantly higher (p<0.05) than swelling indices of 25 ± 2.43 to 47 ± 3.15% and mucoadhesive strengths of 5.52 ± 0.76 to 9.22 ± 1.95 g/cm2 obtained at pH 1.2. The percentage release of DS from the matrix tablets at pH 1.2 after 2 h (T2h) was insignificant. However, the percentage of drug release at pH 7.4 was significant for all the batches and dependent on the CAG concentration. The drug release was in the order of batches containing 3 g (80.44 ± 7.75) < 2 g (86.35 ± 5.65) < 1 g (90.08 ± 6.14) < 0.5 g (99.70 ± 3.90). The time for maximum drug release was 7 h (T7h) for CAG containing 0.5 g and 10 h (T10h) for other batches. This study showed that CAG could be useful for mucoadhesive sustained drug delivery.

Integration of artificial neural network and physiologically based biopharmaceutic models in the development of sustained-release formulations.

Model-informed drug development is an important area recognized by regulatory authorities and is gaining increasing interest from the generic drug industry. Physiologically based biopharmaceutics modeling (PBBM) is a valuable tool to support drug development and bioequivalence assessments. This study aimed to utilize an artificial neural network (ANN) with a multilayer perceptron (MLP) model to develop a sustained-release matrix tablet of metformin HCl 500mg, and to test the likelihood of the prototype formulation being bioequivalent to Glucophage® XR, using PBBM modeling and virtual bioequivalence (vBE). The ANN with MLP model was used to simultaneously optimize 735 formulations to determine the optimal formulation for Glucophage® XR release. The optimized formulation was evaluated and compared to Glucophage® XR using PBBM modeling and vBE. The optimized formulation consisted of 228mg of hydroxypropyl methylcellulose (HPMC) and 151mg of PVP, and exhibited an observed release rate of 42% at 1h, 47% at 2h, 55% at 4h, and 58% at 8h. The PBBM modeling was effective in assessing the bioequivalence of two formulations of metformin, and the vBE evaluation demonstrated the utility and relevance of translational modeling for bioequivalence assessments. The study demonstrated the effectiveness of using PBBM modeling and model-informed drug development methodologies, such as ANN and MLP, to optimize drug formulations and evaluate bioequivalence. These tools can be utilized by the generic drug industry to support drug development and biopharmaceutics assessments.

Formulation and Evaluation of Sustained Release Matrix Tablet Metformin Hydrochloride

Abstract: The present study outlines a systematic approach for designing and development of Metformin Hydrochloride sustained release matrix tablets. Different formulations were formulated by wet granulation technique using Xanthan gum and HPMC K100M as polymers along with other excipients The formulations were evaluated for their physicochemical properties.

Formulation, Evaluation and Comparison of Sustained Release Matrix Tablet of Losartan Potassium Using Natural Polymers

Formulation, Evaluation and Comparison of Sustained Release Matrix Tablet of Losartan Potassium Using Natural Polymers

Preparation, Characterization and Optimization of Sustained Release Matrix Tablets of Repaglinide using Box–Behnken Design

The aim of this investigation was to develop and optimize the Sustained release Matrix formulations of Repaglinide (RLD) using response surface methodology by employing a 3-factor, 3-level Box–Behnken statistical design. The independent variables studied were the amount of hydroxypropyl methylcellulose (HPMC K4M), Ethyl cellulose (EC) and PVP K30. The Swelling index (Y1), drug release at 8 hr and 12hr were the target responses. The response surface methodology and multiple response optimizations utilizing a polynomial equation were used to search for the optimal formulation with a specific release rate at different time intervals. The results showed that the effect of combination of HPMC K4M and EC was the most influencing factor on the drug release from ER matrix tablets. The mechanism of drug release from RLD Matrix tablets was dependent on the added amount of EC. Validation of the optimization technique demonstrated the reliability of the model. The optimized formulation containing 50mg of HPMC K4, 35mg of EC, and 30mg of PVP K30 was prepared according to the software determined levels. DSC and FTIR studies combined with the stability study of the optimized formulation proved the integrity of the developed formulation. The Box–Behnken experimental design facilitated the formulation and optimization of extended release hydrophilic matrix systems of RLD in a short period of time and with the fewest number of experiments. The optimized Matrix tablet of Repaglinide showed good pharmacokinetic result over conventional formulation.

Formulation and Evaluation of Novel Aceclofenac Matrix Tablet Using Natural Polymers

The current study attempted to design and create Aceclofenac sustained release matrix tablets employing different proportions of Hibiscus rosa-sinensis mucilage, Mimosa Pudica mucilage as natural polymers and povidone.Aceclofenac is widely used as a centrally acting muscle relaxant; therefore, have been selected to prepare sustained release dosage forms.Different types of evaluation parameters were evaluated like appearance, thickness, diameter, weight variation, hardness, friability, drug content, in-vitro dissolution studiesand stability studies.Sustained release matrix tablets can improve patient compliance by lowering the total dose and dosing schedule, which can be extremely beneficial in the treatment of chronic illnesses.&#x0D; Key words:S, , .

EVALUATION OF VATERIA INDICA MODIFIED GUM AS A RELEASE RETARDANT MATRIX IN THE TABLET DOSAGE FORM

Objective: A natural gum from Vateria indica was investigated as a novel matrix-forming material for sustained drug delivery using diclofenac potassium as a model drug. Methods: In the current investigation, we formulated a matrix tablet using chloroform soluble gum portion of Vateria indica modified gum (VIMG) as a natural matrix-forming agent. It was used with a drug-polymer ratio ranging from 1:0.5 to 1:4.5. The pre-compression study of the powder blends was done by calculating bulk density, tapped density, angle of repose, and carr’s index, compressibility, and hausner’s ratio. The tablets were prepared by direct compression method and prepared tablets were evaluated and were found according to the official guidelines by pharmacopeia. The in vitro drug release was carried out using USP paddle type II apparatus and the release was found to be sustained. Results: The formulation VIMG-5 containing drug: polymer ratio 1:2.5 showed the 96.26%±1.73 drug release in 12 h. The results showed that chloroform soluble fraction of Vateria indica can be used as a drug release modifier to delay the rate of drug release, which depended on the amount of gum composition, as the concentration of gum was increased, there was sustained the drug release with promising accelerated stability. Conclusion: The evaluation studies on sustained release matrix tablets using Vateria indica chloroform soluble portion of gum as natural material demonstrate the multivariate applications such as matrix forming, binder, and release retardant of the gum in tablet formulation.

A review of medicines with sustained release

Sustained-release matrix tablets allow for continuous drug release while also optimizing a drug's biologic, pharmacokinetic, and pharmacodynamic properties for maximum therapeutic efficacy. The matrix regulates the rate at which the drug is released. Because it facilitates prolonged release, the major excipient in the formulation is a release retardant. The technology may promote patient compliance and efficiently treat chronic illnesses by decreasing the overall dosage and dosing schedule. The drug is supplied in this system via diffusion- and dissolution-controlled methods. The primary goal of this analysis is to provide comprehensive information on the sustained release system and to discuss the many selection criteria for medicines used in medication administration system

Formulation and Evaluation of Sustained Release Linezolid Tablet using Natural Antibacterial Polymer - &lt;i&gt;Aegle marmelos&lt;/i&gt;

The objective of the current research study was to formulate and evaluate a sustained-release linezolid tablet using the natural antibacterial polymer Aegle marmelos. The natural gum of Aegle marmelos is becoming increasingly used in pharmaceutical formulations as a beneficial medication with excipients. Natural-based plant materials are biocompatible, free of side effects, biodegradable, and economic. Therefore, in order to maintain the drug releases from the matrix system, Aegle marmelos fruit gum as a natural polymer and HPMC grade (K100M) as a synthetic polymer were used in the formulation of the linezolid matrix tablet. The formulation of sustained-release matrix tablets included the wet granulation technique. The formulated matrix tablets were evaluated in terms of weight variation, hardness, diameter, physical appearance, friability, thickness, and in vitro drug release. Each formulation’s matrix tablet passed the required physical assessment tests. The formulation analyses of the tablets’ dissolution showed sustained releases of drugs for up to 10–12 hours. Additionally, several polymer combinations and fillers were used to improve drug release factors using the 32 factorial design approach, drug release kinetics were optimized, and the antibacterial study was evaluated.

Design and Evaluation of Colon Targeted Sustained Release Matrix Tablet of Naproxen Sodium

Design and Evaluation of Colon Targeted Sustained Release Matrix Tablet of Naproxen Sodium

Novel Approaches of Polyherbal Matrix Tablet and its Evaluation Parameters

According to WHO, approximately 80 percent of people in developing countries still rely on traditional medicine, which is based primarily on plant and animal species, for primary health care. Because of the toxicity and side effects of allopathic drugs, herbal therapy is becoming more popular. Medicinal plants are crucial in the development of powerful therapeutic agents. Natural products derived from plants, animals, and minerals have long been used to treat human disease Plant medicines are frequently used in combination rather than alone to maximise the benefit of their combined strength. Because of synergism, polyherbalism provides a variety of benefits not found in single herbal formulations. Polymers are the building blocks of a pharmaceutical drug delivery system because they control drug release from the device. Polymers are used to protect drugs from the physiological environment and to extend their release time in order to improve their stability. This review focuses on matrix tablets, which are one of the most practical methods for developing sustained-release dosage forms, as well as the approaches used in their formulation and evaluation. The therapeutic efficacy of a sustained release matrix tablet with improved efficacy can be increased. It also emphasizes the significance of polyherbalism and matrix Tablet.

Role of Aminated Derivatives of Natural Gum in Release Modulating Matrix System of Losartan Potassium

Objective: The investigation aimed to synthesize amino derivatives of various natural gums like Xanthan gum and Tamarind gum for using them as a release modulating polymer in the formulation of the hydrophilic matrix system of losartan potassium and to find the best amongst them. Developing oral sustained release matrix tablets for a drug with a constant release rate has always been a challenge to the pharmaceutical technologist. &#x0D; Materials and Methods: Release modulating hydrophilic matrix tablets of losartan potassium were prepared by wet granulation method. A total number of 6 formulations of release modulating hydrophilic matrix tablets of losartan potassium were prepared using different polymeric ratios of Carbopol 934, aminated Tamarind gum and aminated Xanthan gum based on preliminary trial bathes. The formulated tablets were evaluated for both pre-compression and post-compression evaluation studies. &#x0D; Results: Based on in vitro drug release study the effective formulations AXG 3 are shows a maximum similar release profile to other remains formulations with a theoretical drug release profile of losartan potassium for sustained release. Finally optimized formulation AXG 3 containing carbopol 934 (60 mg), aminated xanthan gum (40 mg), MCC (190 mg) and magnesium stearate (10 mg) showed 100±0.024 % drug release in 12 hr which is acceptable with theoretical drug release of losartan potassium for sustain release dose. Conclusion: Aminated derivatives of xanthan gum and Tamarind gum extend the drug release for 12 hr. Based on in vitro drug release studies of formulations, we concluded that the alteration in the concentration of carbopol 934 with an aminated derivative of xanthan gum in sustain release formulation development was more effective and economical.

Formulation and Evaluation of Metformin Hydrochloride Sustained Release Tablet

Metformin hydrochloride (MET) is an oral hypoglycemic agent which improves glucose tolerance in patients with type 2 diabetes and diminishes basal plasma levels of glucose. The aim of this study was to develop and optimize MET matrix tablets for SR application. The SR matrix tablet of MET was prepared by wet granulation technique using Polyvinyl pyrrolidone K30 and hydroxyl propyl methylcellulose of different viscosity grades (HPMC K4M, HPMC K15M, and HPMC K100M). The influence of varying the polymer ratios was evaluated. The excipients used in this study did not modify physicochemical properties of the drug. MET has relatively short plasma half-life, low absolute bioavailability. The need for the administration 2 to 3 times a day when larger doses are required can decrease patient fulfillment. SR formulation that would maintain plasma level for 8-12 h might be sufficient for daily dosing of MET. SR products are needed for MET to prolong its duration of action and to improve patient compliances. The development of oral sustained release systems has been a challenge to formulation scientists due to their inability to restrain and localize the system at targeted areas of the gastrointestinal tract. From all the formulation trial batches, formulation F3 shows the best results. It has been observed that HPMC K100M alone cannot give satisfactory drug release profile but the blend of HPMC K100M and Polyvinyl pyrrolidone K30 together give the best drug release kinetics. Thus, sustained release matrix tablets of metformin hydrochloride can be expected to reduce the frequency of administration and decrease the dose dependent side effects. Keywords: Metformin hydrochloride, SR matrix tablet, HPMC K100M, Wet granulation technique

Preparation and Evaluation of Sustained Release Tablet of Rifaximin by using Cross linked Sodium Alginate

Rifaximin treats traveler's diarrhea and irritable bowel syndrome by stopping the growth of the bacteria that cause diarrhea. Rifaximin treats hepatic encephalopathy by stopping the growth of bacteria that produce toxins and that may worsen liver disease. The short half life and high frequency of administration of drug makes it a suitable candidate for designing sustained drug delivery system. The aim of the present investigation was to develop a sustained release matrix tablet of Rifaximin using sodium alginate and cross linked sodium alginate and to evaluate the drug release kinetics. In order to achieve the required sustained release profile, the tablets were prepared by a wet granulation method. The formulated tablets were characterized for pre-compression and post-compression parameters and they were in the acceptable limits. The drug release data obtained after an in vitro dissolution study was fitted to various release kinetic models in order to evaluate the release mechanism and kinetics. The criterion for selecting the best fit model was linearity (coefficient of correlation). Drug release mechanism was found to follow a complex mixture of diffusion, swelling and erosion. The dosage form holds the potential to control the release rate of drug and extend the duration of action of a drug.