Sustained-release Tablet Formulation Research Articles

Formulation Strategies for Sustained-Release Tablet Dosage Forms

Sustained-release or extended-release tablet formulations are designed to release the active pharmaceutical ingredient at a slower rate and over an extended period compared to conventional immediate-release dosage forms. This controlled drug delivery approach offers several advantages including improved patient compliance, maintenance of therapeutic drug levels, reduced side effects, and protection of drug molecules from degradation. [1,2] Various formulation approaches have been explored for achieving sustained drug release from tablet matrices. This review discusses key formulation aspects like rate-controlling polymers, factors influencing drug release, manufacturing techniques, and recent advances aided by quality-by-design principles and mathematical modeling for optimizing sustained-release profiles. Regulatory considerations for evaluation and approval are also highlighted

Mucilage from Basella rubra Linn. stems as a release modifier in sustained release tablet formulation

Mucilage from Basella rubra Linn. stems as a release modifier in sustained release tablet formulation

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.

Fabrication and Evaluation of Aceclofenac-loaded Sustained-Release Mucoadhesive Tablet Composed of Cassia fistula Seed Gum-Grafted-Poly (Sodium Acrylate)

Aim: This study was aimed to fabricate gastroretentive mucoadhesive sustained-release tablets of aceclofenac with Cassia fistula seed gum-grafted-poly(sodium acrylate) and evaluate them.&#x0D; Background: Aceclofenac has several gastric related side effects such as increase in acid secretion, gastritis, burning sensation, nausea, vomiting, etc. Sustained-release tablet may reduce these because of slow drug release. But long term use of conventional sustained-release tablets of NSAIDs showed to develop colorectal ulcer. Gastroretentive sustained-release devices may eliminate this problem.&#x0D; Objective: The objective was to synthesis Cassia fistula seed gum-grafted-poly(sodium acrylate) and apply it in the fabrication of novel mucoadhesive sustained-release tablet for aceclofenac delivery in stomach.&#x0D; Method: CFSG-grafted-poly(sodium acrylate) (CFSG-g-PSA) was synthesized by microwave-assisted free-radical initiation method using ceric ammonium nitrate (CAN) as free-radical initiator. The tablets were prepared with the graft-copolymer by wet granulation technique. Compatibility between drug and graft-copolymer was checked by FTIR, DSC and PXRD. Surface topography of the uncoated matrix tablets was studied by SEM. The tablets were evaluated for weight variation, content uniformity, dimension, disintegration test, mucoadhesive and drug-release. accelerated stability study was also done.&#x0D; Results: FTIR, DSC and PXRD studies substantiated the drug-polymer compatibility. The evaluation parameters were within prescribed limit. The study revealed excellent mucoadhesive property over 10 h and sustained-drug-release pattern following zero order kinetic. Similarity factor was found to be 83.4.&#x0D; Conclusion: The study demonstrates a simple approach of functionalization of biopolymer towards development of gastroretentive mucoadhesive sustained-release tablet formulation.

Optimasi Formulasi Tablet Lepas Lambat Ekstrak Seledri (Apium graveolens L.) Menggunakan Polimer Xanthan Gum dan Lubrikan Magnesium Stearat dengan Metode Simplex Lattice Design (SLD)

Antihypertensive drugs undergo first-pass metabolism and therefore have low oral bioavailability. It causes an increase in the frequency of drug use and concentration fluctuations that affect patient comfort. The sustained release tablet formulation was chosen because it can deliver the active substance with good bioavailability. An active antihypertensive substance that can be used is celery extract because it contains flavonoids, so a sustained release tablet formulation was made using xanthan gum and magnesium stearate to produce a constant and controlled release rate. This study aims to knowing the results of celery extract sustained release tablet evaluation using different concentrations of xanthan gum and magnesium stearate, and also obtains the optimal formulation. The manufacture of tablets uses the direct compression method. Powder evaluations include flow property through a funnel, angle of repose, compressibility index, and moisture content. Tablet evaluations include organoleptic, weight uniformity, size uniformity, hardness, friability, disintegration time, and dissolution tests. The evaluation results data were analyzed using Simplex Lattice Design. The powder evaluation result of all formulations meets the requirements of flow property through a funnel, angle of repose, compressibility index, and moisture content. Physical evaluation of the tablets shows all formulations meet the requirement of weight uniformity, hardness, and friability tests. On the size uniformity test, all formulations do not meet the requirement. The disintegration time test results show that F1 does not meet the requirement. Meanwhile, the dissolution test results show that F4 is the best formula because it shows constant and controlled release rate. Based on analyzed using Simplex Lattice Design, the F4 is the most optimal formula with xanthan gum 52 mg and magnesium stearate 3 mg.

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.

3D Printing of Baclofen Gastro-Floating Drug Delivery Systems: A Comparison Study with In vitro and In vivo Evaluation

This study aims to formulate baclofen gastro-floating drug delivery dosage forms in two different approaches using hot melt extrusion and FDM 3D printing and then compare the effectiveness and select the best formula from the two approaches for further characterization. The first approach involved the preparation of baclofen-loaded filament by HME and then FDM 3D printing of floating tablets with low infill percentages. The second approach involved the formulation of sustained-release tablets by HME and 3D printing of a gastro-floating device (GFD) that holds the tablet inside it. Prepared tablets were tested for drug content, in vitro floating behavior, and in vitro dissolution test, and the optimized formula was tested for DSC, FT-IR, and in vivo radiographic study. Filaments prepared by HME with a diameter of less than 1.3 mm were not printed. Variations in filament diameter affect the printing quality of the 3D printed tablets resulting in tablets' weight variation and failure to float sometimes otherwise tablets were successfully printed and remained floating for 12 hr. Formulas prepared by both approaches with the same composition were found to have significant different dissolution profiles due to the rigid structure formed by 3D printing compared to a compressed tablet. Formulation of the HME tablet and 3D printing of GFD were more reliable and were able to float for more than 12 hr. Optimized formula containing Eudragit RS-100 and ethyl cellulose as release modifier polymers, released the drug and remained floating over 12 hr and this was confirmed by x-ray imaging of Albino rabbit. Formulation of sustained-release tablets by HME and inserting them into 3D printed GFD were found to be superior in terms of producing floating dosage forms compared to 3D printed tablets with low infill percentage.

ENHANCED ORAL BIOAVAILABILITY OF NANONIZED PROGESTERONE IN HEALTHY AND PREGNANT RABBITS (NPROBIO STUDY)

The aim of this study is to evaluate and compare the oral bioavailability of nanonized progesterone (nano-PG) and micronized progesterone (micro-PG) sustained release tablet formulation in healthy and pregnant rabbits. High pressure compressed gas technology reduces the particle size from 1.72 ± 2.5 µm (micro-PG) to 800 ± 35 nm (nano-PG). DSC and XRD showed that both micro-PG and nano-PG were crystalline and exist as form I. Higher melting enthalpy of nano-PG indicated improved drug stability whereas XRD showed slight reduction in degree of crystallinity following nanonization. Nano-PG demonstrated 2-fold higher solubility in SDS aqueous solution and signicantly higher permeability (p &lt; 0.05) across porcine intestine compared to micro-PG. The pharmacokinetics of nano-PG and micro-PG was conducted in healthy and pregnant rabbits. The Cmax of nano-PG was higher in healthy and pregnant rabbits however the difference was signicant in healthy rabbits only. The nano-PG demonstrated 30% and 18% higher bioavailability compared to micro-PG in healthy and pregnant rabbits, respectively. In conclusion, nanonization improves solubility, dissolution and bioavailability of PG in rabbits without affecting solid state characters

Nanonized progesterone formulation for improved oral bioavailability in healthy and pregnant rabbits

The aim of this study is to evaluate and compare the oral bioavailability of nanonized progesterone (nano-PG) and micronized progesterone (micro-PG) sustained release tablet formulation in healthy and pregnant rabbits. High pressure compressed gas technology reduces the particle size from 1.72 ± 2.5 μm (micro-PG) to 800 ± 35 nm (nano-PG). DSC and XRD showed that both micro-PG and nano-PG were crystalline and exist as form I. Higher melting enthalpy of nano-PG indicated improved drug stability whereas XRD showed slight reduction in degree of crystallanity following nanonization. Nano-PG demonstrated 2-fold higher solubility in SDS aqueous solution and significantly higher permeability (p &lt; 0.05) across porcine intestine compared to micro-PG. The pharmacokinetics of nano-PG and micro-PG was conducted in healthy and pregnant rabbits. The Cmax of nano-PG was higher in healthy and pregnant rabbits however the difference was significant in healthy rabbits only. The nano-PG demonstrated 30% and 18% higher bioavailability compared to micro-PG in healthy and pregnant rabbits, respectively. In conclusion, nanonization improves solubility, dissolution and bioavailability of PG in rabbits without affecting solid state characters.

Pharmacokinetic and Bioequivalent Study of Potassium Chloride Sustained-Release Tablet Under Different Dietary Conditions in Healthy Chinese Subjects.

Potassium (K+ ) is an endogenous substance that is an essential dietary component. However, the interaction between dietary arrangements and specific effects of dietary K+ intake in bioequivalence studies remains unclear. To investigate the influence of dietary arrangement on the bioequivalence of potassium chloride (KCl) sustained-release tablets in healthy Chinese volunteers, the pharmacokinetics of KCl were compared in two open-label, single-center, randomized, two-period crossover studies with different dietary conditions. All volunteers received an oral dose of 6g of KCl sustained-release tablets under fasting conditions, with different dietary arrangements. Urine samples were collected on baseline days and 48hours after tablet consumption. Inductively coupled plasma-optical emission spectrometry was used to measure the concentration of K+ in the urine samples. Pharmacokinetic parameters were analyzed using Phoenix WinNonlin software in a noncompartmental model. In either clinical trial, no significant differences were observed in the maximal rate of urinary excretion and cumulative urinary excretion from 0 to 24 hours of K+ between the reference and test drugs. The bioequivalence studies of both KCl sustained-release tablet formulations were successfully conducted under different dietary conditions.

Formulation and evaluation of sustained release tablets of propranolol hydrochloride

The main objective of sustained release drug delivery system is to provide a steady state blood plasma level concentration which is non-toxic and therapeutically active for a longer period of time. Owing its increased patient compliance and prolonged release of action in delivering drugs several benefits can be contemplated in delivering of sustained release dosage form[1]. Among various route of drug delivery Sustained release drug delivery is most widely preferred as it’s less frequency of dosing and controls the release of drugs. Natural polymers are biodegradable and nontoxic in nature with reduced side effects. It is also eco-friendly and safe to be administered as compared to synthetic polymers. The current work was based on preparation of sustained release tablets of Propranolol Hydrochloride using natural polymers like Gum Acacia, Hibiscus Rosasinesis and Microcrystalline cellulose. Presently much attention is being paid for formulation of sustained release tablets that contains matrix system. Direct compression method was used for formulation of sustained release tablets of Propranolol Hydrochloride. The prepared tablets were evaluated for different pre-formulation studies and in vitro dissolution studies were performed using USP-III dissolution apparatus. Dissolution studies of different formulations were evaluated for 24 hours at 370C.

Assessing compatibility of excipients selected for a sustained release formulation of bilberry leaf extract

The study is aimed to assess the compatibility of bilberry leaf powder extract (BLPE) with six excipients selected for sustained-release (SR) tablet formulation. The BLPE was obtained with the addition of L-arginine and Myo-inositol as the carriers. Thermogravimetric (TG-DTG) analysis and Fourier-transform infrared spectroscopy (FTIR), supported by Pearson correlation analysis, were applied to detect possible interactions in the binary mixtures (1:1) of the BLPE with each excipient. The TG-DTG showed some deviations in the thermal behavior of the BLPE / excipient mixtures. However, only the thermal behavior of magnesium stearate in the mixture significantly differed from individual samples, which suggested chemical interaction for this excipient. The FTIR analysis confirmed that the BLPE is compatible with Eudragit L100, Methocel K4M, Methocel K100LV, Avicel PH-101, and Plasdone S-630. Whereas it undergoes solid-state chemical interaction in the binary mixture with magnesium stearate. According to the FTIR-spectra, it is suggested that this interaction results in the formation of stearic acid and alkalization of the medium. These findings evidence for the possibility of using TG-DTG analysis as an independent thermal technique for compatibility studies and also confirm the earlier reported interaction of basic lubricants, e.g., stearic salts, with active ingredients containing amino groups.

Design and Characterization of Sustained Release Tablet Formulation Containing Metformin Hydrochloride and Simvastatin

The aim of the present work was to develop pharmaceutical combinational dosage form for simultaneous treatment of patients with type 2 diabetes with at high-risk of coronary disease associated co-morbidities. Metformin, an antidiabetic drug is used to treat the diabetic patient and combined with Simvastatin which is HMG-CoA reductase inihibitor drug to treat the high-risk coronary disease simultaneously. In this formulation, three batches were prepared by the direct compression method. Preformulation parameters such as identification, solubility, melting point, compatibility studies, Pre-compression parameters such as bulk density, tapped density, angle of repose, Hausner ratio, compressibility index, and Post-compression parameters like weight uniformity, hardness, drug content, thickness, in-vitrodrug release. In-vitrodrug release of all formulations, B1, B2, and B3 was carried out in 0.1N HCl for 2hrs and 10 hrs in phosphate buffer (pH 6.8) dissolution media. Among all the formulations, B3 was an optimized batch. B3 formulations showed drug release of 85% for Metformin Hydrochloride and 93% for Simvastatin over a period of 12hrs.©2022iGlobal Research and PublishingFoundation. All rights reserved.

Formulation and Development of Metoprolol Succinate Sustained Release Matrix tablet using Remusatia vivipara tubers mucilage

The purpose of this research was to formulate and evaluate sustained release tablet by using novel polymer Remusatia vivipara tubers mucilage. Currently natural gums and mucilages are being used extensively comparable to synthetic drug release modifiers. Natural plant materials possess various advantages. These are very cheap, biocompatible, biodegradable and free from side effects. In present research Metoprolol succinate matrix tablets were prepared by using Remusatia vivipara tubers mucilage. For the formulation of sustained release matrix tablets, direct compression method was used. The formulated matrix tablets were then evaluated for thickness, diameter, hardness, weight variation, friability, drug content, swelling index, in-vitro drug release and stability studies. The formulated sustained release tablet passed all tests required. The dissolution profile of prepared tablets showed sustained release of drug up to 11 hours compared to the reference tablet formulation PROLOMET XI 100. Drug release data were then fitted in to release kinetic models such as zero order kinetic, first order kinetic, Higuchi model and Korsmeyer-Peppas model to study the release pattern of drug from each formulation. The prepared sustained release tablet formulation was compared with marketed formulation (reference formulation) for drug release study and factor f1 (difference factor) and f2 (similarity factor) were determined. From this study it can be concluded that as the concentration of Remusatia vivipara mucilage increases, there is decrease in the rate of drug release from the formulation. The best formulation was found to be F3 which consists of 20% Remusatia vivipara mucilage but did not give comparable drug release profile to the reference formulation with factor f1 69.4 % and f2 34.8%. But it can be said that Remusatia vivipara gum mucilage can be used in tablet formulation to give sustained release effect up to 10 hours or in combination with other natural gum mucilage it may enhance the release retardant effect of drug up to or more than 20 hrs. The release kinetic study showed that the prepared sustained release tablet formulation shows anomalous (non-fickian) diffusion pattern and follows both diffusion controlled and swelling controlled mechanisms for drug release.

Application of optimization tools for preparation of nebivolol liquid solid composite compressed tablet

The purpose of this study is to make Nebivolol more efficient by converting it into a liquid solid composite compressed tablet. Blending cum sonication process was used to create the liquid solid composite. By altering the independent variables such as vehicle, carrier, and superdisintegrants, nearly 12 compositions were created in a 23 factorial design with four centre points. The influence on response, such as disintegration time in seconds and wetting time in seconds, was then determined. In addition, the liquid solid composite was compacted into a tablet and its percent invitro drug release was assessed. Based on disintegration time and wetting time, the optimal solid liquid compacts sustained release tablet formulation was identified to be LSC6 , which may be ideal candidates for boosting the solubility and dissolution rate of less soluble medications like Nebivolol.

Develop and evaluate novel drug delivery system of valsartan for treatment of Hypertension: A review

The sustained release tablets were formulated by using the combination of various release retardant polymers/excipient. The polymers used were hydroxypropyl methylcellulose, Micro Crystalline Cellulose and Sodium starch glycolate. The present investigation involves formulation and evaluation of sustained release tablets of Valsartan with a view to prolong the drug release in the gastrointestinal tract and consequently into the plasma. It showed good linearity and reproducibility which also indicated the analytical method used in the present study to be suitable for the estimation of the drug candidates in different dissolution media. Evaluation parameters such as thickness and diameter, weight variation and drug content uniformity test. The observation for all above evaluation parameters indicate that the values are within the IP specified limits. Thus, on the basis of our research findings it could be concluded that the performance of the developed sustained release tablets was found to be promising for the treatment of hypertension.

DEVELOPMENT OF SUSTAINED RELEASE ALOGLIPTIN TABLETS USING A MULTIPARTICULATES SYSTEM MADE OF BENTONITE

Objective: This study was designed to evaluate the use of bentonite in the formulation of sustained-release tablets containing alogliptin benzoate after granulation.&#x0D; Methods: Bentonite was used for preparing tablets after granulation. The prepared tablets were tested for their pharmacopeial requirements. Further, a high-performance liquid chromatography (HPLC) method was developed to assess the release pattern of alogliptin from the tablets. Besides, differential scanning calorimetry (DSC), fourier transform infrared spectroscopy (FTIR), and powder X-ray diffraction (XRD) were used for evaluating the compatibility the drugs and bentonite. Finally, the release from the tablets was tested using the paddle apparatus.&#x0D; Results: The FTIR and DSC did not show any interaction between the drug and the excipient in contrast to the powder-XRD pattern, which showed a shift for montmorillonite crystal peak. This shift was interpreted by increasing in the spacing of the crystalline structure of montmorillonite. However, the results of pharmacopeial tests showed that the prepared tablets comply with the compendial requirements, In addition, the release profiles of these tablets with aid of hydroxypropyl methylcellulose (HPMC) as a binder revealed a sustained release of alogliptin. Furthermore, the fitting of release data showed that the release from these tablets followed Fickian diffusion that alogliptin released by diffusion from bentonite gel matrix.&#x0D; Conclusion: Bentonite was successfully used for producing sustained-release tablets of alogliptin. However, maintaining the crystal structure of montmorillonite was essential for building the gel structure of bentonite and releasing the drug in a controlled manner.

Evaluation of the matrix-forming ability of Chrysophyllum albidum Linn fruit gum in sustained-release tablet formulations

Background: Plant gums are extensively being exploited as pharmaceutical excipients due to the ease of availability, biodegradability, and reduced costs. Aim: This study investigated the application of the fruit gum of Crysophyllum albidum (CFG) as a matrix former in the formulation of chlorpheniramine maleate and theophylline hydrochloride tablets. Materials and Methods: The gum was extracted using acetone and evaluated for flow, swelling, and hydration capacity. Effects of temperature on CFG and drug compatibility were evaluated using differential scanning calorimetry (DSC). Granules containing CFG at 10, 20, and 30% w/w were prepared using the wet granulation method and evaluated for flow properties. Compressed tablets were evaluated for uniformity of weight, hardness, friability, and drug content. In vitro drug release studies were carried out in simulated gastric (pH 1.2) and simulated intestinal (pH 6.8) fluids. Pearson’s similarity correlations were used to analyze results. Results: CFG had a swelling capacity of 22% and hydration capacity of 1.44 with an angle of repose of 30o and Carr’s index of 7.6 signifying good flow. DSC thermogram returned an endothermic glass transition peak at 72.1oC with no appreciable shifts in the peak when CFG was incorporated into the drug. Tablet hardness and friability were concentration dependent with values of 6.5–8.5kg F and 0.04–0.4%, respectively; drug content was within official specifications. Formulations containing 30%w/w CFG sustained drug release for over 12 h and showed better ability to control drug release than HPMC at same concentration. Conclusion: This study shows the propensity of CFG to be used in the formulation of sustained-release tablet formulations.

Formulation, Development and Evaluation of Bisoprolol Sustained Release Tablets

Bisoprolol is a type of antihypertensive drug (β-blocker). It is a poorly water-soluble and highly permeable drug that belongs to class II biopharmaceutical classification. This investigation represents the formulation development of bisoprolol to sustain the drug release. Different types of polymers like hypromellose, xanthan gum, avicel, poly ethylene glycol (PEG) were used in this study. Three different formulations were developed by using different excipients at various ratios. The granules were evaluated for bulk density, tapped density, flow property whereas tablets were evaluated for thickness, hardness, weight variation, compressibility index, uniformity of content, disintegration time, and drug release profile. The concentration of the diffused drug was measured using a UV-visible spectrophotometer at λmax= 225 nm. Granules showed good flow ability and all the formulations passed the quality. Among all the formulations, F-2 and F-3 showed better efficiency. PEG along with hypermellose, and guar gum showed a good combination for sustaining the drug release

Modulation of Drug Release from Natural Polymer Matrices by Response Surface Methodology: in vitro and in vivo Evaluation.

PurposeThe present work aimed at challenging the efficacy of natural gums, karaya and locust bean gum, as matrix-forming polymers for the formulation of sustained-release tablets of diltiazem, a model drug.MethodsCentral design composite was adopted for the formulation and optimization of tablet formulations. The two gums have been selected as independent variables. The dependent factors chosen were the amount of drug released in 1st hour (Y1), amount of drug released after 12 h (Y2), diffusion exponent (Y3), and time for half of the total drug released (T50%) (Y4). Wet granulation approach was used for the formulation of tablets. FT-IR, DSC, in vitro dissolution, swelling-erosion investigations, SEM, and stability studies were carried out.Results and DiscussionIt was evident that the release pattern from the prepared formulations was significantly influenced by the quantity of gum(s) in the tablet. FT-IR and DSC results confirm drug–polymer compatibility. Polynomial equations were used for the prediction of quantitative impact of independent factors at different levels on response variables. After ANOVA analysis, the significant factors were considered for constrained optimization to get the optimized formula. The optimized formula generated by the response surface methodology was evaluated both for in vitro and in vivo properties. The optimized formula and a sustained-release marketed product were subjected to in vivo studies in rabbits and the results of the t-test demonstrated insignificant variation in pharmacokinetic parameters among the two formulations, confirming that the prepared tablet showed sustained-release profile.ConclusionThe results indicated that karaya and locust bean gum can be effectively used to formulate sustained-release tablets.