Formulation Of Matrix Tablets Research Articles

Formulation and In Vivo Evaluation of Trilayer Matrix Tablets of Rosuvastatin Solid Dispersions by Geomatrix Technology

The current research is aimed at enhancing the aqueous solubility and sustains the drug release of rosuvastatin BCS Class II drug. 15 solid dispersion (SD) formulations of rosuvastatin prepared by solvent evaporation technique and evaluated. In vitro drug dissolution study indicated higher drug dissolution rate for SD13 of 99.74±5.39 % within 60 min. Eight formulations of rosuvastatin trilayer matrix tablets (AF10-HF10) were prepared by incorporating optimized SD13 by direct compression method. These trilayer formulations characterized for flow properties and physicochemical parameters. The maximum drug release was exhibited by trilayer matrix formulation (HF10) of 99.48±5.40 % over a period of 24 h. The release profile of the optimized formulation (HF10) was described by the zero order and best fitted to Higuchi and Korsmeyer-Peppa’s model. The results demonstrated the sustainability of rosuvastatin trilayer tablets with enhanced release time and linearity upto 24 h. From in vivo bioavailability studies Cmax of the rosuvastatin optimized ER tablets and marketed product was found to be 28.46±0.07 ng/mL and 30.94±0.75 ng/mL respectively. Tmax of both rosuvastatin optimized ER tablets formulation and rosuvastatin marketed product was 5±0.06 and 4±0.03 h, respectively. AUC0-∞ infinity for optimised formulation was higher (395.54±1.37 ng.h/ml) than the rosuvastatin marketed product formulation 212.54±0.42 ng.h/ml. Statistically, AUC0-t of the optimized ER tablets formulation was significantly higher (p<0.05) as compared to rosuvastatin marketed product formulation. In vivo pharmacokinetic studies in rabbits confirmed the prolonged release by showing increase in bioavailability for Rosuvastatin from optimized ER tablets than marketed formulation.

Formulation and Evaluation of Sustained Release Matrix Tablets of Aceclofenac

This study aimed to improve the dissolution rate of aceclofenac and release the drug in a controlled manner over a period of 24 hours. Matrix tablets were prepared by direct compression method, using hydrophilic polymers (HPMC/guar gum). Matrix tablets were prepared by wet granulation method using different hydrophilic polymers (HPMC/guar gum). Tablets were evaluated for in vitro drug release profile in phosphate buffer with pH 6.8 (without enzymes). The thickness and hardness of prepared tablets were 3.23 ± 0.035 to 3.28 ± 0.008 mm and 3.26 ± 0.115 to 3.60 ± 0.200 kg/cm2, respectively. The friability was within the acceptable limits of pharmacopoeial specifications (0.31 to 0.71%), which indicates the good mechanical strength of the tablets. Drug release was retarded with an increase in polymer concentration due to the gelling property of polymers. 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. The results clearly indicate that guar gum could be a potential hydrophilic carrier in developing oral controlled drug delivery systems. Based on the study results, formulations F8 was selected as the best formulation.

Formulation Development and Characterization of Darunavir and Ritonavir Immediate Release Tablets using Quality by Design approach

Darunavir is a nonpeptidic inhibitor of protease and is primarily metabolized by cytochrome P450 3A (CYP3A) isoenzymes. It is usually Coad ministered with low-dose ritonavir (Darunavir/r). Ritonavir is an inhibitor of CYP3A isoenzymes and pharmacologically enhances Darunavir which leads to increased plasma concentrations of darunavir and allows for daily lower dose. Here, we have developed combination IR formulation of Darunavir and Ritonavir and evaluated. In vitro drug release of all formulations was carried out in dissolution medium 900ml of pH 3.0 0.05 M Sodium Phosphate Buffer + 2% Tween 20 for 75 Min USP II apparatus (paddle). The results shown that, all the formulations of matrix tablets shown the good release of drug from trialed formulations however all formulations were not releasing the drug in enough amount. In matrix tablets F8, the release of drug shows 99%. So, the formulation F8 has been considered as suitable for the immediate release of Darunavir and Ritonavir. Tablets were also evaluated for physic chemical properties, dissolution studies and though Quality by Design (QbD) method.

Cross linked plantain starch-urea as a polymer in matrix tablets of ambroxol hydrochloride

Plantain (Musa paradisiaca) starch, prepared as crosslinked starch-urea (CSU), was utilized in the formulation of matrix tablets of ambroxol hydrochloride. CSU was synthesized by gelatinization of plantain starch in urea, crosslinked with calcium chloride. Native starch and CSU were characterized using scanning electron microscopy (SEM), X-ray diffraction (XRD), chemical and material properties. Ambroxol hydrochloride tablets were prepared with CSU, 1:1 blend of CSU and Hydroxyl propyl methylcellulose (HPMC K15M) and HPMC K15M alone at 20, 30 and 40%w/w. The 32 factorial design was used to optimize tablets using polymer type (X1) and polymer concentration (X2) as independent variables, crushing strength-friability ratio (CSFR) and time for 80% drug release (t80) as responses. The SEM revealed changes in the ovoid granules of native starch to larger, irregular granules of CSU. The XRD spectra revealed a more crystalline CSU with higher swelling and better flow. Polymer type had more influence on CSFR and t80. The optimized batch containing CSU at 40 %w/w exhibited the highest values of CSFR and drug release. Experimental responses of the optimised batch had close proximity with the predicted value. Cross-linked plantain starch-urea polymer was found suitable as a polymer in matrix tablets of ambroxol hydrochloride.

Formulation and Development of Metoprolol Succinate Sustained-Release Matrix Tablet Using Eulophia Herbacea Tuber Mucilage as A Novel Polymer

Formulation and Development of Metoprolol Succinate Sustained-Release Matrix Tablet Using Eulophia Herbacea Tuber Mucilage as A Novel Polymer

Pectin from Okra (Abelmoschus esculentus L.) Has Potential as a Drug Release Modifier in Matrix Tablets

Natural polymers have become attractive to pharmaceutical researchers and manufacturers as excipients because of the advantages they possess relative to their semisynthetic and synthetic counterparts. Although pectin from some natural sources has been investigated for use in the pharmaceutical industry as excipients, pectin from okra, which is readily available and used as food in many parts of the world, has not been extensively investigated as a potential control-releasing agent in tablets. This study thus seeks to determine the drug release modifying properties of okra pectin from 6 different genotypes of okra cultivated and available in Ghana. Pectin was extracted from different genotypes of okra, physicochemical properties were characterized, and control release matrix tablets of metformin (F1–F6) were formulated using the wet granulation method with the okra pectin as the drug release modifier, respectively. The drug content, in vitro drug release, and mathematical kinetic modeling of drug release from the matrix tablets were studied. Drug release profiles of formulated matrix tablets were compared to an existing (innovator) brand of metformin sustained-release tablet on the market using the similarity and difference factors, respectively. The extracted pectin had percentage yields ranging from 6 to 20% w/w with swelling indexes and water-holding capacities between 300–500% and 9-10 mL/g, respectively, and pH within 6.20–6.90. All the formulated batches passed the drug content test (90–105%) and produced the optimal release of metformin (>80%) after 24 hours. Different batches of formulated tablets exhibited different mechanisms of drug release with batches F1, F2, F5, and F6 being similar (ƒ2 values being >50 and ƒ1 values <15) to the innovator brand. Pectin from the 6 different genotypes of okra studied has the potential for use as drug release modifiers in pharmaceutical manufacturing of control release matrix tablets and production of more affordable medicines.

Formulation and evaluation of miglitol matrix tablets by using Hibiscus rosa sinensis leaves mucilage

Formulation and evaluation of miglitol matrix tablets by using Hibiscus rosa sinensis leaves mucilage

Formulation and In-Vitro Evaluation of Sustained Release Matrix Tablets of Domperidone

INTRODUCTION&#x0D; Domperidone is a unique compound with gastro kinetic and antiemetic effects. It is used in the management of disorder by impaired motility like gastroesophageal reflux (in some instances), gastroparesis, dyspepsia, heartburn, epigastric pain, nausea, vomiting, and colonic inertia. The sustained release system is a widely accepted approach for slow drug release over an extended period to address the challenges of conventional oral delivery, including dosing frequency, drug safety, and efficacy. The study aims to formulate a domperidone sustained release tablet and compare the dissolution rate with the marketed formulations.&#x0D; MATERIAL AND METHODS&#x0D; Sustained release matrix tablets of domperidone were prepared by wet granulation method using different polymers such as HPMC K4M, ethyl cellulose, Gum acacia. Pre-compression studies like angle of repose, bulk density, tapped density, Carr's index, and Hausner’s ratio, and post-compression studies like weight variation, thickness, hardness, friability, drug content, and in-vitro drug release were evaluated.&#x0D; &#x0D; RESULTS&#x0D; The release profile of domperidone sustained-release tablets was studied spectrophotometrically. The in-vitro dissolution study suggests the minimum %-cumulative drug release with 98.33% in F5. The %-cumulative drug release was maximum in F3 with 99.69%. The in-vitro drug release of all the formulations was non-significant compared to the marketed formulation (p&lt;0.05), exhibiting the sustained-release property by all the formulations.&#x0D; CONCLUSION&#x0D; The pre-compression study concludes the better flow property of the granules of different formulations. The sustained release domperidone tablets were prepared successfully by the wet granulation method. The post-compression parameters of different formulations were within the acceptable range.

DEVELOPMENT OF FLOATING GASTRORETENTIVE DRUG DELIVERY SYSTEM BASED ON A NOVEL EXCIPIENT FOR METFORMIN HYDROCHLORIDE USING MIXTURE DESIGN

Objective: The present study aimed to develop a new SR metformin hydrochloride (MH) gastroretentive formulation with novel excipient (NE), which has better floatation and can be prepared with more simple pharmaceutical techniques for the treatment of diabetes Mellitus.&#x0D; Methods: A gastro-retentive floating matrix tablet (GFT) formulation of MH was prepared using various concentrations of PEO (Polyox WSR-303) and hydroxypropyl methylcellulose K100M (HPMC K100 M) and Floating agent (novel excipient) to achieve desirable TFT, FLT and drug release. The wet granulation method was selected using isopropyl alcohol as a binder for the preparation of tablets. D-optimal non-simplex mixture design was used for the selection of suitable polymer concentrations and floating agents. Release kinetics was used to determine the mechanism of drug release.&#x0D; Results: It was observed that GFT with optimum quantities of PEO, HPMC K100M, and the floating agent showed 100 % of drug release in 24h with FT up to 24h and minimum FLT of less than 2 min. Formulation with an in vitro release profile slower to the marketed sample was prepared.&#x0D; Conclusion: A sustained-release (GFT) of MH tablets using PEO-, HPMC K100M, and an effervescent system was successfully prepared. AGFT formulation with an in vitro release profile slower to the marketed sample that releases MH for 24h may suitable for once-daily dosing can be prepared.

A Study on The Formulation of Plant Matrix Tablets From Coarse Botanical Materials Using Cinnamon Bark and Areca Nut as The Model Botanical Materials

Background: There is much interest in formulating botanical materials into tablets due to the compactness and ease of administration. However, tableting of coarse milled botanical materials poses a challenge due to poor tableting properties. Objective: To evaluate the feasibility of wet granulation to produce tablets from coarse milled botanical materials and to assess the effect of formulation on properties of the tablets. Materials and Methods: Cinnamon bark and areca nut were milled to obtain 1–2 mm particle size, which was subsequently used in wet granulation using maltodextrin solution as a granulating liquid. Two diluents were tried; microcrystalline cellulose (MCC) or mannitol at a different ratio to the botanical materials. Tablets were then produced from the granules and evaluated for tensile strength and surface roughness. Results: Tablets formulated with MCC had higher tensile strength than tablets formulated with mannitol. Additionally, granules prepared using mannitol were more friable than those with MCC. The effect of diluent to botanical material ratio was more prominently observed on tablet surface roughness. Tablets containing a higher ratio of botanical material had a rougher surface, which could have implications on the mouth-feel of the tablets. Conclusion: Wet granulation could be a viable pre-processing method to produce tablets from coarse milled botanical materials.

Preparation and Evaluation of Ternary Polymeric Blends for Controlled Release Matrices Containing Weakly Basic Model Drug.

The objective of this study was to evaluate the suitability of a ternary mixture of smart polymers comprised of Eudragit®E100, Eudragit®L100, and sodium alginate to serve as a carrier for sustained drug release for weakly basic drugs. The model drug chosen in this part of the study is Metronidazole. Matrix tablet formulations were prepared by either direct compression or by wet granulation. Dissolution studies were conducted using USP XXΠ rotating paddle apparatus in three different consecutive stages (pH 1.2, 4.8, and 6.8). Tablets made of low to intermediate proportions of sodium alginate and approximately equal proportions of Eudragit®E100 and Eudragit®L100 were found to have a significant modification of drug release rates. Thus, indicating a potential for controlling the drug release for 12 hours depending on polymers ratios in the formulation. The ratio of sodium alginate to total Eudragit® polymers and the ratio of Eudragit®E100 to Eudragit®L100 within the ternary polymeric composition were found critical in determining the controlled release performance. Results of swelling studies were in agreement with the dissolution behaviors of the tablets. The findings suggest the significance of the ternary polymeric compositions in controlling the release of a weakly basic drug, Metronidazole.

Design and Evaluation of Lovastatin Solid Dispersions Incorporated Trilayer Matrix Tablets

The current work is aimed to design, prepare and evaluate the trilayer matrix tablets incorporated with lovastatin solid dispersion (SD) for extend drug release. The lovastatin SD prepared by using solvent evaporation technique with varying amounts of polymers (GMS II, Soluplus, Kolliphor ELP, PEG 2000 and Urea) for enhancing the drug solubility. All the formulations examined for physicochemical parameters are within the permissible limits. The optimized SD formulation was incorporated into trilayer matrix tablets which were prepared using different polymers (HPMC 15M &amp; K100M, Chitosan, xanthan gum) by direct compression method for sustaining the drug release. The drug dissolution of optimized lovastatin SD formulation SD15 (drug, soluplus and SLN) was 99.88±5.32% within 60 min which is higher than pure drug 47.33±2.25% and other formulations. The FT-IR, XRD and SEM data assure the compatibility of drug and excipients and amorphous nature of lovastatin. The solid dispersions were further incorporated in to trilayer matrix tablets with active layer and barrier layers. Eight formulations of lovastatin trilayer matrix tablets (AF9-HF9) designed and checked for pre compression parameters. Formulation GF9 demonstrated highest drug release of 99.41±5.28% for 24 hours sustainably over an extended period of time and excellent flow properties. The release order kinetics data indicate the zero order release with highest R2 of 0.9957 for GF9, superior than market extended release formulation (R2=0.9934). All the formulations showed best fit to Higuchi model and Korsmeyer-Peppa’s model indicating diffusion and non-Fickian diffusion process of drug release. GF90 was found to be stable for 180 days at accelerated conditions. Hence the solubility, dissolution rate of lovastatin was enhanced by SD technique further incorporated in to trilayer matrix tablets for sustainable extended drug release upto 24 h.

Formulation development and characterization of cellulose/ polyacrylic acid – based polymers on the release of celecoxib from extended release tablets

The study was aimed to formulate an extended release matrix tablets of celecoxib and to investigate the influence of different types and concentration of polymers on release of drug. Six formulations namely F1 – F6 were manually designed using different proportions of polymers. The matrix tablets formulations (F1 – F5) were composed of using different polymers such as, hydroxypropyl methylcellulose (HPMC-K4M), carboxymethyl cellulose (CMC), ethylcellulose (EC-10 cps) and Carbopol-940, whereas plain tablets formulation (F6) without polymer contained microcrystalline cellulose (MCC), lactose monohydrate, sodium lauryl sulfate (SLS) and polyvinylpyrrolidone (PVP-K30). The MCC, SLS and PVP-K30 were used in a fixed quantity in all formulations except F6 i.e. 20.7%, 6.7%, and 2%, respectively. Multiple point dissolution was performed in phosphate buffer of pH 7.4. Dissolution profiles indicated that formulations F2 and F3 extended the drug release up to the desired time period of 12 h. DD Solver (an add-in software for MS Excel) was used to analyze the dissolution profile data for drug release kinetics such as first order, Zero-order, Higuchi and Korsmeyer–Peppas models. However, formulation (F3) containing HPMC – K4M as a matrix former showed concentration-independent drug release as highest linearity was observed when zero-order model was applied (R2 = 0.933). Release mechanism of formulations F3 was super case-II transport. Fourier transform infrared spectroscopy (FTIR) was used to assess the drug polymers compatibility and no drug– excipients interaction was found. The present study accomplished that ethylcellulose and HPMC can be used successfully to develop an extended release matrix tablet formulation.

Formulation of Sustained Release Hydrophilic Matrix Tablets of Tolcapone with the Application of Sedem Diagram: Influence of Tolcapone's Particle Size on Sustained Release.

Hydrophilic matrix tablets are a type of sustained release dosage form characterized by distributing a drug in a matrix that is usually polymeric. Tolcapone is a drug that inhibits the enzyme catechol-O-methyl transferase. In recent years, it has been shown that tolcapone is a potent inhibitor of the amyloid aggregation process of the transthyretin protein, and acts by stabilizing the structure of the protein, reducing the progression of familial amyloid polyneuropathy. The main objective of this study was to obtain a sustained release tablet of tolcapone for oral administration with a preferred dosage regimen of 1 administration every 12 or 24 h and manufactured, preferably, by direct compression. The SeDeM Diagram method has been used for the formulation development of hydrophilic matrix tablets. Given the characteristics of tolcapone, the excipient selected for the formation of the polymeric matrix was a high viscosity hydroxypropylmethylcellulose (Methocel® K100M CR). A decrease in the particle size of tolcapone resulted in a slower dissolution release of the formulation when the concentration of the polymer Methocel® K100M CR was below 29%. These surprising and novel results have given rise to patent number WO/2018/019997.

Formulate and evaluate once daily sustained release tablet of highly soluble drug of metformin HCL

The aim of the present study was to design an oral sustained release matrix tablet of highly water soluble biguanide anti diabetic drug. The matrix tablets are prepared by melt granulation method using HPMC K 200M as hydrophilic drug release retarding polymer, and stearic acid as melt able binder as well as hydrophobic carrier. The drug and excipients compatibility was studied by FT – IR. The formulated matrix tablets were characterized for physical parameters and in vitro dissolution profile. FT – IR spectra revealed the absence of drug excipients interaction. The physical parameters of the tablets were found within the limits. The drug release kinetics demonstrated that by increasing the concentration of hydrophilic polymer and hydrophobic carrier the drug release rate was retarded proportionally. Kinetic modelling of in vitro release profile revealing that the drug release from the matrix tablets following first order kinetics, and the drug release mechanism of optimized (F7) formula following non fickian transport mechanism. Accelerated stability studies were performed according to ICH guide lines. Temperature 40±20 c and relative humidity 75±5% RH to study physical and chemical changes of formulation. No physical or chemical changes were observed after t accelerated stability studies.

Formulation and evaluation of matrix tablets of Eperisone hydrochloride

The aim of the present research is to develop and optimize Eperisone Hydrochloride extended release matrix tablets. Eperisone Hydrochloride is an antispasmodic drug mainly used to relieve pains it acts by relaxing the skeletal and smooth vascular muscles by blocking spinal reflexes drug which has oral bioavailability of 70% due to hepatic metabolism. Sustained release matrix tablets of Eperisone Hydrochloride were prepared through wet granulation technique by using HPMC K4M and EC as polymers, PVPK30 as binder, Magnesium stearate as lubricant and Talc as glidant. The granules of different formulations were determined for pre compression parameters. The prepared granules along with the excipients were then compressed. The formulated tablets were evaluated for physical characteristics viz. Hardness, Thickness, % Weight variation, Friability and the drug content. Furthermore the tablets evaluated for the in vitro release studies. Out of all the 8 formulations F7 showed desired characteristics in the physical parameters and in vitro drug release of 85.48% in 12hrs.The F7 dissolution data was best fitted to the Zero order model. The prepared Eperisone Hydrochloride matrix tablets found to be having a potential extended drug release.

Development and Characterization of Controlled Release Tablets of Candesartan Cilexetil/ β‑Cyclodextrin Inclusion Complex

Objective: Matrix tablet approach is one of the delivery systems intended for poorly water-soluble drugs, like candesartan cilexetil (CC). CC is a class II drug used for the treatment of hypertension. Methods: Matrix tablets from (F1x to F18z) were prepared in the presence of β‑cyclodextrin. Matrix tablet formulation ensures control release of the drug and higher dissolution by β‑cyclodextrin. Fourier transform infrared spectroscopy (FTIR), and differential scanning calorimetry (DSC) were used to study compatibility. Results: The angle of repose determination showed good flow for most of the formulas, besides having good compressibility. Weight variation test for all formulas showed accepted value. Drug content measurement showed accepted values. Friability and hardness of tablets were within the allowed values. Higher tablet swelling was obtained for the formulas containing hydroxypropyl methylcellulose (HPMC) K100M (F3x and F15z), in which the ratio of the polymer was 1:1 and 1:3, respectively. In vitro release showed that F1x to F13z were studied depends on the type and amount of polymer, i.e., 1:1, 1:2, and 1:3, respectively. F1x release after 8 hours was 95%, which contains 1:1 polymer ratio in comparison to F3x, which showed 85% after 8 hours, which includes 1:3 (drug: HPMC K100). Kinetic studies showed a zero-order model. Conclusion: The use of β‑cyclodextrin modifies the release profile of the drug, and some control the more sustained-release formulas. The lower the time of the release but in a range that a sustained release of the drug was observed in comparison with the formulas prepared without β‑cyclodextrin.

A PROMISING APPROACH TO PROVIDE APPROPRIATE COLON TARGET DRUG DELIVERY SYSTEMS OF METRONIDAZOLE: DEVELOPMENT AND EVALUATION

The aim of present study was to develop colon targeted system for Metronidazole using guar gum and xanthan gum. Tablet matrices containing 10–60% of tablet weight of guar gum (F1–F6) were prepared by direct compression and subjected to in vitro release studies to explore their sustained release in the colon. Various release retarding synthetic and natural polymers, namely, hydrogenated castor oil, hydroxypropyl methyl cellulose, xanthan gum, and ethyl cellulose, Eudragit RL 100, were incorporated to modify the drug release rate from the guar gum matrix tablets. Matrix tablets were enteric coated with hydroxypropyl methyl cellulose phthalate as an enteric polymer. Various synthetic and natural polymers were incorporated to F6 to modify the drug release rate. Different 15 matrix tablet formulations (F6–F20) were enteric coated with hydroxypropyl methyl cellulose phthalate. The in-vitro drug release study was undertaken at 37±0.5°C in 0.1N HCl for 2 h; followed by pH 7.4 phosphate buffer (3h) finally in, simulated colonic fluid pH 6.8 phosphate buffer 20 h. The formulation F6, F13 and F20 showed promising sustained release results having median dissolution time (MDT) values: 8.25, 7.97, and 7.64, respectively. When studies were continued in colonic fluids, matrix tablets released almost 100% drug. whereas, Metronidazole enteric formulations did not release drug in stomach and small intestine, but delivered drug to the colon resulting in slow absorption of the drug and making drug available for local action in the colon.&#x0D; Keywords: Colon Target Delivery, Guar gum, Metronidazole, Enteric coated, Tablet Matrices

Evaluating Hydrocolloids of Sida Acuta as Sustained Release Matrix for Ibuprofen Tablet

Background and Objectives: Matrix tablet formulation for ibuprofen using natural hydrocolloids are a good alternative to conventional ibuprofen immediate-release tablet and would be a desired option as opposed to the use of synthetic polymer. This work was to prepare and evaluate sustained-release ibuprofen matrix tablets using Sida acuta gum. Guar gum is the reference natural polymer. Materials and Methods: Sida gum was obtained from aqueous macerate of Sida acuta leaves then precipitated using acetone, whereas guar gum was purchased. Both gums were characterized for micromeritics, swelling properties, and hydration capacities. The granules of ibuprofen, using a gum for a separate batch, were prepared by wet granulation method. The matrix tablets were produced, physical properties determined, and dissolution studies carried out. The release kinetics values obtained were fit into equations for kinetic studies.

Physical stability of different chitosan salts in matrix tablet formulations

Physical stability of different chitosan salts in matrix tablet formulations