scholarly journals Optimization of Carboxymethyl-Xyloglucan-Based Tramadol Matrix Tablets Using Simplex Centroid Mixture Design

2013 ◽  
Vol 2013 ◽  
pp. 1-11
Author(s):  
Ashwini R. Madgulkar ◽  
Mangesh R. Bhalekar ◽  
Rahul R. Padalkar ◽  
Mohseen Y. Shaikh
Keyword(s):  
Drug Release ◽  
Oral Drug Delivery ◽  
Release Kinetics ◽  
Matrix Tablets ◽  
Oral Drug ◽  
Release Mechanism ◽  
Wet Granulation ◽  
Drug Release Profile ◽  
Independent Variables ◽  
Dependent Variables

The aim was to determine the release-modifying effect of carboxymethyl xyloglucan for oral drug delivery. Sustained release matrix tablets of tramadol HCl were prepared by wet granulation method using carboxymethyl xyloglucan as matrix forming polymer. HPMC K100M was used in a small amount to control the burst effect which is most commonly seen with natural hydrophilic polymers. A simplex centroid design with three independent variables and two dependent variables was employed to systematically optimize drug release profile. Carboxymethyl xyloglucan , HPMC K100M , and dicalcium phosphate were taken as independent variables. The dependent variables selected were percent of drug release at 2nd hour and at 8th hour . Response surface plots were developed, and optimum formulations were selected on the basis of desirability. The formulated tablets showed anomalous release mechanism and followed matrix drug release kinetics, resulting in regulated and complete release from the tablets within 8 to 10 hours. The polymer carboxymethyl xyloglucan and HPMC K100M had significant effect on drug release from the tablet (). Polynomial mathematical models, generated for various response variables using multiple regression analysis, were found to be statistically significant (). The statistical models developed for optimization were found to be valid.

FORMULATION AND EVALUATION OF DRUG RELEASE PROFILE OF HYDROPHILIC POLYMER BASED INDOMETHACIN PROLONG RELEASE MATRIX TABLETS

2021 ◽  
pp. 30-33
Author(s):  
Jayashree B. Gaja ◽  
Jesindha Beyatricks ◽  
Monisha R
Keyword(s):  
Drug Release ◽  
Release Rate ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Dosage Forms ◽  
Matrix Tablets ◽  
Wet Granulation ◽  
Drug Release Profile ◽  
Drug Release Rate ◽  
Weight Variation

An oral modied release dosage forms have always been more effective therapeutic alternative to conventional dosage forms. The present invention is directed to a modied release pharmaceutical composition of indomethacin by using hydrophilic release retardant polymers like HPMC K15M, Na CMC alone or in combination. Matrix embedded prolong release tablet formulations of Indomethacin were prepared by wet granulation technique and evaluated for tablet properties such as the thickness, hardness, friability, weight variation, drug content, drug release kinetics and in vitro release studies. The inuence of drug polymer ratio on drug release was studied by dissolution test. The FTIR studies showed no interactions among drug and polymers. The tablets formulation (F7 and F8) containing combined polymers of HPMC K15M and Na CMC resulted in slower drug release rate form the matrix. So, it can be concluded that Indomethacin prolong release tablets using HPMC K15M and Na CMC as the retardant has successfully extended the release of indomethacin from its formulations. The mixing of two cellulose polymers, ionic and non-ionic, for the formulation of hydrophilic matrices, resulted in a valuable decrease in drug release rate. All the formulations showed KorsmeyerPeppa’s model as a best t.

scholarly journals Optimizing the Role of Polymer Blend in the Preparation of Acyclovir Controlled-Release Tablets: An Approach for Better Patient Compliance

2018 ◽  
Author(s):  
Barkat Khan ◽  
Faheem Haider ◽  
Kifayat Shah ◽  
Bushra Uzair ◽  
Kaijian Hou ◽  
...  
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Release Kinetics ◽  
Immediate Release ◽  
Matrix Tablets ◽  
Release Mechanism ◽  
In Vitro Drug Release ◽  
Solubility Study ◽  
Release Data

This study was carried out to formulate and evaluate controlled release (CR) matrix tablets of Acyclovir using combination of hydrophilic and hydrophobic polymers. Acyclovir is a guanine derivative and is its half-life is short hence administered five times a day using immediate release tablets. Six formulations (F1-F6) were developed using Ethocel and Carbopol in equal combinations at drug-polymer (D:P) ratio of 10:5, 10:6, 10:7, 10:8, 10:9 and 10:10. Solubility study was performed using six different solvents. The compatibility studies were carried out using FTIR and DSC. According to USP, Quality Control and dimensional tests (hardness, friability, disintegration and thickness) were executed. In-vitro drug release studies of Acyclovir was carried out in dissolution apparatus using using 0.1 N HCl medium at constant temperature of 37 ± 0.5 ºC. In order to analyze the drug release kinetics, five different mathematical models were applied to the release data. The results showed that there was no incompatibility between drug and polymers. Physical QC tests were found within limits of USP. The release was retarded upto 24 hrs and non-fickian in-vitro drug release mechanism was found. A formulation developed using blend of polymers, showed excellent retention and desired release profiles thus providing absolute control for 24 hrs.

scholarly journals DESIGN AND IN VITRO/IN VIVO EVALUATION OF EXTENDED RELEASE MATRIX TABLETS OF NATEGLINIDE

2018 ◽  
Vol 7 (6) ◽  
Author(s):  
Mohini Sihare ◽  
Rajendra Chouksey
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Release Profile ◽  
Matrix Tablets ◽  
In Vivo Studies ◽  
Release Mechanism ◽  
In Vivo Evaluation

Aim: Nateglinide is a quick acting anti-diabetic medication whose potent activity lasts for a short duration. One of the dangerous side effects of nateglinide administration is rapid hypoglycemia, a condition that needs to be monitored carefully to prevent unnecessary fatalities. The aim of the study was to develop a longer lasting and slower releasing formulation of nateglinide that could be administered just once daily. Methods: Matrix tablets of nateglinide were prepared in combination with the polymers hydroxypropylmethylcellulose (HPMC), eudragits, ethyl cellulose and polyethylene oxide and the formulated drug release patterns were evaluated using in vitro and in vivo studies. Conclusion: Of the seventeen formulated matrix tablets tested, only one formulation labelled HA-2 that contained 15% HPMC K4M demonstrated release profile we had aimed for. Further, swelling studies and scanning electron microscopic analysis confirmed the drug release mechanism of HA-2. The optimized formulation HA-2 was found to be stable at accelerated storage conditions for 3 months with respect to drug content and physical appearance. Mathematical analysis of the release kinetics of HA-2 indicated a coupling of diffusion and erosion mechanisms. In-vitro release studies and pharmacokinetic in vivo studies of HA-2 in rabbits confirmed the sustained drug release profile we had aimed for. Keywords: Hydroxypropylmethylcellulose, Matrix tablets, Nateglinide, Sustained release

scholarly journals Formulation and Evaluation of Sustained Release Matrix Tablets of Aceclofenac

2021 ◽  
Vol 4 (2) ◽  
pp. 99-109
Author(s):  
Priyanka Singh ◽  
Amit Kumar Shrivastava ◽  
Sachin Kumar ◽  
Manish Dhar Dwivedi
Keyword(s):  
Drug Release ◽  
Guar Gum ◽  
Polymer Concentration ◽  
Matrix Tablets ◽  
Hydrophilic Polymers ◽  
Wet Granulation ◽  
Drug Release Profile ◽  
In Vitro Drug Release ◽  
Study Results

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.

scholarly journals Development and evaluation of sustained release losartan potassium matrix tablet using kollidon SR as release retardant

2012 ◽  
Vol 48 (4) ◽  
pp. 621-628 ◽  
Author(s):  
Shahid Sarwar ◽  
Mohammad Salim Hossain
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Release Kinetics ◽  
Polymer Concentration ◽  
In Vitro Release ◽  
Matrix Tablets ◽  
Losartan Potassium ◽  
Dissolution Time ◽  
Release Mechanism ◽  
Matrix Tablet

The present study was undertaken to develop sustained release (SR) matrix tablets of losartan potassium, an angiotensin-II antagonist for the treatment of hypertension. The tablets were prepared by direct compression method, along with Kollidon SR as release retardant polymer. The amount of losartan potassium remains fixed (100 mg) for all the three formulations whereas the amounts of Kollidon SR were 250 mg, 225 mg, and 200 mg for F-1, F-2, and F-3 respectively. The evaluation involves three stages: the micromeritic properties evaluation of granules, physical property studies of tablets, and in-vitro release kinetics studies. The USP apparatus type II was selected to perform the dissolution test, and the dissolution medium was 900 mL phosphate buffer pH 6.8. The test was carried out at 75 rpm, and the temperature was maintained at 37 ºC ± 0.5 ºC. The release kinetics was analyzed using several kinetics models. Higher polymeric content in the matrix decreased the release rate of drug. At lower polymeric level, the rate and extent of drug release were enhanced. All the formulations followed Higuchi release kinetics where the Regression co-efficient (R²) values are 0.958, 0.944, and 0.920 for F-1, F-2, and F-3 respectively, and they exhibited diffusion dominated drug release. Statistically significant (P<0.05) differences were found among the drug release profile from different level of polymeric matrices. The release mechanism changed from non-fickian (n=0.489 for F-1) to fickian (n=0.439 and 0.429 for F-2, and F-3 respectively) as a function of decreasing the polymer concentration. The Mean Dissolution Time (MDT) values were increased with the increase in polymer concentration.

DEVELOPMENT AND EVALUATION OF MODIFIED RELEASE MATRIX TABLETS OF MILNACIPRAN HCL USING MELT GRANULATION TECHNIQUE

INDIAN DRUGS ◽  
2018 ◽  
Vol 55 (02) ◽  
pp. 68-71
Author(s):  
N. C Ratnakara ◽  
◽  
M. C. Gohel
Keyword(s):  
Drug Release ◽  
Matrix Tablets ◽  
Matrix Tablet ◽  
Modified Release ◽  
Independent Variables ◽  
Dependent Variables ◽  
Formulation Parameters ◽  
Predicted Values ◽  
Melt Granulation

The objective of the present study was to identify critical formulation parameters affecting the drug release from modified release wax matrix tablet of milnacipran hydrochloride employing the concept of design of experiments.The optimized amount of Compritol 888 ATO(intragranular) (X1), lactose (X2) and Compritol 888ATO (extragranular)(X3) were determined employing simplex latticedesign. The tablets were prepared using melt granulation technique. The in vitro drug release study was carried out in an acidic medium (pH 1.2) for 2 h and thereafter the dissolution study was conducted in phosphate buffer (pH 6.8).The selected dependent variables were the cumulative percentage of milnacipran hydrochloride dissolved at 1 (Y1), 8 (Y8), 16 (Y16) and 24 h (Y24). Mathematical models, correlating the independent variables with dependent variables were evolved. Optimization was performed for the three independent variables using the stated target ranges; Y1≤20%; Y8=45±5%; Y16=72±5%; Y24=100%. The optimized amounts of Compritol ATO888 (intragranular)(X1), lactose (X2) and Compritol 888ATO (extragranular)(X3), were found to be 60, 55 and 30 mg, respectively.The optimized formulation showed a release profile that was close to the predicted values. The drug was released by anomalous diffusion from the optimized formulation. Compritol 888ATO (intragranular) (X1), lactose (X2) and Compritol 888ATO(extragranular) (X3) were identified as critical variables.

scholarly journals Synthesis and characterization of oral drug delivery, a pH – sensitive silver nanocomposite based on sodium alginate extracted from Sargassum asperifolium collected from Jazan coasts, KSA

2019 ◽  
Author(s):  
Fatimah. A. Agili ◽  
Sahera. F. Mohamed
Keyword(s):  
Electron Microscope ◽  
Drug Release ◽  
Sodium Alginate ◽  
Oral Drug Delivery ◽  
Drug Carrier ◽  
Gastric Fluid ◽  
Ph Sensitive ◽  
Oral Drug ◽  
Release Mechanism ◽  
X Ray

AbstractThe pH-sensitive nanocomposite composed of sodium alginate/ Pectin/ Tannic acid – silver SA/Pec/TA-Ag was prepared using microwave irradiation and employed as a carrier for Propranolol drug. Physico-chemical characteristics of the prepared systems using Fourier Transform Infrared Spectroscopy (FTIR), X-ray Diffraction (XRD), Field Emission Scanning Electron Microscope (FESEM), High-Resolution Transmission Electron Microscope (HRTEM), Dynamic light Scattering instrument (DLS), and Energy Dispersive X-Ray Analysis (EDX). The percentage drug release was 96% at pH 7.4 within 420 min. The drug release data was fitted into different kinetic models included zero order, First order, Higuchi and Ritger-Peppas model. The release mechanism is non-Fickian character where it controlled by diffusion and relaxation of polymer chains. It can be concluded that SA/Pec/TA-Ag nanocomposite is candidate for the oral drug carrier specific for intestinal system and has stability against gastric fluid.

scholarly journals Formulation and Evaluation of Gabapentin Sustained Release Matrix Tablet Using Hibiscus rosa sinensis Leaves Mucilage as Release Retardant

2021 ◽  
pp. 564-572
Author(s):  
P. Amsa ◽  
G. K. Mathan ◽  
S. Magibalan ◽  
E. K. Velliyangiri ◽  
T. Kalaivani ◽  
...  
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Magnesium Stearate ◽  
Matrix Tablets ◽  
Wet Granulation ◽  
Matrix Tablet ◽  
Hibiscus Rosa Sinensis

The major goal of this study was to develop and evaluate Sustained release matrix tablets of Gabapentin with Hibiscus rosa - sinensis leaves mucilage prepared by using wet granulation technique with microcrystalline cellulose as a diluents and magnesium stearate as a lubricant. Pre-compression and post-compression evaluation of physicochemical parameters were carried out and to be within acceptable limits. Drug and polymer compatibility were validated by FTIR measurements. Further, tablets were evaluated for in vitro release study. To get the sustained release of Gabapentin, the concentration of Hibiscus rosa- sinensis mucilage was tuned with a gas-generating agent. The % drug release of all formulation from F1 to F5 showed 91.24%, 80.24%, 70.53%, 62.12% and 49.83% respectively. All the dosage form release kinetics was computed using zero order, first order, Higuchi, and Korsmeyer–Peppas methods. From the above results, it is concluded that the n value of formulation F5 showed 0.78 suggesting anomalous (non-fickian) behavior of the drug. Mucilage from the leaves of Hibiscus rosa-sinensis has a great retarding effect in drug release from sustained release tablets.

scholarly journals Design, Fabrication and Evaluation of Drug Release Kinetics from Aceclofenac Matrix Tablets using Hydroxypropyl Methyl Cellulose

1970 ◽  
Vol 8 (1) ◽  
pp. 23-30 ◽  
Author(s):  
Abul Kalam Lutful Kabir ◽  
Bishyajit Kumar Biswas ◽  
Abu Shara Shasur Rouf
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Release Kinetics ◽  
Matrix Tablets ◽  
Angle Of Repose ◽  
Release Mechanism ◽  
Matrix Tablet ◽  
Drug Content ◽  
Compressibility Index

The objective of this study was to develop a sustained release matrix tablet of aceclofenac usinghydroxypropyl methylcellulose (HPMC K15M and HPMC K100M CR) in various proportions as release controllingfactor by direct compression method. The powders for tableting were evaluated for angle of repose, loose bulkdensity, tapped bulk density, compressibility index, total porosity and drug content etc. The tablets were subjected tothickness, weight variation test, drug content, hardness, friability and in vitro release studies. The in vitro dissolutionstudy was carried out for 24 hours using United States Pharmacopoeia (USP) 22 paddle-type dissolution apparatus inphosphate buffer (pH 7.4). The granules showed satisfactory flow properties, compressibility index and drug contentetc. All the tablets complied with pharmacopoeial specifications. The results of dissolution studies indicated that theformulations F-2 and F-3 could extend the drug release up to 24 hours. By comparing the dissolution profiles with themarketed product, it revealed that the formulations exhibited similar drug release profile. From this study, a decreasein release kinetics of the drug was observed when the polymer concentration was increased. Kinetic modeling of invitro dissolution profiles revealed the drug release mechanism ranges from diffusion controlled or Fickian transport toanomalous type or non-Fickian transport, which was only dependent on the type and amount of polymer used. Thedrug release followed both diffusion and erosion mechanism in all cases. The drug release from these formulationswas satisfactory after 3 months storage in 40°C and 75% RH. Besides, this study explored the optimum concentrationand effect of polymer(s) on acelofenac release pattern from the tablet matrix for 24 hour period.Key words: Aceclofenac; sustained release; hydrophillic matrix; HPMC; direct compression.DOI: 10.3329/dujps.v8i1.5332Dhaka Univ. J. Pharm. Sci. 8(1): 23-30, 2009 (June)

scholarly journals Development and evaluation of gastroretentive norfloxacin floating tablets

2009 ◽  
Vol 59 (2) ◽  
pp. 211-221 ◽  
Author(s):  
Ramesh Bomma ◽  
Rongala Swamy Naidu ◽  
Madhusudan Yamsani ◽  
Kishan Veerabrahma
Keyword(s):  
Drug Release ◽  
Hydroxypropyl Methylcellulose ◽  
Matrix Tablets ◽  
Fickian Diffusion ◽  
Release Mechanism ◽  
Wet Granulation ◽  
Drug Bioavailability ◽  
Floating Tablets

Development and evaluation of gastroretentive norfloxacin floating tabletsFloating matrix tablets of norfloxacin were developed to prolong gastric residence time, leading to an increase in drug bioavailability. Tablets were prepared by the wet granulation technique, using polymers such as hydroxypropyl methylcellulose (HPMC K4M, HPMC K100M) and xanthan gum. Tablets were evaluated for their physical characteristics,viz., hardness, thickness, friability, and mass variation, drug content and floating properties. Further, tablets were studied forin vitrodrug release characteristics for 9 hours. The tablets exhibited controlled and prolonged drug release profiles while floating over the dissolution medium. Non-Fickian diffusion was confirmed as the drug release mechanism from these tablets, indicating that water diffusion and polymer rearrangement played an essential role in drug release. The best formulation (F4) was selected based onin vitrocharacteristics and was usedin vivoradiographic studies by incorporating BaSO4. These studies revealed that the tablets remained in the stomach for 180 ± 30 min in fasting human volunteers and indicated that gastric retention time was increased by the floating principle, which was considered desirable for the absorption window drugs.

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