Formulation and Evaluation of Extended Release Matrix Tablets of Metoprolol Succinate Using Natural Polymers (original) (raw)
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Asian Journal of Pharmaceutics, 2011
T he purpose of the present work is to design and evaluate extended release matrix tablets of metoprolol succinate to reduce the dosing frequency and to improve patient compliance. The matrix tablets were prepared by the combination of hydrophilic and hydrophobic polymers, using methocel 10000 Cps in combination with ethyl cellulose 7 Cps, Eudragit ® RS100, Eudragit ® S100, and Eudragit ® L100.The tablets were prepared by direct compression technique. Prepared formulations were evaluated for various parameters like weight variation, thickness, hardness, friability, and % drug content. Tablets were subjected to in vitro drug release studies. The formulations containing methocel 10000 Cps, Eudragit ® L100 showed good release retardation. All the prepared formulations showed first-order release kinetics with matrix diffusion mechanism of release. The formulation containing 52.06% w/w of methocel 10000 Cps, 8.75% Eudragit ® L100 offered the required release rate according to USP Pharmacopoeial guidelines. The combination of hydrophilic and hydrophobic polymers can effectively control the drug release for freely water-soluble drugs in case of extended release formulations which are the upcoming dosage forms for patient compliance in all aspects.
METOPROLOL SUCCINATE SUSTAINED RELEASE MATRIX TABLETS-FORMULATION DEVELOPMENT AND INVITRO EVALUATION
International journal of Pharmacy and Pharmaceutical Sciences, 2014
Objective: Metoprolol succinate is a Beta 1 selective antagonist used as an Anti hypertensive, Anti angina, Anti arrhythmic. The aim of present investigation was to develop matrix tablets of Metoprolol succinate using different polymers. Methods: Metoprolol succinate matrix tablets were prepared by direct compression and wet granulation method using different polymers. All the formulations were evaluated for weight variation, thickness, hardness, friability and dissolution. Results: It has been studied that a matrix tablet containing hydroxyl propyl methyl cellulose polymers for oral controlled delivery of Metoprolol succinate has been formulated with greater significance; hence it was decided to check the in-vitro drug-polymer study in formulating a sustained release tablet for Metoprolol succinate. All the formulations are prepared by using polymers include HPMC K15M, HPMC K100M, Ghatti gum, Sodium CMC, Pectin. All the formulation is subjected to invitro dissolution studies. Conclusion: Among all these formulations F-11 is optimized. This formulation containing 50mg of drug, 150mg of HPMC K15M, 3mg of Mg stearate, 3mg of talc, and 69mg of MCC. As the result of this study it may conclude that the formulation meet the needed theoretical drug release profile and has the sustain action i.e., retarding the drug release so the release is for a long time and thus more bio availability.
2014
Objective: Metoprolol succinate is a Beta 1 selective antagonist used as an Anti hypertensive, Anti angina, Anti arrhythmic. The aim of present investigation was to develop matrix tablets of Metoprolol succinate using different polymers. Methods: Metoprolol succinate matrix tablets were prepared by direct compression and wet granulation method using different polymers. All the formulations were evaluated for weight variation, thickness, hardness, friability and dissolution. Results: It has been studied that a matrix tablet containing hydroxyl propyl methyl cellulose polymers for oral controlled delivery of Metoprolol succinate has been formulated with greater significance; hence it was decided to check the in-vitro drug-polymer study in formulating a sustained release tablet for Metoprolol succinate. All the formulations are prepared by using polymers include HPMC K15M, HPMC K100M, Ghatti gum, Sodium CMC, Pectin. All the formulation is subjected to invitro dissolution studies. Concl...
Journal of Chemical and Petroleum Engineering (JChPE), 2023
Metoprolol has been widely used for controlling high blood pressure, preventing myocardial reinfarction, setting rate changes, setting heart rhythm, treatment of chronic angina, and preventing excessive bleeding during surgery. The purpose of this research is the formulation and manufacture of extended-release tablets of metoprolol succinate that conform to all the in vitro physicochemical US Pharmacopoeia national formulary (USP32). For preparing the tablets, the hydrophilic HPMC(K100M) polymer was used in the direct compression method. The release of metoprolol in phosphate buffer having pH=6.8 (USP32) was measured by HPLC. Also, using experimental correlation of diffusivity in a buffer medium and Gurney-Lurie charts during tablet enlargement with time, diffusion coefficients of drug and partition coefficients were obtained at different time steps. The rate of drug release depends on the type, viscosity, and polymer concentration. Drug release results over 20 hours for polymers of HPMC(K100M), HPMC(K4M), HPMC(K15M), polyethylene oxide, ethyl cellulose, and Eudragit (RL100) were investigated and compared. The results demonstrated that HPMC(K100M) met the standards of USP32 very well and was superior over the other polymers tested.
Journal of Applied Pharmaceutical Science, 2012
The objective of this study was to develop a sustained release matrix tablet Metoprolol Succinate by cost saving and production efficient process. Among various tablet manufacturing process, direct compression is the simplest and cost saving process. Different trials were formulated and evaluated using different concentrations of directly compressible grade Kollidon SR as release retardant. The formulated tablets were evaluated for physical and dissolution study using buffer medium. The most outstanding aspect of this study is to monitor the influence of different percentage of Kollidon SR on release rate from the matrix tablet. In this study, influence of different ratio of polymer concentration on drug release was evaluated. The release pattern of different batches were evaluated for Zero order, Higuchi, First order, Krosmeyer-Peppas and Hixson-Crowell kinetics and showed that all the batches followed best the Higuchi kinetics. The drug release kinetics was found to be governed by the amount of the polymer in the matrix system. The higher polymeric content in the matrix decrease the release rate of the drug. The nature of the drug release from the matrix tablets was dependent on drug diffusion and polymer relaxation and therefore followed non-Fickian or anomales release. The studies indicated that the drug release can be modulated by varying the concentration of the polymer. Among the four formulations, formulation 1 is the best formulation as it controls the release best and best linearity for zero order plots.
The objective of the present study was to formulate and develop extended release drug delivery system of anti-hypertensive drug Metoprolol succinate. The major indications of Metoprolol succinate is treatment and management of hypertension, angina, acute myocardial infarction, supraventricular tachycardia, congestive heart faiure, and migrane. Hypertension (HTN)is a chronic medical condition in which the blood pressure in the arteries is elevated. High blood pressure is said to be present if it is persistently at or above 140/90 mmHg pressure. The dosage for adults is 2-3 times a day, to reduce the dosing interval to one time a day Metaprolol succinate developed as extended release capsules. Which reduces the dosing interval. Preliminary studies with different polymers such as Surelase, Ethyl cellulose N22, Kollicoat SR 30D were performed. The results of in-vitro release data showed that Kollicoat SR 30D can Extend the drug release upto 24hr. The drug content was within the range, 98.23±0.25 to 102.03±2.45%. The in-vitro metoprolol succinate release from the capsules was found Extended over 24 hours with korsmeyer-peppas kinetics of drug release and release pattern followed Super case-II transport. The Fourier transform Infrared spectroscopy (FT-IR) analyses indicated that there was absence of any chemical interaction between the drug and the excipients. Thus the objective of extended release drug delivery system of anti-Hypertensive drug Metoprolol succinate with extended release profile was achieved.
Drug Delivery and Translational Research, 2018
The current study reports on the manufacturing of extended release dosage forms of Metoprolol succinate via hot-melt extrusion (HME) technology. Either Eudragit ® S100 and Eudragit ® L100 alone or in combination with release modifying agent Polyox TM WSR 303 and Eudragit ® L100-55 were processed to obtain complete and faster release. Metoprolol Succinate with similar solubility parameters to polymer were dispersed in polymer matrix, and was characterized by Fourier Transform Infra-red Spectroscopy (FT-IR), differential scanning calorimetry (DSC), Xray diffraction (XRD) and Scanning electron microscopy (SEM). Stability of drug after extrusion was confirmed by thermogravimetric analysis and high performance liquid chromatography. Physical characterization method exhibited that the drug was homogeneously dispersed in noncrystalline state in Eudragit ® L100-55 based formulations whereas in semi-crystalline state in Polyox TM WSR 303. The drug release percentage was below 3% and 40% in 0.1N HCL with Eudragit ® L100-55 and Polyox TM WSR 303 containing formulations, respectively and exhibited pH dependent dissolution properties. The drug release mechanism was anomalous with Polyox TM WSR 303 formulations whereas diffusion through pore formation was obtained with Eudragit ® L100-55. Both Eudragit ® L100-55 and Polyox TM WSR 303 changed the release mechanism and kinetics of drug release from thermally processed dosage forms. The optimized stable formulation is similar to the marketed formulation with F2 value is 72.36. Thus, it can be concluded that HME was exploited as an effective process for the preparation of controlled release matrix system based on pH dependent polymer matrices Eudragit ® S100 and Eudragit ® L100.
international journal of chemical sciences, 2009
In the present study, metoprolol tartrate (MT) was chosen as a model drug, which is a -1- selective adrenergic blocking agent and is prescribed widely in diverse cardiovascular diseases like hypertension; angina pectoris, arrhythmias and myocardial infarction but because of its short half life (3-4 hrs) and its high water solubility, it was chosen as a suitable candidate for sustained release matrix tablet formulation. It was formulated into matrix tablet using hydrophilic polymers such as hydroxy propyl methyl cellulose (HPMC 15 cps), sodium carboxy methyl cellulose (NaCMC) and guar gum (GG) as release retardants. All the precompressional parameters like angle of repose, Hausner’s ratio and Carr’s index were found to be within the standard limits. Tablets were evaluated for hardness, friability, thickness, drug content, in vitro release, swelling and stability study. The effect of polymer concentration, binary polymer mixture and wet granulation methods on drug release profiles was...
The main objective of present investigation is to formulate the sustained release tablet of Metoprolol Succinate using 32 factorial design. Metoprolol Succinate, is a selective β1blocker, to treat Hypertension & Heart Failure. The SR tablets of Metoprolol Succinate were prepared employing different concentrations of HPMCK15M and HPMCK100M in different combinations as a rate retardants by Direct Compression technique using 32 factorial design. The quantity of rate retarders, HPMCK15M and HPMCK100M required to achieve the desired drug release was selected as independent variables, X1 and X2 respectively whereas, time required for 10% of drug dissolution (t10%), 50% (t50%), 75% (t75%) and 90% (t90%) were selected as dependent variables. Totally nine formulations were designed and are evaluated for hardness, friability, thickness, % drug content, In-vitro drug release. From the Results it was concluded that all the formulation were found to be with in the Pharmacopoeial limits and the Invitro dissolution profiles of all formulations were fitted in to different Kinetic models, the statistical parameters like intercept (a), slope (b) & regression coefficient (r) were calculated. Polynomial equations were developed for t10%, t50%, t75%, t90%. Validity of developed polynomial equations were verified by designing 2 check point formulations(C1, C2). According to SUPAC guidelines the formulation (F5) containing combination of 10% HPMCK15M and 10% HPMCK100M, is the most similar formulation (f2=92.38 & No significant difference, t= 0.0216) to marketed product (Metocard). The selected formulation (F5) follows Higuchi’s kinetics, the mechanism of drug release was found to be Super case II transport (Non-Fickian, n= 0.981).