Development and evaluation of buccal film containing antihypertensive agent (original) (raw)
Related papers
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.
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...
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.
Journal of Pharmaceutical Innovation, 2019
The aim of this work was to optimize unidirectional buccal patches loaded with metoprolol (MT-MBPs) to provide adequate mucoadhesive and water uptake properties as well as controlled drug release for the effective treatment of different cardiovascular diseases. Methods The patches were prepared layer-by-layer using the solvent casting method. A central composite design was employed to statistically optimize the formulation variables. Chitosan and Pluronic® F-127 (poloxamer 407) concentrations were chosen as the independent variables, while ex vivo mucoadhesive force, ex vivo residence time, in vitro water uptake (%), and in vitro drug release (%) were to be considered the dependent variables. The optimized formulation was also characterized and evaluated in terms of morphology, thermal behavior, tensile strength, elongation at break, and ex vivo drug permeation. Results The optimized MT-MBPs were successful in terms of mucoadhesive force (3.58 ± 0.62 N), residence time (342.67 ± 17.21 min), and water uptake at 1 h (24.53 ± 3.62%). A controlled drug release was obtained for 8 h. Thermal and morphologic analyses demonstrated that metoprolol was homogeneously distributed throughout the microporous chitosan-based polymer matrix. Furthermore, the MT-MBPs exhibited a tensile strength of 3.76 ± 0.55 N/mm 2 and an elongation at break of 36.52 ± 13.88%. The results of ex vivo permeation through pig buccal mucosa indicated that therapeutic metoprolol concentrations can be reached by using a patch of 5.62 cm 2. Conclusions Optimal composition of the MT-MBPs included 2.9% (w/v) and 2.6% (w/v) of chitosan and Pluronic® F-127, respectively, which constitutes the most suitable makeup for metoprolol buccal delivery.
FORMULATION AND EVALUATION OF CONTROLLED POROSITY OSMOTIC TABLET OF METOPROLOL SUCCINATE
Objectives: Metoprolol Succinate is mainly used to treat hypertension. It has a short elimination half- life and rapidly absorbed in GIT. Conventional tablets of Metoprolol succinate require multiple dosing with resulting inconvenience to the hypertensive patient and the possibility of reduced patient compliance. Experimental Work: Core tablets for drug were prepared by direct compression technique using mannitol, fructose, KCl as osmogens and Avicel PH101 as direct compressible diluents. The prepared core tablets were coated by coating agent cellulose acetate (2%w/v) with PEG400 and PEG 6000as water soluble pore former and dibutyl-pthalate as plasticizer. The formulations were evaluated for their pre compression and post compression characterizations. Results and discussion: The present study confirmed that the drug release depends on the % weight gain of tablet and it is inversely proportional to membrane weight gain. The combination of two osmogens shows better drug release as compared to individual.
https://www.ijhsr.org/IJHSR\_Vol.9\_Issue.4\_April2019/IJHSR\_Abstract.031.html, 2019
The objective of this study was to design and evaluate an oral extended drug delivery system for Metoprolol succinate using natural hydrophilic gums such as Xanthan Gum, Guar Gum, Pectin and Carrageenan as a release modifier. Twenty four batches were prepared by using in combination of 1:1, 1:2 and 2:1 ratios of Natural polymers and Avicel RS 581. Matrix tablets were prepared by wet granulation method and granules are coated with rate release polymers like Ethyl cellulose and Hydroxy propyl methyl cellulose. The formulations were evaluated for angle of repose, bulk density, tapped density, Compressibility Index, % LOD (Pre compression properties) and weight variation, content uniformity, friability, hardness, thickness, in vitro drug release studies(Post compression properties). Among the formulations studied formulation H-MSG 1 containing combination of Guar Gum and Avicel RS 581 (1:1) showed extended release of drug for 24 hrs with cumulative percent release of 99.46% ± 0.01%. The kinetic treatment showed that the optimized formulation followed first order kinetics and the release exponent (n) 1.199 through Korsmeyer and Peppas equation shown that the formulation follows super case II. The matrix formulation H-MSG 1 showed sustained release of Metoprolol succinate by the diffusion mechanism. On comparison with the marketed formulation, the best formulation H-MSG 1 showed similarity factor (f 2) of 80.09 indicted more significant in drug release behaviour.
Development and evaluation of floating tablet of metoprolol succinate for increased bioavailability
International Journal of Advances in Pharmaceutical Sciences, 2018
The present study is based on development and evaluation of gastroretentive floating tablets of metoprolol succinate by direct compression method, to increase the oral bioavailability of MS. For this, we used a combination of two different hydrophilic polymers that is polyethylene oxide PEO N-80 (X1) and hydroxyethylcellulose HEC (X2) as independent variables and studied its effect on drug release (as dependent variable) at 20h for MS. A 3 2 factorial design was used for optimization purpose. The DSC result shows no interaction between two polymers and the drug (MS). Further, invitro drug release studies have shown a sustained drug release for more than 20h in upper gastrointestinal region (stomach). In vivo study using rabbits have shown increased AUC0-24 (bioavailability) of prepared optimized F6 formulation as compared to the marketed sustain release tablet of MS. Stability study shows no comparable differences on physical parameters and the drug release after 3 months of accelerated stability testing. Hence, we can conclude that a floating tablet containing combination of hydrophilic polymers can be used for gastric retention for more than 20hr which will increase the oral bioavailability of MS.
Mucoadhesive Buccal Films: A Novel Approach for the Delivery of Anti-Hypertensive Drugs
Asian Journal of Pharmaceutical and Clinical Research
The buccal drug delivery system is a prominent route of administration for drug delivery through the buccal mucosa. It is rich in blood supply with more surface area for rapid absorption as well as provides direct entry of drugs from the site of application into the systemic circulation through the jugular vein. Buccal drug delivery systems consist of various approaches such as lozenges, wafers, gels, microparticles, patches or films from which mucoadhesive buccal film is an attractive dosage form in terms of flexibility and high systemic bioavailability. Since most of the antihypertensive drugs show first-pass metabolism which leads to less oral bioavailability generally up to 20–50%. Thus, incorporation of antihypertensive drugs in mucoadhesive buccal films using mucoadhesive polymers can provide higher systemic bioavailability. The films can be formulated using various techniques such as solvent casting method and hot extrusion melt method. These films can be evaluated based on v...
The current study was aimed to formulate a continuous release mucoadhesive buccal tablet containing propranolol HCl. The type and quantities of polymers as well as method of compression were set in a preliminary study (F1-F13). Direct compression method was employed in the main study (F14-F24) using Carbopol ® 934P (CP), ethylcellulose (EC), sodium alginate (SA), hydroxypropyl methylcellulose (HPMC k4M) and carboxymethylcellulose (CMC) as mucoadhesive polymers and were tested for physicochemical tests i.e. swellability, surface pH, mucoadhesive time, mucoadhesive strength, in vitro release etc. Results obtained from the study were optimized using NeuralPower ® 3.1, an artificial intelligence approach. Against the desirability of physico-chemical parameters, the software optimized the ingredients as HPMC (150mg), CMC (25mg), CP (20mg) and EC (20mg). Outcome revealed that HPMC primarily contributed to the physicochemical properties of mucoadhesive formulation. To compare prediction, optimized ingredients were formulated (F25) and tested. The swellability index of confirmation formulation (F25) was 102% at 6 h. As predicted, similar release pattern was of F25 was obtained as 26% (0.5h), 34% (1h), 40% (2h), 45% (3h), 50% (4h), 62% (5h), 76% (6h), 85% (7h) and 97% (8h) respectively. For release kinetics, DD solver ® suggested the release of the drug to be non-Fickian.
In the present context the buccal route ranks with oral treatment as the successful innovative research area in the drug delivery. However the success of a drug to be used for systemic delivery via buccal route depends mainly on the ability of the drug to permeate through buccal mucosa in sufficient quantities which can be achieved with the help of penetration enhancers. Metoprolol tartrate is the preferred drug because it has plasma half life of 3-4 hrs and has low bioavailability which is an essential condition for formulation of buccal patches. In this study, hydrophilic polymers like Gelatin, Na alginate were used in different concentrations. The result of present investigation stated that the Sod. Gelatin and Na Alginate have good matrix/film forming characteristics which was confirmed by the visual and physiological characterization of the patches. In-vitro and exvivo studies indicated that successful buccal patches of Metoprolol Tartrate could be prepared using hydrophilic polymers viz. Gelatin and Na Alginate employing solvent casting technique.