Immediate Release Tablets of Telmisartan Using SuperdisintegrantFormulation, Evaluation and Stability Studies (original) (raw)
Related papers
Preparation and Evaluation of Rapidly Dissolving tablet of Telmisartan
Journal of Advanced Pharmacy Research, 2018
Objective: The aim of this work was to enhance the dissolution rate of telmisartan with the goal of developing fast disintegrating tablets (FDTs) with subsequent rapid dissolution for sublingual administration. Methods: Binary solid dispersion systems (SDS) were prepared by solvent evaporation technique for the drug with Gelucire 44/14 (formula A), polyethylene glycol 4000 (PEG4000) (formula B), Pluronic F68 (formula C), hydroxypropyl methylcellulose E5 (HPMC E5) (formula D), and finally by using sodium bicarbonate with the drug in (0.5: 1) ratio (formula E), and (1:1) ratio (formula F). These systems were evaluated for drug dissolution in addition to the physicochemical changes of the drug utilizing FTIR spectroscopy, thermal analysis, and X-ray diffraction. Results: The prepared formulations using sodium bicarbonate significantly enhanced the dissolution rate of the drug compared with those prepared using different types of polymers. The order of enhanced dissolution of the drug in the first 5 min Q5 (%) was: formula E > F > D5, where the % drug dissolved was 88.94 ± 1.31, 84.77 ± 1.1 and72.6 ± 0.81 (mean + SD) for each formula, respectively. Formula E was selected for the formulation of the rapidly dissolving tablet of telmisartan since it showed enhanced dissolution of the drug, more palatable taste in the buccal cavity, relatively inexpensive material and ease of processing compared with a solid dispersion prepared using polymer. Conclusion: Sodium bicarbonate can be utilized in the preparation of telmisartan FDT with fast dissolution rate.
SOLUBILITY ENHANCEMENT OF TELMISARTAN BY VARIOUS TECHNIQUES
International Journal of Food and Nutritional Sciences, 2023
Aim/Background:-The objective of present research was aimed to intensify the bioavailability of drug Telmisartan by enhancing its solubility. It is a drug that belongs to BCS class II and has high permeability but low solubility, which is an anti-hypertensive agent. As it is low soluble its generally showing poor bioavailability. Materials/Methods:-An effort was made to improve dissolution rate through the preparation of solid dispersions of Telmisartan with water soluble carries like polyethylene glycol and beta cyclodextrin by solvent evaporation method, melt evaporation method, kneading method. Nine formulation like were prepared in the ratio of 1:1, 1:3,1:5(drug : polymer). Results/Discussion:- Evaluation tests like physiochemical parameters, wettability and in vitro dissolution study were done accordingly. All of the polymers were found to be efficient in speeding the dissolution of Telmisartan in solid dispersions as compared to the pure drug. Additional FTIR spectroscopy, different scanning calorimetry, and X-ray diffractometry investigations were carried out to characterise the drug and solid dispersion. Formulation F9 was found as best among all.
FORMULATION, OPTIMIZATION AND EVALUATION OF TELMISARTAN TABLETS
International Journal of Pharmacy & Therapeutics, 2013
The purpose of this work was to develop solid oral formulations of Telmisartan tablets using high shear granulation process with a relatively rapid drug release similar to that of the reference product Micardis. The Formulation development work was initiated with wet granulation as the API is very static in nature and having very poor flow property. In order to improve solubility and drug release, Telmisartan is converted to its sodium salt by dissolving in aqueous solution of Sodium Hydroxide. Tablets were evaluated for various parameters such as Weight variation, Thickness, Hardness, Disintegrating Time; Friability and In-vitro dissolution studies were performed using United States Pharmacopeia (USP) apparatus type II. Telmisartan has poor and pH dependent water solubility in order to enhance its dissolution surfactant and different alkalizers were used in an appropriate ratio. Nine batches of conventional Telmisartan tablet were developed and among them F-8 showed satisfactory physical parameters and release of a drug within 60 minutes with maximum release of 99.9% which is comparable to reference product.
2013
The objective of this study was to prepare and evaluate solid dispersion of Telmisartan to increase solubility and for enhancement of bioavailability. The solid dispersions were prepared by physical mixture method using PEG 6000, Eudragit L 100 and PVP K 30 as a carrier in various ratios. Optimized solid dispersion was evaluated for % CDR and Time for CDR, FTIR, DSC, SEM, and in vitro drug release study. The results showed that among the various batches containing the polymer being used in the study, F2 formulation containing DRUG: EUD L 100 in the ratio 1:1exhibited significant enhancement in solubility and dissolution profile of the drug. The results were supported by the DSC, FTIR, SEM and stability studies.
International Journal of Applied Pharmaceutics, 2020
Objective: In the present investigation, an attempt was made to improve the surface characters and solubility of the drug by solid dispersion and coating it on the nonpareil sugar beads as pellets. Methods: Telmisartan solid dispersions were prepared by kneading method using soluplus. Crospovidone was added as disintegrant in pellets. Telmisartan pellets were prepared by dissolving soluplus and crospovidone in ethanol in different ratios and coated on nonpareil sugar beads as a drug layer by pan coating technique. Various physicochemical parameters like particle size, friability, angle of repose and drug content were evaluated for the prepared solid dispersions and pellet formulations. In vitro dissolution studies were carried out in pH 7.5 phosphate buffer using USP apparatus II. Fourier Transform Infrared Spectrometry, Differential Scanning Calorimetry and Scanning Electron Microscopic analysis were performed for solid dispersions, pellet formulations and its polymers to determine the interactions and surface characteristics. Results: The physicochemical parameters were within the specified I. P limits. It was observed that the solid dispersion formulation TS5 containing 1:5 ratio of telmisartan to soluplus showed better dissolution rate to the extent of 1.143 folds and 2.033 folds when compared to a marketed formulation and the pure drug, respectively. Similarly, pellet formulation TP3 containing 1:3 ratio of telmisartan to soluplus showed an improved dissolution rate to the extent of 1.221 folds and 2.170 folds when compared to the marketed formulation and the pure drug, respectively. FTIR and DSC analysis revealed that there was no major interaction between the drug and the excipients. Conclusion: From the present study, it was observed that the solubility of telmisartan was enhanced by soluplus in pellet formulations when compared to solid dispersions.
International Journal of Applied Pharmaceutics, 2019
Objective: The main objective of the current study is to enhance the solubility of Biopharmaceutical Classification System (BCS) Class-II drug Telmisartan using jack fruit seed starch as super disintegrant which increases drug release. Methods: Starches were extracted using alkali technique using sodium hydroxide at 0.1%, 0.25%, and 0.5% concentrations and water from Jack fruit seed powder. These starches were evaluated for various phytochemical and physicochemical tests. Fast dissolving tablets were prepared using Telmisartan, jack fruit seed starch and Croscarmellose sodium in various concentrations using wet granulation technique. Various pre and post-compression parameters were evaluated along with in vitro drug release studies, characterization studies like Fourier Transform Infra-Red spectroscopy (FTIR), Differential Scanning Calorimetry (DSC), Scanning Electron Microscopy (SEM), X-Ray Diffraction (XRD) and accelerated stability studies. Results: Phytochemical tests revealed t...
The objective of the present study is optimization of telmisartan tablet formulation employing βCD, Starch 1500, and Soluplus by 2 3 factorial design to achieve NLT 85% dissolution in 10 min. Eight telmisartan tablet formulations were prepared using selected combinations of the three factors as per 23 factorial design. Telmisartan tablets were prepared by direct compression method and were evaluated. The individual and combined effects of the three factors, βCD, Starch 1500 and Soluplus are highly significant (P < 0.01) in influencing the dissolution rate of Telmisartan tablets.Telmisartan tablet formulations Fb and Fbc disintegrated rapidly in 20 and 40 seconds and gave very rapid dissolution of telmisartan, 96.1% and 95.8% in 10 min respectively. The increasing order of dissolution rate (K1) observed with various formulations was Fc< F1< Fac< Fa< Fabc< Fab< Fbc< Fb. The polynomial equation describing the relationship between the response, percent drug dissolved in 10min (Y) and the levels of βCD (X1) , Starch 1500 (X2) and Soluplus (X3) based on the observed results was found to be Y = 55.33 + 3.61(X1) + 35.07(X2) – 9.18(X1 X2) – 3.76(X3) – 3.31(X1 X3) + 2.06(X2 X3) + 1.77(X1 X2 X3) Based on the above equation, the formulation of optimized telmisartan tablets with NLT 85% dissolution in 10 min require βCD at 1:3.5 ratio of drug: βCD, Starch 1500 at 27.82% of drug and βCD content , and Soluplus at 1% of drug and βCD content. The optimized telmisartan tablet formulation gave 85.5% dissolution in 10min fulfilling the target dissolution requirement. Formulation of telmisartan tablets with NLT 85% dissolution in 10 min could be optimized by 2 3 factorial design. Key words: Formulation Development, Telmisartan tablets, Optimization, Factorial Design, βCD,Starch 1500,Soluplus
Formulation And Development Of Telmisartan Tablets Employing Factorial Designs And Stability
2017
The individual main effect and combined effect of commonly used β Cyclodextrin, Binders, disintegrants on the dissolution rate of telmisartan tablets were studied in 23 factorial designs employing selected combinations of 3 factors (β Cyclodextrin, Binders, disintegrants) of eight formulations of telmisartan tablets were prepared and evaluated All the telmisartan tablets were prepared good quality with regard to drug content, hardness, friability and disintegration time to fulfill official (IP) specifications of uncoated tablets. Many variations were observed in all the dissolution parameters of tablets prepared due to formulation variables. The ANOVA of dissolution rate (K1) indicates the individual main effect and combined effect of β Cyclodextrin, Binders, disintegrants on the dissolution rate constant (K1) are significant (P < 0.05). The ANOVA of dissolution efficiency (DE30) indicates that individual main effect and combined effect of β Cyclodextrin, Binders, disintegrants o...
Formulation and Evaluation of Telmisartan Fast Dissolving Tablets by Direct Compression Method
Research Journal of Pharmaceutical Dosage Forms and Technology, 2017
Objective: The main objective of the current study is to enhance the solubility of Biopharmaceutical Classification System (BCS) Class-II drug Telmisartan using jack fruit seed starch as super disintegrant which increases drug release. Methods: Starches were extracted using alkali technique using sodium hydroxide at 0.1%, 0.25%, and 0.5% concentrations and water from Jack fruit seed powder. These starches were evaluated for various phytochemical and physicochemical tests. Fast dissolving tablets were prepared using Telmisartan, jack fruit seed starch and Croscarmellose sodium in various concentrations using wet granulation technique. Various pre and postcompression parameters were evaluated along with in vitro drug release studies, characterization studies like Fourier Transform Infra-Red spectroscopy (FTIR), Differential Scanning Calorimetry (DSC), Scanning Electron Microscopy (SEM), X-Ray Diffraction (XRD) and accelerated stability studies. Results: Phytochemical tests revealed the presence of only starch in all the extracts. The starch prepared from 0.1% sodium hydroxide (JFS2) showed best physicochemical properties. From in vitro dissolution studies, it was observed that formulations F5 and F11 containing 15% w/w of JFS2 and 15% w/w of croscarmellose sodium showed faster disintegration and increased dissolution rate compared with other formulations. FTIR and DSC studies showed that there were no major interactions among drug and excipients. XRD studies revealed the nature of formulations. Accelerated stability studies revealed the stability of tablets. Conclusion: Thus, the tablets prepared using Jack fruit seed starch revealed the super disintegrant property of starch.
ENHANCEMENT OF AQUEOUS SOLUBILITY AND DISSOLUTION OF TELMISARTAN USING SOLID DISPERSION TECHNIQUE
The present study was aimed to improve the water solubility and bioavailability of telmisartan by solid dispersion technique. Telmisartan is 4'-[(1,4'-dimethyl-2'-propyl[2,6'-bi-1H-benzimidazol]-1'- yl)methyl]-[1,1'-biphenyl]-2-carboxylic acid. Telmisartan is practically insoluble in water. Telmisartan is an angiotensin II receptor antagonist (ARB), used in the management of hypertension. Solid dispersions of telmisartan were prepared by using poly ethylene glycol 4000 and mannitol as hydrophilic carriers in different weight ratios by solvent evaporation method. The drug and the solid dispersions were characterized by saturation solubility studies, in-vitro dissolution study, Fourier-transform infrared spectroscopy, differential scanning calorimetry, drug content estimation and stability study. Based on physical characters and drug release pattern, formulation F2 (1 g drug, 4 g PEG 4000 and 1 g mannitol) exhibited the best results. The carriers, poly ethylene glycol 4000 and mannitol were found to be effective in increasing the aqueous solubility and dissolution rate of telmisartan in solid dispersions when compared to the pure drug.