PHYSICOCHEMICAL CHARACTERIZATION AND EVALUATION OF TELMISARTAN: HYDROXYPROPYL-β-CYCLODEXTRIN: TWEEN 80 INCLUSION COMPLEX

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.

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“…100 in each case. Various solid dispersions and their drug to carrier ratios are indicated in table 1 [13][14][15]. Telmisartan: Soluplus 1:5…”

Section: Preparation Of Solid Dispersions By Kneading Methodsmentioning

confidence: 99%

Solubility and Dissolution Rate Enhancement of Telmisartan by Solid Dispersion and Pelletization Techniques Using Soluplus as Carrier

Kunam¹,

Garikapati

Vidyadhara³

et al. 2019

Int J App Pharm

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“…Cyclodextrin complexation can increase the solubility and hence aid for the dissolution of the drugs from the FDTs. 11,12 Further, the complexes obtained after solvent evaporation method can have improved compressibility so as to make these high dosed drugs suitable for direct compression. 13 Hence, in this work inclusion complexes were prepared using three types of CDs at different ratios.…”

Section: Introductionmentioning

confidence: 99%

Optimization of Fast-dissolving Tablets of Ledipasvirsofosbuvir Inclusion Complexes by Design of Experiments

Thummala¹,

MADDI²,

Avula³

2023

Ind. J. Pharm. Edu. Res

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Background: Fast-dissolving tablets (FDTs) were aimed to be developed for the latest approved combination drugs for Hepatitis-C treatment, Ledipasvir (LDV) and sofosbuvir (SBV) which suffered with poor water solubility. Materials and Methods: Cyclodextrin (CD) complexation was done for the drugs to improve their solubility. The optimized CD complexes were taken for developing FDTs to improve dissolution limited bioavailability of these drugs. FDTs were developed by adopting design of experiments approach using Design Expert software. Type of β-CD, type of disintegrant and concentration of disintegrant were taken as the factors. Disintegration time, time for 90% dissolution of LDV and SBV were taken as the responses. The prepared tablets as per the selected experimental design were evaluated for the responses and also other characteristics like tensile strength, packing fraction, wettability. The results were analyzed by ANOVA and numerical optimization was performed with the desirability of minimizing all the responses. Results: All the selected factors were found to influence disintegration and dissolution times significantly. Dimethyl β-CD, croscarmellose sodium at 8% w/w was obtained as the optimized combination of the factors for the FDTs. The FTDs at this optimized combination of the factors were found to have 79.6 sec of DT, 17.72 and 13.68 min. of time for 90% dissolution of LDV and SBV respectively. Conclusion: These results which were significantly much better than those of the marketed tablets indicated that the FTDs were successfully developed using Design of experiments.

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“…This feature has been advantageously exploited for increasing the stability and bioavailability of drugs [7][8][9]. Instead of attempting only binary inclusion complex addition of small amounts of water-soluble polymers to the system, which causes an increase in solubilization efficiency and may result in reducing amounts of CD [10,11]. These results can be attributed to the synergistic effect of polymer and CD solubilization on the formation of drug: CD:water-soluble polymer ternary complexes [12,13].…”

Section: Introductionmentioning

confidence: 99%

MELOXICAM-PECTIN-β-CYCLODEXTRIN TERNARY COMPLEX BY KNEADING FOR ENHANCEMENT OF SOLUBILITY AND DISSOLUTION RATE

Jagtap¹,

Mohite²

2019

Asian J Pharm Clin Res

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Objective: The objective of the present investigation was to improve the solubility and dissolution rate of poorly soluble drug meloxicam by its ternary inclusion complexation with natural polymers and beta-cyclodextrin (β-CD) by kneading. Methods: Equimolar physical mixture (1:1) was prepared by homogeneously kneading drug and β-CD using a solution of agar and pectin in water to get a paste, then paste was dried overnight to get inclusion complex. Inclusion complex was evaluated for drug content, the yield of the adsorption process, Fourier-transform infrared (FTIR), differential scanning calorimeter (DSC), powder X-ray diffractometry (PXRD), scanning electron microscopy (SEM), dissolution, and stability studies. Results: The phase solubility diagrams exhibit AL showing a linear increase of drug solubility and indicating the formation of soluble complexes. The FTIR and DSC show compatibility between meloxicam and β-CD, while slight broadening in the peak with a reduction in intensity and early onset indicates the reduction in drug crystallinity which confirms in PXRD pattern. The SEM of binary, as well as ternary, showed no aggregation, and there was a gap between the particles also indicating good redispersibility. The dissolution rate of the drug from the kneaded ternary complex with pectin was significantly rapid compared with the pure drug. The maximum drug release was observed at 85.21±1.84% at the end of 60 min. The ternary complex was found stable after 3 months stability studies. Conclusion: The results indicated that ternary inclusion complexation with natural polymers and β-CD was most useful for enhancement of solubility and dissolution rate of a poorly soluble drug like meloxicam.

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PHYSICOCHEMICAL CHARACTERIZATION AND EVALUATION OF TELMISARTAN: HYDROXYPROPYL-β-CYCLODEXTRIN: TWEEN 80 INCLUSION COMPLEX

Cited by 7 publications

References 29 publications

Solubility and Dissolution Rate Enhancement of Telmisartan by Solid Dispersion and Pelletization Techniques Using Soluplus as Carrier

Solubility and Dissolution Rate Enhancement of Telmisartan by Solid Dispersion and Pelletization Techniques Using Soluplus as Carrier

Optimization of Fast-dissolving Tablets of Ledipasvirsofosbuvir Inclusion Complexes by Design of Experiments

MELOXICAM-PECTIN-β-CYCLODEXTRIN TERNARY COMPLEX BY KNEADING FOR ENHANCEMENT OF SOLUBILITY AND DISSOLUTION RATE

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