Absorption Enhancer and Polymer (Vitamin E TPGS and PVP K29) by Solid Dispersion Improve Dissolution and Bioavailability of Eprosartan Mesylate

Ahn, Jae-Soon; Kim, Kang-Min; Ko, Chan-Young; Kang, Jae-Seon

doi:10.5012/bkcs.2011.32.5.1587

Cited by 9 publications

(3 citation statements)

References 15 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Moreover, the dissolution rate of eprosartan mesylate with solid dispersion formulation VI was more rapid than the rates achieved by the solid dispersions discussed in some recent studies. 33,34 As compared to formulation VI, the dissolution profile of the corresponding physical mixture was inferior and erratic. This behavior can be ascribed to the presence of the crystalline form of the drug and the heterogeneity of the physical mixture.…”

Section: Resultsmentioning

confidence: 96%

The preparation and physicochemical characterization of eprosartan mesylate-laden polymeric ternary solid dispersions for enhanced solubility and dissolution rate of the drug

Yousaf

Zulfiqar²,

Shahzad

et al. 2019

Polim. Med.

View full text Add to dashboard Cite

Background. Eprosartan mesylate is a poorly water-soluble drug. It does not dissolve well in the aqueous gastrointestinal fluid, which means it is not absorbed well via the oral route, because a drug can cross cell membranes when it is dissolved in the gastrointestinal fluid. Objectives. The purpose of this research was to enhance the aqueous solubility and dissolution rate of eprosartan mesylate using the solid dispersion technique. Enhancing the solubility and dissolution leads to better absorption via the oral route. Material and methods. A number of eprosartan mesylate-laden polymeric solid dispersions were prepared with hydroxypropyl methylcellulose (HPMC) and polysorbate 80 by means of the solvent evaporation technique. The impact of the weight ratios of the constituents on the solubility and dissolution rate was studied in comparison with the plain drug. The formulation presenting the optimal solubility and dissolution underwent the solid-state characterization using X-ray diffraction (XRD), differential scanning calorimetry (DSC), scanning electron microscopy (SEM), and Fourier-transform infrared spectroscopy (FTIR). Results. Both polysorbate 80 and HPMC positively affected the solubility and dissolution of eprosartan mesylate. Conclusions. In particular, a ternary solid dispersion consisting of eprosartan mesylate, HPMC and polysorbate 80 at a weight ratio of 1:4.2:0.3 showed the highest solubility (36.39 ± 3.95 mg/mL) and dissolution (86.19 ±4.09% in 10 min). Moreover, the drug was present in the amorphous form in the solid dispersion with no covalent drug-excipient interactions.

show abstract

Section: Resultsmentioning

confidence: 96%

The preparation and physicochemical characterization of eprosartan mesylate-laden polymeric ternary solid dispersions for enhanced solubility and dissolution rate of the drug

Yousaf

Zulfiqar²,

Shahzad

et al. 2019

Polim. Med.

View full text Add to dashboard Cite

show abstract

“…It is inconvenient to administer eprosartan mesylate (735.8 mg of drug substance) or metformin hydrochloride (1000 mg of drug substance) due to their large size. There is a report that bioavailability of eprosartan, a poorly water-soluble drug, can be improved by dispersion technique [13,14]. It is noteworthy because improved bioavailability of the drug can lead to reduction of the necessary dose, which enables to reduce the weight and size of drug.…”

Section: Preliminary Excipient and Process Studymentioning

confidence: 99%

A Study of Fluid Bed Granulation of Pravastatin Tablet Using Design of Experiments

Kim

Pyo

2018

Asian J Pharm Clin Res

View full text Add to dashboard Cite

Objective: The objective of this study was to reduce size and weight of pravastatin tablet through quality by design approach; potential factors (spray rate, atomizing pressure, and inlet temperature) which could influence on the production process for critical process parameters of wet granulation using fluid-bed granulator were examined.Methods: The manufacturing process of the reduced weight and size formulation pravastatin tablet involves wet granulation, drying, granulate screening, blending, and tableting. Design of experiments study for wet granulation of the reduced weight/size pravastatin tablet was produced on 11 combinations of three factors (spray rate, atomizing pressure, and inlet temperature), which were chosen through initial risk assessment. The process of wet granulation was rated by measuring four responses: loss on drying (LOD) (%), bulk density (g/ml), product temperature (°C), and dissolution similarity (f2).Results: It was measured that LOD varied from 1.46 to 3.24%, bulk density from 0.34 to 0.51 g/ml, product temperature from 40.12 to 51.69°C, and dissolution (f2) of pravastatin from 52.14 to 58.91. Control strategy for wet granulation production of the reduced weight and size pravastatin tablet by our results demonstrated that the most optimized condition of three factors for wet granulation is spray rate (3–5 g/min), atomizing pressure (about 1 bar), and inlet temperature (65–90°C), respectively. Updated risk assessment and justification by all experimental data safely existed within the range of acceptance criteria were presented.Conclusion: It can be concluded that the ideal ranges of three factors (spray rate, atomizing pressure, and inlet temperature) in wet granulation were successfully identified.

show abstract

“…Eprosartan mesylate (EM, Figure 1(A) ) is considered a promising angiotensin II receptor antagonist (Ahad et al., 2018 ). EM is licensed for the management of hypertension in some more than 20 countries including the UK, Germany, and USA (Ahn et al., 2011 ).…”

Section: Introductionmentioning

confidence: 99%

Formulation and characterization of eprosartan mesylate and β-cyclodextrin inclusion complex prepared by microwave technology

et al. 2022

View full text Add to dashboard Cite

The goal of this work was to improve the aqueous solubility and dissolution rate of eprosartan mesylate by preparing inclusion complex of drug with β-cyclodextrin (β-CD) by microwave technique. In order to determine the solubility of eprosartan, phase solubility was determined and dissolution study was also conducted. Further, analytical techniques for instance, particle size distribution, differential scanning calorimetry, powder X-ray diffraction, scanning electron microscopy, Fourier-transform infrared spectroscopy, and nuclear magnetic resonance spectroscopy were used for the characterization of inclusion complex. In addition, the binding pattern of eprosartan with the β-CD was investigated by molecular modeling study. Phase solubility study revealed that approximately 4.48 folds improvement in the solubility of drug was noted with β-CD (10 mM). The estimated stability constant ( K c ) values for eprosartan:β-CD binary mixture was found to be 280.78 M –1 . The prepared inclusion complex of drug with β-CD presented better drug release profile (62.96 ± 2.01% in 1 h) as compared to their physical mixture (41.41 ± 1.77% in 1 h) or drug per se (29.97 ± 3.13%). The inclusion complex demonstrated different features and properties from pure drug, and we inferred that this could be due to the inclusion of drug into cyclodextrin cavity that confirmed by different analytical method. Molecular modeling study demonstrated a good affinity of eprosartan to entangle to β-CD. The outcomes have shown that guest molecule has many significant interactions with the host molecule. These observations are very interesting and may be a valuable approach to improve the solubility and in turn the bioavailability of eprosartan.

show abstract

Absorption Enhancer and Polymer (Vitamin E TPGS and PVP K29) by Solid Dispersion Improve Dissolution and Bioavailability of Eprosartan Mesylate

Cited by 9 publications

References 15 publications

The preparation and physicochemical characterization of eprosartan mesylate-laden polymeric ternary solid dispersions for enhanced solubility and dissolution rate of the drug

The preparation and physicochemical characterization of eprosartan mesylate-laden polymeric ternary solid dispersions for enhanced solubility and dissolution rate of the drug

A Study of Fluid Bed Granulation of Pravastatin Tablet Using Design of Experiments

Formulation and characterization of eprosartan mesylate and β-cyclodextrin inclusion complex prepared by microwave technology

Contact Info

Product

Resources

About