Liquid Chromatography Study on Atenolol--Cyclodextrin Inclusion Complex

Buha, Shailesh M; Baxi, Girin A.; Shrivastav, Pranav S.

doi:10.5402/2012/423572

Cited by 6 publications

(5 citation statements)

References 32 publications

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“…Based on the characterization of the crystallographic aspects, atenolol has sharp peaks with high intensity, meaning that pure atenolol has high crystallinity (Buha et al, 2012). Meanwhile, β-cyclodextrin has lower intensity than atenolol.…”

Section: Resultsmentioning

confidence: 99%

Formulation of orodispersible atenolol-β-cyclodextrin tablets with co-processed crospovidone-croscarmellose sodium and poloxamer 188

et al. 2019

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The use of conventional tablets in geriatric patients is currently limited because of a decrease in their physiological functions, such as tremor and difficulty of swallowing pills, which lowers their compliance with drug therapy. Hypertension, one of the degenerative diseases suffered by geriatric patients, is treatable with atenolol tablets or capsules that are less soluble in water or, in other words, has a poor dissolution. This research attempted to improve the dissolution of atenolol by formulating it into orodispersible tablets (ODTs), and as such, the disintegration time was modified by adding co-processed crospovidone-croscarmellose sodium in 1:1 ratio. Moreover, Poloxamer ® 188 was added to the formulation of atenolol-β-cyclodextrin inclusion complex. The post-compression test revealed that ODTs disintegrated quickly within 36.67±1.21 seconds (<60 seconds) and had physical characteristics that met the pharmaceutical requirements. The amount of atenolol dissolved within 30 minutes in the dissolution study was 84.39% (%Q 30 minutes ). The results of the accelerated stability study (at 40 °C and RH 75±5 %) for two weeks proved that the physical and chemical characteristics of the produced orodispersible atenolol tablets were stable. 284 The use of conventional tablets today raises problems in geriatric patients, especially who receive long-term therapy for degenerative diseases. Patients in this age group show changes in their physiological conditions that often lead to tremor, difficulty in chewing and swallowing, and proneness to choking (Dashora, 2013). An example of degenerative diseases is hypertension (Dipiro, 2008). Atenolol is a hypertension drug that is rather difficult to dissolve in water and has low dissolution. Dissolution is a process preceding the absorption of drug substances after which the drug can provide the desired pharmacological effect for a particular time (Qiu et al., 2009). Dissolution can be improved by modifying the physical features of the drug using specific materials to form molecular complexes (Shargel and Yu, 2017). An example of these materials is β-cyclodextrin. The outer part of β-cyclodextrin is hydrophilic, while the interior is hydrophobic (Vivek et al., 2012;Sinko, 2011). Previous research has proven how the formation of inclusion complexes can increase the dissolution of water-insoluble drugs, such as rosuvastatin. Rosuvastatin reacts to the addition of β-cyclodextrin, and in rosuvastatin-β-cyclodextrin inclusion complex, the crystallinity of this drug decreases (Akbari et al., 2011). Based on this result, the formation of atenolol-β-cyclodextrin inclusion complex is assumed to be able to increase the dissolution of atenolol.Another strategy to improve the dissolution of atenolol is by formulating orodispersible dosage forms. Orodispersible tablets break down or dissolve quickly in the mouth without water or chewing. U.S. Food and Drug Administration defines them as tablets that can disintegrate in the oral cavity in less than 60 seconds (FDA, 2008). One way to im...

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Section: Resultsmentioning

confidence: 99%

Formulation of orodispersible atenolol-β-cyclodextrin tablets with co-processed crospovidone-croscarmellose sodium and poloxamer 188

et al. 2019

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“…The enantioseparation of several drug racemates based on hostguest complex formation are discussed in the literature. [117][118][119] 2.3.2.7. Molecular complex formation.…”

Section: Racemic Drug Resolution (Covalent or Transient Diastereomer ...mentioning

confidence: 99%

Racemic drug resolution: a comprehensive guide

Mane

2016

Anal. Methods

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“…The solubility of atenolol in water (25 °C) is approximately 13.3 mg/ml [13,14]. Consequently, in order to increase the solubility and dissolution rate of atenolol, inclusion complex formation with cyclodextrin becomes imperative [15]. β-cyclodextrin as host molecules can interact with various drugs through the ability to entrap low solubility drugs in the hydrophobic cavity.…”

Section: Introductionmentioning

confidence: 99%

PREPARATION AND EVALUATION OF ATENOLOL-β-CYCLODEXTRIN ORALLY DISINTEGRATING TABLETS USING CO-PROCESS CROSPOVIDONE-SODIUM STARCH GLYCOLATE

et al. 2018

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Objective: The aim of this current research was to formulate and analyze the characteristics of atenolol-β-cyclodextrin which using co-process crospovidone-sodium starch glycolate as the disintegrants. Evaluation which has been conducted on orally disintegrating tablets consist of wetting time, water absorption ratio, in vitro dispersion time, and dissolution.Methods: Inclusion complex of atenolol-β-cyclodextrin which were prepared using solvent evaporation method, then formulated using co-processed crospovidone-sodium starch glycolate 1:1 (formula 1) and 1:2 (formula 2) into orally disintegrating tablets by direct compression technique. Orally disintegrating tablets of atenolol-β-cyclodextrin using a physical mixture of crospovidone-sodium starch glycolate 1:1 (formula 3), 1:2 (formula 4) was also prepared as a control. The prepared formulations (F1-F4) were evaluated by several parameters such as wetting time, water absorption ratio, in vitro dispersion time, and dissolution.Results: Orally disintegrating tablets of atenolol-β-cyclodextrin using co-processed crospovidone-sodium starch glycolate 1:1 (formula 1) showed shorter wetting time (53.53±2.26 seconds) and in vitro dispersion time (47.44±2.49 seconds) compare to the other formulas. Formula 1 also exhibited the highest dissolution efficiency compare to the formula which was used in the physical mixture. The results of this study also revealed that there was a high correlation between in vitro dispersion time and dissolution efficiency of atenolol-β-cyclodextrin orally disintegrating tablets.Conclusion: Orally disintegrating tablets of atenolol-β-cyclodextrin showed enhanced dissolution efficiency due to the presence of inclusion complex and co-processed crospovidone-sodium starch glycolate. Formula 1 was found to be the best formula in this study. This formula effectively reduces in vitro dispersion time, hence the dissolution efficiency became higher.

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Liquid Chromatography Study on Atenolol--Cyclodextrin Inclusion Complex

Cited by 6 publications

References 32 publications

Formulation of orodispersible atenolol-β-cyclodextrin tablets with co-processed crospovidone-croscarmellose sodium and poloxamer 188

Formulation of orodispersible atenolol-β-cyclodextrin tablets with co-processed crospovidone-croscarmellose sodium and poloxamer 188

Racemic drug resolution: a comprehensive guide

PREPARATION AND EVALUATION OF ATENOLOL-β-CYCLODEXTRIN ORALLY DISINTEGRATING TABLETS USING CO-PROCESS CROSPOVIDONE-SODIUM STARCH GLYCOLATE

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