Development and Evaluation of Mucoadhesive Tablets of Atenolol and It’s Β-Cyclodextrin Complex

Gite, Sandip

doi:10.15272/ajbps.v4i37.595

Cited by 5 publications

(11 citation statements)

References 8 publications

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“…The transmittance peak at 3178.11 cm -1 does not appear in the infrared spectrum of the inclusion complex. These results suggest that an interaction between the functional groups of the drug molecules and the groups located in the βcyclodextrin cavity has occurred through hydrogen bonding (Gite, 2014). In the atenolol inclusion complex, the new peak at 3724.87 cm -1 replaces the old peak of pure atenolol, i.e., at 1613.16 cm -1 .…”

Section: Resultsmentioning

confidence: 85%

“…In the atenolol inclusion complex, the new peak at 3724.87 cm -1 replaces the old peak of pure atenolol, i.e., at 1613.16 cm -1 . This condition suggests the loss of the -CO-NHgroup in the inclusion complex (Gite, 2014).…”

Section: Resultsmentioning

confidence: 96%

“…Thermal characterization was carried out in a Differential Scanning Calorimeter (DSC) (Mettler Toledo). The samples of atenolol, β-cyclodextrin, and atenolol-β-cyclodextrin inclusion complex weighing ±4 mg were heated at a scanning rate of 10°C/minute from 40°C to 200°C and flowed with nitrogen at a rate of 40 ml/minute (Gite, 2014).…”

Section: Introduction Thermal Characterization With Differential Scanmentioning

confidence: 99%

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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: 85%

Section: Resultsmentioning

confidence: 96%

Section: Introduction Thermal Characterization With Differential Scanmentioning

confidence: 99%

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

et al. 2019

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“…Bahan [8]. Setelah terbentuk, dikarakterisasi dengan analisis termal dengan DSC, analisis aspek kristalografi dengan XRD, analisis morfologi permukaan dengan SEM, penetapan kadar atenolol pada kompleks inklusi atenolol-β-siklodekstrin, dan uji disolusi.…”

Section: Bahanunclassified

“…Penurunan intensitas puncak atenolol dapat teramati pada kompleks inklusi atenolol-β-siklodekstrin. Kondisi ini mengindikasikan terjadinya perubahan kisi-kisi kristal atenolol setelah terbentuk kompleks inklusi [8].…”

Section: Karakterisasi Kompleks Inklusi Atenolol-β-unclassified

Pengaruh Co-Process Superdisintegran Crospovidone- Croscarmellose Sodium (1:3) pada Sediaan Orally Disintegrating Tablet Atenolol-β-Siklodekstrin

Parfati

Rani

Saputra

2018

MPI

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ABSTRAK:Orally Disintegrating Tablet (ODT) merupakan bentuk sediaan yang dikembangkan untuk mempercepat waktu hancur, meningkatkan kepatuhan pasien dan efek terapi obat. ODT dirancang memiliki sifat mudah hancur pada rongga mulut kurang dari 1 menit, sehingga geriatri tidak memerlukan tambahan air untuk membantu menelan dan cocok untuk penderita geriatri. Pada penelitian ini dilakukan formulasi sediaan ODT dengan pembentukan kompleks inklusi atenolol-β-siklodekstrin dengan penambahan superdisintegran co-process crospovidone-croscarmellose sodium (1:3) menggunakan metode cetak langsung. Evaluasi pembuatan ODT terdiri dari uji pre-kompresi dan postkompresi. Hasil pembuatan ODT atenolol-β-siklodekstrin juga diuji statistik dari segi waktu pembasahan, rasio penyerapan air, waktu hancur, waktu dispersi in vitro, dan parameter disolusi (AUC, %ED, dan Kr). Penambahan co-process superdisintegran menunjukkan waktu pembasahan 44,45 ± 2,76 detik; rasio penyerapan air 26,27 ± 1,1%; waktu hancur 38,07 ± 4,56 detik; dan waktu dispersi in vitro 73,83 ± 2,71 detik. Hasil Uji disolusi didapatkan nilai AUC 3983,40 ± 189,60; ED 66,39 ± 3,16%; dan Kr 0,0778 ± 0,04. Campuran fisik menunjukkan waktu pembasahan 44,87 ± 3,33 detik; rasio penyerapan air 27,76 ± 1,35%; waktu hancur 38,28 ± 5,32 detik; dan waktu dispersi in vitro 83,20 ± 2,67 detik. Hasil uji disolusi didapatkan nilai AUC 3916,20 ± 235,80; ED 65,27 ± 3,93%; dan Kr 0,0655 ± 0,03. Berdasarkan hasil penelitian yang diperoleh, dapat dilihat bahwa penambahan superdisintegran co-process menunjukkan hasil yang tidak berbeda bermakna dengan campuran fisik.Kata kunci: atenolol; β-siklodekstrin; orally disintegrating tablet; co-process; crospovidone-croscarmellose sodium revealed AUC 3983.40 ± 189.60; ED 66.39 ± 3.16%; and Cr 0.0778 ± 0.04 ABSTRACT: Orally Disintegrating Tablet (ODT) is a dosage form that was developed to improve the quality of therapy and patient's compliance. Orally disintegrating tablet can disintegrate easily in the oral cavity in less than 1 minute, so it does not require water to help swallow. In this research, ODT was formulated using inclusion complexes of atenolol-β-cyclodextrin and the addition of co-process superdisintegrant crospovidone-croscarmellose sodium (1:3). The tablet was prepared by direct compression method. The evaluation of ODT consists of pre-compression and post-compression tests. The results also were tested statistically in terms of wetting time, water absorption ratio, disintegration time, in vitro dispersion time and dissolution parameters (AUC, %ED, and Cr

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Rani¹,

Parfati²,

stephanie³

2020

IJPSR

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Atenolol is a hypertension drug that has a low solubility characteristic in water and gastric fluid. The rate of absorption of the drug with poor solubility characteristics is determined by the dissolution process. In this study, an attempt has been conducted to increase the dissolution of atenolol by increasing its solubility. The solubility of atenolol has been enhanced by the inclusion complex using βcyclodextrin made by several methods (physical mixing, kneading, and solvent evaporation). Evaluation and characterization of atenolol-βcyclodextrin inclusion complex consist of drug content, dissolution test, Fourier Transformed Infrared analysis (FT-IR), Differential Scanning Calorimetry (DSC), X-ray Diffraction (XRD) and Scanning Electron Microscope (SEM). The results of the drug content analysis, dissolution test, and characterization showed that atenolol-β-cyclodextrin inclusion complex, which has been made by the solvent evaporation method was the best approach. Therefore, a solvent evaporation method was chosen to formulate orally disintegrating tablets of atenolol-β-cyclodextrin using direct compression technique. Orally disintegrating tablets of atenolol-βcyclodextrin were prepared using crospovidone as disintegrant. The results of pre-compression test and the post-compression test revealed that orally disintegrating tablets of atenolol-β-cyclodextrin inclusion complex disintegrate within 8.17 ± 0.41 sec. In-vitro dispersion time in simulated saliva was found to be 45.33 ± 0.58 sec and the percentage of atenolol dissolved from this formula was 92.22% in 30 min. Hence, this formula shows good physicochemical characteristics and fulfill pharmaceutical quality requirements of orally disintegrating tablet.

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Development and Evaluation of Mucoadhesive Tablets of Atenolol and It’s Β-Cyclodextrin Complex

Cited by 5 publications

References 8 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

Pengaruh Co-Process Superdisintegran Crospovidone- Croscarmellose Sodium (1:3) pada Sediaan Orally Disintegrating Tablet Atenolol-β-Siklodekstrin

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