Using fluid bed granulation to improve the dissolution of poorly water-soluble drugs

Takahashi, Andrea Ikeda; Lourenço, Felipe Rebello; Duque, Marcelo Dutra; Consiglieri, Vladi Olga; Ferraz, Humberto Gomes

doi:10.1590/s1516-89132012000300020

Cited by 6 publications

(4 citation statements)

References 13 publications

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“…Perhaps, this could also be explained by the dissolution efficiency of the formulated diosmin due to the granulation process of using the fluid bed. This is consistent with results of Takahashi et al [ 17 ] indicating the dissolution rate of nimodipine and spironolactone tablets improved after bed fluid granulation.…”

Section: Discussionsupporting

confidence: 93%

Comparative Bioavailability of Two Diosmin Formulations after Oral Administration to Healthy Volunteers

Russo¹,

Divya²,

Tommasi

2018

Molecules

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Diosmin is a flavonoid commonly found in citrus fruits, largely used as adjuvant treatment for circulatory disorders, including chronic venous insufficiency (CVI) and hemorrhoids. Following oral administration, diosmin is not directly absorbed but must first be hydrolyzed into its aglycone, diosmetin, which is then absorbed into the systemic circulation. The aim of the current cross-over clinical study was to assess the pharmacokinetic profile of µSmin® Plus, a micronized diosmin flavonoid complex standardized in diosmin and formulated with a buffering agent (tested formulation). The study compared this to unformulated micronized diosmin (reference), in 16 healthy volunteers. Plasma samples were analyzed by HPLC-MS and plasma diosmetin concentration was measured after deconjugation with β-glucuronidase. For the tested formulation area under the curve (AUC0-t), and maximum plasma and time concentration (Cmax; tmax) were found to be 298.4 ± 163.7, 50.3 ± 22.6 and 2.2 ± 2.9, respectively. AUC0-t and Cmax of the reference were 31.9 ± 100.4 and 2.4 ± 1.9, respectively. The tested formulation showed higher plasmatic concentrations of diosmetin in comparison to those obtained after the administration of unformulated micronized diosmin. The relative bioavailability was 9.4 greater for the tested formulation than in micronized diosmin. In conclusion, our data indicate that µSmin® Plus was rapidly and well absorbed into systemic circulation and may therefore be ideally suitable to deliver diosmin in human interventional trials.

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Section: Discussionsupporting

confidence: 93%

Comparative Bioavailability of Two Diosmin Formulations after Oral Administration to Healthy Volunteers

Russo¹,

Divya²,

Tommasi

2018

Molecules

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“…A peristaltic pump was switched off once the desired quantity of polymeric dispersion was applied, and the fluidization rate was reduced to allow particles to dry until the desired moisture level was achieved 26 . As a part of the granulation process, the bed temperature and pressure differential were also recorded 27 .…”

Section: Preparation Of Taste Masked Lcdh Granulesmentioning

confidence: 99%

Untitled

2022

IJPSR

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The goal of this study was to develop taste-masked orally disintegrating tablets of the bitter-tasting levocetirizine dihydrochloride (LCDH) to improve the accessibility and adherence of pediatric, elderly, non-cooperative and paraplegic patients. Methods: In the present study, orally disintegrating Levocetirizine dihydrochloride tablets were formulated by direct compression. Taste masking was achieved using a pH-independent polymeric dispersion of Surelease E-7-19040 in combination with Opadry YS-1-19025-A in different ratios. In-vivo taste evaluation was done to see if the tablets produced utilizing the direct compression approach were successfully disguised. Results: The present study investigated uncoated and coated drug substances and prepared tablets of coated LCDH for flow as well as compression behaviour, Fourier Transform Infrared absorption spectra, Differential scanning calorimetry, powder X-ray diffraction, scanning electron microscopy and in-vitro dissolution and disintegration properties. Conclusion: Using a combination of two polymeric dispersions "Sure lease E-1-19040" and "Opadry" coating for the delivery of LCDH, it was shown that a taste-masking evaluation could be performed to identify effective polymer-carriers for the LCDH. INTRODUCTION:Taste is one of the important quality attributes that govern the palatability of the formulation and, in turn acceptability by the patient. The bitter taste is one of the foremost challenges that formulators encounter while working with bitter-taste drug molecules.

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“…The granulation procedure of the extracted material can boost solubility while masking the extract's disagreeable flavor (8,9). The use of appropriate polymers facilitates this.…”

Section: Introductionmentioning

confidence: 99%

Instant Granules of Mangosteen Peel (Garcinia Mangostana L.) Ethanol Extract as Antioxidants

Fadhila

Sriwidodo

Chaerunisaa

2022

sciphar

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Free radicals in the air can trigger dangerous diseases, such as cancer and premature aging. To avoid this, antioxidant compounds are needed to donate electrons to free radicals, causing them to become more stable. A powerful antioxidant can be found in nature, including the mangosteen peel. This study aimed to find the best instant granule preparation formula from mangosteen peel extract (MPE) that can be practically consumed and the antioxidant stability during preparation. The wet granulation method was used to make instant granules, which have four formulas with varying amounts of xanthan gum as a suspending agent and maltodextrin as a solubility enhancer. The antioxidant activity was examined using the DPPH method. Based on the findings, formula 4 had the best properties with a drying shrinkage of 1.80%, a flow rate of 11.54 ± 1.56 g/s, repose's angle of 29.112 ± 0.45ᵒ, carr index of 14.043 ± 1.9%, and dispersion rate of 0.164 g/s. There is no residue in the solution. The shape and taste of this formula were most acceptable. The antioxidant activity of the extract and instant granules was not significantly different, with the IC50 of 34.64 μg/ml and 44.12 μg/ml, respectively. Based on the test result, it can be concluded that formula 4 with a concentration of xanthan gum 1% and 20% maltodextrin is a potent antioxidant supplement.

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Using fluid bed granulation to improve the dissolution of poorly water-soluble drugs

Cited by 6 publications

References 13 publications

Comparative Bioavailability of Two Diosmin Formulations after Oral Administration to Healthy Volunteers

Comparative Bioavailability of Two Diosmin Formulations after Oral Administration to Healthy Volunteers

Untitled

Instant Granules of Mangosteen Peel (Garcinia Mangostana L.) Ethanol Extract as Antioxidants

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