scholarly journals An Overview on Dietary Polyphenols and Their Biopharmaceutical Classification System (BCS)

2021 ◽  
Vol 22 (11) ◽  
pp. 5514
Author(s):  
Francesca Truzzi ◽  
Camilla Tibaldi ◽  
Yanxin Zhang ◽  
Giovanni Dinelli ◽  
Eros D′Amen
Keyword(s):  
Phenolic Compounds ◽  
Human Body ◽  
Classification System ◽  
Oral Absorption ◽  
Bioactive Constituents ◽  
Dietary Polyphenols ◽  
Digestion Process ◽  
Natural Organic Compounds ◽  
Daily Diet ◽  
Biopharmaceutical Classification System

Polyphenols are natural organic compounds produced by plants, acting as antioxidants by reacting with ROS. These compounds are widely consumed in daily diet and many studies report several benefits to human health thanks to their bioavailability in humans. However, the digestion process of phenolic compounds is still not completely clear. Moreover, bioavailability is dependent on the metabolic phase of these compounds. The LogP value can be managed as a simplified measure of the lipophilicity of a substance ingested within the human body, which affects resultant absorption. The biopharmaceutical classification system (BCS), a method used to classify drugs intended for gastrointestinal absorption, correlates the solubility and permeability of the drug with both the rate and extent of oral absorption. BCS may be helpful to measure the bioactive constituents of foods, such as polyphenols, in order to understand their nutraceutical potential. There are many literature studies that focus on permeability, absorption, and bioavailability of polyphenols and their resultant metabolic byproducts, but there is still confusion about their respective LogP values and BCS classification. This review will provide an overview of the information regarding 10 dietarypolyphenols (ferulic acid, chlorogenic acid, rutin, quercetin, apigenin, cirsimaritin, daidzein, resveratrol, ellagic acid, and curcumin) and their association with the BCS classification.

scholarly journals Investigation of biopharmaceutical drug properties suitable for orally disintegrating tablets

ADMET & DMPK ◽  
2016 ◽  
Vol 4 (4) ◽  
pp. 335 ◽  
Author(s):  
Asami Ono ◽  
Takumi Tomono ◽  
Takuo Ogihara ◽  
Katsuhide Terada ◽  
Kiyohiko Sugano
Keyword(s):  
Classification System ◽  
Immediate Release ◽  
Basic Drugs ◽  
Font Size ◽  
Net Charge ◽  
Solubility In Water ◽  
Orally Disintegrating Tablets ◽  
Significant Difference ◽  
Dose Number ◽  
Biopharmaceutical Classification System

<span style="color: black; font-family: 'Calibri','sans-serif'; font-size: 10pt; mso-fareast-font-family: 'Times New Roman'; mso-bidi-font-family: 'Times New Roman'; mso-ansi-language: EN-GB; mso-fareast-language: DE; mso-bidi-language: AR-SA;" lang="EN-GB">The purpose of this study was to evaluate the biopharmaceutical drug properties suitable for orally disintegrating tablets (ODTs). The net charge at pH 7.4, log D<sub>6.5</sub>, the highest dose strength, solubility in water, dose number, and elimination t<sub>1/2</sub> of 57 ODT drugs and 113 drugs of immediate-release (IR) formulations were compared. These drugs were classified according to the Biopharmaceutical Classification System (BCS). A lower dose strength and a longer elimination t<sub>1/2</sub> have been observed as characteristic properties of ODTs. The proportion of basic drugs was higher in the ODTs than in the IR. A significant difference was not observed between the ODT and the IR formulation for log D<sub>6.5</sub>, solubility in water, and dose number. The distributions of the ODT and IR formulations among each BCS class were similar, suggesting that an ODT can be developed regardless of the BCS class of a drug</span>.

scholarly journals Anti-aggregation Effects of Phenolic Compounds on α-synuclein

Molecules ◽  
2020 ◽  
Vol 25 (10) ◽  
pp. 2444
Author(s):  
Kenjiro Ono ◽  
Mayumi Tsuji ◽  
Tritia R. Yamasaki ◽  
Giulio M. Pasinetti
Keyword(s):  
Phenolic Compounds ◽  
Gut Microbiota ◽  
Lewy Bodies ◽  
Hydroxybenzoic Acid ◽  
Dietary Polyphenols ◽  
Pathologic Features ◽  
Hydroxyphenylacetic Acid ◽  
A Cell ◽  
The Brain

The aggregation and deposition of α-synuclein (αS) are major pathologic features of Parkinson’s disease, dementia with Lewy bodies, and other α-synucleinopathies. The propagation of αS pathology in the brain plays a key role in the onset and progression of clinical phenotypes. Thus, there is increasing interest in developing strategies that attenuate αS aggregation and propagation. Based on cumulative evidence that αS oligomers are neurotoxic and critical species in the pathogenesis of α-synucleinopathies, we and other groups reported that phenolic compounds inhibit αS aggregation including oligomerization, thereby ameliorating αS oligomer-induced cellular and synaptic toxicities. Heterogeneity in gut microbiota may influence the efficacy of dietary polyphenol metabolism. Our recent studies on the brain-penetrating polyphenolic acids 3-hydroxybenzoic acid (3-HBA), 3,4-dihydroxybenzoic acid (3,4-diHBA), and 3-hydroxyphenylacetic acid (3-HPPA), which are derived from gut microbiota-based metabolism of dietary polyphenols, demonstrated an in vitro ability to inhibit αS oligomerization and mediate aggregated αS-induced neurotoxicity. Additionally, 3-HPPA, 3,4-diHBA, 3-HBA, and 4-hydroxybenzoic acid significantly attenuated intracellular αS seeding aggregation in a cell-based system. This review focuses on recent research developments regarding neuroprotective properties, especially anti-αS aggregation effects, of phenolic compounds and their metabolites by the gut microbiome, including our findings in the pathogenesis of α-synucleinopathies.

Formulation and evaluation of liquisolid compacts of itraconazole to enhance its oral bioavailability

2020 ◽  
Vol 11 (2) ◽  
pp. 83-96
Author(s):  
Hetal P Thakkar ◽  
Deepika Vasava ◽  
Arpita A Patel ◽  
Rahul D Dhande
Keyword(s):  
Antifungal Activity ◽  
Classification System ◽  
Oral Bioavailability ◽  
Room Temperature ◽  
Coating Material ◽  
Drug Dissolution ◽  
Dry Powder ◽  
Liquisolid Compacts ◽  
Biopharmaceutical Classification System ◽  
Peg 600

Aim: Formulate and evaluate liquisolid compacts of Itraconazole, a biopharmaceutical classification system class II drug, which has poor bioavailability. Materials & methods: PEG 600 was used as a nonvolatile solvent, Alfacel PH 200 as a carrier and Aerosil 200 as a coating material. The Itraconazole solution upon mixing with a carrier and coating material resulted in a dry powder, which was compressed into tablets. Results & conclusion: The optimized formulation exhibited a significantly higher drug dissolution (90.73% in 90 min) compared with conventional tablets and marketed capsules. The antifungal activity was retained in the formulation. Higher values of Cmax and AUC0-24 of the formulation compared with the plain drug indicated enhancement in oral bioavailability. The formulation was stable at room temperature as well as in accelerated conditions.

scholarly journals Evolution of Choice of Solubility and Dissolution Media After Two Decades of Biopharmaceutical Classification System

2017 ◽  
Vol 19 (4) ◽  
pp. 989-1001 ◽  
Author(s):  
Nadia Bou-Chacra ◽  
Katherine Jasmine Curo Melo ◽  
Ivan Andrés Cordova Morales ◽  
Erika S. Stippler ◽  
Filippos Kesisoglou ◽  
...  
Keyword(s):  
Classification System ◽  
Biopharmaceutical Classification System
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