scholarly journals Global testing of a consensus solubility assessment to enhance robustness of the WHO biopharmaceutical classification system

ADMET & DMPK ◽  
2020 ◽  
Author(s):  
Valeria Gigante ◽  
Giovanni M. Pauletti ◽  
Sabine Kopp ◽  
Minghze Xu ◽  
Isabel Gonzalez-Alvarez ◽  
...  
Keyword(s):  
Classification System ◽  
Global Network ◽  
Essential Medicines ◽  
Health Coverage ◽  
Pharmaceutical Ingredients ◽  
Fraction Absorbed ◽  
Practical Tool ◽  
Low Solubility ◽  
Biopharmaceutical Classification System

The WHO Biopharmaceutical Classification System (BCS) is a practical tool to identify active pharmaceutical ingredients (APIs) that scientifically qualify for a waiver of in vivo bioequivalence studies. The focus of this study was to engage a global network of laboratories to experimentally quantify the pH-dependent solubility of the highest therapeutic dose of 16 APIs using a harmonized protocol. Intra-laboratory variability was ≤5 %, and no apparent association of inter-laboratory variability with API solubility was discovered. Final classification “low solubility” vs “high solubility” was consistent among laboratories. In comparison to the literature-based provisional 2006 WHO BCS classification, three compounds were re-classified from “high” to “low-solubility”. To estimate the consequences of these experimental solubility results on BCS classification, dose-adjusted in silico predictions of the fraction absorbed in humans were performed using GastroPlus®. Further expansion of these experimental efforts to qualified APIs from the WHO Essential Medicines List is anticipated to empower regulatory authorities across the globe to issue scientifically-supported guidance regarding the necessity of performing in vivo bioequivalence studies. Ultimately, this will improve access to affordable generic products, which is a critical prerequisite to reach Universal Health Coverage.  

scholarly journals Profil Laju Disolusi Kokristal Simvastatin Menggunakan Koformer Aspartam, Nikotinamid, dan Sakarin

2020 ◽  
Vol 4 ◽  
Author(s):  
Dolih Gozali ◽  
Popy Sarah Chairunnisa ◽  
Iyan Sopyan
Keyword(s):  
Classification System ◽  
Biopharmaceutical Classification System

Simvastatin merupakan obat golongan HMG-CoA reduktase inhibitor yang banyak diberikan pada pasien sebagai obat antikolesterol. Kelarutannya yang rendah dalam air dan permeabilitas yang tinggi menyebabkan rendahnya bioavaibilitas sehingga simvastatin tergolong kedalam obat kelas II berdasarkan Biopharmaceutical Classification System (BCS). Skrining penggunaan koformer pada pembentukan kokristal simvastatin dengan 12 koformer menunjukkan pengaruh signifikan pada peningkatan kelarutan dan uji disolusi. Kokristal yang memiliki profil kelarutan dan disolusi terbaik adalah kokristal simvastatin:aspartam (KKA), simvastatin:nikotinamid (KKN), dan simvastatin:sakarin (KKS). Salah satu instrumen spesifik yang dapat digunakan untuk karakterisasi fase padat suatu obat yang telah dimodifikasi adalah evaluasi disolusi. Kokristal KKA, KKN, KKS diuji lanjut dengan disolusi intrinsik dan disolusi-absorpsi in vitro. Metode Disolusi-Absorpsi in vitro dilakukan untuk melihat laju penyerapan obat dan sebagai langkah awal pendekatan uji bioavaibilitas secara in vivo. Kokristal KKN dan KKS secara signifikan meningkatkan laju disolusi intrinsik simvastatin sebanyak 9 dan 21 kalinya. Laju disolusi-absorpsi in vitro simvastatin secara signifikan meningkat pada KKS hingga 9 kali zat murninya.

FORMULATION AND EVALUATION OF LIPID BASED SELF EMULSIFYING DRUG DELIVERY SYSTEM OF GLIMEPIRIDE

INDIAN DRUGS ◽  
2013 ◽  
Vol 50 (11) ◽  
pp. 48-51
Author(s):  
K Sneha Latha ◽  
◽  
G. B Kiran Kumar ◽  
G. A Mohammed ◽  
S.K Chowdary ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Oleic Acid ◽  
Drug Release ◽  
Dissolution Rate ◽  
Drug Delivery System ◽  
Delivery System ◽  
Classification System ◽  
Tween 80 ◽  
Low Solubility ◽  
Biopharmaceutical Classification System

Aim of the present investigation was to develop lipid based self-emulsifying drug delivery system (SEDDS) to improve bioavailability of glimepiride. Glimepiride is a class II molecule according to BCS (Biopharmaceutical Classification System), having low solubility. Optimized self-emulsifying drug delivery system of glimepiride comprising oil (oleic acid), surfactant (Tween 80®) and co-surfactant (PEG 200®) was prepared. Optimized SEDDS of glimepiride showed increase in dissolution rate. It was concluded that the formulation was found to be showing significant improvement in terms of the drug release with complete release of drug within 18 minutes. Thus, self-emulsifying formulation of glimepiride was successfully developed.

In vitro -in vivo correlation and biopharmaceutical classification system

2011 ◽  
Vol 2 (3) ◽  
pp. 126
Author(s):  
G Tiwari ◽  
B Srivastawa ◽  
S Pandey ◽  
R Tiwari ◽  
AK Rai ◽  
...  
Keyword(s):  
Classification System ◽  
Biopharmaceutical Classification System

PLANT BASED BIOAVAILABILITY ENHANCERS

2022 ◽  
Vol 28 ◽  
Author(s):  
Sweta Patel ◽  
Shruti Chopra ◽  
Simran Chaurasia ◽  
Maryam Sarwat
Keyword(s):  
Systemic Circulation ◽  
Drug Dose ◽  
Main Concern ◽  
Permeation Enhancers ◽  
Anti Cancer ◽  
Site Of Action ◽  
Low Solubility ◽  
Biopharmaceutical Classification System

Abstract: Many of the synthetic as well as herbal drugs despite of their notable in vitro finding demonstrate insignificant in vivo activity majority of times due to poor bioavailability. As per Biopharmaceutical Classification System (BCS) one of the main concern is low solubility and/or permeation of drugs resulting in reduced absorption and poor bioavailability. To overcome these issues the various strategies have been adopted including use of permeation enhancers which are also known as bioenhancers. Bioenhancers are synthetic or natural compounds that increases the bioavailability of drugs and nutrients such as vitamins, amino acids, minerals, etc. into the systemic circulation and at the site of action for exhibiting improved therapeutic action. By improving bioavailability, bioenhancers can lead to reduction in drug dose, decrease in the treatment period and can circumvent the problem of drug resistance. Numerous studies have reported application of synthetic bioenhancers. On the other hand, owing to the natural origin, plant based bioenhancer can serve as better alternative. Literature review have revealed that the plant-based bioenhancers have been used in with a wide varieties of drugs including antibiotics, antiviral and anti-cancer. These can be categorized based on their sources and the mechanism of activity. This review will provide a systematic and detailed overview of the various plant based bioenhancers and applications.

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 Implementing Cancer Care in Rwanda: Capacity Building for Treatment and Scale-Up

2021 ◽  
Vol 13 (13) ◽  
pp. 7216
Author(s):  
Paul H. Park ◽  
Cyprien Shyirambere ◽  
Fred Kateera ◽  
Neil Gupta ◽  
Christian Rusangwa ◽  
...  
Keyword(s):  
Capacity Building ◽  
Scale Up ◽  
Implementation Strategies ◽  
Sub Saharan Africa ◽  
Essential Medicines ◽  
Cancer Center ◽  
Health Coverage ◽  
Cancer Centers ◽  
Implementation Approach ◽  
Single Cancer

Background: The majority of countries in sub-Saharan Africa are ill-prepared to address the rising burden of cancer. While some have been able to establish a single cancer referral center, few have been able to scale-up services nationally towards universal health coverage. The literature lacks a step-wise implementation approach for resource-limited countries to move beyond a single-facility implementation strategy and implement a national cancer strategy to expand effective coverage. Methods: We applied an implementation science framework, which describes a four-phase approach: Exploration, Preparation, Implementation, and Sustainment (EPIS). Through this framework, we describe Rwanda’s approach to establish not just a single cancer center, but a national cancer program. Results: By applying EPIS to Rwanda’s implementation approach, we analyzed and identified the implementation strategies and factors, which informed processes of each phase to establish foundational cancer delivery components, including trained staff, diagnostic technology, essential medicines, and medical informatics. These cancer delivery components allowed for the implementation of Rwanda’s first cancer center, while simultaneously serving as the nidus for capacity building of foundational components for future cancer centers. Conclusion: This “progressive scaling” approach ensured that initial investments in the country’s first cancer center was a step toward establishing future cancer centers in the country.

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