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

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.

scholarly journals ICH Guideline for Biopharmaceutics Classification System-Based Biowaiver (M9): Toward Harmonization in Latin American Countries

Pharmaceutics ◽  
2021 ◽  
Vol 13 (3) ◽  
pp. 363
Author(s):  
Claudia Miranda ◽  
Alexis Aceituno ◽  
Mirna Fernández ◽  
Gustavo Mendes ◽  
Yanina Rodríguez ◽  
...  
Keyword(s):  
Latin American ◽  
Classification System ◽  
Biopharmaceutics Classification System ◽  
In Vitro Dissolution ◽  
Ich Guidelines ◽  
Latin American Region ◽  
Regulatory Guidelines ◽  
Biopharmaceutics Classification

The biopharmaceutical classification system (BCS) is a very important tool to replace the traditional in vivo bioequivalence studies with in vitro dissolution assays during multisource product development. This paper compares the most recent harmonized guideline for biowaivers based on the biopharmaceutics classification system and the BCS regulatory guidelines in Latin America and analyzes the current BCS regulatory requirements and the perspective of the harmonization in the region to develop safe and effective multisource products. Differences and similarities between the official and publicly available BCS guidelines of several Latin American regulatory authorities and the new ICH harmonization guideline were identified and compared. Only Chile, Brazil, Colombia, and Argentina have a more comprehensive BCS guideline, which includes solubility, permeability, and dissolution requirements. Although their regulatory documents have many similarities with the ICH guidelines, there are still major differences in their interpretation and application. This situation is an obstacle to the successful development of safe and effective multisource products in the Latin American region, not only to improve their access to patients at a reasonable cost, but also to develop BCS biowaiver studies that fulfill the quality standards of regulators in developed and emerging markets.

scholarly journals Caco-2 Cells, Biopharmaceutics Classification System (BCS) and Biowaiter

2011 ◽  
Vol 54 (1) ◽  
pp. 3-8 ◽  
Author(s):  
Libuše Smetanová ◽  
Věra Štětinová ◽  
Zbyněk Svoboda ◽  
Jaroslav Květina
Keyword(s):  
Drug Absorption ◽  
Classification System ◽  
Drug Transport ◽  
Biopharmaceutics Classification System ◽  
Phenol Red ◽  
Basolateral Side ◽  
Free Transport ◽  
Biopharmaceutics Classification

Almost all orally administered drugs are absorbed across the intestinal mucosa. The Caco-2 monolayers are used as an in vitro model to predict drug absorption in humans and to explore mechanism of drug absorption. The Caco-2 cells are derived from a human colon adenocarcinoma and spontaneously differentiate to form confluent monolayer of polarized cells structurally and functionally resembling the small intestinal epithelium. For studying drug permeability, Caco-2 cells are seeded onto the Transwell inserts with semipermeable membrane and grown to late confluence (21 days). After determination of cell viability, the integrity of monolayer is checked by phenol red permeability and by 14C-mannitol permeability. The transport from apical to basolateral (AP-BL) and basolateral to apical (BL-AP) is studied by adding the diluted drug on the apical or basolateral side and withdrawing the samples from the opposite compartment, respectively, for HPLC analysis or liquid scintillation spectrometry. Ca2+- free transport medium is used to determine paracellular component of the drug transport. On the basis of permeability and solubility, drugs can be categorized into four classes of Biopharmaceutics Classification System (BCS). For certain drugs, the BCS-based biowaiver approach can be used which enables to reduce in vivo bioequivalence studies.

scholarly journals Overview on Biopharmaceutics Classification System (BCS) based biowaiver requirements in African countries

2021 ◽  
Vol 9 (2) ◽  
pp. 26-29
Author(s):  
Nidhi Sagar ◽  
Iva Dhulia ◽  
Himani Patel ◽  
Umesh Dobariya ◽  
Sandip Sarvaiya
Keyword(s):  
Classification System ◽  
Aqueous Solubility ◽  
Pharmaceutical Product ◽  
Biopharmaceutics Classification System ◽  
In Vivo Studies ◽  
Pharmacokinetic Studies ◽  
African Countries ◽  
Biopharmaceutics Classification

Biopharmaceutics Classification System (BCS)-based biowaiver are meant to reduce the need for establishing in vivo bioequivalence in situations where in vitro data may be considered to provide a reasonable estimate of the relative in vivo performance of two products. The BCS is a scientific approach designed to predict medicinal absorption based on the aqueous solubility and intestinal absorptive characteristics of the Pharmaceutical product. To ensure interchangeability, the multisource product must be therapeutically equivalent to the comparator product. Types of in vivo equivalence studies include comparative pharmacokinetic studies, comparative pharmacodynamic studies and comparative clinical studies. This article briefly explains the BCS based biowaiver requirements in six major African countries i.e. Zimbabwe, South Africa, Uganda, Kenya, Botswana and Tanzania which facilitates regulatory medicine approval process when the dossier (application) is approved based on evidence of equivalence other than In vivo studies.

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.

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