Biowaiver extension potential and IVIVC for BCS Class II drugs by formulation design: Case study for cyclosporine self-microemulsifying formulation.
Summary of "Biowaiver extension potential and IVIVC for BCS Class II drugs by formulation design: Case study for cyclosporine self-microemulsifying formulation."
The objective of this work was to suggest the biowaiver potential of biopharmaceutical classification system (BCS) Class II drugs in self-microemulsifying drug delivery systems (SMEDDS) which are known to increase the solubility, dissolution and oral absorption of water-insoluble drugs. Cyclosporine was selected as a representative BCS Class II drug. New generic candidate of cyclosporine SMEDDS (test) was applied for the study with brand SMEDDS (reference I) and cyclosporine self-emulsifying drug delivery systems (SEDDS, reference II). Solubility and dissolution of cyclosporine from SMEDDS were critically enhanced, which were the similar behaviors with BCS class I drug. The test showed the identical dissolution rate and the equivalent bioavailability (0.34, 0.42 and 0.68 of p values for AUC(0→24h), C(max) and T(max), respectively) with the reference I. Based on the results, level A in vitro-in vivo correlation (IVIVC) was established from these two SMEDDS formulations. This study serves as a good example for speculating the biowaiver extension potential of BCS Class II drugs specifically in solubilizing formulation such as SMEDDS.
Utah-Inha DDS and Advanced Therapeutics, Incheon, 406-840, Korea, Sugeun.Yang@Inha.ac.kr.
This article was published in the following journal.
Name: Archives of pharmacal research
- PubMed Source: http://www.ncbi.nlm.nih.gov/pubmed/21116787
- DOI: http://dx.doi.org/10.1007/s12272-010-1116-2
Medical and Biotech [MESH] Definitions
A field of biological research combining engineering in the formulation, design, and building (synthesis) of novel biological structures, functions, and systems.
The molecular designing of drugs for specific purposes (such as DNA-binding, enzyme inhibition, anti-cancer efficacy, etc.) based on knowledge of molecular properties such as activity of functional groups, molecular geometry, and electronic structure, and also on information cataloged on analogous molecules. Drug design is generally computer-assisted molecular modeling and does not include pharmacokinetics, dosage analysis, or drug administration analysis.
Authoritative works containing lists of drugs and preparations, their description, formulation, analytic composition, main chemical properties, standards for strength, purity, and dosage, chemical tests for determining identity, etc. They have the status of a standard.
The use of computers for designing and/or manufacturing of anything, including drugs, surgical procedures, orthotics, and prosthetics.
Drugs intended for human or veterinary use, presented in their finished dosage form. Included here are materials used in the preparation and/or formulation of the finished dosage form.
The Biopharmaceutics Classification system (BCS) classifies drug substances based on aqueous solubility and intestinal permeability. The objective of this study was to use the World Health Organizatio...
PURPOSE: To determine if an IVIVC model can predict PK profiles of varying formulations of a BCS Class 1 drug that is a salt of a weak base. METHOD: An IVIVC model (Level A) was created by correlating...
In vitro-in vivo correlation (IVIVC) is a biopharmaceutical tool recommended to be used in development of formulation. When validated, it can speed up development of formulation, be used to fix dissol...
High lipophilicity and high lattice energy of drugs, which result in poor solubility are major real challenges in the pharmaceutical industry for the successful development and commercialization of su...
In vitro-in vivo correlation (IVIVC) models prove very useful during drug formulation development, the setting of dissolution specifications and bio-waiver applications following post approval changes...
The process of drug elimination that occurs within the kidneys is complex, and involves filtration, secretion and absorptive mechanisms. Many drugs, metabolites and toxins, including organ...
To identify the proportion of patients remaining medically castrated (testosterone level < 50 ng/dL) on Day 240 following two administrations of a 4-month sustained-release (SR) formulatio...
The primary objective is to determine the safety and tolerability of the new IV formulation versus the current formulation of MOA-728 focusing on the theoretical potential for infusion-rel...
Description: To investigate bioavailability of two anti-viral drugs (lamivudine and zidovudine) from a new oral formulation (trial formulation) especially designed for pediatric use....
This is a Phase 1, randomized, open label, 2 treatment, 2 period, 2-way crossover study, with an extension phase design in which the steady state PK of ARQ 197 will be investigated using t...