NDLI: The Twofold Advantage of the Amorphous Form as an Oral Drug Delivery Practice for Lipophilic Compounds: Increased Apparent Solubility and Drug Flux Through the Intestinal Membrane

Please wait, while we are loading the content...

Pharmacokinetics of Levodopa, Carbidopa, and 3-O-Methyldopa Following 16-hour Jejunal Infusion of Levodopa-Carbidopa Intestinal Gel in Advanced Parkinson’s Disease Patients

Highly Stabilized Curcumin Nanoparticles Tested in an In Vitro Blood–Brain Barrier Model and in Alzheimer’s Disease Tg2576 Mice

Simultaneous Analysis of Multiple Monoclonal Antibody Biotherapeutics by LC-MS/MS Method in Rat Plasma Following Cassette-Dosing

The Twofold Advantage of the Amorphous Form as an Oral Drug Delivery Practice for Lipophilic Compounds: Increased Apparent Solubility and Drug Flux Through the Intestinal Membrane

Translational Pharmacokinetic-Pharmacodynamic Modeling from Nonclinical to Clinical Development: A Case Study of Anticancer Drug, Crizotinib

Controlled Release of Simvastatin from In situ Forming Hydrogel Triggers Bone Formation in MC3T3-E1 Cells

Dose Selection Based on Physiologically Based Pharmacokinetic (PBPK) Approaches

Regulatory Administrative Databases in FDA's Center for Biologics Evaluation and Research: Convergence Toward a Unified Database

TargetHunter: An In Silico Target Identification Tool for Predicting Therapeutic Potential of Small Organic Molecules Based on Chemogenomic Database

Improper Selection of a Pre-specified Primary Dose–Response Analysis Delays Regulatory Drug Approval

In Vivo Quantitative Prediction of the Effect of Gene Polymorphisms and Drug Interactions on Drug Exposure for CYP2C19 Substrates

Strategic Applications of Gene Expression: From Drug Discovery/Development to Bedside

Animal Models of Osteoarthritis: Challenges of Model Selection and Analysis

Strategic Biomarkers for Drug Development in Treating Rare Diseases and Diseases in Neonates and Infants

A Workflow Example of PBPK Modeling to Support Pediatric Research and Development: Case Study with Lorazepam

A Sensitivity Analysis of the Modified Chi-square Ratio Statistic for Equivalence Testing of Aerodynamic Particle Size Distribution

The Interaction of Fatty Acid Amide Hydrolase (FAAH) Inhibitors with an Anandamide Carrier Protein Using $^{19}$ F-NMR

Drug Discovery and Regulatory Considerations for Improving In Silico and In Vitro Predictions that Use Caco-2 as a Surrogate for Human Intestinal Permeability Measurements

Simultaneous Pharmacokinetic Model for Rolofylline and both M1-trans and M1-cis Metabolites

Chemical Imaging of Drug Delivery Systems with Structured Surfaces–a Combined Analytical Approach of Confocal Raman Microscopy and Optical Profilometry

Effect of Device Design on the Aerosolization of a Carrier-Based Dry Powder Inhaler—a Case Study on Aerolizer$^{®}$ Foradile$^{®}$

Nonaqueous Gel for the Transdermal Delivery of a DTPA Penta-ethyl Ester Prodrug

Predictions of In Vivo Prolactin Levels from In Vitro K $_{i}$ Values of D$_{2}$ Receptor Antagonists Using an Agonist–Antagonist Interaction Model

Modeling NSCLC Progression: Recent Advances and Opportunities Available

Modeling, Simulation, and Translation Framework for the Preclinical Development of Monoclonal Antibodies

Population-Based Efficacy Modeling of Omalizumab in Patients with Severe Allergic Asthma Inadequately Controlled with Standard Therapy

Influences of Organic Cation Transporter Polymorphisms on the Population Pharmacokinetics of Metformin in Healthy Subjects

Organic Cation Transporter OCTs (SLC22) and MATEs (SLC47) in the Human Kidney

Regional-Dependent Intestinal Permeability and BCS Classification: Elucidation of pH-Related Complexity in Rats Using Pseudoephedrine

The Challenges of Assessing Osteoarthritis and Postoperative Pain in Dogs

In Vitro and In Vivo Evaluation of Amorphous Solid Dispersions Generated by Different Bench-Scale Processes, Using Griseofulvin as a Model Compound

Direct and Rapid Genotyping of SLCO1B1 388A>G and 521T>C in Human Blood Specimens Using the SmartAmp-2 Method

The AAPS Journal : Volume 15, Issue 1, January 2013

The AAPS Journal : Volume 14

The AAPS Journal : Volume 13

The AAPS Journal : Volume 12

The AAPS Journal : Volume 11

The AAPS Journal : Volume 10

The AAPS Journal : Volume 9

The AAPS Journal : Volume 8

The AAPS Journal : Volume 7

The AAPS Journal : Volume 6

The AAPS Journal : Volume 5

The AAPS Journal : Volume 4

The AAPS Journal : Volume 3

The AAPS Journal : Volume 2

The AAPS Journal : Volume 1

The Twofold Advantage of the Amorphous Form as an Oral Drug Delivery Practice for Lipophilic Compounds: Increased Apparent Solubility and Drug Flux Through the Intestinal Membrane

Content Provider	Springer Nature Link
Author	Dahan, Arik Beig, Avital Ioffe Dahan, Viktoriya Agbaria, Riad Miller, Jonathan M
Copyright Year	2012
Abstract	The purposes of this study were to assess the efficiency of different nifedipine amorphous solid dispersions (ASDs) in achieving and maintaining supersaturation and to investigate the solubility–permeability interplay when increasing the apparent solubility via ASD formulations. Spray-dried ASDs of nifedipine in three different hydrophilic polymers, hydroxypropyl methylcellulose acetate succinate (HPMC-AS), copovidone, and polyvinylpyrrolidone (PVP), were prepared and characterized by powder X-ray diffraction and differential scanning calorimetry. The ability of these formulations to achieve and maintain supersaturation over 24 h was assessed. Then, nifedipine’s apparent intestinal permeability was investigated as a function of increasing supersaturation in the parallel artificial membrane permeability assay model and in the single-pass rat intestinal perfusion model. The efficiency of the different ASDs to achieve and maintain supersaturation of nifedipine was found to be highly polymer dependent; while a dispersion in HPMC-AS enabled supersaturation 20× that of the crystalline aqueous solubility, a dispersion in copovidone enabled 10×, and PVP allowed supersaturation of only 5× that of the crystalline solubility. Nifedipine flux across the intestine from supersaturated solutions was increased, and the apparent intestinal permeability was constant, irrespective of the degree of supersaturation or the polymer being used. In conclusion, while with other solubility-enabling approaches (e.g., surfactants, cyclodextrins, cosolvents), it is not enough to increase the apparent solubility, but to strike the optimal solubility–permeability balance, which limits the chances for successful drug delivery, the amorphous form emerges as a more advantageous strategy, in which higher apparent solubility (i.e., supersaturation) will be readily translated into higher drug flux and overall absorption.
Starting Page	347
Ending Page	353
Page Count	7
File Format	PDF
ISSN	12341234
Journal	The AAPS Journal
Volume Number	15
Issue Number	2
e-ISSN	15507416
Language	English
Publisher	Springer US
Publisher Date	2012-12-15
Publisher Institution	American Association of Pharmaceutical Scientists
Publisher Place	Boston
Access Restriction	One Nation One Subscription (ONOS)
Subject Keyword	amorphous solid dispersions intestinal permeability lipophilic drugs oral absorption solubility–permeability interplay Pharmacology/Toxicology Biochemistry Biotechnology Pharmacy
Content Type	Text
Resource Type	Article

Sl.	Authority	Responsibilities	Communication Details
1	Ministry of Education (GoI), Department of Higher Education	Sanctioning Authority	https://www.education.gov.in/ict-initiatives
2	Indian Institute of Technology Kharagpur	Host Institute of the Project: The host institute of the project is responsible for providing infrastructure support and hosting the project	https://www.iitkgp.ac.in
3	National Digital Library of India Office, Indian Institute of Technology Kharagpur	The administrative and infrastructural headquarters of the project	Dr. B. Sutradhar bsutra@ndl.gov.in
4	Project PI / Joint PI	Principal Investigator and Joint Principal Investigators of the project	Dr. B. Sutradhar bsutra@ndl.gov.in Prof. Saswat Chakrabarti will be added soon
5	Website/Portal (Helpdesk)	Queries regarding NDLI and its services	support@ndl.gov.in
6	Contents and Copyright Issues	Queries related to content curation and copyright issues	content@ndl.gov.in
7	National Digital Library of India Club (NDLI Club)	Queries related to NDLI Club formation, support, user awareness program, seminar/symposium, collaboration, social media, promotion, and outreach	clubsupport@ndl.gov.in
8	Digital Preservation Centre (DPC)	Assistance with digitizing and archiving copyright-free printed books	dpc@ndl.gov.in
9	IDR Setup or Support	Queries related to establishment and support of Institutional Digital Repository (IDR) and IDR workshops	idr@ndl.gov.in

The Twofold Advantage of the Amorphous Form as an Oral Drug Delivery Practice for Lipophilic Compounds: Increased Apparent Solubility and Drug Flux Through the Intestinal Membrane

Hydrotropic Solubilization of Lipophilic Drugs for Oral Delivery: The Effects of Urea and Nicotinamide on Carbamazepine Solubility–Permeability Interplay

Co-Amorphous Solid Dispersions for Solubility and Absorption Improvement of Drugs: Composition, Preparation, Characterization and Formulations for Oral Delivery

Regional Intestinal Drug Absorption: Biopharmaceutics and Drug Formulation

In silico Predictions of Drug Solubility and Permeability: Two Rate-limiting Barriers to Oral Drug Absorption

BCS Class IV Oral Drugs and Absorption Windows: Regional-Dependent Intestinal Permeability of Furosemide

Prediction of Solubility and Permeability Class Membership: Provisional BCS Classification of the World’s Top Oral Drugs

Advantageous Solubility-Permeability Interplay When Using Amorphous Solid Dispersion (ASD) Formulation for the BCS Class IV P-gp Substrate Rifaximin: Simultaneous Increase of Both the Solubility and the Permeability

A Systematic Approach to Design and Prepare Solid Dispersions of Poorly Water-Soluble Drug

The Twofold Advantage of the Amorphous Form as an Oral Drug Delivery Practice for Lipophilic Compounds: Increased Apparent Solubility and Drug Flux Through the Intestinal Membrane

Similar Documents

The Twofold Advantage of the Amorphous Form as an Oral Drug Delivery Practice for Lipophilic Compounds: Increased Apparent Solubility and Drug Flux Through the Intestinal Membrane

Hydrotropic Solubilization of Lipophilic Drugs for Oral Delivery: The Effects of Urea and Nicotinamide on Carbamazepine Solubility–Permeability Interplay

Co-Amorphous Solid Dispersions for Solubility and Absorption Improvement of Drugs: Composition, Preparation, Characterization and Formulations for Oral Delivery

Regional Intestinal Drug Absorption: Biopharmaceutics and Drug Formulation

In silico Predictions of Drug Solubility and Permeability: Two Rate-limiting Barriers to Oral Drug Absorption

BCS Class IV Oral Drugs and Absorption Windows: Regional-Dependent Intestinal Permeability of Furosemide

Prediction of Solubility and Permeability Class Membership: Provisional BCS Classification of the World’s Top Oral Drugs

Advantageous Solubility-Permeability Interplay When Using Amorphous Solid Dispersion (ASD) Formulation for the BCS Class IV P-gp Substrate Rifaximin: Simultaneous Increase of Both the Solubility and the Permeability

A Systematic Approach to Design and Prepare Solid Dispersions of Poorly Water-Soluble Drug

The Twofold Advantage of the Amorphous Form as an Oral Drug Delivery Practice for Lipophilic Compounds: Increased Apparent Solubility and Drug Flux Through the Intestinal Membrane