Hot Melt Coating of Amorphous Carvedilol

Pharmaceutics
Jacob BannowThomas Rades

Abstract

The use of amorphous drug delivery systems is an attractive approach to improve the bioavailability of low molecular weight drug candidates that suffer from poor aqueous solubility. However, the pharmaceutical performance of many neat amorphous drugs is compromised by their tendency for recrystallization during storage and lumping upon dissolution, which may be improved by the application of coatings on amorphous surfaces. In this study, hot melt coating (HMC) as a solvent-free coating method was utilized to coat amorphous carvedilol (CRV) particles with tripalmitin containing 10% (w/w) and 20% (w/w) of polysorbate 65 (PS65) in a fluid bed coater. Lipid coated amorphous particles were assessed in terms of their physical stability during storage and their drug release during dynamic in vitro lipolysis. The release of CRV during in vitro lipolysis was shown to be mainly dependent on the PS65 concentration in the coating layer, with a PS65 concentration of 20% (w/w) resulting in an immediate release profile. The physical stability of the amorphous CRV core, however, was negatively affected by the lipid coating, resulting in the recrystallization of CRV at the interface between the crystalline lipid layer and the amorphous drug cor...Continue Reading

References

Mar 4, 1999·International Journal of Pharmaceutics·D Q CraigM L Hopton
Aug 14, 2001·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·N H ZangenbergL Hovgaard
Sep 6, 2003·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Jörg BreitkreutzWolfgang Wiedey
Aug 24, 2006·Pharmaceutical Research·Tian Wu, Lian Yu
Apr 3, 2007·Langmuir : the ACS Journal of Surfaces and Colloids·Tian WuLian Yu
May 13, 2009·Molecular Pharmaceutics·Lei ZhuLian Yu
Apr 24, 2010·Pharmaceutical Research·Lei ZhuTian Wu
Mar 30, 2011·Proceedings of the National Academy of Sciences of the United States of America·Ye SunLian Yu
Jul 21, 2011·Physical Review Letters·L ZhuL Yu
Aug 4, 2011·Expert Opinion on Drug Delivery·Abhishek SinghGuy Van den Mooter
Sep 8, 2011·Expert Opinion on Drug Delivery·Peter van HoogevestAlfred Fahr
Nov 3, 2011·International Journal of Pharmaceutics·R WitzlebP Kleinebudde
May 10, 2012·International Journal of Pharmaceutics·Riikka LaitinenThomas Rades
Oct 24, 2012·International Journal of Pharmaceutics·Vincent Jannin, Yvonne Cuppok
Sep 10, 2013·International Journal of Pharmaceutics·Petra A PriemelClare J Strachan
Apr 24, 2014·Expert Opinion on Drug Delivery·Holger GrohganzThomas Rades
Apr 24, 2015·Journal of Pharmaceutical Sciences·Maxx Capece, Rajesh Davé
Dec 2, 2015·International Journal of Pharmaceutics·Karin BeckerSharareh Salar-Behzadi
Jan 18, 2016·Advanced Drug Delivery Reviews·Lian Yu
May 8, 2016·Advanced Drug Delivery Reviews·Marc Descamps
Dec 23, 2016·International Journal of Pharmaceutics·Diogo Gomes LopesSharareh Salar-Behzadi
Aug 27, 2017·International Journal of Pharmaceutics·Diogo Gomes LopesAndreas Zimmer
Jan 7, 2018·Pharmaceutical Research·Rattavut TeerakapibalLian Yu

❮ Previous
Next ❯

Citations

Aug 29, 2021·Pharmaceutics·Xin YaoLian Yu

❮ Previous
Next ❯

Methods Mentioned

BETA
X-ray
scanning electron microscopy
scanning

Software Mentioned

TRIOS
Mercury
AZtecLive

Related Concepts

Trending Feeds

COVID-19

Coronaviruses encompass a large family of viruses that cause the common cold as well as more serious diseases, such as the ongoing outbreak of coronavirus disease 2019 (COVID-19; formally known as 2019-nCoV). Coronaviruses can spread from animals to humans; symptoms include fever, cough, shortness of breath, and breathing difficulties; in more severe cases, infection can lead to death. This feed covers recent research on COVID-19.

Blastomycosis

Blastomycosis fungal infections spread through inhaling Blastomyces dermatitidis spores. Discover the latest research on blastomycosis fungal infections here.

Nuclear Pore Complex in ALS/FTD

Alterations in nucleocytoplasmic transport, controlled by the nuclear pore complex, may be involved in the pathomechanism underlying multiple neurodegenerative diseases including Amyotrophic Lateral Sclerosis and Frontotemporal Dementia. Here is the latest research on the nuclear pore complex in ALS and FTD.

Applications of Molecular Barcoding

The concept of molecular barcoding is that each original DNA or RNA molecule is attached to a unique sequence barcode. Sequence reads having different barcodes represent different original molecules, while sequence reads having the same barcode are results of PCR duplication from one original molecule. Discover the latest research on molecular barcoding here.

Chronic Fatigue Syndrome

Chronic fatigue syndrome is a disease characterized by unexplained disabling fatigue; the pathology of which is incompletely understood. Discover the latest research on chronic fatigue syndrome here.

Evolution of Pluripotency

Pluripotency refers to the ability of a cell to develop into three primary germ cell layers of the embryo. This feed focuses on the mechanisms that underlie the evolution of pluripotency. Here is the latest research.

Position Effect Variegation

Position Effect Variagation occurs when a gene is inactivated due to its positioning near heterochromatic regions within a chromosome. Discover the latest research on Position Effect Variagation here.

STING Receptor Agonists

Stimulator of IFN genes (STING) are a group of transmembrane proteins that are involved in the induction of type I interferon that is important in the innate immune response. The stimulation of STING has been an active area of research in the treatment of cancer and infectious diseases. Here is the latest research on STING receptor agonists.

Microbicide

Microbicides are products that can be applied to vaginal or rectal mucosal surfaces with the goal of preventing, or at least significantly reducing, the transmission of sexually transmitted infections. Here is the latest research on microbicides.