Increased dissolution rates of carbamazepine - gluconolactone binary blends processed by hot melt extrusion

Pharmaceutical Development and Technology
Hiren G MoradiyaD Douroumis

Abstract

Carbamazepine (CBZ) shows a poor dissolution, therefore, it is important to enhance its dissolution in GI tract to improve its bioavailability. In the present study, a new hydrophilic carrier, d-gluconolactone (GNL), was extruded with CBZ at various molar ratios to produce granules by using hot melt extrusion (HME) processing. The granular extrudates were characterised by X-ray powder diffraction, differential scanning calorimetry and hot stage microscopy to determine the solid state of CBZ. It was found that bulk CBZ (Form-III) transformed to the polymorphic Form-I during the HME processing. GNL was proved to be an efficient carrier for CBZ to enhance the dissolution rate. The increase in the dissolution rate was observed for both physical mixtures and the extrudates of CBZ-GNL. However, the extrudates showed faster dissolution rates compared to physical mixtures in an ascending order of 2:1 < 1:1 < 1.5:1 (CBZ:GNL). The increase in the dissolution rates was attributed to the transformation of CBZ III to Form-I and also to the increased drug wettability/solubilisation in the presence of the carrier.

References

Dec 22, 1999·International Journal of Pharmaceutics·Y KobayashiK Yamamoto
Apr 28, 2001·Advanced Drug Delivery Reviews·S R VippaguntaD J Grant
Jun 14, 2002·International Journal of Pharmaceutics·R NairStephen W Hoag
Sep 17, 2002·Pharmaceutical Development and Technology·Mariarosa MoneghiniFrancesco Princivalle
Nov 7, 2003·Journal of Pharmaceutical Sciences·Adam L GrzesiakAdam J Matzger
Jun 8, 2004·Pharmaceutical Research·Tiffani D DavisStephen R Byrn
Nov 30, 2005·Journal of Pharmaceutical Sciences·Stephen R CarinoMichael Hawley
Feb 3, 2007·The Journal of Pharmacy and Pharmacology·Fang TianThomas Rades
May 15, 2007·International Journal of Pharmaceutics·Yousef JavadzadehAli Nokhodchi
Aug 3, 2010·Colloids and Surfaces. B, Biointerfaces·Hiba Al-HamidiAli Nokhodchi
Jul 31, 2012·Therapeutic Delivery·Matthew WilsonGavin P Andrews
Nov 28, 2012·International Journal of Pharmaceutics·Sejal ShahMichael A Repka
Dec 4, 2012·Colloids and Surfaces. B, Biointerfaces·Hiba Al-HamidiAli Nokhodchi
Dec 25, 2012·International Journal of Pharmaceutics·Mohammed ManiruzzamanDennis Douroumis
Jan 18, 2013·ISRN Pharmaceutics·Mohammed ManiruzzamanDennis Douroumis
Dec 30, 2014·International Journal of Pharmaceutics·J ThiryB Evrard

❮ Previous
Next ❯

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.