A New Extrudable Form of Hypromellose: AFFINISOL™ HPMC HME

Huang, Siyuan; O’Donnell, K. P.; Keen, Justin M.; Rickard, Mark A.; McGinity, James W.; Williams, Robert O.

doi:10.1208/s12249-015-0395-9

Cited by 76 publications

(54 citation statements)

References 55 publications

(66 reference statements)

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The slope of the best-fit line of the plotted Equation (3) is considered to be equivalent to χ. By understanding χ as a function of temperature, metastable and unstable regions for the combination can be predicted by generating a spinodal (boundary between unstable and metastable regions) and binodal (boundary between metastable and stable regions) curves [ 46 ].…”

Section: Methodsmentioning

confidence: 99%

A Repurposed Drug for Brain Cancer: Enhanced Atovaquone Amorphous Solid Dispersion by Combining a Spontaneously Emulsifying Component with a Polymer Carrier

et al. 2018

View full text Add to dashboard Cite

Glioblastoma multiforme (GBM) is the most common and lethal central nervous system tumor. Recently, atovaquone has shown inhibition of signal transducer and activator transcription 3, a promising target for GBM therapy. However, it is currently unable to achieve therapeutic drug concentrations in the brain with the currently reported and marketed formulations. The present study sought to explore the efficacy of atovaquone against GBM as well as develop a formulation of atovaquone that would improve oral bioavailability, resulting in higher amounts of drug delivered to the brain. Atovaquone was formulated as an amorphous solid dispersion using an optimized formulation containing a polymer and a spontaneously emulsifying component (SEC) with greatly improved wetting, disintegration, dispersibility, and dissolution properties. Atovaquone demonstrated cytotoxicity against GBM cell lines as well as provided a confirmed target for atovaquone brain concentrations in in vitro cell viability studies. This new formulation approach was then assessed in a proof-of-concept in vivo exposure study. Based on these results, the enhanced amorphous solid dispersion is promising for providing therapeutically effective brain levels of atovaquone for the treatment of GBM.

show abstract

Section: Methodsmentioning

confidence: 99%

A Repurposed Drug for Brain Cancer: Enhanced Atovaquone Amorphous Solid Dispersion by Combining a Spontaneously Emulsifying Component with a Polymer Carrier

et al. 2018

View full text Add to dashboard Cite

show abstract

“…More interestingly, the melt viscosity and corresponding extruder torque load is reported to be independent of the polymer molecular weight, with Affinisol® HPMC 6LV, 100LV, and 4M exhibiting a comparable maximum torque load of approximately 20% on a Leistritz nano-16 extruder (107). In addition, the crystallization inhibition properties of the polymer remain, with demonstrated dissolution performance of ASDs containing the poorly soluble drugs loratidine (107), carbamazepine (108), and itraconazole (109).…”

Section: Designer Polymers For Extrusion Processingmentioning

confidence: 99%

Challenges and Strategies in Thermal Processing of Amorphous Solid Dispersions: A Review

2015

Self Cite

View full text Add to dashboard Cite

Abstract. Thermal processing of amorphous solid dispersions continues to gain interest in the pharmaceutical industry, as evident by several recently approved commercial products. Still, a number of pharmaceutical polymer carriers exhibit thermal or viscoelastic limitations in thermal processing, especially at smaller scales. Additionally, active pharmaceutical ingredients with high melting points and/or that are thermally labile present their own specific challenges. This review will outline a number of formulation and process-driven strategies to enable thermal processing of challenging compositions. These include the use of traditional plasticizers and surfactants, temporary plasticizers utilizing sub-or supercritical carbon dioxide, designer polymers tailored for hot-melt extrusion processing, and KinetiSol® Dispersing technology. Recent case studies of each strategy will be described along with potential benefits and limitations.

show abstract

“…HPMC-based coating barriers applied by different techniques onto drug-containing cores were already demonstrated, to be able to provide reproducible lag phases prior to drug release [45]. Novel grades of HPMC with improved thermal properties (i.e., AffiniSol™) were recently proposed and mainly employed for the preparation of solid dispersions [46][47][48]. These grades are expected to maintain the crystallization-inhibiting properties of standard HPMCs, but can be extruded over a wider range of temperatures than the latter.…”

Section: Hot-processability Of the Starting Materialsmentioning

confidence: 99%

Injection Molded Capsules for Colon Delivery Combining Time-Controlled and Enzyme-Triggered Approaches

Casati

Melocchi

Moutaharrik

et al. 2020

IJMS

View full text Add to dashboard Cite

A new type of colon targeting system is presented, combining time-controlled and enzyme-triggered approaches. Empty capsule shells were prepared by injection molding of blends of a high-amylose starch and hydroxypropyl methylcellulose (HPMC) of different chain lengths. The dissolution/erosion of the HPMC network assures a time-controlled drug release, i.e., drug release starts upon sufficient shell swelling/dissolution/erosion. In addition, the presence of high-amylose starch ensures enzyme-triggered drug release. Once the colon is reached, the local highly concentrated bacterial enzymes effectively degrade this polysaccharide, resulting in accelerated drug release. Importantly, the concentration of bacterial enzymes is much lower in the upper gastrointestinal tract, thus enabling site-specific drug delivery. The proposed capsules were filled with acetaminophen and exposed to several aqueous media, simulating the contents of the gastrointestinal tract using different experimental setups. Importantly, drug release was pulsatile and occurred much faster in the presence of fecal samples from patients. The respective lag times were reduced and the release rates increased once the drug started to be released. It can be expected that variations in the device design (e.g., polymer blend ratio, capsule shell geometry and thickness) allow for a large variety of possible colon targeting release profiles.

show abstract

A New Extrudable Form of Hypromellose: AFFINISOL™ HPMC HME

Cited by 76 publications

References 55 publications

A Repurposed Drug for Brain Cancer: Enhanced Atovaquone Amorphous Solid Dispersion by Combining a Spontaneously Emulsifying Component with a Polymer Carrier

A Repurposed Drug for Brain Cancer: Enhanced Atovaquone Amorphous Solid Dispersion by Combining a Spontaneously Emulsifying Component with a Polymer Carrier

Challenges and Strategies in Thermal Processing of Amorphous Solid Dispersions: A Review

Injection Molded Capsules for Colon Delivery Combining Time-Controlled and Enzyme-Triggered Approaches

Contact Info

Product

Resources

About