scholarly journals Using Acetone/Water Binary Solvent to Enhance the Stability and Bioavailability of Spray Dried Enzalutamide/HPMC-AS Solid Dispersions

Author(s):  
Xiaoting Zhang ◽  
Qiuhong Rao ◽  
Zhenwen Qiu ◽  
Yisheng Lin ◽  
Lei Zhang ◽  
...  
Pharmaceutics ◽  
2020 ◽  
Vol 12 (3) ◽  
pp. 197 ◽  
Author(s):  
Mahbubur Rahman ◽  
Stephanie Ahmad ◽  
James Tarabokija ◽  
Nathaniel Parker ◽  
Ecevit Bilgili

This study aimed to elucidate the impact of a common anionic surfactant, sodium dodecyl sulfate (SDS), along with hydroxypropyl cellulose (HPC) and Soluplus (Sol) on the release of griseofulvin (GF), a poorly soluble drug, from amorphous solid dispersions (ASDs). Solutions of 2.5% GF and 2.5%–12.5% HPC/Sol with 0.125% SDS/without SDS were prepared in acetone–water and spray-dried. The solid-state characterization of the ASDs suggests that GF–Sol had better miscibility and stronger interactions than GF–HPC and formed XRPD-amorphous GF, whereas HPC-based ASDs, especially the ones with a lower HPC loading, had crystalline GF. The dissolution tests show that without SDS, ASDs provided limited GF supersaturation (max. 250%) due to poor wettability of Sol-based ASDs and extensive GF recrystallization in HPC-based ASDs (max. 50%). Sol-based ASDs with SDS exhibited a dramatic increase in supersaturation (max. 570%), especially at a higher Sol loading, whereas HPC-based ASDs with SDS did not. SDS did not interfere with Sol’s ability to inhibit GF recrystallization, as confirmed by the precipitation from the supersaturated state and PLM imaging. The favorable use of SDS in a ternary ASD was attributed to both the wettability enhancement and its inability to promote GF recrystallization when used as a minor component along with Sol.


Pharmaceutics ◽  
2021 ◽  
Vol 13 (11) ◽  
pp. 1938
Author(s):  
Lena Ritters ◽  
Yuanyuan Tian ◽  
Stephan Reichl

The formulation of active pharmaceutical ingredients (APIs) in amorphous solid dispersions (ASDs) is a promising approach to improve the bioavailability of poorly soluble compounds. However, problems often arise in the production of tablets from ASDs regarding the compressibility and recrystallization of the API. In the present study, the preparation of spray-dried ASDs of paracetamol (PCM) and four different types of polyvinylpyrrolidone (PVP) and their further processing into tablets were investigated. The influence of PVP type on the glass transition temperature (Tg) and the physical stability of ASD powders were characterized by differential scanning calorimetry (DSC) and powder X-ray diffraction (XRD). ASD powders with 10 to 30% PCM were stable for at least 48 weeks. PCM contents of 40 to 50% led to recrystallization of the amorphous PCM within a few days or weeks. ASD with PVP/vinyl acetate (VA) copolymer (PVP/VA) was the most unstable and tended to recrystallize in PCM polymorphic form II. This formulation was therefore used for tablet studies. The influence of compression force on recrystallization, crushing strength, and drug release was investigated. Even high compression forces did not affect the stability of the ASD. However, the ASD tablets led to slow release of the API.


2009 ◽  
Vol 98 (12) ◽  
pp. 4724-4737 ◽  
Author(s):  
Hisham Al-Obaidi ◽  
Steve Brocchini ◽  
Graham Buckton

2016 ◽  
Vol 42 (11) ◽  
pp. 1813-1824 ◽  
Author(s):  
Jessica Mendes Nadal ◽  
Mona Lisa Simionatto Gomes ◽  
Débora Maria Borsato ◽  
Martinha Antunes Almeida ◽  
Fernanda Malaquias Barboza ◽  
...  

2020 ◽  
pp. 141-148
Author(s):  
Rosalinda C Torres ◽  
Rowelain Mae G Yumang ◽  
Chelsea Kate F Jose ◽  
Danielle Camille P Canillo

Dragon fruit (Hylocereus polyrhizus) is known for its purple-coloured peels and pulp, which can be attributed to the presence of betalains. In this study, the potential of red dragon fruit as a source of natural colorant was investigated. Betacyanins were extracted from red dragon fruit peels and flesh in 1:3 ratio with water. Microencapsulation by spray-drying was done by adding 5% and 10% (w/v) maltodextrin (DE 11.8) to peels and flesh extracts, respectively. The spray-dried colorant powders all obtained <10% moisture content, 5.261-6.409 g/100g hygroscopic moisture content, and 5.317-7.349(mg/100L) betacyanin content. Morphological characterization revealed spherical, agglomerated particles with visible cracks on the surface. The stability study conducted showed that pigment retention was lowest at 70°C and highest at 4°C. Keywords: Hylocereus polyrhizus; Red dragon fruit; Betacyanin; Microencapsulation; Physicochemical properties


2007 ◽  
Vol 57 (3) ◽  
pp. 287-300 ◽  
Author(s):  
Ravindra Dhumal ◽  
Shamkant Shimpi ◽  
Anant Paradkar

Development of spray-dried co-precipitate of amorphous celecoxib containing storage and compression stabilizersThe purpose of this study was to obtain an amorphous system with minimum unit operations that will prevent recrystallization of amorphous drugs since preparation, during processing (compression) and further storage. Amorphous celecoxib, solid dispersion (SD) of celecoxib with polyvinyl pyrrollidone (PVP) and co-precipitate with PVP and carrageenan (CAR) in different ratios were prepared by the spray drying technique and compressed into tablets. Saturation solubility and dissolution studies were performed to differentiate performance after processing. Differential scanning calorimetry and X-ray powder difraction revealed the amorphous form of celecoxib, whereas infrared spectroscopy revealed hydrogen bonding between celecoxib and PVP. The dissolution profile of the solid dispersion and co-precipitate improved compared to celecoxib and amorphous celecoxib. Amorphous celecoxib was not stable on storage whereas the solid dispersion and co-precipitate powders were stable for 3 months. Tablets of the solid dispersion of celecoxib with PVP and physical mixture with PVP and carrageenan showed better resistance to recrystallization than amorphous celecoxib during compression but recrystallized on storage. However, tablets of co-precipitate with PVP and carageenan showed no evidence of crystallinity during stability studies with comparable dissolution profiles. This extraordinary stability of spray-dried co-precipitate tablets may be attributed to the cushioning action provided by the viscoelastic polymer CAR and hydrogen bonding interaction between celecoxib and PVP. The present study demonstrates the synergistic effect of combining two types of stabilizers, PVP and CAR, on the stability of amorphous drug during compression and storage as compared to their effect when used alone.


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