Spray drying is one of the most frequently used solvent-based processes for manufacturing amorphous solid dispersions (ASDs). However, the resulting fine powders usually require further downstream processing when intended for solid oral dosage forms. In this study, we compare properties and performance of spray-dried ASDs with ASDs coated onto neutral starter pellets in mini-scale. We successfully prepared binary ASDs with a drug load of 20% Ketoconazole (KCZ) or Loratadine (LRD) as weakly basic model drugs and hydroxypropyl-methyl-cellulose acetate succinate or methacrylic acid ethacrylate copolymer as pH-dependent soluble polymers. All KCZ/ and LRD/polymer mixtures formed single-phased ASDs, as indicated by differential scanning calorimetry, X-ray powder diffraction and infrared spectroscopy. All ASDs showed physical stability for 6 months at 25 °C/65% rH and 40 °C/0% rH. Normalized to their initial surface area available to the dissolution medium, all ASDs showed a linear relationship of surface area and solubility enhancement, both in terms of supersaturation of solubility and initial dissolution rate, regardless of the manufacturing process. With similar performance and stability, processing of ASD pellets showed the advantages of a superior yield (>98%), ready to use for subsequent processing into multiple unit pellet systems. Therefore, ASD-layered pellets are an attractive alternative in ASD-formulation, especially in early formulation development at limited availability of drug substance.
Download full-text PDF |
Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC10054131 | PMC |
| http://dx.doi.org/10.3390/pharmaceutics15030764 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Molecular structure characteristic of coals of different rank.
J Mol Model
January 2025
School of Chemical and Environmental Engineering, China University of Mining and Technology-Beijing, Haidian District, Ding No.11 Xueyuan Road, Beijing, 100083, People's Republic of China.
Context: Understanding the structural characteristics of coal at the molecular level is fundamental for its effective utilization. To explore the molecular structure characteristic, the long-flame coal from Daliuta (DLT), coking coal from Yaoqiao (YQ), and anthracite from Taixi (TX) were investigated using various techniques such as elemental analysis, Fourier transform infrared spectroscopy, solid-state C nuclear magnetic resonance spectroscopy, and X-ray photoelectron spectroscopy. Based on the structural parameters, the coal molecular model was constructed and optimized.
View Article and Find Full Text PDFDrug Property Optimization: Design, Synthesis, and Characterization of Novel Pharmaceutical Salts and Cocrystal-Salt of Lumefantrine.
Mol Pharm
January 2025
Department of Industrial and Molecular Pharmaceutics, College of Pharmacy, Purdue University, 575 Stadium Mall Drive, West Lafayette, Indiana 47907, United States.
Lumefantrine (LMF) is a low-solubility antimalarial drug that cures acute, uncomplicated malaria. It exerts its pharmacological effects against erythrocytic stages of spp. and prevents malaria pathogens from producing nucleic acid and protein, thereby eliminating the parasites.
View Article and Find Full Text PDFUptake and Transpiration of Solid and Hollow SiO Nanoparticles by Terrestrial Plant (Apium Graveolens var. secalinum).
Chemosphere
January 2025
Department of Chemical and Biological Engineering, The Hong Kong University of Science and Technology, Clear Water Bay, Kowloon, Hong Kong SAR, China; Division of Environment and Sustainability, The Hong Kong University of Science and Technology, Clear Water Bay, Kowloon, Hong Kong SAR, China; HKUST Shenzhen-Hong Kong Collaborative Innovation Research Institute, Futian, Shenzhen, Guangdong Province, China. Electronic address:
Recent studies have raised concerns about the potential toxicity of amorphous silica (SiO) nanoparticles (NPs). This investigation explores the uptake, transport, and transpiration of silica NPs in Apium graveolens var. secalinum.
View Article and Find Full Text PDFPreparation and mechanical performance of fluorite tailings geopolymer precursor under alkaline heat activation.
Sci Rep
January 2025
School of Civil Engineering and Communication, North China University of Water Resources and Electric Power, Zhengzhou, 450045, People's Republic of China.
As one of the bulk solid wastes in the Yellow River basin in China, fluorite tailings urgently need to be utilized as resources. In this paper, NaOH and NaCO were used for alkali thermal activation of ground fluorite tailings under different temperature conditions, and the reactivity was analyzed by XRD, SEM and compressive strength after hydration, so as to evaluate the feasibility of fluorite tailings as geopolymer precursor. The results show that the fluorite tailings can exhibit certain reactivity under alkaline heat excitation, and significant amorphous glass phase can be detected.
View Article and Find Full Text PDFMelt electrowriting of amorphous solid dispersions: Influence of drug and plasticizer on rheology and printing performance.
Int J Pharm
January 2025
Soft Matter Chemistry, Department of Chemistry, and Helsinki Institute of Sustainability Science, Faculty of Science, University of Helsinki, PB55 00014 Helsinki, Finland. Electronic address:
Drug loaded microfiber scaffolds have potential for sublingual drug delivery due to their fast dissolution time and tunable porosity. Such microfiber scaffolds can be prepared by melt electrowriting (MEW), wherein a polymer melt is electrostatically drawn out of a syringe onto a computer controlled moving collector. The fabrication of such scaffolds via MEW has previously been shown for a polymer with a glass transition temperature (T) just above room temperature, making handling challenging.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!