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HPMCAS – Hydroxypropyl methylcellulose acetate succinate
Can the Oral Bioavailability of the Discontinued Prostate Cancer Drug Galeterone Be Improved by…
Galeterone, a novel prostate cancer candidate treatment, was discontinued after a Phase III clinical trial due to lack of efficacy. Galeterone is weakly basic and exhibits low solubility in biorelevant media (i.e., ~ 2 µg/mL in fasted simulated intestinal fluid). It was formulated as a 50–50 (w/w)…
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Viscoelastic Behavior of Supercooled and Glassy ASDs at Humid Conditions Can Be Predicted
Amorphous solid dispersions (ASDs) are commonly used to increase the dissolution rate of poorly soluble active pharmaceutical ingredients (APIs). Unfortunately, most ASDs are thermodynamically unstable and, even though kinetically stabilized, will thus eventually crystallize. The crystallization…
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Supersaturating lipid-based solid dispersion of atazanavir provides enhanced solubilization and…
Understanding and controlling the drug solubilization in digestive environment is of great importance in the design of lipid based solid dispersion (LBSD) for oral delivery of poorly aqueous soluble drugs. In the current study we determined the extent of drug solubilization and supersaturation of…
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Evaluating Spray Drying and Co-precipitation as Manufacturing Processes for Amorphous Solid…
Amorphous solid dispersions feature prominently in the approach to mitigate low bioavailability of poorly water-soluble small molecules, particularly in the early development space focusing on toxicity evaluations and clinical studies in normal healthy volunteers, where high exposures are needed to…
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Downstream processing of amorphous solid dispersions into tablets
Amorphous solid dispersions have gained tremendous attention as a commercially viable solubility enhancement technique for poorly water-soluble drugs. However, poor drug loading associated with poor drug-polymer miscibility is a major challenge in the downstream processing of ASDs. While many…
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Downstream Processing of Amorphous Solid Dispersions into Orodispersible Tablets
The formulation development of amorphous solid dispersions (ASDs) towards a patient-friendly oral solid dosage form is proving to be still challenging. To increase patient’s compliance orodispersible tablets (ODTs) can be seen as promising alternative. Two different ASDs were prepared via hot melt…
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The impact of applying an additional polymer coating on high drug-loaded amorphous solid dispersions…
Inhibiting surface crystallization is an interesting strategy to enhance the physical stability of amorphous solid dispersions (ASDs), still preserving high drug loads. The aim of this study was to investigate the potential surface crystallization inhibitory effect of an additional polymer coating…
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Commercially Available Enteric Empty Hard Capsules, Production Technology and Application
Currently, there is a growing need to prepare small batches of enteric capsules for individual therapy or clinical evaluation since many acidic-sensitive substances should be protected from the stomach’s acidic environment, including probiotics or fecal material, in the fecal microbiota…
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Impact of Aluminum Oxide Nanocoating on Drug Release from Amorphous Solid Dispersion Particles
Atomic layer coating (ALC) is emerging as a particle engineering strategy to inhibit surface crystallization of amorphous solid dispersions (ASDs). In this study, we turn our attention to evaluating drug release behavior from ALC-coated ASDs, and begin to develop a mechanistic framework.…
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Recent Advances in Amorphous Solid Dispersions: Preformulation, Formulation Strategies,…
Abstract
Amorphous solid dispersions (ASDs) are among the most popular and widely studied solubility enhancement techniques. Since their inception in the early 1960s, the formulation development of ASDs has undergone tremendous progress. For instance, the method of preparing ASDs evolved from…
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