This study investigates the influence of surfactant sodium lauryl sulfate (SLS) on the solubility of poorly-water soluble drug substances, model Compound X and Compound Y, used in a fixed dose combination oral solid dosage form. To determine the impact of SLS concentration on the solubility of compounds X and Y, we experimentally determined the critical micelle concentration (CMC) of SLS in water, simulated gastric fluid (SGF), and fed state simulated intestinal fluid (FeSSIF) in the presence of Compound X and Compound Y using UV/Visible spectrophotometry at 25°C. The aggregation of SLS was characterized by calculating the standard Gibbs free energy of micellization in all the media investigated. To enhance the understanding of SLS aggregation, high throughput experiments and in-vivo mechanistic modelling were used to determine the effect of increasing levels of SLS on the solubility of compounds X and Y as both single agent and combination products to be formulated into a suitable oral solid dosage form. Micellar formation of SLS is a spontaneous process as shown by the negative values of the standard free energy of micellization. The CMC of SLS in the various media investigated in the presence of compounds X and Y decreases in the following order: water> FeSSIF> SGF. However, the aggregation of SLS in the various media is overall more spontaneous in the following order: SGF>FeSSIF>water. Using high throughput experimentation and in-vivo mechanistic modelling, it was determined that a combination oral solid product of compounds X and Y will have optimum solubility and in-vivo absorption if 2 mg of SLS was used in the oral solid dosage form. The results obtained from this study will help broaden the understanding of the micellization process involving SLS and poorly-water soluble drugs used in combination oral solid dosage forms.
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http://dx.doi.org/10.18433/jpps30347 | DOI Listing |
Pharmaceutics
December 2024
College of Pharmacy, Dongguk University-Seoul, Dongguk-ro-32, Ilsan-Donggu, Goyang 10326, Republic of Korea.
Background/objectives: A sustained-release formulation of fenofibrate while enhancing drug dissolution with minimal food effect is critical for maximizing the therapeutic benefits of fenofibrate. Therefore, this study aimed to develop an effective solid dispersion formulation of fenofibrate for simultaneous enhancement in the extent and duration of drug exposure.
Methods: Fenofibrate-loaded solid dispersions (FNSDs) were prepared using poloxamer 407 and Eudragit RSPO at varied ratios via solvent evaporation.
Pharmaceutics
December 2024
Department of Obstetrics and Gynecology, Grigore T. Popa University of Medicine and Pharmacy, 700111 Iasi, Romania.
Diabetes is a widespread metabolic illness. Mismanagement of diabetes can lead to severe complications that tremendously impact patients' quality of life. The assimilation of nanotechnology in diabetes care holds the potential to revolutionize treatment paradigms, improve patient outcomes, and reduce the economic burden associated with this pervasive disease.
View Article and Find Full Text PDFPharmaceutics
November 2024
UCIBIO (Applied Molecular Biosciences Unit), Laboratory of Pharmaceutical Technology, Faculty of Pharmacy, University of Porto, 4050-313 Porto, Portugal.
As life expectancy rises and modern lifestyles improve, there is an increasing focus on health, disease prevention, and enhancing physical appearance. Consumers are more aware of the benefits of natural ingredients in healthcare products while also being mindful of sustainability challenges. Consequently, marine bioactive compounds have gained popularity as ingredients in cosmetics and food supplements due to their diverse beneficial properties.
View Article and Find Full Text PDFPharmaceutics
November 2024
College of Pharmacy and Research Institute for Drug Development, Pusan National University, 63 Busandaehak-ro, Geumjeong-gu, Busan 46241, Republic of Korea.
This study investigates the impact of supercritical antisolvent (SAS) process parameters on the particle formation of telmisartan, a poorly water-soluble drug. A fractional factorial design was employed to examine the influence of the SAS process parameters, including solvent ratio, drug solution concentration, temperature, pressure, injection rate of drug solution, and CO₂ flow rate, on particle formation. Solid-state characterizations of the SAS process particles using XRD and FT-IR confirmed their amorphous nature.
View Article and Find Full Text PDFPharmaceutics
November 2024
Merck Life Science KGaA, Frankfurter Straße 250, 64293 Darmstadt, Germany.
Melt-based 3D printing technologies are currently extensively evaluated for research purposes as well as for industrial applications. Classical approaches often require intermediates, which can pose a risk to stability and add additional complexity to the process. The Advanced Melt Drop Deposition (AMDD) technology, is a 3D printing process that combines the principles of melt extrusion with pressure-driven ejection, similar to injection molding.
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