A Comparison of Spray-Drying and Co-Precipitation for the Generation of Amorphous Solid Dispersions (ASDs) of Hydrochlorothiazide and Simvastatin

Myślińska, Monika; Stöcker, Michael; Ferguson, Steven; Healy, Anne Marie

doi:10.1016/j.xphs.2023.02.012

Cited by 5 publications

(2 citation statements)

References 63 publications

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“…The method of directly co-precipitating amorphous solid dispersions (ASDs) during the last phase of chemical processing is known as co-processing. [52]. The use of co-precipitation represented an innovative approach to enhance the functional characteristics of proteins in their pure form [53].…”

Section: Co-precipitate Methodsmentioning

confidence: 99%

A review on solubility enhancement technique for pharmaceutical drugs

Vaishnavi B. Borgaonkar,

Chetan M. Jain,

Amit R. Jaiswal

et al. 2024

GSC Biol. Pharm. Sci.

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Solubility, a critical parameter governing the bioavailability and therapeutic efficacy of pharmaceutical compounds, often poses a significant challenge in drug development. This review article offers a thorough examination of several methods used to improve the solubility of medications that have low solubility, in order to overcome their limits. The discussion encompasses both conventional and emerging strategies, highlighting their mechanisms, advantages, and limitations. The study examines conventional methods such as particle size reduction, solid dispersion, and cosolvency, focusing on their historical importance and extensive use. Advances in nanotechnology, including nanosuspensions, nanocrystals, and lipid-based nanocarriers, are discussed for their potential to revolutionize solubility enhancement through improved drug delivery systems. An essential determinant in achieving optimal medication dosage absorption into the circulatory system is the demonstration of a pharmacological action is directly linked to the solubility of a substance. The primary challenge in formulating the new medicinal chemical is its limited water solubility. Medications with low solubility in water need large doses in order to achieve their highest effective concentration in the bloodstream when taken orally. The biopharmaceutical categorization system (BCS) classifies substances according to their solubility and permeability. Regulatory agencies and health organizations have used this categorization approach to validate bioequivalence for chemicals that are both highly soluble and very permeable by using dissolution as a form of confirmation. Medications that have a poor capacity to dissolve in water have a slow pace of breaking down, which results in a reduction in the amount of the medication that may be absorbed into the bloodstream when taken orally.

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Section: Co-precipitate Methodsmentioning

confidence: 99%

A review on solubility enhancement technique for pharmaceutical drugs

Vaishnavi B. Borgaonkar,

Chetan M. Jain,

Amit R. Jaiswal

et al. 2024

GSC Biol. Pharm. Sci.

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show abstract

“…At present, most studies on the stability of solid dispersion (CD) are focused on amorphous drugs, and the influencing factors mainly include: (1) Different preparation methods: there are significant differences in the stability of amorphous drugs prepared by different methods. The factors that lead to these differences include the residual composition of the crystal nucleus in the amorphous form (it is easy to induce crystallization in the crystal nucleus), the free energy state of an amorphous state, and the arrangement and orientation of microscopic molecules in amorphous drugs [15][16][17]. (2) Properties of drugs: Trasi et al found that amorphous compounds that are more prone to rapid crystallization usually have smaller relative molecular mass, higher melting point and density, and lower melting entropy and viscosity [18].…”

Section: Introductionmentioning

confidence: 99%

Influence Mechanism of Drug–Polymer Compatibility on Humidity Stability of Crystalline Solid Dispersion

Hu,

Yan,

Zhang

et al. 2023

Pharmaceuticals

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This study investigates the influence of humidity on the dissolution behavior and microstructure of drugs in crystalline solid dispersions (CSDs). Using Bifonazole (BFZ) as a model drug, CSDs were prepared through spray drying with carriers such as Poloxamer 188 (P188), Poloxamer 407 (P407), and polyethylene glycol 8000 (PEG8000). The solubilization effect and mechanism were initially evaluated, followed by an examination of the impact of humidity (RH10%) on the dissolution behavior of CSDs. Furthermore, the influence of humidity on the microstructure of CSDs was investigated, and factors affecting the humidity stability of CSDs were summarized. Significant enhancements in the intrinsic dissolution rate (IDR) of BFZ in CSDs were observed due to changes in crystalline size and crystallinity, with the CSD-P188 system exhibiting the best performance. Following humidity treatment, the CSD-P407 system demonstrated the least change in the IDR of BFZ, indicating superior stability. The CSD-P407 system was followed by the CSD-P188 system, with the CSD-PEG8000 system exhibiting the least stability. Further analysis of the microstructure revealed that while humidity had negligible effects on the crystalline size and crystallinity of BFZ in CSDs, it had a significant impact on the distribution of BFZ on the CSD surface. This can be attributed to the water’s potent plasticizing effect, which significantly alters the molecular mobility of BFZ. Additionally, the compatibility of the three polymers with BFZ differs, with CSD-P407 > CSD-P188 > CSD-PEG8000. Under the continuous influence of water, stronger compatibility leads to lower molecular mobility and more uniform drug distribution on the CSD surface. Enhancing the compatibility of drugs with polymers can effectively reduce the mobility of BFZ in CSDs, thereby mitigating changes caused by water and ultimately stabilizing the surface composition and dissolution behavior of drugs in CSDs.

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Drug–drug co-amorphous systems: An emerging formulation strategy for poorly water-soluble drugs

Wang,

Zhao,

et al. 2024

Drug Discovery Today

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A Comparison of Spray-Drying and Co-Precipitation for the Generation of Amorphous Solid Dispersions (ASDs) of Hydrochlorothiazide and Simvastatin

Cited by 5 publications

References 63 publications

A review on solubility enhancement technique for pharmaceutical drugs

A review on solubility enhancement technique for pharmaceutical drugs

Influence Mechanism of Drug–Polymer Compatibility on Humidity Stability of Crystalline Solid Dispersion

Drug–drug co-amorphous systems: An emerging formulation strategy for poorly water-soluble drugs

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