Amorphous Drug Solubility and Absorption Enhancement

Enhancing the Solubility of Curcumin Using a Solid Dispersion System with Hydroxypropyl-β-Cyclodextrin Prepared by Grinding, Freeze-Drying, and Common Solvent Evaporation Methods

“…Based on the solubility and permeability of active pharmaceutical ingredients (APIs) that regulate drug absorption, Amidon et al divided drugs into the following four categories [ 1 ]: class I (high solubility–high permeability), class II (low solubility–high permeability), class III (high solubility–low permeability), and class IV (low solubility–low permeability). Approximately 70% of new pharmaceutical substances are classified as class II and class IV drugs, meaning they have poor aqueous solubility [ 2 ]. To address this, one of the basic goals of drug formulations is to improve the solubility of these two drug classes.…”

Preparation and Characterization of Solid Dispersions Composed of Curcumin, Hydroxypropyl Cellulose and/or Sodium Dodecyl Sulfate by Grinding with Vibrational Ball Milling

“…The temperature was controlled at 37 ± 0.5 • C and the rotating paddle speed was set at 100 rpm throughout this study. At defined time intervals (1,3,5,10,15,30,45,60, 90 and 120 min), 5 mL aliquots were withdrawn, and an equal volume of fresh DW was added. The sample solutions were filtered through a 0.45-µm membrane filter and assayed for CUR content using UV-visible spectroscopy at 432 nm as described in the section "Quantification of CUR".…”

“…Solubility is one of the most important physicochemical properties affecting drug bioavailability. It is estimated that approximately 70% of the current new drug candidates have poor solubility [1]. One methodology that can enhance the solubility of poorly water-soluble drugs and their bioavailability is amorphization [2][3][4][5].…”

“…Amorphous substances can be classified into two categories: molecularly pure drugs and solid dispersions (SDs), where the active pharmaceutical ingredient (API) is dispersed within a carrier(s). Vo et al have demonstrated that SDs can be categorized into four distinct subcategories [10]: (1) SDs that use a crystalline carrier, such as urea [11][12][13] or sugar [11]; (2) SDs that use a polymeric carrier, such as povidone [14], polyethylene glycol [15], hydroxypropyl cellulose [16] or cyclodextrin [17][18][19][20][21]; (3) SDs that use a carrier with surface activity, such as surfactant(s) or a mixture of polymers and surfactants [22]; and (4) controlled release SDs or SDs that use swellable/water insoluble polymers, such as Eudragit ® [23] and Carbopol ® [23].…”

Is it possible to predict the stability of a crystal structure under the influence of pressure? Quantum chemical study of ibuprofen crystals

“…In both cases, changes in the crystal structure are accompanied by changes in bioavailability, solubility, permeability, compressibility, and other characteristics of drugs. 22–26 Therefore, the study of the capability of the crystal structure to be deformed is of great importance for the pharmaceutical industry.…”