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Orally administered drugs primarily enter the systemic circulation via passive diffusion through the intestinal membranes. The drug's absorption is influenced by drug stability in the gastrointestinal GI tract, membrane permeability, the surface area available for absorption, luminal drug concentration, and residence time in the lumen. Drug permeability can be enhanced by adjusting the lipophilicity, polarity, or molecular size of the drug, promoting its passive transport across intestinal...
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Polymorphism refers to the existence of a drug substance in multiple crystalline forms, known as polymorphs. Recently, this term has been expanded to include solvates (forms containing a solvent), amorphous forms (non-crystalline forms), and desolvated solvates (forms from which the solvent has been removed).
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Solid dosage forms such as tablets and capsules undergo rigorous manufacturing processes to ensure stability and effectiveness. Their dissolution and absorption properties are influenced significantly by the choice of excipients (inactive ingredients that serve various roles in the formulation), and the methodology applied during production. The manufacturing parameters, such as compression force and granulation techniques, significantly affect dissolution rates. Elevated compression forces...
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Improving Lurasidone Hydrochloride's Solubility and Stability by Higher-Order Complex Formation with

María Elena Gamboa-Arancibia1, Nelson Caro2, Alexander Gamboa1,2

  • 1Facultad de Química y Biología, Universidad de Santiago de Chile, Av. Libertador Bernardo O'Higgins 3363, Estación Central, Santiago 9170022, Chile.

Pharmaceutics
|January 21, 2023
PubMed
Summary

Hydroxypropyl-β-cyclodextrin inclusion complexes significantly enhance lurasidone hydrochloride solubility and stability. This strategy improves drug formulation by preventing recrystallization and increasing drug dissolution, addressing common challenges with low-solubility drugs.

Keywords:
cyclodextrinhost–guest inclusionlurasidonepoorly water-soluble drugsstability

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Area of Science:

  • Pharmaceutical Sciences
  • Drug Delivery Systems
  • Physical Chemistry

Background:

  • Many new drugs, including lurasidone hydrochloride for schizophrenia and bipolar depression, exhibit poor solubility and stability, hindering effective pharmaceutical formulation.
  • Lurasidone hydrochloride's susceptibility to alkaline hydrolysis and oxidation limits its use in liquid dosage forms.
  • The biopharmaceutical classification system categorizes drugs with low solubility into Class II and IV, necessitating strategies to improve bioavailability.

Purpose of the Study:

  • To investigate the enhancement of lurasidone hydrochloride solubility and stability through the formation of higher-order inclusion complexes.
  • To explore various stoichiometric ratios of hydroxypropyl-β-cyclodextrin to lurasidone hydrochloride.
  • To characterize the resulting inclusion complexes and assess their impact on drug properties.

Main Methods:

  • Formation and characterization of hydroxypropyl-β-cyclodextrin-lurasidone hydrochloride inclusion complexes at different molar ratios (0.5-3).
  • Assessment of solubility and stability of the drug-cyclodextrin complexes.
  • Solid-state characterization using infrared spectroscopy, differential scanning calorimetry, and X-ray diffraction.
  • Phase solubility studies, 1H-NMR, and docking simulations to determine stoichiometry and binding interactions.

Main Results:

  • Inclusion complex formation dramatically increased lurasidone hydrochloride solubility, with higher ratios yielding greater solubility.
  • Characterization confirmed the drug's transition from crystalline to amorphous state within the complexes, inhibiting recrystallization.
  • Phase solubility, NMR, and computational studies indicated a primary 1:1 stoichiometric ratio, with potential for a 1:2 complex enhancing stability.

Conclusions:

  • Higher-order inclusion complexes of lurasidone hydrochloride with hydroxypropyl-β-cyclodextrin are a successful strategy for improving drug solubility and stability.
  • The amorphous state and inhibited recrystallization contribute to enhanced drug dissolution and formulation potential.
  • This approach offers a viable solution for overcoming formulation challenges associated with poorly soluble and unstable drugs like lurasidone hydrochloride.