Related Experiment Video
Updated: Apr 15, 2026
07:58
Formulation and Characterization of Bioactive Agent Containing Nanodisks
Published on: March 17, 2023
1.8K
Pharmaceutical Co-Crystal Formulation of Rivaroxaban with Niacinamide: Preparation, Characterization, and In Vitro
Cristina Solomon1, Iulian Sarbu2, Valentina Anuța3
1Faculty of Pharmacy, "Carol Davila" University of Medicine and Pharmacy, 6 Traian Vuia St., 020956 Bucharest, Romania.
Materials (Basel, Switzerland)
|April 14, 2026
Summary
Forming rivaroxaban-niacinamide co-crystals significantly improved the drug's dissolution rate and solubility. Stoichiometric ratios are key for enhancing rivaroxaban's (RIV) physicochemical and biopharmaceutical properties.
Area of Science:
- Pharmaceutical Sciences
- Materials Science
Background:
- Rivaroxaban (RIV) is a potent oral anticoagulant with poor water solubility, limiting its bioavailability.
- Co-crystallization is a strategy to enhance the physicochemical and biopharmaceutical properties of poorly soluble drugs.
Purpose of the Study:
- To investigate the co-crystallization of rivaroxaban with niacinamide (NIA) to improve RIV's dissolution rate and aqueous solubility.
- To explore the effect of different molar ratios (1:1 and 1:2) on the formation and properties of rivaroxaban-niacinamide co-crystals.
Main Methods:
- Solvent evaporation technique was employed for co-crystal formation.
- Characterization of co-crystals using scanning electron microscopy (SEM), Fourier-transform infrared spectroscopy (FTIR), powder X-ray diffraction (XRD), and thermal analysis.
- In vitro dissolution studies were conducted to assess the dissolution rate enhancement.
Main Results:
- Successful formation of new rivaroxaban-niacinamide (RIV-NIA) co-crystalline phases (F1 and F3) was confirmed by various analytical techniques.
- Co-crystals exhibited significantly enhanced in vitro dissolution rates compared to pure rivaroxaban.
- Stoichiometric variation (1:1 and 1:2 molar ratios) influenced co-crystal performance and solubility improvement.
Conclusions:
- Niacinamide is an effective co-former for improving the dissolution and physicochemical properties of rivaroxaban.
- Co-crystallization with niacinamide offers a promising approach to enhance the biopharmaceutical profile of rivaroxaban.
- Stoichiometry plays a critical role in optimizing the performance of drug co-crystals.
More Related Videos
Related Concept Videos
01:18Anticoagulant Drugs: Vitamin K Antagonists and Direct Oral Anticoagulants
2.8K
Oral anticoagulants are vital tools in preventing and treating blood clotting disorders. This diverse class of medications can be categorized as vitamin K antagonists, exemplified by warfarin, and direct thrombin inhibitors (DTIs), such as dabigatran, as well as factor Xa inhibitors, including rivaroxaban.
Warfarin, a prominent vitamin K antagonist family member, exerts its effect by inhibiting the enzyme VKORC1 (vitamin K epoxide reductase complex 1). By hindering this enzyme, warfarin...
Warfarin, a prominent vitamin K antagonist family member, exerts its effect by inhibiting the enzyme VKORC1 (vitamin K epoxide reductase complex 1). By hindering this enzyme, warfarin...
2.8K
01:30Anticoagulant Drugs: Low-Molecular-Weight Heparins
2.5K
Hemostasis is a crucial process that prevents excessive blood loss from damaged blood vessels. It involves various mechanisms such as vasoconstriction, platelet adhesion and activation, and fibrin formation. The importance of each mechanism depends on the type of vessel injury. In contrast, thrombosis is the abnormal formation of a blood clot within the blood vessels, leading to potential complications if the clot obstructs blood flow. Thrombosis can be caused by increased coagulability of the...
2.5K
01:26Pharmaceutical Equivalents
267
As defined by regulatory standards, pharmaceutical equivalents require generic drug products to have identical dosage forms and chemically identical active pharmaceutical ingredients (APIs). They must adhere to compendial or applicable standards for potency, content uniformity, disintegration times, and dissolution rates. In the case of modified-release dosage forms, variations in drug content are permissible as long as the delivered amount remains consistent with the innovator drug product.
267
01:27Pharmaceutical Alternatives: Polymorphic Form-Related and Particle Size-Related Therapeutic Nonequivalence
224
Changes in polymorphic forms can significantly influence the bioavailability of poorly soluble drugs. Although the FDA defines pharmaceutical equivalence based on having the same active ingredient, dosage form, and route of administration, it does not automatically disqualify products with different polymorphic forms. This means two products with different polymorphs can still be deemed pharmaceutically equivalent. However, polymorphic differences can affect properties like wettability,...
224
01:26Pharmacokinetics: Drug–Food and Drug–Viral Interactions
626
A drug interaction occurs when the concurrent use of another drug, food, or an external substance alters the pharmacological activity of a drug. This interaction can modify the action of the original drug, affecting its effectiveness and safety.Drug–food interactions are significant as they impact drug absorption, metabolism, and excretion. For example, grapefruit juice is a well-known disruptor of drug metabolism. It inhibits the cytochrome P450 3A4 enzyme, crucial for the metabolism of...
626
01:05Bioavailability Enhancement: Drug Stability Enhancement and GI Retention
314
Improving a drug's stability in the gastrointestinal (GI) tract is paramount for enhancing its bioavailability and therapeutic effectiveness. Various strategies are employed to protect the drug from the harsh gastric milieu and to ensure its release and absorption at the desired site within the GI tract.Polymer coatings are one such method used to shield drugs from the stomach's acidic environment. By preventing premature drug release, these coatings improve the bioavailability of unstable...
314