Very fast dissolving acid carboxymethylcellulose-rifampicin matrix: Development and solid-state characterization

Controlling Particle Size and Release Kinetics in the Sustained Delivery of Oral Antibiotics Using pH-Independent Mucoadhesive Polymers

“…Most of the previous publications in which Rif is gastroprotected aim to obtain an improved drug solubility and a fast drug release in the stomach because under acidic conditions, the drug solubility increases, being principally absorbed in the stomach and duodenum. , Herein, we show that different drug release kinetics can be obtained under simulated intestinal conditions, avoiding gastric degradation.…”

“…Those reason can explain the differences on the encapsulation efficiencies observed for the electrosprayed particles compared to the nanoparticles obtained by emulsion. Despite this reduced drug loading, its release from the nanoparticles under simulated intestinal conditions was very rapid (Figure 3) which would overcome the large limitation of reduced water solubility for Rif and its reduced bioavailability being a class II drug in the Biopharmaceutics Classification System (BCS) 43 .…”

“…Most of the previous publications in which Rif is gastroprotected aim to obtain an improved drug solubility and a fast drug release in the stomach because under acidic conditions the drug solubility increases being principally absorbed in the stomach and duodenum 43,44 . Herein, we…”

“…Despite this reduced drug loading, the release from the nanoparticles under simulated intestinal conditions was very rapid (Figure 3), which would overcome the large limitation of reduced water solubility for Rif and its reduced bioavailability being a class II drug in the biopharmaceutics classification system. 43 Another advantage of using these micro-and nanoparticulated antibiotic carriers is that the residence time in the stomach would be shorter than the one obtained from conventional solid oral dosage forms having larger sizes (e.g., tablets or capsules) and, therefore, the acidic degradation of Rif (∼26.5% 9 ) would be reduced. The large surface area per volume ratio available in the micro-and nanoparticles would also reach homogeneously a large surface area in the intestinal lining instead of providing with a local release from the conventional solid oral dosage forms.…”

Application of 1-Dimensional and 2-Dimensional Solid-State Nuclear Magnetic Resonance Spectroscopy to the Characterization of Morphine, Morphine Hydrochloride, and Their Hydrates

“…Active pharmaceutical ingredients (API) may exist in various solid forms, which can lead to differences in the intermolecular interactions, affecting the internal energy and enthalpy, and the degree of disorder, affecting the entropy. 1 The development of new formulations or materials based on a particular API requires a detailed knowledge of the solid form because they can contain the API in a different crystalline form 2 or as an amorphous material, which could affect the interaction with the rest of the components. 3 In fact, different solid forms of an API often lead to differences in physicochemical properties, for example, solubility, dissolution rate, stability, and mechanical properties.…”