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1.
ADMET DMPK ; 11(4): 615-627, 2023.
Artículo en Inglés | MEDLINE | ID: mdl-37937245

RESUMEN

Introduction: Olanzapine (OLZ) is a psychotropic class drug commonly used to treat schizophrenia, bipolar disorder, and acute manic episodes. It has less water solubility, resulting in a slow dissolution rate and oral bioavailability. Therefore, the development in oral dosage forms is required to enhance the drug solubility. Method: The solid dispersion of olanzapine is prepared by spray drying technique. The solution of polyvinylpyrrolidone K-30 (PVP K-30), mono amino glycyrrhizinate pentahydrate (GLY), OLZ and silicon dioxide were dissolved in distilled water and ethanol and spray dried to get the solid dispersion. Solid dispersion was characterized for surface morphology, solubility, encapsulation efficiency (EE), X-ray diffraction (X-RD), Differential Scanning Calorimeter (DSC) and drug-polymer interaction by Fourier transforms infrared spectroscopy. Results: The amorphous nature of the drug's incorporation in solid dispersion was confirmed by X-RD analysis. Prepared solid dispersion showed higher solubility, 11.51 mg, than pure OLZ (0.983 mg ml-1), while the range of EE was found to be between 64 to 90 %. Conclusions: The solubility and dissolution rate of the OLZ can effectively increase by spray-dried solid dispersion. Plackett-Burman screening design plays a vital role in understanding the effect of independent variables on EE and solubility.

2.
Mater Sci Eng C Mater Biol Appl ; 77: 282-292, 2017 Aug 01.
Artículo en Inglés | MEDLINE | ID: mdl-28532031

RESUMEN

In the present work, inclusion complex of famotidine (FMT) was prepared with (2-HydroxyPropyl)-ß-Cyclodextrin (HP-ß-CyD) and polyvinylpyrrolidone K-30 (PVP K-30) by spray drying technique to enhance the solubility of famotidine. FMT is a potent histamine H2-receptor antagonist having low solubility as well as oral bioavailability. In order to enhance the solubility of FMT, a quality by design (QbD) approach has been used by employing Plackett-Burman design (PBD). With the application of PBD, seven independent process variables were investigated and optimized for maximum solubility. The developed inclusion complex was characterized for solubility, encapsulation efficiency, FTIR, FESEM, XRD. In-vitro drug release study was also performed by preparing fast dissolving tablets of inclusion complex. Solubility of FMT in prepared complex was found 38 fold higher than pure FMT while %EE was found 92.10%. Statistical analysis of the data (ANOVA) indicates an adequate model fitting predicting the effect of process parameters affecting the solubility. In conclusion, spray dried inclusion complex can effectively increases the solubility as well as dissolution rate of the FMT and other active pharmaceutical ingredients in combination of the fast dissolving tablets.


Asunto(s)
Famotidina/química , 2-Hidroxipropil-beta-Ciclodextrina , Química Farmacéutica , Solubilidad , beta-Ciclodextrinas
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