Enhanced Solubility of Albendazole in Cyclodextrin Inclusion Complex: A Molecular Modeling Approach and Physicochemical Evaluation.

BACKGROUND: Albendazole (ABZ) is the drug of choice for the treatment of a variety of human and veterinary parasites. However, it has low aqueous solubility and low bioavailability. Cyclodextrins (CD) are pharmaceutical excipients with the ability to modulate the solubilization property of hydrophobic molecules. OBJECTIVE: The aim of the study was to analyze through in vitro and in silico studies (Autodock Vina software and CycloMolder platform) the formation of inclusion complexes between ABZ, ß-cyclodextrin (ß-CD) and its derivatives Methyl-ß-cyclodextrin (M-ß-CD) and Hydroxypropyl-ß-cyclodextrin (HP-ß-CD). METHODS: The most stable inclusion complexes were produced by the kneading method and characterized by Fourier Transform Infrared Spectroscopy (FTIR), Differential Scanning Calorimetry (DSC), X-Ray Diffraction (XRD), determination of the ABZ content and in vitro dissolution profile. RESULTS: Molecular modeling revealed that inclusion complexes between HP-ß-CD:ABZ (in the proportion 1:1 and 2:1) presented the lowest formation energy and the highest number of intermolecular interactions, showing that the use of more cyclodextrins does not generate gains in the stability of the complex. On the characterization tests, the complexes experimentally obtained by the kneading method demonstrated highly suggestive parameters, including ABZ in HP-ß-CD in both molar proportions, suppression of bands in the infrared spectrum, displacement of the drug's melting temperature in DSC, crystallinity halos instead of the characteristic peaks of ABZ crystals in the XRD and a release of more than 80% of ABZ in less than 5 minutes, dissolution efficiency of up to 92%. CONCLUSION: In silico studies provided a rational selection of the appropriate complexes of cyclodextrin, enabling the elaboration of more targeted complexes, decreasing time and costs for elaboration of new formulations, thereby increasing the oral biodisponibility of ABZ.

[Medical prescriptions: adequate orientation to medicine use?]. / Prescrição médica: orientações adequadas para o uso de medicamentos?

During physician's consultation, the lack of adequate information on medication to the patient is a major problem to reach the correct pharmacotherapy. This study aims at assessing the patient knowledge about prescribed drugs. In order to proceed the investigation, interviews were performed about type of medication, dosage, administration schedule, purpose, duration of treatment and side effects. From 199 patients interviewed after they had received a prescription, 53.8% didn't have any information about the medicine, 20.3% didn't know the dosage and 25.4% didn't know the medication schedule. The purpose of the medication was the information with the highest percentage of correct answers, with 75.1% of the patients showing good level of knowledge. Regarding to the duration of the treatment and side effects, 57.4% and 94.4% of the patients, respectively, didn't present any correct information. Results suggest that the majority of the patients didn't have sufficient and safe knowledge to the use of prescribed medication.