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Development of Pediatric Orodispersible Tablets Based on Efavirenz as a New Therapeutic Alternative

Author(s):

José Lourenço de Freitas Neto, Ilka do Nascimento Gomes Barbosa*, Camila Gomes de Melo, Matheus Alves Ângelos, Larissa Morgana dos Santos Mendes, Magda Rhayanny Assunção Ferreira, Larissa Araújo Rolim, Luiz Alberto Lira Soares, Rosali Maria Ferreira da Silva and Pedro José Rolim Neto   Pages 1 - 12 ( 12 )

Abstract:


Background: Efavirenz is the most used medication in the treatment of Acquired Immunodeficiency Syndrome (AIDS). The limited number of pediatric antiretroviral formulations approved by regulatory agencies is the most significant obstacle to adequate and efficient pharmacotherapy for this group of patients. The efavirenz has excellent therapeutic potential, but has low aqueous solubility/bioavailability.

Methods: To minimize these limitations, multicomponent systems with β-cyclodextrin and polyvinylpyrrolidone K-30 were obtained. Due to the limited number of pediatric antiretroviral formulations, the development of a pediatric orodispersible tablet is an alternative seen as easy to administer, since it disintegrates rapidly in the oral cavity. The multicomponent systems were obtained by the method of kneading and characterized by solubility test, X-ray diffraction, differential scanning calorimetry and infrared absorption spectroscopy by Fourier transform. The orodispersible tablets were prepared by direct compression. The quality control of hardness, friability, disintegration, and dissolution were performed. The influence of the components of the formulation on the characteristics of the tablets was evaluated through a 22 factorial design added with three central points, to compare the effect of the dependent variables on the responses.

Results: An increase in drug solubility was observed, with a decrease in crystallinity. Besides that, presented an excellent dissolution profile, with more than 83% of the drug's content dissolved in less than 15 minutes. Presented satisfactory disintegration time and friability.

Conclusion: It was observed that reduced concentrations of mannitol decrease the hardness and disintegration time of the formulations. The orodispersible tablet composed of efavirenz: β-cyclodextrin: polyvinylpyrrolidone, favors greater absorption and bioavailability. It has several advantages for pediatric patients, as the dosage form disintegrates quickly in the mouth and does not require water for administration, and which improves patient compliance with treatment.

Keywords:

AIDS, efavirenz, multicomponent systems, buccal administration.

Affiliation:

Laboratory of Medication Technology, Department of Pharmaceutical Sciences, Federal University of Pernambuco, Recife 50740-525, Pernambuco, Laboratory of Medication Technology, Department of Pharmaceutical Sciences, Federal University of Pernambuco, Recife 50740-525, Pernambuco, Laboratory of Medication Technology, Department of Pharmaceutical Sciences, Federal University of Pernambuco, Recife 50740-525, Pernambuco, Laboratory of Medication Technology, Department of Pharmaceutical Sciences, Federal University of Pernambuco, Recife 50740-525, Pernambuco, Laboratory of Medication Technology, Department of Pharmaceutical Sciences, Federal University of Pernambuco, Recife 50740-525, Pernambuco, Laboratory of Pharmacognosy, Department of Pharmaceutical Sciences, Federal University of Pernambuco, Recife 50740-525, Pernambuco, Analytical Center of Drugs, Medicines and Food, Federal University of San Francisco Valley, Petrolina 56304-205, Pernambuco, Laboratory of Pharmacognosy, Department of Pharmaceutical Sciences, Federal University of Pernambuco, Recife 50740-525, Pernambuco, Laboratory of Medication Technology, Department of Pharmaceutical Sciences, Federal University of Pernambuco, Recife 50740-525, Pernambuco, Laboratory of Medication Technology, Department of Pharmaceutical Sciences, Federal University of Pernambuco, Recife 50740-525, Pernambuco



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