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Development of Pediatric Orodispersible Tablets Based on Efavirenz as a New Therapeutic Alternative.
Curr HIV Res. 2020 Jul 02 [Online ahead of print]CH

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.

Authors+Show Affiliations

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

Pub Type(s)

Journal Article

Language

eng

PubMed ID

32614748

Citation

de Freitas Neto, José Lourenço, et al. "Development of Pediatric Orodispersible Tablets Based On Efavirenz as a New Therapeutic Alternative." Current HIV Research, 2020.
de Freitas Neto JL, do Nascimento Gomes Barbosa I, de Melo CG, et al. Development of Pediatric Orodispersible Tablets Based on Efavirenz as a New Therapeutic Alternative. Curr HIV Res. 2020.
de Freitas Neto, J. L., do Nascimento Gomes Barbosa, I., de Melo, C. G., Ângelos, M. A., Dos Santos Mendes, L. M., Ferreira, M. R. A., Rolim, L. A., Soares, L. A. L., da Silva, R. M. F., & Neto, P. J. R. (2020). Development of Pediatric Orodispersible Tablets Based on Efavirenz as a New Therapeutic Alternative. Current HIV Research. https://doi.org/10.2174/1570162X18666200702130449
de Freitas Neto JL, et al. Development of Pediatric Orodispersible Tablets Based On Efavirenz as a New Therapeutic Alternative. Curr HIV Res. 2020 Jul 2; PubMed PMID: 32614748.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Development of Pediatric Orodispersible Tablets Based on Efavirenz as a New Therapeutic Alternative. AU - de Freitas Neto,José Lourenço, AU - do Nascimento Gomes Barbosa,Ilka, AU - de Melo,Camila Gomes, AU - Ângelos,Matheus Alves, AU - Dos Santos Mendes,Larissa Morgana, AU - Ferreira,Magda Rhayanny Assunção, AU - Rolim,Larissa Araújo, AU - Soares,Luiz Alberto Lira, AU - da Silva,Rosali Maria Ferreira, AU - Neto,Pedro José Rolim, Y1 - 2020/07/02/ PY - 2020/02/04/received PY - 2020/05/28/revised PY - 2020/06/09/accepted PY - 2020/7/3/entrez PY - 2020/7/3/pubmed PY - 2020/7/3/medline KW - AIDS KW - buccal administration. KW - efavirenz KW - multicomponent systems JF - Current HIV research JO - Curr. HIV Res. N2 - 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. SN - 1873-4251 UR - https://www.unboundmedicine.com/medline/citation/32614748/Development_of_Pediatric_Orodispersible_Tablets_Based_on_Efavirenz_as_a_New_Therapeutic_Alternative DB - PRIME DP - Unbound Medicine ER -