Experimental design approach for development of novel microemulsion system and immediate release self microemulsifying tablet of nebivolol HCl
Document title: Experimental design approach for development of novel microemulsion system and immediate release self microemulsifying tablet of nebivolol HCl
Journal: Brazilian Journal of Pharmaceutical Sciences
Database: PERIÓDICA
System number: 000451362
ISSN: 1984-8250
Authors: 1
1
1
Institutions: 1Rashtrasant Tukadoji Maharaj Nagpur University, Department of Pharmaceutical Sciences, Nagpur, Maharashtra. India
Year:
Volumen: 56
Country: Brasil
Language: Inglés
Document type: Artículo
Approach: Experimental, aplicado
English abstract The objective of this study was to determine specific combination of pharmaceutical excipients that lead to formulation of efficient nebivolol hydrochloride SMEDDS and its subsequent formulation into IR-SET (Immediate release- Self emulsifying tablet) which will enhance its solubility and dissolution. Solubility and Pseudo-ternary phase studies were carried out to identify the excipients showing highest solubility and to identify the zone of microemulsion with selected ingredients. Liquid-SMEDDS (L-SMEDDS) were optimized for Concentration of oil(X1) and Smix(X2) and formulated using a combination of Kollisolv GTA as oil, Tween 80 as surfactant and propylene glycol as co-surfactant which gave smaller droplet size(Y1) 55.98nm , Emulsification time (Y2) 16±1.5 s,% transmittance (Y3) 99.94±0.47%. Neusilin US2 was used as solid carrier for solidification of L-SMEDDS in to Solid-SMEDDS (S-SMEDDS) by adsorption technique. IR-SET of nebivolol were formulated with S-SMEDDS and optimized for the concentration of binder (X1) (PVP K30) and superdisintegrant (X2) (KOLLIDON CL) which showed low Disintegration time (Y1) (92±0.5s) and low Friability(Y2)(0.424±0.03%). Also the DSC and XRD data revealed the molecular state of the drug in S-SMEDDS. The extent of in-vivo drug release and ex-vivo diffusion values from L-SMEDDS and IR-SET was much higher than pure drug and marketed tablet. In conclusion, the results showed potential of SMEDDS to improve solubility and thus the bioavailability
Disciplines: Química
Keyword: Química farmacéutica,
Tabletas,
Microemulsiones,
Tabletas microemulsificantes,
Clorhidrato de nebivolol,
Diseño factorial
Keyword: Medicinal chemistry,
Tablets,
Microemulsions,
Microemulsifying tablets,
Nebivolol hydrochloride,
Factorial design
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