Solid Self-Microemulsifying Formulation for Candesartan Cilexetil |
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Authors: | Vijaykumar Nekkanti Pradeep Karatgi Raghavendra Prabhu Raviraj Pillai |
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Institution: | (1) NCE Product Development, Integrated Product Development Organization, Dr Reddy’s Laboratories Limited, Innovation Plaza, Bachupally, Qutubullapur, Hyderabad, 500 072, India;(2) CPS Product Development, Generic Product Development, Integrated Product Development Organization, Dr Reddy’s Laboratories Limited, Innovation Plaza, Bachupally, Qutubullapur, Hyderabad, 500 072, India; |
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Abstract: | Sparingly, water-soluble drugs such as candesartan cilexetil offer challenges in developing a drug product with adequate bioavailability.
The objective of the present study was to develop and characterize self-microemulsifying drug delivery system (SMEDDS) of
candesartan cilexetil for filling into hard gelatin capsules. Solubility of candesartan cilexetil was evaluated in various
nonaqueous careers that included oils, surfactants, and cosurfactants. Pseudoternary phase diagrams were constructed to identify
the self-microemulsification region. Four self-microemulsifying formulations were prepared using mixtures of oils, surfactants,
and cosurfactants in various proportions. The self-microemulsification properties, droplet size, and zeta potential of these
formulations were studied upon dilution with water. The optimized liquid SMEDDS formulation was converted into free flowing
powder by adsorbing onto a solid carrier for encapsulation. The dissolution characteristics of solid intermediates of SMEDDS
filled into hard gelatin capsules was investigated and compared with liquid formulation and commercial formulation to ascertain
the impact on self-emulsifying properties following conversion. The results indicated that solid intermediates showed comparable
rate and extent of drug dissolution in a discriminating dissolution medium as liquid SMEDDS indicating that the self-emulsifying
properties of SMEDDS were unaffected following conversion. Also, the rate and extent of drug dissolution for solid intermediates
was significantly higher than commercial tablet formulation. The results from this study demonstrate the potential use of
SMEDDS as a means of improving solubility, dissolution, and concomitantly the bioavailability. |
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