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Preparation and Characterization of Self-Microemulsifying Drug Delivery System of Olmesartan Medoxomil for Bioavailability Improvement.

Prajapati ST, Joshi HA, Patel CN - J Pharm (Cairo) (2012)

Bottom Line: The optimized formulation S2 contained OLM (20 mg), Tween 80 (33%v/v), Transcutol P (33%v/v), and Acrysol EL 135 (34%v/v) had shown the smallest particle size, maximum solubility, less emulsification time, good optical clarity, and in vitro release.The in vitro and ex vivo diffusion rate of the drug from the SMEDDS was significantly higher than that of the plain drug suspension.It was concluded that SMEDDS would be a promising drug delivery system for poorly water-soluble drugs by the oral route.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutics and Pharmaceutical Technology, Shri Sarvajanik Pharmacy College, Near Arvind Buag, Gujarat, Mehsana 384001, India.

ABSTRACT
Olmesartan medoxomil (OLM) is an angiotensin II receptor blocker (ARB) antihypertensive agent administered orally that has absolute bioavailability of only 26% due to the poor aqueous solubility (7.75 μg/ml). The aim of the present investigation was to develop a self-microemulsifying drug delivery system (SMEDDS) to enhance the oral absorption of OLM. The solubility of OLM in various oils, surfactants, and cosurfactants was determined. Pseudoternary phase diagrams were constructed using Acrysol EL 135, Tween 80, Transcutol P, and distilled water to identify the efficient self-microemulsification region. Prepared SMEDDS was further evaluated for its emulsification time, drug content, optical clarity, droplet size, zeta potential, in vitro dissolution, and in vitro and ex vivo drug diffusion study. The optimized formulation S2 contained OLM (20 mg), Tween 80 (33%v/v), Transcutol P (33%v/v), and Acrysol EL 135 (34%v/v) had shown the smallest particle size, maximum solubility, less emulsification time, good optical clarity, and in vitro release. The in vitro and ex vivo diffusion rate of the drug from the SMEDDS was significantly higher than that of the plain drug suspension. It was concluded that SMEDDS would be a promising drug delivery system for poorly water-soluble drugs by the oral route.

No MeSH data available.


In vitro drug diffusion study of optimized SMEDDS (batch S2) formulation and plain drug.
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Related In: Results  -  Collection


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fig5: In vitro drug diffusion study of optimized SMEDDS (batch S2) formulation and plain drug.

Mentions: In vitro diffusion of plain drug suspension and optimized SMEDDS is shown in Figure 5. The plain drug suspension was prepared by dispersing 20 mg of the drug in 5 mL of the distilled water. In vitro drug diffusion profiles are strong indicators of bioavailability. The amount of drug diffuse from SMEDDS was doubled than that of the plain OLM suspension. After 8 hours, 86.4% the drug was diffused from the SMEDDS, as compared with 46.39% diffused from the OLM suspension, indicating almost a twofold increase in the diffusion. The increased solubility and the dissolution rate are the main factors responsible for increased diffusion rates.


Preparation and Characterization of Self-Microemulsifying Drug Delivery System of Olmesartan Medoxomil for Bioavailability Improvement.

Prajapati ST, Joshi HA, Patel CN - J Pharm (Cairo) (2012)

In vitro drug diffusion study of optimized SMEDDS (batch S2) formulation and plain drug.
© Copyright Policy - open-access
Related In: Results  -  Collection

Show All Figures
getmorefigures.php?uid=PMC4595970&req=5

fig5: In vitro drug diffusion study of optimized SMEDDS (batch S2) formulation and plain drug.
Mentions: In vitro diffusion of plain drug suspension and optimized SMEDDS is shown in Figure 5. The plain drug suspension was prepared by dispersing 20 mg of the drug in 5 mL of the distilled water. In vitro drug diffusion profiles are strong indicators of bioavailability. The amount of drug diffuse from SMEDDS was doubled than that of the plain OLM suspension. After 8 hours, 86.4% the drug was diffused from the SMEDDS, as compared with 46.39% diffused from the OLM suspension, indicating almost a twofold increase in the diffusion. The increased solubility and the dissolution rate are the main factors responsible for increased diffusion rates.

Bottom Line: The optimized formulation S2 contained OLM (20 mg), Tween 80 (33%v/v), Transcutol P (33%v/v), and Acrysol EL 135 (34%v/v) had shown the smallest particle size, maximum solubility, less emulsification time, good optical clarity, and in vitro release.The in vitro and ex vivo diffusion rate of the drug from the SMEDDS was significantly higher than that of the plain drug suspension.It was concluded that SMEDDS would be a promising drug delivery system for poorly water-soluble drugs by the oral route.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutics and Pharmaceutical Technology, Shri Sarvajanik Pharmacy College, Near Arvind Buag, Gujarat, Mehsana 384001, India.

ABSTRACT
Olmesartan medoxomil (OLM) is an angiotensin II receptor blocker (ARB) antihypertensive agent administered orally that has absolute bioavailability of only 26% due to the poor aqueous solubility (7.75 μg/ml). The aim of the present investigation was to develop a self-microemulsifying drug delivery system (SMEDDS) to enhance the oral absorption of OLM. The solubility of OLM in various oils, surfactants, and cosurfactants was determined. Pseudoternary phase diagrams were constructed using Acrysol EL 135, Tween 80, Transcutol P, and distilled water to identify the efficient self-microemulsification region. Prepared SMEDDS was further evaluated for its emulsification time, drug content, optical clarity, droplet size, zeta potential, in vitro dissolution, and in vitro and ex vivo drug diffusion study. The optimized formulation S2 contained OLM (20 mg), Tween 80 (33%v/v), Transcutol P (33%v/v), and Acrysol EL 135 (34%v/v) had shown the smallest particle size, maximum solubility, less emulsification time, good optical clarity, and in vitro release. The in vitro and ex vivo diffusion rate of the drug from the SMEDDS was significantly higher than that of the plain drug suspension. It was concluded that SMEDDS would be a promising drug delivery system for poorly water-soluble drugs by the oral route.

No MeSH data available.