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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.


Dissolution profile of SMEDDS formulations and plain drug.
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fig4: Dissolution profile of SMEDDS formulations and plain drug.

Mentions: Dissolution studies were performed for the SMEDDS formulations in phosphate buffer pH 6.8, and the results were compared with the pure drug (Figure 4). There is no any significant difference in dissolution of four SMEDDS formulations. As the emulsification time is below 35 s, about 100% of the drug is released within 15 min in case of SMEDDS, while plain drug showed only 14.1% dissolution at the end of 15 min. The dissolution studies were conducted for 1 hr to observe the variation or occurrence of precipitation over a time. The in vitro dissolution studies indicate that formulation of OLM in the form of SMEDDS formulation enhances the dissolution properties.


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)

Dissolution profile of SMEDDS formulations and plain drug.
© Copyright Policy - open-access
Related In: Results  -  Collection

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

fig4: Dissolution profile of SMEDDS formulations and plain drug.
Mentions: Dissolution studies were performed for the SMEDDS formulations in phosphate buffer pH 6.8, and the results were compared with the pure drug (Figure 4). There is no any significant difference in dissolution of four SMEDDS formulations. As the emulsification time is below 35 s, about 100% of the drug is released within 15 min in case of SMEDDS, while plain drug showed only 14.1% dissolution at the end of 15 min. The dissolution studies were conducted for 1 hr to observe the variation or occurrence of precipitation over a time. The in vitro dissolution studies indicate that formulation of OLM in the form of SMEDDS formulation enhances the dissolution properties.

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.