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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.


Particle size distribution of batches S1 to S4.
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Related In: Results  -  Collection


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fig3: Particle size distribution of batches S1 to S4.

Mentions: In a similar manner, calculations for the other ratios of oil and Smix were also done. For each Smix ratio, a separate phase diagram was constructed, and for each phase diagram visual observations were recorded. The pseudoternary phase diagram (Figure 3) was constructed using CHEMIX software based on the visual observations noted. In Figure 3, only microemulsion points are plotted (shaded area), so that there is no overcrowding of the phases in the diagram, as for formulation development only the microemulsion area is of interest.


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)

Particle size distribution of batches S1 to S4.
© Copyright Policy - open-access
Related In: Results  -  Collection

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

fig3: Particle size distribution of batches S1 to S4.
Mentions: In a similar manner, calculations for the other ratios of oil and Smix were also done. For each Smix ratio, a separate phase diagram was constructed, and for each phase diagram visual observations were recorded. The pseudoternary phase diagram (Figure 3) was constructed using CHEMIX software based on the visual observations noted. In Figure 3, only microemulsion points are plotted (shaded area), so that there is no overcrowding of the phases in the diagram, as for formulation development only the microemulsion area is of interest.

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.