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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.


FTIR spectra of olmesartan medoxomil and formulation.
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Related In: Results  -  Collection


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fig1: FTIR spectra of olmesartan medoxomil and formulation.

Mentions: FTIR Studies. An FTIR-8400S spectrophotometer (Shimadzu, Japan) equipped with attenuated total reflectance (ATR) accessory was used to obtain the infrared spectra of drug in the isotropic mixtures of excipients. Analysis of pure drug, Acrysol EL135, Transcutol P, Tween 80, physical admixtures of the drug with the excipients (in 1 : 2 ratio), and their comelts (in 1 : 2 ratio) were carried out using diffuse reflectance spectroscopy (DRS)-FTIR with KBr disc. All the samples were dried under vacuum prior to obtaining any spectra in order to remove the influence of residual moisture. For each the spectrum, 8 scans were obtained at a resolution of 4 cm−1 from a frequency range of 4000–600 cm−1 as shown in Figure 1.


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)

FTIR spectra of olmesartan medoxomil and formulation.
© Copyright Policy - open-access
Related In: Results  -  Collection

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

fig1: FTIR spectra of olmesartan medoxomil and formulation.
Mentions: FTIR Studies. An FTIR-8400S spectrophotometer (Shimadzu, Japan) equipped with attenuated total reflectance (ATR) accessory was used to obtain the infrared spectra of drug in the isotropic mixtures of excipients. Analysis of pure drug, Acrysol EL135, Transcutol P, Tween 80, physical admixtures of the drug with the excipients (in 1 : 2 ratio), and their comelts (in 1 : 2 ratio) were carried out using diffuse reflectance spectroscopy (DRS)-FTIR with KBr disc. All the samples were dried under vacuum prior to obtaining any spectra in order to remove the influence of residual moisture. For each the spectrum, 8 scans were obtained at a resolution of 4 cm−1 from a frequency range of 4000–600 cm−1 as shown in Figure 1.

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.