Determination of oleanolic acid in human plasma and study of its pharmacokinetics in Chinese healthy male volunteers by HPLC tandem mass spectrometry

Song, Min; Hang, Taijun; Wang, Ying; Jiang, Li; Wu, Xiao-luan; Zhang, Zhengxing; Shen, Jian‐Yong; Zhang, Yindi

doi:10.1016/j.jpba.2005.06.034

Cited by 88 publications

(73 citation statements)

References 3 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The absorption of OA from the SNEDDS formulation resulted in a 2.4-fold increase in bioavailability (as calculated by AUC), although the SNEDDS formulation did not significantly change the C max compared with the tablet formulation (p>0.05). In addition, large variability of the plasma concentrations from both formulae were observed, which was consistent with previous pharmacokinetic studies in human and rat (5,6). It is expected that the poor oral absorption and individual variation may be the reason that lead to these large variability.…”

Section: Bioavailability Studysupporting

confidence: 89%

“…Simulated gastric fluid was prepared according to the USP 30-NF25 (2007). Samples (5 ml) were withdrawn at regular time intervals (5,10,20,30,45,60,90, and 120 min) and filtered using a 0.45-μm filter. An equal volume of the dissolution medium was added to maintain the volume constant.…”

Section: In Vitro Drug Release Studymentioning

confidence: 99%

“…During in vitro dissolution study, less than 1 μg/ml oleanolic acid was dissolved from raw solid form into an aqueous buffer (pH 1 or 7) after 2 h (4). In a human pharmacokinetic study, T max was reported to be 5.2 h after oral administration of oleanolic acid capsule, indicating that it had delayed in vivo absorption (5). In addition, absolute oral bioavailability of oleanolic acid was only 0.7% for oral doses of 25 and 50 mg/kg in rat, and it has been suggested that the poor oral bioavailability of oleanolic acid is due to poor solubility/dissolution and extensive metabolic clearance (6).…”

Section: Introductionmentioning

confidence: 99%

See 2 more Smart Citations

Formulation Development and Bioavailability Evaluation of a Self-Nanoemulsified Drug Delivery System of Oleanolic Acid

Xi¹,

et al. 2009

View full text Add to dashboard Cite

Abstract. This study aims to formulate and evaluate bioavailability of a self-nanoemulsified drug delivery system (SNEDDS) of a poorly water-soluble herbal active component oleanolic acid (OA) for oral delivery. Solubility of OA under different systems was determined for excipient selection purpose. Four formulations, where OA was fixed at the concentration of 20 mg/g, were prepared utilizing Sefsol 218 as oil phase, Cremophor EL and Labrasol as primary surfactants, and Transcutol P as cosurfactant. Pseudoternary phase diagrams were constructed to identify self-emulsification regions for the rational design of SNEDDS formulations. Sefsol 218 was found to provide the highest solubility among all medium-chained oils screened. Efficient self-emulsification was observed for the systems composing of Cremophor EL and Labrasol. The surfactant to cosurfactant ratio greatly affected the droplet size of the nanoemulsion. Based on the outcomes in dissolution profiles, stability data, and particle size profiles, three optimized formulations were selected: Sefsol 218/Cremophor EL/Labrasol (50:25:25, w/w), Sefsol 218/Cremophor EL/Labrasol/Transcutol P (50:20:20:10, w/w), and Sefsol 218/Cremophor EL/Labrasol/Transcutol P (50:17.5:17.5:15, w/w). Based on the conventional dissolution method, a remarkable increase in dissolution was observed for the SNEDDS when compared with the commercial tablet. The oral absorption of OA from SNEDDS showed a 2.4-fold increase in relative bioavailability compared with that of the tablet (p<0.05), and an increased mean retention time of OA in rat plasma was also observed compared with that of the tablet (p<0.01). These results suggest the potential use of SNEDDS to improve dissolution and oral bioavailability for poorly water-soluble triterpenoids such as OA.

show abstract

Section: Bioavailability Studysupporting

confidence: 89%

Section: In Vitro Drug Release Studymentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

See 1 more Smart Citation

Formulation Development and Bioavailability Evaluation of a Self-Nanoemulsified Drug Delivery System of Oleanolic Acid

Xi¹,

et al. 2009

View full text Add to dashboard Cite

show abstract

“…Despite the limited number of studies in humans, it is accepted that OA is a safe phytochemical. None of these trials have recorded significant adverse effects (Xu, 1980;Minich et al, 2007;Song et al, 2006;Chen et al, 2010;Rada et al, 2015). Nevertheless, further investigations in humans will be necessary to extend the use of OA in the design of new drugs and functional foods, which allow for personalized diets and nutrigenomic approaches for the prevention of high-prevalence chronic disorders such as diabetes.…”

Section: Discussionmentioning

confidence: 99%

Free radical scavenging and α-glucosidase inhibition, two potential mechanisms involved in the anti-diabetic activity of oleanolic acid

et al. 2016

View full text Add to dashboard Cite

SUMMARY:This work investigates the role of oleanolic acid (OA), isolated from the olive (Olea europaea L.) leaf, as a radical scavenger and inhibitor of the hydrolyzing enzymes of dietary carbohydrates. New evidence is provided showing that OA may capture 2,2'-azino-bis (3-ethylbenzothiazoline-6-sulphonic acid) and peroxyl radicals, and also exert a strong and non-competitive inhibition of α-glucosidase (IC 50 10.11 ± 0.30 µM). The kinetic and spectrometric analyses performed indicate that OA interacts with this enzyme inside a hydrophobic pocket, through an endothermic and non spontaneous process of a hydrophobic nature. These are two possible mechanisms by which OA may facilitate a better control of post-prandial hyperglycaemia and oxidative stress, so contributing to preserving insulin signalling. Obesity, insulin resistance and Type 2 Diabetes Mellitus are considered the first pandemics of the 21st century. In this sense, OA might be used in future preventive and therapeutic strategies, as an ingredient in new drugs and functional foods.KEYWORDS: Anti-diabetic activity; Antioxidant; α-glucosidase inhibitor; Olea europaea; Oleanolic acid RESUMEN: La Captación de radicales libres y la inhibición de α-glucosidasa, dos posibles mecanismos involucrados en la actividad antidiabética del ácido oleanólico. Este trabajo estudia el papel del ácido oleanólico (OA), aislado de la hoja de olivo, como secuestrador de radicales libres e inhibidor de enzimas implicados en la hidrolisis de los carbohidratos de la dieta, dos mecanismos por los que el triterpeno podría mitigar la hiperglicemia postprandial y el estrés oxidativo. Se aportan nuevas evidencias que muestran que el OA puede capturar radicales ácido 2,2'-azino-bis-(3-etilbenzotiazolín)-6-sulfónico y peroxilo, y que ejerce una potente inhibición nocompetitiva de α-glucosidasa (IC 50 10.11±0.30 µM). El análisis cinético y espectrométrico llevado a cabo indica que OA interacciona con este enzima en el interior de un bolsillo hidrofóbico, mediante un proceso endotér-mico no espontáneo, de naturaleza hidrofóbica. Estos son dos posibles mecanismos por los cuales el OA puede facilitar un mejor control de la hiperglucemia postprandial y el estrés oxidativo, lo que contribuye a preservar la señalización de la insulina. La obesidad, la resistencia a la insulina y la diabetes mellitus tipo 2 se consideran la primera pandemia del siglo XXI. En este sentido, el OA podría ser utilizado en futuras estrategias preventivas y terapéuticas, como ingrediente de nuevos fármacos y alimentos funcionales. Free radical scavenging and α-glucosidase inhibition, two potential mechanisms involved in the anti-diabetic activity of oleanolic acid. Grasas Aceites 67 (3): e142. doi: http://dx

show abstract

“…1,2 OA has multiple pharmaceutical functions such as anti-inflammatory, 3,4 hepato-protection, 1 and enhancement of human body defense systems. 5 Because OA is poorly water soluble, it is important to introduce effective methods to enhance its dissolution.…”

Section: Introductionmentioning

confidence: 99%

Improved dissolution of oleanolic acid with ternary solid dispersions

Liu

Wang

2007

AAPS PharmSciTech

View full text Add to dashboard Cite

The purpose of this study was to enhance the dissolution of oleanolic acid by solid dispersions consisting of the drug, a polymeric carrier, and a surfactant. Binary solid dispersions consisting of oleanolic acid and polyvinylpyrrolidone were prepared for comparison. Polysorbate 80, a nonionic surfactant, was incorporated into binary solid dispersions as the third component to prepare ternary solid dispersions. Solid dispersions were characterized by differential scanning calorimetry, Fourier transform infrared spectroscopy, and dissolution tests. The crystallinization of OA was prohibited in solid dispersions. Both the binary and ternary solid dispersions enhanced the dissolution of OA. Moreover, the dissolution of ternary solid dispersion was faster compared with that of binary solid dispersion. Polysorbate 80 played an important positive role in dissolution of the solid dispersion.

show abstract

Determination of oleanolic acid in human plasma and study of its pharmacokinetics in Chinese healthy male volunteers by HPLC tandem mass spectrometry

Cited by 88 publications

References 3 publications

Formulation Development and Bioavailability Evaluation of a Self-Nanoemulsified Drug Delivery System of Oleanolic Acid

Formulation Development and Bioavailability Evaluation of a Self-Nanoemulsified Drug Delivery System of Oleanolic Acid

Free radical scavenging and α-glucosidase inhibition, two potential mechanisms involved in the anti-diabetic activity of oleanolic acid

Improved dissolution of oleanolic acid with ternary solid dispersions

Contact Info

Product

Resources

About