Resveratrol

 

Resveratrol, a polyphenol present in several plants including grapes and peanuts has been shown to have a number of physiological properties that could be useful in human medicine. Several in vitro studies have shown that Resveratrol may have cardioprotective, antioxidant, anti-inflammatory, neuro-protective and anti-aging activities.

 

Resveratrol has high oral absorption but undergoes rapid and extensive metabolism. This results in only trace amounts of un-changed Resveratrol in the systemic circulation, which has raised concerns regarding its systemic efficacy. After oral administration, the amount of free Resveratrol or even was not detectable.

 

MicroActive Resveratrol SR improves on Standard Resveratrol through the following:

 

Sustained release

 

Increased systemic exposure

 

High bioavailability

 

MicroActive Resveratrol SR Support: Dissolution Studies

 

MicroActive Resveratrol SR was compared to 99% Resveratrol powder in dissolution studies that approximated transport through both the gastric and inestinal environments.

 

The dissolution study was performed using the USP method in a dissolution tester. Samples equivalent to 25 mg Resveratrol filled in hard gelatin capsules were introduced in 750 ml of 0.1N hydrochloric acid (similar to gastric fluid minus the enzymes). At the end of the 2 hours, the pH of the medium was adjusted to 6.5 (similar to intestinal fluid minus the enzymes). Samples were withdrawn at known intervals and analyzed for Resveratrol content.

 

Compared to Resveratrol powder, MicroActive Resveratrol SR dissolves slowly and demonstrates sustained release over a longer period. The Resveratrol powder showed complete dissolution (100%) in 4 hours (Figure 1). THe MicroActive formula showed sustained release over 12hrs, with 97% of the dose released.

 

 

Human Study

 

In a pilot study, healthy subjects were administered MicroActive Resveratrol SR capsules after breakfast and blood samples were drawn as before at 1,2,4,8,9 and 24 hrs post-dose. After a one-week washout period same process was repeated with 98% Resveratrol powder. Plasma total Resveratrol (Resveratrol conjugates and free Resveratrol) and free Resveratrol were determined.

 

Resveratrol powder showed a rapid absortion with a sharp peak at Tmax of 2 hrs post-dose. After 3 hrs, the plasma levels of total Resveratrol decline rapidly with a small increase at 9 hrs. MicroActive Resveratrol SR also showed a Tmax at 2 hr, but a lower Cmax (maximum concentration at Tmax) with a broader peak and higher plasma levels compared to the control for >9 hrs (Figure2). This implies that while 98% Resveratrol powder is rapidly absorbed and excreted, MicroActive Resveratrol SR continues to remain in the circulation for a long time.

 

 

MicroActive Resveratrol SR Product Specifications:

 

30% Resveratrol concentration

 

Resveratrol, b-cyclodextrin in a sustained-release matrix

 

Off-white granular powder

 

Storage between 4-10°C, protected from light, heat and moisture

 

Shelf Life of 4 years

 

Suitable for hard gel capsules