Oral Absorption and Bioavailability
A lot of supplements don’t work. Not a big surprise, right? Now, these supplements may have been manufactured with honest intentions, but the sad-sack designers often fail to take into consideration two huge factors: oral absorption and bioavailability.
I’ll spare you a long discourse on pharmacokinetics, but you should at least know that a lot of things need to be just right in order for a supplement to enter the bloodstream and affect target tissues.
For instance, a supplement can be highly hydrophobic or hydrophilic and either condition can determine whether it even has a shot of getting into your system. How well it stands up to certain digestive enzymes, how well it reacts to the stomach’s pH, and even how it interacts with other supplements, foods, or drugs affect its chances as well.
There are, however, things a manufacturer can do to make sure a supplement is both absorbable and bioavailable. Following are 6 supplements and the “upgrades” that turn something that only works in theory into something that works in real life.
1 – Curcumin
This bright yellow substance is produced by plants and it’s known as a potent pain reliever and anti-inflammatory. It also increases testosterone levels and simultaneously exhibits anti-aromatase properties. It enhances cardiovascular health and seems to thwart prostate cancer. It reduces body fat. Hell, it even seems to fight mosquito-born viral diseases.
Recent research shows that curcumin even enhances the effects of exercise, helping muscles perform better, generate more energy, and repair themselves better.
Many curcumin supplements on the market contain wildly inconsistent levels and strengths of curcumin. Not only that, but curcumin’s bioavailability is notoriously poor. It generally causes only a tiny rise in blood levels. As soon as it clears the small intestine, the liver makes it water-soluble and bam! It’s out of your body as fast as a can of Budweiser. As a result, the average user sees (or feels) little benefit from average curcumin products.
First, make sure your curcumin supplement is standardized to contain at least 90% total curcuminoids (the active ingredients), like Biotest® Curcumin.
Secondly, it also needs to contain something to make it more bioavailable, like piperine. The substance works by inhibiting drug metabolism in general. In the case of curcumin, piperine interferes with the liver’s efforts to make it more water-soluble, thus enhancing absorption by about 2,000 percent.
2 – Cyanidin 3-Glucoside (C3G)
This polyphenol is found in blueberries, grapes, black beans, and pretty much any fruit or vegetable that has a reddish blue or indigo cast to it.
Studies have shown it to have anti-diabetic effects, which means that it makes you more insulin sensitive so that nutrients can be preferentially shuttled off to muscle tissue. We also know C3G has anti-obesity effects (by raising levels of adipokinectin) and improves exercise capacity by activating fatty acid oxidation.
Users of the supplement can actually eat more carbs without getting fat and, provided they’re working out, have the energy provided by those carbs ferried off to fuel and build muscle. C3G also has phenomenal potential to fight diabetes, improve vision, and promote liver health.
Most C3G products have two huge problems. First, the substance is pretty expensive and manufacturers who sell to retail outlets have to price the product at about 4 to 6 times manufacturing cost to take care of all the middlemen. As such, they typically under-dose the product and the end result is an ineffective supplement that has no noticeable effect.
Secondly, while C3G seems to be absorbed by both the stomach and the intestines fairly well, the stuff is broken down really quickly and enters the bloodstream as metabolites rather than the whole compound. While these metabolites may have unique health benefits all their own, they’re not necessarily doing all the same things as the parent compound (purging fat and helping build muscle).
An effective C3G supplement should provide at least 500 to 600 mg. of cyanadin 3-glucoside per serving. Since it’s intrinsically so expensive, you need to get it from a company that sells direct to the consumer so as to avoid all those retail, pay-the-middleman charges.
Additionally, it should use an innovative delivery system to protect, enhance, and stabilize the parent compound. Gelucire does the job nicely. The compound is derived from mixtures of mono, di, and triglycerides and widely used in the pharmaceutical industry to improve the bioavailability of drugs. Indigo-3G® checks all the boxes.
3 – Forskolin
This testosterone and thyroid hormone raising supplement is derived from the herb, Coleus forskohlii, and some pretty good studies have shown it to increase lean body mass, decrease body fat, and lower blood pressure while raising metabolic rate.
It does all this by elevating levels of cAMP (cyclic adenosine monophosphate), which is an interesting compound because it acts as a kind of chemical switch that turns all kinds of body cells on and off.
For instance, increased levels of cAMP can cause the Leydig cells of the testicles to produce more testosterone, which in itself can lead to additional lean body mass. Increased levels of cAMP can also lead to the increased production of hormone-sensitive lipase (HSL), which leads to the release of free fatty acids to be used as fuel by the body.
Forskolin also upregulates the thyroid, causing some researchers to compare its effectiveness with thyroid stimulating hormone (TSH).
Since, like many supplements, it’s derived from a plant, standardization is a pretty big problem. A lot of forskolin products are just “grass clippings” (the whole plant dried, crumbled, and stuffed into a capsule).
The herb also has a short half-life of about 4 hours, so you need to take it pretty often for best results. Not ideal. And while its oral absorption is good, its bioavailability is questionable because a lot of things seem to interfere with how successfully it makes it into the bloodstream.
Just as you’d like all the tomatoes you buy to taste great, you also want every batch of forskolin to work like advertised. But plants are fickle. One batch isn’t like the one before it or the next, so you need to make sure you get a product that’s made entirely of the active ingredient – forskolin carbonate – and not the aforementioned “grass clippings.”
By extracting and purifying the active ingredient, you extend the duration of action from 4 to 12 hours. Secondly, you need to improve its bioavailability by combining it with the aforementioned gelucire, a compound made from mixtures of mono, di, and triglycerides. Carbolin 19® is pure forskolin carbonate and uses the proper delivery system.
4 – Phosphatidic Acid (PA)
This molecule is a phospholipid that regulates mTOR (mammalian target of rapamycin). Simply put, if you control mTOR, you control the switch that turns on muscle protein synthesis in response to exercise. “On” means muscle. “Off” means no muscle. It’s as simple as that. It’s found naturally in the diet, but only in very small, inconsequential amounts.
One study, using 16 weight lifters, found that 750 mg. of PA increased squat 1RM and body mass. Another, also using 750 mg. (split into two doses, one before lifting and one after) in 28 weight lifters found that the PA group gained 2.4 more pounds of muscle than the placebo group. Still another study found that lower doses of PA (250 mg. and 375 mg.) increased lean body mass and cross-sectional area of the rectus femoris in a different group of 28 men.
In order for PA to work, it has to enter the muscle cell and bind to mTOR. It can also work indirectly by converting to lyso-phosphatidic acid and attaching to the muscle membrane, which increases intracellular PA and in turn activates mTOR.
However, different sources of PA can have varying degrees of saturated or unsaturated fatty acid chains and this influences how PA works. Two saturated fatty acids doesn’t promote mTOR signaling, but one saturated fatty acid and one unsaturated fatty acid does.
Chemi Nutra, one of the country’s most innovative materials manufacturers, has developed an unsaturated form of PA. That means it’s orally absorbed with high bioavailability, leading to an 8-fold activation of mTOR that persists for around 7 hours. Consequently, you should only use PA supplements that source from Chemi Nutra, like Micro-PA®.
5 – Resveratrol
The public knows this plant compound as the life-extending stuff found in red wine, but athletes know it for its ability to raise testosterone levels, lower estrogen, reduce fat storage, or how it makes young muscle cells grow longer and thicker.
It also lowers blood sugar in general (thus combating diabetes) and fights cancer, Alzheimer’s, cardiovascular disease, and a long list of other maladies.
Most resveratrol supplements just contain powdered resveratrol. Unfortunately, while resveratrol generally has good absorption of about 70%, its bioavailability is still low because it’s rapidly metabolized by the intestine and liver. You can drink all the resveratrol-rich red wine you want, but all you’ll get is drunk.
Obviously, an effective resveratrol product needs to contain something to help with that low bioavailability, and again, the poly ethylene glycol ester gelucire does the job nicely. Rez-V™ is a top choice.
6 – Casein Protein
There are plenty of studies comparing the muscle-building effects of casein and whey, with casein generally coming out on top. There are all kinds of reasons for this, but the main point is this: Casein is generally a better muscle builder, a better strength builder, and a better fat burner than whey.
Unlike the other supplements in this article, this particular bodybuilding staple is often absorbed too quickly. Case in point, most inexpensive casein protein powders are composed partially or totally of sodium or calcium caseinate, both of which the body absorbs fast like a bunny. As such, they cause a rapid rise of insulin. They also don’t provide sustained levels of amino acids.
They’re not a complete waste, but they’re kind of anemic when it comes to doing the basic job of protein powders, which is building muscle.
If you want a casein-based, general use protein powder – one that does what’s it supposed to do, i.e., bolster your daily protein intake for the purpose of muscle building – look for protein powder products that contain micellar casein. Micellar casein is composed of soap-bubble like molecules (micelles) that form a bolus in the stomach when consumed. That makes them digest really slowly.
It’s really hard to make a protein powder from micellar casein – hence their relative rarity and higher price. You have to process it carefully and leave the milk proteins largely unmolested. As I often write, manufacturing micellar casein is almost like catching snowflakes in Maine and shipping them intact to California with a truck driver who stops outside a bar in the Mojave Desert to slam down a few tequilas.
It’s worth the trouble, though, because micellar casein is the only protein that’s been shown in lab studies to actually be anti-catabolic (Boire, 1997), meaning not only does it increase protein synthesis, it helps prevent muscle breakdown during and after intense exercise. Metabolic Drive® Protein contains an ample amount of micellar casein.
Yeah, I Know…
Yeah, yeah, the supplements described are all things that Biotest® produces, but I make no apologies. They’re products I know really well because I played a small role in helping Tim Patterson and the rest of the research team develop them. More importantly, I know the reason Biotest® made them. We made them because, first and foremost, they’re products WE wanted to use.
We didn’t take “price points” into consideration so we didn’t scrimp on quality or dosage. We didn’t consult marketing gurus to determine exactly which products the 18-30 year-old sweet-spot demographic would give up beer money to buy.
We just looked at the science behind various compounds or formulations, in some cases doing some of our own studies, and if we got excited, we turned them into supplements that we wanted to use. If anybody else got equally excited about them, they can buy and use them, too.