The Importance of Bioavailability in a Sleep Product

Sleep disorders are so common these days. The stresses of life in the modern world cause many to turn to various medications to help them get through the night. Melatonin supplements have emerged as a convenient answer to sleeplessness since their approval and introduction in the mid 1990s. In fact, their use has more than quintupled between 1999 and 2018. A new kid on the block, Zelatonin, however, removes many of the barriers to the safety of this popular supplement.

The National Sleep Foundation, which takes regular surveys about the state of sleep in the US recently determined that 27.4% of American adults take a melatonin supplement regularly. Eighty eight percent of those respondents said that these supplements help them fall asleep faster. This would appear to be helping many people, but there are some specific challenges that come with relying on melatonin supplements.

One challenge is called the “first-pass effect”. The first-pass effect refers to a type of filtration that happens naturally in the body when a compound like a medication or melatonin is taken orally, resulting in an erosion of the drug’s power. Often, the site of this metabolism in the body is the liver. With synthetic melatonin, it must first pass through the liver which decreases its concentration before reaching the intended location in the brain, lessening its effectiveness.

A typical dose of melatonin is between 1 and 10 mg before bedtime. Oral melatonin helps with sleep onset, but another attribute of synthetic melatonin is that it does not help so much in the middle of the night. This is partially due to the ‘half life’ of melatonin. Melatonin does not last long in the body and, therefore, is considered to have a short half life which means the time it takes for the body to eliminate half of the drug. For melatonin that is 40-60 minutes. When you want to sleep up to 8 hours, that is a rapid fall-off.

So, the challenge many face before bed is, how much to take? The long-term effects of
synthetic melatonin have not been adequately tested. Many consider it a “natural” product, but it may not be what you think. Sources of synthetic melatonin are primarily derived from animals or microorganisms, but most often they’re made synthetically. In order to get enough sleep, some people take more than recommended hoping that it will last throughout the night and prevent those frustrating nighttime awakenings. This is a risky gamble as too much melatonin can be problematic. You can overdose on melatonin. Too much can also affect other medications you are on.

But, even so, do you really even know what you are getting? Another cause for concern is that you don’t really know the level of melatonin in many supplements, despite what it says on the label. One study found that there is very wide variability in melatonin supplements that were tested, compared to what they declared on the label. Some had very little melatonin, and some added way more than was declared. This has dangerous potential consequences as we have seen.

A new product, Zelatonin Sublingual Spray, takes the best of melatonin supplementation and administers it in a way that eliminates the first-pass effect and blows past the short half life issue. The key is how it is suspended in a liquid and administered with a spray under the tongue. The sublingual spray format has been proven to be 5 times more bioavailable than oral dosages. This means you can take a much smaller amount because all of it gets to where it needs to go fast and efficiently. There is no delay in feeling the effect and none wears off travelling through your body. Check, check and check.

Zelatonin Sublingual Spray uses a safe, low dose of melatonin and combines it with a proven natural formulation that has a time release mechanism to keep you sleeping through the night. You get the rapid onset of the melatonin in a bioavailable format. The authors of this study that demonstrated rapid bioavailability stated that, “Melatonin is a good candidate for sublingual administration, considering its variable oral absorption, short biological half-life and extensive first pass metabolism… Melatonin food supplement in emulsion spray improves melatonin absorption, ensuring higher concentrations after administration, compared to the standard oral tablet formulation of melatonin.”

When only 15% of conventional oral melatonin actually reaches its goal, it’s almost impossible to know how much oral melatonin to take or how much you are getting. It’s really a shot in the dark. With Zelatonin Sublingual Spray, the amount of synthetic melatonin is very safe and targeted. There is no erosion of the effect and this unique, proven formulation keeps you safely slumbering all night long.