Developing Efficacious Sleep Formulas

Many consumers work hard burning the midnight oil with very little sleep and, consequently, usually feel burned out the following day. New research shows when a naturally occurring brain neurotransmitter, orexin-A, is administered to sleep-deprived animals it can significantly improve cognitive function. Orexin-A has the ability to offset mental function decline and the changes in brain metabolism by controlling sleep and brain activity.

Although it is exciting for a formulator to find new research on brain neurotransmitters such as this, to actually develop a product so that people can stay up all night is probably not in the consumer’s best interest. Neglecting sleep is unhealthy and is not beneficial to overall well-being.

In fact, insomnia is a serious issue among Americans. Some wake up in the middle of the night and have difficulties falling back to sleep, while others have trouble just falling asleep. Many of these U.S. consumers are taking action—simply look at the growth of the OTC and pharmaceutical market for sleep aids. However, there is growing interest among consumers in finding natural products that will relax the mind and act as a sleep aid, without the short or long term side effects of drugs.

Formulators should thoroughly investigate the body’s physiology and become knowledgeable about the limbic system, the region of the brain that is involved in regulating emotions and the stress response. The limbic system contains the hypothalamus, which regulates many functions including sleep and stress reactions. Understanding the activities of the limbic system will clarify how the brain neurotransmitters function and help a formulator select the best nutrients to support sleep and relaxation. There are over 30 brain neurotransmitters, but serotonin, norepinephrine and dopamine are the key ones to help regulate sleep and emotion.

A good understanding of brain function makes it easier to review the scientific literature on the various nutritional ingredients that support sleep. These include melatonin, L-tryptophan, 5- HTP, vitamin B12, magnesium, valerian and hops, among others.

Formulators may consider adding the hormone melatonin to sleep formulations since it has been shown to help individuals with insomnia. Melatonin helps regulate circadian rhythms and has been used as a dietary supplement since 1993. Since melatonin as an endogenous nutrient declines with age, it may be helpful to add it to an anti-aging product for older Americans. The body produces melatonin from serotonin, which itself is manufactured via tryptophan hydroxylase.

In fact, the amino acid L-tryptophan may be a good addition to sleep formulations. Clinical research shows it is effective as a sleep aid; since it is converted to serotonin, it may be beneficial to those with low levels. Another dietary ingredient, 5-HTP, is also converted to serotonin and may be an option in sleep products.

Basic nutrients can also support the sleep response. Vitamin B12, for example, has been used at doses of 1,500 to 3,000 mcg/d for insomnia. However, such high levels of B12 may impede absorption of other B vitamins. The mineral magnesium may be used as a secondary component to a sleep formula to promote sleep. Some research has shown significant benefits from administering magnesium to individuals with restless legs syndrome who also experienced insomnia.

Many herbal ingredients can be successfully combined in a product formulation to support sleep. One common herb, valerian (Valeriana officinalis) has been studied alone and with other herbs to promote sleep. For example, valerian has been effectively used in formulations with hops (Humulus lupus) for sleep. Valerian has been shown to increase deep sleep and dreaming and has not been shown to cause drowsiness or a hangover effect in the morning. On its own, hops has been used historically as a sleeping aid and has not demonstrated any known adverse effects. Most research on its efficacy for sleep has been in animal studies.

A more controversial botanical in the relaxation and sleep category is kava kava, an herb consumed for relaxation in various Pacific cultures, such as Polynesia. Clinical studies on kava extract, standardized to kava lactones, have shown it effectively induces relaxation. However, several years ago, there were reports of possible hepatotoxicity associated with kava use; FDA and other regulatory agencies around the globe investigated the allegations, and there is still research ongoing to address the toxicity concerns.

Many compounds are available for formulating effective and safe sleep formulations, but it all starts with in-depth investigation of the scientific literature. Evaluate the region of the brain where sleep is controlled to better understand the function of the various studies performed with nutritional ingredients. Consumers will be well pleased with their product when a company has taken the time to review the research to help them rest easy and get a good night sleep.

Judi Quilici-Timmcke, M.S., is president of Q-Tech Services Inc. (JudiQ.com). She is a product formulation specialist who holds a master’s degree in dietetics and exercise physiology. Previously, Quilic-Timmcke worked as vice president for R&D for Weider Nutrition and as head of product development for Rexall Showcase.