Why Dissolvable Vitamins?

Why Dissolvable Vitamins?

This is a detailed evaluation of why dissolvable vitamins are overall a better choice over swallowed vitamins with unnecessary additives, preservatives, and coatings. The vitamin industry is forming a TANK around the vitamin to protect it against the stomach acids and not to protect or benefit you. The concept of bypassing the stomach by changing the route of absorption from swallowing the vitamin to under the tongue placement is the main advantage that we present in today’s blog.

Vitamin Coating Process

The industrial scale production of vitamins has been evolving over the century and it is an extremely complex and complicated process. We shall touch upon the different tablet coating processes in this blog and the advantage we feel Frunutta Micro Quick Soft Molded tablets offer over the more traditional vitamin coatings. There are two principal methods of coating tablet: sugar coating and film coating. Both have advantages and disadvantages, and both coatings consist of a sugar or cellulose based binder, plasticizer, film forming agent and colorant.

In addition to enhancing the appearance and aiding identification of the product, tablet coatings perform several functions:

  • To protect the tablet from moisture and other adverse conditions.
  • To lubricate the tablet to ease swallowing.
  • To disguise unpleasant tastes.
  • To create a barrier between the active ingredient and the gastrointestinal tract.
  • To control the release of the drug into the body.

SUGAR COATING

Compressed tablets are often coated with a layer of sugar that may be colored or uncolored depending on the purpose of the tablet. The sugar coating is water-soluble making it easier to dissolve quickly when it meets any liquid medium such as gastrointestinal fluids.

Four processes are commonly involved in sugar coating, in the following order:

  • Sealing (Water Proofing)
  • Grossing (Smoothing)
  • Coloring
  • Polishing

Sealing involves hardening the external surface of the tablet by supplying a moisture barrier. Sealants that are commonly used include ShellacZinc oxideCellulose acetate phthalatePolyvinyl  acetate phthalate, HyroxylpropylcelluloseHyroxypropylmethylcellulose

Binders that are commonly used: Gelatin, Acacia Gum, Sucrose

Sub-coatings that are commonly used: Calcium carbonate, Titanium dioxide, Talc (asbestos free) Sucrose, Acacia gum.

Grossing or smoothing step involves filling out and smoothing irregular features or areas of the tablet. An application of approximately 60-70% of sugar solids is enough to smooth the tablet. The solution usually contains a mixture of starch, pigments, acacia, and gelatin.

In certain instances, color may be added in during the grossing stage to give the appearance of a homogenous coating layer.

Coloring is the most crucial stage. In the coating process as multiple sugar solutions are added to ensure that the predetermined color is achieved. Soluble dyes have been used to give the desired color as these stick to the surface of the tablet during the drying process.

Recently, companies prefer the use of insoluble certified aluminum lake pigments. These are materials that tint the tablet by dispersion. Lakes are produced from dyes but are oil dispersible, but not oil soluble, and thus can be mixed with oils and fats. They can also be dispersed or suspended in other carriers such as propylene glycolglycerin, and sucrose (water and sugar).

Polishing the last step in the sugar-coating process finishes the tablet to give it a glossy and professional appearance. This is carried out to impart a shiny distinctive appearance to the tablet. Polishers that commonly used are wax such as carnauba waxcandelilla waxbeeswax and hard paraffin.

FILM COATING

Film coating starts by enveloping the tablet’s core with a thin film of protective polymer. Think of trying to protect the ingredients of the tablet with protective layers. The polymer that is to serve as the coating film is dissolved in a suitable solvent, together with additives such as pigments and plasticizers.

Ingredients used in film coating process are the following:

Film Formers commonly used in the industry include Hydroxy Propyl Methyl Cellulose (HPMC), Methyl Hydroxy Ethyl Cellulose (MHEC), Ethyl Cellulose (EC), Hydroxy Propyl Cellulose (HPC), Povidone (PVP), Sodium Carboxy Methyl Cellulose, Polyethylene glycol (PEG), Acrylate Polymers.

Enteric Coating is a term used to describe the coating that gives complete protection to the core of the tablet. Enteric coating protects the active ingredients against attack by acids in the stomach. Providing the tablet with sort of resistance to attack by the gastric fluids.

Solvents are used to dissolve the polymers and other additives. Film coating requires lots of Solvents. Examples include ethanol, chloroform, water, methanol, isopropanol, acetone, and methylene chloride.

Plasticizers that are commonly used are Castor oilPG, glycerin, and PEG.

Colorants most used lakes and dyes are the certified FD & C and D &C type.

Opaquant-Extenders are fine inorganic powders used to increase the fill coverage and supply more pastel color shade to the tablet. Common inorganic powders include:

OTHER VITAMIN COATING TECHNIQUES

In addition to the two commonly used coating methods described above, there are other specialized coating methods that can be applied for specific circumstances such as the following:

  • Compressed coating
  • Electrostatic coating,
  • Dip coating
  • Vacuum film coating

HEALTH CONCERNS

All above named added ingredients or ‘other ingredients’ as is commonly seen on vitamin labels are what the industry calls excipients. Excipients for the tablet industry are not limited to the above-named products which are mostly impossible to pronounce. At this time, it should be quite clear that there is a plethora of other excipients in any named group mentioned in this article.

It should be noted that many of the products mentioned above are used in the wood, iron, steel and cream industries.

While FDA considered all categories and excipients as Generally Recognized As Safe (GRAS), and considered nontoxic with no pharmacological actions, but, there are no data on the prevalence of long term side effects.

Delayed hypersensitivity reactions (DHR) can be one such reaction with clinical signs of allergy to excipients which can range from skin disorders to life-threatening systemic reactions.

Always remember, everyone who prescribes a modern formulated drug or supplement is aware of the risks of adverse reactions due to the properties inherent in the active ingredients, but not all are aware of the risks due to the properties of the added excipients.

The risks of adverse reaction to excipients are intensified when inappropriate and inferior quality excipients are used.

ARE VITAMIN POWDERS BETTER?

There is now a new trend for consumers to use vitamin powders. These powders are to be mixed with water or other liquids to be consumed orally. The concept is that the powders are without additives and preservatives and easier to swallow as a liquid drink. We want to shed some light about vitamin powders since there are many issues with powders that the consumers need to be aware!

Measuring problem

Vitamin powders are measured using a simple kitchen spoon. The issue is that vitamins are dosed in micrograms and the smallest deviation in the spoon scoop can make huge deviations in the actual dose taken. There can be issues of underdosing or toxicity which is not seen in tablets or capsules or packets.

 Why Dissolvable Vitamins?

Blend Separation

Powders are made up of many particles of varied sizes which are not uniform, large particles and small particles. The smaller particles tend to collect towards the bottom of a powdered mixture and larger particles to the top making it extremely hard or impossible to get a consistent recommended dosage of the same vitamins and minerals every time.

Mixing and Storage

If powdered supplement needs to be mixed with a drink, then must stir thoroughly, and consume the full contents of the drink, some ingredients are insoluble, like calcium, iron, boron, selenium, vanadium, manganese, magnesium, etc. Some material may remain at the bottom of the cup, while some ingredients stick to the side.

Storing powdered supplement is difficult due to the moisture exposure and clumping problems, issues which may make their shelf life shorter.

Absorption

Taking too many vitamins and minerals all together can block each other’s absorption and many vitamins are poorly absorbed by the intestinal tract. Hence the route of absorption is the most crucial point the consumer can learn from how a vitamin should be ingested, see the discussion below.

Preservatives

The issue of additives and preservatives still exists with powders since they must still survive the stomach acids and remain stable on store shelves and storage rooms. Hence the powders have improved on the swallowing aspect that many large vitamins capsules or tablets have, but the other issues remain.

Under the Tongue Absorption

 Why Dissolvable Vitamins?

Sublingual, meaning literally 'under the tongue' refers to a method of administering substances via the mouth in such a way that the substances are rapidly absorbed via the blood vessels under the tongue rather than via the digestive tract see picture to the left. The route of absorption via the highly vascularized buccal mucosa allows the substances a more direct access to the blood circulation, thus providing direct systemic administration.

Medically, sublingual drug administration is applied in the field of cardiovascular drugs, steroids, some barbiturates, and enzymes. It has been a developing field in the administration of many vitamins and minerals which are found to be readily and thoroughly absorbed by this method. Sublingually absorbed nutrition, which avoids exposure to the gastric system and liver, means direct nutritional benefits, particularly important for sufferers of gastro-intestinal difficulties such as ulcers, hyperactive gut, coeliac disease, those with compromised digestion, the elderly, and anyone that is unable to swallow tablets or pills – the nutritional benefit is independent of gastro-intestinal influences.

 

Why Dissolvable Vitamins?

There is considerable evidence that most sublingual substances are absorbed by simple molecular diffusion; the sublingual area acting rather like litmus paper, readily soaking up the substances. Buccal mucosa presents an ideal site for absorption.

One of the best known drugs used regularly with great success is Glyceryl Trinitrate better known as nitroglycerin, is a potent coronary vasodilator which is used for the rapid symptomatic relief of angina. It has been found impressively effective when administered sublingually; pharmacologically active after only 1 two 2 minutes also nitrate appears in plasma and concentrations can be maintained for 24 hours.

The Molecular Mechanism

Osmosis

For a nutrient to be effectively absorbed sublingually, it needs to be able to travel across the buccal mucous membranes; by a process of diffusion known as molecular osmosis which applies to all forms of absorption by the body; governing both intestinal and sublingual absorption. The distribution of water across cell walls depends on the osmotic difference in the blood between the intracellular and extracellular fluid. The distribution of water across blood vessel walls is determined by the in-vivo osmotic pressure of plasma and the total outward hydrostatic pressure. Unlike the cell membrane, the capillary wall is freely and rapidly permeable to small molecules. The diffusion of water across a membrane that is only permeable to water depends on the molecular weight of the particle. Small particles that readily dissolve in water, rarely present a problem in permeation and diffusion, and so can move freely between the tissues of the body. Active transportation into cells leads to rapid metabolism of the substances. The  main  mechanism  for  the  absorption  of  the  drug or vitamin in to the oral mucosa is via molecular osmosis as stated into the lipoidal membrane and this also could explain the absorption of non-water soluble vitamins since the lipoidal membrane which is the cellular barrier is made of lipid fats and hence drug absorption in many studies has been shown to be 3 to 10 times faster than the regular oral route and is only surpassed by the intravenous method of injection.

Endocytosis

The cells of the oral epithelium and epidermis are also capable of absorbing by endocytosis, the uptake of particles by a cell as if by hollowly wrapping itself around it. These engulfed particles are usually too large to diffuse through its wall.

Sublingual Nutrition

The advantages of sublingually administering nutrients seem to be manifold, offering improved bioavailability and more rapid metabolism of the nutrients which are absorbed more fully. It allows individual control over the dosage for optimum benefit, within safe guidelines, and can allow absorption in a palatable and easily administered form, regardless of gastro-intestinal difficulties. It is especially useful for those who have trouble in swallowing tablets. Sublingual nutrients are available in readily dissolved tablets, which are placed under the tongue, until dissolved. For these formulations, the small volume of saliva is usually sufficient to result in tablet disintegration in the oral cavity.

The Sublingual Advantage

Zinc and Copper Absorption!

Zinc and Copper are both major components of antioxidant enzymes important in boosting your immune system. During the current pandemic when many are taking large doses of zinc, copper deficiency may become a major issue since in the gut absorption zinc blocks the absorption of copper. Under the tongue Zinc tablets are simply absorbed under your tongue - sublingually - bypassing the need to be swallowed, survive the harsh environment of the gut or causing issues with copper absorption.

Some in the medical community believe that zinc dosing throughout the day is more effective in supplying a constant flow of the supplement to your blood stream than once a day dosing. There are even some who recommend taking lower doses up to every 3 hours to improve boosting the immune response.

Iron Supplements and Intestinal Issues.

Intravenous iron is the best way to absorb iron supplements into our blood directly avoiding the common side effects of constipation, nausea, and vomiting. However, this method is tedious, inefficient, inconvenient, and not cost effective. Oral iron supplements are notorious for causing nausea, vomiting and constipation. Also, they must be dosed multiple times a day for long term due to their poor absorption. In a recent study in New England Journal of Medicine, study participants were given standard swallowed high dose iron tablets two to three times a day, but the results of their blood studies showed only absorptions of 22.6 to 23.6mg per day. One can avoid the poor iron absorption and its associated intestinal side effects. The medical community believes that under the tongue absorption is a more efficient method of absorption for any product hence Iron absorption by under the tongue tablets should not only supply less gastric side effects but should also supply a higher absorption and less need for multiple daily dosing.

Vitamin D

National Institute of Health (NIH) states that Vitamin D is considered “a fat-soluble prohormone” which is involved in many aspects of our wellbeing and regulatory functions just like a hormone. Everyone is aware that calcium absorption and bone health are major part of vitamin D benefits. However, most people may not know that Vitamin D is also involved in control of inflammation, sugar control, proper cell death, proper cell growth, and many other cellular and system regulation. Most people in the western hemisphere do not obtain their vitamin D from sun exposure or foods sources and need to be supplemented to obtain optimal levels.  Due to its inability to dissolve in water D3 is at times difficult to absorb without large fatty meal or a glass of whole milk. Hence many find that they are D3 deficient even though they have been taking their supplements regularly. If you take vitamin D tablets under the tongue for better absorption, you do not need to worry about any of the above since it absorbs under your tongue and directly into your bloodstream. No need to plan a fatty meal or worry about an upset stomach because under the tongue D3 absorbs directly into the bloodstream from the tongue blood plexus and avoids the passage through the gastrointestinal tract.

There is also debate about when is the best time of day to take your vitamin D3 – there is some research that suggests vitamin D may negatively impact your sleep. Until further research is available, we recommend you consume your Vitamin D supplements first thing in the morning. Make it part of your morning ritual. It is easier than having to remember to take them later in your busy day.

Turmeric vs. Curcumin

Curcuma longa, better known as Turmeric, is a flowering plant native to the Indian subcontinent and Southeast Asia. Turmeric is in the same family as ginger (Zingiberoside), and just like ginger, the use of turmeric is focused on the roots.

Although the over 600 studied benefits of Turmeric are just now getting international attention and recognition in recent years, it has been used in Ayurvedic medicine for over 6,000 years.

The roots of turmeric are chock full of bioactive compounds, the most studied class of which are the curcuminoids. Within the class of curcuminoids, we are often most interested in a single compound called Curcumin, which besides being a bright orange pigment, also has a plethora of health benefits.

Turmeric has been used for centuries for both culinary, textile dyeing and supplement applications. It is most known for its bright orange color and pungent earthy flavor in Indian cuisine. The flavor of turmeric can be attributed primarily to its essential oil content with the main essential oil being alpha-turmerone. In addition to being used as a staple spice in cooking, the anti-inflammatory benefits have become a major attraction for the supplement world.

If you think Turmeric has a strong bitter and pungent taste, then you can only imagine what pure curcumin tastes like, which is the bioactive root of turmeric plant. It is true that curcumin provides mostly the coloring associated with turmeric plant but the essential oils that are so pungent to taste buds are more concentrated in most products that contains Curcumin. It is probably impossible to make a sublingual curcumin product that can be acceptable to the palate without adding artificial flavors that could take away from the benefit of the curcumin in the first place.

Turmeric alone is difficult to absorb through digestion. This is because it is fat soluble just like Vitamin D. Without fat, the active part in turmeric, curcumin, has a tough time making it past the stomach, into the small intestine, and into the blood where it can offer the greatest benefits.

Another way to help with the absorption of Turmeric is to take it with black pepper. The compound piperine, which is responsible for the pungent flavor in black pepper, is also a potent inhibitor of drug metabolism. One of the ways our liver gets rid of foreign substances is by making them water soluble so they can be easily excreted. The piperine molecule, however, prevents that process. The bioavailability of curcumin (turmeric) will shoot up 2,000% when taken with piperine (black pepper). Since after intestinal absorption the liver takes what is called a first pass metabolism piperine allows Curcumin and Turmeric to survive the first pass metabolism of the liver and be secreted into the blood stream. However, this is not at all needed if the Turmeric is taken under the tongue (sublingually) since it is completely bypassing the intestinal absorption and the liver first bypass metabolism.

Vitamin B12 and Intrinsic Factor!

The problem with any oral vitamin B12 is that it must be swallowed. Now, whether you chew, drink or swallow your B12 the biggest issue is that after surviving the harsh environment of acidic stomach B12 requires to be bound to a protein called Intrinsic Factor (IF) to be absorbed into our body. As we age our body makes less and less IF and hence, we absorb less B12. Many complain of chronic fatigue or tiredness as they reach their 30’s, 40’s and 50’s and worsens with advancing age. What is your best option if you do not want to get a B12 shot in the butt? An excellent source of under the tongue B12 currently available in the market allows bypass of the harsh environment of the gut or the need for attachment to IF. Under the tongue B12 is absorbed directly into the blood stream by osmosis as described above without the need of Intrinsic Factor (IF). 

SUMMARY

It should be obvious that the industry has many reasons for its use of excipients, or other ingredients in tablet manufacturing which we tried to touch on briefly in this article. We at Frunutta have used a radical approach to tablet production and absorption with bypassing the need for coating. Our soft molded tablets are free of any coating and unnecessary and unnatural excipients. By using the under the tongue ‘sublingual’ route for absorption of our tablets we have done away with the need to produce coatings on our tablets and hence we have been able to avoid all the above what we consider unnecessary ingredients.

Read our labels and compare us to your current products and you can see for yourself the Frunutta difference.

This information is only for educational purposes and is not medical advice or intended as a recommendation of any specific products. Consult your health care provider for more information. These statements have not been evaluated by the Food and Drug Administration. These products are not intended to diagnose, treat, cure, or prevent any disease.

References:

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