Understanding Excipients

August 17, 2020

Understanding Excipients

In this article:

  • What are excipients anyways?
  • How do excipients affect drug & supplement formulations?
  • The roles & functions of each kind of excipient
  • Pharmaceuticals vs. Supplements: How excipients differ
  • Excipient safety & GRAS certification
  • Spotlight on Nu-Flow & its role in Boswellia Serrata formulation

Reading the ingredient list is the ultimate staple of nutrition. Whether you’re shopping for a supplement or processed foods, it is of utmost importance to carefully read the label - every single bit of it, even the small print. While certain nutritionists and experts will encourage you to stay away from any kind of additives in your products, we’ll have to play the devil’s advocate in case of harmless, efficient elements such as excipients. Instead of categorically rejecting additives altogether, we advise you to invest some time in educating yourself on the topic.

In case you’ve already tried to do your research, you’ve probably come across a bunch of conflicting information and confusing science. Today, it is our mission to remove the veil once and for all, and demystify excipients in layman’s terms.

What are excipients?

By definition, an excipient is an inactive substance that has the role of a medium for active substances. Basically, they help active ingredients in supplements & medications do their job properly. While there are certain supplements, such as collagen powder and whey powder, that don’t require these kinds of mediums, excipients are necessary for other products. Why is that? Well, even though they add no therapeutic value to these products, excipients have been found to promote conservation, efficiency, and quality. What’s more, excipients appear to act as protective and bulking agents, improving the overall bioavailability of certain drugs.

The term excipient is used for any substance other than active drug or the active pharmaceutical ingredient that is contained in a certain product. Therefore, excipients are perceived as indispensable components of medical products, forming the bulk of the formulation, a review article on pharmaceutical excipients states. However, not all excipients can be used in the manufacturing process of all products, as it has to meet specific requirements. Nevertheless, there are “common” quality standards for all excipients, as all of them should be non-reactive, chemically stable, non-toxic, economical, low-equipment and process-sensitive, inert to the human body, efficient in regards to the intended use, and in accordance with organoleptic characteristics.

Even though the significance of excipients is not the most popular discussion, it is important to state that these elements greatly contribute to the overall product performance and the drug delivery within the body. When talking about product structure, you’ll rarely encounter an active ingredient administered alone, as excipients are necessary to enhance, mask, suspend, or dissolve it for improved quality. Therefore, excipients may be seen as vehicles transforming the desired active ingredient into a more efficient, bioavailable form. Excipients are also added with the intent of preventing microbial contamination and degradation of a certain product.

It would be wrong to think of excipients strictly as inactive support, as they’re much more than that. Some of the most pronounced excipient roles include increasing drug solubility, formulation and drug shelf life, absorption as well as the stability of the dosage form; formulating and providing identity for the dosage form, decreasing therapy cost, enhancing drug targeting, etc. Therefore, the activity of these elements is multilayered, and it encompasses stabilizing, protecting, increasing, enhancing the overall product formulation and quality.

Excipient Categories & Their Roles

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As we already mentioned, there are certain quality characteristics that all excipients should possess. However, not all of them are suitable for all products, and compatibility is one of the most important factors for optimal product stability. Therefore, we’ll briefly touch upon different excipient categories and their specific uses.

Fillers

As the name itself implies, the sole purpose of fillers (or diluents) is to increase the bulk volume of a product, as well as the hardness of certain tablets, hence the term “bulking agents”. Fillers act as carriers, making sure that the desired size and form of a capsule or tablet is achieved. Excipients known as fillers come in various forms, including oils and rice flour, as well as more controversial agents such as magnesium stearate. Without fillers, some products could not be manufactured as capsules due to their miniature size and the inability to fill up a certain capsule.

Binders

Binders justify their name just like fillers. These excipients bind all the ingredients in a tablet together, providing the necessary cohesiveness. Binders provide cohesiveness by holding the product particles intact and strengthening the final dosage form. Without binders, products would easily crumble and break apart, which would jeopardize their efficiency. This group of excipients includes Polyvinyl Pyrrolidone-K, Hydroxyethyl Cellulose, Hydroxy Propyl Methyl Cellulose, and starch paste.

Flow Agents - Lubricants - Glidants

Flow agents are added in small quantities, and their purpose is to prevent clumping, as well as sticking of drugs against machines. They allow for the capsule processing to run smoothly, without any sticking on the way. While these excipients are not as necessary as fillers and binders, their role in quality product manufacturing should not be overlooked, as they keep the production cost low. The most commonly used lubricants include talc, vegetable stearin, magnesium stearate, magnesium carbonate, and colloidal silicon dioxide.

Disintegrants

In order for a product to be advertised as “fast-acting”, it should contain disintegrants. These excipients allow for a tablet to easily break apart in the digestive system and release the active ingredients, providing them for the body to absorb. A product containing a disintegrant will quickly dissolve in the presence of liquids.

Preservatives

Without preservatives, the shelf life of a product would be quite limited, as they prevent microbial growth in the formulation. Therefore, these excipients are added in order to protect the product against decomposition and avoid any harmful chemical change that would compromise the formulation. Vitamin C, A, and E, as well as specific amino acids cysteine and methionine, are natural preservatives commonly found in supplementation. As far as artificial preservatives are concerned, this category encompasses parabens, benzoates, sorbates, sulfites - all of which should generally be avoided in a healthy, balanced diet.

Magnesium Stearate

According to the FDA, magnesium stearate is generally recognized as a safe substance, which leaves little room for concern. This excipient is mostly utilized as a lubricant, acting similarly to the aforementioned flow agents. There are, however, certain speculations surrounding this particular excipient, such as the ones that it inhibits harmful T-cells and that it could jeopardize nutrient absorption. Nevertheless, with the small amount of magnesium stearate found in products, it could hardly have any impact on bioavailability.

Coloring & Flavoring

Coloring and flavoring is something you’ll mostly find in a cheap product, as quality manufacturers aren’t known to take that direction in their production. Quality supplementation will mostly incorporate natural flavors, such as fruit extracts, to get the desired taste and color. Also, certain sweeteners are considered a safe alternative to sugar and artificial sweeteners such as saccharin and corn syrup.

Excipients in Pharmaceutical products

Excipients in Pharmaceutical Products

Excipients are present in the manufacturing process of numerous pharma companies due to their efficiency-boosting activity. When talking about excipients in drugs, there are 3 predominant roles: increasing production and manufacturing efficiency through optimal lubrication (which allows the production machines to run smoothly and limits product damage), preservation, and filling. For instance, Magnesium Stearate can be found in numerous drugs acting as a lubricant which allows for capsules to close properly.

Preservatives, as we’ve already discussed, prolong the shelf life of products by acting as drying mediums to avoid clumping. A smoother, more coherent structure of a drug product grants a more pleasant experience for the user. On the other hand, fillers are necessary for a substance to meet a certain weight or shape, hence the addition of excipients such as rice powder.

Excipients in the Supplement Industry

Excipients utilized in the production of nutritional supplements have the role of providing the needed weight, volume, and consistency for the product, a study on the use of excipients in dietary supplements suggests. Furthermore, excipients are necessary in order to achieve the desired tolerability, bioavailability, and efficiency of a supplement.

Simply put, without them, the targeted nutrient would not be able to reach your bloodstream in an absorbable form. The commonly encountered excipients in the supplement industry belong to the following categories: plant-sourced (cellulose, sugars, starches, arginates), animal-sourced (gelatin, lactose, stearic acid), mineral (silica, calcium phosphate), and synthetic (povidone, polysorbates, and PEGs).

Without excipients, the majority of supplements (excluding the free-flowing powders such as collagen powder and whey) would lack the consistency of dose and would not have the desirable form. Furthermore, the taste and flow of certain dietary supplements rely solely on excipients. In addition, specific ingredients found in supplementation require excipients in order to blend seamlessly without clumping.

Are Excipients Safe?

In a perfect world, we’d be able to obtain the desired nutrient in its pure form, without having to think about any additional ingredients. However, it is clear that certain products require these additions to reach their full potential. As you could already see in this article, not all excipients can be labeled as “bad”, and some of them offer nothing but beneficial effects. While it is always our recommendation to consult with your nutritionist or health care provider before starting any kind of supplementation, the majority of excipients in the supplement world are considered generally safe.

To quote the FDA, the majority of excipients designated by them are Generally Recognized As Safe (GRAS). When used in correct practices, excipients are considered to be absolutely harmless. However, an overview of pharmaceutical excipients suggests that product formulas should be simplified as much as possible and that only the necessary excipients should be added. The excipients considered necessary are the ones providing volume, uniformity, and the required dose.

On the other hand, excipients have been found to contribute to the overall safety of the supplement, ensuring their stability not only in the manufacturing process but once the product reaches the customer, as well. What’s more, excipients grant accuracy and precision when it comes to the administered dose, which is one of the most important factors when it comes to both drugs and supplements. Finally, it is safe to say that excipients are responsible for product safety and efficacy in both the formulation stage and the storage period, as well as during its administration.

Once again, you should always keep in mind that there are different categories of excipients, each of which come from different sources and provide different effects. Therefore, not all excipients should be regarded as an entity and valued equally.

NU-Flow: Uses & Safety

NU-Flow is an excipient you may have noticed on the ingredient list of numerous all-natural supplements, including our own Boswellia Serrata Extract. You may wonder how can a product be advertised as “all-natural” if it contains additives? As we’ve explained earlier, not all excipients are necessarily artificial, and Nu-Flow certainly belongs to the group of natural, harmless excipients.

NU-Flow (preferably NU-Flow® by RIBUS, Inc, of St. Louis, Mo. - the excipient we’ve chosen for our Boswellia extract) is essentially a rice concentrate. It offers a powerful anti-caking activity, as it is a natural desiccate and silicate. Rice concentrate is a commonly used ingredient of natural origin, aiding in supplement production, storage, and packaging. It is important to mention that NU-Flow is recognized as a completely harmless supplement ingredient, being that it meets all the organic labeling guidelines.

What’s more, rice concentrate represents an ideal natural substitute for artificial and synthetic excipients, such as SiO2 and talc, which makes it far more suitable for quality natural products. It has been shown to aid the overall product flow while preventing caking and clumping in the supplement structure.

When it comes to the very structure of NU-Flow, it is manufactured from sterilized rice hulls in the form of fine powder. What makes rice concentrate an ideal natural excipient is the fact it contains natural silica from the soil, being an equally effective (but much healthier) alternative to silicon dioxide and similar flow agents.

Marketing can be deceiving, so we highly encourage you to read the label, ask all the necessary questions, and always do your research. Nutrition is, without a doubt, the foundation of health, so you should cherry-pick the supplements and ingredients to include in your diet. For our selection of non-GMO supplementation, head over to our online store.

Article Summary

  • Excipients are inactive substances that are formulated in drugs & supplements to help them do their job
  • Excipients offer the needed weight, volume, and consistency for the product
  • Without excipients most supplements would lack the consistency of dose & form to be effective
  • Types of excipients include: Fillers, binders, flow agents, disintegrants, preservatives, magnesium stearate, coloring & flavoring
  • Generally Recognized As Safe (GRAS) is the FDA designation given to excipients suitable for formulations
  • NU-Flow is the excipient formulated with Amandean's Boswellia Extract for pain management & mobility




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