Natural alternative ingredients for tableting and capsule filling

The trend towards organic food has been evident in the trade for several years now. Consumers seem to be developing a greater awareness of organic products [1]

Manufacturers of dietary supplements are also slowly changing their formulations to organic, as consumers are increasingly looking at the list of ingredients and do not want to find any chemical or synthetic ingredients there. Now it is important to find substitutes for the excipients in oral dosage forms that have been tried and tested for years and that meet the strict organic certification requirements.

When we look at dietary supplements, a large number of them are available in solid oral dosage forms. Vitamins, minerals etc. can be easily pressed into tablets by wet granulation or direct compression. Good binders are needed for this. Binders that have so far been tried and tested by the industry and are often used for this purpose are, for example cellulosic components (Hydroxypropyl cellulose (HPC) or Microcrystalline cellulose (MCC)) or synthetic polymers (Polyvinyl pyrrolidones (PVP)). But for the organic oriented consumer these excipients sound synthetic and not natural. Therefore, manufacturers of dietary supplements need to exchange these common binders to more natural ingredients.

The same challenge applies to fillers, flow agents, lubricants, disintegrants and pigments when it comes to natural formulations for tableting and capsule filling. Magnesium stearate, stearic acid, silica, synthetic colors are some of the excipients that need to be replaced when meeting the needs of consumers who care about organic products. That is why this adaptation of the ingredient list is also called “Clean Label” - a more natural ingredient list. Even discredited, supposedly natural raw materials such as palm oil are considered critical by consumers, who also attach importance to the sustainability of the raw materials.

Finding replacements for synthetic binders

Binders are used to give cohesion to the loose particles/granules. This ensures that the tablet remains intact after compression. Conventional binders are celluloses and polymers like HPC, PVP or MCC. Now it is a matter of replacing these with natural raw materials while still maintaining the mechanical strength and release properties of the tablet. Natural binders such as starches, gums, mucilages or dried fruits have binding capacity as well as some other properties such as filler, disintegrant and could be an alternative to synthetic binders.

The company BIOGRUND has been a formulation specialist for oral dosage forms for decades. The company quickly adapts to market changes and requirements of its customers. Through developments together with the customer, formulation changes from synthetic to natural/organic raw materials can be easily established. It often turns out that a synthetic raw material cannot be replaced 1:1. To achieve the same function of a synthetic binder, users usually have to add several natural raw materials in different concentrations to the tablet mass to achieve the desired binding properties. Customer-specific premixes, like CompactCel natural or organic, from various naturally certified raw materials, on the other hand, can simplify development, handling and the manufacturing process.

Natural disintegrants to control the fast release of a drug

Disintegrants are substances or mixture of substances added in drug formulations which increases dispersion or breakup of tablets and capsules into smaller particles for fast dissolution. Popular synthetic superdisintegrants include e.g. cross-linked PVP, MCC, croscarmellose sodium, sodium starch glycolate. All of them are chemical sounding names that are undesired on the list of ingredients for clean label products. More natural sounding raw materials who also act as a disintegrant are for example:

Mucilage of isapghula or psyllium husks, cress, gum karaya, fenugreek seed and gum of locust bean, chitin and chitosan, gellan, agar, alginates, oat fiber, xanthan, Cucurbita maxima pulp powder, Hibiscus rosa-sinensis Linn, Mango peel pectin.

A dry powdered premix compound, like CompactCel DIS, based on natural and certified organic ingredients can be used for replacing the above listed synthetic excipients. Here developers face the same challenges as when replacing the dry binders. A 1:1 replacement is not possible in most cases. The premix compound is suited for the use in tablet, capsule and granule formulations. To correspond to the requirements of a fast release dosage form, it enables a rapid break-up of solid oral dosage forms when they come into contact with moisture.

From oil to powder to capsules in a natural way

Industries are looking to add natural high-sources of vitamins, probiotics, omega 3-6-9 fatty acids, antioxidants, amino acids and hemp to their natural supplement products. Often in form of an oil or oily powder. Talking about the latter, manufacturers can achieve some benefits when incorporating the oil into a powder blend by using CompactCel MAB, which has good absorbing and free flowing properties. Especially, if the oil powder is then filled into hard gelatine capsules, precision dosing of exact amounts of ingredients or nutrients can be achieved. Flavour and odour masking can minimize unpleasant tastes and smells associated with certain nutrients. Protection from moisture, acids, heat and oxygen. It enhances stability, bio-availability and delivery. As well as ease of handling due to dry and free flowing.

Looking at the individual excipients necessary for the formulation of solid oral dosage forms, it can be said that there is a natural substitute for each synthetic filler, binder, flow agent, lubricant and disintegrant. However, with the restriction that a 1:1 replacement in the formulation is not always sufficient to replace 100% of the characteristic of a synthetic excipient.

References:

1. Survey data from the Organic Trade Association (OTA) (https://ota.com/organic-market-overview/organic-industry-survey)

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Biogrund (more information, website)