Taste Masking of Bitter Drugs for Paediatric Dosage Forms

October 27, 2021 Spread the awareness:

Most pharmacological actives have a disagreeable taste with intensities ranging from mild to high. Unfortunately, the most often necessary and consumed pediatric dosage forms, namely liquids and oral solid dosage forms. A range of technical solutions has been devised to reduce the impact of bad-tasting actives in liquid and chewable tablet formulations. Liquid formulations feature the broadest range of technical solutions, which is unsurprising considering the dosage form’s versatility in weight-based dosing and the particular issues it poses either in pure liquid form or as a suspension system.

Distinctions between adult and pediatric taste preferences

The distinctions between adult and pediatric taste preferences are evident, and one only needs to reflect on his/her own childhood to recall how those tastes evolved as they grew older. 

As youngsters, people develop acquired appetites for flavors or foods that they deem repulsive. Bitterness is an example of a flavor often avoided by youngsters yet is tolerated by adults in many items. Although taste and sensory perception researchers have documented differences in taste preference and palate sensitivity between children and adults, a stroll down the candy aisle at your local supermarket will reveal the wide range of flavor, texture, and sweetness characteristics that major confectionery manufacturers have developed to appeal to children’s tastes.

However, there is limited testing on the palatability of pharmacological formulations in the pediatric population, primarily because of ethical and safety considerations. Using the adult palate to determine the ideal levels of sweetness and flavor in a pediatric formulation can under-deliver sensory satisfaction to the intended patient population. An excellent place to start is by modeling goal taste and sweetness levels on confectionary products. 

Children’s taste preferences

Pediatric medicine producers must be conscious of children’s taste preferences, as the product’s flavor will significantly impact the child’s willingness to take the drug regularly. 

If it’s an over-the-counter drug, this may be evidenced by the parent’s or caregiver’s desire to repurchase it, or if it’s a prescription drug, like an antibiotic, it could be evidenced by the parent’s or caregiver’s willingness to stick to the dosing schedule.

As a result, in pediatric medicine, compliance becomes a primary driver of product formulation. A considerable amount of research on the effect of flavor on compliance in children has found that the taste of most pharmacological actives is unpleasant, ranging from a lasting chemical flavor to a strong bitterness with intensities ranging from mild to high. 

This is a dilemma for pharmaceutical companies because the most frequent pediatric dose forms, liquids, and chewable tablets, have the highest risk of drug exposure in the mouth, resulting in a terrible taste and poor compliance. 

Masking of bad-tasting actives is required to address these concerns, and several specialized techniques have been developed for different dosage forms and active medicinal components.

  • Formulations In Liquid Form

Some scientific ways to reduce poor taste in liquid formulations, like solutions and suspensions, include the following:

  • Taste Masking
  • Solubility Modification
  • Adsorption
  • Complexation, and
  • Barrier Systems

Taste Masking is the process of using flavors and/or sweetening substances to conceal any unpleasant flavors that may be present. Many pharmaceutical active ingredients have distinct medical flavor characteristics that can be off-putting for children. 

Identifying complementing flavors that disguise or hide any medicinal tastes can help lessen these medical overtones, making the product more bearable. As a result, aldehydes, esters, and ionones in red berry flavors are used for masking chemical tastes. Citrus flavors are also popular because their aldehydes, esters, ketones, and other flavor components substantially impact flavor and can help hide a variety of chemical notes. 

It is vital not to over-flavor the formulation as these sophisticated flavors might enhance chemical notes if they are not balanced in the formulation.

Formulations for Solid Doses

Because the off-tasting or bitter pharmaceutical active can be immediately exposed in the oral cavity, Taste Masking is equally crucial in pediatric solid dose forms. When a swallowable tablet is used, the tablet may be coated on the outside to create a barrier between the medicine and the oral cavity. Film coatings are commonly employed, and these coatings may contain high-intensity sugars and tastes for better palatability.

Chewable tablets are an appealing alternative to oral solid dosage forms, increasing compliance and simplicity of administration in children who have difficulties swallowing tablets. Manufacturers of chewable pills have developed them softer during the last 10 years to make chewing easier, allowing them to be taken without water. 

The famous red berry and citrus flavors have dominated, with sweetness levels ranging from moderate to high to help offset any bitterness. However, the fact that these tablets are supposed to be chewed presents unique hurdles in disguising the active medication components through taste.

Chewable tablets often contain coated medication particles to avoid excessive drug exposure in the mouth. Coatings should, in general, be somewhat insoluble in the mouth, release drugs quickly in the gastrointestinal tract, and have no chemical interactions with the medicine. 

These particles are coated with various water-soluble and water-insoluble polymers, latexes, lipids, and waxes, many of which are commercially available. Unlike those used in liquid formulations, solid dosage medication particles are frequently granulated and more significant in size, ranging from 100 to 400 microns which allows better mixing and blends homogeneously with other excipients, segregation resistance, and bulk flow from storage bins into and throughout the tablet press. When the particle size of high-dose actives is appropriate, the particles can be coated directly without the requirement for granulation.

Conclusion

One of the most important factors influencing patient compliance is a taste making it one of several significant formulation issues that certain drugs face. For health care practitioners, oral administration of bitter medications with a reasonable level of palatability is a key challenge, particularly for pediatric patients. 

Unpleasant, bitter flavors can be found in various oral medications, food and beverage products, and bulking agents. As a result, any pharmaceutical formulation with a pleasant taste would be preferred over a competitor’s product, resulting in better patient compliance and therapeutic value and increased sales and profits for the company. 

About ZIM Laboratories

ZIM Labs is an innovative drug delivery solution provider focusing on improving patient convenience and adherence to drug intake. We offer a range of technology-based drug delivery solutions and non-infringing proprietary manufacturing processes for the production and supply of innovative and differentiated generic pharmaceutical products to our customers globally. At ZIM Labs we provide our customers a comprehensive range of value-added solid dosage differentiated generic products in semi-finished and finished categories/formulations. These include granules, pellets (sustained, modified, extended-release), taste-masked powders, suspensions, tablets, capsules, and recently developed Oral Thin Films (OTF).

 

WhatsAppFor inquiries chat with us