Novel Oral Dosage Forms : Introduction and the Requirement for Quality

Testing the alternatives to traditional tablet-form medications
 
Oral drug delivery represents the largest share of the pharmaceutical market, accounting for approximately 90% of all medicines prescribed. 

The oral route remains the perfect one for the administration of therapeutic agents, due to the general simplicity and cost-effectiveness of the therapy, the accuracy of dosing, the avoidance of pain and the ability to self-medicate. Whilst it is considered the most traditional and easiest route of delivery, it is – perhaps surprisingly – not always the most user-friendly, for a number of reasons.

Traditional orally-administered drugs are dispensed in solid dosage forms such as capsules, caplets or tablets and liquid forms such as solution, suspension and emulsion. Tablets are the most widely accepted given the convenience in terms of self-administration, compactness and ease of manufacture. 

However, children, geriatric patients and, for example, disabled people often have trouble in swallowing the traditional solid dosage forms and therefore do not take their medicines as prescribed. Sensation in the mouth, taste, package opening and ease of intake are major factors influencing the experience of patients taking their medication. 

According to a recent market study commissioned by Hermes Pharma, difficulty in swallowing (or dysphagia) is seen to affect nearly 55% of the general population. 

Furthermore, dosing is an issue with tablets or capsules as most medications are available in doses that are significantly too large for the paediatric population and cannot easily and reproducibly be divided into smaller doses. 

To overcome difficulties of tablets being too big, becoming stuck in the throat and having an unpleasant taste/odour, people will turn to breaking tablets before swallowing, chewing or crushing them up. Crushing tablets to mix them with food or water may change the API release profile and therefore the rate or extent of drug absorption e.g. for enteric-coated tablets. 

Another common practice of cutting tablets may be acceptable for some drugs, however this practice can introduce considerable variability between doses. More worrying is the percentage of people who would resort to not taking their medication at all in the face of swallowing difficulties.

Apart from these problems experienced by consumers, there are other drawbacks of oral delivery such as degradation of the drug by the stomach’s enzymes and acids and first pass liver metabolism. 

In addition, consumer habits and demands are changing. Today’s patients have grown accustomed to having freedom of choice and the benefits of convenience. Instant access to a wealth of medical information and the ability to become more involved in their personal therapy decisions is leading to them requesting specific products and treatments.

Some new developments taking place in the area of oral delivery include delivering medication through quick-dissolving tablets or strips and designing drugs to deliver macromolecules such as proteins and peptides. Pharmaceutical products now need to appeal to a wider range of preferences, from the most successful treatment needs through to lifestyle requirements, in order to deliver medical and commercial success in the future.

Conventional tablets and capsules exhibit a range of drawbacks and may no longer be the best solution for large segments of the population. By offering products that taste favourable, are easy to swallow and convenient to take, companies can improve patient experience, increase compliance, and boost the effectiveness of treatment. 

Dosage forms such as effervescent tablets, orally disintegrating granules, films, lozenges and chewable tablets are truly user-friendly. They allow healthcare companies to expand existing product lines, prolong product lifecycles, revitalise brands and, at the same time, grow revenues. Several of these alternative dosage formulations have already been introduced to fill the need for easy administration and reliability and are ideally suited for those unable to swallow traditional solid dosage forms.

The global pharmaceuticals market is worth US$300 billion a year, a figure expected to rise to US$400 billion within three years, according to the World Health Organisation. Driving forces behind this fast-moving, global growth are increasingly strong drug development pipelines, the ongoing demand for innovative therapies and the increase in average human life span leading to the decline, with age, in swallowing ability.  

All these developments have served to intensify competition, and competitive advantage is increasingly being defined not in terms of price, but effectiveness, safety, hypoallergy and, most importantly, quality. 

The Requirement for Quality

Billions of euros are pumped into research and development programmes lasting more than a decade, and millions of man-hours are spent maintaining rigorous control of quality standards. 

In both areas, manufacturers naturally require equipment and processes which are both reliable and cost-effective, to save time and lower overheads. 

One field becoming increasingly significant is that of texture analysis, which is being used to uphold quality standards, whilst providing essential product data and benchmarking statistics.

The science of texture analysis has its roots in the food industry in the mid-1950s, when manufacturers began to require more sophisticated and objective assessment of their products. Human taste testing panels could help clarify preferences and descriptions of visual appeal and taste, but the definition of texture, and man’s perception of it, was more complex. 

Tablet indentation test
using a spherical probe

The analysis of textural (or rheological) properties is an assessment or measurement of a particular characteristic, such as adhesiveness, hardness, break strength or elasticity. Contrary to verbal description (sticky, tacky, gooey, gummy), texture analysis made these rheological characteristics quantifiable – and therefore comparable. 

Since its introduction into pharmaceuticals, the scope of texture analysis has widened considerably – into cosmetics, packaging, personal care products and medical devices. Instruments such as Stable Micro Systems’ TA.XTplus texture analyser may be supplied with a range of optional Probes and Attachments, which are fitted to the body of the machine in order to perform various tests on different products during research and development, production and quality control.

As the pharmaceutical industry continues to grow and diversify, NPD and quality control departments have never been busier – or more challenged. In today’s tough environment, diverse regulatory requirements have to be juggled with innovative ingredients, new packaging formats, changing consumer demand and financial pressures. Never before has it been so difficult to perfect a product and achieve long-term commercial success.

A summary of how to perform texture analysis on the alternatives to traditional tablet-form medications using a TA.XTplus Texture Analyser can be viewed in this video...

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We can design and manufacture probes or fixtures for the TA.XTplus texture analyser that are bespoke to your sample and its specific measurement.

Once your measurement is performed, our expertise in its graphical interpretation is unparalleled. Not only can we develop the most suitable and accurate method for the testing of your sample, but we can also prepare analysis procedures that obtain the desired parameters from your curve and drop them into a spreadsheet or report designed around your requirements.

For more information on how to measure texture, please visit the Texture Analysis Properties section on our website.

The TA.XTplus texture analyser is part of a family of texture analysis instruments and equipment from Stable Micro Systems. An extensive portfolio of specialist attachments is available to measure and analyse the textural properties of a huge range of food products. Our technical experts can also custom design instrument fixtures according to individual specifications.

No-one understands texture analysis like we do!

To discuss your specific test requirements click here...