Oral solid dosage is still the preferred method of drug delivery, however, the patient’s experience when taking medication can mean they adhere to the regimen or not. Here, Dr Brian Wilson and Dr Graeme MacLeod from SPI Pharma look at the challenges of giving the patient the best experience possible and how these challenges can be solved.
formulation solution
Oral solid dose forms are still the most preferred method of delivering drugs to patients within the global pharmaceutical market. Not only do they offer a convenient, stable and efficacious route for administration of medicines but they also have the potential to improve the patient experience in taking the medication over the treatment process.
This latter point is key when considering patient adherence. If the patient has a good experience when taking the medication they are more likely to adhere to the treatment regimen. As a result of improved adherence it is possible to guarantee the efficacy of the treatment and reduce the total cost to healthcare providers.
The goal in a patient friendly dosage form is to reduce any unpleasant characteristic in taking the dosage regimen. Negative perception or failure of the formulated dosage can come from taste, mouthfeel, number of tablets needed, residence time in the mouth, and difficulty in swallowing. Some examples of dosage forms that have the patient experience in mind and are considered to be ‘patient friendly’ are chewable tablets, fast melt tablets, orally disintegrating tablets or orally dispersible powders.
Making convenient doses
Both seniors and paediatric patients present challenges when it comes to making convenient dosage forms. The task is to make the dosage form easy to take orally. Some dosage forms are required to be relatively large and often-above 1000 mg, while patients with dysphagia find tablets at 100–200 mg difficult.
Tablet size is less important in rapidly disintegrating dosages since they form an easily swallowed matrix. This can assist patients who display any degree of dysphagia. The fast disintegration time and positive organoleptics are key for patient acceptance. An alternative approach would be to formulate the drug as an orally dispersible powder that again disperses rapidly in the mouth.
We have also designed products that specifically target dosage forms with high drug loads. This provides the formulator with the ability to reduce the number of tablets that a patient requires. One aspect of patient-adherence is reducing the number of tablets taken and reducing the perception of dosing fatigue.
The right approach
Reducing unpleasant dosage attributes starts with the excipients used and the manufacturing approach. Our excipients and preformulated systems offer a positive sensory perception in terms of taste, smell, mouth feel, number of tablets needed, and residence time in the mouth.
However, every drug or compound that our customers formulate may have its own unique challenges that require careful thought and consideration. Our technical experts have years of experience in the design and the manufacture of oral dosage forms. Our customers can leverage this expertise to ensure the final dosage form meets the correct requirements for the patient. We also offer services to address taste and sensory issues if the attributes of the API negatively influence the taste or organoleptics.
SPI Pharma has a number of global customers that formulate a variety of actives into a range of oral dosage forms. A common theme with these customers are the challenges that prevent them from getting to market fast. An easy to use, preformulated and coprocessed platform requires minimal development time. This enables our customers to accelerate product development and provide speed to market strategies. This also means that patients benefit by having convenient dose engineered to enhance their medicine taking experience. In addition to our formulation and technical support, we also have a dedicated team of regulatory professionals who can help our customers navigate the license application process, again increasing the speed to market.
Products and selection
We offer a number of products used to formulate the range of orodispersible patient friendly dosage forms. Our base excipients can be used to custom build a formulation. The preformulated products already contain the functionality desired for that dosage form, which significantly decreases development time. These systems only require dry blending in the active, flavours, colours and lubricant to obtain near optimal performance on standard tablet presses. See below for more detailed information on the products offered.
Products offered for patient friendly dosage forms
Mannogem product line — This product line contains powdered, granulated and spray dried mannitols that provide specific performance attributes used in chewable or fast melt tablets.
Advantol 300 — This coprocessed, preformulated system delivers speed in development for chewable and fast melt dosage forms. Advantol 300 offers exceptional compaction and disintegration times.
Pharmaburst 500 — This coprocessed, preformulated system provides an excellent carrying capacity for high drug loads. In addition, these tablets retain very short disintegration times, which is a requirement from patients and regulators regardless of the tablet size. Pharmaburst 500 is engineered to significantly reduce development time, as it offers a complete formulation solution.
Pharmasperse 415 — This is a preformulated product for the creation of orally dispersible powders, packaged in stickpacks or sachets. The strength of this product is not only the shorter development time, but also that it is designed to be used without the need for a water or food vehicle.
Lubripharm SSF (sodium stearyl fumarate) — This is a lubricant system that offers a lower impact to disintegration time and tablet hardness. This is often essential for developing orally disintegrating tablet or fast melt tablets. In addition, Lubripharm gives fewer incompatibilities compared to standard direct compression lubricants.
Additionally, we have found that our customers look for information in various ways depending on how they are tackling the formulation and with what type of information they are given at the start of a project.
We have a table for Mannogem Mannitol,1 which differentiates the grades, notes the target applications, and lists the possible dosage forms. If the formulator already knows what application they need, this will help them to determine which grade is best suited for their requirements.
SPI Pharma table
We also offer product selection guides for our Antacid Active and DC Calcium Carbonate products. These tools allow our customers to follow a thought process to determine what product grade would work best for their formulation and then steers them to further information about that product. The comparison guide is a quick reference to explain what the components are, how they work and why they are used in a formulation.2
Advancing approaches
One of the main advances we have seen in OSD formulation over the past decade is in the development and use of co-processed excipients and the use of full pre-formulated solution platforms that provide the requisite functional attributes for both compaction and disintegration. These engineered solutions provide improved performance and also simplify formulation time; thus, leading to a decreased development time and products getting to market to help patients more quickly.
In the future, we believe that some advancement will come in the manufacturing approach, leading to unique process improvements in creating the dosage forms. As an example, the pharma industry is moving toward continuous processes that will require even more pre-engineered or co-processed excipient platforms to help with the upcoming unique challenges.
An increased emphasis will likely be put on the development of specific formulations for certain groups of patients, such as paediatrics and geriatrics where there are still minimal amounts of specifically designed products catering to the specific challenges of these patient groups. Flexible dosing, palatability and swallowability will be absolute key considerations for future oral dose forms. As a result, designing improved and novel, agile excipient platforms that meet these specific challenges will become a core requirement.
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