The new formulation technique – known as a ‘dry syrup’ - uses the artificial sweetener sucralose to mask the taste of bitter active pharmaceutical ingredients (API), making drugs easier to take and thereby increasing the likelihood patients adhere to treatment regimen.
Japan became the first country to approve a ‘dry syrup’ formulation late last month when regulators cleared a version of Aricept (donepezil hydrochloride) according to Eisai VP of corporate affairs, Sayoko Sasaki, who told in-Pharmatechnologist.com about its advantages for patients.
“Because the formulation can be taken in liquid form with the dry syrup powder suspended in water, it facilitates administration of the drug for patients prone to choking or coughing fits, or for whom administration of the existing tablet formulations is difficult,” Sasaki said.
Sasaki added that the dry syrup “can also be taken with water while still in powder form.”
A US NIH (National Institutes of Health) study from 2010 found that only 58% of more than 3000 Alzheimer’s patients adhered to their oral dosage therapy. The study found a variety of factors, including formulation, played a role in adherence levels.
The advantages of the dry syrup formulation “are not only an improvement in terms of facilitating drug compliance among patients with difficulties in taking existing formulations of the drug, but are also expected to reduce the burden placed on caregivers who assist with patient drug administration,” Sasaki said.
Aricept is also the only Alzheimer’s drug approved to treat all stages of the disease, according to the Mayo Clinic, though it’s available in other formulations as well, including film-coated tablets, orally disintegrating tablets, a jelly formulation, and fine granules, Sasaki said.
In addition to these formulations, an NIH study from 2007 found that a transdermal patch might be another effective formulation to optimize treatment compliance for Alzheimer’s.
Creation of the Formulation
From a production standpoint, the process of reformulating Aricept “presented no major difficulties as the formula and manufacturing method adopted for the formulation were both conventional,” Sasaki continued.
“Although masking techniques such as coating and other methods were considered when deciding how to mask the bitter taste of donepezil hydrochloride, ...the drug’s dry syrup formulation contains sucralose, a high-intensity sweetener that is also highly water soluble. Furthermore, the majority of the additive components selected for this formulation also easily dissolves in water,” he added.