 |
Pilobuc™
Insert For Xerostomia
Controlled Therapeutics has developed its controlled release
polymer as a means to deliver the cholinergic agent, pilocarpine
across the buccal mucosa for treatment of xerostomia.
The advantages of buccal delivery of pilocarpine over
other routes are:
|
|
Rapid
absorption and onset of action |
|
|
Bypass
of first pass liver metabolism |
|
|
Reduced
side effects due to local delivery and lower, sustained-release
dosing |
The hydrogel polymer system is particularly well-suited
to buccal delivery because of its natural muco-adhesive
properties. The swelling and softening of the polymer
make it an effective and comfortable vehicle for oromucosal
delivery of pilocarpine.
Disease state
Xerostomia, meaning dry mouth is characterised by an uncomfortable sensation of oral dryness and is commonly associated with changes in salivary gland function. It may result from various medications, radiotherapy or various systemic autoimmune diseases.
The most significant disease, which causes salivary hypo-function and dry mouth, is Sjögren's syndrome, an autoimmune disorder, characterised by the chronic loss of lachrymal and salivary gland function. A reduction in salivary output causes oral dryness, which may lead to dysphagia, difficulty speaking, alteration in taste accompanied by an increase in the incidence of oral infections, including candida and dental caries. In the US alone over 4 million people suffer from Sjögren's disease. The global Sjögren's Disease market is estimated to be about £55million in 2004 increasing to $120million in 2010.
Therapeutic Indication
The most common therapy for xerostomia is oral pilocarpine using Salagen® tablets (MGI Pharma Inc.). This treatment which requires frequent oral dosing due to the short serum half-life of the active and this regimen can often cause doe limiting side effects in a significant number of patients.
Administration
The Pilobuc™ insert is a modified release hydrogel polymer buccal insert containing pilocarpine. It has been developed for the treatment of symptoms associated with primary and secondary Sjögren's the buccal insert is placed between the buccal mucosa and gingiva towards the back of the mouth. The bio-adhesive hydrogel polymer swells in the presence of moisture, but does not dissolve. The active drug is released from the hydrogel polymer insert in a controlled manner for up to three hours, thus reducing frequent administration. The Pilobuc™ buccal insert is gains maximum therapeutic effect without high peaks of drug release and the consequential side effect profile of pilocarpine oral tablets.
Clinical
Studies
Controlled Therapeutics have carried out four clinical studies with the Pilobuc™ insert. The results from these studies have been highly encouraging and the company is now looking to form a partnership with a marketing partner to complete the development program required to bring the product to market.
Potential
Market
It is estimated that more than 2 million patients suffer
from Sjögren’s Syndrome in the USA and EU.
|
