Baclofen GRS once-a-day capsule
Baclofen is the 1st line treatment for more than half million people in the USA suffering from spasticity related to several underlying causes – multiple sclerosis, traumatic brain and spinal cord injuries, cerebral palsy and stroke. Oral Baclofen has a short t1/2 resulting into b.i.d. or t.i.d. dosing which increases the challenge of spasticity therapy due to reduced patient compliance.
Any conventional approach to design once-a-day formulation is challenged by Baclofen’s narrow window of absorption – restricted in duodenum part of GI tract.
Baclofen GRS is designed to improve the quality of spasticity treatment by providing a reliable “once-a-day” dosing option for the patients undergoing treatment for spasticity. The physiological challenge of absorption window is addressed by retaining the drug product in stomach for longer period (about 6 to 8 hours) which is achieved by combination of three mechanisms – Flotation, Size expansion and Muco-adhesion.
- Gas generating coat helps the formulation to remain floated on gastric content in the stomach.
- Expandable outer coat absorbs gastric medium and swells up to 8 to 10 times in size thus avoids passage of the capsule through pylorus during gastric emptying.
- The expandable outer coat also provides muco-adhesion so that capsule stays in the stomach for longer period of time
When Baclofen GRS is ingested, the outer most drug layer releases the drug which ensures plasma drug concentration immediately reaches within therapeutic window. The specialized capsule device remains floating on the gastric content and slowly releases remaining drug through controlled release core at a constant rate through pylorus – its site of absorption thus maintaining plasma drug concentration within therapeutic window for as long as 12 to 16 hours.
During the drug release process, the specialized capsule device maintains physical integrity but it is free of rigidity and sharpness, thus has no harmful effect on the gastric lining.
Baclofen GRS provides “once-a-day” dosage form by ensuring predictive, reliable and prolong plasma drug concentration within therapeutic window by overcoming anatomical and physiological barriers.