QUALITY BY DESIGN (QBD) TO OPTIMIZATION OF SEMI-SOLID SUSPENSION TYPE OF CAPTOPRIL TRANSDERMAL DRUG DELIVERY SYSTEM
Keywords:
Transdermal system, Captopril, Release liner, backing film, penetration enhancers, matrix stiffener, semi-solid suspension.Abstract
Introduction: In recent year, USFDA and EMA have issued the guideline on Quality by design (QBD). PAT and DOE are the essential tolls for QBD to evaluate the product. Focusing on the insight provided in these guideline as initiative was taken for the development of captopril transdermal system.
Objective: Optimization of the penetration enhancer, drug delivery and in-vitro adhesion of captopril transdermal system by QBD.
Material and Method: Captopril used as active moiety for transdermal systems. Captopril was obtained as a free sample from torrent pharma, Dipropylene glycol and oleyl alcohol was taken from croda. Bio PSA AC7-4202 silicone pressure sensitive adhesive was obtained from dow corning and Duro-tak®87-4287 acrylate pressure sensitive adhesive was obtained from national starch. Other excipients were used, colloidal silicone dioxide, tween-80, povidone K-12 and dehydrated alcohol. Matrix type of captopril transdermal system with combination of silicone and acrylate adhesive was prepared. Different concentration of captopril (5-15% w/w), di propylene glycol, oleyl alcohol (2.5-7.5% w/w) was used to get the desired delivery and different drying conditions (25-500C temperature, 20-40 min residence time) was used to get the desired volatile content.
Results: Captopril was delivered from 1.38-1.51 mg/day and 69.07-75.57 mcg/cm2/hr. 12% w/w of captopril and 7-9% w/w of dipropylene glycol concentration were required to get the desired delivery of captopril. 300C for 30 min was required to get the desired level of DPG to get drug delivery and residual solvent to get the desired adhesion.
Conclusion: Captopril and DPG concentration is responsible for drug delivery and drying condition is responsible to get the desired adhesion of the transdermal system. Further preclinical investigations are essential before to use of transdermal as an alternative with longer duration of action, improved bioavailability and patient convenience.
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