Drotaverine Hydrochloride Superporous Hydrogel Hybrid System: a Gastroretentive Approach for Sustained Drug Delivery and Enhanced Viscoelasticity

This study aims to prepare drotaverine hydrochloride superporous hydrogel hybrid systems (DSHH systems) to prolong its residence time in the stomach, provide extended release and reduce its frequency of administration. Drotaverine hydrochloride (DRH) is a spasmolytic drug that suffers from brief residence due to intestinal hypermotility during diarrheal episodes associated with gastrointestinal colics resulting in low bioavailability and repeated dosing. Eight DSHH systems were prepared using gas blowing technique. The prepared DSHH systems were evaluated regarding their morphology, incorporation efficiency, density, porosity, swelling ratio, viscoelastic property, erosion percentage and release kinetics. The FH8 formula containing equal proportion of chitosan (3%) /polyvinyl alcohol (3%) as strengthener and crosslinked with tripolyphosphate showed the highest incorporation efficiency (91.83 +/- 1.33%), good swelling ratio (28.32 +/- 3.15% after 24 h), optimum viscoelastic properties (60.19 +/- 3.82 kPa) and sustained release profile (88.03 +/- 2.15% after 24 h). A bioequivalence study was done to compare the bioavailability of the candidate formula versus Spasmocure (R). Statistical analysis showed significant (P < 0.05) increase in bioavailability 2.7 folds with doubled Tmax (4 h) compared to the marketed product (2 h). These results declared that the superporous hydrogel hybrid systems could be a potential gastroretentive approach for the sustained delivery of drugs with short residence time with enhanced viscoelasticity.

Automated summary

This study aimed to prepare superporous hydrogel hybrid systems of drotaverine hydrochloride (DSHH systems) to extend its residence time in the stomach and achieve sustained release. The FH8 formula showed the highest incorporation efficiency, good swelling ratio, optimal viscoelastic properties, and sustained release profile. A bioequivalence study revealed increased bioavailability and delayed Tmax compared to the marketed product. These results suggest that the DSHH systems could be a potential gastroretentive approach for drugs with short residence time.