Abstract
Expandable drug delivery systems are one of many gastroretentive delivery systems which have emerged during the last few years. Expandable systems are usually folded in a capsule and expand to dimensions greater than the pyloric sphincter upon contact with gastric fluid. This prevents them from being evacuated by gastric emptying. The main objective of developing such systems is to increase the residence time of a specific drug in stomach; controlling its release, increasing its bioavailability and decreasing its side effects and dosing frequency. An expandable gastroretentive drug delivery system containing Gabapentin was developed using experimental design (D-optimal reduced quadratic design). This system was able to unfold at stomach pH in less than 15 minutes and obtain a controlled release of 78.1 ± 4.7% in 6 hours following zero-order release kinetic model. It is rigid in stomach and its rigidity decreases at intestinal pH. FTIR analysis indicated the occurrence of hydrogen bonding in Gabapentin when present in the developed system, which might be responsible for the drug’s controlled release. XRD analysis indicated that Gabapentin physical properties changed from crystalline in the typical state to amorphous in the developed system.
Highlights
IntroductionRepresents a matrix system in the form of a layer
Represents a matrix system in the form of a layer. This system was developed using methodical optimization techniques based on experimental design (D-optimal reduced quadratic design). It is comprised of the active ingredient (Gabapentin), a plasticizer to increase the flexibility of the layer (Poloxamer P407), a mixture of hydrophobic polymers stable at stomach pH to control the drug release (Eudragit L100, S100, L100-55) and a swellable hydrophilic polymer which will expand as a result of fluid absorption (Gelatin)
Citric acid and sodium bicarbonate were tested on three additional samples and provided positive results
Summary
Represents a matrix system in the form of a layer. This system was developed using methodical optimization techniques based on experimental design (D-optimal reduced quadratic design). It is comprised of the active ingredient (Gabapentin), a plasticizer to increase the flexibility of the layer (Poloxamer P407), a mixture of hydrophobic polymers stable at stomach pH to control the drug release (Eudragit L100, S100, L100-55) and a swellable hydrophilic polymer which will expand as a result of fluid absorption (Gelatin). In the present research; drug release, unfolding, degradability and elasticity tests were performed on the developed formulations. Physical and chemical characteristics of Gabapentin were inspected using XRD and FTIR analyses, respectively
Sign-in/Register to view highlights & summary Sign-in/Register to access full text options 
Free) 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a call
