Abstract
Several drugs have poor oral bioavailability due to low or incomplete absorption which is affected by various effects as pH, motility of GI, and enzyme activity. The gastroretentive drug delivery systems are able to deal with these problems by prolonging the gastric residence time, while increasing the therapeutic efficacy of drugs. Previously, we developed a novel technology to foam hot and molten dispersions on atmospheric pressure by a batch-type in-house apparatus. Our aim was to upgrade this technology by a new continuous lab-scale apparatus and confirm that our formulations are gastroretentive. At first, we designed and built the apparatus and continuous production was optimized using a Box–Behnken experimental design. Then, we formulated barium sulfate-loaded samples with the optimal production parameters, which was suitable for in vivo imaging analysis. In vitro study proved the low density, namely 507 mg/cm3, and the microCT record showed high porosity with 40 μm average size of bubbles in the molten suspension. The BaSO4-loaded samples showed hard structure at room temperature and during the wetting test, the complete wetting was detected after 120 min. During the in vivo study, the X-ray taken showed the retention of the formulation in the rat stomach after 2 h. We can conclude that with our device low-density floating formulations were prepared with prolonged gastric residence time. This study provides a promising platform for marketed active ingredients with low bioavailability.
Highlights
Oral drug delivery systems are the most common and convenient forms to administer drugs due to their various advantages such as good compliance, low costs for storage and transport, and various forms which can be manufactured [1]
Our aim was to design, build, and optimize a novel foaming apparatus that is suitable for continuous production of foamed molten dispersions
The foaming process was optimized by a Box–Behnken experimental design to determine the most effective setup to create solid foams
Summary
Oral drug delivery systems are the most common and convenient forms to administer drugs due to their various advantages such as good compliance, low costs for storage and transport, and various forms which can be manufactured [1]. The development of a formulation of oral drug delivery systems is highly challenging due to the physiological variability of the gastrointestinal tract. Several drugs have poor oral bioavailability due to low or incomplete absorption which is affected by the various effects as mentioned above [4]. Some of the active ingredients (API) have an absorption window that is located on the upper part of the gastrointestinal tract: these are the stomach, jejunum, and duodenum in many cases [5]. The gastroretentive drug delivery systems are able to deal with these problems, by prolonging the gastric residence time while increasing the therapeutic efficacy of drugs [6]. The most important feature of these systems is that their density is below 1.00
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
