Development of a gastroretentive pulsatile drug delivery platform

作者：Thitinan Sumalee; McConville Jason T^*

来源：Journal of Pharmacy and Pharmacology, 2012, 64(4): 505-516.

DOI：10.1111/j.2042-7158.2011.01428.x

• chronotherapy
• floating drug delivery
• gastroretention
• lag-time
• pulsatile drug delivery

Objectives To develop a novel gastroretentive pulsatile drug delivery platform by combining the advantages of floating dosage forms for the stomach and pulsatile drug delivery systems.
Methods A gastric fluid impermeable capsule body was used as a vessel to contain one ormore drug layer(s) aswell as one ormore lag-time controlling layer(s). A controlled amount of air was sealed in the innermost portion of the capsule body to reduce the overall density of the drug delivery platform, enabling gastric floatation. An optimal mass fill inside the gastric fluid impermeable capsule body enabled buoyancy in a vertical orientation to provide a constant surface area for controlled erosion of the lag-time controlling layer. The lag-time controlling layer consisted of a swellable polymer, which rapidly formed a gel to seal the mouth of capsule body and act as a barrier to gastric fluid ingress.
Key findings By varying the composition of the lag-time controlling layer, it was possible to selectively program the onset of the pulsatile delivery of a drug.
Conclusions This new delivery platform offers a new method of delivery for a variety of suitable drugs targeted in chronopharmaceutical therapy. This strategy could ultimately improve drug efficacy and patient compliance, and reduce harmful side effects by scaling back doses of drug administered.

• 出版日期2012-4