Design and evaluation of a dry coated drug delivery system with floating-pulsatile release.
The objective of this work was to develop and evaluate a floating-pulsatile drug delivery system intended for chronopharmacotherapy. Floating-pulsatile concept was applied to increase the gastric residence of the dosage form having lag phase followed by a burst release. To overcome limitations of various approaches for imparting buoyancy, we generated the system which consisted of three different parts, a core tablet, containing the active ingredient, an erodible outer shell and a top cover buoyant layer. The dry coated tablet consists in a drug-containing core, coated by a hydrophilic erodible polymer which is responsible for a lag phase in the onset of pulsatile release. The buoyant layer, prepared with Methocel K4M, Carbopol 934P and sodium bicarbonate, provides buoyancy to increase the retention of the oral dosage form in the stomach. The effect of the hydrophilic erodible polymer characteristics on the lag time and drug release was investigated. Developed formulations were evaluated for their buoyancy, dissolution and pharmacokinetic, as well gamma-scintigraphically. The results showed that a certain lag time before the drug released generally due to the erosion of the dry coated layer. Floating time was controlled by the quantity and composition of the buoyant layer. Both pharmacokinetic and gamma-scintigraphic data point out the capability of the system of prolonged residence of the tablets in the stomach and releasing drugs after a programmed lag time.
Zou
Hao
H
Department of Pharmaceutics, School of Pharmacy, Second Military Medical University, No. 325 Guohe Road, Shanghai 200433, PR China.
Jiang
Xuetao
X
Kong
Lingshan
L
Gao
Shen
S
D000328:Adult; D000818:Animals; D055598:Chemical Phenomena; D002626:Chemistry, Pharmaceutical; D002627:Chemistry, Physical; D002851:Chromatography, High Pressure Liquid; D003692:Delayed-Action Preparations; D004285:Dogs; D016503:Drug Delivery Systems; D015195:Drug Design; D005079:Excipients; D005746:Gastric Emptying; D006801:Humans; D065347:Hypromellose Derivatives; D007553:Isotope Labeling; D008297:Male; D008747:Methylcellulose / Q000031:analogs & derivatives; D004364:Pharmaceutical Preparations / Q000008:administration & dosage / Q000378:metabolism; D010599:Pharmacokinetics; D012995:Solubility; D013607:Tablets; D013667:Technetium