Preparation and Evaluation of a Novel Mucoadhesive Extend Release Microcapsule with Ion-exchange Resin Core Loaded with Beberine Hydrochloride
|School||Shenyang Pharmaceutical University|
|Keywords||An ion exchange resin Berberine hydrochloride Microcystis Gastric adhesion sustained-release formulations|
This selection of antibacterial drugs berberine hydrochloride (Berbamine hydrochloride, BH) as a model drug, the ion exchange resin with a novel drug carrier (Ion-exchange resin, IER) are combined to form the drug-resin complexes (Drug-Ion Exchange Resin Complexes DRC), and the emulsion solvent play dry wrapped stomach adhesion extended release coating layer, the final product - the the Berberine Hydrochloride resin complexes stomach adhesion the microcapsules (ad-ERDRC). In this article, the preparations in vitro and in vivo kinetics and release mechanism of the discussion and evaluation. The details are as follows: 1) static exchange kinetics and thermodynamics of the prepared drug-resin complexes, the effects of different factors affect the of resin drug loading capacity, ion exchange reaction and resin drug loading process are discussed. Determined according to the results of different drug loading factors influencing the final drug loading conditions: optional IRP88 of ion-exchange resin as a carrier, in the 37 ℃, pH5.0, the initial solution concentration under conditions of 1.0mg.mL-1 drug loading; use Poor Scanning Calorimetry (DSC), that a drug with an ion exchange resin between closely; Thermodynamic Study results show that the reaction can be spontaneous forward the endothermic reaction. 2) f2 similarity factor as indicators effects of temperature, speed, whether the changes in hydrogen ion concentration on the release of the drug-resin complexes impact. Experimental results show that the temperature and hydrogen ion concentration of the drug in the drug-resin complexes release significant effect the speed conditions no significant effect on the release, while drug release found Viswanathan equation. 3) the use of the W / O type emulsion - solvent volatile dry DRC wrapped sustained release the adhesion coat layer, through the optimization of the investigation of the coating process and coating prescription, considering the end of the coating process as follows: ethanol (V ): liquid paraffin (V): Span 80 (W) = 4:30:3 cured under the conditions of 30 ° C, 300 r · min-1 stirring Hui the 8h after Buchner funnel filtration collect microcapsules, petroleum ether washing , 25 ℃ vacuum dried for 24 h. Reach design release and adhesion requirements of the coating prescription: Carbopol 934 (Cp934) with DRC ratio of 0.75; proportion of Eudragit with DRC 0.9; Eudragit RS (ERS) and Eudragit RL (ERL) ratio is 0.6. 4) to create BH drug concentration in gastric tissue and mucosal tissue detection and monitoring of drug concentration in gastric tissue in the mucosal tissue of the rat oral drug trends change over time using this method. The results showed that the test formulation (ad-ERDRC) with reference ordinary preparations compared to similar gastric tissue drug concentrations high drug concentration can be maintained for a long time, but in the stomach tissue. Model fitting, the Senate eliminated from the stomach tissue preparation and test formulation in line with a speed equation. 5) the minimum inhibitory proved berberine hydrochloride Helicobacter pylori MIC for 500μg · mL-16) by gamma-scintigraphy tracer method to prove the test preparation (ad-ERDRC) with reference normal preparation indeed has better gastric retention capacity.