Study On Preparation Of Cold-Water-Soluble Starch And Including Ibuprofen In Situ

Ibuprofen is commonly used as a kind of non-steroidal anti-inflammatory drugs(NSAIDs),and it is widely used in clinical treatment of inflammatory diseases.However,its application is limited due to disadvantages of its low solubility in water,fast drug metabolism,short half-life,severe mucosal irritation of intestines and stomach and so on.In order to overcome these problems,various medicament dosage forms of ibuprofen were prepared.Starch possesses good biocompatibility and biodegradability.It can be induced to produce a single-helix structure because of the presence of hydrophobic ligands.The guest molecules can be trapped within its helices to form supermolecule assemblies(inclusion complexes).Cold water soluble starch exhibited good cold water solubility,which can increase the chance of interaction with ibuprofen,thereby increasing the dose of drugs.In this work,cold water soluble starch-ibuprofen inclusion complex(CWS-IBU)was in-situ prepared,so as to find a new method of preparing sustained-release preparations for NSAIDs,which can alleviate their adverse reactions and improve their bioavailability.Cold water soluble starches(CWS)were prepared from potato starch by using alcoholic-alkaline method,and CWSs with different solubility were obtained according to the orthogonal test conditions.Based on this process,the CWS-IBU complexes were in-situ prepared and their structural and release properties were characterised.Through the orthogonal test,the optimal conditions of preparing CWS were as follows:lOg of starch was dispersed in 200 mL 50%(V/V)ethanol solution by stirring at 45?,and then 20 mL NaOH solution(3.0 mol/L)was added;the mixture was kept to react for 50 min.Under these conditions,the solubility of CWS was 88.0%.The CWS-IBU(CWS/IBU ratio of 4:1)complexes were in-situ synthesized.The optimum drug loading of CWS-IBU complex was 12.1%.The X-ray diffraction(XRD)analysis indicated that CWS and IBU formed the V-type crystalline.The FTIR results confirmed that starch molecules interacted with ibuprofen through hydrogen bonding.Thermogravimetric analysis(TGA)showed CWS-IBU complex was cleavage at 220? or more,so the stability of ibuprofen was improved.The release profile in simulated gastrointestinal fluid indicated that CWS-IBU complexes are stable in simulated gastric fluid;all complexes show sustained release characteristics in simulated small intestinal fluid.This suggested that the CWS-IBU complexes had the property of intestinally targeting and controlled release of IBU.It is thus advantage for improving their bioavailability and alleviating the gastric side effect of IBU.