Study On The Taste-Masking Performance Of Mesoporous Molecular Sieves On Cetirizine

Along with the improvement of life quality, therapy convenience and complianceof patients has drawn increasingly attention. Taste is one of the most important factorsgoverning patients’ compliance. Among those771kinds of chemical entities recordedin the first part of the main body of Chinese Pharmacopoeia2010Edtion Version2,one third are described to have some degrees of bitter taste. What’s more, bitter tastehas a unpleasant character of a little perception and long duration. Since drugs withunpleasant bitter-tasting components would limit their clinical use and oralpreparations severely, how to reduce or inhibit the bad taste has become an importantissue. Now there are various approaches to mask drug’s bitter taste, however, the drugdosage problem appears on condition the good taste is achieved. It can be explainedthat too much excipient such as flavors has to be added in order to achieve propertaste and disintegration, thus the application of large doses bitter drug is limitedawfully. To solve this problem, the efficiency of taste-masking agents must beincreased.Mesoporous molecular sieve is a kind of porosint that has regular pore diameter(2-50nm), large surface area and large pore volume with no pharmacological activityor toxicity. In recent decades, mesoporous molecular sieves are widely used inbio-medicine field. Yet the current reports mainly concentrated in material synthesisand drug release performance, the applications of mesoporous molecular sieves indrug taste-masking field has not yet been reported. Considering the outstanding drugloading capacity, it may provide a new approach to large dosage drug taste mask.Thus, it is of great theoretical significance and application value to explore the newtaste-masking function of mesoporous molecular sieves.In this paper, MCM-41, MCM-48and hollow mesoporous silica sphere (HMSS)were synthesized using hydrothermal method. With bitter drug cetirizine (CTH) asmodel drug, CTH-sieve composites were prepared with impregnation method andthose composites were characterized by means of X-ray diffraction (XRD), Infraredspectroscopy (IR), nitrogen physical adsorption and thermogravimetric analysis (TGA). In addition, three commonly used taste-masking agents including aspartame(APM), β-cyclodextrin (β-CD) and ion exchange resins were adopted to cover theCTH bitter flavor. The taste-masking performance of CTH-sieve composites andCTH-taste-masking agent composites was compared, and the mechanism of tastemasking was analyzed. Efforts were also made to explore the new function ofmesoporous molecular sieve to cover bitter taste.Main findings are:(1) MCM-41, MCM-48and HMSS each showed a large CTHloading capacity, and could effectively reduce the CTH bitter taste and cover the oralmucous membrane irritation;(2) The pore structure of mesoporous molecular sievelargely affected taste masking efficiency. The hollow cavity of HMSS could storemore drugs, so the drug loading content was higher; the mesoporous shell had atwo-dimensional channel structure similar to MCM-41but a little bit smaller, so thedrug release rate was slower than MCM-48which had three-dimensional channelstructure, and also slower than MCM-41. It was suggested that the drugs contactingtaste buds which HMSS carried were least, making the taste covering performancebest;(3) Comprehensive comparison of the taste masking performances of HMSS,APM, β-CD and Amberlite IRP-69found that APM dosage was too large and couldnot hide drug pungency; β-CD tasted good yet drug loading content was too small;ion exchange resin Amberlite IRP-69could be loaded in higher content and improvedtaste significantly, however it had limited application field; HMSS showed strongdrug loading capacity, significant taste masking effect and wide application. It isbelivable that HMSS with obvious advantages can be named as a new taste-maskingagent, providing a new approach to bitter drug taste mask, especially to large dosebitter drugs. This work also provides some theoretical and experimental basis for theapplication of ordered mesoporous materials in drug taste mask field.