The Preparation And Quality Control Of Candesartan Cilexetil Tablets

ObjectiveThe purpose of this study is to explore and optimize the formulation and preparation method of candesartan cilexetil tablets,and estabilish its quality standard.We plan to build a sound,scientific preparation method suitable for industrial production.Then,we plan to establish methods for detecting the solubility and other quality control items in candesartan cilexetil tablets.At last,we carried out the stability study of self-made candesartan cilexetil tablets.MethodsThree sections of the research are as follows.The first section is the optimization of the formulation and preparation for self-made candesartan cilexetil tablets.The second section is the application of the quality control to the prepared candesartan cilexetil tablets.The third section is the study of the stability of self-made tablets.On the basis of a wide range of literature reviewing,the reasonable design of the tablet formula was carried out.By comparing with the reference preparation "Blopress",we investigated the formulation,excipients,related substance,dissolution,tested the compatibilities of pharmaceutical excipients with active pharmaceutical ingredients,solubility and hygroscopicity of the drug,the mixing method and parameter,the amount of additives,wet granulation process and investigated the precision and reproducibility of dissolution,we also tested the stability of the preparation,and then the final formula and preparation method were established.Scientific and reliable quality standards and quality control methods for candesartan cilexetil tablets were established,through screening and validation of analytical methods for identification,related substances,assay,uniformity of content and dissolution,etc.The stability tests were carried out preliminarily to provide the reference data and information for the quality control,package,transportation and establishment of storage conditions of home-made candesartan cilexetil tablets.ResultsThe formula of self-made tablets(8 mg)was determined: candesartan cilexetil 8 mg,lactose 79 mg,HPMC(E5)4mg,pregelatinized starch 30 mg,PEG6000 6 mg,CCNa 3 mg,magnesium stearate 0.6 mg,30 % ethanol(about 12 μL).The self-made tablets(8 mg)were prepared as follows.Pretreatment: passing the excipients except PEG6000 through 80 mesh whirlpool vibrating screen;Blending: mixing the formulation amount of pregelatinized starch,CMC and the lactose in the horizontal quick mixing granulator to obtain Mixer Ⅰ,dissolving PEG6000 of formulation amount in proper amount of 30 % ethanol,then adding the active ingredients into the PEG6000 solution,mixing at 5 kr/min for 3～5 min to obtain MixerⅡ,blending Mixer Ⅰ and Mixer Ⅱ;Granulating: granutaing through 24 mesh pendular granulator;Drying: drying at 50 ℃ to keep the water amount below 3 %;Sizing: passing through 24 mesh pendular granulator;Mixing: adding magnesium stearate and CCNa to the materials and mixing in the three-dimensional blender;Tablet pressing: calculating the weight of tablets,and controlling the uniformity of weight in the range of ±5 %.HPLC method were applied to identify self-made tablets.We determined the dissolution,content of active ingredient and the related substance by HPLC method,established the quality standards and the stability was tested.The test results obtaind met the related national standards.ConclusionsIn this research,the formulation and preparation methods of candesartan cilexetil tablets were optimized,the quality standards were established and the stability was tested.The quality of self-made candesartan cilexetil tablets in in vitro pharmaceutical research is basically consistent with the original product "Blopress",which conforms to the conformance assessment standards of State Food and Drug Administration.