浅论甲钴胺片处方优选（Discussion on the optimization of the formulation of Mecobalamin Tablets）

浅论甲钴胺片处方优选（Discussion on the optimization of the formulation of Mecobalamin Tablets） 浅论甲钴胺片处方优选(Discussion on the optimization of the formulation of Mecobalamin Tablets) Discussion on the optimization of the formulation of Mecobalamin Tablets Date: 07, 10 Abstract: Mecobalamin Tablets; prescription; orthogonal design test; dissolution Objective to screen the best prescription composition [Mecobalamin Tablets. Methods: microcrystalline cellulose (MCC), excipients in twelve sodium dodecyl sulfate (SDS-Na), sodium carboxymethyl starch (CMS-Na), silica gel (SiliciiDoxydum) as investigation factors, each factor three levels, L9 (34) orthogonal test table layout, with Mecobalamin Tablets's dissolution as the main index the tablet weight difference as reference index, orthogonal test was 1. The influence of Mecobalamin Tablets stripping the main influencing factors of twelve sodium dodecyl sulfate adjuvant, the best prescription for the composition of microcrystalline cellulose (PH101) 35g, twelve sodium dodecyl sulfate 4.0g, sodium carboxymethyl starch 1.5g, silica powder 1.5g. Conclusion the formulation and preparation of the Mecobalamin Tablets dissolution is higher, and the product quality is stable, the preparation process is simple and feasible, suitable for industrial production. [Mecobalamin Tablets; prescription; orthogonal design test; dissolution Study, on, formulation, and, preparation, technique, of, Mecobalamin, tablets Abstract Objective To select the [optimum formulation technique of mecobalamin tablets. Methods The L9 (34) orthogonal table and four factors (dissolution as main factor, weight difference as reference factor were to select the) used best formulation by taking MCC (HP101), SDS-Na, CMS-Na and silicii doxydum as the four factors, and three levels were adopted for each factors. Results The experimental resultes indicated SDS-Na was the chief factor of influencing dissolution of macobalamin tablets. The optimum formulation was composed of MCC (HP101) 35g, SDS-Na 4.0g, CMS-Na 1.5g and silicii doxydum 1.5g. Conclusion The optimum formulation and preparing technique are reliable. Becasue the quatily of macobalamin tablets a Ccords, with, China, Pharmacopoeia, standard., preparing, technique, are, simple, and, feasible, it, is, The, suitable, for, industrialized, production. [Key, words, macobalamin, tablet; formulation; orthogonal, experiment, design; dissolution Methylcobalamin (Mecobalamin) is the endogenous coenzyme a derivative of vitamin B12 preparations. The Japanese who developed material, mainly used for diabetic neuropathy, polyneuritis four neuropathy and megaloblastic anemia. Methylcobalamin has achieved good effect in the treatment of many diseases, more and more by the clinician's attention, its prospect is quite broad. In this study, the dissolution rate was taken as the main index, and the difference of tablet weight was taken as the reference index. The orthogonal design was used to optimize the prescription composition. 1 instruments and reagents 1.1 instrument Agilent1100 high performance liquid chromatograph (Agilent Co); fluidized bed (German GEA company); S250/40 tablet machine (Germany KILIAN company); AG285 electronic balance (Mettler Toledo, Switzerland); dissolution tester (Tianjin University ZRS-8G intelligent wireless power plant); BGB-150C coating machine (Institute of Beijing aviation industry). 1.2 control samples (China reagent Mecobalamin for the control of pharmaceutical and Biological Products Institute); microcrystalline cellulose PH101 (Huzhou prospect); sodium carboxymethyl starch (Huzhou prospect); silica powder (Huzhou prospect); brown opadry (Shanghai Colorcon Ltd.). 2 methods and results Two 1 Orthogonal design according to the relevant literatures and tablet production practice of the company for many years, the four kinds of materials as a factor of four, respectively, microcrystalline cellulose (A), twelve sodium dodecyl sulfate (B), sodium carboxymethyl starch (C), silica powder (D). Each factor was taken at three levels, and the experiment was arranged with L9 (34) orthogonal table, with dissolution as the main index, as shown in table 1. Table 1 factor level table (omitted) 2.2 Mecobalamin Tablets prepared according to table 1 prescriptions of microcrystalline cellulose and sodium carboxymethyl starch 40s mixture, then add the prescription dose Mecobalamin raw medicine and twelve sodium dodecyl sulfate, with 50% ethanol solution into the wet granulation, drying room, 60 DEG C after drying, 30 mesh whole grain, then add the prescription the silica powder, magnesium stearate is the final mix, intermediate particles of Mecobalamin Tablets. For intermediate examination, the quality standards should be consistent with the intermediates. Make sure the tablets are weighed and pressed, then coated. According to the same method to 9 different groups of Mecobalamin Tablets. 2.3 determination of dissolution 2 Chinese according to pharmacopoeia version two appendix third determination of dissolution of 2 XC, light operation, take this product with water as solvent, 100ml, 50 revolutions per minute, in accordance with the law, by 40min, the solution of 2ml, filtration, the filtrate continued as for the test solution. Another Mecobalamin control amount, dissolved in water and diluted into each 1ml solution containing about 5 g, as the reference solution. According to the method of content determination, the two solutions mentioned above are 20 l each. They are injected into the liquid chromatograph and recorded respectively. According to the external standard, the dissolution amount of each piece was calculated by peak area. The limit is 75% of the mark (dissolution results are shown in Table 2). Table 2 the results of orthogonal design experiment (omitted) R value of Table 2 shows that the degree of dissolution of four excipients factors is B > A > C > D. 2.4 variance analysis is shown in table 3. Table 3 Variance analysis table note Abstract: F0.05 (2, 3) =9.55 Table 3 shows, the B factors on the dissolution of Mecobalamin Tablets have a significant effect, no significant effect of D factors. Combining the extreme range (R) analysis, the optimum prescription composition was determined to be A1B3C2D2. 2.5 after confirmatory test to determine the best prescription composition, according to the new prescription produced 6 batches of samples, according to law. Results the dissolution rates of batches of 6 batches of 06020101, 06020201, 06020301, 06020401, 06020501 and 06020601 were 92.5%, 90.6%, 92.2%, 92.1%, 92.3%, 93.1% and 91.8%, respectively. It can be seen that the products produced by the optimized formula have higher dissolution rate and the dissolution rate of 40min is above 90%. And the product quality is stable, other indicators are in line with product quality standards. The cumulative release percentage was measured by the same method commercially imported Mecobalamin Tablets, two sets of data for statistical analysis, the results show that the optimum prescription of the measured volume better, see figure 1. The cumulative release percentage figure 1 for the import sale of Mecobalamin Tablets and the (omitted) 3 discussion Methylcobalamin is red or dark red powder, see light decomposition, in the production and inspection process to avoid light operation. Twelve alkyl sodium sulfate is an anionic surfactant with strong emulsification function. It is often used as a solubilizing agent for some insoluble drugs. The results of orthogonal test showed that the solubilization agent twelve sodium dodecyl sulfate on Mecobalamin Tablets's dissolution has significant effect in the premise of ensuring product quality should be the amount of the solubilizing agent. Selected by the orthogonal test of the preparation process of Mecobalamin Tablets, the dissolution is higher, and the product quality is stable, all indexes meet the requirements. The preparation process is simple and convenient, and is suitable for industrial production. [References 1. Formulation of Doxazosin Mesylate Tablets's Su Qing research. Journal of Guangdong Pharmaceutical University, 2004, 20 (2) Abstract: 115. 2 National Pharmacopoeia Commission. Pharmacopoeia of the People's Republic of China (two parts). Beijing, abstracts: Chemical Industry Press, 2005, appendix XC.