Preparation and Quality Evaluation of Carboprost Methyl-hydroxypropyl-β-cyclodextrin Clathrate Sublin-gual Tablets / 中国药房

ABSTRACT

OBJECTIVE:To prepare the Carboprost methyl-hydroxypropyl-β-cyclodextrin (HP-β-CD) clathrate sublingual tab-lets,and conduct quality evaluation. METHODS:Wet granulation method was used to prepare Carboprost methyl-HP-β-CD clath-rate sublingual tablets. Using the appearance,calving time,wetting time and main drug content as investigation indexes,mass ratio of mannitol-lactose,povidone volume fraction and amount of low-substituted hydroxypropylcellulose(L-HPC)as factors,orthogo-nal test was used to screen the formulation. The calving time,wetting time,main drug content,content uniformity,dissolution de-gree of sublingual tablets with optimal formulation were evaluated. RESULTS:The optimal formulation was as follow as 78.82 mg of carboprost methyl-HP-β-CD clathrate (containing carboprost methyl 1 mg),100 mg of mannitol-lactose (mass ratio of 91) mixed powder,appropriate amount of 2% povidone solution,30 mg of L-HPC,and 1 mg of magnesium stearate. The calving time of prepared 3 batches of sublingual tablets was(25.30±3.21)-(26.53±2.69)s;wetting time was(64.65±8.07)-(65.54±7.21)s;main drug content was (96.13 ± 0.43)%-(97.06 ± 0.82)%;content uniformity was 5.95-7.68;the cumulative dissolution degree within 10 min was more than 50%,and it can completely dissolute within 30 min. CONCLUSIONS:Carboprost methyl- HP-β-CD clathrate sublingual tablets,which are up to requirements,are prepared successfully.