盐酸益母草碱片的制备及质量评价

OBJECTIVE To prepare Leonurine hydrochloride tablets and evaluate the quality. METHODS The wet granulation technology was adopted;leonurine hydrochloride was used as the crude drug, and the types of fillers, disintegrants, binders and lubricants were screened by single-factor experiments. Combined with orthogonal experiments, using the cumulative dissolution rate within 15 minutes (using water as dissolution media) as index, the proportion of disintegrants, the mass fraction of binder solution, and the proportion of lubricants were screened and verified. The in vitro dissolution behavior of the prepared Leonurine hydrochloride tablets(dissolution media were hydrochloric acid solution of pH1.2, acetic acid-sodium acetate solution of pH4.5, phosphate buffer solution of pH6.8, water), tablet appearance, hardness, friability and content uniformity were tested according to the general principles in 2020 edition of Chinese Pharmacopoeia(part Ⅳ). RESULTS The optimal formulation of Leonurine hydrochloride tablets included leonurine hydrochloride crude drug of 500 mg, dextrin of 9 250 mg, crosslinking polyvingypyrrolidone of 200 mg, magnesium stearate of 50 mg, 1％ hydroxypropyl methyl cellulose solution of 4 mL. The average 15-minute cumulative dissolution rate of the three batches of tablets was 81.25％(RSD＝1.12％, n＝3). In above 4 dissolution media, the dissolution equilibrium of prepared tablets could be reached within 30 minutes, and the cumulative dissolution rates exceeded 85％. The prepared tablets had uniform beige in color, smooth surface, complete edge, no mottle, spot, foreign matter, etc., hardness of 57.3 N(n＝6), weight loss rate of 0.15％. The content uniformity was in accordance with relevant provisions in 2020 edition of Chinese Pharmacopoeia(part Ⅳ). CONCLUSIONS Leonurine hydrochloride tablets are successfully prepared, and the quality comply with relevant regulations.