科研之友
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摘要
The dissolution test is usually employed to evaluate the performance of drug products. In this study, we compared the in vitro dissolution profiles of two diltiazem hydrochloride tablet formulations with that of a diltiazem hydrochloride compounded capsule formulation. Other characteristics investigated were average weight, drug content, disintegration, and uniformity of dosage units according to the USP monograph. The paddle apparatus was set at 75 rpm in 900 mL of water at 37.0 +/- 0.1 degrees C. Samples of 10 mL were withdrawn at 15, 30, 60, 120, 180, and 210 min without replacement and immediately filtered with 0.45-mu m PVDF syringe filters. The samples were then analyzed employing a spectrophotometer at 237 nm. The similarity (f(2)) and difference (f(1)) factors were calculated for dissolution profile comparison. The drug contents of the reference, generic, and compounded products were 100.01%, 93.17%, and 98.48%, respectively. All of the products showed suitable acceptance values for drug content uniformity (3.16, 8.37, and 4.76 for reference drug, generic drug, and compounded capsule, respectively). The generic drug formulation showed a calculated f2 value between 50 and 100 and an f(1) value less than 15. It was not possible to calculate the f(1) and f(2) values for the compounded capsules because they showed a drug release greater than 85% in 15 min. The generic and reference drugs were similar in relation to all tests. Furthermore, the generic and reference drug dissolution profiles were similar. The compounded capsules, which readily released the active ingredient, were not adequate only in the dissolution test. Further studies are necessary to investigate if the quick release of diltiazem from the drug products may pose any risks for patients, especially in Brazil where the compounded capsules are prescribed interchangeably with the reference drug.
- 出版日期2017-5
