LAUSR

Purpose: To carry out a post-marketing evaluation of the stability and drug dissolution of Qingkailing soft/hard capsules. Methods: High performance liquid chromatography with diode array detection (HPLC-DAD) method was developed for the determination of three key ingredients (chlorogenic acid, geniposide and baicalin) and fingerprints of QKL soft/hard capsules. Stability tests were carried out based on long-term testing. The drug release profile of Qingkailing soft and hard capsules were studied using semi-bionic incubation experiments. Results: The linearity, precision, stability, repeatability and recovery of HPLC and fingerprint all met the requirements of CFDA. Stability data from long-term studies showed that within 6 months the contents of the three key ingredients in both soft and hard capsules remained > 90 %. However, fingerprint pattern statistical analysis showed that the soft capsule is more stable than the hard capsule. Furthermore, the key ingredients of the hard capsule dissolved much faster ( p < 0.05) than from the soft capsule. The level of dissolved drug of hard capsule is about 4 times the rate of soft capsule, after a 4-h incubation in gastric lavage fluid. In intestinal lavage fluid, more than 90 % of chlorogenic acid, geniposide and baicalin of hard capsule were dissolved in 2 h, while the soft capsule displayed a 12 h sustained release. Fingerprint pattern statistical analysis also showed that most of the components of soft capsule dissolved after 8 h. Conclusion: Compared with the hard capsule, Qingkailing soft capsule has certain advantages in stability and drug dissolution, which may affect the biopharmaceutics and the clinical effects of the drug. Keywords: Qingkailing capsule, Chlorogenic acid, Geniposide, Baicalin, Fingerprint, Sustained release, Principal component analysis