Abstract
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
Highlights
Qingkailing (QKL) is a famous herbal compound prescription in China, which consists of Radix isatidis, Flos lonicerae, Fructus gardeniae, Bubali cornu, Concha margaritifera, baicalin, cholic acid and hyodeoxycholic acid
A previous study has shown that the bioavailability of baicalin in soft capsule is higher than that of hard capsule [2]
Long-term stability comparison between soft and hard capsules based on multi-component quantification
Summary
Qingkailing (QKL) is a famous herbal compound prescription in China, which consists of Radix isatidis, Flos lonicerae, Fructus gardeniae, Bubali cornu, Concha margaritifera, baicalin, cholic acid and hyodeoxycholic acid. There are two marketed forms of QKL capsules in China, hard and soft capsule, with annual sales exceeding RMB 1 billion (US$ 0.15 billion) Evaluation of long-term stability of soft and in 2016. A previous study has shown that the bioavailability of baicalin in soft capsule is higher than that of hard capsule [2]. Soft capsule had a longer mean residence time (MRT), a higher maximum concentration (Cmax), and a larger area under the curve (AUC). Soft capsule may be more beneficial to the stability of the active ingredients both in vitro and in vivo. The drug dissolution behavior may affect the pharmacokinetic behavior in vivo
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