Shanghai Meiyou Pharmaceutical Co. Ltd.

The purpose of the present study was to prepare a clonidine hydrochloride (CH) sustained-release suspension.

The processes involved in the drug formulation included drug loading, impregnating, and suspension preparation. Clonidine hydrochloride drug-resin complexes (CH-DRC) were prepared using the bath method and the CH-DRC impregnated before the microencapsulation process. Based on the bottom spray fluidized bed coating method, the CH microencapsulated drug-resin complexes (CH-MC) were also prepared using Surelease^® (the suspension of ethyl cellulose aqueous dispersion) as the coating material. The effects of coating (process/formulation) on the in vitro release of coating microcapsule were evaluated via single factor investigation and orthogonal design optimization. The CH-MC with optimized formulation was further dispersed in a suitable medium to obtain a sustained-release suspension. Rats were given commercial CH ordinary tablets and the CH sustained-release suspension via intragastric administration. The plasma concentration-time curve and related pharmacokinetic parameters were investigated using the non-compartment model.

The T_max of the CH sustained-release suspension was delayed from 2 h to 5 h compared with the CH ordinary tablets. Similarly, the C_max was reduced from 32.138 µg·mL^-1 to 18.150 µg·mL^-1 with the concentration-time curve being more gentle compared with the commercially CH ordinary tablets. After oral administration, the relative bioavailability of CH sustained-release suspension (AUC_0-24 of 137.703 µg·h·mL^-1) to its CH ordinary tablets (AUC_0-24 of 123.337 µg·h·mL^-1) was 111.65%.

The findings showed that the CH sustained-release suspension for oral administration was successfully formulated.

Oxymatrine has antagonisms to kidney ischemia/reperfusion injury, endotoxic renal injury, CCl4-inguced chronic renal injury, adriamycin nephrosis, renal interstitial fibrosis after ureteral obstruction in rat, and renal fibrosis induced by high glucose and high fat.Its mechanisms of renal protection are antioxidation, anti-inflammation, hypoglycemia, and hypolipemia of oxymatrine, and inhibiting signaling pathways of ROS/TLR4, PERK/ATF4/CHOP, JAK2/STATs, TGF-β1/Smads, and NF-κB/TNF-α, to alleviate renal tissue inflammation and extracellular matrix deposit, and block renal injury and fibrogenesis.

Matrine has the effects in the prophylaxis and treatment of rat hepatoma induced by diethylnitrosamine, and growth of murine hepatocarcinoma cell H22 transplantation tumor in mice.Matrine inhibits proliferation, adhesion, migration, invasion, and induces apoptosis in association with dosage on hepatoma H22 cells, SMMC-7721 cells, BEL-7702 cells, BEL-7704 cells, Hep3 B cells, QGY cells, QGY/CDDP cells, 97 H cells, CRBH-7919 cells, CRBH-7919/mdr1 cells in vitro.Matrine induces differentiation in hepatoma SMMC-7721 cells, BEL-7702 cells, BEL-7404 cells, and poorly differentiated hepatic oval cells too.Matrine elevates immunoregulative function in tumor-bearing body too.In clin. application matrine is being tried to treat and prevent recurrence of heptocarcinoma.