Design and evaluation ofSan-huangdispersible tablet – an efficient delivery system for Traditional Chinese Medicine

Abstract

San-huang dispersible tablet (SHDT) was designed with a patented technology to enrich the active ingredients in rhubarb and with a wide selection of excipients in the new manufacturing procedure. The total rhubarb anthraquinones were first enriched in the extract by our patented technology. Eudragit L100, S100 and PEG-6000 were used to release a part of the total rhubarb anthraquinones at the colon to induce the cathartic effect of the anthraquinones by another patented technology. Microcrystalline Cellulose (MCC), low-substituted hydroxypropyl cellulose (L-HPC), sodium carboxymethyl starch (CMS-Na), and hydroxypropyl methylcellulose (HPMC) were used to ensure quick release of baicalin and berberine hydrochloride in the stomach. The dissolution of SHDT was evaluated by a method in 2005 Chinese Pharmacopoeia along with San-huang tablet (SHT), and the results demonstrated that the dissolution of baicalin and berberine hydrochloride more than double that of SHT and release of half of the rhubarb anthraquinones in colon.

Dissolution and pharmacokinetics of baicalin–polyvinylpyrrolidone coprecipitate

“…A dispersible tablet of San‐huang , composed of the three herbs baicalin, emodin and berberine hydrochloride, was prepared to improve their dissolution. The results of a dissolution test in 900 ml of 0.05% sodium dodecyl sulfate demonstrated that the dissolution of the baicalin was more than double that of the San‐huang tablet, but the bioavailability in vivo has not yet been reported . A baicalin–phospholipid complex was prepared to improve the bioabsorption of baicalin.…”

“…The results of a dissolution test in 900 ml of 0.05% sodium dodecyl sulfate demonstrated that the dissolution of the baicalin was more than double that of the San-huang tablet, but the bioavailability in vivo has not yet been reported. [9] A baicalin-phospholipid complex was prepared to improve the bioabsorption of baicalin. A pharmacokinetic study in eight rats after oral intake of baicalin and its phospholipid complex showed the mean areas under the concentration-time curves (AUC) were 4.9 and 14.6 mg h/ml, respectively.…”

The pharmacokinetic study on the mechanism of toxicity attenuation of rhubarb total free anthraquinone oral colon-specific drug delivery system

“…[3][4][5] showed no significant endogenous peaks interfering with any of all analytes or IS at the retention times under the described chromatographic conditions. Calibration curves of the five analytes showed good linearity with correlation coefficients greater than 0.9983 in relatively wide dynamic concentration ranges.…”

“…Briefly, 3 kg of rhubarb medicinal materials was extracted by 30% ethanol for three times using the described method to obtain rhubarb total free AQs [4]. 28 g of rhubarb total free AQs was sieved and mixed with MCC, PEG-6000 and fixed amount of aqueous solvent containing 2% (w/v) PEG-6000 and 2% (w/v) HPMC.…”

“…Moreover, the heterogeneity and complexity of rhubarb herbs, such as geographic origin, production batch and harvest season, may lead to the difference of constituent components and pharmacodynamic instability. In view of these problems, rhubarb total free AQs containing no less than 50% free AQs had been extracted and played purgative efficacy through OCDDS [4]. Anthraquinone aglycone colon-targeted capsule was stable in the stomach and small intestine, and began to degrade in the colon.…”