ABSTRACT
OBJECTIVE@#Traditional Chinese medicine (TCM) has been widely used throughout China to prevent and cure diseases for thousands of years, and now it is a part of the integrative medicine field that is available in Western societies. To ensure the safety and quality of the herbal medicines that are a major part of the TCM tradition, they must be held to modern pharmaceutical standards. Erzhi pill (EZP) is a Chinese Pharmacopeia-listed herbal preparation that is used in the long-term clinical management of post-menopausal symptoms, osteoporosis and menstrual disorders. Until now, whether the drug release mechanism of EZP is in line with its intended TCM usage has not been studied.@*METHODS@#The release of specnuezhenide from three EZPs (self-made, Leiyunshang and Renhe) in simulated gastric fluid (SGF), acetate buffer (pH 4.5 buffer) and simulated intestinal fluid (SIF) was investigated in a dissolution test. The water uptake capacity and erosion extent of the three EZPs were investigated using swelling and erosion studies. The drug release mechanism was further assessed through statistical model fitting, using DDSolver software.@*RESULTS@#The release of specnuezhenide from all three EZPs in SGF was less than 50% within a 4 h period. However, over 70% of the specnuezhenide was released from each EZP in both pH 4.5 buffer and SIF in the same time. Analysis of the swelling and erosion behaviors and the drug release mechanism of the three EZPs confirmed that the release rate from EZP followed a sustained release profile, which was an interactive combination of swelling and erosion.@*CONCLUSION@#This study showed that the release pattern from the pills was in line with the intended TCM use of EZP. TCM had not only theoretically considered sustained release from the pills, but also formulated them to achieve this release pattern. When establishing quality control standards for pills, the theoretical TCM usage and the actual release patterns need to be considered.
ABSTRACT
There have been numerous efforts to formulate insulin into an oral dosage form. The major problems involved with the oral administration of insulin are acidic and enzymatic decomposition by the gastric medium, and poor absorption in the small intestine due to its macromolecular structure. This study attempted to test the enhancing ability of two absorption enhancers, sodium glycocholate [Na-GC] and sodium salicylate [Na-Sal], in different parts of rat's gastrointestinal tract. The amount of insulin in each formulation was 0.6 iu/kg body weight. The concentration of enhancers [Na-Sal or Na-GC] in each formulation was 10 micro g/ml. Formulations made of insulin and enhancers were prepared and injected directly to stomach, duodenum, jejunum and ileum of anesthetized rats through an abdominal incision. Blood samples were taken at 45 and 60 min intervals. The glucose concentration was determined by the o-toluidine method. Injections [IP] of insulin and normal saline were positive and negative controls, respectively. The blood glucose concentrations showed a significant decrease [p<0.05] due to the injection of insulin into duodenum, while the effect noted in jejunum was insignificant [p>0.05]. Also, there was no anti-hyperglycemic effect accompanied by formulations administered into the stomach and ileum. It could be concluded that insulin, if formulated in a protected form to prevent acidic and enzymatic decomposition, in combination with such enhancers may overcome hyperglycemia due to insulin deficiency