Preparation Process And Quality Control Standard Of Extract "Frankincense Total Triterpenic Acids"

Rheumatism is the leading disease of causing serious damage of human health. Rheumatism shares two characteristics:they cause chronic (though often intermittent) pain, and they are difficult to treat. The signs and symptoms include:joint pain, difficulty sitting or bending over, joint stiffness, bone pain, muscle weakness and pain etc.Access to a limited number of chemotherapeutic agents which are including NSAIDS, steroids and cytotoxic drug, their deleterious side effects may cause drug poisoning. A vast number of traditional herbal remedies because of their minor side effects were recommended for "rheumatism". Thus, there is a growing focus on the traditional Chinese medicine in the treatment of rheumatism. A large number of clinical applications and related literature suggest that Chinese medicine frankincense had some beneficial effects on Rheumatism because it can open up the meridians and relieve pain and importantly, it is no side effect. To retain the characteristics of frankincense traditional medication and play the advantage of its clinical application, we explore the quality control and process evaluation of frankincense.Frankincense is used in traditional medicine in China for rheumatism.The boswellic acids which have unique mechanism of anti-inflammatory caused no adverse effect and used for drug for rheumatism. The boswellic acids exhibit anti-inflammatory behaviour by inhibiting leukotriene synthesiss, inhibiting the activity of the enzyme5-lipoxygenase through a non-redox reaction and inhibiting the activity of topoisomerase. The objective of this study include the preparation process of frankincense extractive, the isolation of chemical constituents of frankincense extractive, the pharmaceutical and toxic test, establishing characteristic chromatogram, the quality control standard of extractive, the stability study of frankincense extractive.1. The preparation process of frankincense extractive:Based on a large amount of literatures, we selected ethanol as the extraction solvents. The extract percentage, the total organic acids contents and TLC was regarded as the target of the experiments. The extract preparation by different methods was regarded as the target to evaluation the extraction methods. Thus on the basis of the two factors and three levels, the extraction process was optimized; on the basis of the three factors test, the puration process was optimized. Thus the preparation process of frankincense extractive was optimized.2. The isolation of chemical constituents of frankincense extractive. The extractive subjected to silica gel CC with petroleum ether-EtOAc to yield10fractions. The main compounds were isolated by recrystallization and HPLC. Their structures were elucidated by spectroscopic methods, including1H and13C NMR and UV.3. The pharmaceutical and toxic test. With reference of "Drug registration and management approach", the pharmaceutical and toxic test were conducted. It is to explore the anti-inflammatory and analgesic effect of Frankincense extraction in some kind of rats.It is to explore the effect of frankincense extraction on blood pressure, breathing, electrocardiogram in mongrel dogs. The results showed there is no obvious difference.It is to explore the toxic effect of Frankincense extraction in rats. The results showed there is no toxic reaction.It is to explore the long-term toxic effect of frankincense extraction in rats and mongrel dogs. It is showed that there is no obvious difference in hematology, blood biochemistry detection, organ coefficients and histopathologic examination between the dosage group and the control group.4. Establishing characteristic chromatogram. The fingerprint of extractive was based on technical requirements of fingerprints of Traditional Chinese medicine injection and compared with similarity evaluation software published by the Committee of China Codex. The fingerprint was established by HPLC-ELSD methods.12common characteristic peaks were identified as the characteristic fingerprints. The method by selecting extaction solvent, extraction methods, eluting solvent and chromatographic column can be used for the quality control and process evaluation of extractive. The established HPLC fingerprints have precision, reproducibility, an experimental basis for futher quality control.5. Establishing the quality control standard of extractive. To esablish the quality control standard of extractive on the basis of the Chinese pharmacopoeia (2010edition, parts2of the appendix), the total organic acids content, the11-hydroxy-β-acetoxyl-boswellic acids content, solublity, heavy metal were considered.6. The stability study of frankincense extractive. With reference of the technical requirements of new drug research, the influencing factors were investigated and the stability study were proceed for determining the product packaging and the validity period.Conclusion We established the preparation process of frankincense extractive. The extractive exhibited anti-inflammatory behaviour and had minor side effect and used for drug for rheumatism.Fingerprint was established for controlling the herb source and extraction process to control quality. The methods of determining the contents of main active compounds can establish the quality control standard of extractive.In conclusion, the modern methods including the preparation of frankincense extractive, the establishing characteristic chromatogram, the quality control of main active compounds can control the quality of Chinese Traditional Medicine and declare new drug as effective part. It is of high scientific value and clinical application prospects.