Study On YinLing Troche

Background:With the higt speed development of Xiushan honeysuckle industrial, the planting area was reached 300 thousands mu, it had brought economic benefits to local farmers, but it was crude drug in whole for the end product, a serious shortage of self-digestion, the market value-added and risk-resisting ability is extremely low. How to further expand the Lonicera macranthoides economic value, to make full use of medicinal resources and increase the income of farmer become urgent to solve the problem. The study based on the honeysuckle with good clear heat and purging fire for removing toxin of traditional efficacy, and strong anti-bacterial, anti-virus, anti-inflammatory and other pharmacological effects, and the clear pharynx troche to be developed as honeysuckle as the main raw material. This study is support strongly by the special fund of the National Science and Technology Support Program topics (2006BAC01A16) and the "Eleventh Five-Year Plan" program of Chongqing Municipality (It was funded by Xiushan government).Objective:In accordance with the publish《health food management approach》by the State Food and Drug Administration released.YinLing troche is a compound preparation of traditional Chinese medicine (TCM), which is developed by our team. We determine its anagraph and preparation technology, establish quality criteria, study the pharmacodynamics, and preliminary investigaton of its safety. Methods:1. The prepare technology. According to the prescription drμg effective components of physicochemical properties about total flavonoids and caffeotannic acid, the extraction process is select the water precipitated by alcohol extraction, the extraction process was optimized using the extract yield, extraction rate of total flavonoids and chlorogenic acid as the index by the orthogonal experiment. According to the extracts properties, we investigating the adjuvant and dosage with the single factor experiment, using the wet granμlation and tabletting to prepare; and chosing the best prescription and technology by integrating survey the of various subjective and objective index as the taste, the disintegration time.2. Quality standard. (1)Identification:we used the HPLC and TLC on Xiushan honeysuckle for qualitative identification. (2) Check:①Dissolution, according to the second method "paddle method" in second part appendix XC of Chinese Pharmacopoeia 2010 edition to determined:②Moisture, used the rapid moisture analyzer to measured;③Other:we ordered inspection item including the disintegration time, weight variation and friability which according to the preparations General Clauses ID of appendix I in part one of China pharmacopoeia 2010 edition. (3) Assaying:we used HPLC and UV to quantitative determination of chlorogenic acid and total flavonoids content in YinLing troche, and to determine the limits of its content.3. Stability:With the 40±2℃for high temperature experiments.92.5% for the high humidity experiments and with bright light in 4500±500Lx for highlight experiments, and use 40℃.75% humidity under 6 months for accelerated test. With 25℃.60% humidity under 36 months for long-term experiment to examine the stability of the YinLing troche.4. Preliminary pharmacodynamic study. Xylene was used to induce mice ear swelling and the carrageenan-induced rat paw swelling experiment was used to validate the anti-inflammatory effect of YinLing troche. 5. Safety evaluation. To inspect YinLing troche safety, we used maximum dose in the acute toxicity test to calculate the LD50 for mice by intragastric administration, verify the mucosal toxicity by golden hamster mucous membrane irritation test. Forthermore. the long term toxicity test was used to inspect adverse reaction of rats.Results:1. The prepare technology. The extraction process was determined:take the prescriptions Xiushan honeysuckle, crushed into coarse powder, plus A times water and boiled D times at temperature of C℃, each time for B hour. Affiliate filtrate, concentrate to the relative density for 1.1, adjusted to contain alcohol amounted to 75% ethanol. standing for 16h. recovery of ethanol. have to concentrate. Extracts concentrate decompression and vacuum drying, crushing into powder. Take extract powder, adding mannitol, lactose and some correctant, misce bene, wet granulation, pressing.2. Quality standard:(1) Identification:HPLC and TLC identification Xiushan honeysuckle. (2)Check:①dissolution, Chlorogenic acid’s dissolution rate>95%;②Moisture:moisture content<5%;③Other:consistent with rμles of the preparations General Clauses ID of appendix I in part one of China pharmacopoeia 2010 edition. (3) Assaying:The consistent of chlorogenic acid and total flavonoids in YinLing troche were above 15 mg and 50 mg respectively per-piece.3. Stability:By influential factor test, accelerated testing and long-term trial investigation, get the result of YinLing troche in production, packaging, storage should be avoid highlight for longtime, it should be stored place with ventilated, cool and dry. Its validity is tentatively scheduled for 2 years.4. Preliminary pharmacodynamic experimental results showed that YinLing troche had good anti-inflammatory effects, significantly inhibited auricle swelling in mice and foot swelling in rats, and the inhibition rate of auricle in mice were 48.85%, 54.48%,73.25% respectively for different dose groups; and the lowest was 5.3%. and the maximum was 44.2% in rats.5. Safety:YinLing troche has no obvious symptoms on mouse acute toxicity test. and it was unable to calculate the LD50, and the maximum dose is 20 g·kg-1. which is equivalent to clinical dose 400 times. The YinLing troches’ mucous membrane irritation experiment showed that there was no manifest golden hamster was irritated on golden hamster’s oral mucosa. And the YinLing troche has no effect on their general behavior, physiological, biochemical, organ coefficient and organ pathology-examination of rats by successive administration for 30 days. It showed the YinLing troche is non-toxic products and safety.Conclusions:This study was using water extract and alcohol sediment to extract the main active ingredient of the Xiushan honeysuckle, we acquired the YinLing troche was put the powdered extract with lactose, and other adjuvants, mixing, granulating, tabletting. packing. The prescription and preparation process is reasonable, it is stability, quality control by this way, and it has a strong anti-inflammatory effects. The YinLing troche is avoid bright light for a long time irradiation, and the validity period is tentatively scheduled for 2 years.