Study On Antialcoholism And Hepatoprotective Compound Dispersible Tablets

Compound antialcoholism and hepatoprotective dispersible tablet consisted of three herbs. The main effective components are the isoflavone compounds, to achieve efficient and available, We wi ll extract and purify the active ingredients, because of its low solubility and dissolution, poor bioa vailability, we use inclusion technique to make inclusion compound to increase its solubility, dissol ution and the drug rapid absorption and improve the bioavailability of the drug. Dispersible tablets of traditional Chinese medicine application to insoluble drug, it is convenient to take, rapidly disi ntegration, collapse of fine particles is beneficial to drug dissolution and accelerate drug absorption and improve the bioavailability of drugs. In addition, the Chinese medicine is prepared into dispe rsible tablet, for more convenient drug, can swallow, including and flushing after taking and its pr oduction process is simple and the cost is low, is suitable for industrial production. Therefore, this article will focus on the authentic herbs, extracted from the main ingredient, the purification proc ess, quality control, inclusion technology, health formulations, quality of study based, product effica cy and other aspects were studied and developed a fast and efficient, safe and controllable quality,taking convenience dispersible tablets, which provide a scientific basis on the comprehensive deve lopment and utilization of Radix Puerariae.1. The establishment of Puerarin and Rutin in vitro analysis methodSystem, the establishment of the comprehensive and perfect quality control method is an impo rtant mean to guarantee the quality of preparation and measures. Respectively establish puerarin an d rutin HPLC?UV analysis method, and methodology, the results show that the established puerari n and rutin in the puerarin and rutin cyclodextrin inclusion compound dispersible tablets HPLC U V analysis method system suitability, specificity, precision, recovery were complex requirements, for prescription design, stability test provides a sensitive, accurate and reliable analytical method.2. Study on extraction and purification of active ingredientsActive ingredients puerarin hepatoprotective effect of isoflavones, which is the main function o f puerarin. Puerarin can protect the liver, which play a major pharmacological effect of Radix Puer ariae. The current research on the optimization of extraction technology of puerarin mainly focusedon individual process conditions, and on the different extraction methods were few reported. As i s reported, for comparisons between traditional extraction process by orthogonal design, and the tra ditional process optimization, extracting rate of puerarin was 39.40 mg·g-1. Ethanol reflux extractio n, ultrasonic extraction, supercritical CO2 fluid extraction and flash extraction technology were con ducted to extract puerarin in this experiment. With the puerarin consociation sibeline content as an index. The optimum technology for the best method was also studied. Results revealed that the e xtraction efficiency of flash extraction technology was the highest. The optimum extraction technol ogy was as following: extracted 2 min with 30 times the amount of 58 % ethanol at 90 V. Under these conditions, extracting rate of puerarin was 50.72 mg·g-1, this optimized process is stable an d reproducible with short extracting time, and this method for the determination of high sensitivity,accurate result, provide a scientific basis for the development and utilization of Pueraria Lobata.This study extracted the flavonoids of hovenia dulcis thunb by ultrasonic extraction, on the ba sis of single factor and orthogonal design, results show: ethanol concentration: 70 % ethanol soluti on, ratio of liquid to material 14 ml/g, ultrasonic extraction power: 160 W, ultrasonic extraction te mperature: 70 ?, ultrasound extraction time: 1 h, and the resultant total flavonoids yield was 1.17mg·g-1.The AB-8 macroporous resin was used to purify the pueraria total flavonoid, and established t he best purification process. ethanol concentration:50 % ethanol solution, dosage: 500 ml, flow rate:6 ml/min, the purity of puerarin reached 60 %3. Study on ?-cyclodextrin inclusionIn order to prepare the pueraria isoflavones-?-cyclodextrin inclusion, Magnetic stiring method, grinding method, ultrasonic method, stirring paddle method, milk homogenization method were con ducted to prepared pueraria isoflavones-?-cyclodextrin inclusion in this experiment. With the inclusi on rate and dissolution as indexs. The optimum technology for the best method was also studied. Results revealed that the stirring paddle method was the best. The optimum preparation technology was as following: mole ratio was 1:1.19, inclusion temperature was 50 ?, inclusion time was 30 min, under these conditions, inclusion rate: 93.68 %, dissolution: 95.33 %. Each index of the opti mized pueraria isoflavones-?-cyclodextrin inclusion was well fitted with the predicted value. The optimized process is reliable, stable.We determined the pueraria isoflavones-?-cyclodextrin inclusion by infrared spectroscopy, differ ential scanning calorimetry. Results show that puerarin has indeed been involved into the cavity str ucture of ?-cyclodextrin. After drug form inclusion compound, could change the crystal lattice arra ngement, therefore the lord, the guest molecules, the shape of inclusion compound, the physical an d chemical properties were different, increased the solubility in water obviously. and provided theor etical basis for developing new puerarin oral dosage forms.We determined the stability of pueraria isoflavones-?-cyclodextrin inclusion, influence factors te st show that the pueraria isoflavones-?-cyclodextrin inclusion will keep stable under low temperatur e, low humidity, under the environment of high temperature, high humidity, sample character, conte nt will be changed. so it should be kept in the condition of low temperature, low humidity.In this study, we used Hovenia dulcis Thunb isoflavones as raw material medicine, mole ratio was 1:1, inclusion temperature was 60 ?, inclusion time was 30 min, prepared Hovenia dulcis T hunb isoflavones-?-cyclodextrin inclusion.4. Study on the properties of powderThrough the investigation of the fluidity, compressibility and moisture absorption of the powde r, the results indicate that the repose angle of the pueraria isoflavones, the pueraria isoflavones-?-c yclodextrin inclusion, the Hovenia acerba isoflavones extraction, the Hovenia acerba isoflavones-?-c yclodextrin inclusion and the Astragalus polysaccharide were greater than 40 degrees, its liquidity i s not good, the repose angle of the antialcoholism and hepatoprotective compound dispersible table ts granules were less than 40 degrees, and its liquidity has improved.The compression degree of the pueraria isoflavones, the pueraria isoflavones-?-cyclodextrin incl usion, the Hovenia acerba isoflavones extraction, the Hovenia acerba isoflavones-?-cyclodextrin incl usion and the Astragalus polysaccharide were greater than 20 %, and the compression degree of th e antialcoholism and hepatoprotective compound dispersible tablets granules were less than 20 %, i ndicating that the package of pharmaceutical raw materials and compound compression of liquidity is not good, not easy to flow out automatically, while the particle compression is small, the flow of good.In order to determine the tabletting environment, We determined the critical relative humidity of the podwer, the hygroscopicity were evaluated. Results show that When the relative humidity is56.5 %, the moisture absorption rate increases obviously. Therefore, the preparation process of tab lets should be strictly controlled environment humidity.5. In vitro activity test of antialcoholism and hepatoprotectiveTo study the effect on antialcoholism and hepatoprotective, The experiment of influence of dif ferent dose of Flos puerariae isoflavones and Puerarin isoflavones on alcohol dehydrogenase activit y and superoxide dismutase activity were determined through methods of Vallee & Hoch and Thre e phenol self oxidation method. The results show that influence of two substances on ADH and S OD is promote. But activation rate of puerarin isoflavones on ADH and SOD were significantly lo wer than Flos puerariae isoflavones. And with the dosage increased, the effect was significantly in creased. Therefore, this study took 1.2 times of the Puerarin isoflavones of ADH, SOD activation rate of 61.23 %, 35.84 %, close to the Flos puerariae isoflavone of ADH, SOD activation rate of 63.35 %, 36.10 %.6. Preparation of antialcoholism and hepatoprotective compound dispersible tabletsOn the basis of literature data and preliminary experiment, based on the investigation to the i nfluence factors and the prescription adjustment, by Box-Behnken-response surface methodology, th en chose the amounts of disintegrant, disintegrating agent compatibility proportion, the categories o f adhesive as the factors, obtained the optimal formulation with the disintegrating time as index.(PVPP+CMS-Na): 10.06 %, PVPP:CMS-Na=2:1, ethanol concentration: 87.69 %. The dispersible t ablets disintegrated in 67 s, and the dispersible uniform was excellent, and the cumulative dissoluti on quantity was as high as 96.74 % in 10 min.7. The quality standard and stability test of antialcoholism and hepatoprotective compoun d dispersible tabletsIn antialcoholism and hepatoprotective compound dispersible tablets quality inspection of the st udy, the traits, TLC, weight difference, hardness, disintegration time, uniform dispersion, dissolution and content determination of inspection, indicators are in line with the Pharmacopoeia of the peo ple's Republic of China(edition 2015) regulations.In vitro dissolution contrast test results show that: Compound antialcoholism and hepatoprotecti ve dispersion tablets 10 min dissolution rate was above 90 %, and the effects of compound puerar in isoflavones dispersible tablets is only about 10 %. The drug molecules with low solubility and dissolution rate could be used to increase their solubility, increase the dissolution rate, and improve the bioavailability of the drug.Antialcoholism and hepatoprotective compound dispersible tablets and compound Pueraria flow er dispersion tablets enzyme activity test results showed that the ADH activation rate for compoun d pueraria flower dispersible tablets(77.34 %) > alcoholic sobering and hepatoprotective compound dispersible tablets(70.40 %) > hangover Ling(64.27 %); the SOD activation rate for compound Pueraria flowers scattered tablets(46.08 %) > alcoholic sobering and hepatoprotective compound di spersible tablets(45.28 %) > hangover Ling(42.57 %). Show that puerarin of ADH, SOD activati on rate and spend similar, show that puerarin might well instead of Flos puerariae and the alcohol ic sobering and hepatoprotective compound dispersible tablets effect is superior to the one in the s ale of spiritual hangover.Influencing factors test results show that in high temperature, high humidity conditions antialc oholism and hepatoprotective compound dispersible tablets of appearance, properties were varied, b ut the hardness, content, dissolve out degree changed little, and illumination conditions indexes had no significant difference, considering should be under dry conditions at the same temperature purc hase save.The significance of this study lies in alcoholic sobering and hepatoprotective field provides a quick release, efficient, practical strong alcoholic sobering and hepatoprotective health care products.The research results show that the alcoholic sobering and hepatoprotective compound dispersible t ablets have the following advantages: reasonable preparation process, controllable quality and good stability, the activation of ADH and SOD, alcoholic sobering and hepatoprotective.