Preparation Of Ibuprofen-β-CyD Inclusion Complex Cream And Study Its Pharmacodynamics

Background:Ibuprofen,as a kind of non-steroidal anti-inflammatory drugs(NSAIDs), possess better antipyretic action, analgesia, antiphagocytic and antirheumatic action.It has been used clinically for the treatment of rheumatoid arthritis,osteoarthritis,ankylosing spondylitis, soft tissue rheumatism.It can also be used for mild and moderate pain relief,such as the pain caused bu dental operation,obstetric operation,obstetric operation,obstetric operation,orthopedic operation,soft tissue injury.We always use ibuprofen to relive the fever caused by Cold and Influenza.It can relieve inflammation and pain caused bu gout.Since its advent,it proves to have more effect than aspirin,paracetamol,phenylbutazone in anti-inflammatory and analgesia.So far,it has not yet been used to treat hemorrhoids.Based on the effect of analgesia and anti-inflammatory.Based on the effect of the insoluble in water,low dissolution rate,stimulation on gastrointestinal mucosa,we have made it into the inclusion complex. Aim: To prepare Ibuprofen-β-Cy D inclusion complex cream and observe the therapeutic effects on perianal ulcer of mouse and its excitability. Method:(1)Then we did the orthogonal experiment to decide the optimal method.(2)Ibuprofen-β-Cy D inclusion complex was prepared by saturated water solution method. Drug loading,the inclusion rate,the stability,the recovery rate and the solubility were determined by ultraviolet spectrophotometry.(3)We have refered to ?the standard of Chinese hospital preparation ? to prepare the ibuprofen inclusion compound cream.At the same time we have controled the quality of cream.we have tested its release,stability in cold,heat and centrifugal,the concentration of drug,rate of recovery and in vitro percutaneous permeability.(4)36 Kunming mice were randomly divided into three groups,namely blank group,medium group and cream group.The mice in blank group were not given medicine,mice in medium group were given medium and mice in cream group were geven ibuprofen-β-Cy D inclusion complex cream. After ten days,We did the pathological examination of anal mucosa.The aim was to observe the irritation is the cream of the anal mucosa.(5)30 SD rats were randomly divided into three groups,namely control group,experimental group and positive control group.We used acetic acid in rats’ anal mucosa.The rate in blank group were not given medicine,rate in experimental group were given ibuprofen-β-Cy D inclusion complex cream and rate in posive control group were given Ma Yinglong musk hemorrhoids ointment.The aim is to observe of ibuprofen-β-Cy D inclusion complex cream in hemorrhoids. Result:(1)Based on the result of the orthogonal experiment,We concluded the optimal conditions for conditions for preparing ibuprofen-β-Cy D inclusion complex cream: the molar ratio of ibuprofen and β-cyclodextrin is 1:1,the optimum temperature is 40℃,the stirring is 3 hours.(2)We have prepared the ibuprofen-β-Cy D inclusion complex successfully.The concentration of drug was(8.25±0.26)%,n=6.The inclusion rate was(50.27±1.8)%,n=6.Drugs in room temperature for 8 hours had good stability.The recovery rates of inclusion complex solution were(99.62±0.62)%,(97.40±1.08)%,(97.98±3.22)%,n=5。The solubility of ibuprofen-β-Cy D inclusion complex was 451.58ug/ml and the solubility of ibuprofen was 58.8ug/ml.Ibuprofen solubility was increased 7.68 times.(3)The prepared ibuprofen inclusion compound cream was white,delicate and uniform cream.The concentration of drug is(0.99±0.026)%,n=6.The recovery rates of cream were(98.24±2.51)%,(97.35±2.45)%,(97.96±3.14)%,n=5。It had a good stability in cold,heat and centrifugal. The percutaneous permeation of the ibuprofen inclusion compound cream was 0.023cm/h. The percutaneous permeation of the ibuprofen cream was 0.015cm/h.The enhancement ratio was 1.52.(4)After the pathological examination of the anal mucosa,the anal mucosa of the mece in blank group,medium group,cream group were normal.(5)From the seventh day of the experiment,compared with the control group,the ecperimental group and the positive group were significantly different.On the tenth day of the experiment,the rates in experimental group and the positive group were cured. Conclusion:(1)The in vitro percutaneous absorption properties of the ibuprofen-β-Cy D inclusion complex cream were improved obviously.(2)Ibuprofen-β-Cy D inclusion complex cream and its medium did not stimulate the anal mucosa.(3)Ibuprofen-β-Cy D inclusion complex cream have cured the hemorrhoids.The effect was similar with Ma yinglong hemorrhoids ointment.