The Studies Of Nux Vomica Cataplasm

Traditional Chinese medicine nux vomica has the effect of acesodyne and detumescence,pharmacological studies have shown that that it has the pharmacological effects of analgesia,anti arrhythmia,anti tumor and other widely,especially in the analgesic and anti tumor activity is most noticeable.Strychnine alkaloids have definite and extensive analgesic effects,such as gout,arthritis,traumatic injury,cancer and other diseases caused by pain.In recent years,the study of its application in the treatment of cancer pain has attracted more and more researchers' interests,but due to the significant toxicity of nux vomica has severely restricted the application of the medicinal herbs in clinical practice.The traditional way of oral administration is prone to poisoning,and there have been many cases of poisoning in clinical practice.Transdermal drug delivery system is deeply welcomed by patients because of its convenience,compliance,safety and high efficiency,and so on.The subject of application of transdermal delivery of new technologies,will be developed into a transdermal nux vomica cataplasm,for the treatment of cancer pain.It can play a good biological activity of Strychnos,but also to show the transdermal preparations characteristics of long time and stable blood drug concentration,Which can improve the safety of Strychnos,and reduce the risk of poisoning.We will mainly focus on the extraction process of Strychnos alkaloids,the screening and preparation of the cataplasm matrix,the transdermal permeation test in vitro and the screening of the enhancer,the quality standard,safety and stability of the cataplasm.The full text of the study mainly includes the following aspects:1.With the extraction rate of alkaloids as the evaluation index,four factors with the greatest influence screened by single factor experiment were selected to carry out the orthogonal experiment design and the best extraction process was optimized.The optimum extraction process was as follows: the extraction solvent was 75% ethanol,the ratio of material to liquid was 1:10,extraction time was 2 h,pH value was 4.2.The adhesion,repeatedly pasted,comfort,paste residues and appearance traits as evaluation index,the matrix composition of PVA-g-PVP,kaolin,glycerol and glutaraldehyde was determined.by single factor test.Then add the ingredients of Chinese medicine Strychnos alkaloids,according to L9(34)orthogonal test table design experiment,the best matrix prescription for the cataplasm as follows: PVA-g-PVP 6 g,kaolin 1.5 g,glycerol 2.5 mL,glutaraldehyde 0.2 m L.3.The experiment established a test method for in vitro percutaneous penetration,the nux vomica cataplasm permeation properties were studied.The effects of four kinds of azone,DMF,propylene glycol and menthol on the penetration of brucine and strychnine were investigated.The results showed that azone,DMF,propylene glycol and menthol had different degrees of the permeation enhancing effect on brucine and strychnine in cataplasm.The penetration performance of azone and menthol were increased first and then decreased with the increase of the concentration,and the effect of DMF and propylene glycol in the given range(?5%)was enhanced with the increase of the concentration.Comparison of the 24 hour transmittance of the four penetration enhancers,the 5% DMF had the best effect on the penetration of the cataplasm.4.According to "Chinese Pharmacopoeia" of 2015 edition IV of the requirements of cataplasm,the quality standards of the nux vomica cataplasm were developed.The ointment content of nux vomica cataplasm is 18.75 g/100 cm2,and the difference of formability and weight is in accordance with the requirements.The initial sticky test showed that the maximum stickiness of the cataplasm was No.22 balls(14.1 g).TLC was used to identify the brucine and strychnine in the cataplasm.The average content of brucine and strychnine in the cataplacum was 0.579 mg/g,0.895 mg/g determined by RP-HPLC.According to the developed quality standard,the three-month accelerated stability test was carried out for the three batches of nux vomica cataplasm.The test results show that the nux-vomica cataplasm in 40±2 ? and relative humidity RH of 75%±5% for 3 months,the viscosity decreased,and the other indexes did not change obviously.5.New Zealand white rabbits and guinea pigs were used to establish skin irritation test and skin sensitization test to evaluate the safety of cataplasm.In the skin irritation test,the New Zealand white rabbits with single-dose and multiple-dose of nux vomica cataplasm,there were no skin irritation reactions such as erythema,edema and so on in the skin parts.In the skin allergy test,the use of nux vomica cataplasm or excipients did not find the local skin of guinea pigs showed erythema,edema and other allergic reactions.