Pharmacological Research On Improved Chinese Herbal Anti-inflammatory Patch

Traditional Chinese Medicine External Patch 1004 is an external rubber ointment composed of various traditional Chinese medicines such as Aconitum carmichaelii,Kaempferia galanga L.,Angelica sinensis(Oliv.)Diels,etc.It has the functions of dispelling rheumatism,anti-inflammatory and pain relief.Since the preparation still uses the original standard,it is difficult to adapt to the increasingly strict quality control requirements of modern Chinese medicine preparations.In addition,traditional rubber paste formulations have problems such as small drug loading,easy to cause allergies,and difficult release of active ingredients.In order to solve the above problems and improve the controllability of product quality,the matrix of this preparation was improved,and the pharmacological properties,pharmacodynamics and pharmacokinetics of the comparative preparations before and after the improvement were studied.Firstly,using orthogonal experiment and liquid-phase detection method,a method for preparation of test sample and determination of EMC content of active ingredient was preliminarily established.The two preparations were cut into pieces before Soxhlet extraction.The optimal extraction conditions of the rubber paste were 95% ethanol concentration,45 liquid-material ratio,and 3 h extraction time.The modified cataplasm has an ethanol concentration of 95%,a liquid-to-solid ratio of 30,and an extraction time of 3 h.The extract liquid was detected by rotary evaporation,concentration and membrane treatment,and the extraction of both EMC content reached the maximum.Then,a comparative study on the pharmacological properties of the modified cataplasm and traditional rubber paste was carried out.First,a test method for the release characteristics of the active ingredients of the preparation was initially established.The dissolution conditions were optimized,and the dissolution effects of the active ingredients before and after the improvement were compared.The results showed that the release percentage of the former was 9.613%,and the latter was 11.247%,indicating that the cataplasm matrix made up for the rubber matrix.The shortcomings of strong sealing and poor drug release.Second,the conditions such as the rotational speed of the patch in vitro and the receiving fluid were optimized.The rat abdominal skin was selected as the permeable membrane,and the experimental results showed that the cumulative permeation amount in vitro within 24 h of the former was 170.363 μg,and the latter could reach 196.44 μg;Pharmacokinetic law,established the effective ingredient EMC plasma pretreatment and detection methods.The experimental results showed that the AUC of the rubber paste was 4.331 ± 0.62 mg ·h/L,while the AUC of the modified poultice was doubled to 8.902 ± 0.89 mg·h/L The relevant kinetic parameters proved that the average residence time and the area under the curve of the cataplasm were longer after administration.At the same time,UPLC-MS analysis of plasma and tissue has been carried out to prove that EMC has penetrated into the local administration tissue and entered the blood circulation.Finally,the anti-inflammatory pharmacodynamics before and after the modification of the study formulations were compared.That is to say,carrageenan was used to induce inflammation in SD rats,and the swelling inhibition of toes after administration of the two preparations was compared,and analyzed by ELISA,WB,Q-PCR and other molecular biological methods.The experimental results showed that,the anti-inflammatory effect of the improved preparation is better,that is,the inhibition of swelling of toes by the latter is more obvious after administration.