| Objective: According to the research ideas of new traditional Chinese medicine to develop oroxylum indicum spray(OIS),make sugar free oroxylum indicum spray(SFOIS)and sugared oroxylum indicum spray(SOIS),and conduct preclinical pharmaceutical research.The active ingredients and mechanism of action of oroxylum indicum in the treatment of pharyngitis were studied,the extraction,concentration and drying process of oroxylum indicum were optimized,the antibacterial activity of oroxylum indicum extract was studied,suitable auxiliary materials were selected to make oroxylum indicum spray,the quality standard of oroxylum indicum spray was formulated,and the influencing factor test was carried out.Methods: 1.Material basic research: The active ingredients and mechanism of action of oroxylum indicum in the treatment of pharyngitis were screened by network pharmacology,and the active ingredients were verified by molecular docking technology.2.Research on preparation process: optimize the extraction process of oroxylum indicum by design space method;A single factor was used to investigate and optimize the concentration and drying process of wood butterflies and the molding process of oroxylum indicum spray.3.Research on antibacterial activity: oroxylum indicum extract was prepared according to the optimal extraction process of oroxylum indicum,and the antibacterial activity of oroxylum indicum extract was studied by 96-well plate method and agar plate method.4.Research on quality standards:According to the relevant indicators under the four parts of the 2020 edition of the Chinese Pharmacopoeia,formulate the quality standards for oroxylum indicum spray.5.Preliminary stability study: according to the relevant indicators under the four "Guidelines for Stability Testing of APIs and Preparations" in the 2020 edition of the Chinese Pharmacopoeia,the influencing factor test is carried out.Results: 1.Material basic research: The main signaling pathway of oroxylum indicum in the treatment of pharyngitis was obtained by network pharmacology through tumor necrosis factor signaling factor,the key compounds were quercetin,baicalein and aloe emodin,and the binding energy of the molecular docking model was <-5.0 k J/mo L,and the binding conformation was stable.2.Research on preparation process: the best extraction process for wood butterflies obtained by design space method is 30 times the amount of ethanol,30 min of soaking time,50% of ethanol concentration,30 min of extraction time,and 2 times of extraction;The best concentration process to obtain wood butterflies by single-factor investigation method is to concentration time at 80 °C for no more than 6 h,and the best drying process is to dry under reduced pressure at 80 °C.3.Molding process:oroxylum indicum spray is a powder spray sprayed out of the mouth and throat through the solid powder of the No.7 sieve(120 mesh),divided into sugar-free type and sugar-containing type,and the best ratio of pharmaceutical powder and auxiliary materials is pharmaceutical powder:microcrystalline cellulose: chitosan = 1: 1: 1: 1 and powder: microcrystalline cellulose: chitosan: mannitol = 1: 1: 1: 0.1.4.Antibacterial activity study: the MIC value of oroxylum indicum extract against Staphylococcus aureus,Escherichia coli and Bacillus subtilis was 0.3～0.7 mg/m L and MBC value of10～40 mg/m L by 96-well plate method and agar plate method.5.Quality standard research: the pass rate of SFOIS powder and SOIS powder through the No.7 sieve is > 95%.The alcohol-soluble extract content of sugar free oroxylum indicum spray shall not be less than 28.0%,and the water content shall not exceed 2.7%;Each 1 g of SFOIS powder contains baicalein-7-Odiglucoside,baicalin quercetin,baicalein and wogonin,which shall not be less than 1.7%,1.4%,1.1%,0.5% and 0.5%,respectively.The alcohol-soluble extract content of sugared oroxylum indicum spray shall not be less than26.0%,and the water content shall not exceed 2.1%;Each 1 g of SOIS powder contains baicalein-7-O-diglucoside,baicalin,quercetin,baicalein and wogonin,which shall not be less than 1.6%,1.4%,1.1%,0.4% and 0.6%,respectively.SFOIS powder and SOIS powder absorb moisture for 24 h under the condition of air humidity of 43%,and the moisture absorption rate is 5%;Under the condition of air humidity of 60%,moisture absorption is 24 h,and the moisture absorption rate is 7%;Under the condition of air humidity of71%,moisture absorption is 24 h,and the moisture absorption rate is 9%;Under the condition of air humidity of 75%,moisture absorption is 24 h,and the moisture absorption rate is 10%.6.Preliminary stability study: SFOIS powder and SOIS powder have good stability to light and high temperature;It has strong hygroscopicity and needs to be prepared and stored under ambient conditions < 70% relative humidity of the air.Conclusion: In this study,five index components of oroxylum indicum in the treatment of pharyngitis were baicalein-7-O-diglucoside,baicalin,quercetin,baicalein and wogonin as parameters of the preparation process.Network pharmacology and molecular docking technology showed that the two active ingredients of oroxylum indicum in the treatment of pharyngitis were quercetin and baicalein,which were verified by preparation process and antibacterial activity research.The design space method and the single-factor investigation method showed that the optimal extraction,concentration and drying process of oroxylum indicum could effectively increase the content of index components in oroxylum indicum.The 96-well plate method showed that oroxylum indicum extract had strong antibacterial activity against Staphylococcus aureus,Escherichia coli and Bacillus subtilis.Oroxylum indicum spray directly acts on the lesion site of the throat in the form of spray,improving the flexibility of medication and bioavailability,which can provide ideas for the development of new medicinal value and new preparations and dosage forms of oroxylum indicum. |
