| Objective:To prepare Geng Nian An（GNA）granules,a Chinese patent medicine for the treatment of perimenopausal syndrome,and to evaluate its quality and pharmacodynamics.Methods:1.With the content of index components（rehmannitin D and salidroside）and extract yield as evaluation indexes,the extraction time,extraction times and added water as factors,the optimal extraction process was determined by single factor and orthogonal test,and the optimal process was verified.The optimum temperature of decompression concentration was investigated by single factor test with the content of index component and extract yield as evaluation indexes.The optimum drying method and drying condition were investigated by single factor test with the yield of extractum powder,index component content and moisture as the index.Taking particle state,molding rate,Angle of repose,melting rate and moisture absorption rate as investigation indexes,the optimal excipients were investigated by single factor test,and the optimal proportion of excipients,ethanol dosage and ethanol concentration were investigated by orthogonal test,and the optimal forming process was verified.2.The main medicinal materials Rehmannia Rehmannii and Ligustrum liquidum were qualitatively identified by thin layer chromatography;The contents of rehmannioside D and salidroside were determined,and the methods were investigated.The molding rate,water content,solubility,bulk density and critical relative humidity were investigated.3.The effects of GNA Granules on perimenopausal syndrome were studied from five aspects,including weight change,uterine state,serum sex hormone level,depressive mood behavior and bone microstructure,in perimenopausal castrated model rats.Results:The preparation process of GNA granules was as follows:After weighing the prescription amount of medicinal materials,adding 10 times the amount of water,the medicinal materials soaked for 1.0h,adding 1.16 times the amount of water for the first time,decocting and boiling for 3 times,1h each time,combining the decocting liquid and filtering,decompression at 70℃,concentration to the relative density of 1.12,dry extract dried at 70℃,crushing and sifting to extract powder,adding the medication-auxiliary ratio of 1:Mixed excipients of 1（mixed excipients of mannitol:dextrin=2:1）and 85%ethanol equivalent to 25%of the mass of soft wood were used to prepare soft wood,extruded for granulating,and whole grain after vacuum drying at 60℃.The validation test of the molding process showed that the particles were in good condition,and the molding rate,melting rate,moisture absorption rate and Angle of repose were 92.93%,91.56%,38.39%and 7.69°,respectively.A thin layer identification method was established for ripe Rehmannium and Ligustrum Ligustrum.Based on the content determination results,the content limits of Rehmannium D and salidroside per gram in GNA granules were determined to be no less than 2.17mg and no less than 1.56mg respectively.The molding rate,moisture and solubility of GNA granules were all in line with the provisions of the 2020 edition of Chinese Pharmacopoeia.The bulk density was 0.515g·m L-1and the critical relative humidity was 77.5%.GNA granules can effectively relieve the excessive weight gain of rats caused by estrogen deficiency after castration and increase the serum estradiol（E2）content.Reduce the content of follicle-stimulating hormone（FSH）and luteinizing hormone（LH）,improve the uterine coefficient,improve the uterine lesion state,restore the exploration and activity ability and relieve the anhedonia behavior of rats,and improve the osteoporosis caused by estrogen loss.Conclusion:The preparation process of GNA granules screened in this subject has good stability,and the finished granules conform to the relevant provisions of the 2020edition of Chinese Pharmacopoeia.The quality evaluation method is scientific and reasonable with high reproducibility.Preliminary pharmacodynamic study found that GNA granules can promote the secretion of E2 by gonads,inhibit the secretion of FSH and LH,protect the endometrium,improve the depressed mood of rats,and have pharmacological effects on increasing bone mass related parameters such as bone density and bone volume fraction.In summary,GNA granules can relieve the symptoms of weight gain,anxiety,depression,palpitation,insomnia and osteoporosis in women during perimenopause.At the same time,this granule has no sucrose and is suitable for women with high blood sugar during perimenopause. |
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