| Gegenqinlian decoction consisted of four herbs : Radix Puerariae, Radix Scutellariae, Rhizoma Coptidis ,Radic Glyeyrrhiazae.This prescription had the function of relieving exterior syndrome and clearing out the interior heat .In the last few years, the medical scientists have proved that Gegenqinlian decoction had the pharmacological actions by experiment such as: refrigeration, antibacterium, antivirus, spasmolysis, inhibiting stomach and bowel movement, anti-lack of oxygen , antiarrhythmic, strengthening immunity. In the clinical treatment,it was used to treat diseases such as: bacillary dysentery, ileotyphus, acute and chronic gastroenteritis, infantile diarrhea, etc. The common preparation formulations include tablet ,small pellet and composition now.This experiment intent to develop the preparation of Gegenqinlian active fraction and made it to dispersible tablet .The Gegenqinlian Dispersible Tablet can disintegrate quickly, dieperse well and be easily absorbed.The contents of this thesis included the study on extraction and purification process for the active fraction of each herb and make the content of the active fraction above 50% ,the study on the preparation process and the study on the quality standard of product. The details are as follows:1.The study on extraction and purification process for the active fraction of each herb1.1 Extraction and Purification of isoflavonone from Radix Puerariae Puerarin was used to be the standard and UV spectrophotometric method is used to establish the quantitative methods of isoflavonone from Radix Puerariae. Radix Puerariae was extracted in turn with ethanol. The average content of this ethanol extractive was 37% and it was too low. According to the nature of isoflavonone from Radix Puerariae, Macroporous resin was used to purify the ethanol extractive and the average content of the isoflavonone from Radix Puerariae after purification was 65%.The best purification method was as follows: D101 macroporous resin(resin bed volume is 30ml), the extractive of Radix Puerariae was dissolved with water(the content is 9.0 mg/ml),Then, the volume of drug 60ml with the absorption-power 2 ml/min ,and volume of 70% ethanol as eluant 80ml the desorption-power 3ml/min. In result , total isoflavonone’s purity could reach 65% and the migrating rate of puerarin is 49.38%.1.2 Extraction and Purification of flavonoids of Radix ScutellariaeBaicalin was use to be the standard and UV spectrophotometric method was used to establish the quantitative methods of flavonoids from Radix Scutellariae. Radix Scutellariae is extracted by decoction and purified by acid precipitation. According to the orthogonal study ,the best purification method was as follows: the solution was concentrated to 1/3, was acidified with acetic acid to pH 1-2,80℃heat preservation for 2 hours, deposited for 12 hours. The average content of total flavonoids was85 % and the migrating rate of baicalin is 30.18%.1.3 Extraction and Purification of alkalaoids of Rhizoma CoptidisBerberine was use to be the standard and UV spectrophotometric method was used to establish the the quantitative methods of alkalaoids from Rhizoma Coptidis. Rhizoma Coptidis was extracted in turn with ethanol and purified by salting out. According to the orthogonal study ,the best extraction method was as follows: Rhizoma Coptidis was extracted twice in turn with eight times volume of 50% ethanol for two hours. The best purification method was as follows: the solution is concentrated to 1/6, was salted out with NaCL of 5% content and deposited for 24 hours. The average content of total alkalaoids was 70% and the migrating rate of berberine is 38.79%.1.4 Extraction and Purification of glycyrrhizin of Radic GlyeyrrhiazaeGlycyrrhizic acid was use to be the standard and Spectrometry method was used to establish the quantitative methods of glycyrrhizin. According to the orthogonal study,the best extraction method was as follows: Radic Glyeyrrhiazae was extracted in turn with eight times 0.5% ammonia solution by three times for 1.5 hours. The solution was concentrated, was acidified with acetic acid to pH 1, deposited for 30 min and centrifugated for 20 min. The best purification method was as follows: D101 macroporous resin (resin bed volume is 30ml), the extractive of Radic Glyeyrrhiazae was dissolved with water(the content is 0.3 mg/ml).Then, the volume of drug 40ml with the absorption-power 1 ml/min,and volume of 50% ethanol as eluant 140ml the desorption-power 2ml/min.In result, total glycyrrhizin’s purity could reach 50% and the migrating rate of glycyrrhizic acid is 68.3%.2.Studies on the technology of the preparationIn order to improve the solubility of Puerarin in the preparation, the extractive of Radix Puerariae was made solid dispersion.But the dosage of the solid dispersion was too big, so it was not appropriate. According to the orthogonal study, the best preparation was as follows: durgs, the loading agent of MCC(equal to drug), the disintegration agent of C-PVP(20% of the dosage).All of these were mixed, made granulars by 50% ethanol, the particle diameter is between 40 and 60 screen mesh, and tabled.The dispersible tablet can dieperse in 3 rain and the dispersity was satisfactory. In comparison with small pellet,the puerarin‘s dissolution of the dispersible tablet was better. 3 Studies on the quality control of the preparation3.1 Qualitative identificationThe qualitative identification of the herbs in the preparation was performed by TLC and the results were satisfactory.3.2 Quantitative analysis of the active fractionThe quantitative methods of the active fractions were established by UV and the precision, reproducibility and stability were satisfactory. The contents of isolapvone, flavonoids and alkaloids in the preparation were 27.8mg, 62.22mg and 27.8mg per tablet.3.3 Quantitative analysis of the active constituentsThe four active constituents were determined by HPLC and the contents of puerarin, baicalin, berberine and glycyrrhizic acid were 12.54mg, 30.39mg, 17.18mg and 4.45mg per tablet. |
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