Preparation And Quality Study Of Penthorum Chinense Pursh Sustained-release Dropping Pills

Penthorum chinense Pursh(PcP),a plant belonging to the family of Saxifragaceae,has the functions of clearing away fever and toxic materials,promoting diuresis,reducing swelling,eliminating jaundice,eliminating dampness,promoting blood circulation and removing blood stasis,and is often used to treat liver diseases.In the market,the preparations using PcP as raw materials include Gansu granules,Gansu capsules,PcP orally disintegrating tablets and so on,which are often used to treat liver diseases.In 2020,PcP had been listed as a new food raw material for food by National Health Commission of the People’s Republic of China.PcP contains many active ingredients:gallic acid(GA)has anti-inflammatory and liver-protective effects;quercetin has anti-oxidation effects.Dropping pills have as the advantages of high bioavailability and simple preparation process.Therefore,in this paper,using PcP extractive as the raw material,the preparation of PcP dropping pills(PcPDP)and PcP sustained-release dropping pills(PcPSRDP)was studied as follows.Optimization of extraction process of PcP:The standard curve was established with GA as the index by UV-vis.The linear regression equation was A=0.0417 C+0.0297,R~2=0.9998,which showed that the concentration of GA had a good linear relationship with absorbance in the range of 4.56-31.92μg/m L.And the method was specific,precise,stable and accurate.The ultrasonic extraction method was used to extract PcP.Taking the yield of PcP and the content of GA as the inspection indicators,the optimal process conditions for the extraction of PcP by single factor were as follows:60%ethanol as the extraction solvent,solid-liquid ratio was 1:15,ultrasonic extraction at 55℃for 60 minutes and the yield of PcP crude drug was 59.63±0.70 mg/g and the GA content was 25.39±0.50%.The results showed that the weight and GA content of the drug were stable when it was stored at high temperature(60±2℃),light intensity(5000 Lux)for 30 days and high humidity(25±2℃,RH 75±5%)for 15 days.Preparation of PcPDP:Taking roundness,weight difference and dissolution time as indexes,single factor test and orthogonal design were used to optimize the preparation conditions of PcPDP.The optimal preparation conditions were as follows:the ratio of PEG-4000 and PEG-6000 was 1:1,the ratio of raw material medicine and matrix was1:5,the temperature of drug solution was 80℃,the dropping distance was 7 cm and the speed was 40 d/min,the coolant was dimethicone(100 m Pa·s)and the cooling temperature was 5℃.Preparation of PcPSRDP:Taking roundness,weight difference and dissolution in vitro as indexes,single factor test and Box-Behnken design were used to optimize the preparation conditions of PcPSRDP.The optimal preparation conditions were as follows:the content of HPMC in matrix was 24%;the content of raw material medicine was17%;the temperature of drug solution was 86℃;the dropping distance was 7 cm and the speed was 40 d/min;the coolant was dimethicone(100 m Pa·s)and the cooling temperature was 10℃.Study on the quality standard of PcPDP and PcPSRDP:According to Chinese Pharmacopoeia 2020 edition,the quality standard of the preparation was studied on the sensory requirements,weight difference,moisture content,dissolution time or dissolution in vitro and the content of GA.In PcPDP,the average weight was 28.8±0.4mg,the difference coefficient was 0.96±0.05%,the moisture content was 0.16±0.06%,the dissolution time was 5.72±0.25 minutes,and the GA content was 0.99±0.03 mg/pill.In PcPSRDP,the average weight was 25.0±0.6 mg,the difference coefficient was 2.29±0.15%,and the moisture content was 0.22±0.10%,the dissolution in vitro was more than 90%for 12 h,RSD of the content uniformity was1.72%,and the content of GA was 0.76±0.02 mg/pill.The two preparations of PcPDP and PcPSRDP had good stability after being placed for 6 months under long-term(25±2℃,RH 60±5%)and accelerated(40±2℃,RH 75±5%)conditions.We prepared the PcPDP and PcPSRDP after refining Penthorum chinense Pursh.And the quality standards were established for the two dropping pill.Then we investigated the stability of the dropping pill by accelerated test and long-term test for six months.All of these provided the reliable basis for developing drug.