满山红滴丸临床前药学和主要药效学

【Abstract】wWw.shuoshilunwen.com Manshanhong, derived from the dried lees of Rhododendron dauricum L, is commonly used for relieving cough, dispelling the phlegm and suppressing asthma. It is widely applied in the treatments of acute and chronic bronchitis.Folium Rhododendri Daurici Dropping Pill is a simple recipe preparation, developed by the effective fraction of the total flonoids from the dried lees of Rhododendron dauricum L and based on the traditional experience and modern science researches. The new drug has wide application and vast market prospects.Orthogonal tests were used to choose the matrixes proportion, proportion between drug and matrix, temperature of drug, height between dripper and refrigerant, and so on. The results were graded synthetically with the coefficient of weight variation, shape, hardness and resolving time of the drop pill. The optimized process for the preparation of Folium Rhododendri Daurici Dropping Pill was as follows: PEG4000:PEG6000:drug (2:1:1), melted at 90℃, dropped with the dripper 10cm above the refrigerant, at the speed of 30 drips per minute. The internal and external diameter sizes were 4mm and 5mm, respectively. The temperature of refrigerant was 10℃. With the best preparation process, the drop pill was well-formed with good uniformity. The hardness and resolving time met the needs. The technology was stable, which laid the foundation for the future production.A HPLC method was established to determine the content of hyperoside in Folium Rhododendri Daurici. The quality control of Folium Rhododendri Daurici Dropping Pills was made, with an UV method used to determine the content of the total flonoids along with a HPLC method established to determine the content of hyperoside. The methods were reliable, accurate and could be used for the quality control of the drop pill.The factors that influence the stability of the purified extraction were investigated. The purified extraction was steady under 60℃high temperature and 4500 lx±500 lx strong light condition. It was oppositely steady under 75% high humidity though unsteady under 92.5% high humidity condition. The acceleration stability and long-term stability experiments were also carried on the drop pill. The results of current three months shew the drop pill was steady under 37-40℃high temperature, 75% high humidity and normal temperature with 60% humidities conditions. The characteristics didn’t appear obvious variety. The contents of the total flonoids and the hyperoside, the disintegration time all met the requirements. The drop pill has a good stability.Animal models, such as strong aqua induced cough in mice, citric acid induced cough in guinea pigs, phenolsulfonphthalein excretion from trachea in mice, were employed to evaluate the antitussive and eliminating phlegm effects. Antiasthmatic activity in guinea pigs and in vitro guinea pig tracheal ooth muscle experiment, were employed to evaluate the antiasehmatic effects of Folium Rhododendri Daurici Dropping Pill; acute and chronic animal models, such as xylenc-induced ear oedma in mice and cotton ball induced granuloma in rats, were employed to evaluate the antiinglammatory effects. The effect on anoxia resistance in mice under normal pressure and bacteriostatic action in vitro were investigated. LD50 was determined via both oral administration and intrenous injection to evaluate the acute toxicity. The Folium Rhododendri Daurici Dropping Pill had low acute toxicity and significant major pharmacodynamic action. The new drug meets the need of the modernization.In this article the pre-clinical pharmaceutical studies, pharmacological and acute toxicitytest of the new drug were accomplished, which laid foundation to the further development of the fifth kind new traditional Chinese medicine.