| Peganum harmala L., a species of Zygophyllaceae, is used by Uygur and Mongolian as a traditional medicine from very early time. It has been collected by Uygur Drug Standard of Ministry of Public Health. A large quantity of P. harmala resources distribute all over Xinjiang. The seed of P. harmala is usually used as medicine, its pharmacological functions include expelling intestinal gas, strengthening lumbus, diuresis, promoting menstrual flow, removing the phlegm, and anthelminthic, and so on. Research on chemical components of its seed was reported early in 1841, the main components including harmine, harmaline, harmalol, harman, etc. amount to 3. 92~7. 0%. As major active component in seed, harmine has the highest content and stable property.The pharmacological functions of harmine are extensive. In the past time, research on this aspect often focused on central nervous system and inhibition of monoamine oxidase(MAO). Recently it is reported that harmine has functions in radiation protection and antihydatid disease. Since 1980, the total alkaloid preparation has been used to treat malignant tumor of digestive tract in clinic and laboratory in the Second Affiliated Hospital of Xinjiang Medical College, which had an effective result in twenty-one cases treatment and the efficacy was about 85.7%, the antineoplastic function of P. harmala has attracted wide attention of medical scientists both in domestic and abroad, and it has been one of the hot spot in research field. At present, there is no formal product of total alkaloid in market to be used by clinic physician, only had domestic preparation made by the Second Affiliated Hospital of Xinjiang Medical University. Now an industrialized extraction technique has been established and the extraction rate for harmine is about 1. 15% with purity of 99%. The goal of my studies is to prepare harmine hydrochloride capsule. It is confirmed by intelligence center of Military Medicine Academy of Science that the study has not been found in recent literatures home and abroad.The genotype, distribution and ecotope of P. harmala in Xinjiang are investigated in order to study the content of harmine and harmalinein different parts of whole plant and different locations. Through the above investigation, the difference of alkaloid content is analyzed. The results provide theoretical evidences for good variety selection, resources proper collection and preparation development of P. harmala. The HPLC method is employed to measure the content of harmine and harmaline. There is excellent linear correlation in range of 1.18~ 23. 68 and 2. 099~25. 19μg·mL-1 for harmine and harmaline respectively in this quantitative method. The content of total alkaloid of P. harmala in different parts of the plant and different locations is around 0~ 7.68%. The content of total alkaloid in different parts of P. harmala ordering is seed > root > nutshell > stem > leaf (p<0. 01). The results on seasonal variation of alkaloids in different parts of whole plant indicated that the highest content in seed is in July, and it suggested that the optimum time for harvesting is in July. The results of multiple regression analysis show that there is a negative correlation between the content of total alkaloid in seed and precipitation, and so does harmine; there is a negative correlation between the content of harmaline in seed and the longitude.in order to prepare harmine hydrochloride capsule successfully, pharmaceutical preformulation studies have been done in details. The major physicochemical properties of harmine hydrochloridc are studied: (l)The equilibrium solubility or apparent solubility of harmine hydrochloride in water and ethanol is 39. 17 ± 0. 21mg·mL-1 and 7. 68±0. 19mg·mL-1, respectively. (2) The intrinsic dissolution rate of harmine hydrochloride in water and 0.1mol·L-1 HCl determined by using dissolution test is 2. 92±0. 48 and 2. 73±0. 59 mg·cm-2·min-1(50r·min-1). (3) The iso-molarity ultraviolet spectrophotometric method is employed to determine the di... |
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