Application of pinocembrin to preparation of anti-cerebral hemorrhage drugs
A drug and hemorrhagic technology, which is applied in the application field of pinoselin in the preparation of anti-intracerebral hemorrhage drugs, can solve problems such as no report on the application of pinoselin, achieve significant vascular protection effect, reduce vascular damage, reduce The effect of HT risk
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Embodiment 1
[0030]Example 1. Pinocerin injection was prepared according to the following method. (1) pulverize the pinoscelin raw material, cross 100 mesh sieves, and set aside; (2) take by weighing the hydroxypropyl-beta-cyclodextrin of prescription quantity, add 700ml water for injection and stir to dissolve; (3) add 0.5% ( g / ml) gac for injection, kept boiling slightly for 30 minutes, and decarbonized by filtration; (4) took by weighing the pinocerine of prescription quantity, and added in the above-mentioned hydroxypropyl-beta-cyclodextrin aqueous solution at room temperature; (5) ) Slowly add 10% aqueous sodium hydroxide solution dropwise under stirring, adjust and keep the pH value of the solution between 8.4~8.5, stir for about 4 hours, until the pinocerine is completely dissolved; (6) add water for injection to 1000ml, Stir well; (7) add 0.05% (g / ml) activated carbon for injection, stir at room temperature for 30 minutes, and filter; (8) use 0.45 μm and 0.22 μm microporous membran...
Embodiment 2
[0031] Example 2. Pinocerin reduces the exudation of Evan's blue dye in brain tissue during tPA thrombolysis in a rat intravascular thrombosis model of acute stroke.
[0032] Experimental materials: Sprague Dawley (SD) rats were purchased from Weitong Lihua (Beijing Weitong Lihua Experimental Animal Technology Co., Ltd.). tPA was purchased from Boehringer-Ingelheim, Germany. Pinocerin injection (10 mg) was provided by Wu Song's research group at the Institute of Materia Medica, Chinese Academy of Medical Sciences. When injecting, add 1 mL of normal saline for injection (Shijiazhuang Pharmaceutical No. 4 Factory), and use it at a dose of 10 mg / kg. The injections were protected from light and stored in a -20°C refrigerator.
[0033] SD rats with a body weight ranging from 250 to 300 g were anesthetized by intraperitoneal injection of chloral hydrate (350 mg / kg). The hair around the bregma was shaved, and the skin on the top of the head was cut to expose the bregma. Select 2 ...
Embodiment 3
[0040] Example 3. Pinocerin reduces hemoglobin exudation in brain tissue during tPA thrombolysis in a rat intravascular thrombosis model of acute stroke.
[0041] Animal modeling and administration methods are the same as in Example 2. The homogenate of the perfused brain tissue was taken and added with a hemoglobin stabilizer, the absorbance was detected at 575 nm, and the hemoglobin content in the brain tissue was calculated by substituting it into the standard curve. see results figure 2 , after injection of tPA, the blood content in rat brain tissue homogenate showed a rising trend. After the injection of pinocerin, the content of hemoglobin in the homogenate of bilateral brain tissue decreased significantly regardless of whether thrombolytic therapy was performed. Tip pinocerin can significantly reduce the bleeding caused by tPA.
[0042] Table 2. The effect of pinocerin (10mg / kg) on the amount of hemoglobin exudation in the brain tissue after delaying 6h of tPA thr...
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