The prescription and the preparation method of Chinese catalpa Pueraria lobota lyophilized injectable powder
Technical field
The present invention relates to herbal pharmacology and field of traditional Chinese.Be specifically related to the prescription and the preparation method of the lyophilized injectable powder of Chinese medicine Radix Rehmanniae effective ingredient catalpol and kudzu vine root puerarin, clinically can be used for treating cerebral ischemic brain diseases.
Background technology
Cerebrovascular disease is one of three big causes of death of present serious harm human health.Dying from the cerebrovascular patient more than heart disease and cancer in China, occupy three big cause of the death first places, have sickness rate height, disability rate height, characteristics that mortality rate is high, is to threaten the mankind especially commonly encountered diseases, the frequently-occurring diseases of middle-aged and elderly people health.Wherein, ischemic cerebrovascular accounts for 60%~80% in the cerebrovascular disease.Therefore, how to have caused relevant scholar's extensive attention both at home and abroad by the medical treatment cerebral ischemia.
At present, Drug therapy is the Therapeutic Method of main employing clinically.The medicine of treatment cerebral ischemia both at home and abroad can be divided into five classes: antiplatelet drug, anticoagulant, thrombolytic medicine, vasodilation and cerebral protective agent.But the treatment target spot of these medicines is single, and toxic and side effects is bigger, is difficult to the effect that reaches satisfied.Chinese medicine and compound preparation mainly are to play a role by multi-level, the many target spot of methods such as benefiting QI for activating blood circulation, dredge the meridian passage, too many levels, and toxic and side effects is less relatively.Therefore it is remarkable to seek a kind of effect, and the little new drug of toxic and side effects becomes the focus of domestic and international research.
Catalpol (catalpol) is one of main effective ingredient of Chinese medicine Radix Rehmanniae Rehmannia glutinosa Libsch., it is the effective active composition of its " YIN nourishing " effect, be a kind of iridoid glycoside compounds of less stable, multiple pharmacologically active such as have diuresis, cathartic, blood sugar lowering, protect the liver.Up-to-date pharmacological research shows; catalpol has significant neural blood vessel defencive function to ischemic encephalopathy; can pass through blood brain barrier; improve the tolerance of cerebral tissue to hypoxic-ischemic; promote the growth of neuron axon and dendron; strengthen synapse reconstruct, the limbs neurological functional recovery of getting involved after the promotion cerebral ischemia improves significantly to the ischemic stroke tool.
Puerarin (kakkone) is a kind of pyrite glycosides that extracts from Chinese medicine Herba Gelsemii Elegantis Pueraria lobata (Willd) Ohwi root, belongs to isoflavonoid.Be usually used in treating cardiovascular and cerebrovascular disease, and kidney is had certain protective role.Many pharmacological researches show that puerarin has obvious protective effect to cerebral ischemic brain diseases, can pass through blood brain barrier, and expansion of cerebral vascular reduces blood viscosity and improves the cerebral tissue blood supply, and acute cerebrovascular ischemia sexually transmitted disease (STD) is become curative effect certainly.
Summary of the invention
The object of the invention is to provide a kind of middle pharmaceutically active ingredient compound medicinal formulation for the treatment of cerebral ischemia diseases.Said preparation can see through blood brain barrier; alleviate the degree of injury of cerebral ischemia; improve the tolerance of cerebral tissue hypoxic-ischemic; promote cerebral microvascular newborn and ripe, neuroprotective blood vessel unit promotes the growth of neuron axon and dendron; strengthen synapse reconstruct; improve neurobehavioral after the cerebral ischemia, improve function of nervous system's scoring, the extremity motor function that promotes to get involved after the cerebral ischemia recovers.The present invention be directed to the cerebral ischemia pathological change, adopt pharmaceutically active ingredient catalpol and puerarin composition compound recipe in the reliable pharmacological, make that lyophilized injectable powder achieves the above object.
The present invention relates to the medical usage that catalpol and puerarin make up the lyophilized injectable powder of making, promptly be used for the treatment of clinical cerebral ischemic brain diseases; Prescription of lyophilized injectable powder and preparation method thereof is made in catalpol and puerarin combination.
The present invention is used for the treatment of the Chinese catalpa Pueraria lobota injection prescription of freeze-drying powder of cerebral ischemic brain diseases and forms, and comprises catalpol, puerarin, mannitol, trehalose, propylene glycol
Each component is every part of catalpol 1~1000mg in the drug prescription, puerarin 1~3000mg, and mannitol 100~8000mg, trehalose 50~4000mg, 50% propylene glycol is an amount of.
The present invention realizes the object of the invention by implementing following technical scheme.
The specific embodiment
Chinese catalpa Pueraria lobota lyophilized injectable powder prescription:
Embodiment 1 (1000 preparation unit)
Catalpol 1g
Puerarin 1g
Mannitol 100g
Trehalose 50g
50% propylene glycol adds to 2000ml.
Embodiment 2 (1000 preparation unit)
Catalpol 10g
Puerarin 20g
Mannitol 100g
Trehalose 50g
50% propylene glycol adds to 2000ml.
Embodiment 3 (1000 preparation unit)
Catalpol 500g
Puerarin 300g
Mannitol 5000g
Trehalose 2500g
50% propylene glycol adds to 2000ml.
Embodiment 3 (1000 preparation unit)
Catalpol 1000g
Puerarin 3000g
Mannitol 8000g
Trehalose 4000g
50% propylene glycol adds to 2000ml.
Preparation method:
1. recipe quantity catalpol, puerarin and adjuvant decided in accurate title, adds an amount of 50% propylene glycol, fully stirs and make its dissolving, adds 50% propylene glycol again to full dose.
2. aseptic filtration: the microporous filter membrane fine straining of 0.22 μ m.
3. with the medicinal liquid packing, loading amount is every bottle of 3ml, and half tamponade is put into freeze dryer by the lyophilisation condition lyophilization.
4. lyophilization condition
This product eutectic point is-20 ℃;
Pre-freeze: quick freezing ,-45 ℃ of pre-freeze 3h;
Sublimation drying: evacuation with extremely-24 ℃ of plate temperature rises, is incubated 10h with 4h;
Parsing-desiccation: with 3h with plate temperature rise to 40 ℃, insulation 8h, lyophilizing finishes.
The total head plug, roll lid, packing, full inspection, warehouse-in.