Background technology:
According to market survey, the 10%-15% that accounts for that suffers from sterile (pregnant) disease among the married couple at child-bearing age of China, wherein immune infertility (pregnant) reaches about 25%, the Western medicine of treatment immune infertility (pregnant) mainly is a glucocorticoid at present, but because of its side effect big, untoward reaction shortcoming more rambunctious is arranged, on using, be very limited.A lot of prescriptions are also arranged in the Chinese medicine, and method mostly is traditional decocting method, and extracts active ingredients is incomplete, and drug effect can not well be brought into play; As the patent No.: 99120678.9 treatment immune infertility and infertile Chinese medicine, its crude drug mainly comprises Herba Epimedii, Fructus Ligustri Lucidi, Herba Cistanches, Fructus Cnidii, Fructus Alpiniae Oxyphyllae, Radix Angelicae Sinensis, Fructus Lycii, Fructus Schisandrae Chinensis, Semen Persicae, Chinese medicines such as Radix Glycyrrhizae, but owing to failing further to work out preferred manufacturing procedure, only adopt mixing to decoct and take with its decoction, though certain curative effect is also arranged, but there are many extracts active ingredients incomplete after all, volatile ingredient almost completely loses, fat-soluble effective ingredient also is insoluble in the water, greatly reduce the expection therapeutic effect of this medicine, also can't adapt to the requirement of industrialized great production simultaneously.Even after adopting decocting in water, alcohol extraction, with adjuvant mixing reconcentration, drying and make tablet Chinese medicine, its volatile ingredient such as Fructus Alpiniae Oxyphyllae and Fructus Cnidii volatile oil and Radix Angelicae Sinensis volatile ingredient etc. be almost completely loss also, and supplementary product consumption is big, cause dose too big, even surpass 4 grams/time, effect does not still reach the expection therapeutic effect of this medicine.
Summary of the invention:
The objective of the invention is in order further to improve the curative effect of said medicine, reduce dose, guarantee that this medicine can fully extract the active ingredient in the various crude drug, a kind of a kind of preparation method for the treatment of the medicine of male infertility that can adapt to the requirement of industrialized great production is provided.
The active component of medicine of the present invention, mainly be that effective component extracting is formulated from Chinese medicine Herba Epimedii, Fructus Ligustri Lucidi, Herba Cistanches, Fructus Cnidii, Fructus Alpiniae Oxyphyllae, Radix Angelicae Sinensis, Fructus Lycii, Fructus Schisandrae Chinensis, Semen Persicae, Radix Glycyrrhizae, the preferred for preparation method of medicine activity component of the present invention is as follows:
A) proportioning takes by weighing each crude drug Herba Epimedii, Fructus Ligustri Lucidi, Herba Cistanches, Fructus Cnidii, Fructus Alpiniae Oxyphyllae, Radix Angelicae Sinensis, Fructus Lycii, Fructus Schisandrae Chinensis, Semen Persicae, Radix Glycyrrhizae by weight, and is standby;
B) distillation and extraction: the Fructus Alpiniae Oxyphyllae of described weight proportion is extracted volatile oil with vapor distillation; The Radix Angelicae Sinensis of described weight proportion is extracted volatile oil with carbon dioxide supercritical fluid extraction;
C) enclose: take by weighing an amount of cyclodextrin, after adding water and making saturated aqueous solution, add above-mentioned volatile oil respectively, stir, after enclose is finished, leave standstill, cold preservation filters, after the gained clathrate drying, be ground into fine powder, be Fructus Alpiniae Oxyphyllae oil clathrate and Radix Angelicae Sinensis oil clathrate, standby.
D) extraction concentrates: with Fructus Ligustri Lucidi, Herba Cistanches, the Fructus Schisandrae Chinensis of described weight proportion, and alcohol reflux, extracting solution is concentrated into relative density and is the clear paste I of 1.30-1.32 (80 ℃) after reclaiming ethanol, and is standby; The medicinal residues that the alcohol extraction medicinal residues of the full medicine of the Herba Epimedii of described weight proportion, Fructus Lycii, Semen Persicae, Radix Glycyrrhizae and Fructus Ligustri Lucidi, Herba Cistanches, Fructus Schisandrae Chinensis and Fructus Alpiniae Oxyphyllae, Radix Angelicae Sinensis are extracted behind the volatile oil mix, decoct with water, extracting solution filters, be concentrated into relative density and be the clear paste II of 1.32-1.35 (80 ℃), standby;
E) pulverize: the Fructus Cnidii of described weight proportion is ground into≤superfine powder of 20 μ m, standby;
F) with the superfine powder mix homogeneously of clear paste I, clear paste II and Fructus Cnidii, vacuum drying is pulverized; Add Fructus Alpiniae Oxyphyllae oil clathrate and Radix Angelicae Sinensis oil clathrate, mix evenly, just be prepared into the active component of medicine of the present invention.
The active component of medicine of the present invention can be mixed with adjuvants such as tablet adjuvant commonly used such as lubricant, disintegrating agent, adhesive, tabletting, bag film-coat, can be prepared into the medicine of tablet formula treatment male infertility.
The active component of medicine of the present invention also can mix with granule adjuvant commonly used such as dextrin and sweeting agent etc., granulates, dry, granulate and be distributed into and bag can be prepared into the medicine that the granule formula is treated male infertility.
The active component of medicine of the present invention can also be mixed with capsule adjuvant commonly used such as lubricant, disintegrating agent, adhesive etc., granulated, drying, granulate and incapsulate, and can be prepared into the medicine that capsule-type is treated male infertility.
The medicine that the present invention treats male infertility is a natural product, has no side effect, and has effects such as kidney invigorating and YANG supporting, nourishing YIN and benefiting blood, activating blood circulation to dissipate blood stasis, is mainly used in the treatment male infertility, the infertility that is suitable for antisperm antibody to cause especially.The medicine of the treatment male infertility that makes with preparation method provided by the invention can fully extract the fat-soluble and water miscible effective ingredient in the Chinese crude drug; And use cyclodextrin inclusion compound volatile oil, improved the utilization rate and the stability of volatile oil; The employing micropowder is used as medicine, and has both kept its effective ingredient, has reduced supplementary product consumption again.Select rational preparation method for use, make medicine of the present invention become can industrialized great production the effective oral Chinese patent medicine that has no side effect of treatment male infertility.
The specific embodiment:
The present invention is further described and illustrates as follows:
Comprise by weight percentage Chinese medicine Herba Epimedii 8-10%, Fructus Ligustri Lucidi 8-10%, Herba Cistanches 8-10%, Fructus Cnidii 8-10%, Fructus Alpiniae Oxyphyllae 10-15%, Radix Angelicae Sinensis 10-13%, Fructus Lycii 8-10%, Fructus Schisandrae Chinensis 8-10%, Semen Persicae 12-15%, Radix Glycyrrhizae 10-15% in the medicine of the present invention, the crude drug in the aforementioned proportion scope can take following step to extract its effective active composition.
A) proportioning takes by weighing each crude drug Herba Epimedii, Fructus Ligustri Lucidi, Herba Cistanches, Fructus Cnidii, Fructus Alpiniae Oxyphyllae, Radix Angelicae Sinensis, Fructus Lycii, Fructus Schisandrae Chinensis, Semen Persicae, Radix Glycyrrhizae by weight, and is standby;
B) distillation and extraction: the Fructus Alpiniae Oxyphyllae of described weight proportion is extracted volatile oil with vapor distillation; The Radix Angelicae Sinensis of described weight proportion is extracted volatile oil with carbon dioxide supercritical fluid extraction;
C) enclose: take by weighing an amount of cyclodextrin, after adding water and making saturated aqueous solution, add above-mentioned volatile oil respectively, stir, after enclose is finished, leave standstill, cold preservation filters, after the gained clathrate drying, be ground into fine powder, be Fructus Alpiniae Oxyphyllae oil clathrate and Radix Angelicae Sinensis oil clathrate, standby.
D) extraction concentrates: with Fructus Ligustri Lucidi, Herba Cistanches, the Fructus Schisandrae Chinensis of described weight proportion, and alcohol reflux, extracting solution is concentrated into relative density and is the clear paste I of 1.30-1.32 (80 ℃) after reclaiming ethanol, and is standby; The medicinal residues that the alcohol extraction medicinal residues of the full medicine of the Herba Epimedii of described weight proportion, Fructus Lycii, Semen Persicae, Radix Glycyrrhizae and Fructus Ligustri Lucidi, Herba Cistanches, Fructus Schisandrae Chinensis and Fructus Alpiniae Oxyphyllae, Radix Angelicae Sinensis are extracted behind the volatile oil mix, decoct with water, extracting solution filters, be concentrated into relative density and be the clear paste II of 1.32-1.35 (80 ℃), standby;
E) pulverize: the Fructus Cnidii of described weight proportion is ground into≤superfine powder of 20 μ m, standby;
F) with the superfine powder mix homogeneously of clear paste I, clear paste II and Fructus Cnidii, vacuum drying is pulverized; Add Fructus Alpiniae Oxyphyllae oil clathrate and Radix Angelicae Sinensis oil clathrate, mix evenly, just be prepared into the active component of medicine of the present invention.
The active component of medicine of the present invention can be mixed with adjuvants such as tablet adjuvant commonly used such as lubricant, disintegrating agent, adhesive, tabletting, bag film-coat, can be prepared into the medicine of tablet formula treatment male infertility.
The active component of medicine of the present invention also can mix with granule adjuvant commonly used such as dextrin and sweeting agent etc., granulates, dry, granulate and be distributed into and bag can be prepared into the medicine that the granule formula is treated male infertility.
The active component of medicine of the present invention can also be mixed with capsule adjuvant commonly used such as lubricant, disintegrating agent, adhesive etc., granulated, drying, granulate and incapsulate, and can be prepared into the medicine that capsule-type is treated male infertility.
Because Herba Epimedii contains compositions such as chromocor compound such as icariin, precious icariin, arrow icariin and polysaccharide; Fructus Lycii contains compositions such as lycium barbarum polysaccharide, carotene, aminoacid and trace element; Semen Persicae contains the cyanogen glycosides and comprises amygdaloside and compositions such as micro-Virginia prune glucoside, aminoacid, protein and saccharide; Radix Glycyrrhizae contains triterpenes and comprises glycyrrhizin and compositions such as enoxolone, chromocor compound and polysaccharide; The direct water of above-mentioned four Chinese medicine material is carried just can be complete with its extracts active ingredients.
Herba Cistanches contains liposoluble constituent such as 6-methylindole, phenylpropyl alcohol compounds ergosterol and boschnaloside A, B, C, H etc., water soluble ingredient such as N-N-dimethylglycine methyl ester, betanin, cupreol, saccharide etc.; Fructus Ligustri Lucidi contains compositions such as oleanolic acid, acetyloleanolic acid, Fructus Ligustri Lucidi acid, ursolic acid and phospholipid; Fructus Schisandrae Chinensis contains compositions such as schizandrin, deoxyschisandrin, schisandrin, second, organic acid and glycoside; Above-mentioned three flavor medical materials should first alcohol extraction extract its liposoluble constituent, and water extracts its water soluble ingredient again, like this could its extracts active ingredients is complete.
Fructus Alpiniae Oxyphyllae contains volatile oil more than 1.0%, also contains compositions such as flavonoid, aminoacid, saccharide, vitamin; Radix Angelicae Sinensis contains volatile ingredient such as n-butene phthalein lactone, ligustilide etc., also contains compositions such as saccharide, aminoacid, ferulic acid; Therefore above-mentioned two flavor medical materials should adopt steam distillation or carbon dioxide supercritical extraction method to extract volatile oil earlier, and medicinal residues water are again carried to guarantee its extracts active ingredients complete; Volatile oil can directly spray to be added, also can be with adding behind the cyclodextrin inclusion compound, to improve the utilization rate and the stability of volatile oil again; Simultaneously, also can adopt first alcohol extraction again the method carried of water extract its effective ingredient.
Fructus Cnidii contains volatile oil 1.3%, Coumarins comprises compositions such as osthole and bergapten etc., Palmic acid, cupreol, adopts the micropowder of≤20 μ m to be used as medicine, and has both kept its effective ingredient, has reduced supplementary product consumption again, reduces dose greatly; Simultaneously, also can adopt first alcohol extraction again the method carried of water extract its effective ingredient.
Medicine of the present invention can fully extract fat-soluble and water miscible effective ingredient and volatile oil in the above-mentioned raw materials medicine; And use cyclodextrin inclusion compound volatile oil, improved the utilization rate and the stability of volatile oil; The employing micropowder is used as medicine, and has both kept its effective ingredient, has reduced supplementary product consumption again.Compatibility of the present invention is exquisite, has effects such as kidney invigorating and YANG supporting, nourishing YIN and benefiting blood, activating blood circulation to dissipate blood stasis, adds rational preparation method, make medicine of the present invention become can industrialized great production product, be treatment male infertility obvious results oral formulations.Oral during use, each 1 gram, 3 times on the one.
Medicine of the present invention has been finished drug efficacy study on the experimental model basis of the immune infertility of antisperm antibody (AsAb) mediation.The research shows: this medicine can make in the refining, AsAb is cloudy in the serum changes, and sperm number, vigor sport speed are improved, and improves semen quality.Thereby the increase fertility rate reduces abortion ratio.Heavy dose of treatment does not have influence to fetal development.