The application treated osteoporotic plant extracts and its prepare medicine or health products
Technical field
The invention belongs to plant extracts field, it is related to a kind of whorlleaf loosestrife herb with root extract treating osteoporosis.
Background technology
Osteoporosis is broadly divided into primary and Secondary cases, and primary, in addition to idiopathic, is divided into I type and II type, I type is again
Referred to as PMO, is high conversion hysteria, and main cause lacks for female hormone;II type is also called senile sclerotin and dredges
Pine, is low conversion hysteria, aging due to the age.Caused by many factors, its basic pathology mechanism is bone generation to osteoporosis
During thanking, defect in bone information and osteoplastic coupling, lead to the alcium and phosphor metabolization in human body uneven, make bone density gradually
The clinical symptoms reducing and causing.
The cause of disease:1. idiopathic(Primary):Juvenile form, adult, the menopause, senile.2. Secondary cases:(1)Endocrine
Property hypercortisolism, hyperthyroidism, primary hyperparathyroidism, acromegalia, gonad function
Lowly, diabetes etc..(2)Gestation, lactation.(3)In trophism protein shortage, vitamin C, D shortage, low calcium diet, alcohol
Poison etc..(4)Heredity osteogenesis imperfecta chromosome abnormality.(5)Hepatopathy.(6)Kidney trouble chronic nephritis haemodialysis.(7)Medicine
Corticosteroid, anti-insane pain medicine, antineoplastic(As methotrexate (MTX)), heparin etc..(8)Give up and see length with property generalized bone is loose
Phase bed, paraplegia, space flight etc.;Locality see fracture after, amyotrophia etc. after wound.(9)Gastrointestinal malabsorption, stomach are cut
Remove.(10)Rheumatoid arthritis.(11)Tumour Huppert's disease metastatic carcinoma, monocytic leukemia etc..(12)Other
The minimizing of reason smoking sclerotin, transience or migrating property osteoporosis.
Check:(One)Laboratory examination:1. blood calcium, phosphorus and alkaline phosphatase be in primary osteoporosis, serum calcium,
Phosphorus and alkaline phosphatase levels are typically normal, and after fracture, several months alkaline phosphatase levels can increase.2. blood parathyroid gland
Hormone should check secondary osteoporosis except parathyroid function.Primary osteoporosis person's blood parathyroid hormone water
Flat can normally or rising.3. the label patients with osteoporosis part serum studentization index that bone updates can be changed with reactive bone
(Including bon e formation and bone information)State, in the high transition status of bone(Such as I type osteoporosis)Under, these indexs can rise
High it can also be used to the early reaction of monitoring treatment.4. urina sanguinis calcium/creatinine ratio normal ratio is 0.13 ± 0.01, urinary calcium discharge capacity
Cross at most ratio to increase, point out have bone absorption rate may increase.(Two)Auxiliary examination:Bone imaging examination and bone density:(1)Right
In the X-ray film having local symptom patient should absorb diseased region.(2)Bone mineral density Bone mineral density is the best prediction of fracture
Index.
Treatment:1. drug therapy:Clinically have for preventing and treating osteoporotic medicine:Calcium preparation, include escape happy, triumphant
Think vertical, Caltrate D, happy power, calcium gluconate oral solution with effect, imperial prosperous calcium+D oral liquid, strength obtain calcium, huge energy calcium and ultra micro calcium;Suppression
Bone information medicine, heir as pregnant in dehydrogenation, Premarin Tablet and Livial etc.;Bisphosphonates, such as Fosamax, bone unicorn, Bang get Lin and Ji
Power oxazepan;Osteogenic treatment medicine, such as Tridin;Promote the vitamin medicaments of mineralising, such as method energy(L alpha-hydroxy vitamin D 3)、
Rocalcitrol(Calcitriol), to sprout lattice prosperous(Alfacalcidol), vertical celebrating(Alfacalcidol piece).2. surgical intervention:Only because of sclerotin
After osteoporosis are fractured, just need surgical intervention, its object is to treatment fracture, recover normal function as early as possible.
Whorlleaf loosestrife herb with root, is Primulaceae Lysimachia plant wheel blade Lysimachia christinae(Lysimachia klattiana Hance)'s
Herb is dried.Wheel blade Lysimachia christinae be perennial herb, complete stool close by rust the long pubescence of brown many cells.Stem uprightly lacks branch, high by 15
~45 centimetres.3~4 pieces of blade is verticillate, and in stem top majority leaf consor, the lower portion of the stem leaf opposite sometimes, blade is oval or oval
Shape lanceolar, long 2~5 centimetres, wide 7~12 millimeters, the anxious point of tip is to tapering, the narrow wedge shape of base portion, full edge, several stockless.Hua Misheng
In stem top;Calyx 5 drastic crack, sliver lanceolar, tip is tapering, is about 1 centimetre, by hair and have unconspicuous black lines, the back of the body
Portion's middle arteries are raised;Corolla yellow, funnel-form, 5 drastic cracks, sliver ligule is oval, and slightly longer compared with calyx, tip is tapering, blunt circle or micro-
Recessed, there are black lines;5 pieces of stamen, length is only the 1/2 of corolla, is born in the base portion of corolla pipe, filigree base portion symphysis cyclization
Shape;The nearly spheroidal of ovary, Room 1, ovule is most.Capsule is spherical, about 4 millimeters of diameter;Seed is most, smooth.5~June of florescence, really
6~July of phase.It is born in hillside border, under the shrubbery of small stream side or in the thick grass of roadside.Be distributed in Shandong, Jiangsu, Anhui, Zhejiang, Jiangxi,
The provinces and regions such as Fujian, Hubei, Hunan, Guizhou, Sichuan, Henan.Pick and process:5~June harvests the herb with root, cleans, dries.
Medicinal Materials Characters:Herb length 15~40 centimetre is dried, generally distorts.Complete stool is become rusty the elongated pubescence of brown, most with stem.Stem list
Raw, cylindrical, celadon, there are vertical stripe, section hollow.The many shrinkages of blade, broken, 3 to multi-disc is verticillate, after complete leaf flattening is
Ellipse or lanceolar, full edge, several stockless.Spend in the many intensive top armpits in stem;Sepal narrow lanceolar, by pubescence and black line
Bar, corolla yellow, funnel-form, there are black lines.Capsule is subsphaeroidal, and about 4 millimeters of diameter, containing most seeds.Gas is light, the micro- acid of taste.
Done with body, the tender thin, Ye Duo of celadon, cauline leaf, the no miscellaneous person of mud are preferred.Nature and flavor and function:Micro- sour, puckery, cool.Hemostasis, hypotensive, solution
Snake venom.For hypotensive, hemoptysis of pulmonary tuberculosis;Venomous snake bite, traumatism and bleeding are controlled in external application.15~30 grams of usual amounts, are decocted in water for oral dose, or fresh
Grass is smash juice and is taken orally, and external application fresh grass mashes deposited affected part.
The invention provides a kind of whorlleaf loosestrife herb with root extract treating osteoporosis, research has shown that this extract has substantially
Suppression Bone m etabolism, increase the stable effect of bone.
Content of the invention
It is an object of the invention to provide a kind of whorlleaf loosestrife herb with root extract.
It is a further object of the present invention to provide the preparation method of this extract.
The present invention also provides this extract in preparation treatment osteoporosis and rheumatism joint anti-inflammatory drugs
Application.
The purpose of the present invention is achieved in the following ways:
A kind of whorlleaf loosestrife herb with root extract treating osteoporosis, this whorlleaf loosestrife herb with root extract is adopted and is prepared with the following method:
(1)The whorlleaf loosestrife herb with root being dried is pulverized, plus 15~25 times amount 70%~90% ethanol, carry in 60 DEG C~70 DEG C water-bath backflows
Take 2 times~4 times, each 70min~80min, merge extract, reclaim ethanol, obtain whorlleaf loosestrife herb with root total extract medicinal extract;
(2)The whorlleaf loosestrife herb with root obtaining total extract medicinal extract is carried out column chromatography for separation, resin with D-140 type macroporous absorbent resin
Post blade diameter length ratio is 1:7~9, loading volume 6BV~8BV, wash 4BV~6BV removal of impurities, with ethyl acetate:Acetone=10:1 wash-out
Agent 7BV~9BV wash-out, flow velocity is 2BV/h~4BV/h, collects eluent, eluent concentrates, is dried, obtains final product.
Described whorlleaf loosestrife herb with root extract is preferably adopted and is prepared with the following method:
(1)The whorlleaf loosestrife herb with root being dried is pulverized, plus 15 times amount 90% ethanol, in 60 DEG C of water-bath refluxing extraction 4 times, every time
70min, merges extract, reclaims ethanol, obtains whorlleaf loosestrife herb with root total extract medicinal extract;
(2)The whorlleaf loosestrife herb with root obtaining total extract medicinal extract is carried out column chromatography for separation, resin with D-140 type macroporous absorbent resin
Post blade diameter length ratio is 1:7, loading volume 8BV, wash 4BV removal of impurities, with ethyl acetate:Acetone=10:1 eluant, eluent 9BV wash-out, stream
Speed is 2BV/h, collects eluent, and eluent concentrates, and is dried, obtains final product.
Described whorlleaf loosestrife herb with root extract can also preferably employ following method preparation:
(1)The whorlleaf loosestrife herb with root being dried is pulverized, plus 25 times amount 70% ethanol, in 70 DEG C of water-bath refluxing extraction 2 times, every time
80min, merges extract, reclaims ethanol, obtains whorlleaf loosestrife herb with root total extract medicinal extract;
(2)The whorlleaf loosestrife herb with root obtaining total extract medicinal extract is carried out column chromatography for separation, resin with D-140 type macroporous absorbent resin
Post blade diameter length ratio is 1:9, loading volume 6BV, wash 6BV removal of impurities, with ethyl acetate:Acetone=10:1 eluant, eluent 7BV wash-out, stream
Speed is 4BV/h, collects eluent, and eluent concentrates, and is dried, obtains final product.
Described whorlleaf loosestrife herb with root extract can also preferably employ following method preparation:
(1)The whorlleaf loosestrife herb with root being dried is pulverized, plus 20 times amount 80% ethanol, in 65 DEG C of water-bath refluxing extraction 3 times, every time
75min, merges extract, reclaims ethanol, obtains whorlleaf loosestrife herb with root total extract medicinal extract;
(2)The whorlleaf loosestrife herb with root obtaining total extract medicinal extract is carried out column chromatography for separation, resin with D-140 type macroporous absorbent resin
Post blade diameter length ratio is 1:8, loading volume 7BV, wash 5BV removal of impurities, with ethyl acetate:Acetone=10:1 eluant, eluent 8BV wash-out, stream
Speed is 3BV/h, collects eluent, and eluent concentrates, and is dried, obtains final product.
Described whorlleaf loosestrife herb with root extract is it is characterised in that this whorlleaf loosestrife herb with root extract adopts conventional pharmaceutical methods in pharmacy
It is prepared into oral formulations.
Described oral formulations are preferably prepared as tablet, pill, hard capsule, granule, oral liquid.
Described whorlleaf loosestrife herb with root extract can be prepared as follows as hard capsule:Take whorlleaf loosestrife herb with root extract, be ground into thin
Powder, adds auxiliary material, mixes, and loads hard shell capsules, obtains final product.
Described whorlleaf loosestrife herb with root extract can be prepared as follows as tablet:Take whorlleaf loosestrife herb with root extract, be ground into fine powder, plus
Enter auxiliary material, mix, make particle, be dried, tabletted, obtain final product.
Whorlleaf loosestrife herb with root extract of the present invention can be used in preparation treatment osteoporosis agents or health products.
Whorlleaf loosestrife herb with root extract of the present invention can be additionally used in preparation treatment rheumatism joint anti-inflammatory drugs or health products.
Verify the technique effect of the present invention by following experimental study:
Experiment one:The experimental study of whorlleaf loosestrife herb with root extract for treating osteoporosis in castrated rat
1 materials and methods
1.1 4 month female SD rats of animal 32, body weight:260g±30g.
1.2 reagent and medicine whorlleaf loosestrife herb with root, are collected in Jiangsu Province Xinpu District south head forest farm;Whorlleaf loosestrife herb with root extract, according to
Method preparation described in description of the invention embodiment 1;Oestradiol benzoate(2mg/ml), Shanghai the 9th pharmaceutical factory's product;Blood
Calcium determinating reagent box, serium inorganic phosphorus measure kit, ALP kit, Beijing Zhong Sheng company.Yellow Jackets, Shanghai the 6th pharmacy
Factory.
1.3 key instrument BT224 semi-automatic biochemical analyzers, dual intensity X line borne densitometers.
1.4 animal model castration operations:40mg/kg body weight intraperitoneal injection of anesthesia is pressed with 2% nembutal, at back
Cut muscle, peritonaeum under central 12 ribs, open fat deposit, excision left and right ovary.Only make abdominal cavity for wherein 8 to cut and do not excise
The sham-operation of ovary, makees normal blank control group(Control group).
1.5 packets and administration animal used as test are divided into 4 groups:Normal blank control group(Control group)8, that is, do evil through another person
Art group, physiological saline 3ml/kg gavage.24 ovariectomized rats are randomly divided into 3 groups:Model group(OP group), with physiology salt
Water 3ml/kg;E group(Positive controls), it is dissolved in 3 ml physiological saline with estradiol, concentration 200 μ g/kg;FM group, by it
It is dissolved in 3 ml physiological saline, concentration 1.5g/kg.Gavage 1 time daily, successive administration 90d.
1.6 observation index medications take blood after terminating after eyeball, are illustrated according to kit, use colorimetric method for determining Ca2 +、P3+With ALPase vigor.Take big femur and shin bone on the right side of rat again, shave cartilaginous tissue, surveyed with Dual-energy X-rays absorptionmetry
Determine the bone density of femur and shin bone(Bone Mineral Density, BMD).
The all data of 1.7 statistical procedures are all used(±s)Represent, with SPSS 11.0 statistical software one way
ANOVA, LSD method is analyzed, and P < 0.05 is statistically significant.
2 results
2.1 couples of Ca2+、P3+, ALPase impact model group(OP group)Ca in Ovariectomized Rat Serum2+、P3+And ALPase
Vigor and normal blank control group(Control group)Compare all significantly raised.After taking whorlleaf loosestrife herb with root extract extract, Ca2+、P3+
With ALPase vigor and model group(OP group)Compare, whorlleaf loosestrife herb with root extract extract group has bright significantly reducing.It is shown in Table 1.
Ca in table 1 each group serum2+、P3+Compare with ALPase vigor mean value(±s)
Group |
Ca2+ |
P3+ |
ALP |
Control group |
2.54±0.03** |
1.69±0.04** |
54.52±10.2** |
OP group |
2.64±0.03 |
2.14±0.05 |
148.26±15.24 |
E group |
2.53±0.09** |
1.72±0.03** |
65.43±15.51** |
FM group |
2.57±0.08* |
1.73±0.05** |
69.42±11.14** |
Note:Compared with OP group, * * P<0.01.
The mensure of 2.2 bone densities
Model group(OP group)The femur of castrated rats is substantially reduced compared with normal control rat with the BMD of shin bone.Take
After whorlleaf loosestrife herb with root extract extract, the BMD of femur and shin bone and model group(OP group)Compare and significantly improve;With normal blank control group
(Control group), positive controls(Estradiol group)Relatively, its difference is not statistically significant.See accompanying drawing 1:Each group femur
BMD value compares, accompanying drawing 2:The BMD value of each group shin bone compares.Note:Compare with OP group, * * P < 0.01.
3 discuss and conclusion
This research results of animal shows, whorlleaf loosestrife herb with root extract group(FM group)Ca in animal used as test serum2+And P3+Concentration
Reduce, illustrate that whorlleaf loosestrife herb with root extract can reduce calcium and bone phosphorus in bone and lose, promote the calcium and phosphorus deposition in bone.Whorlleaf loosestrife herb with root extracts
Thing group(FM group)Animal used as test ALP is also than model group(OP group)Animal is remarkably decreased, and model group is described(OP group)Animal is due to bone
Hypermetabolism, makes brokenly bone and osteogenic action all vigorous, and broken bone effect exceedes osteogenic action, so osteoporosis;Application Huang is opened
After mouth extract, ALP is decreased obviously, and illustrating that whorlleaf loosestrife herb with root extract can suppress Bone m etabolism, increasing bone stable, thus preventing sclerotin
Osteoporosis occur.Femur and shin bone BDM are as a result, it was confirmed that after application whorlleaf loosestrife herb with root extract, BMD is compared with model group(OP group)Animal shows
Work increases.Show that whorlleaf loosestrife herb with root extract can reduce the bone loss of castrated rats, promoting bone growing, adjust Bone m etabolism balance.
Research, it is also shown that the whorlleaf loosestrife herb with root extract of the present invention also has preferable antiinflammatory action, can be treated rheumatic and close
Section inflammation.
Brief description
Fig. 1:The BMD value of each group femur compares
Fig. 2:The BMD value of each group shin bone compares
Specific embodiment:
Embodiment 1:
(1)The whorlleaf loosestrife herb with root being dried is pulverized 20kg, plus 20 times amount 80% ethanol, in 65 DEG C of water-bath refluxing extraction 3 times, every time
75min, merges extract, reclaims ethanol, obtains whorlleaf loosestrife herb with root total extract medicinal extract;
(2)The whorlleaf loosestrife herb with root obtaining total extract medicinal extract is carried out column chromatography for separation, resin with D-140 type macroporous absorbent resin
Post blade diameter length ratio is 1:8, loading volume 7BV, wash 5BV removal of impurities, with ethyl acetate:Acetone=10:1 eluant, eluent 8BV wash-out, stream
Speed is 3BV/h, collects eluent, and eluent concentrates, and is dried, obtains whorlleaf loosestrife herb with root extract 9.4g.
Embodiment 2:
(1)The whorlleaf loosestrife herb with root being dried is pulverized 20kg, plus 15 times amount 90% ethanol, in 60 DEG C of water-bath refluxing extraction 4 times, every time
70min, merges extract, reclaims ethanol, obtains whorlleaf loosestrife herb with root total extract medicinal extract;
(2)The whorlleaf loosestrife herb with root obtaining total extract medicinal extract is carried out column chromatography for separation, resin with D-140 type macroporous absorbent resin
Post blade diameter length ratio is 1:7, loading volume 8BV, wash 4BV removal of impurities, with ethyl acetate:Acetone=10:1 eluant, eluent 9BV wash-out, stream
Speed is 2BV/h, collects eluent, and eluent concentrates, and is dried, obtains whorlleaf loosestrife herb with root extract 9.2g.
Embodiment 3:
(1)The whorlleaf loosestrife herb with root being dried is pulverized 20kg, plus 25 times amount 70% ethanol, in 70 DEG C of water-bath refluxing extraction 2 times, every time
80min, merges extract, reclaims ethanol, obtains whorlleaf loosestrife herb with root total extract medicinal extract;
(2)The whorlleaf loosestrife herb with root obtaining total extract medicinal extract is carried out column chromatography for separation, resin with D-140 type macroporous absorbent resin
Post blade diameter length ratio is 1:9, loading volume 6BV, wash 6BV removal of impurities, with ethyl acetate:Acetone=10:1 eluant, eluent 7BV wash-out, stream
Speed is 4BV/h, collects eluent, and eluent concentrates, and is dried, obtains whorlleaf loosestrife herb with root extract 9.5g.
Embodiment 4:Tablet
Take whorlleaf loosestrife herb with root extract, add appropriate amount of starch, mix, make particle, be dried, tabletted, coating, obtain final product.
Embodiment 5:Tablet
Take whorlleaf loosestrife herb with root extract, add appropriate dextrin, mix, compressing tablet, obtain final product.
Embodiment 6:Hard capsule
Take whorlleaf loosestrife herb with root extract, add appropriate dextrin, mix, make particle, load capsule, make hard capsule, obtain final product.