CN103830253A - Applications of geniposide in preparation of medicines used for treating diabetic nephropathy - Google Patents
Applications of geniposide in preparation of medicines used for treating diabetic nephropathy Download PDFInfo
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- CN103830253A CN103830253A CN201210474877.5A CN201210474877A CN103830253A CN 103830253 A CN103830253 A CN 103830253A CN 201210474877 A CN201210474877 A CN 201210474877A CN 103830253 A CN103830253 A CN 103830253A
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- jasminoidin
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Abstract
The invention provides applications of geniposide in preparation of medicines used for treating diabetic nephropathy. The invention also provides a pharmaceutical composition used for treating or preventing diabetic nephropathy, wherein geniposide is taken as the active ingredient of the pharmaceutical composition. The pharmaceutical composition can be used for oral administration, injection, or topical administration.
Description
Summary
The invention provides the application of jasminoidin in the medicine of preparation treatment diabetic nephropathy, the present invention also provides being used for the treatment of or the pharmaceutical composition of diabetes and nephropathy preventing taking jasminoidin as active component, and said composition can be oral, injection or topical.
Technical field
The present invention relates to the application of jasminoidin in the medicine of preparation treatment diabetic nephropathy.
Background technology
Diabetic nephropathy (Diabetic nephropathy, DN) is one of topmost vascular complication of diabetes, is also the most important reason that diabetics is lethal, disable, and the danger of DN can occur the nearly 30%-40% of diabetic.In western countries, DN has accounted for 40%(D ' the Amico G. Renal replacement therapy throught the world:the registries. Am J Kidney Dis of end-stage renal failure, 1995,25:113).In China, along with improving constantly of living standard, the sickness rate of diabetes has the trend rising year by year, and DN patient also increases (Li Leishi, Guan Tianjun, Liu Zhihong etc., nephropathy and dialysis renal transplantation magazine, 1997,6:103) year by year.The main pathological change of DN is kidney HT, high filtration, glomerular basement membrane thickening and take glomerular mesangium district as main extracellular matrix accumulation, cause diffusivity and nodular glomerulosclerosis, occur the clinical manifestations such as albuminuria, hypertension and renal insufficiency.The pathogenesis of DN is not also illustrated at present completely, and the factors such as polyhydric alcohol Pathway Activation, protein non-enzyme glycosylation, diacylglycerol-protein kinase C activation, oxidative stress, cell and vasoactive factors, heredity that studies confirm that in a large number all may participate in generation and the development of DN.
Jasminoidin is from the dry mature fruit of Maguireothamnus speciosus Fructus Gardeniae, to use high-tech production technology to extract the refining product forming.Jasminoidin is iridoid glycoside compounds, different name geniposide, all Fructus Armeniacae Mume element glucoside geniposide.Jasminoidin has multiple use, and the fermentation of different condition can be made natural edible coloring agent gardenia blue and gardenia red, is also the material medicine that is used for the treatment of the disease such as cardiovascular and cerebrovascular vessel, liver and gall and diabetes.Jasminoidin has cathartic, analgesia, function of gallbladder promoting, antiinflammatory, treatment soft tissue injury and suppresses gastric secretion and reduce the effects such as pancreatic amylase.
But not yet have renal function injury diabetes being caused about jasminoidin to have relevant report and the research of protective effect, the inventor, through a large amount of experimentatioies, is surprised to find the application of jasminoidin in the medicine of preparation treatment diabetic nephropathy.
Summary of the invention
The invention provides the application of jasminoidin in the medicine of preparation treatment diabetic nephropathy.
The invention provides the pharmaceutical composition of the treatment diabetic nephropathy that contains jasminoidin.
The inventor has confirmed that by following test jasminoidin has the effect for the treatment of or diabetes and nephropathy preventing, but is not limited to this.Test Arctiin used and aretigenin component content and be all greater than 99%.This is tested jasminoidin used and extracts and separate preparation by method described in document [Hu Zhen analyzes Chinese patent medicine, the 03rd phase in 2006 etc., Jasminoidin in G. jasminoides Ellis Var. Grandiflora extraction process and HPLC].By test, the inventor finds that jasminoidin treatment administration obviously reduces diabetes model rat blood sugar, reduce diabetes rat urine protein protein content, reduce diabetes rat serum creatinine level, obviously alleviate the two kidney weights of diabetic mice, Histomorphological show treatment group mouse glomerular mesangial cells hypertrophy, glomerule its intimal hyperplasia, tube wall thicken with luminal stenosis all be improved significantly, morphological analysis shows, the ratio for the treatment of group mice mesangial region area and glomerule area, is starkly lower than model group.Above result shows that jasminoidin can treat diabetic nephropathy.
Jasminoidin can mix or dissolve with any pharmaceutically acceptable or edible carrier makes pharmaceutical composition, and these carriers comprise in skin, mucosa, gastrointestinal and pharmaceutically suitable carrier of parenteral or edible carrier.Pharmaceutical composition provided by the invention can be prepared into by means known in the art can oral formulations, as tablet, capsule, granule, chewing agent, pill, suspension, solution etc., non-intestinal drug delivery agent can be made the dosage form such as injection, freeze-dried powder, and topical can be made as cream, ointment, patch, spray, suppository etc.In this pharmaceutical composition, use pharmaceutically useful excipient and additive, comprise nontoxic compatible filler, binding agent, disintegrating agent, buffer agent, antiseptic, anti-gasifying agent, lubricant, correctives, thickening agent, coloring agent, emulsifying agent, stabilizing agent, such as lactose, citric acid, stearic acid, magnesium stearate Gypsum Fibrosum powder, sucrose, corn starch, Pulvis Talci, gelatin, agar, pectin, Oleum Arachidis hypogaeae semen, cocoa butter, ethylene glycol, glucose, procaine hydrochloride, lidocaine hydrochloride, ascorbic acid etc.This pharmaceutical composition can be by the common process preparation of various preparations.
The pharmaceutical composition that contains jasminoidin of the present invention, during with oral form administration, every consumption per day of jasminoidin is 0.001-100 mg/kg body weight, can repeatedly or once take every day.During with injection administration,, can muscle, subcutaneous or intravenous injection, also can intravenous drip, every consumption per day of jasminoidin is 0.001-50 mg/kg body weight.Can repeatedly or once take every day.
Detailed description of the invention:
test example 1: the therapeutical effect of jasminoidin to diabetic nephropathy rats
1. material:
The jasminoidin method described in document [Hu Zhen analyzes Chinese patent medicine, the 03rd phase in 2006 etc., Jasminoidin in G. jasminoides Ellis Var. Grandiflora extraction process and HPLC] of pressing is extracted to separate and is prepared and identify, purity is respectively 99.8%.
Regular grade Wistar rat, female, 3 ~ 4 monthly ages, body weight 190 ~ 210g.
Blood sugar detection test kit, glucose oxidase method, Great Wall, Baoding clinical reagent has company limited to produce; Determination of Urinary Albumin test kit, puts the method for exempting from, Beijing North Institute of Biological Technology; Other test kits are the conventional test kit of hospital.
2. the preparation of rat diabetes model and medication
70 of Wistar rats, fasting 24 hours, gets at random 10 and makes normal control, tail vein injection saline, 0.2 ml/100g, all the other tail vein injection alloxan 40mg/kg(0.2ml/100g) modeling.After modeling three days, eye socket vein treating the preponderant disease instead of the secondary disease blood 100 μ l, centrifugal collection determination of serum modeling rat blood sugar, shaves except blood glucose value is lower than the rat of 16.7mmol/L, glucose in urine feminine gender, and remaining rat is conventional to be raised 4 weeks.Rat fasting, metabolic cage is collected urine, measures urine protein level.According to urine protein level height, rat is divided into 3 groups at random, is respectively model group, jasminoidin group (25mg/kg).
Jasminoidin dissolves with 0.5% sodium carboxymethyl cellulose.The equal gavage of Normal group and model group gives 0.5% sodium carboxymethyl cellulose 0.2ml/100g, and administration group gavage gives relative medicine.Once a day.
3. result is measured
After successive administration 2 weeks, observe weekly each group of rat general status, comprise the mental status, outward appearance, diet, heavy amplification, urine amount, amount of drinking water etc., claim on every Tuesdays rat body weight, collect urinary assay twenty-four-hour urine amount with metabolic cage, measure 24 little enter amount of drinking water.After administration, respectively organize rat and in metabolic cage, collect twenty-four-hour urine liquid, calculate urine amount, centrifugal rear mensuration urine protein content.Eye socket blood sampling, separation of serum is measured blood glucose and serum creatinine and blood urea nitrogen.After rat is put to death, get two kidneys and weigh, calculate kidney weight/body weight value: kidney weight/body weight (%)=kidney weight by weight × 100.
4. result
The normal rats mental status is good, and reaction is quick, and hair is calm glossy; Model group rat lethargy, the back of a bow body of curling up, slow movement, hair color is dim dirty; Give after jasminoidin, the rat mental status is obviously better than model group, and hair color is compared with gloss, and activity freely.Administration group rat body weight amplification is obviously greater than model group, and amount of drinking water obviously reduces, and twenty-four-hour urine amount is also obviously less than model group (table 1).
The impact of table 1 jasminoidin on diabetes rat body weight, amount of drinking water and urine amount (
)
With normal group comparison:
#, P<0.05,
##, P<0.01; With model group comparison,
*, P<0.05,
*, P, <0.01.
Table 2 blood sugar detection result shows, gives jasminoidin and all can significantly reduce blood glucose in diabetic rats value, (table 2)
The impact of table 2 jasminoidin on blood glucose in diabetic rats (
)
With normal group comparison:
#, P<0.05,
##, P<0.01; With model group comparison,
*, P<0.05,
*, P, <0.01.
As shown in Table 3, rat serum creatinine, blood urea nitrogen and Determination of Urinary Albumin result show, diabetes model rat gives after jasminoidin, and creatinine, blood urea nitrogen and urinaryalbumin level are all starkly lower than model group rat, illustrates that jasminoidin has therapeutical effect (table 3) to diabetic nephropathy
The impact of table 3 jasminoidin on diabetes rat serum creatinine and urea nitrogen levels (
)
With normal group comparison:
#, P<0.05,
##, P<0.01; With model group comparison,
*, P<0.05,
*, P, <0.01.
Preparation example 1: prepare jasminoidin capsule
By jasminoidin 50g, lactose 122g and corn starch 95g mix 10-15 minute in mixer, add magnesium stearate 3g mixing 1-3 minute, pack 1000 seed lac softgel shells into.
Preparation example 2: prepare injection
Get jasminoidin 50g and be dissolved in the appropriate injection normal saline of 60 DEG C, add 0.05% injection-use activated carbon by amount of preparation and stir, leave standstill 15 minutes, 0.22 μ m filtering with microporous membrane.Injecting water, to make final volume be 10000ml, stirs evenly.Sampling and measuring pH value and content, qualified rear filtration, 115 DEG C of pressure sterilizings of embedding 30 minutes, to obtain final product.
Claims (4)
1. the application of jasminoidin in the medicine of preparation treatment diabetic nephropathy.
2. the pharmaceutical composition that is used for the treatment of diabetic nephropathy taking jasminoidin as active component.
3. pharmaceutical composition according to claim 2, it can oral administration, injection and topical approach carry out administration.
4. medicine according to claim 3 is to compound, and it is tablet, capsule, pill, solution, freeze-dried powder, injection.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201210474877.5A CN103830253A (en) | 2012-11-21 | 2012-11-21 | Applications of geniposide in preparation of medicines used for treating diabetic nephropathy |
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| CN201210474877.5A CN103830253A (en) | 2012-11-21 | 2012-11-21 | Applications of geniposide in preparation of medicines used for treating diabetic nephropathy |
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| CN103830253A true CN103830253A (en) | 2014-06-04 |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104814933A (en) * | 2015-04-22 | 2015-08-05 | 张永胜 | Gardenia extract freeze-dried powder injection and preparation method thereof |
-
2012
- 2012-11-21 CN CN201210474877.5A patent/CN103830253A/en active Pending
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104814933A (en) * | 2015-04-22 | 2015-08-05 | 张永胜 | Gardenia extract freeze-dried powder injection and preparation method thereof |
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Application publication date: 20140604 |