CN104815138A - Immature bitter orange extract, preparation and application - Google Patents
Immature bitter orange extract, preparation and application Download PDFInfo
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- CN104815138A CN104815138A CN201510216118.2A CN201510216118A CN104815138A CN 104815138 A CN104815138 A CN 104815138A CN 201510216118 A CN201510216118 A CN 201510216118A CN 104815138 A CN104815138 A CN 104815138A
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Abstract
The invention discloses an immature bitter orange extract, a preparation and an application, belongs to the field of a traditional Chinese medicine, and particularly relates to an immature bitter orange extract and a medicinal preparation containing the extract. The immature bitter orange extract can be used for preparing a medicine for preventing or treating obesity. The immature bitter orange extract, which is obtained by adding a small amount of rhizoma anemarrhenae medicinal material into an immature bitter orange medicinal material, has a significant effect of treating the obesity, and has an unexpected effect in comparison with a single immature bitter orange extracting method. Based on the sufficient and reasonable design, the immature bitter orange extract with a significant effect can be obtained by extracting, denominating and enriching ethanol water with proper concentration.
Description
Technical field
The present invention relates to the field of Chinese medicines, be specifically related to a kind of Furctus Aurantii Immaturus extract and containing the pharmaceutical preparation of this extract, this Furctus Aurantii Immaturus extract can be used for preparing the medicine of prevention or treatment of obesity.
Background technology
Fructus Aurantii Immaturus is clinical conventional Chinese medicine, is rutaceae Citrus aurantium Linn.
citrus aurantiumand variety or Fructus Citri sinensis L.
citrus sinensisthe dry young fruit of Osbeck.5 ~ June collects the fruit from falling, and removing impurity, be two halves from middle part crosscut, dry or cold drying, smaller directly dries or cold drying.The place of production of Fructus Aurantii Immaturus mainly contains the ground such as Sichuan, Jiangxi, Hunan, Fujian, produces Citrus aurantium Linn. for genuine medicinal materials with Jiangxi, and it is best in quality to produce goose eye Fructus Aurantii Immaturus with Jiangxi.
Fructus Aurantii Immaturus has dispelling the stagnated QI removing food stagnancy, effects such as loose painful abdominal mass of reducing phlegm.Clinically to stop in stagnant, feeling of fullness distending pain, heavy after dysentery, constipation, the stagnant vapour lock of expectorant, the thoracic obstruction, blocked-up chest, visceroptosis, in the prescription that " TCM Recipe voluminous dictionary " includes more than in the prescription of 7% containing Fructus Aurantii Immaturus, it serves to show that Fructus Aurantii Immaturus is wide in clinical practice.
Research shows, the principle active component of Fructus Aurantii Immaturus is volatile oil, alkaloids and flavones ingredient thereof.Wherein, volatile oil main component is d-limonen, citric acid etc.; Alkaloids composition is mainly Neosynephrine, N-methyltyramine; Flavones ingredient is mainly naringin, neohesperidin and hesperidin.The content difference of its Neosynephrine of the former different Fructus Aurantii Immaturus of base, naringin and Hesperidin is very large.Containing neohesperidin during Citrus aurantium Linn. fruit immaturity, when fruit maturation, neohesperidin disappears.Sweet orange fruit is not containing neohesperidin.The content of the Fructus Aurantii Immaturus that different growing stages is plucked, its effective ingredient of Fructus Aurantii Immaturus of different-grain diameter size is also different.Composition in Fructus Aurantii Immaturus volatile oil is except outside the Pass having with kind, also relevant with the place of production.The content of Neosynephrine is along with the prolongation of collecting period, and the content of Neosynephrine reduces obviously, but its content difference and kind, the place of production do not have obvious dependency.Along with the increase of Fructus Aurantii Immaturus particle diameter, in Fructus Aurantii Immaturus, the content of naringin is in rising trend.In the Fructus Aurantii Immaturus of Hunan, the content of total alkaloids and volatile oil is the highest, but with Jiangxi Fructus Aurantii Immaturus, Fructus Ponciri Trifoliatae no significant difference, Fructus Citri sinensis Fructus Aurantii Immaturus content is minimum.Wherein, the content of Neosynephrine is the highest with goose eye Fructus Aurantii Immaturus, and the content of Hesperidin is the highest with Fructus Ponciri Trifoliatae, and the content of naringin is the highest with Fructus Citri grandis content.
Summary of the invention
The object of this invention is to provide a kind of Furctus Aurantii Immaturus extract, the pharmaceutical preparation containing this extract and utilize this extract to prepare prevention or the purposes of obesity treating medicine.
Above-mentioned purpose of the present invention is achieved by technical scheme below:
A kind of Furctus Aurantii Immaturus extract, this extract is prepared by following methods:
Step one: be Fructus Aurantii Immaturus 0.05-0.09 rhizoma ane marrhenae co-grinding doubly by Fructus Aurantii Immaturus and weight;
Step 2: the ethanol water circumfluence distillation 2-3 hour by the medical material concentration of pulverizing being 60-85%, extracts 2-3 time, and each ethanol water volume is Fructus Aurantii Immaturus weight 3-5 times;
Step 3: be concentrated into by gained extracting solution without alcohol taste, by D101 type macroporous resin enrichment, first uses the remove impurity of 30-40% ethanol, be eluted to eluent colourless, then use 65%-75% ethanol deposition activity part, be eluted to eluent colourless, 65%-85% ethanol elution is concentrated, spraying dry.
Further, in described Furctus Aurantii Immaturus extract preparation method, rhizoma ane marrhenae weight is 0.06-0.08 times of Fructus Aurantii Immaturus weight.
Further, in described Furctus Aurantii Immaturus extract preparation method, described in step 2, ethanol water is the ethanol water of 75%.
Further, in described Furctus Aurantii Immaturus extract preparation method, step 3 is used for the ethanol of remove impurity is 35% ethanol.
Further, in described Furctus Aurantii Immaturus extract preparation method, step 3 is used for the ethanol of deposition activity component is 70% ethanol.
Pharmaceutical preparation, the described Furctus Aurantii Immaturus extract containing treatment effective dose and pharmaceutically acceptable carrier.
The application of described Furctus Aurantii Immaturus extract in preparation prevention or obesity treating medicine.
When extract of the present invention is used as medicine, directly can uses, or use in the form of a pharmaceutical preparation.
Described pharmaceutical preparation contains the Furctus Aurantii Immaturus extract of the present invention for the treatment of effective dose, and all the other are acceptable on materia medica, nontoxic to humans and animals and pharmaceutically suitable carrier of inertia and/or excipient.
Described pharmaceutically suitable carrier or excipient are that one or more are selected from solid, semisolid and liquid diluent, filler and pharmaceutical preparation adjuvant.Pharmaceutical preparation of the present invention is used with the form of per weight dose.Extract of the present invention is applied to by form that is oral or injection the patient needing treatment.For time oral, tablet, slow releasing tablet, controlled release tablet, capsule, drop pill, micropill, suspensoid, Emulsion, powder or granule, oral liquid etc. can be made into; During for injecting, can be made into aqueous or oily solution, aseptic powder injection, liposome or the Emulsion etc. of sterilizing.
Advantage of the present invention: the present invention, by adding a small amount of rhizoma ane marrhenae in Fructus Aurantii Immaturus, makes final obtained extract have the effect that significantly treatment is fat, has an unexpected effect than extracting tool with Fructus Aurantii Immaturus separately; The present invention is based on fully, rational EXPERIMENTAL DESIGN, to extract by selecting the ethanol water of suitable concn to carry out, remove impurity and enrichment, can Furctus Aurantii Immaturus extract evident in efficacy be obtained.
Detailed description of the invention
Further illustrate essentiality content of the present invention below in conjunction with embodiment, but do not limit scope with this.Although be explained in detail the present invention with reference to preferred embodiment, those of ordinary skill in the art should be appreciated that and can modify to technical scheme of the present invention or equivalent replacement, and does not depart from essence and the scope of technical solution of the present invention.
Main agents and material: Fructus Aurantii Immaturus and rhizoma ane marrhenae are purchased from Hui nationality's Chinese Medicinal Materials Markets; Food-grade ethanol is purchased from Shanghai Ling Feng chemical reagent company limited; Pharmaceutical grade D101 macroporous resin is purchased from sky tunami letter resin company limited.
Embodiment 1: rhizoma ane marrhenae amount is Fructus Aurantii Immaturus weight 0.05 times
Get 10kg Fructus Aurantii Immaturus and 0.5kg rhizoma ane marrhenae co-grinding; With the ethanol water circumfluence distillation 3 times that concentration is 75%, first time 50L extracts 3 hours, and second and third time 30L extracts 2 hours; Gained extracting solution is concentrated into without alcohol taste, by D101 type macroporous resin enrichment, first uses 35% ethanol remove impurity, be eluted to eluent colourless, then use 70% ethanol deposition activity part, be eluted to eluent colourless, 70% ethanol elution concentrated, spraying dry.
Embodiment 2: rhizoma ane marrhenae amount is Fructus Aurantii Immaturus weight 0.06 times
Get 10kg Fructus Aurantii Immaturus and 0.6kg rhizoma ane marrhenae co-grinding; With the ethanol water circumfluence distillation 3 times that concentration is 75%, first time 50L extracts 3 hours, and second and third time 30L extracts 2 hours; Gained extracting solution is concentrated into without alcohol taste, by D101 type macroporous resin enrichment, first uses 35% ethanol remove impurity, be eluted to eluent colourless, then use 70% ethanol deposition activity part, be eluted to eluent colourless, 70% ethanol elution concentrated, spraying dry.
Embodiment 3: rhizoma ane marrhenae amount is Fructus Aurantii Immaturus weight 0.08 times
Get 10kg Fructus Aurantii Immaturus and 0.8kg rhizoma ane marrhenae co-grinding; With the ethanol water circumfluence distillation 3 times that concentration is 75%, first time 50L extracts 3 hours, and second and third time 30L extracts 2 hours; Gained extracting solution is concentrated into without alcohol taste, by D101 type macroporous resin enrichment, first uses 35% ethanol remove impurity, be eluted to eluent colourless, then use 70% ethanol deposition activity part, be eluted to eluent colourless, 70% ethanol elution concentrated, spraying dry.
Embodiment 4: rhizoma ane marrhenae amount is Fructus Aurantii Immaturus weight 0.09 times
Get 10kg Fructus Aurantii Immaturus and 0.9kg rhizoma ane marrhenae co-grinding; With the ethanol water circumfluence distillation 3 times that concentration is 75%, first time 50L extracts 3 hours, and second and third time 30L extracts 2 hours; Gained extracting solution is concentrated into without alcohol taste, by D101 type macroporous resin enrichment, first uses 35% ethanol remove impurity, be eluted to eluent colourless, then use 70% ethanol deposition activity part, be eluted to eluent colourless, 70% ethanol elution concentrated, spraying dry.
Embodiment 5: step 2 60% ethanol water extracts
Get 10kg Fructus Aurantii Immaturus and 0.6kg rhizoma ane marrhenae co-grinding; With the ethanol water circumfluence distillation 3 times that concentration is 60%, first time 50L extracts 3 hours, and second and third time 30L extracts 2 hours; Gained extracting solution is concentrated into without alcohol taste, by D101 type macroporous resin enrichment, first uses 35% ethanol remove impurity, be eluted to eluent colourless, then use 70% ethanol deposition activity part, be eluted to eluent colourless, 70% ethanol elution concentrated, spraying dry.
Embodiment 6: step 2 85% ethanol water extracts
Get 10kg Fructus Aurantii Immaturus and 0.6kg rhizoma ane marrhenae co-grinding; With the ethanol water circumfluence distillation 3 times that concentration is 85%, first time 50L extracts 3 hours, and second and third time 30L extracts 2 hours; Gained extracting solution is concentrated into without alcohol taste, by D101 type macroporous resin enrichment, first uses 35% ethanol remove impurity, be eluted to eluent colourless, then use 70% ethanol deposition activity part, be eluted to eluent colourless, 70% ethanol elution concentrated, spraying dry.
Embodiment 7: step 3 is except using mixedly 30% ethanol
Get 10kg Fructus Aurantii Immaturus and 0.6kg rhizoma ane marrhenae co-grinding; With the ethanol water circumfluence distillation 3 times that concentration is 75%, first time 50L extracts 3 hours, and second and third time 30L extracts 2 hours; Gained extracting solution is concentrated into without alcohol taste, by D101 type macroporous resin enrichment, first uses 30% ethanol remove impurity, be eluted to eluent colourless, then use 70% ethanol deposition activity part, be eluted to eluent colourless, 70% ethanol elution concentrated, spraying dry.
Embodiment 8: step 3 is except using mixedly 40% ethanol
Get 10kg Fructus Aurantii Immaturus and 0.6kg rhizoma ane marrhenae co-grinding; With the ethanol water circumfluence distillation 3 times that concentration is 75%, first time 50L extracts 3 hours, and second and third time 30L extracts 2 hours; Gained extracting solution is concentrated into without alcohol taste, by D101 type macroporous resin enrichment, first uses 40% ethanol remove impurity, be eluted to eluent colourless, then use 70% ethanol deposition activity part, be eluted to eluent colourless, 70% ethanol elution concentrated, spraying dry.
Embodiment 9: step 3 enrichment 65% ethanol
Get 10kg Fructus Aurantii Immaturus and 0.6kg rhizoma ane marrhenae co-grinding; With the ethanol water circumfluence distillation 3 times that concentration is 75%, first time 50L extracts 3 hours, and second and third time 30L extracts 2 hours; Gained extracting solution is concentrated into without alcohol taste, by D101 type macroporous resin enrichment, first uses 35% ethanol remove impurity, be eluted to eluent colourless, then use 65% ethanol deposition activity part, be eluted to eluent colourless, 65% ethanol elution concentrated, spraying dry.
Embodiment 10: step 3 enrichment 85% ethanol
Get 10kg Fructus Aurantii Immaturus and 0.6kg rhizoma ane marrhenae co-grinding; With the ethanol water circumfluence distillation 3 times that concentration is 75%, first time 50L extracts 3 hours, and second and third time 30L extracts 2 hours; Gained extracting solution is concentrated into without alcohol taste, by D101 type macroporous resin enrichment, first uses 35% ethanol remove impurity, be eluted to eluent colourless, then use 85% ethanol deposition activity part, be eluted to eluent colourless, 85% ethanol elution concentrated, spraying dry.
Embodiment 11: comparative example's (not adding the Rhizoma Anemarrhenae)
Get 10kg Fructus Aurantii Immaturus to pulverize; With the ethanol water circumfluence distillation 3 times that concentration is 75%, first time 50L extracts 3 hours, and second and third time 30L extracts 2 hours; Gained extracting solution is concentrated into without alcohol taste, by D101 type macroporous resin enrichment, first uses 35% ethanol remove impurity, be eluted to eluent colourless, then use 70% ethanol deposition activity part, be eluted to eluent colourless, 70% ethanol elution concentrated, spraying dry.
Embodiment 12: the preparation of tablet
By embodiment 2 method first obtained extract, add excipient, pelletizing press sheet in itself and excipient weight than the ratio for 1:8.
Embodiment 13: the preparation of oral liquid
By embodiment 2 method first obtained extract, oral liquid method for making makes oral liquid routinely.
Embodiment 14: the preparation of capsule or granule
By embodiment 2 method first obtained extract, add excipient in itself and excipient weight than the ratio for 1:9, make capsule or granule.
Embodiment 15: the preparation of injection
By embodiment 2 method first obtained extract, inject routinely with water, fine straining, injection is made in embedding sterilizing.
Embodiment 16: the preparation of aseptic powder injection
By embodiment 2 method first obtained extract, be dissolved in sterile water for injection, stirring makes molten, filters with aseptic suction funnel, more aseptic fine straining, and be sub-packed in ampoule, after frozen drying, aseptic sealing by fusing obtains injectable powder.
Embodiment 17: Furctus Aurantii Immaturus extract measures the inhibit activities of pancreatic lipase
First substrate p-Nitrophenyl acetate(sigma company) be made into 1.35M with phosphate buffer (PBS, pH7.4); Porcine pancreatic lipase (sigma company) is made into 10mg/ml with phosphate buffer; The Furctus Aurantii Immaturus extract phosphate buffer obtained according to the method for embodiment 2 is mixed with the solution of variable concentrations.Then add successively in 96 orifice plates 50 μ l dilute 20 times after enzymatic solution, 40 μ l dilute the given the test agent of the substrate solution after 1000 times and 10 μ l variable concentrations, mixing.React 20 minutes at 25 DEG C, under 405nm, detected the absorbance in every hole every 2 minutes.
Calculating given the test agent to the suppression ratio (%) of pancreatic lipase according to the absorbance under 405nm, take distilled water as contrast, and when inhibition of enzyme activity rate (%) being reached 50%, the concentration determination of inhibitor is IC
50value.Suppression ratio (%) calculates according to following formula:
Suppression ratio (%)=[(A-B)-(C-D)]/(A-B) × 100%
In above formula, A represent reaction after the absorbance of blank well under 405nm, B represent reaction before the absorbance of blank well under 405nm, C represent reaction after the absorbance of sample well under 405nm, D represent reaction before the absorbance of sample well under 405nm.
Detect Furctus Aurantii Immaturus extract to the inhibitory action result of pancreatic lipase, IC
50be 10.65 ± 0.139 μ g/ml, show that Furctus Aurantii Immaturus extract has significant inhibitory action to pancreatic lipase.
Embodiment 18: Furctus Aurantii Immaturus extract is to the antiobesity action of obese rat
Zucker rat (heritability obese rat) is bred by Shanghai medicine institute of Chinese Academy of Sciences Animal House, male, 8 week age.Get normal Zucker rat 6, as blank group.Fatty Zucker rats is divided into 12 groups, i.e. model control group, Furctus Aurantii Immaturus extract group (totally 10 groups) and comparative example's group, often organizes 6.By Furctus Aurantii Immaturus extract 0.5%CMC-Na hydrotropy obtained for the method according to embodiment 2, dosage is 1g/kg; Blank and model control group gives the 0.5%CMC-Na of equal volume, oral administration gavage administration two weeks.Periodic detection diet and body weight.The results are shown in Table 1.
Table 1 Furctus Aurantii Immaturus extract is on the impact (± SE) of Zucker rat body weight and diet
Compared with model control group, * * P < 0.05.
Conclusion: as can be seen from Table 1, compared with model control group, Furctus Aurantii Immaturus extract group rat body weight of the present invention increases and obviously declines, and do not have a significant impact, and rat feces is normal to diet.
Fat intake too much may be causeed fat and the decompensated disease such as the diabetes relevant to obesity, hyperlipemia, fatty liver.Suppress pancreatic lipase that fat can be suppressed in the decomposition of small intestinal, thus suppress the absorption of fat.Furctus Aurantii Immaturus extract as pancreatic lipase inhibitor, and has antiobesity action, can be used for the diseases such as prevention or treatment of obesity.
Claims (7)
1. a Furctus Aurantii Immaturus extract, is characterized in that this extract is prepared by following methods:
Step one: be Fructus Aurantii Immaturus 0.05-0.09 rhizoma ane marrhenae co-grinding doubly by Fructus Aurantii Immaturus and weight;
Step 2: the ethanol water circumfluence distillation 2-3 hour by the medical material concentration of pulverizing being 60-85%, extracts 2-3 time, and each ethanol water volume is Fructus Aurantii Immaturus weight 3-5 times;
Step 3: be concentrated into by gained extracting solution without alcohol taste, by D101 type macroporous resin enrichment, first uses the remove impurity of 30-40% ethanol, be eluted to eluent colourless, then use 65%-75% ethanol deposition activity part, be eluted to eluent colourless, 65%-85% ethanol elution is concentrated, spraying dry.
2. Furctus Aurantii Immaturus extract according to claim 1, is characterized in that rhizoma ane marrhenae weight is 0.06-0.08 times of Fructus Aurantii Immaturus weight.
3. Furctus Aurantii Immaturus extract according to claim 1, is characterized in that ethanol water described in step 2 is the ethanol water of 75%.
4. Furctus Aurantii Immaturus extract according to claim 1, is characterized in that step 3 is 35% ethanol for the ethanol of remove impurity.
5. Furctus Aurantii Immaturus extract according to claim 1, is characterized in that step 3 is 70% ethanol for the ethanol of deposition activity component.
6. pharmaceutical preparation, the Furctus Aurantii Immaturus extract according to claim 1 containing treatment effective dose and pharmaceutically acceptable carrier.
7. the application of Furctus Aurantii Immaturus extract according to claim 1 in preparation prevention or obesity treating medicine.
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Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
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| CN105056091A (en) * | 2015-08-20 | 2015-11-18 | 陈鹏 | Cardamom extract, preparation containing cardamom extract, and application of cardamom extract in treatment of obesity |
| CN110772577A (en) * | 2019-12-20 | 2020-02-11 | 北京康比特体育科技股份有限公司 | Weight-losing composition and preparation method and application thereof |
| EP3903801A1 (en) * | 2020-04-23 | 2021-11-03 | Naturextralab S.r.l. | Formulation comprising citrus bergamia l. and fortunella japonica extracts and its use to limit pancreatic lipase |
| CN114470052A (en) * | 2022-02-18 | 2022-05-13 | 江西农业大学 | Application of traditional Chinese medicine immature bitter orange ethanol extract in preparation of antibacterial drugs |
| IT202100007721A1 (en) * | 2021-03-29 | 2022-09-29 | Naturextralab S R L | FORMULATION BASED ON PLANT EXTRACTS AND ITS USE TO LIMIT SERUM LEVELS OF CHOLESTEROL AND THEIR STATIN-LIKE ACTIVITY |
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| CN102370763A (en) * | 2007-08-07 | 2012-03-14 | 北京北大维信生物科技有限公司 | Application of Chinese medicinal herb immature bitter orange extract to preparation of weight-reducing and lipid-lowering medicament or preparation of medicament having lipase activity suppressing effect |
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Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105056091A (en) * | 2015-08-20 | 2015-11-18 | 陈鹏 | Cardamom extract, preparation containing cardamom extract, and application of cardamom extract in treatment of obesity |
| CN110772577A (en) * | 2019-12-20 | 2020-02-11 | 北京康比特体育科技股份有限公司 | Weight-losing composition and preparation method and application thereof |
| EP3903801A1 (en) * | 2020-04-23 | 2021-11-03 | Naturextralab S.r.l. | Formulation comprising citrus bergamia l. and fortunella japonica extracts and its use to limit pancreatic lipase |
| IT202100007721A1 (en) * | 2021-03-29 | 2022-09-29 | Naturextralab S R L | FORMULATION BASED ON PLANT EXTRACTS AND ITS USE TO LIMIT SERUM LEVELS OF CHOLESTEROL AND THEIR STATIN-LIKE ACTIVITY |
| CN114470052A (en) * | 2022-02-18 | 2022-05-13 | 江西农业大学 | Application of traditional Chinese medicine immature bitter orange ethanol extract in preparation of antibacterial drugs |
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Application publication date: 20150805 |