CN108853170A - The composition of oral dissolution calcinm oxalate calculus - Google Patents
The composition of oral dissolution calcinm oxalate calculus Download PDFInfo
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Abstract
A kind of composition of oral dissolution calcinm oxalate calculus, the composition includes 0.1%~10% Garcinia Cambogia extract microcapsule；Or 0.1%~10% hydroxycitric acid or hydroxycitrate derivatives micro-capsule.Due to containing Garcinia Cambogia extract microcapsule, hydroxycitric acid or hydroxycitrate derivatives micro-capsule; effectively dissolution can be realized for calculus is formed by calcium oxalate crystal; the material selection high-molecular organic material of the Garcinia Cambogia extract microcapsule, hydroxycitric acid or hydroxycitrate derivatives micro-capsule; with certain solubility; convenient for the time of control composition disintegration, dissolution, the effective component in composition can be protected to reach the position of efficient absorption.Composition according to the present invention uses natural extract, does not have toxic side effect to human body, and litholytic effect is good, and applicable oral crowd is extensive, and the crowd not limited strictly is with a wide range of applications.
Description
Technical field
The invention mainly relates to oral administered drugs areas, more particularly to one kind by oral absorption and for dissolving by oxalic acid
The composition of the lithogenous orally available calcinm oxalate calculus of dissolution of calcium crystalline.
Background technique
The treatment means of kidney stone mainly have three kinds of operative treatment, extracorporeal shock rubble and drug therapy main means.
Operative treatment has a degree of organ damage risk, and calculus is very easy to recurrence, performs the operation repeatedly and unrealistic.Kidney
Structure is very exquisite subtle, and extracorporeal shock wave lithotripsy is very big to the damage of kidney, it is likely that the structure of injury kidney itself, it is this
Method cannot fundamentally exclude calculus, and since the process of rubble is difficult to manipulate, variable factor is more, the grain diameter of rubble
It is very difficult to control, excessive calculus is possible to cause the tearing at such as urethra position in discharge process, brings to performer
Unnecessary pain.The drug of existing treatment kidney stone has niter element and oral lithagogue liquid etc., does not have obvious effects on, or clothes
It is very long with the time.In addition for some traditional Chinese medicine lithagogue electuaries, the ingredient of its formulation of drug is confirmed without evidence-based medical
And pharmacological mechanism, potential side effect be not apparent.On the other hand, what these treatment means caused more roughly is concurrent
Disease, need to accomplish a period of time, or needs to adhere to for a long time treatment cooperation, does not adapt to present society with fast rhythm's life.
Summary of the invention
For the defect for partially solving the above-mentioned prior art, the present invention provides a kind of combination of oral dissolution calcinm oxalate calculus
Object, the composition include 0.1%~10% Garcinia Cambogia extract microcapsule；Or 0.1%~10% hydroxycitric acid or hydroxyl
Base citric acid derivant micro-capsule.
Preferably, the micro-capsule selects at least one of cellulose, glutinous polysaccharide, gelatin material to be made.
Preferably, the composition further include control pH value range be less than or equal to 7 buffer salt, and/or for
Calcium ion forms the complexant of water-soluble complex.
Preferably, the hydroxycitrate derivatives include by hydroxycitric acid or the derivative obtained esters chemical combination of citric acid
At least one of object, lactone compound, salt, double salt compound.
It preferably, further include that targeting body is formed in conjunction with hydroxycitric acid or hydroxycitrate derivatives in the composition
Carrier.
It is highly preferred that the carrier is made of at least one of polysaccharide, protein, lipid bio-compatible material.
It is highly preferred that the partial size of the carrier is more than or equal to 12 μm.
Preferably, the composition includes sweet flavor modifier and/or flavor improving agent；The sweet flavor modifier includes grape
At least one of sugar, fructose, Aspartame；The flavor improving agent includes fruity flavor and/or colorant.
The present invention provides a kind of compositions of oral dissolution calcinm oxalate calculus can preferably solve partial technical problems, and
Tool has the advantage that：
(1) composition of a kind of oral dissolution calcinm oxalate calculus according to the present invention, due to containing gamboge berry extract
Micro-capsule, hydroxycitric acid or hydroxycitrate derivatives micro-capsule can be realized effectively for calculus is formed by calcium oxalate crystal
Dissolution, the material selection of the Garcinia Cambogia extract microcapsule, hydroxycitric acid or hydroxycitrate derivatives micro-capsule are organic in vivo
High molecular material has certain solubility, convenient for the time of control composition disintegration, dissolution, can protect in composition
The gastrointestinal tract of effective component arrival efficient absorption；
(2) composition of a kind of oral dissolution calcinm oxalate calculus according to the present invention, also addition control in the composition
PH value processed is less than or equal to 7 buffer salt, and addition buffer salt system can protect the effective component of composition, reduction be oxidized or
It is influenced by digestive secretion liquid, keeps effective state；
(3) composition of a kind of oral dissolution calcinm oxalate calculus according to the present invention, also added in the composition
The complexant of soluble complex can be formed with calcium ion, the complexant being capable of stable bond hydroxycitric acid and calcium oxalate
The calcium ion of dissolution is reacted, and forms water-soluble complexes, calcium ion is avoided to react to be formed again with oxalate denominationby
Precipitating, and the direction for forcing reaction to be dissociated to calcium oxalate crystals is mobile；
(4) composition of a kind of oral dissolution calcinm oxalate calculus according to the present invention, use in the composition with
Hydroxycitric acid plays the hydroxycitrate derivatives of similar or stronger dissolution, and hydroxycitrate derivatives are with more stable
The form of (low entropy value) exists, the hydroxycitrate derivatives of the forms such as forming salt, double salt, can also be according to the state for taking orally person
The type of cation is selected, there is broader practice prospect；
(5) composition of a kind of oral dissolution calcinm oxalate calculus according to the present invention, further include in the composition with
Hydroxycitric acid or hydroxycitrate derivatives form the carrier of targeting body, and the carrier can be distinctive physical by itself
Matter or chemical property drive the hydroxycitric acid or hydroxycitrate derivatives, be lifted at privileged site hydroxycitric acid or
Hydroxycitrate derivatives effective concentration；
(6) composition of a kind of oral dissolution calcinm oxalate calculus according to the present invention, it is practical by limiting diameter of carrier
On limit hydroxycitric acid or hydroxycitrate derivatives and the partial size of targeting body is collectively formed in carrier, and then by following in vivo
The targeting body is limited in renal tubule, can effectively promote hydroxycitric acid or hydroxycitrate derivatives in kidney by the characteristic of ring
The effective concentration in tubule region；
(7) composition of a kind of oral dissolution calcinm oxalate calculus according to the present invention, addition sweet taste improvement in composition
Agent, flavor improving agent mode, improve the experience of taking of composition, improve the sensory experience and psychological feelings of oral person.
Detailed description of the invention
Above-mentioned and/or additional aspect and advantage of the invention will become from the following description of the accompanying drawings of embodiments
Obviously and it is readily appreciated that, wherein：
Fig. 1 is the renal tubule microdissection figure that female Drosophila is full of calcium oxalate crystal；
Fig. 2 is the renal tubule microdissection figure of one week female Drosophila of the diet of A containing composition；
Fig. 3 is the renal tubule microdissection figure of one week female Drosophila of the diet of A-1 containing composition；
Fig. 4 is the renal tubule microdissection figure of one week female Drosophila of the diet of A-2 containing composition；
Fig. 5 is the histogram of gamboge berry extract percentage and calculus region area relationship in composition；
Fig. 6 is the calculus renal tubule microdissection figure that calcium oxalate crystal is full of before impregnating hydroxycitric acid；
Fig. 7 is the calculus renal tubule microdissection figure impregnated after 1% hydroxycitric acid 20min；
Fig. 8 is the calculus renal tubule microdissection figure impregnated after 1% hydroxycitric acid 40min；
Fig. 9 is the calculus renal tubule microdissection figure impregnated after 1% hydroxycitric acid 60min；
Figure 10 is the calculus renal tubule microdissection figure impregnated after 1% hydroxycitric acid 100min；
Figure 11 is the calculus renal tubule microdissection figure impregnated after 1% hydroxycitric acid 120min；
Figure 12 is soaking time and calculus area surface in the case where hydroxycitric acid, the gamboge berry extract of various concentration impregnate
The line chart of product relationship.
Specific embodiment
The embodiment of the present invention is described below in detail, examples of the embodiments are shown in the accompanying drawings.Below with reference to
The embodiment of attached drawing description is exemplary, and for explaining only the invention, and is not construed as limiting the claims.In order to just
In the practical application for the composition for showing a kind of oral dissolution calcinm oxalate calculus, following embodiments will introduce the composition
Specific component part makes the application relationship of the composition and effect show more abundant and be easy to understand, it is notable that
Protection scope of the present invention is not by being limited.
Embodiment 1
The present embodiment 1 provide it is a kind of it is oral dissolution calcinm oxalate calculus composition A, the composition A in include gamboge
The Garcinia Cambogia extract microcapsule of berry extract, the conversion of gamboge berry extract is mass percent in the Garcinia Cambogia extract microcapsule
Account for the 1% of composition A.The gamboge berry extract contains a certain amount of hydroxycitric acid, the hydroxycitric acid and calcium oxalate
Crystal can leniently react in vivo, and the calcium oxalate crystals after reaction significantly become smaller, and occur without depositional phenomenon again.
The calcium oxalate crystals just refer to calcinm oxalate calculus.In other possible embodiments, in the Garcinia Cambogia extract microcapsule
Gamboge berry extract account for the 0.1%~10% of the composition A.It is further preferred that in the Garcinia Cambogia extract microcapsule
Gamboge berry extract account for 0.1%, 0.5%, the 10% of the composition A.
Specifically, in the present embodiment, the Garcinia Cambogia extract microcapsule is made of cellulose, the gamboge berry extract
Micro-capsule is the orbicule for being coated with the gamboge berry extract.The cellulose can also be preferably provided with certain water in the present embodiment
The cellulose of dissolubility, such as carboxymethyl cellulose, methylcellulose, ethyl cellulose.Only in the present embodiment, the micro-capsule by
Carboxymethyl cellulose composition, the micro-capsule of formation can partly or entirely dissolve within a certain period of time, in Garcinia Cambogia extract microcapsule
Under protection, gamboge berry extract therein can reach specified absorption site, promote the absorption of gamboge berry extract, avoid simultaneously
Gamboge berry extract is oxidized in early period or is influenced by digestive secretion liquid, makes the absorptivity of effective component in gamboge berry extract
It is promoted.It is highly preferred that in the present embodiment, the multiple Garcinia Cambogia extract microcapsule can be coated again one layer with outermost layer and be easy to mouth
The water-soluble capsulating material of clothes, capsulating material choose the composition that can refer to the Garcinia Cambogia extract microcapsule.In outermost layer
Capsulating material can protect internal Garcinia Cambogia extract microcapsule to a certain degree, the extruding of the chewing, esophagus that avoid tooth makes
The Garcinia Cambogia extract microcapsule ruptures in advance, releases the gamboge berry extract included in advance.
In other possible embodiments, the Garcinia Cambogia extract microcapsule can also be using objects such as glutinous polysaccharide, gelatin
Matter, the substance of selection meet have it is certain water-soluble, there is no toxic side effect to human body or not by the feature of body metabolism, it is general and
Speech, will choose natural or synthetic high molecular material.The formation of the Garcinia Cambogia extract microcapsule can be in a manner of film forming, directly
Connect cladding gamboge berry extract.Either by molecule spraying, deposition in a manner of be attached on gamboge berry extract formed it is micro-
Capsule, further under the action of body fluid, the material part of attachment or all dissolution, disintegration expose internal Garcinia Cambogia and extract
Object.
Specifically, the composition A further includes the buffer salt for controlling pH value, the pH value range of the buffer salt control
Less than or equal to 7.In the present embodiment, the pH value range of the buffer salt control is less than 7, while preferably using carbonate-carbon
Sour hydrogen salt buffer system, be able to maintain the gamboge berry extract in Garcinia Cambogia extract microcapsule and release after certain time
Interior activity.The carbonate-bicarbonate buffer system of use can also avoid the normal of acid excessively high influence stomach in stomach
Work, additionally it is possible to neutralization gastric acid to a certain degree.But for having gastric ulcer, gastric perforation or the oral crowd for having gastric operation history,
Recommend to be applicable in the phosphate buffer substitution carbonate-bicarbonate buffer system.
Specifically, the composition A further includes the complexant for forming water-soluble complex with calcium ion.At this
In embodiment, the preferred sodium ethylene diamine tetracetate of complexant (referred to as " EDTA-Na ") is used as complexant.With the work of EDTA-Na
For, after the hydroxycitric acid is reacted with calcium oxalate, free calcium ion will be by the ethylenediamine tetra-acetic acid root in EDTA-Na
Capture forms Ca-EDTA (referred to as " EDTA-Ca ").The EDTA-Ca is more stable water soluble compound, energy
It is enough to be excreted with body fluid circulatory, and with metabolin.Free calcium ion is coordinated with ethylenediamine tetra-acetic acid root, it is impossible to
Oxalate combines, and forms calcium oxalate crystal again, is equivalent to the formation for inhibiting calcium oxalate.Meanwhile the combination degree of EDTA-Ca
Higher, calcium ion therein will be stablized by ethylenediamine tetra-acetic acid root to be captured, it is more difficult to re-form free state.
Specifically, the composition A can also include sweet flavor modifier, the sweet flavor modifier include glucose, fructose,
Aspartame it is one of or several.Sweet flavor modifier can give oral crowd preferably oral impression, and can give mouth
The psychology of the person's of clothes pleasure promotes oral person periodically to take composition A and reduce conflict sense.Meanwhile when the gamboge berry extract
Micro-capsule due to probability event such as defective workmanship or tooth touching and when rupturing, the sweet flavor modifier can reduce to a certain degree
The influence of hydroxycitric acid in gamboge berry extract mitigates tart flavour, bitter taste etc. and feels.
Specifically, the composition A can also include flavor improving agent, the flavor improving agent include fruity flavor and
Colorant.Fruity flavor can give oral person similar to water to oral smell or taste perception of the person similar to fruit, colorant
The visual experience of fruit.In the present embodiment, the fruity flavor can be described using essence such as apple, strawberry, banana, grapes
Colorant can use and lure the colorants such as red, amaranth, brilliant blue, lemon yellow, sunset yellow.The fruity flavor, colorant it
Between can be used in compounding.More specifically, the fruity flavor and colorant can be with the shapes of the Garcinia Cambogia extract microcapsule
Compounding is mixed at the material of micro-capsule, is formed together the micro-capsule of coating gamboge berry extract, and then simplify process, while being obtained preferable
Vision, smell and taste experience.
Embodiment 2
The present embodiment provides contain hydroxycitrate in the composition B, the composition B of a kind of oral dissolution calcinm oxalate calculus
Sour micro-capsule.Contain the hydroxycitric acid for accounting for the composition B mass percent 0.5% in the hydroxycitric acid micro-capsule.At it
In its possible embodiment, the hydroxycitric acid in the hydroxycitric acid micro-capsule account for the composition B 0.1%~
10%.It is further preferred that the hydroxycitric acid in the hydroxycitric acid micro-capsule account for the composition B 0.1%, 0.3%,
0.6%, 1%, 10%.Hydroxycitric acid can react with calcium oxalate crystals in vivo, and calcium oxalate crystals size is promoted to become
It is small until disappear, it is water-soluble that calcium oxalate crystals, which react the product to be formed with hydroxycitric acid,.The hydroxycitric acid by
In the presence of hydroxyl, the factors such as steric configuration, the electronic configuration of hydroxycitric acid are changed, the carboxylic acid group of hydroxycitric acid is de-
Go hydrionic trend stronger, thus hydroxycitric acid obtains stronger acid and dissociation capability.
In the present embodiment specifically, the orbicule that the micro-capsule is formed by sticking polysaccharide, the micro-capsule are coated with hydroxyl lemon
Lemon acid.Glutinous polysaccharide has certain water solubility, and after certain oral time, under acting in vivo, coated micro-capsule is gradually molten
Solution, releases hydroxycitric acid therein.
It in the present embodiment specifically, further include that water-soluble complex is formed with calcium ion in the composition B
Complexant, preferably asparatate is as the complexant being coordinated with free calcium ions in the present embodiment.The asparatate exists
While binding free ca ions, there is no toxic side effect under normal limitation to human body, have in conjunction with the asparagus amino-acid calcium of formation
There is certain water solubility, avoids that calculus deposition occurs again.In other possible embodiments, can also using other have with
Calcium ion is coordinated the substance to form water-soluble complex, such as partial amino-acid, hyaluronic acid.
It in the present embodiment specifically, further include carrier in the composition B, the carrier and hydroxycitric acid are with negative
Load relationship forms targeting body.Load relationship between the carrier and hydroxycitric acid can be selected including Electrostatic Absorption
Physical absorption, the chemisorption including forming coordinate bond or other chemical bonds, including coating, being imbedded in interior physics mode
Equal different modes load.The targeting body is gradually concentrated in the position or increase that expectation is concentrated during recycling in vivo
In concentration of privileged site, such as renal tubule, bile duct, urethra etc..
More specifically, the carrier selects at least one bio-compatible material of polysaccharide, protein, lipid.In this implementation
In example, the carrier selects lipid.Further specifically, the lipoid core that the lecithin that the carrier is selected in lipid is formed.Institute
Attraction can be generated and then generate combination by stating between lecithin and the hydroxycitric acid, hydroxycitric acid will be in lecithin institute shape
At will further be enriched in specified region under the load of lipoid core.Lecithin can also be built into phospholipid bilayer, and by portion
Divide hydroxycitric acid carboxyl to be exposed at outside bilayer, and then forms lecithin-hydroxycitric acid and target body.The present embodiment
In, ester, the part base of hydroxycitric acid can also can be formed with part of hydroxyl citric acid using the fatty acid in lipid, fatty acid
Group is exposed to formed fatty acid-hydroxycitric acid targeting body surface, and the fatty acid-hydroxycitric acid targeting body concentrates on
Specific region promotes the concentration of the hydroxycitric acid of specific region.
Further specifically, the partial size of the carrier is greater than or equal to 12 μm.In the present embodiment, the lecithin is formed
The partial size of lipoid core carrier be 12 μm, combining the lecithin of hydroxycitric acid-hydroxycitric acid targeting body partial size will also wait
In or greater than 12 μm.The partial size of the carrier is especially influenced due to the influence of body-internal-circulation by renal tubule circulation.?
In the present embodiment, the lecithin of lipoid core carrier and hydroxycitric acid and lipoid core the carrier formation formed with the lecithin
For rouge-hydroxycitric acid targeting body, lecithin of the partial size equal to 12 μm-hydroxycitric acid targeting body will be recycled in vivo
When up to renal tubule, due to renal tubule structural factor itself, lecithin-hydroxycitric acid targeting body more than or equal to 12 μm will be by
It intercepts and then is enriched in kidney region, target the hydroxycitrate that body loads thereon together with the lecithin-hydroxycitric acid is promoted
Concentration of the acid in kidney region.Therefore, hydroxycitric acid can targetedly dissolve calcium oxalate crystals in kidney region.Pass through
The partial size of the carrier is controlled, and then controls and targets body partial size, the structure circulated through in combination, tissue can be intercepted, be stayed
The targeting body is deposited, further promotes hydroxycitric acid in the effective concentration in specified region.
Embodiment 3
The present embodiment provides include hydroxyl lemon in the composition C, the composition C of a kind of oral dissolution calcinm oxalate calculus
The hydroxycitrate derivatives micro-capsule of lemon acid derivative, hydroxycitrate derivatives folding in the hydroxycitrate derivatives micro-capsule
Calculate is that mass percent accounts for the 1% of composition C.In other possible embodiments, the hydroxycitrate derivatives micro-capsule
In hydroxycitrate derivatives account for the 0.1%~10% of the composition C.It is further preferred that the hydroxycitric acid spreads out
Hydroxycitrate derivatives in biological microcapsule account for 0.1%, 0.3%, 0.6%, 1%, the 10% of the composition C.
Specifically, in the present embodiment, the hydroxycitrate derivatives micro-capsule is made of gelatin, the hydroxycitric acid
Derivative micro-capsule is the orbicule for being coated with the gamboge berry extract.It is micro- comprising multiple hydroxycitrate derivatives in composition C
Capsule, multiple hydroxycitrate derivatives micro-capsules are evenly distributed in composition C.
Specifically in the present embodiment, the lactone that the hydroxycitrate derivatives are formed using hydroxycitric acid is derivative
Object.Contain 3 carboxylic acid groups and a hydroxyl group in hydroxycitric acid, does not need additionally to add between carboxylic acid group and hydroxyl
Add reactant, esterification can occur, further decreases the energy of hydroxycitric acid itself, therefore the lactone of hydroxycitric acid
Derivative is more stable, can keep stability to a certain degree, avoids being oxidized during absorbing, transporting.Make playing
Used time, since esterification has invertibity, the lactone derivatives of hydroxycitric acid can generate hydroxycitrate under water environment
Acid.Hydroxycitric acid further dissolves calcium oxalate crystals, while still there are two carboxyl bases on the lactone derivatives of hydroxycitric acid
Group, can react with calcium oxalate crystals, dissolve calcium oxalate crystals.
In other possible embodiments, the hydroxycitrate derivatives can select hydroxycitric acid to contain with other
The ester type compound for thering is hydroxyl group compound to be formed.Hydroxycitrate derivatives can also be the salt that hydroxycitric acid is formed,
Such as hydroxycitrate acid potassium salt, hydroxycitrate acid sodium-salt can also form stability more preferably double salt.Hydroxycitrate derivatives
It can also be the compound for continuing to add hydroxyl or other groups or branch on hydroxycitric acid main chain, to enhance hydroxycitrate
Stability, the acidity of acid derivative reduce toxicity, irritation, and convenient for preferably application, leniently dissolution calcium oxalate is brilliant in vivo
Body.
It specifically, in the present embodiment, further include that targeting is formed in conjunction with hydroxycitrate derivatives in the composition C
The carrier of body.The carrier and hydroxycitrate derivatives by modes such as absorption, electrostatic force, chemical bond, physics claddings in conjunction with.
More specifically, the carrier can use protein or polysaccharide, the protein may include the peptide of small molecule
Chain or glycoprotein, the polysaccharide can choose alkyl glycosides as carrier.The alkyl glycosides is as carrier in conjunction with the hydroxyl
Base citric acid derivant forms alkyl glycosides-hydroxycitric acid and targets body, is further enriched in specified region, promotes hydroxycitrate
The effective concentration of acid derivative.
Embodiment 4
In performance test, take composition A in embodiment 1 as subjects, in order to test repeatability with
And convenient displaying, it will be tested and be shown with drosophila.
Food one week of female Drosophila nursing containing 0.1% sodium oxalate is had, whether is the renal tubule in sampling observation drosophila
Form calculus.The drosophila for there are a large amount of calculus is transferred in the diet environment containing composition A, is raised micro- after a week
There are situations for calculus in observation drosophila renal tubule.
The drosophila renal tubule calculus micrograph of food one week containing 0.1% sodium oxalate is illustrated in Fig. 1, it can be with from Fig. 1
Find out in drosophila renal tubule full of calcium oxalate crystals (namely calcinm oxalate calculus).Referring to FIG. 2, renal tubule is brilliant full of calcium oxalate
The drosophila of body the diet environment containing composition A after a week, it can be observed how drosophila renal tubule calcium oxalate crystal growth in healthy crystal is bright
Aobvious dissolution, does not observe the calcium oxalate crystals for hindering to circulate in renal tubule within sweep of the eye.
Validity for Garcinia Cambogia extract microcapsule in verifying composition A adjusts Garcinia Cambogia on the basis of composition A
The ratio of extract, design gamboge berry extract accounts for the composition A-1 that composition quality percentage is 0.1% and Garcinia Cambogia mentions
Object is taken to account for the composition A-2 that composition quality percentage is 0.5%.Drosophila of the renal tubule full of calcium oxalate crystals is containing combination
The diet environment of object A-1 after a week, dissection micrograph such as Fig. 3 of renal tubule, it is seen that renal tubule calcium oxalate crystal growth in healthy crystal is obvious
There is ablation sign, but still has the presence of more calcium oxalate crystals.
Renal tubule full of calcium oxalate crystals drosophila the diet environment containing composition A-2 after a week, renal tubule
Dissection micrograph such as Fig. 4, it is seen that renal tubule calcium oxalate crystal growth in healthy crystal dissolves substantially, and calcium oxalate crystals substantially can not in field range
See.
The performance test results of composition A, composition A-1, composition A-2 and control group are aggregated into Fig. 5, in Fig. 5
Abscissa is gamboge berry extract (GCE) mass percent, and ordinate is that (unit is (calcium oxalate crystal) calculus region area
104Square micron).Fig. 5 shows that calculus region area is reduced with Garcinia Cambogia extract quality percentage increase in composition,
And it can prove that there is phase between composition (including composition A, composition A-1, composition A-2) and the variation of calculus region area
Guan Xing.
Embodiment 5
To continue to verify effective component --- the effect of hydroxycitric acid in Garcinia Cambogia extract microcapsule, concentration is selected
1% hydroxycitrate acid solution impregnates the in vitro drosophila renal tubule for being full of calcium oxalate crystal.The renal tubule is taken to containing
Food one week drosophila renal tubule of 0.1% sodium oxalate.Microexamination confirmation renal tubule is full of calcium oxalate crystals from Fig. 6.
Hydroxycitrate acid solution through over-richness 1% impregnates the renal tubule of 20min see Fig. 7, the oxalic acid of the renal tubule
There is preliminarily solubilised in calcium crystal, that is, has the phenomenon that small area dissolution.
Hydroxycitrate acid solution through over-richness 1% impregnates the renal tubule of 40min see Fig. 8, the oxalic acid of the renal tubule
There is obvious dissolution in calcium crystal, that is, has the tendency that larger area dissolution.
Hydroxycitrate acid solution through over-richness 1% impregnates the renal tubule of 60min see Fig. 9, and grass occurs in the renal tubule
The phenomenon that sour calcium dissolution of crystals is more and calcium oxalate crystals area is obviously reduced.
Hydroxycitrate acid solution through over-richness 1% impregnates the renal tubule of 100min see Figure 10, the grass of the renal tubule
Sour calcium crystal dissolves substantially, only exists the phenomenon of small area calcium oxalate crystals remnants.
Hydroxycitrate acid solution through over-richness 1% impregnates the renal tubule of 120min see Figure 11, the grass of the renal tubule
Sour calcium crystal all dissolves, and renal tubule is completely unimpeded.
The hydroxycitrate acid solution of above-mentioned concentration 1% impregnates the experimental result full of calcium oxalate crystal renal tubule experimental group and converges
In order to which the hydroxycitrate acid solution of reduced concentration 1% impregnates effect in total visible Figure 12, Figure 12, control group, control group are also added
Hydroxycitrate acid solutions be 0.5%, soaking time be grouped reference experiment group.The abscissa of Figure 12 is that soaking time is (single
Position is minute), ordinate is (calcium oxalate crystal) calculus region area percentage.Trend as can be seen from Fig. 12, when with impregnating
Between growth, calculus region area percentage is remarkably decreased.Hydroxycitrate acid solutions are higher, calculus region area percentage
Decrease speed is also accelerated.Experiment involved in Figure 12 also added the control experiment using 2%GCE (gamboge berry extract),
It is grouped with soaking time 0~160 in 9 groups of constituted experiments, calcium oxalate crystal area does not reduce, it was demonstrated that GCE cannot pass through
Direct interaction in vitro.Illustrate that gamboge berry extract can work by oral way in conjunction with other above-mentioned experimental groups, embodiment.
Result of performance test it can be found that composition in the present invention due to containing Garcinia Cambogia extract microcapsule, hydroxyl lemon
Lemon acid or hydroxycitrate derivatives micro-capsule can realize effectively dissolution for calculus is formed by calcium oxalate crystal.The gamboge
The material selection high-molecular organic material of berry extract micro-capsule, hydroxycitric acid or hydroxycitrate derivatives micro-capsule has one
Fixed solubility can protect the effective component in composition to reach and efficiently inhale convenient for the time of control composition disintegration, dissolution
The position of receipts.Further, also addition control pH value is less than or equal to 7 buffer salt in the composition, adds buffer salt body
System can protect the effective component of composition, and reduction is oxidized, and keep effective state.Further, in the composition also
Be added to can with calcium ion formed soluble complex complexant, the complexant can stable bond hydroxycitric acid with
The calcium ion of calcium oxalate reaction dissolution, and water-soluble complexes are formed, avoid calcium ion and oxalate denominationby from occurring again instead
Precipitating should be formed, and the direction for forcing reaction to be dissociated to calcium oxalate crystals is mobile.
The present invention also provides the hydroxycitrate derivatives that can play similar or stronger dissolution with hydroxycitric acid,
Hydroxycitrate derivatives exist in the form of more stable (low entropy value).It, can also be according to oral if forms such as forming salt, double salt
The type of the state selection cation of person, has broader practice prospect.Further, further include in the composition and hydroxyl
Base citric acid or hydroxycitrate derivatives form the carrier of targeting body, and the carrier can be by itself distinctive physical property
Or chemical property drives the hydroxycitric acid or hydroxycitrate derivatives, is lifted at the hydroxycitric acid or hydroxyl of privileged site
Base citric acid derivant effective concentration.It, can also be with it is worth noting that, add the composition to be formed with Garcinia Cambogia form of extract
With reference to carrier is used, the hydroxycitric acid or hydroxycitrate derivatives effective concentration of targeting moiety are promoted.Further, originally
Invention is according to the property and site of action of hydroxycitric acid or hydroxycitrate derivatives, it is preferred to use polysaccharide, protein, rouge
The carriers such as matter realize the purpose that targeting body is formed with hydroxycitric acid or hydroxycitrate derivatives.Further, the present invention is logical
Limitation diameter of carrier is crossed, hydroxycitric acid or hydroxycitrate derivatives is actually limited and targeting body is collectively formed in carrier
Partial size, and then by the characteristic of body-internal-circulation, the targeting body is limited in renal tubule, can effectively promote hydroxycitric acid or hydroxyl
Effective concentration of the base citric acid derivant in renal tubule region.In order to improve the sensory experience and psychological feelings of oral person, this
Also by way of adding sweet flavor modifier, flavor improving agent into composition, improve composition takes experience for invention.Sweet taste
Modifying agent by glucose, fructose, Aspartame etc., can improve part of hydroxyl citric acid or hydroxycitrate derivatives micro-capsule,
Garcinia Cambogia extract microcapsule is due to the sensory experience that accidental cause ruptures and influences.Flavor improving agent passes through fruity flavor, coloring
Agent etc. can provide the visual experience of similar fruit when oral person takes.The introducing of sweet taste, color can also improve oral
The experience of person mitigates the psychological pressure of oral person.
The above is only some embodiments of the invention, it is noted that for the ordinary skill people of the art
For member, various improvements and modifications may be made without departing from the principle of the present invention, these improvements and modifications are also answered
It is considered as protection scope of the present invention.
Claims (8)
1. a kind of composition of oral dissolution calcinm oxalate calculus, which is characterized in that the composition includes 0.1%~10% rattan
Yellow fruit extract microcapsule；Or 0.1%~10% hydroxycitric acid or hydroxycitrate derivatives micro-capsule.
2. the composition of oral dissolution calcinm oxalate calculus according to claim 1, which is characterized in that the micro-capsule is selected fine
At least one of dimension element, glutinous polysaccharide, gelatin material is made.
3. the composition of oral dissolution calcinm oxalate calculus according to claim 1, which is characterized in that the composition also wraps
The pH value range for including control is less than or equal to 7 buffer salt, and/or for forming matching for water-soluble complex with calcium ion
Position agent.
4. the composition of oral dissolution calcinm oxalate calculus according to claim 1, which is characterized in that the hydroxycitric acid
Derivative include by the derivative obtained ester type compound of hydroxycitric acid or citric acid, lactone compound, salt, double salt at least
A kind of compound.
5. the composition of oral dissolution calcinm oxalate calculus according to claim 1, which is characterized in that in the composition also
Carrier including forming targeting body in conjunction with hydroxycitric acid or hydroxycitrate derivatives.
6. the composition of oral dissolution calcinm oxalate calculus according to claim 5, which is characterized in that the carrier is using more
At least one of sugar, protein, lipid bio-compatible material are made.
7. the composition of oral dissolution calcinm oxalate calculus according to claim 5, which is characterized in that the partial size of the carrier
For more than or equal to 12 μm.
8. the composition of oral dissolution calcinm oxalate calculus according to claim 1, which is characterized in that the composition includes
Sweet flavor modifier and/or flavor improving agent；The sweet flavor modifier includes at least one of glucose, fructose, Aspartame；
The flavor improving agent includes fruity flavor and/or colorant.
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| Publication number | Priority date | Publication date | Assignee | Title |
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| CN113750186A (en) * | 2020-06-03 | 2021-12-07 | 中山大学孙逸仙纪念医院 | A formula containing hydroxycitric acid extract for preventing and treating renal calculus |
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