CN106029218A - Orally administered medical adsorbent with increased strength - Google Patents
Orally administered medical adsorbent with increased strength Download PDFInfo
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- CN106029218A CN106029218A CN201480075093.2A CN201480075093A CN106029218A CN 106029218 A CN106029218 A CN 106029218A CN 201480075093 A CN201480075093 A CN 201480075093A CN 106029218 A CN106029218 A CN 106029218A
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/141—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
- A61K9/143—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with inorganic compounds
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K33/00—Medicinal preparations containing inorganic active ingredients
- A61K33/44—Elemental carbon, e.g. charcoal, carbon black
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- B—PERFORMING OPERATIONS; TRANSPORTING
- B01—PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL
- B01J—CHEMICAL OR PHYSICAL PROCESSES, e.g. CATALYSIS OR COLLOID CHEMISTRY; THEIR RELEVANT APPARATUS
- B01J20/00—Solid sorbent compositions or filter aid compositions; Sorbents for chromatography; Processes for preparing, regenerating or reactivating thereof
- B01J20/02—Solid sorbent compositions or filter aid compositions; Sorbents for chromatography; Processes for preparing, regenerating or reactivating thereof comprising inorganic material
- B01J20/20—Solid sorbent compositions or filter aid compositions; Sorbents for chromatography; Processes for preparing, regenerating or reactivating thereof comprising inorganic material comprising free carbon; comprising carbon obtained by carbonising processes
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- B01—PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL
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- B01J20/00—Solid sorbent compositions or filter aid compositions; Sorbents for chromatography; Processes for preparing, regenerating or reactivating thereof
- B01J20/28—Solid sorbent compositions or filter aid compositions; Sorbents for chromatography; Processes for preparing, regenerating or reactivating thereof characterised by their form or physical properties
- B01J20/28002—Solid sorbent compositions or filter aid compositions; Sorbents for chromatography; Processes for preparing, regenerating or reactivating thereof characterised by their form or physical properties characterised by their physical properties
- B01J20/28011—Other properties, e.g. density, crush strength
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- B—PERFORMING OPERATIONS; TRANSPORTING
- B01—PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL
- B01J—CHEMICAL OR PHYSICAL PROCESSES, e.g. CATALYSIS OR COLLOID CHEMISTRY; THEIR RELEVANT APPARATUS
- B01J20/00—Solid sorbent compositions or filter aid compositions; Sorbents for chromatography; Processes for preparing, regenerating or reactivating thereof
- B01J20/28—Solid sorbent compositions or filter aid compositions; Sorbents for chromatography; Processes for preparing, regenerating or reactivating thereof characterised by their form or physical properties
- B01J20/28054—Solid sorbent compositions or filter aid compositions; Sorbents for chromatography; Processes for preparing, regenerating or reactivating thereof characterised by their form or physical properties characterised by their surface properties or porosity
- B01J20/28069—Pore volume, e.g. total pore volume, mesopore volume, micropore volume
- B01J20/28071—Pore volume, e.g. total pore volume, mesopore volume, micropore volume being less than 0.5 ml/g
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- B01—PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL
- B01J—CHEMICAL OR PHYSICAL PROCESSES, e.g. CATALYSIS OR COLLOID CHEMISTRY; THEIR RELEVANT APPARATUS
- B01J20/00—Solid sorbent compositions or filter aid compositions; Sorbents for chromatography; Processes for preparing, regenerating or reactivating thereof
- B01J20/28—Solid sorbent compositions or filter aid compositions; Sorbents for chromatography; Processes for preparing, regenerating or reactivating thereof characterised by their form or physical properties
- B01J20/28054—Solid sorbent compositions or filter aid compositions; Sorbents for chromatography; Processes for preparing, regenerating or reactivating thereof characterised by their form or physical properties characterised by their surface properties or porosity
- B01J20/28078—Pore diameter
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- B—PERFORMING OPERATIONS; TRANSPORTING
- B01—PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL
- B01J—CHEMICAL OR PHYSICAL PROCESSES, e.g. CATALYSIS OR COLLOID CHEMISTRY; THEIR RELEVANT APPARATUS
- B01J20/00—Solid sorbent compositions or filter aid compositions; Sorbents for chromatography; Processes for preparing, regenerating or reactivating thereof
- B01J20/28—Solid sorbent compositions or filter aid compositions; Sorbents for chromatography; Processes for preparing, regenerating or reactivating thereof characterised by their form or physical properties
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- B01J20/28083—Pore diameter being in the range 2-50 nm, i.e. mesopores
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- B—PERFORMING OPERATIONS; TRANSPORTING
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- B01J—CHEMICAL OR PHYSICAL PROCESSES, e.g. CATALYSIS OR COLLOID CHEMISTRY; THEIR RELEVANT APPARATUS
- B01J20/00—Solid sorbent compositions or filter aid compositions; Sorbents for chromatography; Processes for preparing, regenerating or reactivating thereof
- B01J20/28—Solid sorbent compositions or filter aid compositions; Sorbents for chromatography; Processes for preparing, regenerating or reactivating thereof characterised by their form or physical properties
- B01J20/28054—Solid sorbent compositions or filter aid compositions; Sorbents for chromatography; Processes for preparing, regenerating or reactivating thereof characterised by their form or physical properties characterised by their surface properties or porosity
- B01J20/28078—Pore diameter
- B01J20/28085—Pore diameter being more than 50 nm, i.e. macropores
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Abstract
The present invention relates to an orally administered medical adsorbent, and more specifically, to an orally administered medical adsorbent with increased strength, comprising porous activated carbon. An orally administered medical adsorbent comprising porous activated carbon by using a spherical furan resin as a carbon source, according to the present invention, can maximize the adsorption of indole, which is one among uremic toxins present in the body of a patient, and can maximize the selective adsorption for uremic toxins, on the basis of a new fact which has not been hitherto known in the relevant art.
Description
Technical field
The present invention relates to a kind of oral type medical adsorbent, relate more specifically to a kind of porous increased by intensity and live
Property charcoal composition oral type medical adsorbent.
Background technology
For the defect patient of renal function or liver function, along with their organ function obstacle, in blood etc.
Internal can pile up or generate harmful toxicant, thus cause the brain diseases such as uremia or disturbance of consciousness.These patient's numbers
Amount presents the trend of annual growth, therefore, substitutes defect internal organs and possesses the dirty of the function that can be excreted by toxicant
Device make-shift equipment or medicine be developed into important topic.At present, as artificial kidney, the most widely available mode is to borrow
Help the noxious substance removing method of hemodialysis.But, this hemodialysis type artificial kidney influential point of viscera utilizes special device, because of
This, for the consideration of safety management, need to put into professional and technical personnel, and for patient, the vitro extraction of blood deposited
In shortcomings such as high burdens animally, mentally and economically, it is difficult to satisfactory.
As the method solving this shortcoming, developing and using orally available and that kidney or liver can be treated function to hinder
The oral adsorbent agent hindered.The oral adsorbent agent being made up of surface modified spherical activated carbon, the generally delay in upper small intestine pipe
Time is 3-5 hour.It is therefore preferred that use contact with harmful substance after about 3 hours interior absorbabilitys height and initially inhaling
The surface modified spherical activated carbon of attached excellent performance.
Add, the most promptly adsorb and the toxicant of removing in body is the most important, but noxious substance is showed
Outstanding adsorptivity, and the few selection adsorption rate of the adsorbance of enteral beneficiating ingredient is the most critically important.Digest at stomach, small intestinal etc.
Pipeline exists the indispensable compound of the physiological functions such as sugar, protein and the enzyme etc. from intestinal wall secretion, forms many kinds of substance
The environment being mixed in.It is therefore desirable to a kind of absorption that both can suppress the compound indispensable for physiological function, having again can
Adsorb the medicinal carbon of the selection adsorption rate of uremic reason material.
Korean published Patent 10-2004-0032320 as relating to the invention of a kind of oral type adsorbent, note
Having carried a kind of oral type adsorbent, it more than or equal to 0.04mL/g and is less than 0.10mL/g's at the pore volume of 20-15000nm
Select adsorption rate high in particular range.
Further, in Korean published Patent the 10-2005-0039592nd, record and adsorbed by oral adsorbent agent
The amount of harmful substance, its 7.5～15000nm pore volume more than or equal to 0.25mL/g region in increase, and not with
The increase of specific surface area shows dependency relation.
This be due to existing oral type adsorbent mainly using petroleum-type Colophonium as carbon source, historically in above-mentioned existing
The invention of document, is difficult to develop the oral type medical adsorbent with more careful and effective selection adsorption rate.
Especially, the disclosed product as existing oral type medical adsorbent, it makes powder and takes, and existing
In the case of some porous activated carbons, owing to compressive strength is significantly low, therefore, turn to curable type unit dose to preparation
, such as, in the case of being filled into capsule, there is the problem that activated carbon is pulverized the most in the filling process in type.I.e., so far,
The relevant absorption affinity of adsorption rate and specific uremic material (such as, benzazolyl compounds) is selected as it has been described above, only focus be placed on
Increase and development technique, therefore, relate generally to the minute aperture diameter of activated carbon and volume, specific surface area or tortuosity ratio are relevant grinds
Study carefully, and be not conceived to thus cause the significantly reduced problem of compressive strength of ball shape active carbon itself and attempt to improve asking accordingly
Topic.
But, a dose of oral adsorbent agent is close to number g, therefore, in the case of it being taken in powder mode, many
The inconvenience brought of taking medicine such as induction vomiting, therefore, in actual drug administration process, use the auxiliary such as oblate sphere (Oblate) at present
Means complete to take.
Therefore, though the necessity of the unit curable type preparation for dispensing convenience can be greatly improved is big, but as it has been described above, by
Low in the compressive strength of activated carbon itself, it is therefore contemplated that the most still not met the demand.
To this, the present inventor, during research oral type medical adsorbent, finds oral type medical adsorbent
General knowledge and the limitation of prior art can be surmounted, up-to-date can develop, this completes the present invention.Especially, root of the present invention
According to prior art, only focus on increase and select adsorption rate or increase indole absorption affinity, and for choosing both can be increased
Select the method that adsorption rate can increase again indole absorption affinity, there is no any report, be conceived to this situation, it is provided that one is the fullest
Foot selects adsorption rate and the up-to-date oral type medical adsorbent of indole absorption affinity.Further, this selection adsorption rate and Yin are increased
While diindyl absorption affinity, according to the porous activated carbon of the present invention, compared to existing ball shape active carbon, have the highest strong
Degree, thus, acts not only as powder and is put into, it is also possible to be filled into capsule, it is achieved oral.
Summary of the invention
Solve the technical problem that
It is an object of the invention to provide the pharmaceutical absorption of oral type that a kind of porous activated carbon increased by intensity forms
Agent.
Technical scheme
To achieve these goals, the oral type that the present invention provides the porous activated carbon increased by intensity to form is pharmaceutical
Adsorbent.
Invention effect
According to the present invention, intensity the oral type medical adsorbent that the porous activated carbon increased forms is based on existing
The undocumented up-to-date fact in some industry, can make indole absorption affinity and indole adsorption rate maximize, meanwhile, can make uremic
Material is relevant selects adsorption rate to maximize.Further, owing to having the intensity more than or equal to 10N/sphere, it is possible not only to improve system
Make earning rate, it is also possible to solve in the problem manufactured and in the process of circulation, the shape of activated carbon is pulverized.Further, strong by improving
Degree, can suppress electrostatic, and prevent the pollution of produced ball shape active carbon caused by foreign body in process for making.Commercially available
In the case of preparation, because producing electrostatic, ball shape active carbon can be sticked when taking, discomfort when taking can be caused, and contrary
Ground, the ball shape active carbon of the present invention can suppress the generation of electrostatic, thus have and improve the effect taking convenience.
Detailed description of the invention
Below, will be explained in the present invention.
The medicinal adsorbent of the oral type that the porous activated carbon that present invention offer is increased by intensity forms.
The porous activated carbon that intensity according to the present invention increases, its mean diameter is 0.1 to 0.5mm, preferably 0.3 to
0.4mm。
The porous activated carbon that intensity according to the present invention increases, the pore volume of its hole diameter 7.5～15000nm is
More than or equal to 0.01mL/g and less than 0.10mL/g, it is more preferably, greater than equal to 0.03mL/g and less than 0.08mL/g.
To this, in Korean Patent publication the 10-2005-0039592nd, disclose oral type adsorbent, its feature
Being, mean diameter be 0.01mm to 1mm, the pore volume of hole diameter 7.5～15000nm is 0.25 to 1.0mL/g, and
And be made up of surface modified spherical activated carbon.In the above documents, the absorbability of oral adsorbent agent, i.e. oral adsorbent agent is inhaled
The amount of attached harmful substance increases in above-mentioned pore volume is more than or equal to the region of 0.25mL/g, and not with the increasing of specific surface area
Add and show dependency relation, compared to selecting adsorption rate, be more concerned with how to increase the adsorbance of harmful substance.
But, according to the research of the present inventor, it is different from the record of above-mentioned document, according to being increased by intensity of the present invention
The medicinal adsorbent of the oral type of porous activated carbon composition, the pore volume of hole diameter 7.5～15000nm is for being more than or equal to
0.01mL/g and less than 0.10mL/g, it is highly preferred that more than or equal to 0.03mL/g and less than 0.08mL/g in obtain indole and inhale
The result that attached power and indole adsorption rate increase.
Thus, according to the present invention by the oral type doctor that spherical furane resins are formed as the porous activated carbon of carbon source
Medicinal adsorbent, the pore volume of its hole diameter 7.5～15000nm is more than or equal to 0.01mL/g and less than 0.10mL/g model
Enclose the maximizing adsorption of the interior indole that can make as uremic material.
The porous activated carbon that intensity according to the present invention increases, the pore volume of its hole diameter 20～15000nm is
More than or equal to 0.005mL/g and less than 0.04mL/g, it is highly preferred that pore volume is more than or equal to 0.01mL/g and to be less than
0.03mL/g。
To this, in Korean Patent publication the 10-2004-0032320th, disclosing oral type adsorbent, it is special
Levy and be, the pore volume of a diameter of 0.01 to 1mm, hole diameter 20～15000nm be more than or equal to 0.04mL/g and little
Porous spherical carbonaceous substance in 0.10mL/g forms.In the above documents, the pore volume of hole diameter 20～15000nm exists
Showing outstanding selection adsorption rate more than or equal to 0.04mL/g and less than in the range of 0.10mL/g, above-mentioned pore volume is greatly
In equal to 0.05mL/g and less than showing more excellent selection adsorption rate in the range of 0.10mL/g.
But, according to an example of the present invention, it is known that the mouth that the porous activated carbon increased by intensity in the present invention forms
In the case of taking type medical adsorbent, the pore volume of hole diameter 20～15000nm is more than or equal to 0.005mL/g and little
In the range of 0.04mL/g, it is highly preferred that more than or equal to 0.01mL/g and less than in the range of 0.03mL/g, it selects adsorption rate
Increase.
That is, intensity the medicinal adsorbent of the oral type that the porous activated carbon increased of the present invention forms, is different from existing
Some technology general knowledge, when the pore volume meeting hole diameter 7.5～15000nm is more than or equal to 0.01mL/g and to be less than
0.10mL/g, the pore volume of hole diameter 20～15000nm is more than or equal to 0.005mL/g and the condition less than 0.04mL/g
Time, while selecting adsorption rate to increase, indole absorption affinity and adsorption rate also can increase simultaneously, by confirming this up-to-date thing
Real, thus complete the present invention.
In the present invention, the porous activated carbon that intensity increases refers to, minimum have the pressure more than or equal to 10N/sphere
The porous activated carbon of contracting intensity.The intensity of the porous activated carbon of the present invention, compared to the intensity of existing activated carbon, has
Minimum 2 times～the intensity of maximum 10 times.The porous activated carbon that the intensity of the present invention increases can come using furane resins as carbon source
Preparation.
The porous activated carbon that intensity according to the present invention increases, its quantity of alkali consumption can be 0.1～1.0mmol/g, acid
Consumption can be 0.3～1.0mmol/g.
In sum, the oral type medical adsorbent of the present invention, the pore volume of its hole diameter 7.5～15000nm
For more than or equal to 0.01mL/g and less than 0.10mL/g, it is highly preferred that pore volume is for more than or equal to 0.03mL/g and be less than
0.08mL/g, the pore volume of hole diameter 20～15000nm is more than or equal to 0.005mL/g and less than 0.04mL/g, more excellent
Selection of land, pore volume is more than or equal to 0.01mL/g and less than 0.03mL/g, is more than or equal to 10N/sphere in compressive strength
In the case of, optimized uremic material can be played and remove function.
Oral type medical adsorbent according to the present invention, it selects adsorption rate to be more than or equal to 3.0.
Oral type medical adsorbent according to the present invention, its indole initial adsorption rate is more than or equal to 80%.
The oral type medical adsorbent of the present invention can be used for selecting free chronic renal failure, acute renal failure,
Chronic pyelonephritis, acute pyelonephritis, chronic nephritis, acute nephritic syndrome, rapidly progressive nephritic syndrome, chronic nephritis are combined
Before simulator sickness, nephrotic syndrome, interstitial nephritis, lipoid nephrosis, diabetic nephropathy, pipe hypertension of having a guilty conscience or dialysis
Slight renal insufficiency, chronic hepatitis, alcoholic liver, liver cirrhosis, hepatitis interstitialis chronica, medicament anaphylaxis hepatopathy or primary biliary liver
The prevention of at least one the above disease in the group of cirrhosis composition or treatment, as long as passed through by oral type medical adsorbent
Uremic material is adsorbed the disease improved or treat, is then not particularly limited in above-mentioned disease.
Each physics value that the surface modified spherical activated carbon used as oral type adsorbent of the present invention is had, i.e.
Mean diameter, specific surface area, pore volume, acid consumption, quantity of alkali consumption, selection adsorption rate and intensity are carried out as follows
Measure.
(1) mean diameter
(Sympatec company manufactures, HELOS Particle to use laser diffraction formula particle size distribution granulometry device
Size Analysis), the granularity formulating dimension criteria adds up line chart, will be equivalent to Volume's Mean Diameter (VMD)
Particle diameter is as mean diameter.
(2) specific surface area (by the computational methods of BET method)
Use the specific surface area measuring instrument (MICROMERITICS company manufactures, ASAP 2420) by gas adsorption method,
Measure the gas absorption amount of ball shape active carbon, calculate specific surface area according to BET formula.
Specifically, ball shape active carbon is filled to test tube, carries out under the conditions of 300 DEG C reducing pressure and being dried, and gravimetry.
Test tube is cooled to-196 DEG C, introduces nitrogen and make N2 adsorption to ball shape active carbon, measuring the relation (absorption of nitrogen partial pressure and adsorbance
Isothermal line).Test tube is returned to room temperature, uses thermal conductivity detector that the nitrogen quantity departed from from ball shape active carbon is measured also
As gas absorption amount (v).
Use the approximate expression derived from BET formula
Vm=1/{v × (1-x) },
V is obtained about 1 method (relative pressure x=0.3) of N2 adsorption by liquid nitrogen temperaturem(m2/ g), and by next
Individual formula specific surface area=4.35 × vm and calculate the specific surface area of ball shape active carbon.In above-mentioned each calculating formula, v is actual measurement
Gas absorption amount (m2/ g), x is relative pressure.
(3) by the pore volume of mercury injection method
Use hydrargyrum porosity apparatus (porosimeter) (MICROMERITICS company manufactures, AUTOPORE IV 9500)
Measure pore volume.Ball shape active carbon is put into test portion container, deaerates 30 minutes.Hydrargyrum is imported test portion container, slowly pressurizes,
Hydrargyrum is pressed into the pore of ball shape active carbon.Intrusion relation according to pressure now and hydrargyrum, uses following each calculating formula, measures
The pore volume distribution of ball shape active carbon test portion.
Specifically, at minimum pressure 0.5psia to maximum pressure 61, in the range of 000psia, to being pressed into spheric active
The volume of the hydrargyrum of charcoal is measured.Calculating about hole diameter, presses with pressure (P) in the cylindrical shape pore to diameter (D)
In the case of entering hydrargyrum, the surface tension of hydrargyrum is set to " γ ", and hydrargyrum is set to " θ ", from surface tension and effect with the contact angle of air vent wall
In the equilibrium of the pressure of pore section, following formula is set up ,-π D γ cos θ=π (D/2)2×P.Thus, D=(-4 γ cos θ)/P.
The surface tension of hydrargyrum be the contact angle of 485dynes/cm, hydrargyrum and carbon be 130 °, pressure P is psia, hole diameter D
Represent with μm, by following formula D=180.8/P, obtain pressure P and the relation of hole diameter D.
Such as, in the present invention, the pore volume of hole diameter 7.5～15000nm scope, be equivalent to hydrargyrum press-in pressure from
12.05psia is pressed into the volume of the hydrargyrum of 24106.6psia.
(4) acid consumption
Ball shape active carbon 1.0g is put into 100mL beaker, adds acid consumptive use hydrochloric acid test solution 50mL, 37 ± 1 DEG C of conditions
Lower use agitator vibrates 24 hours.At room temperature filter the content of beaker, gather above-mentioned solution 20mL as test fluid, drip
Determine 0.1mol/L potassium hydroxide solution.(indicator: bromophenol blueness test fluid 2) in this way carries out blank assay complete
Become correction.Acid consumption is calculated by following formula.
0.1mol/L potassium hydroxide consumption (mL) of A: test fluid
0.1mol/L potassium hydroxide consumption (mL) of B: blank assay liquid
The amount (g) of C: test portion
The factor of f:0.1mol/L potassium hydroxide
(5) quantity of alkali consumption
Ball shape active carbon 1.0g is put into 100mL beaker, adds alkali consumptive use hydrochloric acid test solution 50mL, 37 ± 1 DEG C of conditions
Lower use agitator vibrates 24 hours.At room temperature filter the content of beaker, gather above-mentioned solution 20mL as test fluid, drip
Determine 0.1mol/L hydrochloric acid.(indicator: phenolphthalein test solution 2) in this way carries out blank assay and completes correction.Pass through following formula
Calculate quantity of alkali consumption.
0.1mol/L salt acid consumption (mL) of A: test fluid
0.1mol/L salt acid consumption (mL) of B: blank assay liquid
The amount (g) of C: test portion
The factor of f:0.1mol/L hydrochloric acid
(6) adsorption rate is selected
Adsorption rate is selected to calculate as follows.
The dried porous ball shape active carbon 2.5g according to the present invention is put into 100mL beaker, adds DL-beta-amino
The pH 7.4 phosphate buffer 50mL of isopropylformic acid. 100mg/L concentration uses agitator to vibrate under the conditions of 37 ± 1 DEG C 24 hours.
(stock solution), vibrates 3 hours with 200rpm under the conditions of 37 ± 1 DEG C.As test fluid after filtration beaker contents, according to Japanese medicine
Allusion quotation ordinary test method organic body carbon test method(s), after measuring organic body carbon, the remnants calculating DL-B-AIB according to following formula are dense
Degree.
The organism carbon amounts of Tt: test fluid
The organism carbon amounts of Ts: titer (stock solution)
Dried ball shape active carbon 2.5g is put into 100mL beaker, adds the pH 7.4 of α-amylase 100mg/L concentration
Phosphate buffer 50mL (stock solution), vibrates 3 hours with 200rpm under the conditions of 37 ± 1 DEG C.Filter with 0.65 μm film filter
As test fluid after beaker contents, using pH 7.4 phosphate buffer as comparison, according to UV visual portion absorbance measurement
Method, measures the absorbance in wavelength 282nm, calculates the residual concentration of α-amylase according to following formula.
At: the absorbance of test fluid
As: the absorbance of titer (stock solution)
(7) strength detection
About the intensity of porous activated carbon, utilize compressive strength instrument (Digitech company manufacture, AFK-500TE) according to
Following manner is measured.
The ball shape active carbon test portion intending measuring is placed on the centre of compressive strength instrument Tip, with the speed of 20mm/min
Decline compressive strength instrument, using intensity destroyed for initial ball shape active carbon as compression strength values.Method as described above,
After measuring 22 ball shape active carbon test portions respectively, 20 values in addition to maximum and minima obtain meansigma methods, thus obtain
To compression strength values.
The embodiment of invention
Below, by embodiment, the present invention is described in more details, but the invention is not limited in embodiment.
Embodiment 1.
Spherical furane resins (P Co., Ltd. ure Sphere manufacture) 100g is put into metal test portion container (inner capacities
After 1.5L), electric furnace is used to heat 1 hour and carbonization with the temperature of 500 DEG C under a nitrogen.Use rotary exterior-heat stove and steam at water
Heat spherical furane resins carbide 140 minutes with the temperature of 900 DEG C under gas and make its activation, preparing ball shape active carbon.
Use rotary exterior-heat stove, under oxygen-nitrogen mixture gas that oxygen concentration is adjusted to 3vol%, with the temperature of 470 DEG C to spherical work
After property charcoal carries out 5 hours oxidation processes, carry out reduction treatment 15 minutes with the temperature of 900 DEG C under a nitrogen, and obtain porous
Ball shape active carbon.
Embodiment 2
The steam activation time in embodiment 1 is set to 160 minutes, in addition, side same as in Example 1
Prepared by formula.
Embodiment 3
The steam activation time in embodiment 1 is set to 180 minutes, in addition, side same as in Example 1
Prepared by formula.
Embodiment 4
The steam activation time in embodiment 1 is set to 180 minutes and to carry out 1 at carbonization temperature 450 DEG C little
Time, in addition, prepared by mode same as in Example 1.
Comparative example 1
After spherical furane resins 100g is put into metal test portion container (inner capacities 1.5L), use electric furnace under a nitrogen with
The temperature of 400 DEG C heats 1 hour and carbonization.Use rotary exterior-heat stove and under steam with the temperature of 900 DEG C to spherical furan
Furane resins carbide carries out the heating of 180 minutes and makes its activation, prepares ball shape active carbon.Use rotary exterior-heat stove,
Oxygen concentration is adjusted under the oxygen-nitrogen mixture gas of 3vol%, carries out ball shape active carbon at oxidation in 5 hours with the temperature of 470 DEG C
After reason, carry out reduction treatment 15 minutes with the temperature of 900 DEG C under a nitrogen, and obtain porous ball shape active carbon.
Comparative example 2
After spherical phenolic resin 100g is put into metal test portion container (inner capacities 1.5L), use electric furnace under a nitrogen with
The temperature of 450 DEG C heats 1 hour and carbonization.Use rotary exterior-heat stove and under steam with the temperature of 900 DEG C to spherical phenol
Urea formaldehyde carbide carries out the heating of 180 minutes and makes its activation, prepares ball shape active carbon.Use rotary exterior-heat stove,
Oxygen concentration is adjusted under the oxygen-nitrogen mixture gas of 3vol%, carries out ball shape active carbon at oxidation in 5 hours with the temperature of 470 DEG C
After reason, carry out reduction treatment 15 minutes with the temperature of 900 DEG C under a nitrogen, and obtain porous ball shape active carbon.
Experimental example: select adsorption rate, indole absorption affinity and indole adsorption rate
In order to assess the indole absorption affinity of embodiment and comparative example, to indole with pH 7.4 phosphorus contained by 1.0mg/mL concentration
Phthalate buffer 900mL puts into porous ball shape active carbon 300mg, implements the Dissolution Rate Testing of 3 hours under rotating speed 100rpm
(dissolution instrument Agilent company manufactures, 708-DS).Further, about select adsorption rate, with DL-B-AIB remove and
α-amylase removal ability relevant comparison calculates.Indole adsorption rate is with the indole initial adsorption obtained as follows
Rate (%) represents.
Embodiments of the invention, comparative example and existing commercially available product gram U.S.A are only as shown in table 1 below about experimental result.
Table 1
[Table 1]
As shown above, gram U.S. of the pore volume condition of the not met present invention is clean and comparative example 1～2, it is impossible to simultaneously full
Foot selects adsorption rate and indole absorption affinity.Further, using clean as gram U.S. of carbon source for Colophonium and using phenolic resin as the ratio of carbon source
Relatively example 2, the compressive strength of its porous activated carbon is remarkably decreased, therefore, it is impossible to make curable type unit dosage forms, for example it is difficult to fill out
Fill in capsule.
Claims (6)
1. an oral type medical adsorbent, the porous activated carbon that it is increased by intensity forms.
Oral type medical adsorbent the most according to claim 1, wherein, the porous activated carbon that above-mentioned intensity increases
The pore volume of hole diameter 7.5～15000nm is more than or equal to 0.01mL/g and less than 0.10mL/g, hole diameter 20～
The pore volume of 15000nm is more than or equal to 0.005mL/g and less than 0.04mL/g.
Oral type medical adsorbent the most according to claim 1, wherein, the porous activated carbon that above-mentioned intensity increases
The pore volume of hole diameter 7.5～15000nm is more than or equal to 0.03mL/g and less than below 0.08mL/g, hole diameter 20
～the pore volume of 15000nm is more than or equal to 0.01mL/g and less than below 0.03mL/g.
Oral type medical adsorbent the most according to any one of claim 1 to 3, wherein, above-mentioned intensity increases many
The selection adsorption rate of permeability activated carbon is more than or equal to 3.0.
Oral type medical adsorbent the most according to any one of claim 1 to 3, wherein, above-mentioned intensity increases many
The indole initial adsorption rate of permeability activated carbon is more than or equal to 80%.
Oral type medical adsorbent the most according to any one of claim 1 to 3, wherein, above-mentioned intensity increases many
Permeability activated carbon is more than or equal to 10N/sphere.
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| KR10-2014-0014409 | 2014-02-07 | ||
| KR1020140014409A KR101924201B1 (en) | 2014-02-07 | 2014-02-07 | Medicinal adsorbent for oral administration with increased strength |
| PCT/KR2014/009103 WO2015119352A1 (en) | 2014-02-07 | 2014-09-29 | Orally administered medical adsorbent with increased strength |
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| CN1615908A (en) * | 2003-10-22 | 2005-05-18 | 吴羽化学工业株式会社 | Absorbent for oral administration, and agent for treating or preventing renal or liver disease |
| CN1938037A (en) * | 2004-04-02 | 2007-03-28 | 株式会社吴羽 | Adsorbent for oral administration and therapeutic agent or prophylactic agent for kidney disease and therapeutic agent or prophylactic agent for liver disease |
| JP2013035781A (en) * | 2011-08-08 | 2013-02-21 | Asahi Organic Chemicals Industry Co Ltd | Adsorbent for oral administration and medicine using the same |
| CN103260630A (en) * | 2010-10-12 | 2013-08-21 | 二村化学株式会社 | Medical adsorbent and method for producing same |
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| JP3672200B2 (en) * | 2002-11-01 | 2005-07-13 | 呉羽化学工業株式会社 | Adsorbent for oral administration |
| TWI385120B (en) * | 2004-04-02 | 2013-02-11 | Kureha Corp | Process for preparing spherical activated carbon |
| WO2010001485A1 (en) * | 2008-07-04 | 2010-01-07 | 旭有機材工業株式会社 | Adsorbent for oral administration |
| JP5376592B2 (en) * | 2009-10-15 | 2013-12-25 | 産協企業有限股▲ふん▼公司 | Spherical activated carbon and manufacturing method thereof |
| CN103491949B (en) * | 2011-03-04 | 2017-02-08 | 株式会社吴羽 | Tablet-type composition for oral administration and method for producing same |
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| CN1615908A (en) * | 2003-10-22 | 2005-05-18 | 吴羽化学工业株式会社 | Absorbent for oral administration, and agent for treating or preventing renal or liver disease |
| CN1938037A (en) * | 2004-04-02 | 2007-03-28 | 株式会社吴羽 | Adsorbent for oral administration and therapeutic agent or prophylactic agent for kidney disease and therapeutic agent or prophylactic agent for liver disease |
| CN103260630A (en) * | 2010-10-12 | 2013-08-21 | 二村化学株式会社 | Medical adsorbent and method for producing same |
| JP2013035781A (en) * | 2011-08-08 | 2013-02-21 | Asahi Organic Chemicals Industry Co Ltd | Adsorbent for oral administration and medicine using the same |
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| KR101924201B1 (en) | 2018-12-03 |
| KR20150093907A (en) | 2015-08-19 |
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| JP2017507126A (en) | 2017-03-16 |
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