Research Institute
for Physical Chemical Problems of the
Belarusian State University
New Activated
Carbon Drugs
Contact Person:
Dr. D. Grinshpan
Head of the laboratory
of Cellulose Solutions
and Products of their
Treatment
Research Institute
for Physical Chemical
Problems of the
Belarusian State University
14, Leningradskaya, Minsk, RB, 220030
Belarusian State University
Research Institute for Physical Chemical Problems
Tel./fax(+375-17) 226-47-00
E-mail: grinshpan@bsu.by
grinshpan@mail.ru
New Activated Carbon Drugs
«Soluble» activated
carbon – new quickly
disintegrating medicinal
form of activated carbon
Combined drugs
containing both aspirin,
antacid, antibiotics etc.
and carbon
Medicinal forms:
• tablets, granules, capsules
• hydrophilic ointments, gels, liniments
New quickly disintegrating
tablets
New water-soluble cellulose derivative of
polyelectrolyte nature is a binder of
activated carbon drugs
The advantages of medicinal preparations
containing new polymeric binding agent:
 Prompt resolving capacity of granules and
tablets
 High (colloid) degree of dispersiveness
 Coagulating aggressiveness towards colloidstate toxins
 Simultaneous combination of performance
and prolongation
 Absence of ballast fillers
Carbon Tablets
«Ultrasorb»
RI PCP BSU, Minsk
The advantages of carbon tablets
«Ultrasorb»
 spontaneously disperse in the aqueous media in 15-
60 seconds (that is 10-100 times quicker than by the
well-known tablets) forming homogeneous stable
suspension. Up to 10% of its particles have a
colloidal degree of dispersiveness
 Adsorption capacity of tablets determined by
conventional calibrants: methylene blue, antipyrin
and iodine turned out to be higher compared with
the well-known analogues, whereas vitamin B12
sorption was lower
 Such tablets’ properties permit to lower the
therapeutic dose and reduce the treatment period of
different allergies, food poisoning, radioactive
infectiousness etc.
Dispersion is in progress
«Ultrasob»
RI PCP BSU, Minsk
«Carbon tablets»
ICN, Russia
Particle size distribution of activated
carbon tablets suspensions in stomach
medium
New activated carbon drug
dQ/dr
Ordinary activated carbon drug
dQ/dr
in 0.1 M HCl
50
50
40
40
30
30
20
20
10
10
0
5
10
15
20
25
30
35
r
0
in 0.1 M HCl
5
10
15
20
25
30
35
r
Adsorption capacity of various activated
carbon tablets
Adsorption of methylene blue,
mg/g
Adsorption of B12 vitamin,
mg/g
15±5
10±3
Carbon tablets “Carbo medicinalis 0,3 g”
(Poland)
140±10
30±3
Carbon tablets “Norit”
(Netherlands)
170±10
34±3
Carbon tablets
(JSC “Medisorb”, Perm, Russia)
190±10
35±3
Carbon tablets
(Borschagovskii CPP, Ukraine)
195±10
35±3
Carbon tablets
(PO “Kurskii KLS”, Russia)
230±10
35±3
Carbon tablets “Kohle-Сompretten”
(Merck, Germany)
320±10
30±3
Carbon tablets “Ultrasorb”
540±10
11±3
Preparation
Carbon tablets
(Natur Product, France)
Radio nuclides accumulation changes
when using radioprotectors
180
160
140
120
Average
accumulation, 100
Bc/kg
03.сен
80
01.окт
60
40
20
0
Jablopeck
Belsorb
Ultrasorb
Control
Name of a radio protector
The radio protectors favor to excretion of radio nuclides from the
organism in the value of 31 % per 24 days when using 2 tablets a day at
local ration. The merit of Ultrasorb is that is more administration friendly.
Recommendations on use
of carbon enterosorbents
Tablets «Carbo medicinalis 0.3 g» - Poland
Tablet weight - 0,6 g; activated carbon weight – 0,3 g.
auxiliaries: saccharose, polyvinylpyrolidon, magnesium stearate.
2-5 tablets 3-4 times a day or in case of diarrhea 10-20 pills 3-4 times a day.
Grind or crack before use.
12 – 48 g/daily
Tablets«Ultracarbon» – Germany
Tablet weight – 0,4 g; activated carbon weight – 0,25 g.
auxiliary - bentonite
2-4 milled tablets in liquid 3-4 times a day. In case of food poisoning the dose can be
increased up to 50 tablets, stirred up in liquid.
6,4 – 20 g/daily
Powder «BELSORB – P» - Belarus
Daily dose 2,0 g of carbon per 20 kg of patient’s weight is distributed into three
intakes prescribed in the form of aqueous suspension 50-100 ml.
6 – 18 g/daily
Tablets «Ultrasorb» – RI PCP BSU
Tablet weight– 0,17 g; activated carbon weight – 0,16 g.
No ballast fillers.
1 tablet per 20 kg of patient’s weight. Tablets can be previously “solved” in water
and taken in the form of colloid suspension .
1,5 – 3 g/daily
New combined activated carbon drugs
New quickly disintegrating
tablets (granules)












"Carbon–Potassium
Permanganate"
"Carbon–Levomycetin"
"Carbon–Valerian"
"Carbon–Aspirin–Vitamin C"
"Carbon–Aspirin–Vitamin C–
Valerian"
"Carbon–Nicotinic Acid"
"Carbon–Sodium Nucleinat"
"Carbon–Calcium Carbonate"
"Carbon–Calcium Carbonate–
Magnesium Carbonate"
"Carbon–Pectin–Vitamin C–
Sweet"
"Calcium Carbonate"
New hydrophilic ointments,
gels and liniments
hydrocortisone ointment 1 %
lincomycine ointment 2 %
prednisolone ointment 0,5 %
prednisolone gel 0,5 %
dexamethasone gel 0,1 %
tetracycline gel 3 %
liniment "Mumije" 10 %
Aspirin a day: advice that makes sense
«Black» aspirin
(а) – «white» aspirin
(б) – «black» aspirin
Kinetics of acetylsalicylic acid isolation from ordinary
aspirin «Bayer» (a) and «Black» aspirin (b)
а
(in vitro)
b
Content of aspirin in blood
Aspirin concentration, mg/l
(in vivo)
20
15
Black aspirin
10
White aspirin
5
0
0
500
1000time, min1500
American Heart Association recommends the
administration of aspirin from 75 till 325 mg
daily
The main problem of using aspirin - it is its dissolution in gastrointestinal tract (GIT)
Ways of problem solving:
Buffered effervescent "BAYER" aspirin tablets
The basis for these quickly dissolving tablets is the increase of pH medium by buffer,
ionization of ACA and owning to this process the speedup of its dissolution in GIT.
However the sodium form of ACA diffuses through lipidic walls of GIT not nearly so
rapid as the acid one.
Quickly dissolving "Black aspirin" tablets
The basis for this drug form is a principle of a radically different kind. The presence of
a new polymer binder and carbon in these tablets leads to the quick formation of
colloid system in the liquid phase. The high degree of ACA particles dispersiveness
provides for a high dissolution rate. The function of the polymer binder and carbon is
to disperse and disaggregate ACA particles, not to change the degree of its ionization.
Advantages drug form of Black
aspirin
 acts faster than other drug forms (takes effect in 20-30 minutes);
 does not cause ionization of ACA and therefore provides for its





quicker passing through lipidic membranes;
does not produce gassing that irritates mucosa and creates
discomfort in GIT;
does not change pH medium, reduces irritation of stomach
mucosa and duodenum, does not lower the activity of digestive
ferments;
does not contain ballast fillers: sodium bicarbonate, citric acid
which constitute more than 80% of the "BAYER" tablet's mass;
have the same anti-fever effect as the insoluble aspirin, but the
dosage is greatly smaller;
is characterized by a long-lasting effect (up to 180-240 minutes),
due to the fact that 10-15% of ACA (carbon adsorbed ) are
released only in alkaline medium of intestines.
Additional positive effect
 While using "Black Aspirin" side-effects are not likely to appear
due to the fact that its dissolution does not induce the irritation of
stomach mucosa, caused by the pH medium change and there is
no gassing. It can be administrated by patients with stomach or
duodenum ulcer, patients, whom high content of sodium salts is
contra-indicted (patients with high blood-pressure). In case the
tablet is taken by the bed-patients, it will not linger on gullet and
cause its ulceration, owning to its ability to disintegrate quickly.
The tablets containing valerian, that reduces GIT spasms, will be
particularly beneficial for these kinds of patients.
 it can be taken as febrifuge, analgesic, resolvent and cardio
remedy (to prevent cardiovascular diseases);
 at the expense of carbon it helps to deduce toxins from GIT, which
are always present in the patient's organism;
 as the dosage of aspirin in the tablet is significantly small it can be
administrated by children under 4.
Tablets of
buffered
effervescent
“Bayer” aspirin
and “Black
aspirin”
Black Antacid
 Calcium
and magnesium carbonates are the main
representatives of the antacid agents employed to decrease
high acidity of gastric juice ( under gastritis, stomach and
duodenum ulcer). Thanks to the new cohesive used in the
tablets , insoluble calcium and magnesium carbonates
transfer into fine-dyspersated suspension. They quickly
neutralize hydrochloric acid of the stomach contents.
 By comparison with well-known drugs ("Vicair", "Vicalin",
"RENNIE") the application of calcium and magnesium
carbonates in the combination with carbon allows to sorb
carbonic acid, evolved during the neutralization of the
stomach acid. This does not evoke a stimulating effect on the
receptors of the stomach mucosa. This also does not intensify
the secretion of the gastrin and does not cause the
intensification of the secretion for the second time. Do not
contain aluminates.
Kinetics Black antiacid (1) and Renni (2)
interaction with 0,1 M HCI
pH
8
7
1
2
6
5
4
3
2
1
0
0
10
20
30
Time, min.
Degree of readiness for production
 Belarusian pharmaceutical articles for the polymer
binder, activated carbon and their combination are
available;
 there is a laboratory-scale plant for tablets'
formation with capacity of 500 tablets per day;
 there is an experimental-industrial order to
produce polymer binder and carbon tablets,
containing activated carbon and polymer binder;
 in order to accelerate the process of application it
is possible to draw up a joint-patent for new drug
forms.
Possible ways of cooperation:
 Scientific cooperation
 Arrangement of the joint production of
a) polymeric binder
b) active carbon drugs
 Application of the joint patent
 License purchase
a) exclusive
b) non-exclusive