Research Institute for Physical Chemical Problems of the Belarusian State University

1. Research Institutefor Physical Chemical Problems of the Belarusian State University

2. New Activated Carbon Drugs

3. 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, 220030Belarusian State University Research Institute for Physical Chemical Problems Tel./fax(+375-17) 226-47-00 E-mail: grinshpan@bsu.by grinshpan@mail.ru

4. «Soluble» activated carbon – new quickly disintegrating medicinal form of activated carbon Combined drugs containing both aspirin, antacid, antibiotics etc. and carbon New Activated Carbon Drugs • Medicinal forms: • tablets, granules, capsules • hydrophilic ointments, gels, liniments

5. New quickly disintegrating tablets

6. 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 colloid- state toxins • Simultaneous combination of performance and prolongation • Absence of ballast fillers

7. Carbon Tablets «Ultrasorb» RI PCP BSU, Minsk

8. 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.

9. Dispersion is in progress «Ultrasob» RI PCP BSU, Minsk «Carbon tablets» ICN,Russia

10. Particle size distribution of activated carbon tablets suspensions in stomach medium Newactivatedcarbondrug Ordinaryactivatedcarbondrug in 0.1 M HCl in 0.1 M HCl

11. Adsorption capacity of various activated carbon tablets

12. Radio nuclides accumulation changes when using radioprotectors Average accumulation, Bc/kg 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.

13. Recommendations on useof carbonenterosorbents

14. New combined activated carbon drugs • 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 % 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"

15. Aspirin a day: advice that makes sense«Black» aspirin (а) – «white» aspirin (б) – «black» aspirin

16. Kinetics of acetylsalicylic acid isolation from ordinary aspirin «Bayer» (a) and «Black» aspirin (b) (in vitro) b а

17. Content of aspirinin blood(in vivo)

18. The main problem of using aspirin - it is its dissolution in gastrointestinal tract (GIT) American Heart Association recommends the administration of aspirin from 75 till 325 mg daily 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.

19. 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.

20. 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.

21. Tablets of buffered effervescent “Bayer” aspirin and “Black aspirin”

22. 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.

23. Kinetics Black antiacid (1) and Renni (2) interaction with 0,1 M HCI

24. 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.

25. 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