NEW DENTAL COMPOSITION AND A PROCESS FOR THE PREPARATION THEREOF

Abstract: Dental composition comprising an anti-osteoporotic agent, an antiphlogistic agent, optionally a natural or synthetic chemotherapeutic agent or local anaesthetic, furthermore one or more known auxiliary agent(s). The invention also relates to a process for the preparation of the above composition.

Description: KBvϊ DENTAL COMPOSITION AND A PROCESS FOR 'THE PREPARATION THEREOF The invention relates to a new dental composition and to a process for the preparation thereof. As known, caries is the most widespread endemic disease. It is quite obvious to one skilled in the art that a great deal of teeth could be saved by a preservative treat ment performed in due time. In practice, however, patients turn to the dentist only when they suffer from an untolerabl pain, i.e. when at least one complication exists, too. Pain is caused first by pulp hyperaemia, i.e. by the reversible inflammation of the vessels and intravascular nerves of the dental radix. The volume of the narrow pulp canal, closed between hard walls, cannot increase, thus the arteries exert a hard pressure on the veins, which results an early appearance of venal hyperaemia. At the stage of pulp hyperaemia, however, caries does not reach the pulp, since it is separated from it by a thin healthy layer of de When caries proceeds, an infectious inflammation appears in the pulp (pulpitis). Of the various forms of pulpitis only the main types are mentioned now. When an acut inflammation exists and the pulp is only partially damaged, dentists endeavour to save the living tooth. When inflammati gets, however, cronic and the pulp is completely damaged, the goal of dental treatment is to render the further treat¬ ment painless, to exclude additional complications and to ensure a symptom-free recovery. In its. final stage, pulpitis leads to gangrene. Tooth necrosis does not terminate, however, in the pulp. The defensive mechanism of the organism can act against infec¬ tions only at territories with good blood supply. Perio- dontium, which surrounds the tooth, suits this requirement, consequently the next stage is the appearance of periodont- itis. At the appearance of this disorder, causing pains even upon touch, pulp itself is no longer sensitive, the subjective symptoms are, however, very painful. The task of dentists is to ensure the quick alleviation of this complain in the acute stage of inflammation. In chronic stages, how¬ ever, additional complications must be taken into account. Inflammation may spread over the periodontal bony substance where it may lead to pathologic osteoporoses (granuloma, cysts) o Several attempts have been made to defend the exace tion of the above diseases, according to Adler and Zaray /_Kcnzerval<5 fogaszat (Preservative Dentistry) p. 172 (L.edi- cina, Budapest, 1972) (in pulp canal must be sterilized completely. It is very important that the surrou ing tissues be free of inflammation. Therefore pulp ca has been treated with various sterilizing agents, antibioti and antiphlogistics, utilized most frequently as a liquid composition. A disadvantage of this method is that prolonge activity cannot be ensured. Utilization of powders or removable pastes in such treatments has also been attempted _Pogorvosi Szemle (Dent ists* Review) § t 404 (1971) (in Hungarianj/, but prolonged effect could not be achieved. Hungarian patent No. 167,308 suggests the use of pointers comprising a sterilizing (i.e. oxidizing) or anti¬ phlogistic agent and/o -an antibiotic in admixture with an • inert plastic carrier. Penicillin, chloramphenicol and oxy- tetracyclin are mentioned as antibiotics, whereas hydro- cortisone is mentioned as antiphlogistic agent. The major disadvantage of this method is that it can be applied only for the treatment of excavated pulp canal, furthermore it cannot act against osteoporosis coupled with other complica¬ tions. The invention aims at providing a new composition applicable for the treatment of caries and for the healing of acute, subacute or chronic inflammatory lesions of pulp, dental radix or the bony substance surrounding them. Our extensive experimental work has led to the un¬ expected recognition that a particular combination, i.e. a combination of ipriflavone (7-isopropoxy-isoflavone) and an antiphlogistic agent can be utilized with good results for 5 the complex treatment of teeth. Depending on the conditions of use, this combination can be supplemented with chemo¬ therapeutic agents, local anaesthetics and known auxiliary agen s. The above combination can be applied successfully 10 in all stages of pulpitis and periodontitis. Based on the above, the invention relates to a new dental composition comprising an anti-osteoporotic agent, preferably ipriflavone, an antiphlogistic agent, optionally a natural or synthetic chemotherapeutic agent or a local an- I5L aesthetic, furthermore one or more known auxiliary agent(s). The invention also relates to a process for the preparation of the above dental composition. According to the invention 0.1 to 30 "fi> by weight of ipriflavone, 0.5 to 15 by weight of an antiphlogistic agent, preferably triam- 20 cinolone, and optionally one or more natural or synthetic chemotherapeu ic agent(s) or local anaesthetic(s) are ad¬ mixed with auxiliary agents commonly applied in dentistry. As synthetic chemotherapeutic agents e.g. sulphonamides or trimethoprim 2,4-diamino-5-(3' ,4* ,5'-trimethoxybenzyl)- 25 pyrimidine_J whereas as ^ natural chemotherapeutic agent e.g. doxycyclin base (an antibiotic) or a salt thereof can be applied. As local anaesthetic required e.g. to prepare a coating for protecting dental stump_7 ϋdocaine can be used. Of the sulphonamides sulphamethoxazole is particularly pre- 0 ferred. The known auxiliary agents for dental purposes are e.g. zinc oxide, calcium oxide, bismuth oxide, titanium di oxide, eugenol, epoxy resin and dental lacquers. The utilization of more than one active agent in dental filler has led to particularly advantageous and un- 5 expected results. The antimicrobial agent with a broad spectrum of activity is utilized to exterminate the pathogens which ca inflammation. The antimicrobial agent alone does not act o the other components of the inflammatory process. 10 Triamcinolone, utilized as antiphlogistic agent, exerts a very strong effect on the inflammatory process: it suppresses the oedema and stops the other inflammatory comp nents, resulting in a quick alleviation of pain and in the cessation of inflammation. It is known, however, that this - substance may also enhance the activity of osteoklasts caus ing osteoporosis in the bony substance e.g. when a tria - cinolone-containing filling agent is introduced into the pulp canal after the removal of pulp. Ipriflavone, one of the members of the combinatio D according to the invention, supplements the effects of the two former components in a particularly advantageous manner it is able to suppress osteoporosis even alone, furthermore it antagonizes the osteoklast activity-increasing effects o steroidal antiphlogistics. 5 By combining these three types of active agents a series of therapeutic dental fillers, suitable for pre¬ serving the teeth in any stage of pulpitis and periodontiti can be obtained. The most important advantage provided for by the D invention is that the combination can be utilized in several types of dental diseases. The new combinations can be utilized for the following purposes: 1/ In the treatment of pulp hyperaemia and acute partial pulpitis a dental cement comprising 0.1 to 10 , preferably 0.7 to 2 of the combination according to the invention should be placed onto the pulp-side wall of the cavity formed by the dentist, wherefrom the active agents enter the pulp and result in a very quick relief of pain an in the suppression of inflammation. Doxycyclin, mentioned as an example of the chemotherapeutic agents, accumulates in the tooth, resulting in a prolonged effect. Upon the effect of ipriflavone the formation of secondary dentin is also to be expected. 2/ In chronic total pulpitis the treatment is per- formed in two steps. Pirst the treatment described in point 1/ above is performed in order to attain a painless stage, thereafter the pulp canal is excavated to prevent the sprea ing of inflammation, and in the second treatment step the method described in point 3/ below is performed * 3/ In the treatment of periodontitis the therapeuti paste (admixed with appropriate auxiliary agents) is applie into the previously cleaned and dried pulp canal. The anti¬ phlogistic and antimicrobial effects appear quickly, and a very quick relief of pain is to be expected. 4/ When the complications of periodontitis are to b avoided or the already existing complications should be suppressed, the reversal of osteoporoses already formed (ostitis diffusa, granuloma, cysts) is to be expected upon a prolonged application of the anti-osteoporotic therapeuti paste. The final root filling is prepared after the termina tion of the complete bony defects, utilizing an antibiotic free composition comprising anti-osteoporotic agents, X-ra contrast materials and carriers. The invention is elucidated in detail by the aid o the following non-limiting Examples. Example 1 Preparation of a therapeutic cement A mixture of 2 g of doxycyclin hyclate, 0.8 g of triamcinolone, 2.0 g of ipriflavone, 80 g of zinc oxide an 15.2 g of calcium oxide (Component "A") is admixed with eugenol (Component "B") in a ratio to obtain a composition with a consistency required in dentistry. Example 2 Preparation of a therapeutic cement One proceeds a-s described in Example 1 with the difference that doxycyclin hyclate is replaced by 2.2 g of trimethoprim. Example ? Preparation of a therapeutic paste for sterilizing pulp canal 0.2 g of ipriflavone is admixed with 0.2 g of doxy cyclin base, 0.08 g of triamcinolone and 10 g of zinc oxide and the mixture is completed with eugenol in an amount required to obtain a paste. Example 4 Preparation of a therapeutic paste for sterilizing pulp canal One proceeds as described in Example 3 with the difference that sulphamethoxazole is substituted for doxy- cyclin base. Example 5 Preparation of a root filler 0.5 g of ipriflavone are admixed with 0.1 g of tria cinolone, 4.0 g of bismuth oxide, 2.0 g of titanium dioxide and 3»4 g of zinc oxide, and epoxy " resin is added to the mix ture in an amount to obtain a paste. Example 6 Preparation of a coating composition for protecting: dental stump A mixture of 0.3 g of ipriflavone, 0.1 g of triamcin lone and 0.2 g of lidocaine base is dissolved in 5 ml of acetone. This solution can be utilized for the preparation of a single coating or multiple coatings.

Claims: What we claim is : 1. A dental composition which comprises an anti-osteo porotic agent, an antiphlogistic .agent, optionally a natura or synthetic chemotherapeutic agent or local anaesthetic, 5 furthermore one or more known auxiliary agent(s). 2. A composition as claimed in claim 1, which comprise ipriflavone (7-isopropoxy-isoflavone ) as anti-osteoporotic agent, triamcinolone as antiphlogistic agent, an antibiotic, preferably doxycyclin or a salt thereof, a sulphonamide or 10 trimethoprim as a chemotherapeutic agent and lidocaine as local anaesthetic. 3. A composition as claimed in claim 1 or 2, which comprises 0.1 to 30 jό by weight of ipriflavone, 0.5 to 15 % by weight of triamcinolone, optionally 0.1 to 10 % by weight 15. of doxycyclin or a salt thereof, optionally 1 to 20 % by weight of lidocaine, and 35 to 99-4 % by weight of one or more known auxiliary agent(s). 4. A process for the preparation of a dental composi¬ tion, characterized in that 0.1 to 30 jo by weight of ipri- 0 flavone, 0.5 to 15 % by weight of triamcinolone, optionally 0.1 to 10 % by weight of doxycyclin or a salt thereof and optionally 1 to 20 by weight of lidocaine are admixed with 35 to 99.4 TO by weight of one or more known auxiliary agent( 5. A method for protecting pulp of carious teeth, 5 characterized in that a composition as claimed in claim 1 is utilized. 6. A method for preserving the vitality of pulp in early stages of pulpitis, characterized in that a compositio as claimed in claim 1 is utilized. 7. A method for sterilizing pulp canal, characterized in that a composition as claimed in claim 1 is utilized. 8. A method for preparing a final root filling with the provision of an X-ray contrast agent, characterized in that a composition as claimed in claim 1 is utilized.

Inventors: BALOGH TIBOR, CSANYI ENDRE, CSANYI GABOR, NAGY LASZLO, BALOGH, TIBOR, CSANYI, ENDRE, CSANYI, GABOR, NAGY, LASZLO
Applicants: REANAL FINOMVEGYSZERGYAR
Application year: 1988
Main classification: A61K6
IPC codes: A61K6, A61K31, A61P29, A61P43