For the treatment of wounds
(57) Abstract:The main components of the means for the treatment of wounds are balsamic substance and gel-forming base (CSO). As balsamic substances used bornyl or isobutylacetate in the following ratio, wt. %: bornyl or isobutylacetate-10,0-15,0, CSO - 85,0 to 90.0. The vehicle accelerates rejection of necrotic tissue, reduces healing time and promotes the development of young granulation tissue, contributes to the formation of the epithelial layer. table 1. The invention relates to medicine, to facilities for the treatment of wounds.Currently known external tools provide mainly sterility natural healing of wounds and burns. For surgery urgent search for new tools that reduce the phase currents of the wound healing process, and, moreover, if possible, is widely available, less toxic, protecting from penetration of hospital strains of bacteria.Special attention is given in this case balsamic remedies of natural origin (Kurmangaliev S. M. Purulent infection in surgery. - M.: Medicine, 1985, S. 194-195).Balsamic tools used in the practice of medicine in Russia, with the us in the application, unpleasant smell, dirty linen, cause the adherence of the dressing, it is difficult to be washed away. Widely known balsamic liniment by A. C. Vishnevskaya, consisting of tar, kseroforma and castor oil (Mashkovsky M. D. Drugs, so 2. - M.: Medicine, 1993, S. 480), still not enough stimulates regenerative processes in the affected tissues, the treatment of them is delayed for long periods, tar creates inconvenience in use and also contains such toxic ingredients as benzene and its derivatives - phenols.The closest analogue to offer a means of fir oil is already finding application in medicine (see, for example, VFS 42-2109-92 from 31.03.92 year ). It is known that it promotes vascularization of the wound surfaces and acceleration of reparative processes that when used healing comes faster than using streptocide liniment (Val'kov Century. And., Kropacheva E. I.,Radios M. I. Effect of pine oil on the process of vascularization and healing of infected skin and muscle wounds in the experiment. In Proc. of "New drugs from plants of Siberia and the Far East." Tomsk, 1986, S. 26).Because fir oil - liquid, which is able to slide from posledni now scarce (Danilenko C. F. Horuk M. S. Drugs of fir and their application in medical practice. Khabarovsk, 1989, S. 47). You can also add pine oil to the means, and having an independent medicinal value, such as honey (W. Surgery No. 5, 1981, S. 28), which in itself or in the composition of ointments E. A. Kon'kov, can also be used to treat wounds.However, fir oil and its dosage forms has some significant drawbacks. This is an old remedy folk medicine is a complex hydrophobic and fuel mixture unequal biological activity of terpene hydrocarbons, alcohols and esters (Poltavchenko Y. A. Composition and potential use in medicine, essential oils of fir Belokolos. Chem.-Pharm. W. N 3, 1981, S. 52-55). More than half of this mixture are unsaturated terpene hydrocarbons, easily forming harmful, irritating the skin peroxide. Especially harmful 3-Karen, causing allergies and dermatitis: its content in the oil, Siberian fir reaches 15%.The most valuable component of fir oil is barcelonetta acting sedative on macro (Saratikov A. S.,Poltavchenko Y. A. Pharmacological activity of derivatives Campana. Chem.-Pharm. W. N 12, 1 volatile substances drug from Siberian fir needles. News Of The NIB. the CTD. An SSSR, ser. Biol. Sciences, vol. 1, No. 5, 1972, S. 38). Barcelonetta has anti-inflammatory action (Kolesnikov, S., Rjutin N., Antinflamatory properties of acetic esters of borneol // Bulletin of the East-Siberian Center Academy of Medical Sciences of Russia. 1993, N 1, p.37), it is able to enhance nonspecific immune defense of the organism, while fir oil during long use at high doses adversely affects the blood and internal organs (Neesa C. A., Stawska Y. A. and others Research allergenic properties of pine oil and its effect on the primary immune response //Metabolic aspects of the effects of industrial chemicals. Krasnoyarsk, 1988, S. 66-70).The content of barcelonetta different in essential oils of various types and forms of fir, which is reflected in the state standards of different countries on fir oil (Kustov, S. D. Handbook of essential oils. - M.: 1978, 180-183 C.) and may vary within considerable limits. In the essential oil of Siberian fir it varies on average from 29 to 40% (Gordon L. Century. and other Technology-chemical industries. Forest industry here. - M.: 1988, S. 320 and 329). Such instability of this natural product, produced in different geographical and climatic zones on various semi-handicraft the organization of the collection and processing of fir twigs in remote mountainous-taiga districts and semi-artisanal nature of the fishery oil high quality as a rule, scarce, expensive, and often adulterated. Considering this, and released from it by the method of rectification barcelonetta costly.But known much more affordable stereoisomeric double barcelonetta - isobutylacetate that is not part of pine oil. These two siblings differ only in spatial distribution of acetyl groups and the proton. Isobutylacetate can be produced in large quantities and with a high degree of purity in chemical plants, where it is possible intermediate product in the manufacture of camphor (Rudakov, A. Chemistry and technology of camphor. - M.: Forest industry here, 1976, S. 77-120).Bornyl and isobutylacetate long been used in perfumery and cosmetics, for example, to get "patatina", from which are produced odorants (Brutus I. N. Chemistry of fragrant substances. - M.: 1992, S. 104-106), in the food industry as a flavoring of some drinks, for example, type "taiga", "Baikal", "Sayan" (Pokhlebkin centuries of Culinary dictionary. Novosibirsk, 1994, S. 137), isobutylacetate sometimes introduced in the composition of medicines classified as non-narcotic analgesics and used in rheumatoid pain (see, naprimer-, neither isobutylacetate never before been used to treat wounds.Dosage forms of external preparations for the treatment of wounds and burns, as already noted, in most cases, hydrophobic. There are only a few examples of the application burns hydrophilic, water-containing means. Widely used in the past liniment Linimentum Calcis because of the low resistance lost its importance (Sinev D. N.,Gurevich I. J. Manual for pharmacists pharmacies. - M.: Medicine, 1982, S. 96-97). Some gels are too complex and exotic compositions of essential oils and surfactants used not to treat wounds. Known, for example, a gel containing in its complex structure such irritating the skin substances like turpentine, menthol, thymol; he patented as irritating and distracting tool in neurological practice (A. Petraglia Klara, ljusdiffusionsfria geler. - Sweds. Pat. CL 7/00 A 61 N 343759, Appl. 5.03.68, publ. 20.03.72).The authors have aimed to create an effective tool for the treatment of wounds, which would reduce the treatment time and would be more accessible, easy to use without side effects.The problem is solved by developing tools for the treatment of wounds, including balsamic substance, a base and water, otlichnaya and benzyl alcohol, and as the basis of blockcopolymer of polyoxyethylene and polyoxypropylene with AVG. mol. m 2500-3500 in the following ratio, wt.%:
Bornyl or isobutylacetate - 10,0-15,0
Benzyl alcohol - 3,0-4,0
Block copolymers - 28,0-30,0
Distilled water - Rest
A special study has shown that the effectiveness of their bactericidal, physiological and therapeutic action bornyl and isobutylacetate practically equivalent. Both have low toxicity (refer to class IV hazardous substance).Benzyl alcohol extends the antibacterial spectrum of the gel, giving it a analgesic properties. His presence is desirable, but not required. Its content should not exceed 4% due to the deterioration of solubility and increase toxicity.Used block copolymers is practically non-toxic, neutral surface-active substance (products HLB=14,9). The block copolymers of this type are already produced in industry for the purposes of medicine and veterinary specifically at the request of authors (for example, mark "HDPE 106" or "HDPE 107" beyond 38407219-82).Optimum results are obtained when the content bornelh esters in the range from 10 to 15 (examples 2 and 3). species. But the increase in the content of more than 15% (example 4) also leads to a decrease in efficiency, although the bactericidal activity of several increases. In optimal ways (examples 2, 3), we obtain tools feature the best consistency and stability. In appearance obtained in optimal options tools (examples 2-3) is a gelatinous mass with a pleasant balsamic odor, fixed benzyl alcohol.Examples of obtaining funds for the treatment of wounds, the composition of which is specified.Suppose you want to gain 0.5 kg funds isobutylacetate one of the best variants containing ether 10% (example 2, table).A portion of blockcopolymer (140 g) in a beaker melted on a water bath and melt impose a pre-measured volumes of isobutylacetate density 0,9849 (50,8 ml) and benzyl alcohol, density 1,0419 (14.4 ml), and then pour in distilled water (295 ml). When mixing occurs vitrification and is formed balsamic gel.So do they do in the case of barcelonetta (when cooking small amounts, volumes measured barcelonetta almost equal to the volume of isobutylacetate what about the volume will be of 50.7 ml).By analogy with the above-described examples, but taking into account different ratios of ingredients, get the money, containing 15% bornyl and isobutylacetate (example 3, table. 1).Experimentally (on outbred white mice) installed and statistically confirmed that the proposed remedy for the treatment of wounds more effectively than analogues (liniment on Vishnevskaya, "Vinsol" containing balsam of shestakovskaja) and the prototype used in various dosage forms (Voronchikhin S. I., S. P. Timonov. Fir oil in the treatment of purulent wounds. Surgery No. 5, 1981, S. 28; Strelnikov B. that is, the Use of pine oil in the treatment of burn wounds // Abstr. X). proc. IUI, Vladivostok, 1972, S. 270).Examples of the application of funds for the treatment of wounds.Assume that you have to treat small wounds from thermal burns IIIA degree area of 81 mm2. The treatment includes daily application to the wound surface a thin layer of therapeutic agent.Below are examples of treatment in identical conditions, two different forms of the prototype (pine oil) and the proposed remedy.Example 1. Treatment is 20% fir oil using as Rast the scab comes through 9,9 day. Then the healing is accelerated to 9.6% per day over 15 days to 11.9% per day. Complete healing occurs 21.1 day.Example 2. The treatment is carried out fir oil with honey. During the first days of the treatment area of the wound is reduced by 2.1% per day. Rejection of the scab comes through 10,3 day. Then the healing is accelerated to 9.3% per day over 15 days to 11.4% per day. Complete healing occurs 20.1 day.Example 3. Treatment is offered product containing in the best case scenario, 10% bornyl or isobutylacetate (PL., composition 2). The results are characterized by close in value metrics below within: during the first days of the treatment area of the wound is reduced by 3.1 to 3.4% per day. The rejection scab occurs in 8.8 to 9.2 days. Then the healing is accelerated to 10.4-10.9% in the day, after 15 days - up to 15.4% per day. Complete healing occurs by 16.4 and 17.2 days.When more significant wound surfaces possible local applications with bandages, which are easily changed in the course of treatment.The above examples demonstrate the undoubted advantages of the proposed facilities, in composition with isobutylacetate more accessible. This tool haraktirizuetsja be stored for 2 years) deodorizing properties, suppresses the putrid smell of bandages. It does not leak, does not stain lingerie, does not irritate the skin, acts as an analgesic and anti-inflammatory, if necessary, is easily washed off, convenient and safe to use. For the treatment of wounds, including balsamic substance and a base, characterized in that the quality balsamic substances contains bornyl or isobutylacetate when the ratio of components, wt.%:
Bornyl or isobutylacetate - 10,0 - 15,0
Underlying - 85,0 - 90,0 p
FIELD: medicine, pharmacology, pharmacy.
SUBSTANCE: invention relates to composition possessing an anti-inflammatory effect and useful for oral administration in form of emulsion preliminary concentrate. Composition comprises NO-releasing nonsteroid anti-inflammatory drug, surface-active substance, oil or semisolid fat and forms in situ emulsion of type oil-in-water after contact with aqueous medium, such as gastroenteric fluid. Also, invention relates to a medicinal formulation based on thereof, oral emulsion, set based on thereof and a method for treatment of inflammation and pain. Proposed compositions possess the improved availability.
EFFECT: improved and valuable properties of composition.
40 cl, 1 tbl, 20 ex
FIELD: organic chemistry, medicine, endocrinology, pharmacy.
SUBSTANCE: invention relates to new derivatives of acylphenylurea of the formula (I) and to their physiologically acceptable salts possessing property of glycogen phosphorylase inhibitors. In compound of the formula (I) A means phenyl and phenyl residue can be substituted three times with fluorine (F), chlorine (Cl), bromine (Br) atoms, -CF3, -NO2, -O-(C1-C6)-alkyl, -SO2-(C1-C6)-alkyl, (C1-C6)-alkyl, -COOH; R1 means hydrogen atom (H), (C1-C6)-alkyl; R2 means H, (C1-C6(-alkyl, -CO-(C1-C6)-alkyl; 3, R4, R5 and R6 mean independently of one another H, F, Cl, Br, -O(C1-C6)-alkyl, (C1-C6)-alkyl, (C3-C7)-cycloalkyl, -COOH, -COO-(C1-C6)-alkyl; X means oxygen (O), sulfur (S) atom; R7 means (C1-C10)-alkylene-COOH, (C1-C10)-alkylene-COO-(C1-C6)-alkyl, (C1-C10)-alkylene-NH2, (C1-C10)-alkylene-NH-(C1-C6)-alkyl, (C1-C10)-alkylene-N-[(C1-C6)-alkyl]2, (C1-C10)-alkylene-B wherein B means piperidinyl or furyl. Also, invention relates to a pharmaceutical composition and a method for preparing the pharmaceutical composition. Proposed compounds can be used for preparing pharmaceutical composition useful for declining level of blood glucose and for treatment of diabetes mellitus type II.
EFFECT: improved preparing method, valuable medicinal properties of compounds and composition.
7 cl, 2 sch, 2 tbl, 1 ex
FIELD: pharmaceutical industry, in particular cyprofloxacine solution.
SUBSTANCE: claimed solution contains cyprofloxacine hydrochloride, sodium salt of ethylenediamine-N,N,N1,N1-tetraacetic acid, α-hydroxypropionic acid, sodium chloride, water for injections.
EFFECT: drug of increased biological availability without side effects.
FIELD: organic chemistry, medicine, pharmacy.
SUBSTANCE: invention relates to novel ester compounds represented by the formula (1): wherein values for R1, R2, A, X, R3, R4, Alk1, Alk2, l, m, D, R8 and R9 are determined in the invention claim. Also, invention relates to inhibitor of matrix metalloproteinase (MTP), a pharmaceutical composition able to inhibit activity of MTP selectively, agents used in treatment or prophylaxis of hyperlipidemia, arteriosclerosis, coronary artery diseases, obesity, diabetes mellitus or hypertension wherein the pharmaceutical composition is prepared in capsulated formulation, and to a biphenyl compound of the formula (100) given in the invention description.
EFFECT: valuable medicinal properties of compounds.
53 cl, 78 tbl, 17 ex