Vaginal suppositories for the treatment of trichomonas and nonspecific colpitis
(57) Abstract:Vaginal suppositories can be used to treat Trichomonas and nonspecific colpitis. The composition of the suppository in g mass of 1.66 - 1.84 g : Nitazol 0,11 - 0,13; tallow or Witepsol 1,535 - 1,625; emulsifier (glycerol monostearate) 0,015 - 0,085. Adaca invention is to reduce the side effects of suppositories with high efficiency in treatment of Trichomonas and nonspecific colpitis. table 2. Offer suppositories relate to medicine, in particular, pharmacology, and can be used to treat Trichomonas and nonspecific colpitis.Known vaginal suppositories for the treatment of obesity.One of them are vaginal suppositories for the treatment of acute and chronic trichomoniasis in women who as a medicinal substances contain metronidazole.Metronidazole, possessing a broad spectrum of activity, is an effective drug for the treatment of Trichomonas.However, during treatment with vaginal suppositories containing metronidazole, sometimes there is excessive development of the fungal flora of the vagina, which requires additional Lacey purpose to offer vaginal suppositories are known vaginal suppositories for the treatment of Trichomonas and non-specific colitis, which authors selected as a prototype.Known vaginal suppositories for the treatment of Trichomonas and nonspecific colpitis contain as a medicinal substance trichomonacid and the basis of , including tallow or witepsol, representing a mixture of glycerides of high molecular weight saturated fatty acids, mainly C12-C18Aerosil and the emulsifier is glycerol monostearate, in the following ratio of components, g on one suppository mass 2,435 - 2.70 g:
Trichomonacid - 0,05
Solid fat or Witepsol - 2,27 - 2,61
Aerosil - 0,02 - 0,06
The emulsifier is glycerol monostearate - 0,01 - 0,03
Known vaginal suppositories containing trichomonacid, are effective for the treatment of urogenital diseases in women, because Trichomonas has high activity against Trichomonas.Also contained in the basis of solid fat or witepsol allow good quality suppositories to obtain suppositories in a fully automated process mode.Introduction to the basis of the emulsifier is glycerol monostearate allows to obtain the composition of suppositories with a uniform distribution Blocki vagina.Object of the invention is the reduction of side effects of vaginal suppositories and high efficiency of treatment, while expanding arsenals of vaginal suppositories for the treatment of Trichomonas and nespetsificheskogo of obesity.The problem is solved offered by vaginal suppositories for the treatment of Trichomonas and nonspecific colpitis, containing the medicinal substance and the basis, including tallow or Witepsol and the emulsifier is glycerol monostearate, according to the invention as medicinal substances they contain Nitazol, in the following ratio of components, g on one suppository mass of 1.66 - 1.84 g:
Nitazol - 0,11 - 0,13
Solid fat or witepsol - 1,535 - 1,625
The emulsifier is glycerol monostearate - 0,015 - 0,085
The distinguishing characteristics are that the quality of drug substances they contain nitazol, in the following ratio of components, g on one suppository weight of 1.64 - 1.84 g:
Nitazol - 0,11 - 0,13
Solid fat or Witepsol - 1,535 - 1,625
The emulsifier is glycerol monostearate - 0,015 - 0,085
< / BR>C5H5N3O3S - M m 187,18
Yellow with Zelenova the ve medicinal substance Nitazola when the content of 0.11 - 0,13 g for one suppository mass of 1.66 - 1.84 g can effectively treat them Trichomonas colpitis and other nonspecific colpitis, without causing irritation of the mucous membrane and having no contraindications.Introduction part one suppository weight of 1.64 - 1.84 g Nitazola less than 0.11 g reduces the effectiveness of treatment, and the introduction of more of 0.13 g does not increase the effectiveness of treatment.Analysis of scientific-technical and patent documents showed that the proposed vaginal suppositories for the treatment of Trichomonas and nonspecific colpitis are new and meet the criterion of "inventive step".The method of obtaining the proposed vaginal suppositories.First carry out the preparation of a basis for this in the melter load estimated amount of solid fat or witepsol, where it is melted and then passed into a heated reactor, after which it enter the estimated amount of the emulsifier is glycerol monostearate (MSH). The mixture is stirred until complete melting MSG.Ready based on the heated line is passed into the reactor preparation suppozitornyj masses.Prepare the concentrate nitazola, pateyron machine.The prepared concentrate small amounts injected into the remaining hot part of the framework and the mass is thoroughly mixed.The manufacture of suppositories perform on machines with the necessary technological regimes by molding method. In the molding process of the suppository mass in the reactor is continuously stirred and maintain the required temperature.Suppositories are white with green or yellow-greenish, torpedo-shaped shape with a maximum diameter of 1.5 cmThe average weight of the suppository of 1.75 g of 5%.Shelf life 2 years.Offer vaginal suppositories underwent clinical trials in the Kiev scientific research Institute of Pediatrics, obstetrics and gynecology.Treatment with vaginal suppositories with Nitazolom conducted in 60 patients with banal colpitis from 20 to 40 years.Before treatment, all patients in the content of the vagina was determined Trichomonas flora, 35 to 40 cells per field of view (see tab. 1).The distribution of treated women by age.Efficacy of treatment was assessed by clinical data and method to examine the contents of the vagina.lackova, occasionally cocci, leucocytes 10 - 15 in the field of view, and in 2 patients the analysis of allocations remained the same.In table. 2 shows the effectiveness of the treatment.The 2 women in the treatment process appeared itching and burning sensation, redness of the mucous of the vagina, and therefore the treatment is discontinued.As can be seen from the obtained results, the proposed suppositories are effective for the treatment of Trichomonas and nonspecific colpitis.Were conducted clinical trials offer suppositories in Sverdlovsk research Institute of maternity and infancy.Clinical trials offer suppositories conducted in 50 women affected by Trichomonas colpitis.Treatment consisted of 2 to 3 cycles of 15 days each.Treatment was started immediately after menstruation.Bacteriological and bacterioscopic was 3-fold in each patient.The age of the women was from 16 to 47 years.The clinical picture of Trichomonas vaginitis was profuse vaginal discharge, burning, itching, redness of the mucous of the vagina, the presence of microarray cervix. 12 Jania Trichomonas detected in 60% of women 10 - 15% of women allocated conditionally pathogenic and pathogenic microflora-klebisella, E. coli, epidermis, Staphylococcus aureus. The degree of cleanliness of a vagina all women was III - IV.As a result of treatment after the first year of full clinical effect was observed in 60 % of women, the rest after the 2nd and 3rd courses (mainly in women with stable trihomoniaza).Offer vaginal suppositories with nitazolom are effective especially when persistent course of trihomoniaza and sustainable forms of non-specific colitis, which allows you to expand the Arsenal of vaginal suppositories for the treatment of these diseases.Sources of information
1. M. D. Mashkovsky. Medicinal product. o'clock P, M.: Medicine, 1984, S. 343.2. M. D. Mashkovsky. Medicinal product. o'clock P, M.: Medicine, S. 347 Vaginal suppositories for the treatment of Trichomonas and nonspecific colpitis, containing the medicinal substance and the basis, including tallow or Witepsol and the emulsifier is glycerol monostearate, characterized in that, as a medicinal substance they contain Nitazol in the following ratio of components, g on one suppository mass 1 is a - 0,015 - 0,085 Sch
FIELD: organic chemistry, biochemistry.
SUBSTANCE: invention relates to epothilones with modified thiazole substituent, methods for production thereof and pharmaceutical composition capable of cell growth inhibiting containing the same. Claimed compounds have general formula I , wherein P-Q represents double carbon bond or epoxy; R represents H, C1-C6-alkyl; G represents ; R1 represents and ; G1 and G2 represent hydrogen; G3 represents O, S, and NZ1; G4 represents H, optionally substituted C1-C6-alkyl, OZ2, Z2C=O and Z4SO2; G5 represents halogen, N3, CN, NC, heteroaryl containing nitrogen or oxygen, and heterocycle; G6 represents H, C1-C6-alkyl, or OZ5, wherein Z5 represents H, C1-C6-alkyl; G9 represents oxygen; Z1 represents H, optionally substituted C1-C6-alkyl, optionally substituted acyl; Z2 represents optionally substituted C1-C6-alkyl or aryl; Z4 represents optionally substituted aryl.
EFFECT: new epothilones capable of cell growth inhibiting.
19 cl, 39 ex