Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form
Patent
1994-11-17
1996-08-06
Page, Thurman K.
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
424444, 544309, 514269, 514270, A61L 1516
Patent
active
055431470
DESCRIPTION:
BRIEF SUMMARY
FIELD OF TECHNOLOGY
The present invention pertains to organic chemistry or, more exactly to a new crystalline modification of 2,4-dioxo-6-methyl-1,2,3,4-tetrahydropyrimidine, a method for the preparation thereof, and a medicinal preparation based on it.
PRIOR ART
There is a known crystalline form of 2,4-dioxo-6-methyl-1,2,3,4-tetrahydropyrimidine (SU, A, 194096) characterized by the following set of values of interplane spacings d and relative intensities of reflexes I:
______________________________________ d, .ANG.
I
1 2
______________________________________
8.005
17
5.497
9
5.315
100
4.105
4
4.004
2
3.648
38
3.411
16
3.332
3
3.169
23
3.110
4
2.805
3
2.723
1
2.667
3
2.613
3
2.569
27
2.469
1
2.382
1
2.340
1
2.275
11
1.929
3
1.867
1
1.828
2
1.712
5
1.640
1
1.599
1
1.588
1
______________________________________
The said crystalline form of 2,4-dioxo-6-methyl-1,2,3,4-tetrahydropyrimidine is prepared by crystallization of the said compound out of its aqueous solution. The resulting product is a white crystalline powder poorly soluble in water and ethyl alcohol, insoluble in ether, chloroform, characterized by the above-described values of interplane spacings d and relative intensities of reflexes I. This compound posessing the antiinflammatory and wound healing effect is characterized by insufficiently high effectiveness, toxicity, and induction of side effects.
The said compound finds an application as the active substance of a medicinal preparation for treatment of wounds, burns, bone fractures, X-ray disease, leukopenia, gastric and duodenal ulcer, hepatitis, pancreatitis and others (M. D. Mashkovsky, Pharmaceuticals, 1984, Medizina Publishers, Moscow, v. 2, p. 138).
For instance, there is a known pharmaceutical containing the said compound as the active substance used for treatment of pure postoperation wounds by the intramuscular or oral routes (G. L. Bilich--Stimulation of regeneration and defence mechanisms in infantile surgery, 1976, Medizina Publishers, Moscow, p. 31-32).
The intramuscular inoculation of the drug facilitates the spread of the greater part of the drug in other tissues and organs as a result of which no necessary topical concentration of the drug is achieved reculting in no efficacy of the treatment.
After oral administration of the drug part of it is destroyed in the stomach and no necessary concentration of the drug in the area of the wound is achieved either. This does not create a sufficient wound-healing effect of the drug and prolongs the period of treatment.
There is known pharmaceutical containing as the active substance the saif compound in the form of 5-10% liniment for topical treatment of wounds (M. D. Mashkovsky, Pharmaceuticals, 1984, Medizina Publishers, Moscow, v. 2, p. 48-60). The said drug does not accelerate the wound healing greatly (by 19.4%) and is not highly effective in treatment of suppurating wound.
Also known is an eye ointment containing the said compound as the active substance (E. A. Egorov, Application of methyluracil in ophthalmology, 1968, Kazan Medical Journal, No. 4, p. 71-72).
The said eye ointment is used for treatment of different kinds of eye cornea wounds. The use of this ointment facilitates wound healing, however, in severe forms of burns against the background of treatment there appears cicatricial tissue impairing the vision, there also frequently occur cases of secondary infection and inflammatory processes.
The said eye ointment was tested only experimentally in animals but not clinically in human patients.
The claimed crystalline modification of 2,4-dioxo-6-methyl-1,2,3,4-tetrahydropyrimidine, the method for its production and use are novel and have not been described in the literature.
DISCLOSURE OF THE INVENTION
The invention was aimed at the creation of a new crystalline modification of 2,4-dioxo-6-methyl-1,2,3,4-tetrahydropyrimidine possessing high antiinflammatory and wound-healing activity, the development of a
REFERENCES:
patent: 4986985 (1991-01-01), Grossman et al.
patent: 5162316 (1992-11-01), Coates
Mashkovsky, M. D. "Lekarstvennye sredstva". posobie po farmakoterapii dlya vrachei, 1986, izdanie desyate, tom 2, izd. Meditsina M., pp. 138-139.
Leonidov Nikolai B.
Selezenev Nikolai G.
Benston, Jr. William E.
Leonidov Nikolai B.
Page Thurman K.
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