JPS5933218A - Pharmaceutical composition - Google Patents

Abstract

(57) [Summary] This bulletin contains application data before electronic filing, so abstract data is not recorded.

Description

DETAILED DESCRIPTION OF THE INVENTION The present invention discloses that noaminodiphenylsulfone (DI)8) and 2. - A novel pharmaceutical preparation containing a mixture of 1-diami/-5-(4-bromo-3,5-dimethoxybenzyl)-pyrimidine [prosimopri A (1+rodimopri+o)].

The present invention relates to leprosy (leprosy) and/or mycobacteriosis (mycobacteriosis).
It also concerns the use of the above-mentioned combinations of substances for the treatment of es).

The use of 1') DS for the treatment of leprosy is known. The mixture of OS and prodimoprim is effective against leprosy-causing organisms.
It has now been found that the compound exhibits additively increased activity when compared to the activity of the individual components.

Preferred Embodiment 1: In the present invention, the preparations are prepared in a molar ratio of DO8 to prodimoprim of 1:1 to 1.
: Contains 1-th active substance at 10.

The significant complementary activity of the combination of DI') S and prodimobrim according to the invention against leprogenic organisms is evident from the tests described hereinafter.

bovine serum albumin
umin) (7 Luxion V) ('1.25 wt/vol% modified Dubosugvis nutrient solution (Dul+
os-Davisnutrient 5olu1.1o
4-6 week old Gottsucker agar slant culture (G
Myco7 from ottsacker 5lanL culLure), Mycol+uclpr
iu+nl ur Ll). To obtain a homogeneous suspension, the bacteria were homogenized in 5 ml of medium, then the suspension was diluted with +5+nl of Jr'X and centrifuged at 150 g for 1 min. 1- A portion of the clear liquid was used for the culture. suspension i1k
diluted to approximately 105 cells/+1+ l and 50 ml
Magnetically stir Alifu 1 (al iqt+of, s) 4'l
! +fi was added to a 3 +'l (1+nl Erlenmeyer culture flask). Inhibitor was added and the culture was kept at 31 °C. The culture was magnetically Stir for 1 min.
t+nLpr). To determine the total bacterial count, culture samples were divided into 5 (i l'1~2 + l
The l'l l'l li organisms were diluted with particle-free sodium chloride, (f'l, 85%/formaldehyde (+1.2%)) solution so that 1 u of the organism was obtained. To determine live bacterial counts, 1.5 ml samples were removed from time to time, added to 50 ml of fresh nutrient solution, and incubated at 31 °C.
After 811, the number was counted using a Coulter counter as described in ij.

For a particular inhibitor (f) was determined by the change in the rate of growth of the culture in the lower right.For this, the observed first-order development rate in the presence and absence of the inhibitor is determined by the rate constant K apl+ (sec') is calculated by the formula 1, where N is the number of organisms in a defined culture volume, t is the time in seconds, and No is the a, ξ at time 1 = (). was determined from the increase in the growth curve according to the number of bacteria at

r) I') S-susceptible mycobacteria (M,
lt mountain-) and DDS resistance (
2"00μMDI')S)vI, Fuhacteria (M, 1
ufu) are listed in Table II. A constant is given for the steady-state rate of development for M,lt mountain 1 at 1°C:) in the presence of various inhibitors at various concentrations.

Human - ■ - Table 11 In the active substance superposition provided by the present invention (f lower right, no growth of microorganisms was observed and even a decrease in the number of living bacteria in the culture was observed; In contrast, the values given in the table show that when the active substances are present individually, the growth of the culture continues, albeit slowly. is also completely suppressed by the DDS-prodimobrim combination at appropriate concentrations.

The pharmaceutical preparations provided by the present invention contain the above-mentioned active substance combinations with compatible pharmaceutical preparations.

The carrier may be any organic or inorganic carrier suitable for enteral, transdermal, or parenteral administration; active carrier materials such as water, gelatin, acacia, lactose, starch, magnesium stearate, talc, vegetable oils, polyalkylene glycols, etc. I can do it. The pharmaceutical preparation is a fever-lowering agent (rever-
IoweriB agenl. s), pain relievers (pa)
It can also contain other pharmaceutically valuable substances, such as in-alleviatin-g Bents, etc. Pharmaceutical preparations include, for example, tablets, capsules, tablets, powders, granules;
It can be administered orally in the form of a suspension, elixir, etc. However, dosages may be administered, for example, in the form of sterile solutions, suspensions, or emulsions for oral purposes, or for topical purposes in the form of solutions, suspensions, ointments, powders, or aerosols. You can also do it. The pharmaceutical preparation can be sterilized and/or preserved.
It is possible to include ingredients such as agents, stabilizers, humectants, emulsifiers, salts for proper pressure, and buffer substances.

According to the invention l) 4+7 The preparation provided is leprosy 1
d, 1) l) Even λJ can be used for the treatment of S-resistant leprosy. The preparation is a non-medical control therapy for leprosy (non-mpd:r:u1conlr+
+l Il+erapy)l and I)l)S
In order to avoid the development of resistance in the case of lit therapy (+noI+o1.11 therapy), the preparation provided by the present invention is particularly suitable for 67' therapeutic applications. 111+'11118 I)
l) FI JI of pronomoprim to correspond to S &
J? Completed with ii! (You can throw something like this.)

-1-Casting I) lI) 1. tjij - It can be thrown as a throw or in a partial throw that is divided into 11 by λ·j <-). Preferably one tablet is administered at 111.

The following are examples of typical dosage forms: Tablet I')r>S I (l +')I+lli Bronomoprim 211 fl +
n.

Primodiel (1'ri+no, 1el) (starch derivative) 6+nB Povidone K
3! ') ([-'ovidoncl)K:', +
1 (Polyvinylpyrrolidone) 8 +nH
Magnesium stearate (imH total weight 32 (1+nH

Claims (1)

Claims: 1. A pharmaceutical preparation containing cyami/cy-phenyl sulfone and 2,4-cyami/-5-(=1-bromo-3,5-enemethoxybennol)-pyrimidine. 2. Preparation according to claim 1 for leprosy and/or pond mycobacteriosis. 3. diami/cyphenylsulfone pair 2, 4-noami/-5-(/1-70m, '4.5-i)/
) The molar ratio of xyhe:, -E/l)-pyrimidine is I:
A preparation according to claim 1 in which I 7'7 total 1:I ('l).