Drug – bio-affecting and body treating compositions – Effervescent or pressurized fluid containing – Organic pressurized fluid
Reexamination Certificate
1999-08-06
2001-10-09
Page, Thurman K. (Department: 1615)
Drug, bio-affecting and body treating compositions
Effervescent or pressurized fluid containing
Organic pressurized fluid
C424S046000, C424S434000, C424S489000
Reexamination Certificate
active
06299861
ABSTRACT:
The invention relates to the use, by inhalation, of (endo,syn)-(−)-3-(3-hydroxy-l-oxo-2-phenylpropoxy)-8-methyl-8-(1-methylethyl)-8-azoniabicyclo [3,2,1]octane salts as bronchospasmolytics with a powerful and particularly long-lasting effect and the use of the salts in the manufacture of asthma preparations.
The racemate of the above-mentioned compound (in the form of the bromide) is on sale under the name Ipratropium bromide as an active substance in anticholinergic drugs.
It has now been found, surprisingly, that the conditions of activity of the racemate, laevorotatory and dextrorotatory enantiomers are significantly different and have major peculiarities which differ substantially from the norm. The eutomer (i.e. the enantiomer having the desired or sought activity) is the L-(−)-enantiomer. Receptor binding studies on CHO-HM receptors have shown that the L-(−)-enantiomer has approximately twice as high an affinity as the racemate. This ratio corresponds to observations which have frequently been made when comparing the effects of enantiomers and racemates.
However, what is surprising in the present case is that administration by inhalation to the (anaesthetised) dog in a comparison of the eutomer with the racemate in the weight ratio 1:2 exhibits not only a higher potency but also a considerably longer duration of activity.
REFERENCES:
patent: 4385048 (1983-05-01), Mygind et al.
patent: 5225183 (1993-07-01), Purewal et al.
Durgs: Facts and Comparisons, 1994 edition, pp. 965 and 966.*
Physicians Desk Reference on lin, Atrovent Inhalation Solution.
Banholzer Rolf
Disse Bernd
Reichl Richard
Speck Georg
Boehringer Ingelheim KG
Devlin Mary-Ellen M.
Page Thurman K.
Pulliam Amy E
Raymond Robert P.
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