Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Nitrogen containing other than solely as a nitrogen in an...
Patent
1997-07-01
1998-10-06
Henley, III, Raymond
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Nitrogen containing other than solely as a nitrogen in an...
A61K 3113
Patent
active
058176977
DESCRIPTION:
BRIEF SUMMARY
The invention relates to the use of nitroglycerine to prevent undesired labor in mammals, in a transdermal form of application.
Nitroglycerine, also known as glycerol trinitrate (GTN), is a long-known chemical substance with manifold applications. Chemically, GTN is described as 1,2,3-propanetriol trinitrate. In particular, nitroglycerine is a valuable substance for treating coronary heart diseases. In view of this significance, many pharmaceutical formulations are now available. The galenical preparations of this substance by now include tablets, capsules, ointments, solutions, IV solutions, sprays, and patches for transdermal application.
Surprisingly, it has now been discovered that the use of nitroglycerine in a transdermal form of application prevents undesired labor in mammals.
Studies in animals and human beings have shown that it is possible to stop labor with this galenical form of preparation of nitroglycerine with the purposeful use of nitroglycerine in a given test subject.
The invention will be described in further detail below in terms of the study performed with human beings.
The study encompassed 18 pregnant women, each showing signs of premature labor. Their pregnancies were already advanced; they were already between 25 and 34 weeks pregnant. The GTN patches used were each applied instead of Ritodrin, a labor-inhibiting substance. All the pregnant subjects exhibited the following characteristics:
their amniotic sacs had not yet broken;
they had not had premature bleeding;
the fetuses had no abnormalities.
The patients were given up to two GTN patches simultaneously per day, each with 10 or 10.8 mg of 1,2,3-propanetriol trinitrate. The surface area of the patch was 32 cm.sup.2 when DEPONIT.RTM. 10 was used and 16 cm.sup.2 when a novel GTN patch made by SCHWARZ PHARMA A.G. was used. This latter patch contains the nitroglycerine in an adhesive composition based on a cross-linked acrylate vinyl acetate copolymer.
There were no evident differences in terms of the success in use. Both patches prevented premature labor, stopped premature labor or ended irregular labor.
Tables 1 and 2 show that nitroglycerine in a transdermal galenical preparation prevents undesired premature labor in pregnant mammals.
It can be seen from the tables that labor was stopped after application of the patches. None of the patients suffered an unwanted premature birth. By dose-dependent administration of patches containing nitroglycerine until the expected date for the birth, it was possible to stop strong labor or to regulate irregular labor.
EXEMPLARY EMBODIMENT 1
The patch is produced in the manner described in detail in exemplary embodiment 1 of European Patent Disclosure EP 0 144 486 B1.
A pharmaceutical product according to the present invention with a three-layer reservoir structure is produced as follows:
A pressure-sensitive adhesive composition containing nitroglycerine is prepared.
0.175 kg polyisobutylene (mean molecular weight from 900,000 to 1,400,000; commercial product OPPANOL.RTM. B 100),
0.157 kg solid aliphatic hydrocarbon resin (commercial product PICCOTAC CBHT),
0.157 kg hydrated rosin (commercial product ABITOL),
0.0105 kg 5% solution of nitroglycerine in a medium-chained triglyceride (commercial product MIGLYOL.RTM. 812),
1.174 kg petroleum spirit 80-110 as a solvent.
The product is applied onto a protective layer, on which aluminum is vapor-deposited on one side and which is equipped antiadhesively on both sides, in such a way that after the solvent evaporates, a layer of approximately 20 g/m.sup.2 is obtained. Onto the thus-obtained pressure-sensitive adhesive layer, the first reservoir layer is applied as a coating, with a weight per unit of surface area of approximately 20 g/m.sup.2.
The production of this reservoir layer is done by the application of a dispersion comprising:
0.05 kg 10% (G/G) ground mixture of nitroglycerine and lactose,
0.153 kg polyisobutylene (mean molecular weight from 900,000 to 1,400,00.0; commercial product OPPANOL.RTM. B 100),
0.137 kg solid aliphatic hydrocarbon
De Belder Adam Julian
Feelisch Martin
Lees Christoph Christopher
Martin John Francis
Ramsay Bruce
Henley III Raymond
Schwarz Pharma AG
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