Etofenamate formulation
AssigneeTroponwerke GmbH & Co. KG
InventorsHans-Dieter Dell, Reinhold Kraus, Detlef Schierstedt
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AssigneeTroponwerke GmbH & Co. KG
InventorsHans-Dieter Dell, Reinhold Kraus, Detlef Schierstedt
Estimating the term…
The invention relates to topical antiinflammatory medicament formulations which also have analgesic activity and contain 2-(2-hydroxyethoxy)-ethyl N-(.alpha.,.alpha.,.alpha.,-trifluoro-m-tolyl) anthranilate as the active ingredient and an adjuvant which is preferably a triglyceride.
A cream or ointment formulation comprising (a) 2-(2-hydroxyethoxy)ethyl N-(.alpha.,.alpha.,.alpha.-trifluorom-tolyol)anthranilate,
Dependencies are inferred from the claim text.
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Containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides: alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene…
Galenical forms characterised by the site of application: skin, i.e. galenical aspects of topical compositions
Having an amino or nitro group: amino benzoic acid types, e.g. procaine, novocaine
Containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides: esters of carboxylic acids, e.g. fatty acid monoglycerides,…
Term ended 15 Mar 2005 (estimated)
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The present invention relates to an antiinflammatory medicament formulation which has an analgesic action and is to be applied topically, and which contains 2-(2-hydroxyethoxy)-ethyl N-(.alpha.,.alpha.,.alpha.-trifluoro-m-tolyl)anthranilate, called Etofenamate below, as the essential active compound. Etofenamate has the following structure: ##STR1##
Etofenamate is already known as a non-steroid medicament with a good antiinflammatory action and outstanding tolerance, compare Arzneimittelforschung 27 (I) Special Edition 6 b, 1299-1364, 1977. Etofenamate has hitherto been used in the form of alcohol-containing gels. Because of the alcohol, the gel has a cooling action when applied, and this has not been found pleasant by all patients. Furthermore, such a gel can be applied only to intact skin, and a desirable application in cases of trauma with open wounds is thus not possible. In addition, such a formulation is of only limited suitability for patients with an exceptionally dry skin.
An object of the present invention is thus to overcome the disadvantages described by providing a new formulation which, however, has the antiinflammatory and analgesic action to the same degree as the gel form.
The present invention may be illustrated in more detail by the following examples.
__________________________________________________________________________ Example 1 2 3 4 5 6 __________________________________________________________________________ Etofenamate 100 100 100 100 100 50 (mg) H.sub.2 O 522.5 512.5 509 522.5 613 679 (mg) Adjuvant Isopropyl Isopropyl Diisopropyl Miglyol 840 .RTM. Diisopropyl Diisopropyl (mg) myristate myristate adipate 100 100 adipate adipate 100 100 130 110 Emulsifier Myrj. 59 .RTM. Myrj. 59 .RTM. Myrj. 59 .RTM. Myrj. 59 .RTM. Myrj. 59 .RTM. Myrj. 59 .RTM. (mg) 50 50 50 50 50 50 Benzyl alcohol 15 15 15 15 15 15 (mg) Tylose MH 4000 7.5 7.5 7.5 7.5 -- -- (mg) Agent which Cutina MD .RTM. Cutina MD .RTM. Cutina MD .RTM. Cutina MD .RTM. Cutina .RTM. Cutina .RTM. gives con- 175 175 175 175 GMS 37 GMS 41 sistency (mg) Citrate 30 30 30 30 30 30 buffer solu- tion (mg) Benzyl -- 10 -- -- -- 10 nicotinate Cetyl alcohol 10 10 Veegum 15 15 __________________________________________________________________________ Example 7 8 9 10 11 __________________________________________________________________________ Etofenamate 100 100 200 50 200 (mg) H.sub.2 O 603 605 442 582 442 (mg) Adjuvant Diisopropyl Miglyol 810 .RTM. Isopropyl- Isopropyl- Diisopropyl- (mg) adipate 130 130 myristate myristate adipate 100 100 100 Emulsifier Myrj. 59 .RTM. Myrj. 59 .RTM. Myrj. 59 .RTM. Myrj. 59 .RTM. Myrj. 59 .RTM. (mg) 50 50 50 50 50 Benzyl alcohol 15 15 15 15 15 (mg) Tylose MH 4000 -- -- 8.0 8.0 8.0 (mg) Agent which Cutina .RTM. Cutina .RTM. Cutina MD .RTM. Cutina MD .RTM. Cutina MD .RTM. gives con- GMS 37 GMS 45 155 165 155 sistency (mg) Citrate 30 30 30 30 30 buffer solu- tion (mg) Benzyl -- -- -- -- -- nicotinate Cetyl alcohol 10 10 Veegum 15 15 __________________________________________________________________________
TABLE __________________________________________________________________________ Agent which Cetyl Exam- Etofenamate Adjuvant I Adjuvant II Emulisifier I gives con- Aerosil .RTM. alco- PEG Benzyl ple (mg) (mg) (mg) (mg) sistency (mg) (mg) hol 400 nicotinate __________________________________________________________________________ 12 50 Diisopropyl -- Cremophor EL .RTM. -- 80 adipate 820 50 13 200 Diisopropyl -- Cremophor EL .RTM. -- 80 adipate 670 50 14 50 Isopropyl -- Cremophor EL .RTM. -- -- myristate 900 50 15 200 Isopropyl -- Cremophor EL .RTM. -- -- myristate 750 50 16 50 Myglyol 840 .RTM. -- Tween 40 .RTM. -- -- 900 50 17 200 Myglyol 670 .RTM. -- Tween 40 .RTM. -- 80 900 50 18 50 Miglyol 812 .RTM. -- Tween 60 .RTM. -- 80 820 50 19 200 Miglyol 750 .RTM. -- Tween 60 .RTM. -- -- 820 50 20 50 Oleyl alcohol Diisopropyl Cremophor EL .RTM. -- -- 450 stearate 450 50 21 100 Isopropyl -- Tween 40 .RTM. -- 80 myristate 770 50 22 100 Isopropyl Diisopropyl Tween 60 .RTM. -- 80 myristate 500 adipate 260 50 23 50 Diisopropyl -- Myrj 59 .RTM. Wool wax alcohol -- 20 -- -- adipate 100 50 ointment DAB 8 780 24 200 Diisopropyl -- Myrj 59 .RTM. Wool wax alcohol -- 30 -- -- adipate 150 50 ointment DAB 8 570 25 50 Isopropyl -- Myrj 59 .RTM. Softisan 378 .RTM. 30 -- -- -- myristate 100 50 770 26 200 Isopropyl -- Myrj 59 .RTM. Softisan 378 .RTM. 35 -- -- -- myristate 110 50 615 27 200 Isopropyl -- Myrj 59 .RTM. PEG 4000 .RTM. -- -- 230 -- myristate 120 50 400 28 50 Miglyol 810 .RTM. -- Myrj 59 .RTM. Wool wax alcohol -- 20 -- -- 100 50 ointment DAB 8 780 29 200 Miglyol 810 .RTM. -- Myrj 59 .RTM. Wool wax alcohol 25 30 -- -- 150 50 ointment DAB 8 545 30 50 Miglyol 840 .RTM. -- Myrj 59 .RTM. Wool wax alcohol -- 20 -- -- 100 50 ointment DAB 8 780 31 200 Miglyol 840 .RTM. -- Myrj 59 .RTM. Wool wax alcohol 25 30 -- -- 150 50 ointment DAB 8 545 32 50 Isopropyl -- Myrj 59 .RTM. Cutina MD .RTM. -- -- -- -- myristate 520 50 380 33 200 Isopropyl -- Myrj 59 .RTM. Cutina MD .RTM. -- -- -- -- myristate 450 50 300 34 100 Diisopropyl -- Myrj 59 .RTM. -- -- -- -- 10 adipate 840 __________________________________________________________________________