DE1767957B2 - PRODUCTION OF POWDERED COMPOSITIONS CONTAINING 3,5-DINITRO-O-TOLUYLIC ACID - Google Patents
PRODUCTION OF POWDERED COMPOSITIONS CONTAINING 3,5-DINITRO-O-TOLUYLIC ACIDInfo
- Publication number
- DE1767957B2 DE1767957B2 DE19681767957 DE1767957A DE1767957B2 DE 1767957 B2 DE1767957 B2 DE 1767957B2 DE 19681767957 DE19681767957 DE 19681767957 DE 1767957 A DE1767957 A DE 1767957A DE 1767957 B2 DE1767957 B2 DE 1767957B2
- Authority
- DE
- Germany
- Prior art keywords
- dinitro
- water
- acid amide
- toluic acid
- sodium lauryl
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- 239000000203 mixture Substances 0.000 title claims description 17
- 238000004519 manufacturing process Methods 0.000 title claims description 3
- YTUKZWSMRTXUPV-UHFFFAOYSA-N 2-methyl-4,6-dinitrobenzamide Chemical compound CC1=CC([N+]([O-])=O)=CC([N+]([O-])=O)=C1C(N)=O YTUKZWSMRTXUPV-UHFFFAOYSA-N 0.000 claims description 13
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 13
- DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical compound [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 claims description 12
- 235000019333 sodium laurylsulphate Nutrition 0.000 claims description 12
- 239000003814 drug Substances 0.000 description 4
- 239000000243 solution Substances 0.000 description 3
- OWEGMIWEEQEYGQ-UHFFFAOYSA-N 100676-05-9 Natural products OC1C(O)C(O)C(CO)OC1OCC1C(O)C(O)C(O)C(OC2C(OC(O)C(O)C2O)CO)O1 OWEGMIWEEQEYGQ-UHFFFAOYSA-N 0.000 description 2
- 229930091371 Fructose Natural products 0.000 description 2
- 239000005715 Fructose Substances 0.000 description 2
- RFSUNEUAIZKAJO-ARQDHWQXSA-N Fructose Chemical compound OC[C@H]1O[C@](O)(CO)[C@@H](O)[C@@H]1O RFSUNEUAIZKAJO-ARQDHWQXSA-N 0.000 description 2
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 description 2
- GUBGYTABKSRVRQ-PICCSMPSSA-N Maltose Natural products O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@@H]1O[C@@H]1[C@@H](CO)OC(O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-PICCSMPSSA-N 0.000 description 2
- CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 description 2
- 229930006000 Sucrose Natural products 0.000 description 2
- 238000004090 dissolution Methods 0.000 description 2
- 229940079593 drug Drugs 0.000 description 2
- 150000004676 glycans Chemical class 0.000 description 2
- 239000008101 lactose Substances 0.000 description 2
- 239000000693 micelle Substances 0.000 description 2
- 150000002772 monosaccharides Chemical class 0.000 description 2
- 229920001282 polysaccharide Polymers 0.000 description 2
- 239000005017 polysaccharide Substances 0.000 description 2
- 238000002360 preparation method Methods 0.000 description 2
- 239000000126 substance Substances 0.000 description 2
- 239000005720 sucrose Substances 0.000 description 2
- 239000004094 surface-active agent Substances 0.000 description 2
- GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 description 1
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 description 1
- 241001465754 Metazoa Species 0.000 description 1
- 150000001408 amides Chemical class 0.000 description 1
- 239000007864 aqueous solution Substances 0.000 description 1
- WQZGKKKJIJFFOK-VFUOTHLCSA-N beta-D-glucose Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 description 1
- GUBGYTABKSRVRQ-QUYVBRFLSA-N beta-maltose Chemical compound OC[C@H]1O[C@H](O[C@H]2[C@H](O)[C@@H](O)[C@H](O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@@H]1O GUBGYTABKSRVRQ-QUYVBRFLSA-N 0.000 description 1
- 230000015572 biosynthetic process Effects 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 230000002192 coccidiostatic effect Effects 0.000 description 1
- 150000001875 compounds Chemical class 0.000 description 1
- 239000003651 drinking water Substances 0.000 description 1
- 235000020188 drinking water Nutrition 0.000 description 1
- 239000008103 glucose Substances 0.000 description 1
- 238000005063 solubilization Methods 0.000 description 1
- 230000007928 solubilization Effects 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
Description
Gegenstand der Erfindung ist die Herstellung von pulverförmigen 3,5-Dinitro-o-toluylsäureamid enthaltenden Zusammensetzungen unter Verwendung von Natriumlaurylsulfat und wasserlöslichem Mono- oder Polysaccharid, die — bezogen auf das 3,5-Dinitro-o-toluylsäureamid — 3 bis 7 Gew.-°/o Natriumlaurylsulfat enthalten und in Wasser bei Zimmertemperatur so aufgelöst werden, daß die Lösung einen Gehalt an 0,1 bis 0,4 g 3,5-Dinitro-o-toluylsäureamid je Liter aufweist.The invention relates to the production of pulverulent 3,5-dinitro-o-toluic acid amide containing Compositions using sodium lauryl sulfate and water-soluble mono- or Polysaccharide which - based on the 3,5-dinitro-o-toluic acid amide - 3 to 7% by weight of sodium lauryl sulfate contained and dissolved in water at room temperature so that the solution has a content of 0.1 to Has 0.4 g of 3,5-dinitro-o-toluic acid amide per liter.
Das 3,5-Dinitro-o-toluylsäureamid besitzt hervorragende coccidiostatische Wirkung und wird daher in der Veterinärmedizin in großem Umfang angewendet, hat aber den Nachteil, daß es sich bei Raumtemperatur nicht gut in Wasser löst. Es wird deshalb im allgemeinen zusammen mit Futtermitteln verabreicht. Wenn sich die Tiere jedoch schlecht fühlen oder krank sind, d. h. gerade dann, wenn die Verabreichung des Mittels erforderlich wäre, nehmen sie normalerweise kein Futter, aber weiterhin Trinkwasser auf.The 3,5-dinitro-o-toluic acid amide has an excellent coccidiostatic effect and is therefore used in the Veterinary medicine is widely used, but has the disadvantage that it is not at room temperature dissolves well in water. It is therefore generally administered together with feed. If the However, animals feel bad or are sick, d. H. just when the administration of the agent would be required, they normally do not eat food but continue to consume drinking water.
Die Herstellung einer Zusammensetzung mit einem wirksamen Gehalt an 3,5-Dinitro-o-toluylsäureamid, die sich bei Raumtemperatur ohne weiteres in Wasser löst, ist daher von erheblicher Bedeutung für die Veterinärmedizin. The preparation of a composition with an effective content of 3,5-dinitro-o-toluic acid amide, the dissolves readily in water at room temperature is therefore of considerable importance for veterinary medicine.
Es ist bekannt, daß sich in Wasser schwerlösliche oder unlösliche Stoffe mit Hilfe von Tensiden solubilisieren lassen, vgl. u. a. Fortschritte in der Arzneimittelforschung, Bd. 10, 1966, S. 263-265. Eines der hierfür bevorzugten Tenside ist Natriumlaurylsulfat, vgl. beispielsweise F. G s t i r η e r, Einführung in die Arzneibereitung, Stuttgart 1963, S. 222—224. Die Solubilisierung geht so vor sich, daß der Lösungsvermittler oberhalb einer für ihn kritischen Konzentration Mizellen bildet, in denen sich der normalerweise in Wasser unlösliche Stoff unter Bildung einer scheinbaren Lösung löst. Die kritische Konzentration der Mizellbildung beträgt für Natriumlaurylsulfat 0,2 Gew.-°/o bzw. 2 g/Liter.It is known that substances which are sparingly soluble or insoluble in water can be solubilized with the aid of surfactants let, see inter alia. Advances in Drug Research, Vol. 10, 1966, pp. 263-265. One of the for this The preferred surfactant is sodium lauryl sulfate, cf., for example, F. G s t i r η e r, Introduction to Drug Preparation, Stuttgart 1963, pp. 222-224. The solubilization goes on in such a way that the solubilizer is above In a concentration that is critical for him, micelles are formed in which the substance, which is normally insoluble in water, is found solves to form an apparent solution. The critical concentration of micelle formation is for Sodium lauryl sulfate 0.2% by weight or 2 g / liter.
In den erfindungsgemäßen pulvrigen, in wäßrige Lösungen überführbaren Zusammensetzungen kommt
eine weitaus geringere Konzentration an Natriumlaurylsulfat zur Anwendung, die überraschenderweise
dennoch zu einer Lösung des schwerlöslichen 3,5-Dinitro-o-toluylsäureamids
in Wasser von Raumtemperatur führt. Sie beträgt nur 0,003 bis 0,028 g/Liter.
Geeignete wasserlösliche Monosaccharide für die erfindungsgemäßen Zusammensetzungen sind beispielsweise
Glukose und Fruktose. Als Polysaccharide kommen z. B. Saccharose, Laktose und Maltose in
Frage. Die Menge an Natriumlaurylsulfat beträgt, ίο bezogen auf das 3,5-Dinitro-o-toluylsäureamid, 3 bis 7
Gew.-% und vorzugsweise 5 bis 7 Gew.-°/o. Zur Erleichterung der sofortigen Lösung der Zusammensetzung
wird das 3,5-Dinitro-o-toluylsäureamid vorzugsweise vor der Zugabe zu der Zusammensetzung fein
gemahlen.In the powdery compositions according to the invention which can be converted into aqueous solutions, a much lower concentration of sodium lauryl sulfate is used, which surprisingly nevertheless leads to a solution of the sparingly soluble 3,5-dinitro-o-toluic acid amide in water at room temperature. It is only 0.003 to 0.028 g / liter.
Suitable water-soluble monosaccharides for the compositions according to the invention are, for example, glucose and fructose. As polysaccharides, for. B. sucrose, lactose and maltose in question. The amount of sodium lauryl sulfate is, based on the 3,5-dinitro-o-toluic acid amide, 3 to 7% by weight and preferably 5 to 7% by weight. To facilitate instant dissolution of the composition, the 3,5-dinitro-o-toluic acid amide is preferably finely ground prior to addition to the composition.
Die wirksame Menge an 3,5-Dinitro-o-toluylsäureamid beträgt nach dem Lösen nicht mehr als 0,4 g je Liter Wasser. Im allgemeinen reicht eine noch geringere Konzentration von z. B. 0,1 bis 03 g je Liter aus. Diese Konzentrationen werden leicht beim Lösen der Zusammensetzung in Wasser von Zimmertemperatur, d. h. von etwa 200C, erhalten, wobei besondere Mischvorrichtungen nicht erforderlich sind.The effective amount of 3,5-dinitro-o-toluic acid amide after dissolution is no more than 0.4 g per liter of water. In general, an even lower concentration of e.g. B. 0.1 to 03 g per liter. These concentrations are easily obtained when the composition is dissolved in water at room temperature, that is to say at about 20 ° C., special mixing devices not being required.
Die Herstellung der pulvrigen Zusammensetzung erfolgt auf herkömmliche Weise, d. h. durch Vermischen der verschiedenen Bestandteile.The powdery composition is prepared in a conventional manner; H. by mixing of the various components.
Die folgenden Beispiele erläutern die Erfindung.The following examples illustrate the invention.
2 g feingemahlenes 3,5-Dinitrc-o-toluylsäureamid wurden gründlich mit 0,1 g Natriumlaurylsulfat und 17,88 g pulverförmiger Saccharose vermischt. Man erhielt eine 10%ige Mischung. 0,4 g dieser Zusammensetzung lösen sich schnell in 100 ml Wasser von 25" C.2 g finely ground 3,5-dinitrc-o-toluic acid amide were mixed thoroughly with 0.1 g of sodium lauryl sulfate and 17.88 g of powdered sucrose. Man received a 10% mixture. 0.4 g of this composition will quickly dissolve in 100 ml of 25 "C of water.
10 g feingemahlenes 3,5-Dinitro-o-toluylsäureamid wurden homogen mit 0,5 g Natriumlaurylsulfat und 39,5 g pulverförmiger Laktose vermischt. Es wurde eine Mischung mit einem Gehalt von 20% der aktiven Verbindung erhalten. 1,5 g dieser Mischung lösen sich bei Raumtemperatur sofort in 1 Liter Wasser.10 g of finely ground 3,5-dinitro-o-toluic acid amide were homogeneous with 0.5 g of sodium lauryl sulfate and 39.5 g powdered lactose mixed. It became a mixture containing 20% of the active Connection received. 1.5 g of this mixture dissolve immediately in 1 liter of water at room temperature.
10 g feingemahlenes 3,5-Dinitro-o-tohivlsäureamid wurden gründlich mit 0,5 g Natriumlaurylsulfat und anschließend mit 89,5 g Fruktose vermischt. 3 g dieser 10% aktive Verbindung enthaltenden Mischung lösen sich leicht in 1 Liter Wasser von Raumtemperatur.10 g of finely ground 3,5-dinitro-o-tohalic acid amide were mixed thoroughly with 0.5 g of sodium lauryl sulfate and then with 89.5 g of fructose. 3 g of this Mixture containing 10% active compound easily dissolves in 1 liter of room temperature water.
2 g feingemahlenes 3,5-Dinitro-o-toluylsäureamid2 g finely ground 3,5-dinitro-o-toluic acid amide
wurden gründlich mit 0,10 g Natriumlaurylsulfat und 17,90 g Maltose zu einer 10%igen Mischung vermengt.were thoroughly mixed with 0.10 g sodium lauryl sulfate and 17.90 g maltose to form a 10% mixture.
2 g dieser Zusammensetzung lösen sich leicht in 1 Liter Wasser von Raumtemperatur.2 g of this composition easily dissolves in 1 liter of room temperature water.
Claims (1)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IL2827267A IL28272A (en) | 1967-07-07 | 1967-07-07 | Emulsifiable powder containing 3,5-dinitro-o-toluic-acid amide(d.o.t.) |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| DE1767957A1 DE1767957A1 (en) | 1971-09-30 |
| DE1767957B2 true DE1767957B2 (en) | 1978-02-02 |
| DE1767957C3 DE1767957C3 (en) | 1978-10-05 |
Family
ID=11044208
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DE19681767957 Expired DE1767957C3 (en) | 1967-07-07 | 1968-07-05 | Manufacture of powdery compositions containing 3,5-dinitro-o-toluic acid amide |
Country Status (6)
| Country | Link |
|---|---|
| BE (1) | BE717660A (en) |
| DE (1) | DE1767957C3 (en) |
| FR (1) | FR1586876A (en) |
| GB (1) | GB1192479A (en) |
| IL (1) | IL28272A (en) |
| NL (1) | NL6809498A (en) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS5924132B2 (en) * | 1980-12-02 | 1984-06-07 | 株式会社 林原生物化学研究所 | Manufacturing method for nutritional supplement emulsion |
| CH689139A5 (en) * | 1995-04-03 | 1998-10-30 | Cerbios Pharma Sa | Process for the preparation of a liposomal, in water dispersable, orally administrable, solid, dry therapeutic formulation. |
-
1967
- 1967-07-07 IL IL2827267A patent/IL28272A/en unknown
-
1968
- 1968-07-05 DE DE19681767957 patent/DE1767957C3/en not_active Expired
- 1968-07-05 GB GB3210668A patent/GB1192479A/en not_active Expired
- 1968-07-05 FR FR1586876D patent/FR1586876A/fr not_active Expired
- 1968-07-05 NL NL6809498A patent/NL6809498A/xx unknown
- 1968-07-05 BE BE717660D patent/BE717660A/xx unknown
Also Published As
| Publication number | Publication date |
|---|---|
| IL28272A (en) | 1970-12-24 |
| DE1767957C3 (en) | 1978-10-05 |
| GB1192479A (en) | 1970-05-20 |
| NL6809498A (en) | 1969-01-09 |
| BE717660A (en) | 1969-01-06 |
| FR1586876A (en) | 1970-03-06 |
| DE1767957A1 (en) | 1971-09-30 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C3 | Grant after two publication steps (3rd publication) | ||
| EHJ | Ceased/non-payment of the annual fee |