MX2008000499A

MX2008000499A - Pharmaceutical composition.

Info

Publication number: MX2008000499A
Application number: MX2008000499A
Authority: MX
Inventors: Walter Wilhelm Focke; Ernest Schay; Lushane Walbrugh
Original assignee: Bayer Healthcare Ag
Priority date: 2005-07-14
Filing date: 2006-07-01
Publication date: 2008-03-07
Also published as: ZA200800392B; BRPI0612872A2; AR055352A1; WO2007031133A1

Abstract

A pharmaceutical composition is provided comprising an active pesticidal composition contained in an effervescent dosage form.

Description

PHARMACEUTICAL COMPOSITION DESCRIPTION OF THE INVENTION This invention relates to a pharmaceutical composition and, more particularly, to a pharmaceutical composition in the form of a solid dosage form soluble in water. In this specification, the term "pesticide" should have its broadest meaning and is intended to encompass within its scope herbicides and compositions for eradicating or controlling animal pests. Liquids in general, and pesticides in particular, are usually marketed as liquid concentrate in metal or plastic containers from which a desired amount of the product is decanted before use. Pesticides, by their nature, are dangerous chemicals and the disposal of empty containers of pesticides is a problem since the containers usually contain a pesticide residue that can leach into the environment with disastrous consequences. Similar problems can be experienced to some extent with full or partially filled containers, particularly metal containers or plastic containers having bare headed screws. In addition, containers frequently fall off and break during transport. Another problem with containers is the use, Ref .: 189134 particularly in developing countries where services such as running water are lacking, empty containers to store water for domestic use. The dangers of such a practice need no explanation. An attempt to address the above problem involves supplying the active pesticidal ingredient in powder form in plastic bags. A desired amount of the active ingredient is weighed and mixed with water just before use. To a large extent, plastic bags, while requiring less storage space than metal or plastic containers, experience the same disadvantages as containers particularly when stored in humid environments and also when measuring the correct amount of the powder. It is an object of this invention to provide a pharmaceutical composition and, more particularly, to provide a pharmaceutical composition in the form of a water soluble solid dosage form that at least partially mitigates the aforementioned disadvantages. In accordance with this invention there is provided a pharmaceutical composition comprising an active pesticidal composition contained in an effervescent dosage form. Additionally, it is envisioned that the composition includes an acid, preferably citric acid and a carbonate or bicarbonate, preferably an alkaline carbonate such as sodium carbonate or an alkaline bicarbonate such as sodium bicarbonate. Additionally it is envisaged that the active pesticidal composition is a herbicide. Alternatively it is envisioned that the active pesticidal composition is suitable for controlling or eradicating mammalian pests, preferably ectoparasites and preferably additionally an acaricide. It is also envisioned that the acaricide belongs to the amidine group of pesticides, preferably amitraz. According to another embodiment, the acaricide belongs to the group of pyrethroids, preferably alpha-cyano pyrethroids, in particular, deltamethrin. The pharmaceutical composition generally includes at least one binder, preferably propylene glycol and at least one surfactant, for example, a condensation product bound to methylene of arylsulfonic acids, preferably Baykanol SL and / or a sodium salt of alkylnaphthalenesulfonate, preferably Nekal BX, and / or a nonionic surfactant belonging to the nonylphenol ethoxylate group, preferably ARKOPAL N090. Additionally, the composition according to the present invention can include one or more of the following ingredients: • at least one suitable dispersant, preferably a sodium salt of the condensation product of naphthalene sulfuric acid, in particular, WETTOL D2; • at least one disintegrant, preferably sodium starch glycolate • at least one antioxidant, preferably butylated hydroxytoluene (BHT). Generally the concentrations of the ingredients in the composition are in the following ranges: Ingredient from 10 to 60% m / m active Carbonate from 5 to 25% m / m, Acid from 4 to 21% m / m Binder from 10 to 40% m / m Surfactant from 1 to 25% m / m, Dispersant from 0.6 to 2% m / m Antioxidant from 0.3 to 1% m / m (In the case that combinations of different ingredients of one type are used - for example, more than one surfactant - the concentration ranges are given for the sum of the concentrations of the respective ingredients.) The concentration of the active ingredient in the composition it will vary according to the required effective concentration and the solubility of the respective compound. Typical concentrations are, for example, 20 to 60% m / m (of the final composition) for amitraz or 12 to 16% m / m (of the final composition) for deltamethrin. According to one embodiment, it is envisioned that the pharmaceutical composition includes at least one suitable dispersant, and / or at least one disintegrant, and / or at least one surfactant, and / or at least one binder; it is envisioned that the dispersant is a sodium salt of the condensation product of naphthalene sulfuric acid, preferably WETTOL D2; the disintegrant is expected to be sodium starch glycolate; it is envisioned that the surfactant is a nonionic surfactant belonging to the group of nonylphenol ethoxylate nonylphenol, preferably ARKOPAL N090; and it is envisaged that the binder is propylene glycol. According to a preferred embodiment of the invention it is provided that the composition includes amitraz, sodium carbonate, citric acid monohydrate, ARKOPAL N090, WETTOL D2 and propylene glycol; the constituents are expected to be present in the following ranges (% m / m in the final composition): Amitraz from 20 to 60% m / m Sodium carbonate from 5 to 17% m / m, Citric acid monohydrate from 4 to 9% m / m ARKOPAL N090 from 1 to 4% m / m, WETTOL D2 from 0.6 to 2% m / m, and Propylene glycol from 10 to 40% m / m.

According to a particular preferred embodiment of the invention, it is provided that the composition is constituted as follows: Amitraz 50.1% m / m Sodium carbonate 12.5% m / m, Citric acid monohydrate 7.3% m / m ARKOPAL NO90 2.4% m / m, WETTOL D2 1.2 2% m / m, and Propylene glycol 26.4% m / m. According to another preferred embodiment of the invention it is provided that the composition includes deltamethrin, sodium bicarbonate, citric acid monohydrate, Baykanol SL (condensation product bound to methylene of arylsulfonic acids), Nekal BX (sodium salt of alkylnaphthalenesulfonate), propylene glycol and , 6-di-tert-butyl-4-methylphenol (BHT); the constituents are expected to be present in the following ranges (% m / m, based on the final composition) Deltamethrin from 12 to 16% m / m Sodium bicarbonate from 20 to 25% m / m Citric acid monohydrate from 17 to 21 % m / m Baykanol SL from 19 to 24% m / m Nekal BX from 1.2 to 1.6% m / m Propylene glycol from 19 to 24% m / m 2, 6-di-tert-butyl-4-methylphenol (BHT) from 0.5 to 0.7% m / m According to a particular preferred embodiment of the invention it is provided that the composition is constituted as follows: Deltamethrin 13.9% m / m Sodium bicarbonate 22.2% m / m Citric acid monohydrate 18.8% m / m Baykanol SL 21.7% m / m Nekal BX 1.36% m / m Propylene glycol 21.5% m / m 2, 6-di-tert-butyl-4-methylphenol (BHT) 0.56% m / m The invention will now be described by way of example only and with reference to the accompanying examples that are for an acaricidal composition. A pharmaceutical composition according to the invention was produced by grinding together Amitraz, sodium carbonate and citric acid and then agglutinating the powder formed using propylene glycol. Sodium carbonate and citric acid together provide an effervescent disintegrant. The desired dispersants and surfactants were also added to the mixture. The resulting effervescent dosage form produced in this way is individually sealed with a film of aluminum or plastic sheet material. The following formulation was used: CONSTITUENT% m / m Deltamethrin 13.9 NaC03 12, 5 Citric acid monohydrate 7.3 ARKOPAL N90 2.4 WETTOL D2 1.2 Propylene glycol 26.4 A composition containing deltamethrin was produced in a similar manner. The following formulation was used: CONSTITUENT% m / m Amitraz 13.9 NaHCO3 22.2 Citric acid monohydrate 18.8 BAYKANOL SL 21.7? EKAL BX dry 1, 4 Propylene glycol 21.5 BHT 0.6 It has been observed that Effervescent dosage forms dissolve quickly, on average between 1.5 and 2 minutes in 10 liters of water. This makes them highly suitable for applications where rapid release is required. The material remained in suspension for 4 hours and after 20 hours it had precipitated. The concentration of Amitraz and deltamethrin, respectively, was the conventional one and was based on an effective concentration to control or eradicate acarids when the solid dosage form produced was dissolved in 10 liters of water.

It is conceived that the effervescent dosage forms can be used as a viable alternative to liquid and powder concentrates, thus mitigating at least partially some of the disadvantages associated with the use of the liquid and the powder. It is conceived that several effervescent dosage forms can be added to any suitable volume of water to produce sufficient pesticide for application to an animal, in which case an effervescent dosage form of the pesticide can be obtained in a bucket and applied with a sponge or sprayed on the animal, or on various animals, in which case several effervescent dosage forms of the pesticide may be dissolved in an immersion tank or in a spray sleeve reservoir. By varying the amount of the active ingredient and the excipients in a formulation it is possible to control the rate of dissolution of the solid dosage form. It will be understood that a wide variety of pesticides and additives may be used in the above invention without departing from the scope thereof. In particular, the active ingredient of the pesticide may be an acaricide as described or the pesticide may be directed to other ectoparasites. Alternatively, the active ingredient of the pesticide may be directed to a variety of endoparasites such as nematodes and cestodes to name but two. When the target is an endoparasite it is conceivable that the solid dosage form can be dissolved in water in a reservoir for an oral dosing gun. Importantly, any suitable effervescent composition can be used. In addition to the above, the active ingredient of the pesticide can also be a herbicide and the effervescent dosage form can be dissolved in water in a suitable reservoir shortly before it is applied.

Additionally, the active ingredient may also be a protein or a disinfectant, or any other pharmacologically active material. It is noted that in relation to this date, the best method known to the applicant to carry out the aforementioned invention, is that which is clear from the present description of the invention.

Claims

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CLAIMS Having described the invention as above, the content of the following claims is claimed as property: 1. A pharmaceutical composition characterized in that it comprises an active pesticidal composition contained in an effervescent dosage form. 2. A pharmaceutical composition according to claim 1, characterized in that it includes a carbonate or bicarbonate and an acid.
3. A pharmaceutical composition according to claim 1, characterized in that the carbonate is sodium carbonate or sodium bicarbonate.
4. A pharmaceutical composition according to claim 1, characterized in that the acid is citric acid.
5. A pharmaceutical composition according to any of the preceding claims, characterized in that it additionally includes at least one binder.
6. A pharmaceutical composition according to claim 15, characterized in that the binder is propylene glycol.
7. A pharmaceutical composition according to any of the preceding claims, characterized in that the active pesticidal composition is a herbicide. - -
8. A pharmaceutical composition according to any of claims 1 to 6, characterized in that the active pesticidal composition is suitable for controlling or eradicating mammalian pests.
9. A pharmaceutical composition according to claim 8, characterized in that the pesticide is suitable for controlling or eradicating ectoparasites.
10. A pharmaceutical composition according to claim 8, characterized in that the pesticide is an acaricide.
11. A pharmaceutical composition according to claim 10, characterized in that the acaricide belongs to the amidine group of pesticides.
12. A pharmaceutical composition according to claim 11, characterized in that the pesticide is amitraz.
13. A pharmaceutical composition according to claim 12, characterized in that the amitraz is present in the range of 20 to 60% m / m.
14. A pharmaceutical composition according to claim 13, characterized in that it comprises: from 20 to 60% m / m of amitraz, from 5 to 17% m / m of sodium carbonate, from 4 to 9% m / m of citric acid monohydrate, from 1 to 4% m / m of ARKOPAL N090, - - from 0.6 to 2% m / m of WETTOL D2, and from 10 to 40% m / m of propylene glycol.
15. A pharmaceutical composition according to claim 10, characterized in that the acaricide belongs to the pyrethroid group of pesticides.
16. A pharmaceutical composition according to claim 15, characterized in that the pesticide is deltamethrin.
17. A pharmaceutical composition according to claim 16, characterized in that the deltamethrin is present in the range of 10 to 20% m / m.
18. A pharmaceutical composition according to claim 17, characterized in that it comprises: from 12 to 16% m / m of deltamethrin, from 20 to 25% m / m of sodium bicarbonate, from 17 to 21% m / m of citric acid monohydrate, from 19 to 24% m / m of Baykanol SL, from 1.2 to 1.6% m / m of Nekal BX, from 19 to 24% m / m of propylene glycol and from 0.5 to 0.7% m / m of 2,6-di-tert-butyl-4-methylphenol (BHT).