WO2007031133A1 - Préparation pharmaceutique - Google Patents

Préparation pharmaceutique Download PDF

Info

Publication number
WO2007031133A1
WO2007031133A1 PCT/EP2006/006435 EP2006006435W WO2007031133A1 WO 2007031133 A1 WO2007031133 A1 WO 2007031133A1 EP 2006006435 W EP2006006435 W EP 2006006435W WO 2007031133 A1 WO2007031133 A1 WO 2007031133A1
Authority
WO
WIPO (PCT)
Prior art keywords
pharmaceutical composition
composition
pesticide
propylene glycol
citric acid
Prior art date
Application number
PCT/EP2006/006435
Other languages
English (en)
Inventor
Ernest Schay
Walter Wilhelm Focke
Lushane Walbrugh
Original Assignee
Bayer Healthcare Ag
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Bayer Healthcare Ag filed Critical Bayer Healthcare Ag
Priority to MX2008000499A priority Critical patent/MX2008000499A/es
Priority to BRPI0612872-6A priority patent/BRPI0612872A2/pt
Publication of WO2007031133A1 publication Critical patent/WO2007031133A1/fr

Links

Classifications

    • A—HUMAN NECESSITIES
    • A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N25/00—Biocides, pest repellants or attractants, or plant growth regulators, characterised by their forms, or by their non-active ingredients or by their methods of application, e.g. seed treatment or sequential application; Substances for reducing the noxious effect of the active ingredients to organisms other than pests
    • A01N25/12—Powders or granules
    • A01N25/14—Powders or granules wettable
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents

Definitions

  • This invention relates to a pharmaceutical composition and, more particularly, to a pharmaceutical composition in the form of a water-soluble solid dosage form.
  • herbicide shall have its widest 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 sold as a liquid concentrate in metal or plastic containers from which a desired quantity of the product is decanted before use.
  • Pesticides by their nature, are hazardous chemicals and disposal of empty pesticide containers is a problem as the containers usually contain a pesticide residue which can leach into the environment with disastrous consequences. To an extent, similar problems can be experienced with full or partially full containers, particularly metal containers or plastic containers that have stripped cap screws. Also, containers frequently fall and break during transport.
  • a pharmaceutical composition comprising an active pesticidal composition contained in an effervescent dosage form.
  • composition to include an acid, preferably citric acid and a carbonate or bicarbonate, preferably an alkali carbonate like sodium carbonate or an alkali bicarbonate like sodium bicarbonate.
  • an acid preferably citric acid and a carbonate or bicarbonate, preferably an alkali carbonate like sodium carbonate or an alkali bicarbonate like sodium bicarbonate.
  • the active pesticidal composition is a herbicide.
  • the active pesticidal composition is suitable for controlling or eradicating mammalian pests, preferably ectoparasites and further preferably an accaricide.
  • the accaricide to belong to the amidine group of pesticides, preferably amitraz.
  • the accaricide 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 methylene-linked condensation product of arylsulphonic acids, preferably Baykanol SL and/or a sodium salt of alkylnaphthalenesulphonate, preferably Nekal BX, and/or a non ionic surfactant belonging to the nonylphenol ethoxylate group, preferably ARKOPAL N090.
  • arylsulphonic acids preferably Baykanol SL and/or a sodium salt of alkylnaphthalenesulphonate, preferably Nekal BX
  • a non ionic surfactant belonging to the nonylphenol ethoxylate group preferably ARKOPAL N090.
  • compesition according to the present invention may include one or more of the following ingredients:
  • At least one suitable dispersant preferably a sodium salt of the condensation product of naphthalene sulphuric acid, in particular WETTOL D2;
  • antioxidant preferably butylated hydroxytoluene (BHT).
  • concentrations of the ingredients in the composition are in the following ranges:
  • concentration of the active ingredient in the composition will vary according to the required effective concentration and 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.
  • the pharmaceutical composition to include at least one suitable dispersant, and/or at least one disintegrant, and/or at least one surfactant, and/or at least one binder; for the dispersant to be a sodium salt of the condensation product of naphthalene sulphuric acid, preferably WETTOL D2; for the disintegrant to be sodium starch glycolate; for the surfactant to be a non ionic surfactant belonging to the nonylphenol ethoxylate group, preferably ARKOPAL N090; and for the binder to be propylene glycol.
  • the dispersant to be a sodium salt of the condensation product of naphthalene sulphuric acid, preferably WETTOL D2
  • the disintegrant to be sodium starch glycolate
  • the surfactant to be a non ionic surfactant belonging to the nonylphenol ethoxylate group, preferably ARKOPAL N090
  • the binder to be propylene glycol.
  • the composition to include amitraz, sodium carbonate, citric acid monohydrate, ARKOPAL N090, WETTOL D2 and propylene glycol; for the constituents to be present in the following ranges (%m/m in the final composition):
  • the composition to include deltamethrin, sodium bicarbonate, citric acid monohydrate, Baykanol SL (methylene- linked condensation product of arylsulphonic acids), Nekal BX (sodium salt of alkylnaphthalene- sulphonate), propylene glycol and 2,6-di-tert.-butyl-4-methylphenol (BHT); for the constituents to be present in the following ranges (%m/m, based on the final composition)
  • BHT 2,6-Di-tert.-butyl-4-methylphenol
  • Citric acid monohydrate 18.8 %m/m
  • Nekal BX 1.36 %m/m Propylene glycol 21.5 %m/m
  • BHT 2,6-Di-tert.-butyl-4-methylphenol
  • a pharmaceutical composition according to the invention was produced by milling together Amitraz, sodium carbonate and citric acid and then binding the powder formed using propylene glycol.
  • the sodium carbonate and citric acid together provide an effervescent disintegrant. Desired dispersants and surfactants were also added to the mixture.
  • the resultant effervescent dosage form so produced is individually sealed with a plastics or foil material film.
  • the following formulation was used:
  • composition containing deltamethrin was produced.
  • the following formulation was used:
  • the effervescent dosage forms have been found to dissolve rapidly, on average between 1.5 and 2 minutes in 10 litres;pf 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 were standard and based on an effective concentration to control or eradicate accarinids when the solid dosage form produced was dissolved on 10 litres of water.
  • the effervescent dosage forms can be used as a viable alternative to liquid and powder concentrates thus, at least partly, alleviating some of the disadvantages associated with the use of the liquid and powder. It is envisaged that a number of effervescent dosage forms can be added to any suitable volume of water to make up enough pesticide for application to one animal, in which case one effervescent dosage form of the pesticide can be made up in a bucket and sponged or sprayed onto the animal, or to several animals, in which case several effervescent dosage forms of the pesticide can be dissolved in a dip tank or in a spray race reservoir. By varying the amount of active ingredient and excipients in a formulation it is possible to control the dissolution rate of the solid dosage form.
  • the pesticide active ingredient can be an accaricide as described or the pesticide may target other ectoparasites.
  • the pesticide active ingredient may target a variety of endoparasites such as nematodes and cystodes to name but two.
  • the target is an endoparasite it is envisaged that the solid dosage form can be dissolved in water in a reservoir for an oral dosing gun.
  • any suitable effervescent composition can be used.
  • the pesticide active ingredient may also be a herbicide and the effervescent dosage form dissolved in water in a suitable reservoir shortly before it is applied. Additionally, the active ingredient may also be a protein or disinfectant, or any other pharmacologically active material.

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Toxicology (AREA)
  • Engineering & Computer Science (AREA)
  • Dentistry (AREA)
  • Wood Science & Technology (AREA)
  • Zoology (AREA)
  • Environmental Sciences (AREA)
  • Pest Control & Pesticides (AREA)
  • Agronomy & Crop Science (AREA)
  • Chemical & Material Sciences (AREA)
  • Plant Pathology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)
  • Medicinal Preparation (AREA)

Abstract

La présente invention concerne une préparation pharmaceutique qui comprend une formule pesticide active sous une forme galénique effervescente.
PCT/EP2006/006435 2005-07-14 2006-07-01 Préparation pharmaceutique WO2007031133A1 (fr)

Priority Applications (2)

Application Number Priority Date Filing Date Title
MX2008000499A MX2008000499A (es) 2005-07-14 2006-07-01 Composicion farmaceutica.
BRPI0612872-6A BRPI0612872A2 (pt) 2005-07-14 2006-07-01 composição farmacêutica

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
ZA2005/5664 2005-07-14
ZA200505664 2005-07-14

Publications (1)

Publication Number Publication Date
WO2007031133A1 true WO2007031133A1 (fr) 2007-03-22

Family

ID=37076077

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2006/006435 WO2007031133A1 (fr) 2005-07-14 2006-07-01 Préparation pharmaceutique

Country Status (5)

Country Link
AR (1) AR055352A1 (fr)
BR (1) BRPI0612872A2 (fr)
MX (1) MX2008000499A (fr)
WO (1) WO2007031133A1 (fr)
ZA (1) ZA200800392B (fr)

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0415569A2 (fr) * 1989-09-01 1991-03-06 Zeneca Limited Compositions agrochimiques
WO1991003936A1 (fr) * 1989-09-15 1991-04-04 Auchincloss Thomas R Compositions effervescentes
EP0480679A1 (fr) * 1990-10-11 1992-04-15 Sumitomo Chemical Company, Limited Composition pesticide
US6071539A (en) * 1996-09-20 2000-06-06 Ethypharm, Sa Effervescent granules and methods for their preparation

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0415569A2 (fr) * 1989-09-01 1991-03-06 Zeneca Limited Compositions agrochimiques
WO1991003936A1 (fr) * 1989-09-15 1991-04-04 Auchincloss Thomas R Compositions effervescentes
EP0480679A1 (fr) * 1990-10-11 1992-04-15 Sumitomo Chemical Company, Limited Composition pesticide
US6071539A (en) * 1996-09-20 2000-06-06 Ethypharm, Sa Effervescent granules and methods for their preparation

Also Published As

Publication number Publication date
ZA200800392B (en) 2009-04-29
MX2008000499A (es) 2008-03-07
AR055352A1 (es) 2007-08-22
BRPI0612872A2 (pt) 2010-11-30

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