AU2006235798B2 - Topical composition - Google Patents

Topical composition Download PDF

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Publication number
AU2006235798B2
AU2006235798B2 AU2006235798A AU2006235798A AU2006235798B2 AU 2006235798 B2 AU2006235798 B2 AU 2006235798B2 AU 2006235798 A AU2006235798 A AU 2006235798A AU 2006235798 A AU2006235798 A AU 2006235798A AU 2006235798 B2 AU2006235798 B2 AU 2006235798B2
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AU
Australia
Prior art keywords
topical composition
chlorhexidine
topical
microorganism
salts
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AU2006235798A
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AU2006235798A1 (en
Inventor
Michael Lindsay Grayson
Suzanne Wendy Kirsa
Alan Douglas Shilson
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Austin Health
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Austin Health
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Priority to AU2006235798A priority Critical patent/AU2006235798B2/en
Publication of AU2006235798A1 publication Critical patent/AU2006235798A1/en
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  • Medicinal Preparation (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Cosmetics (AREA)

Description

AUSTRALIA
Patents Act 1990 COMPLETE SPECIFICATION STANDARD PATENT Applicant: Invention Title: AUSTIN HEALTH TOPICAL COMPOSITION The following statement is a full description of this invention, including the best method of performing it known to us: 00 2 The entire disclosure in the complete specification of our Australian Patent Application O No. 2003203452 is by this cross-reference incorporated oo into the present specification.
TECHNICAL FIELD 00 tt3 The present invention relates to topical CA compositions, which may be used as an antiseptic and/or
\O
disinfectant.
BACKGROUND
Control of nosocomial infection and exposure to infectious disease is of paramount concern to doctors, nurses, and clinicians that work in hospitals, clinics and surgical and medical centres. One of the most effective methods for controlling infection is regimented hand disinfection before and after each patient contact and before invasive procedures.
Hand disinfection is generally accomplished using anti-microbial soaps with water. These soaps are usually formulated to include either povidone-iodine or chlorhexidine gluconate as the active anti-microbial agent. In addition, these formulated soaps may contain surfactants and possibly low levels of humectants such as glycerin.
Hand disinfection is also accomplished using hand wash replacements. These are used instead of the soap and water scrub. Hand wash replacements ideally achieve bacterial kill equal to or better than a traditional soap N \Melborn\ca~es\Patenr\49000-49999\P49134. \Specia\P49134 .AU.1 *pecification 2008.1112.do 16/11/0 3 00 3 and water scrub and in a shorter period of time.
Additionally, they maintain or improve the skin's natural O barrier to microbial and chemical contamination while 00 providing acceptable tactile properties. Examples of hand wash replacements include hydroalcoholic gels, which generally include high levels of either ethanol or 00 C isopropanol as the disinfecting agent and also include a V) thickener and/or surfactant and optionally include a C humectant glycerin).
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C< SUMMARY The present invention provides a topical composition for application to any part of the body excluding mucous membranes, the topical composition comprising: isopropanol in an amount from about 65% v/v to about 70% v/v of the total concentration of the topical composition; chlorhexidine, one or more salts of chlorhexidine, or both chlorhexidine and one or more salts of chlorhexidine, in an amount of from about 4 g/L to about 7g/L of the topical composition; and polyethylene glycol in an amount of from about to about 1.8% of the total the concentration of the topical composition.
The present invention also provides a method of reducing and/or preventing the transmission of a microorganism by applying an effective amount of a topical composition as defined above to any part of the body excluding mucous membranes.
The topical composition as defined above may N:\eboue\Cas$e\Pactnt\490O-49999\P4S4 .4AU. 1\Specig\P49134 AU.1 opecificaLion 2008-i-12.doc 18/11/00 4 00 o therefore be used to reduce and/or prevent the transmission of a microorganism.
O
The topical composition may also be used in the 00 manufacture of a disinfectant and/or antiseptic to reduce and/or prevent the transmission of a microorganism.
00 The microorganism is preferably a multi- Ci resistant organism such as, for example, methicillian- S 10 resistant staphylococcus aureus.
The topical composition may be applied before and after routine or specialised health-care delivery or preparatory to invasive procedures.
An effective amount of the topical composition is preferably about 1 ml to about 3 ml.
The present invention further provides a method of preparing a topical composition as defined above comprising the step of mixing isopropanol, chlorhexidine, one or more salts of chlorhexidine, or both chlorhexidine and one or more salts of chlorhexidine, and polyethylene glycol, with stirring, until complete homogenisation is achieved.
DETAILED DESCRIPTION The present invention relates to topical compositions comprising an alcohol, an anti-microbial, and an emollient.
N:\MoIbo-ne\Case\Paen\49O0-4999\P4914.AU.\Specia\P49134.AU.1 epecMc8Lton 2DOB-11-12.d6c 1$/11/08 5 00 Alcohols O Alcohol is an effective vehicle for a disinfectant. It provides a broad spectrum bactericidal 00 effect and is fast drying.
00 Alcohols may include straight or branched chain i alcohols. Suitable C 1 to C 4 alkanols include ethanol, n- Ci propanol and isopropanol.
IND
CA While topical compositions may comprise only one alcohol, a combination of alcohols may be used.
Isopropanol is a good disinfectant with a pleasant odour and, compared to other alcohols, it has a less cutaneous drying effect of the skin. Therefore, isopropanol is the alcohol used in the topical composition of the present invention.
The alcohol concentration of the topical composition should provide the greatest possible bacterial kill effect. Therefore, the alcohol concentration is preferably about 65% v/v to about 75% v/v, more preferably about 70% v/v, of the total concentration of the topical composition.
Anti-microbials The term "anti-microbials" is used herein in its broadest sense and refers to any agent that can treat any infection caused by a microorganism and includes viral and bacterial infections. Examples of such infectious microorganisms may be found in a number of well known N:\Melbourn\Ca~e.\Patenr\49DOO-49999\P49134.AU. 1\Speci\P49134.AU specification 2008-1-12.doc 11/11/08 6 00 6 texts such as 'Medical Microbiology' (Greenwood, D., Slack, Peutherer, Churchill Livingstone Press, O 2002); 'Mims' Pathogenesis of Infectious Disease' (Mims, Nash, Stephen, Academic Press, 2000); 00 '"Fields" Virology. (Fields, Knipe, Howley, Lippincott Williams and Wilkins, 2001).
00 SChlorhexidine and its salts are is an anti- CA microbial effective against a wide-range of Gram-positive
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and Gram-negative bacteria.
While chlorhexidine may be used as an antimicrobial in the topical composition of the present invention, a salt of chlorhexidine is preferred due to its solubility properties. Preferred salts of chlorhexidine include chlorhexidine gluconate, chlorhexidine acetate and chlorhexidine hydrochloride. The most preferred antimicrobial for the topical composition of the present invention is chlorhexidine gluconate because it has excellent instantaneous bacterial effect that persists after use.
The amount of anti-microbial present in the topical composition should provide a balance between the desired antibacterial effect and unwanted adverse effects.
The anti-microbial is preferably present in an amount of about 4 g/L to about 7 g/L, more preferably about 5 g/L of the topical composition.
While a single anti-microbial may be used in the topical composition of the present invention, additional anti-microbials may be added to enhance the anti-microbial N;\Meoboeurn\ Ca.. \Patnt\49OO- -4999\P4934AU.1\SpPcli\P49134.AU.1 specification 200811-12.dc 1/11/0 7 00 9 action of the topical composition. This may be particularly desirable in critical uses such as 00 O preparatory to invasive procedures.
Emollients 00 h Emollients are typically added to topical V) compositions because they act to increase the moisture Cl content of the stratum corneum.
CI Emollients are generally separated into two broad classes based on their function. The first class of emollients function by forming an occlusive barrier to prevent water evaporation from the stratum corneum. The second class of emollients penetrate into the stratum corneum and physically bind water to prevent evaporation.
The first class of emollients is subdivided into compounds that are waxes at room temperature and compounds that are liquid oils. The second class of emollients includes those that are water-soluble and are often referred to as humectants.
Emollients may be selected from the following non-limiting list of general emollients, occlusive emollients and humectants.
Examples of general emollients include short chain alkyl or aryl esters (C 1
-C
6 of long straight or branched chain alkyl or alkenyl alcohols or acids (C 8
-C
32 and their polyethoxylated derivatives; short chain alkyl or aryl esters (CI-C 6 or C 4
-C
12 diacids or diols optionally substituted in available positions by -OH; alkyl or aryl
C
1 -Cio esters of glycerol, pentaerythritol, ethylene N:\Mlbourne\Cames\Patent\49000-49999\P49134.AU.I\SpCi.\P49134 AU I specification 200-11.12.doc 18/11/08 8 00 glycol, propylene glycol, as well as polyethoxylated derivatives of these and polyethylene glycol; C 12
-C
22 alkyl O esters or ethers of polypropylene glycol; C 12
-C
22 alkyl esters or ethers of polypropylene glycol/polyethylene 00 glycol copolymer; and polyether polysiloxane copolymers.
00 h Examples of occulsive emollients include cyclic n3 and linear dimethicones, polydialkysiloxanes, Ci polyaryl/alkylsiloxanes, long chain (C 8
-C
36 alkyl and C 10 alkenyl esters of long straight or branched chain alkyl or CI alkenyl alcohols or acids; long chain (C 8
-C
36 alkyl and alkenyl amides of long straight or branched chain alkanes and alkenes such as squalene, squalane and mineral oil; jojoba oil polysiloxane polyalkylene copolymers, dialkoxy dimethyl polysiloxanes, short chain alkyl or aryl esters
(CI-C
6 of C 12
-C
22 diacids or diols optionally substituted in available positions by -OH, such as diisostearyl dimer dilinoleate; lanolin and lanolin derivatives, and beeswax and its derivatives.
Examples of humectant type emollients include glycerol, propylene glycol, dipropylene glycol, polypropylene glycol, polyethylene glycol, sorbitol, pantothenol, gluconic acid salts and the like.
A humectant type emollient is preferred for the topical composition of the present invention. The most preferred humectant is polyethylene glycol. Polyethylene glycol is pleasant to use, readily available and economical.
The concentration of the emollient in the topical composition is preferably about 1.5% to about N. \MeI bourn\Ca Patent\4900-4999 9\P4914 AU. 1\Specia\F49134 AU. I specificatio 2000-11-12 .do 18/11108 00 more preferably about
(N
O The inventors have determined that having a oo concentration of polyethylene glycol in the topical composition of the present invention provides adequate moisturising while not causing irritation and/or allergic 00 h reactions. There are also no unwanted abnormal feelings V after application such as sliminess or stickiness.
cN S 10 Additional ingredients
(N
The topical composition may optionally comprise ingredients such as water, oils, salts, fragrances, perfumes, colorants, stabilisers, emulsifiers, propellants, additives, preservatives or preserving agents, anti-oxidants, surfactants, thickeners and other excipients normally used in topical compositions. If additional ingredients are included in the topical composition, ingredients that are known to cause skin irritation and/or sensitisation reactions should be avoided.
Formulations The topical composition may be formulated into the form of an aerosol, balm, cream, emolument, foam, gel, liniment, lotion, ointment, salve, solution, spray, suspension, unguent or the like.
Application The present invention is a topical composition, which is useful as a broad-spectrum antiseptic and/or N;\Wlbourne\Caoes\Patent\49000-49999NP4913 .*U.1\Spaciig\P4913 .AU.1opecific.Lion 2008-11-132Oo 1/11/08 10 00 Sdisinfectant for use in many environments including hospitals and clinics, veterinarian, industrial, food 0 industry, livestock and home environments. The topical O0 composition may be used, for example, as a skin disinfectant.
00 C The topical compositions of the present invention V) are highly efficacious in preventing the transmission of Cl microorganisms within hospitals.
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CI The term "microorganism" includes any microscopic organism or taxonomically related macroscopic organism within the categories algae, bacteria, fungi, protozoa, viruses and subviral agents or the like. The microorganism is preferably a multi-resistant organism such as, for example, methicillian-resistant staphylococcus aureus.
In addition, preferred topical compositions of this invention maintain moisture after both single and multiple applications without allergic reaction or unwanted side effects such as abnormal feelings of sliminess or stickiness.
Topical compositions of the present invention are suitable for frequent and repeated usage during routine and specialised health-care delivery in environments such as hospital or clinic. In hospitals and clinics, these topical compositions may be used before and after each patient contact or preparatory to invasive procedures.
If topical compositions of the present invention N:\Mlbourne\Cages\Patent\49000-49999\P4914AU.1\Specia\P49134 AU.1 ,peCification 2008.11-12.do 10/111/0 11 00 are formulated into a hand lotion, only a small amount, about 1 ml to about 3 ml, of the hand lotion would be O needed to be effective disinfectant and/or antiseptic.
z 00 Topical compositions of the present invention have advantages over known topical compositions in that 00 they may be applied frequently with minimal adverse Seffects, dry rapidly, provide both instantaneous and Ci prolonged anti-microbial activity, and have a low toxicity
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profile.
The term "topical composition" as used herein generally refers to a composition that is applied externally to any part of the body excluding mucous membranes such as the eyes, mouth, and so on. The topical composition may, therefore, be applied directly to any part of the body excluding mucous membranes such as the eyes, mouth, and so on. However, topical compositions of the present invention may also be incorporated into sponges, swabs, pads and/or wipes, which are then used to apply the topical solution to any part of the body excluding mucous membranes such as the eyes, mouth, and so on. The topical compositions may also be incorporated into cosmetic products.
Stability The topical composition of the invention conserves its activity for, at least, two years from its production. However, it is preferable to use it at least within 12 months of being prepared. Even so, incorporating appropriate preserving agents can extend the period to sustain activity.
N lbourne\Ca~\Pat 9000-9999 AU.\SpCi\P49134AU I specifiction 008-11-12.doc 18/11/08 12 00 In this specification, except where the context 0 requires otherwise, the words "comprise", "comprises", and OO "comprising" mean "include", "includes", and "including", respectively, i.e. when the invention is described or defined as comprising specified features, various 00 C embodiments of the same invention may also include V additional features.
cN 0 10 EXAMPLES The invention will now be further described with reference to the following Examples. These Examples are not intended to limit the invention in any way.
The topical composition of the present invention may be prepared by a variety of techniques.
One method of preparing the topical composition of the present invention involves mixing the components of the topical composition, in suitable quantities, with stirring, until complete homogenisation is achieved.
The following examples are topical compositions of the present invention that were prepared according to the above method.
Example 1 isopropyl alcohol 70% v/v chlorhexidine gluconate 5 g/L polyethylene glycol 1.5% concen.
water balance bvlourne\C~aoae$\l'ent\4900.49999\P49134AU.1\Speci.\P49134.AU.1 Spoci-icion 2008-11-12.doc 18/11/08 13 00 The topical composition of Example 1 was 0 formulated into the form of a lotion, in particular a hand lotion.
The hand lotion was shown to be an effective 00 C disinfectant and/or antiseptic. It was also gentle on the V) skin, dried rapidly and provided both instantaneous and C prolonged anti-microbial activity. The hand lotion showed
\O
0 10 no unwanted side effects such as abnormal feelings of CI sliminess or stickiness.
The hand lotion of Example 1 was also trialed as a disinfectant hand lotion in an intervention/study ward of the Austin Repatriation Medical Centre, Victoria, Australia.
The trial was conducted over a period of ten or so months.
The staff of the intervention/study ward were instructed to use about 1 ml to about 3 ml of the disinfectant hand lotion before and after each patient contact.
The results of the trial showed that there was an approximately 21% to 25% reduction in clinical infections with methicillian-resistant staphylococcus aureus ("MRSA").
Since the disinfectant hand lotion was easy to use, there was also a 25% to 100% improvement in hand hygiene compliance. Hand hygiene compliance refers to the N:\M lbourne\Cases\Patent\49000-49999\P49134.AU. \Speci\P49134AU.1 specifIcation 2008-11-12.dc 18/ /1108 00 14 00 p rates of hand washing, which in the present case would refer to the rates of use of the topical composition as a 0 disinfectant hand lotion.
00 Furthermore, there were no allergic reactions identified through repeated use of the hand lotion during 00 C the trial.
Ni, CA Accordingly, this trial showed that the topical composition of the present invention would be very C( effective as a disinfectant hand lotion in hospitals, clinics, surgical and medical centres and the like.
Example 2 isopropyl alcohol 70% v/v chlorhexidine gluconate 5 g/L polyethylene glycol 2.0% concen.
water balance The topical composition of Example 2 was formulated into the form of a lotion, in particular a hand lotion.
The hand lotion was shown to be an effective disinfectant and/or antiseptic. It was also gentle on the skin, dried rapidly and provided both instantaneous and prolonged anti-microbial activity.
The hand lotion was found, however, to have a slight unwanted after effect. Specifically, after repeated use of the hand lotion, there was a feeling of stickiness.
N ourne\C a\Pten 49999\P4 I\SpoCi.\P49134AU.1 opecifioaon 2008-11-12.d IA/11/08 00 15 00 It will be appreciated by persons skilled in the art that numerous variations and/or modifications may be O made to the invention as shown in the specific embodiments without departing from the spirit or scope of the 00 invention as broadly described. The present embodiments are, therefore, to be considered in all respects as 00 0 illustrative and not restrictive.
IO
0q N:\Mlbou\C.e.\Pp.eet\49OO-49999\P49134 .AU.1\Speci\P49134 .AU.1 specification 2008-11-12.doc 18/11/08

Claims (20)

  1. 2. A topical composition according to claim 1, wherein isopropanol is present in an amount of about v/v of the total concentration of the topical composition.
  2. 3. A topical composition according to claim 1 or claim 2, wherein the salt of chlorhexidine is selected from chlorhexidine gluconate, chlorhexidine acetate, and chlorhexidine hydrochloride.
  3. 4. A topical composition according to claim 3, wherein the salt of chlorhexidine is chlorhexidine gluconate.
  4. 5. A topical composition according to any one of claims 1 to 4, wherein chlorhexidine, one or more salts of chlorhexidine, or both chlorhexidine and one or more salts of chlorhexidine is present in an amount of about 5 g/L of N \eltbom\Case.\Patent490OO.49999\P49134AU. I\Speci9\P49134.AU.1 Bpecificatio 2008-11-12.doc 18/11/08 17 00 the total the concentration of the topical composition. O 6. A topical composition according to any one of z claims 1 to 5, wherein the polyethylene glycol is present 00 in an amount of about 1.5% of the total the concentration of the topical composition. 00 S7. A topical composition according to any one of Cl claims 1 to 6 further comprising water, oils, salts, S 10 fragrances, perfumes, colorants, stabilisers, emulsifiers, CI propellants, additives, preservatives or preserving agents, anti-oxidants, surfactants, thickeners, and/or other excipients normally used in topical compositions.
  5. 8. A topical composition according to any one of claims 1 to 7, wherein the topical composition is formulated into the form of an aerosol, balm, cream, emolument, foam, gel, liniment, lotion, ointment, salve, solution, spray, suspension, unguent, or the like.
  6. 9. A topical composition according to any one of claims 1 to 8, wherein the topical composition is incorporated into sponges, swabs, pads, and/or wipes.
  7. 10. A topical composition according to any one of claims 1 to 9, wherein the topical composition is incorporated into cosmetic products.
  8. 11. A method of reducing and/or preventing the transmission of a microorganism by applying an effective amount of a topical composition as defined in any one of claims 1 to 10 to any part of the body excluding mucous membranes. N.\MelboAe\CU\Paen49000-U9999\P.I apscification 2008-11.12 .doc 1111/08 18 00
  9. 12. The method according to claim 11, wherein the O microorganism is a multi-resistant organism. 00
  10. 13. The method according to claim 12, wherein the multi-resistant organism is methicillian-resistant 00 0 0 staphylococcus aureus. t-- CI 14. The method according to any one of claims 11 to 0 10 13, wherein the topical composition is applied before and C after routine or specialised health-care delivery or preparatory to invasive procedures. The method according to any one of claims 11 to 14, wherein an effective amount is about 1 ml to about 3 ml.
  11. 16. Use of a topical composition as defined in any one of claims 1 to 10 to reduce and/or prevent the transmission of a microorganism.
  12. 17. The use according to claim 16, wherein the microorganism is a multi-resistant organism.
  13. 18. The use according to claim 17, wherein the multi-resistant organism is methicillian-resistant staphylococcus aureus.
  14. 19. The use according to any one of claims 16 to 18, wherein the topical composition is used before and after routine or specialised health-care delivery or preparatory to invasive procedures. N:\M1elburn\Cas.\Ptent\4900-49999\P49134.AU. \SpeCi.\P49134AU.1 specification 2008-1-12.1dc 1811/08 19 00
  15. 20. The use according to any one of claims 16 to 19, wherein about 1 ml to about 3 ml of the topical 0 composition is used. 00
  16. 21. Use of a topical composition as defined in any one of claims 1 to 10 in the manufacture of a disinfectant 00 0 and/or antiseptic to reduce and/or prevent the ln transmission of a microorganism. cN
  17. 22. The use according to claim 21, wherein the Cl microorganism is a multi-resistant organism.
  18. 23. The use according to claim 22, wherein the multi-resistant organism is methicillian-resistant staphylococcus aureus.
  19. 24. A disinfectant and/or antiseptic comprising a topical composition as defined in any one of claims 1 to A method of preparing a topical composition as defined in any one of claims 1 to 10 comprising the step of mixing isopropanol, chlorhexidine, one or more salts of chlorhexidine, or both chlorhexidine and one or more salts of chlorhexidine, and polyethylene glycol, with stirring, until complete homogenisation is achieved.
  20. 26. A topical composition, a method of preparing the topical composition, methods and uses involving the topical composition, or a disinfectant hand lotion comprising the topical composition, substantially as herein described with reference to Example 1. N \Mebourn\Case,\Patent\49O-4999\P4914 .AU. \Speci.\P49134 AU.1 specificaion 2008-11-12.doe 18/11/08
AU2006235798A 2003-03-28 2006-11-01 Topical composition Expired AU2006235798B2 (en)

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AU2003203452A AU2003203452A1 (en) 2003-03-28 2003-03-28 Topical composition
AU2006235798A AU2006235798B2 (en) 2003-03-28 2006-11-01 Topical composition

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* Cited by examiner, † Cited by third party
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DE102004062775A1 (en) 2004-12-21 2006-06-29 Stockhausen Gmbh Alcoholic pump foam
CN105147829B (en) * 2015-08-28 2019-05-10 爱品尚客(北京)电子商务有限公司 A kind of maca externally applied spray

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5951993A (en) * 1995-06-22 1999-09-14 Minnesota Mining And Manufacturing Company Stable hydroalcoholic compositions
US6090395A (en) * 1995-06-22 2000-07-18 Minnesota Mining And Manufacturing Company Stable hydroalcoholic compositions
WO2001041556A1 (en) * 1999-12-06 2001-06-14 Københavns Universitet Method of using mapk4 and orthologues thereof to control plant disease resistance and plant growth

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5951993A (en) * 1995-06-22 1999-09-14 Minnesota Mining And Manufacturing Company Stable hydroalcoholic compositions
US6090395A (en) * 1995-06-22 2000-07-18 Minnesota Mining And Manufacturing Company Stable hydroalcoholic compositions
WO2001041556A1 (en) * 1999-12-06 2001-06-14 Københavns Universitet Method of using mapk4 and orthologues thereof to control plant disease resistance and plant growth

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AU2003203452A8 (en) 2010-04-29
AU2003203452A1 (en) 2004-10-14

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