Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Biocides; animal or insect repellents or attractants
Reexamination Certificate
1998-02-24
2002-04-30
Levy, Neil (Department: 1616)
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Biocides; animal or insect repellents or attractants
C424S405000, C424S459000, C514S557000, C514S939000
Reexamination Certificate
active
06379688
ABSTRACT:
TECHNICAL FIELD OF THE INVENTION
The present invention relates to a preservative for emulsion, said preservative containing sorbic acid or a pharmaceutically acceptable salt thereof and exhibiting superior preservation effect at a low concentration, and to an emulsion containing said compound or a preservative for emulsion containing said compound, along with an active ingredient, which can be administered safely to humans. The present invention further relates to a method for preserving an emulsion, which comprises adding a sorbic acid or a pharmaceutically acceptable salt thereof to said emulsion. The present invention moreover relates to use of sorbic acid or a pharmaceutically acceptable salt thereof for the preservation of an emulsion, as well as to use of said compound for the production of an emulsion and a preservative for emulsion.
BACKGROUND OF THE INVENTION
When formulating a drug into an eye drop, a nasal drop or an ear drop, a preservative is added to eliminate a secondary contamination with microorganisms present in the air, lacrimal fluid, meatus nasi, external auditory meatus and the like. The same applies to an emulsion. Thus, paraoxybenzoate, benzalkonium chloride and the like are generally added as a preservative when formulating a drug into an emulsion. However, such conventional preservatives cannot provide an emulsion, particularly an oil in water type (o/w type) emulsion, with a sufficient preservation effect. In addition, when a dispersion medium has a relatively high pH, microorganisms tend to proliferate, further reducing the preservation effect. Nevertheless, an increased amount of a preservative for a higher preservation effect is associated with possible side effects such as greater irritation etc. to the living body due to the high concentration preservative.
Thus, there is a dilemma as to whether to add a preservative at a high concentration to increase preservation effect or limit the amount to be added to avoid side effects caused by the high concentration preservative, when formulating a drug into an emulsion. Therefore, development of a preservative capable of imparting a superior preservation capability to an emulsion at a low concentration has been demanded.
SUMMARY OF THE INVENTION
It is therefore an object of the present invention to provide a compound capable of imparting a superior preservation capability to an emulsion even when added at a low concentration, particularly an oil in water type (o/w type) emulsion, among others, an oil in water type emulsion comprising a dispersion medium having a high pH, and a preservative for emulsion containing said compound.
Another object of the present invention is to provide an emulsion containing said compound or said preservative, which has superior preservation effect and which can be administered safely to humans, particularly an emulsion for an eye drop, a nasal drop and an ear drop.
As a result of intensive studies in an attempt to solve the above-mentioned problems, it has now been found that the addition of sorbic acid or a pharmaceutically acceptable salt thereof to an emulsion leads to a high preservation effect of the emulsion, even when the concentration thereof is low. It has also been found that, when the emulsion has a high pH, the addition, at a low concentration, of sodium edetate and boric acid along with the sorbic acid or a pharmaceutically acceptable salt thereof also leads to a more superior preservation effect of the emulsion.
In one aspect, the present invention provides a preservative for emulsion which contains sorbic acid or a pharmaceutically acceptable salt thereof, particularly such preservative for emulsion which contains said compound at a concentration of 0.001-5 w/v %, preferably 0.01-1 w/v %; further, the above-mentioned preservative for emulsion which contains, in addition to said compound, sodium edetate and boric acid, particularly said preservative for emulsion which contains sodium edetate at a concentration of 0.001-0.2 w/v %, preferably 0.005-0.1 w/v %, and boric acid at a concentration of 0.001-10 w/v %, preferably 0.01-5 w/v %; and further, the above-mentioned preservative for emulsion which is in the dosage form of an eye drop, a nasal drop or an ear drop.
In another aspect, the present invention provides an emulsion which contains sorbic acid or a pharmaceutically acceptable salt thereof, or a preservative for emulsion containing said compound, together with an active ingredient and a pharmaceutically acceptable carrier, particularly, the above-mentioned emulsion containing sorbic acid or a pharmaceutically acceptable salt thereof at a concentration of 0.001-5 w/v %, particularly 0.01-1 w/v %; further, an emulsion comprising a preservative containing sorbic acid or a pharmaceutically acceptable salt thereof, sodium edetate and boric acid, together with an active ingredient and a pharmaceutically acceptable carrier, or an emulsion comprising a preservative containing sorbic acid or a pharmaceutically acceptable salt thereof, sodium edetate and boric acid, together with an active ingredient and a pharmaceutically acceptable carrier; particularly, the above-mentioned emulsion containing sorbic acid or a pharmaceutically acceptable salt thereof at a concentration of 0.001-5 w/v %, preferably 0.01-1 w/v %, sodium edetate at a concentration of 0.001-0.2 w/v %, preferably 0.005-0.1 w/v %, and boric acid at a concentration of 0.001-10 w/v %, particularly 0.01-5 w/v %; and further, the above-mentioned emulsion which is in the dosage form of an eye drop, a nasal drop or an ear drop.
In another aspect, the present invention provides a commercial package containing a preservative for emulsion containing sorbic acid or a pharmaceutically acceptable salt thereof, and, where necessary, sodium edetate and boric acid, along with a pharmaceutically acceptable carrier, and a package insert stating that said preservative is useful for the preservation of the emulsion; and a commercial package comprising either an emulsion containing sorbic acid or a pharmaceutically acceptable salt thereof, and, where necessary, sodium edetate and boric acid, together with an active ingredient and a pharmaceutically acceptable carrier, or a preservative for emulsion containing sorbic acid or a pharmaceutically acceptable salt thereof, and, where necessary, sodium edetate and boric acid, together with an active ingredient and a pharmaceutically acceptable carrier, and a package insert stating that sorbic acid, a pharmaceutically acceptable salt thereof and the combination of said compound, sodium edetate and boric acid are useful for the preservation of an emulsion.
Also, the present invention provides a preservation method of an emulsion, which comprises adding sorbic acid or a pharmaceutically acceptable salt thereof to an emulsion at a concentration pharmaceutically acceptable and effective for the preservation of the emulsion, particularly, sorbic acid or a pharmaceutically acceptable salt thereof at a concentration of 0.001-5 w/v %, preferably 0.01-1 w/v %. The present invention further provides a preservation method of an emulsion, which comprises adding sorbic acid or a pharmaceutically acceptable salt thereof, sodium edetate and boric acid to an emulsion at concentrations pharmaceutically acceptable and effective for the preservation of the emulsion, particularly, sorbic acid or a pharmaceutically acceptable salt thereof at a concentration of 0.001-5 w/v %, preferably 0.01-1 w/v %, sodium edetate at a concentration of 0.001-0.2 w/v %, preferably 0.005-0.1 w/v %, and boric acid at a concentration of 0.001-10 w/v %, preferably, 0.01-5 w/v %. The present invention is a preservation method of the above-mentioned emulsion in the dosage form of an eye drop, a nasal drop or an ear drop.
The present invention also provides use of sorbic acid or a pharmaceutically acceptable salt thereof for the preservation of an emulsion, particularly, use comprising adding sorbic acid or a pharmaceutically acceptable salt thereof at a concentration of 0.001-5 w/v %, particularly 0.01-1 w/v %. Further, t
Inada Katsuhiro
Yamaguchi Masayo
Yamaguchi Masazumi
Levy Neil
Senju Pharmaceutical Co. Ltd.
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