Method for transferring one or more active ingredients...

Drug – bio-affecting and body treating compositions – Effervescent or pressurized fluid containing – Organic pressurized fluid

Reexamination Certificate

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Details

C424S043000, C424S464000, C424S485000, C424S078040, C514S052000, C514S912000, C128S200140, C239S338000

Reexamination Certificate

active

06461592

ABSTRACT:

BACKGROUND OF THE INVENTION
1. Field of the Invention
The present invention relates to a method for controlling administration, particularly to a method for transferring one or more active ingredients between different phase carriers.
2. Description of Related Art
U.S. Pat. No. 5,698,533 discloses “Ophthalmic Pharmaceutical Composition”, which provides a method of administering a drug to an eye including the steps of: (a) admixing a pharmaceutically acceptable hydrocarbonaceous semi-solid or oil which contains the drug with water at a temperature above the melting point of the semi-solid or oil; and (b) nebulizing the admixture to form liquid drops; and (c) applying the liquid drops to the eye.
SUMMARY OF THE PRESENT INVENTION
It is an object of the present invention to provide a method, which enables one or more active ingredients to be conveniently transferred between different phase carriers, so that the active ingredient can be stored and used optionally.
It is another object of the present invention to provide a method, which enables one or more active ingredients to be transferred between different phase carriers. For example, the active ingredient unstable in water can be stored in an oil phase carrier (oil phase) or non-aqueous liquid phase carrier to keep the active ingredient stable. When desired to use, then the active ingredient can be transferred to water or water solution (aqueous phase carrier), and then be transferred to liquid fine drops (vapor phase).
It is the other object of the present invention to provide a method, which enables one or more active ingredients stored in a solid phase carrier (solid phase) to be transferred to an aqueous phase carrier, and then be transferred to liquid fine drops (vapor phase).
One aspect of this invention relates to a method for transferring one or more active ingredients between different phase carriers comprising the steps of: (a) providing a solid, semi-solid, or non-aqueous liquid drug which contains at least one active ingredient; (b) admixing said drug with water or water solution to form an admixture; and (c) nebulizing said admixture to form liquid fine drops containing said active ingredients.
The aforesaid solid drug can be a solid active ingredient (or active ingredients) without a carrier, or an active ingredient (or active ingredients) mixed with a solid carrier. The solid drug can be in the form of powder, granule, tablet or capsule, wherein the powder is preferred. In order to control the amount of the active ingredient in the powder, a solid powdered diluent can be added. The solid powdered diluent can be selected from the group consisting of dicalcium phosphate, calcium sulfate, lactose, kaolin, sodium chloride, dry starch, and powdered sugar.
The aforesaid semi-solid drug can be an active ingredient (or active ingredients) mixed with a grease, fat or wax carrier.
The aforesaid non-aqueous liquid drug can be an active ingredient (or active ingredients) stored in a non-aqueous liquid carrier such as oil phase carrier, alcohol carrier, or other organic carriers. The oil phase carrier is not limited here, but must enable the active ingredient to remain stable therein. The oil phase carrier can be animal oil (for example: lanolin), plant oil (for example: olive oil, corn oil, soybean oil), or mineral oil.
There is no special limitation on the water solution of step (b). Example of the water solution is an aqueous solution containing active ingredients.
The drug of the present invention can be contained one or more active ingredients. The active ingredient is selected from the group consisting of ophthalmic agents, dermal agents (including cosmetic agents), ENT (ear, nose and throat) agents, and respiratory agents.
The ophthalmic agents can be selected from the group consisting of vitamins, steroids (e.g. betamethasone, or dexamethasone), cephalosporins (e.g. cephradine, or cephalexin), penicillins (e.g. amoxicillin, or ampicillin), tetracyclines (e.g. chlorotetracycline, or demeclocycline), macrolides (e.g. erythromycin base, erythromycin propionate), aminoglycosides (e.g. gentamicin, tobramycin or neomycin), sulfonamides (e.g. sulfamethomidin, sulfamethoxypyridazine), polypetides (e.g. bacitracin) and naphazoline hydrochloride.
The dermal agents can be selected from the group consisting of vitamins, steroids (e.g. betamethasone, or dexamethasone), cephalosporins (e.g. cephradine, or cephalexin), penicillins (e.g. amoxicillin, or ampicillin), tetracyclines (e.g. chlorotetracycline, or demeclocycline), macrolides (e.g. erythromycin base, erythromycin propionate), aminoglycosides (e.g. gentamicin, tobramycin or neomycin), sulfonamides (e.g. sulfamethomidin, sulfamethoxypyridazine), polypetides (e.g. bacitracin) hydroquinone, piroxicam, and indomethacin.
The ENT (ear, nose and throat) agents can be selected from the group consisting of vitamins, steroids (e.g. betamethasone, or dexamethasone), cephalosporins (e.g. cephradine, or cephalexin), penicillins (e.g. amoxicillin, or ampicillin), tetracyclines (e.g. chlorotetracycline, or demeclocycline), macrolides (e.g. erythromycin base, erythromycin propionate), aminoglycosides (e.g. gentamicin, tobramycin or neomycin), sulfonamides (e.g. sulfamethomidin, sulfamethoxypyridazine), polypetides (e.g. bacitracin), naphazoline hydrochloride, and acetylcysteine.
The respiratory agents can be selected from the group consisting of vitamins, steroids (e.g. betamethasone, or dexamethasone), cephalosporins (e.g. cephradine, or cephalexin), penicillins (e.g. amoxicillin, or ampicillin), tetracyclines (e.g. chlorotetracycline, or demeclocycline), macrolides (e.g. erythromycin base, erythromycin propionate), aminoglycosides (e.g. gentamicin, tobramycin or neomycin), sulfonamides (e.g. sulfamethomidin, sulfamethoxypyridazine), polypetides (e.g. bacitracin), ephedrine sulfate, methylephedrine, acetylcysteine, isoproterenol sulfate, and aminophylline.
In order to transfer the active ingredient into water after the drug is mixed with water or water solution to form the admixture in the step (b), it may be necessary to stir, oscillate, or heat the admixture.
The nebulizer is a wellknown device and is easily obtained and operated by one skilled in the art. In the present invention, the nebulizer is used for providing energy to oscillate water and form a liquid fine drops escaping from the surface of the admixture (active ingredient with water or water solution). The temperature of the nebulized fine drops of liquid was about 25° C. The active ingredient of the admixture can be brought out with liquid fine drops to achieve the object of controlling drug delivery.
DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENTS
The characteristic of the present invention is the transfer of active ingredients. The method provided in the present invention enables one or more active ingredients stored in a carrier in a certain phase (such as an oil phase carrier, a grease phase carrier, or a solid phase carrier) to transfer into an admixture (water or water solution phase). Then, the active ingredient can be brought out with liquid fine drops (vapor phase) from the admixture by means of ultrasonic vibration.
The present invention can be applied in many situations. For example, the active ingredient (e.g. cephalosporin, vitamin C, or penicillin, etc) unstable in water can be stored in an oil phase carrier, a grease phase carrier, or a solid phase carrier to form a non-aqueous drug to keep the active ingredient stable. When desired to use, then the drug can be mixed with water or water solution to form an admixture. The admixture was then placed in a nebulizer to form fine drops of liquid. The nebulized fine drops of liquid can then be easily and smoothly delivered to the patient's body by gentle currents of air (e.g. provided by a fan installed in the nebulizer).
In general, the oil phase carrier or the grease phase carrier in the admixture is not brought out with liquid fine drops. Only the active ingredient is brought out with liquid fine drops. The method of the present invention enables an active i

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