JPH09143096A - Medicinal composition for viral disease - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain a medicinal composition with high bioavailability, and useful for the treatment of, onset prevention or infection prevention for, viral diseases such as herpes zoste and herpes simplex, containing an antiviral agent and a polyhydric alcohol. SOLUTION: This medicinal composition contains (A) pref. 0.1-10wt.% of an antiviral agent such as acyclovir, gancticlovir, sorivudine, bromovinyl deoxyuridine, azidothymidine, dideoxythymidine, dideoxyinosine or arabinosyladenine and (B) pref. 0.1-20wt.% of a polyhydric alcohol such as propylene glycol, polyethylene glycol, glycerol, 1,3-butanediol, sorbitol or maltitol, and, optionally, furthermore, (C) pref. 0.01-10wt.% of a nonionic surfactant.

Description

Detailed Description of the Invention

[0001]

TECHNICAL FIELD The present invention relates to a pharmaceutical composition useful for treating, preventing the onset and preventing infection of viral diseases.

[0002]

2. Description of the Related Art For viral diseases, there are few effective drugs for their treatment methods, and the effective drugs that have been found in recent years have been found to have side effects, and resistant strains have emerged. No cure has been found. For example,
For viral diseases that are completely cured by the autoimmune system such as colds, chicken pox, rubella, etc.
Shingles, herpes simplex, cytomegalovirus,
Even if the symptoms of sudden fever and the like are subsided, the virus itself is not exterminated and it is hidden in the ganglia and the like, so treatment with a drug must be performed every time the symptoms appear.
However, since all of these antiviral agents are water-soluble, their administration had to be performed several times a day, and the emergence of continuous preparations was required. As a continuous preparation,
An eye ointment in which an antiviral agent was kneaded in vaseline was known, but this one uses a hydrocarbon as a base, so although the durability is improved, the amount of the antiviral agent released to the affected area is small and the amount of the living body is small. From the viewpoint of usability, it was hard to say that it has improved.

[0003]

The present invention has been made in view of such circumstances, and an object thereof is to provide an antiviral preparation having high bioavailability.

[0004]

In view of such circumstances, the present inventors have conducted extensive studies to improve the bioavailability of antiviral agents in antiviral formulations, and as a result, The inventors have found that the bioavailability is enhanced by adding a polyhydric alcohol to a virus preparation, and completed the invention. Hereinafter, the present invention will be described in detail.

The antiviral preparation of the present invention is characterized by containing an antiviral agent and a polyhydric alcohol. The antiviral agent that can be used in the present invention can be used without particular limitation as long as it is usually used in clinical practice, and examples of such agents include, for example, acyclovir, Ganciclovir, soribudine, bromovinyldeoxyuridine, azidothymidine,
Examples thereof include dideoxythymidine, dideoxyinosine, arabinosyl adenine and the like. Among these, the most preferable application of the formulation of the present invention is acyclovir. This is because it is most widely used, has high water solubility, and has low durability. The present invention may contain one or more of these antiviral agents. The preferred compounding amount is 0.1 to 10% by weight, and more preferably 0.5 to 5% by weight, although it depends on the antiviral agent.

In addition to antiviral agents, polyhydric alcohols can be cited as essential constituents of the present invention. Polyhydric alcohol is a general term for those in which two or more hydrogen atoms of an aliphatic hydrocarbon are substituted with a hydroxyl group, and since these are generally low in toxicity, any of them is not particularly limited in the present invention. Although it can be contained, preferred examples include, for example, propylene glycol, polyethylene glycol, glycerin, 1,3-butanediol,
Examples thereof include sorbitol, maltitol and the like, and of these, propylene glycol is most preferable from the viewpoint of its action and achievement in medicine. In the present invention, these polyhydric alcohols may be used alone or in combination of two or more kinds. The preferred content of polyhydric alcohol in the antiviral preparation of the present invention is 0.1 to 20% by weight.
And more preferably 0.5 to 10% by weight.

[0007] As a component which enhances the effect of the antiviral preparation of the present invention, a nonionic surfactant can be mentioned. Examples of the nonionic surfactant include polyoxyethylene hydrogenated castor oil, polyoxyethylene fatty acid, polyoxyethylene higher alcohol ether, polyoxyethylene sorbitan fatty acid ester, polyoxyethylene glycerin fatty acid ester and the like. The most preferred of these is polyoxyethylene sorbitan fatty acid ester. In the present invention, these nonionic surfactants may be used alone or in combination of two or more kinds. In the present invention, when the nonionic surfactant is blended, the preferable blending amount is 0.01 to 10% by weight, and the more preferable blending amount is 0.05 to 5% by weight.

The composition for viral diseases of the present invention may contain, in addition to the above-mentioned components, optional components for various preparations usually used in pharmaceutical compositions. Examples of such optional components include a binder, a disintegrating agent, a filler, a flavoring agent, a coloring agent, an isotonic agent, and a pH adjusting agent. or,
This is a method of preparing a composition using the above-mentioned components and optional components, and this may be carried out according to a usual method for producing a pharmaceutical composition. The administration route of the composition of the present invention can be applied without particular limitation as long as it is a usual administration route, but the most preferable are eye drops, eye ointments, nasal drops, nose, vagina, genital area or It is a spray on the throat. The applied amount may be in conformity with those of these dosage forms, and the above-mentioned compounded amount may be administered to an appropriate amount site at the time of use.

[0009]

BEST MODE FOR CARRYING OUT THE INVENTION In order to explain the content of the present invention in more detail, embodiments of the invention will be described with examples.

Example 1 An eye drop was prepared according to the following prescription. That is, the prescription components were dissolved by heating, sterile filtered, and then aseptically filled to prepare an eye drop. Acyclovir 1 part by weight Propylene glycol 5 parts by weight Sodium chloride 0.9 parts by weight Methylparaben 0.1 parts by weight Distilled water for injection 97 parts by weight

Example 2 An eye drop was prepared according to the following prescription. That is, the prescription components were dissolved by heating, sterile filtered, and then aseptically filled to prepare an eye drop. Ganciclovir 1 part by weight Glycerin 5 parts by weight Sodium chloride 0.9 parts by weight Methylparaben 0.1 parts by weight Distilled water for injection 97 parts by weight

Example 3 An eye drop was prepared according to the following formulation. That is, the prescription components were dissolved by heating, sterile filtered, and then aseptically filled to prepare an eye drop. Soribudine 1 part by weight Ethylene glycol 400 5 parts by weight Sodium chloride 0.9 parts by weight Methylparaben 0.1 parts by weight Distilled water for injection 97 parts by weight

Example 4 An eye drop was prepared according to the following formulation. That is, the prescription components were dissolved by heating, sterile filtered, and then aseptically filled to prepare an eye drop. Bromovinyl deoxyuridine 1 part by weight Propylene glycol 5 parts by weight Sodium chloride 0.9 parts by weight Methyl paraben 0.1 parts by weight Distilled water for injection 96.9 parts by weight Polyoxyethylene (60) hydrogenated castor oil 0.1 parts by weight

Example 5 An eye drop was prepared according to the following formulation. That is, the prescription components were dissolved by heating, sterile filtered, and then aseptically filled to prepare an eye drop. 1-arabinosyl adenine 1 part by weight maltose 5 parts by weight sodium chloride 0.9 parts by weight methylparaben 0.1 parts by weight distilled water for injection 97 parts by weight

Example 6 A nasal drop was prepared according to the following formulation. That is, the prescription ingredients were dissolved by heating, sterile filtered, and then aseptically filled in a spray container to prepare a nasal drop. Acyclovir 2 parts by weight Sorbitol 5 parts by weight Propylene glycol 10 parts by weight Methylparaben 0.1 parts by weight Distilled water for injection 82 parts by weight Sodium chloride 0.9 parts by weight

(Example 7) A skin external preparation for genitals was prepared according to the following formulation. That is, the prescription ingredients were dissolved by heating and cooled to prepare a skin external preparation. Soribudine 3 parts by weight Acyclovir 2 parts by weight Ethanol 65 parts by weight Isopropanol 30 parts by weight

Example 8 A nasal drop was prepared according to the following formulation. That is, the prescription ingredients were dissolved by heating, sterile filtered, and then aseptically filled in a spray container to prepare a nasal drop. Acyclovir 1 part by weight Propylene glycol 5 parts by weight Polyoxyethylene monooleate 3 parts by weight Methylparaben 0.1 parts by weight Distilled water for injection 90 parts by weight Sodium chloride 0.9 parts by weight

[0018]

【Example】

Example 1 Usage Test Using the eye drop of Example 1 and the eye drop of Comparative Example 1 in which propylene glycol of the eye drop of Example 1 was replaced with water, 10 patients with herpes simplex type I ophthalmitis were randomly assigned to each of 2 patients. Divided into groups,
Example 1 and Comparative Example 1 were administered to each group and the progress was observed. Table 1 shows the results. From this, it can be seen that the eye drop of the present invention has an excellent effect as compared with Comparative Example 1 which is a conventional eye drop. This is because the eye drop of Example 1, which is the composition for viral diseases of the present invention, has excellent bioavailability.

[0019]

[Table 1]

[0020]

Since the composition for viral diseases of the present invention has high bioavailability, it is suitable for treatment and prevention of viral diseases.

Claims (6)

[Claims] 1. A pharmaceutical composition for viral diseases, which comprises an antiviral agent and a polyhydric alcohol. 2. The antiviral agent according to claim 1, which is one or more selected from acyclovir, gancyclovir, soribudine, bromovinyldeoxyuridine, azidothymidine, dideoxythymidine, dideoxyinosine, and arabinosyladenine. Pharmaceutical composition. 3. The pharmaceutical composition according to claim 1, wherein the polyhydric alcohol is one or more selected from propylene glycol, polyethylene glycol, glycerin, 1,3-butanediol, sorbitol and maltitol. Stuff. 4. The content of antiviral agent is 0.1 to 10% by weight, and the content of polyhydric alcohol is 0.1 to 20% by weight.
The pharmaceutical composition according to any one of claims 1 to 3, which is: 5. The pharmaceutical composition according to claim 1, which contains a nonionic surfactant. 6. The content of the nonionic surfactant is 0.01.
The pharmaceutical composition according to any one of claims 1 to 5, which is -10% by weight.