JP2002128666A - Prescribed medicine for local injection - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain a prescribed medicine for local injection, which is directly and locally injected into a lesion of a malignant tumor to differentiate, reduce or eliminate the malignant tumor. SOLUTION: This prescribed medicine for local injection, is obtained by dissolving theanine in water. The prescribed medicine for the local injection is suitably injected into the tumor-lesion site of a mammal including homo, the peripheral portion of the tumor-lesion site, and further an artery directed to the lesion site to reduce or eliminate the tumor.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

TECHNICAL FIELD The present invention relates to a formulation prepared for local injection for treating malignant tumors found in mammals in general.

[0002]

2. Description of the Related Art The most common approach to treating a malignant tumor is to resect the affected area or administer an antitumor agent.

[0003]

However, in the treatment by excision of the affected part, the area around the affected part is atrophied and cannot be restored before the excision. Furthermore, it is not always possible to remove all or most of the organs if the tumor has spread. Further, the antitumor agent only suppresses the spread or metastasis of the tumor to the last, and it is difficult to substantially directly act on the tumor to reduce or eliminate it. The present invention has been made to solve the problems involved in the conventional technology. It is an object of the present invention to provide a local injection prescription that differentiates a malignant tumor by direct local injection into the affected area of the malignant tumor and reduces or eliminates the malignant tumor.

[0004]

Means for Solving the Problems In order to solve the above problems, in the invention of claim 1, an aqueous solution mainly containing an α-amino acid having the following functional group in the molecule is used as a formulation for local injection. This is the gist.

[0005]

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The gist of the invention of claim 2 is that the α-amino acid is dissolved in water or a physiological salt solution as the formulation for local injection according to claim 1. The gist of the third aspect is that a lower alcohol is added as the formulation for local injection according to the first or second aspect.
The gist of the invention of claim 4 is that the α-amino acid is theanine as the formulation for local injection according to any one of claims 1 to 3. Here, the functional group is an L-type or D-type functional group, and includes a racemic type. Examples of the α-amino acid having such a functional group include α-aminobutyric acid, glutamic acid, and theanine. For example, L-α-aminobutyric acid is represented by the following chemical formula.

[0007]

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[0008] Based on several findings regarding the antagonistic action of inhibitory neurons on L-γ-aminobutyric acid, which has an affinity for the GABA receptor, it was found that similar L-α-aminobutyric acid itself has a function of promoting cell differentiation. Can be assumed. Although its function has not been completely elucidated, it can be speculated that it suppresses the internal respiratory action of nerve cells and induces apoptosis of nerve cells. Therefore, it is considered that local use for malignant tumors has an effect of promoting apoptosis of nerve cells of malignant tumors. In addition, it has been found that glutamate has an effect of promoting apoptosis of nerve cells by stagnating in synaptic clefts. For this reason, the applicant prescribes theanine having the above-mentioned functional group, particularly theanine as a main component, and treats malignant tumors. Here, theanine mainly refers to L-theanine, also known as γ
-Ethylamide-L-glutamic acid (L-Glutamic acid
-Γ-monoethylamide) and is represented by the following chemical formula.

[0009]

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[0010] Theanine is a white crystalline powder known as one of the delicious components of tea and is odorless. In addition, there is a finding that theanine has an effect of preventing hypertension and an effect of acting on brain nerve cells to prevent necrosis of cells due to ischemia. Theanine is soluble in water and insoluble in alcohol and ether. Therefore, it shows good solubility in water and physiological salt solutions. Here, the physiological salt solution is a concept including physiological saline and Ringer's solution (Ringer-Rock's solution). Ringer solution is a concept that includes Ringer acetate and Ringer lactate. Glutamic acid is an α-amino acid widely known mainly as an umami component. For example, L-glutamic acid is represented by the following descriptive formula.

[0011]

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The lower alcohol is preferably a monohydric alcohol. Divalent and trivalent cannot be used alone due to their high viscosity at room temperature. Further, as the monohydric lower alcohol, those having up to C4 are preferable. Particularly preferred are low molecular weight methyl alcohol and ethyl alcohol. Methyl alcohol may be used because it is a local injection and the amount used is small, but ethyl alcohol is most preferred. Lower alcohols have a low molecular weight and thus easily pass through cell membranes. Alcohols have hydrophilic and hydrophobic groups and thus have a property of easily penetrating into sites with high water content in cells. In addition, alcohol inactivates glycogen, the energy source of cancer cell growth, as is the case with ethanol infusion for treating liver cancer. Therefore, it is preferable to add this as a formulation in the present invention. The formulations of the present invention are used for malignant tumors found throughout mammals. Malignant tumors include, for example, sarcomas, adenomas, and skin cancers. In addition, mammals include humans.

[0013]

According to the invention described in claims 1 to 4,
It is suitable as a prescription for local injection, since the tumor is reduced or disappeared by injection into the affected area of the tumor of a mammal including a human, around the affected area, and further into the artery toward the affected area.

[0014]

Hereinafter, an embodiment of the present invention will be described. In the present embodiment, distilled water was used in Formula 1 as a solvent for L-theanine, and physiological saline was used in Formula 2. In Formula 2, physiological saline was used instead of distilled water, and 70% ethyl alcohol was further added. The mixing ratio of each prescription is as follows. Formula 1 Theanine 33.33% by weight Distilled water 66.66% by weight Formulation 2 Theanine 33.33% by weight Physiological saline 33.33% by weight 70% Ethyl alcohol 33.33% by weight Although it was directly injected into an artery, it may be injected into an artery that supplies blood to the affected part depending on the site.

[0015]

Example (No. 1) A large dog (male, about 30 kg) was locally injected with Formulation 1 into a skin / mast cell tumor in the center of the left neck. Table 1 shows the findings in which the treatment was performed only once with 1.0 cc as an injection amount. (No. 2) Formula 1 was locally injected into the anal tumor of a medium-sized dog (male, about 12 kg). Table 1 shows the results of the findings in which 1.0 cc was applied only once as an injection amount. (No. 3) A small dog (female, about 3 kg) was locally injected with Formulation 1 for multiple skin cancers scattered on the midline of the left shoulder. Table 1 shows the results of the findings in which a total of 10 treatments were performed once a month with 1.0 cc as an injection amount. (No. 4) A cat (female, about 3.5 kg) was excreted into a mammary tumor associated with subcutaneous exudate, and the exudate was drained and formulation 1 was locally injected. Table 1 shows the results of the findings in which the treatment was performed 5 times a month, with 1.0 cc as the injection amount per time. (No. 5) A cat (female, about 3.5 kg) was excreted into a mammary tumor associated with a subcutaneous exudate, and the exudate was drained off, and Formula 1 was locally injected. Table 1 shows the results of the findings in which the treatment was carried out twice a month for a total of 8 times, with 1.0 cc to 3.0 cc as an injection amount per injection. (No. 6) Formula 2 was locally injected to a malignant tissue tumor that occurred in the lower leg outside the lower leg and below the saphena vein (upper leg part) in a medium-sized dog (shiba inu, about 10 kg). At the first time, 1.0 cc was locally injected into the affected part and several places around the affected part in two divided doses. Also, in the second time, 1.
2 cc of the injection was divided into two times and locally injected into the affected area and several places around the affected area. On the 15th, measures were taken twice a month.
Table 1 shows the findings at the 15th day medical examination. (No. 7) Formula 2 was locally injected into the right mammary gland of a small dog (female, about 5 kg). At the first time, 1.0 cc was locally injected into the affected part and several places around the affected part in two divided doses. Similarly, at the second time, 2.0 cc of the injection was locally divided into two portions and locally injected into the affected part and several places around the affected part.
On the 15th, measures were taken twice a month. Table 1 shows the findings at the January screening.

[0016]

[Table 1]

 ────────────────────────────────────────────────── ─── Continuing from the front page (72) Inventor Naotake Ishikawa 6-2-28 Tokugawayamacho, Chikusa-ku, Nagoya-shi, Aichi (72) Inventor Hirohiko Matsumoto 3-57 Ikehata, Chiryu-shi, Aichi 9F term ( Reference) 4C076 AA12 BB11 BB14 CC27 DD37 FF15 4C206 AA01 AA02 FA53 MA01 MA04 MA05 MA37 MA86 NA10 NA14 ZB26

Claims (4)

[Claims] 1. A formulation for topical injection which is obtained as an aqueous solution mainly containing an α-amino acid having the following functional group in the molecule. Embedded image 2. The formulation for topical injection according to claim 1, wherein the α-amino acid is dissolved in water or a physiological salt solution. 3. The formulation for topical injection according to claim 1, wherein a lower alcohol is added. 4. The formulation for topical injection according to claim 1, wherein the α-amino acid is theanine.