JPS608227A - Antiallergic enhancer - Google Patents

Abstract

PURPOSE:The titled enhancer containing a protease as an active ingredient. CONSTITUTION:An antiallergic enhancer containing a protease (e.g., pronase, trypsin, bromelain, papain, etc.) as an active ingredient. It has merits of restoring immunoglobulin value to a normal value as well as remedying or improving allergic symptoms. The use of it together with another antiallergic (e.g., diphenphydramine hydrochloride, diphenphydramine salicylate, beclometasone propionate, etc.) further raises remedy ratio of allergic disease, and restors immunoglobulin value to a normal value in high ratio. In medication, it can be administered orally as tablet, capsule, powder, granule, etc., or parenterally as injection, suppository, or ointment. A dose is 1-5,000mg/person by oral medication. Preferably it is processed into enteric oral pharmaceutical preparation.

Description

[Detailed description of the invention] The present invention relates to an anti-allergy enhancer.

Currently, treatments for allergic diseases include desensitization therapy, antiallergic agents, and treatment with globulin preparations.

Although these treatments can alleviate symptoms such as nasal allergies, bronchial asthma, and hives, they are not completely cured, and the reality is that the attacks often return.

Under these circumstances, there has been a strong desire for an excellent allergy treatment and ameliorating drug.

As a result of extensive research into allergic diseases, the present inventors have discovered that proteolytic enzymes are effective in treating allergic diseases, and are particularly effective as enhancers of anti-allergic agents, leading to the present invention.

Allergy in the present invention includes, for example, nasal allergy,
Refers to diseases such as bronchial asthma and measles.

Allergic diseases are generally accompanied by abnormalities in immunoglobulin levels, and all current anti-allergic drugs temporarily improve symptoms, but they do not improve abnormalities in immunoglobulin levels.

On the other hand, surprisingly, the antiallergy enhancer of the present invention has the feature of curing or improving allergic symptoms and at the same time returning immunoglobulin levels to normal, and when used in combination with other antiallergic agents, the cure rate of allergic diseases can be further increased. It has the feature of increasing immunoglobulin levels and returning them to normal at a high rate.

Examples of proteolytic enzymes that are active ingredients of the present invention include trypsin, α-chymo]-lipsin, promelain, papain, seratiopeptidase, peptidase, cephabrose, protease, pronase, prozyme, urokinase, pancreatin, fifurinoridine, and elastase. , collagenase, etc., and these may be used singly or in an appropriate combination of two or more.

In addition, other antiallergic agents preferably used in combination with the antiallergic enhancer of the present invention include, for example, Shifuen Hydrochloride 1
- Lamin, diphenhydramine salicylate, diphenhydramine tannate, chlorphenoxamine hydrochloride, phenyl-1-loxamine citrate, carbinoxamine maleate, chlorpheniramine maleate, chlorpheniramine d-maleate, prompheniramine d-maleate, hydrochloric acid 1-riperenamine, 1-riperenamine citrate, tonzylamine hydrochloride, phenetazine, promethacin hydrochloride, me-1-silazine hydrochloride, 1-rimebrazine tartrate, isothipendyl hydrochloride, 1-riprolidine hydrochloride, mebhydrorinnapadicire-1-, diphenylimidazole, Clemizole hydrochloride, dimethinthene maleate, sibuhebutadine hydrochloride, homochlorcifrizine, diphenylbilarine hydrochloride, pipurinhydriner 1-1 methoxy-phenamine hydrochloride, isopsopylaminomethylhebutane hydrochloride, ocitumemacin, flemastine, fumaric acid There are various antiallergic agents containing active ingredients such as remastine, hetamethacin, mono-lium cromolycate, histamine-added immunoglobulin, and vectormethacin propionate. These drugs may be used in combination at conventional dosages.

The anti-allergy enhancer of the present invention can be prepared using conventional formulation techniques.
For example, it can be administered orally as a tablet, capsule, powder, granule, etc., or parenterally as an injection, herbal medicine, or ointment.

Furthermore, the main rule is that other drugs such as anticancer drugs, liver drugs, kidney drugs,
Can be used in combination with antibiotics, immunostimulants, antihypertensive drugs, etc.

The dosage varies depending on the type of enzyme, degree of disease, route of administration, dosage form, type of anti-allergic agent used in combination, etc., but in the case of oral administration, the objective can be achieved with 1 to 5000 mg per adult.

Depending on the type of enzyme, it is preferable to use enteric-coated oral preparations.

In addition, when the dosage is expressed in units of each enzyme, 1 to 800,000 to 800,000 units for serratiopeptidase, 20,000 to 1,000,000 units for promeline (Streb)
Kinase is 10,000 to 1 million units, elastase is 1,000 to 1,000,000 units.
The purpose can be achieved by oral administration of 200,000 units of lastase and 10,000 to 500,000 units of tyrosine for pronase.

Formulation Example 1 After mixing 100 g of serratiopeptidase, 50 g of lactose + 0 g of cornstarch, a 3% aqueous hydroxymethylcellulose solution is kneaded in Ebetsu. The mixture is sized, and the granules are mixed with 0.3% magnesium stearate and compressed into tablets.

Formulation Example 2 Elastase Log and 20 g of lactose are mixed and formed into granules, and then mixed with magnesium stearate to form tablets.

Formulation Example 3 20 g of pronase and 40 g of lactose are mixed, 1 og of hydroxypropyl methyl cellulose is added and formed into granules, which are then evenly coated with cellulose acetate to form enteric-coated granules.

Formulation Example 4 20 g of serratiopeptidase + 40 g of lactose were mixed, 10 g of hydroxypropyl methylcellulose was added, the mixture was formed into granules, and the mixture was evenly coated with cellulose acetate.
Enteric-coated granules.

Formulation Example 5 The pronase enteric-coated granules obtained in Formulation Example 3 are filled into mold cells to form capsules.

,/ /″′ ,,/’ Clinical case 1 : 33 years old, A-sex.

Diagnosis: Allergic rhinitis and bronchial asthma Since childhood, I have suffered from bronchial wheezing and asthma, often accompanied by sneezing and watery hearts.

Allergen test: U, D, (phase), cedar pollen (+1)
), Wool (-), Kaya (-), Cotton (4), Butafusa (-
), Candida (=).

Immunoglobulin level (see Table 1) Treatment with pronase: 6 tablets of Empinase P (manufactured by Kaken Pharmaceutical Co., Ltd., enteric coated, each tablet contains 9,000 tyrosine units of pronase),
After 2 months of oral administration of 2 tablets after each meal, all immune globulin values returned to normal and allergy symptoms were alleviated.

The results are shown in Table 1.

Table 1 Statistical Observation 1 Thirty patients with allergic diseases were treated with the antiallergic drug celestamine [F] or Tavezil (■) and the nasal spray (■) Intal or Beconase 0, and their progress was observed.

Three months after administration, the subjective symptoms of allergic disease had improved considerably, but the immunoglobulin levels had hardly improved.

The results are shown in Table 2.

Table 2 Statistical Observation 2 - In addition to the antiallergic drug Celestamine ■ or Tavezil 0 and the nasal spray Intal ■ or Beconase ■, 1 1116 tablets of Empinase P were administered to 38 patients with allergic diseases, and their progress was observed. .

After 3 months of treatment, immunoglobulin levels improved at a high rate, and allergic symptoms compared to statistical observation 1.
A high percentage of cases were cured or improved. The results are shown in Table 3.

As shown in Table 3 above, out of 38 patients with allergic diseases, 27 cases had all abnormal immunoglobulin values returned to normal (
71%).

Comparing this with Table 2, it can be seen that the rate of improvement in immunoglobulin values is remarkable when the antiallergic enhancer of the present invention is used in combination.

Animal experiment results: Pronase foil monocompatibility rat blood for lymphocytes 4. Mix 12J pronase 0.5μCi cpm with 4.0ml of physiological saline mixture,
Incubate L/ for 5 minutes at 37.0°C. If this is centrifuged, 125 tobronase will be added to the lymphocyte membrane.
cpm was deposited, but only a very small amount was observed in the cleaning solution.

This indicates that pronase has a strong affinity for lymphocyte membranes.

Immunoglobulins are produced by lymphocytes, and pronase has an extremely strong affinity for lymphocytes, suggesting that it has a significant influence on immunoglobulin production.

Applicant Kaken Pharmaceutical Co., Ltd.

Claims (1)

[Scope of Claims] 1. An antiallergic enhancer containing a carp autolytic enzyme as an active ingredient. 2. An antiallergic enhancer according to claim 1, characterized in that the protease is pronase.