CS203552B1 - Fluid desensibilization alergene preparation - Google Patents

Description

The present invention relates to liquid desensitizing elergen preparations obtained by extraction of allergens.

Atopic allergy (type I allergy) is the basis of the whole group of allergic diseases. A characteristic feature is the disposition factor, which, together with the non-physiological change and harmful effects of the environment and the sensitization antigens, explains the steady increase in the number of allergy sufferers, especially in the youngest generation. The need for effective treatment with simple application Increasingly, it is increasing. Oral application of desensitizing allergens is particularly suitable for pediatric allergy sufferers.

Unlike adults, the enteral antigen barrier in children is readily permeable to relatively large antigen molecules, such as pollen, yeast, bacteria, and the like, which therefore enter the lymphatic system and result in the desired immunological stimulation.

The invention relates to a process for the production of desensitizing allergens used for treatment in droplet dosage form for children and adolescents up to 18 years of age, with a treatment result equal to, sometimes better than, traumatizing injectable forms.

So far, various ad hoc non-standard labile solutions, even raw pollen or dust, have been used worldwide

20355?

with ether, honey, etc., where precise dosing or allergen specificity is not possible.

This implies that a standard, stable and effective peroral allergen should be introduced for a child's practice on a socially significant scale and in the required amount. ·.

[0008] The present invention eliminates these drawbacks by providing a liquid desensitizing agent obtained by extracting allergens, wherein the extract of at least one allergen is formulated into an oral dosage form by the addition of at least one non-toxic substance selected from sorbitol, aldopentose and aldohexose as a stabilizer.

The liquid desensitizing allergen composition according to the invention may contain a flavoring or flavoring agent, for example a fruit syrup or an aromatic essential oil of vegetable origin. A preferred flavor correction is raspberry syrup, a preferred flavor correction is peppermint oil or menthol alcohol solution. Said corrigeneia may be added either directly by the manufacturer of the preparation or by the consumer [patient] of his own taste.

He did

7,5 g mixed pollen from plants:

j

Agrostis alba,

Alopecurus pratensis (Meadow Foxtail), Anthoxanthus odoratum (Tomato), Apera spica valve (Chundelka metlice), Arrhenatherum elatius (Oatmeal), Avenstrum pratense (Oatmeal)

Holcus lanatus,

Lolium sp. (Rye grass),

Phleum pratense (Timothy),

Poa pratensis,

Secale cereale,

Plantago lanceolata (Plantago lanceolata) is extracted in 100 ml solution of the following ^composition: Sodium chloride 5 g Sodium bicarbonate 2.75 g Ethanol 95% · 20.0 g Methylparaben 0.67 g Propylparaben 0.33 g Distilled water to 100 ml

The solution was adjusted to pH 8.2-8.4 by bubbling CO 2 solution. Extract for 48 to 72 hours at +2 to + 10 ° C by shaking for 2 hours after standing for 2 hours.

The first dose of extractant is 40 to 50 ml, the next 2 to 3 doses of 25 or 20 ml each. After centrifugation and filtration, the individual extracts are combined, stabilized, for example by adding 1: 20,000 nonionic surfactant, 1 ml per 1000 ml stabilized solution, and the pH is adjusted to 6.4 to 7.4; The solution obtained is sterilized by filtration through a 0.22 μΐη bacteriological filter, such as the Milipore filter. '. :

The sterile allergen solution is diluted with a 10% sterile aqueous sorbitol solution containing 5% raspberry syrup and a 0.1% / 10% menthol solution in .60% alcohol after the protein nitrogen content (PNJ) has been determined.

The following applies to the definition of an international entity:

PNU = 0.00001 mg PN in 1 ml solution.

Example 2 40 g of housing dust, i.e. dust collected from at least 40 bytes of allergy sufferers and mixed, biologically active, supplied by allergy centers, collected and screened to No. VII nets according to U.S. Pat. of the pharmacopoeia CsL 3 (mesh side length 0,08 mm), extracted in 100 ml of a solution of the following composition:

sodium chloride 5.0 g primary sodium phosphate 0.36 g secondary sodium phosphate 1.43 g ethanol 95% 20.0 g methylparaben 0.67 g propylparaben 0.33 g; distilled water up to a total volume of 100 ml.

The pH of the solution was adjusted to 6.8 to 7.1 with 1 N NaOH or 1 N HCl.

Extract for 48 to 72 hours at +2 to +10 ° C by shaking for 2 hours after standing for 2 hours. The first dose of extractant is 40 to 50 ml, the next 2 to 3 doses of 25 or 20 ml each. After centrifugation and filtration, the individual extracts were collected. they are combined, stabilized, for example by adding a nonionic surfactant at a concentration of 1: 20,000 - in a ratio. 1 ml per 1000 ml of solution and the pH is adjusted to 6.4 to 7.4. The obtained allergen solution is diluted with a 15% sterile solution of sorbitol in water with 10% raspberry syrup and 0.1% alcohol menthol (10 g menthol in 90 g 60% ethanol) after the previous determination of the protein nitrogen (PN) content in 1 ml per ml requested content of International Units (PNU).

Example 3.

Combinations of sterile allergen solutions according to the individual prescriptions of a physician-allergologist (eg house dust + pollen, mold + + pollen, bacterial allergens + house dust + mites, etc. J.

May be a mixture of the extracts indicate _seven out in Examples 1 and 2 in a ratio determined by the physician.

He attaches

The procedure is as in Example 1 or 2, except that ribose in 10% aqueous solution is used instead of sorbitol. Example 5

The procedure is as in Example 1 or 2, except that a 15% aqueous glucose solution is used instead of sorbitol. Example 6

The procedure is as in Example 1 or 2, except that a 10% aqueous mannose solution is used instead of sorbitol.

Individual dilutions (according to Examples 1 to 6) are filled in 10 ml in vials with a cap that can be sterilized.

The invention allows for oral treatment that fully replaces the hitherto used injection treatment.

The invention removes injectable treatment, previously used in pediatric allergy practice, to achieve the same or even higher treatment effect.

. Production process of allergen solutions for kap203552

The dosage form, described in more detail in the examples, is simple, does not require production equipment, material and attendance, and allows reproducible preparation of the allergen, stable and effective. The extraction and dilution procedures with a suitable vehicle aid in the mycelization of the high molecular weight species

Claims (2)

Liquid desensitization allergen composition obtained by extracting allergens, characterized in that the extract of at least one allergen is formulated into an oral dosage form by the addition of at least one non-toxic substance selected from the group consisting of sorbitol, aldopentose and aldohexose as a stabilizer. and prevents alkaline hydrolysis of the allergen molecules. In this way, it is possible to produce different types of allergens in solutions (pollen, dust, bacterial, or a combination thereof) as desired by the physician-allergologist and treatment needs resulting from the specific reactivity of the patient. YNÁLEZU Liquid desensitizing allergen composition according to claim 1 or 2, characterized in that it contains a flavoring or aroma-correcting agent, e.g.