Sublingual temperature-sensitive gel containing mite allergen and preparation method of sublingual temperature-sensitive gel

A temperature-sensitive gel and allergen technology, which is applied in the direction of allergen antigen components, medical preparations of non-active ingredients, pharmaceutical formulas, etc., can solve the problem of poor treatment effect of mite allergens, short sublingual mucosal residence time, immune Low response level and other problems, to achieve the effect of facilitating accurate dosing, shortening gelation time, and prolonging residence time

Pending Publication Date: 2021-10-26
微缔医药科技(杭州)有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The Chinese patent with publication number CN102014954A discloses a mucosal allergen-specific immunotherapy using seasonal allergens, and proposes the idea of ​​developing pollen allergens into solid dosage forms (including sublingual gel preparations), However, the disadvantages of this patent are: ① only the pollen allergen sublingual gel is proposed, and the retention problem of the gel has not yet been solved; ② whether quantitative administration can be achieved when the gel is administered , have no way of knowing
[0007] The Chinese patent with the publication number CN1840190A discloses a pharmaceutical composition for treating allergic diseases. The composition contains dust mite allergens, pollen allergens and pharmaceutically acceptable carriers. The composition can be developed into sublingual But the weak point of this technology is: from the preparation of the sublingual buccal preparation of its embodiment 4, it can be known that it is a drop, and there is the defect of "the residence time of subli...

Method used

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  • Sublingual temperature-sensitive gel containing mite allergen and preparation method of sublingual temperature-sensitive gel
  • Sublingual temperature-sensitive gel containing mite allergen and preparation method of sublingual temperature-sensitive gel
  • Sublingual temperature-sensitive gel containing mite allergen and preparation method of sublingual temperature-sensitive gel

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Example 1 Preparation of sublingual thermosensitive gel for mite allergens

[0027] Prepare the temperature-sensitive gel material and cationic monomer into a 1mol / L mixed aqueous solution, adjust the pH to 7.2, add an initiator, and pass N 2 A copolymer was obtained after 2 h of polymerization. The product is purified by dialysis in water, and a cross-linking agent is added to obtain a copolymer hydrogel. The resulting hydrogel was soaked in distilled water for 1 week to remove unreacted monomer, crosslinker and initiator molecules in the gel. Then, under magnetic stirring at 4°C, slowly add the mite allergen and mix evenly to obtain the finished product.

Embodiment 2

[0028] Example 2 Screening of thermosensitive gel materials

[0029] Assuming that the content ratio of the temperature-sensitive gel material to the cationic monomer is a certain value (such as 1:1), the temperature-sensitive gel material is one of poloxamer and poly(N-isopropylacrylamide) (PNIPAM), and the cationic monomer The body is one of chitosan, carboxymethyl chitosan, (2-diethylamino) ethyl methacrylate, and trimethyl-3-acrylamidopropylamine chloride; by measuring the phase transition temperature , mucosal retention to explore the effects of different types of thermosensitive gel materials and cationic monomers.

[0030] In this example, the preparation method of the sublingual thermosensitive gel for mite allergens is shown in Implementation 1, and the measurement results are shown in Table 1.

[0031] 1. Phase transition temperature measurement method:

[0032]Take 10g of the prepared temperature-sensitive gel solution and pour it into a vial, put a magnetic stirr...

Embodiment 3

[0044] Example 3 Screening of the Content Ratio of Thermosensitive Gel Material and Cationic Monomer

[0045] This example intends to explore the influence of the content ratio of different temperature-sensitive gel materials and cationic monomers on the aforementioned indicators by measuring the phase transition temperature, logG*, adsorption rate, and gelation time.

[0046] In this example, see Example 1 for the preparation method of the sublingual temperature-sensitive gel for mite allergens; see Example 2 for the determination methods of phase transition temperature, mucosal retention, and adsorption rate; and see Table 2 for the measurement results.

[0047] 1. Determination method of gelation time:

[0048] Take 10g of the prepared temperature-sensitive gel solution and pour it into a vial, put a magnetic stirrer in the vial, put it in a constant-temperature water bath at 25°C for 20 minutes, then place it in a constant-temperature water bath at 37°C, start timing immed...

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Abstract

The invention discloses a sublingual temperature-sensitive gel containing mite allergen. The sublingual temperature-sensitive gel is composed of mite allergen, a cationic monomer and a temperature-sensitive gel material, wherein the content ratio of the cationic monomer to the temperature-sensitive gel material is (1:2)-(1:1). According to the sublingual temperature-sensitive gel containing mite allergen, the sublingual temperature-sensitive gel is provided on the basis of a common sublingual drop containing mite allergen, the advantage of convenience in administration of the sublingual drop is maintained, the retention time of a vaccine under the tongue is prolonged, and the drug effect is improved; the gelling time of the temperature-sensitive gel is shortened, the loss caused by swallowing in the administration process is reduced, and the dosage is reduced; and the thermo-sensitivity of the temperature-sensitive gel to adsorb protein is overcome, the adsorption of the gel to the protein in a liquid state is improved, and then the dosage is reduced.

Description

technical field [0001] The invention relates to the technical field of administration of mite allergens, in particular to a sublingual thermosensitive gel containing mite allergens and a preparation method thereof. Background technique [0002] Allergy is considered by the World Health Organization (WHO) to be a major global health problem at present, and the incidence rate of allergy is very high. According to literature reports, about 1 / 3 of people have suffered from allergic diseases in their lifetime. According to the data of WHO, 22% to 25% of people in the world suffer from allergic diseases at present, and the rate of increase is 23 times every 10 years. At present, there are more than 200 million people in my country alone suffering from allergic diseases. Therefore, allergy and anti-allergy are unavoidable serious problems faced by modern people. The allergens that cause allergic reactions mainly include dust mites, pollen, dust, catkins, animal dander, etc., and m...

Claims

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Application Information

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IPC IPC(8): A61K39/35A61K9/06A61K47/36A61K47/10A61K47/32A61P33/14
CPCA61K39/35A61K9/06A61K9/006A61K47/36A61K47/10A61K47/32A61P33/14
Inventor 不公告发明人
Owner 微缔医药科技(杭州)有限公司
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