Drug release system for delaying water-soluble drug in hydrogel

Abstract

The invention discloses a system for delaying drug release of a water-soluble drug in hydrogel, and relates to the technical field of drugs, the system comprises a hydrogel, the interior of the hydrogel contains EGCG (epigallocatechin gallate), silver ions and NSAIDs (non-steroidal anti-inflammatory drug: diclofenac), and the hydrogel contains a water-soluble drug. The concentration range of the EGCG is 2-3%, the dosage of the EGCG is 0.2-0.3 g per 10 ml, the concentration range of the silver ions is 0.01-0.05%, the dosage of the silver ions is 0.001-0.005 g per 10 ml, the concentration range of the NSAIDs is 0.05-0.1%, the dosage of the NSAIDs is 0.005-0.0.01 g per 10 ml, a staged release mechanism of different drugs is adopted, the dosage of the EGCG is 0.2-0.3 g per 10 ml, the dosage of the silver ions is 0.01-0.05%, and the dosage of the NSAIDs is 0.05-0.1%. The sequential release of EGCG, silver ions and NSAIDs is realized by using the characteristics of concentration, molecular size, crosslinking, hydrophilicity and the like, and each component is ensured to act in the most effective time period.

Description

Technical Field

[0001] The invention relates to the technical field of medicines, in particular to a drug release system for delaying water-soluble drugs in hydrogels. Background Art

[0002] Oral care is the cleaning and protection of the teeth, tongue, palate, cheeks and other parts of the oral cavity, aiming to ensure the health of the oral cavity and avoid dental diseases such as oral inflammation, gingivitis, and periodontitis.

[0003] After checking the publication (announcement) number: CN101573087A, a drug release system for delaying the release of a water-soluble drug is disclosed, including an internal part of a water-soluble drug, which is in a drug matrix material that stabilizes the drug. The external part of the drug release system separates the internal part from the surrounding environment and includes a hydrophobic non-polymer compound and a binder. The hydrophobic compound can be another drug that can be released and treat the same or different diseases according to completely different release kinetics from the water-soluble drug. When the drug release system is implanted in the body, the external part delays the release of the water-soluble drug by controlling the fluid entering the internal part from the body and by controlling the passage of the water-soluble drug from the internal part into the body.

[0004] Based on the above-mentioned prior art, the existing drug release system for delaying water-soluble drugs in hydrogels still has the following problems: the drugs are easily lost quickly in the humid oral environment and cannot stay in the damaged tissue for a long time. In order to achieve long-term drug treatment, it is difficult to gradually control the release of different drugs, prolong the efficacy, avoid frequent use of drugs, and improve the efficacy. To this end, the present invention provides a drug release system for delaying water-soluble drugs in hydrogels. Summary of the invention

[0005] In view of the deficiencies in the prior art, the present invention provides a drug release system for delaying water-soluble drugs in hydrogels, which solves the following problems of the prior art drug release system for delaying water-soluble drugs in hydrogels: the drugs are easily lost rapidly in a humid oral environment and cannot stay in damaged tissues for a long time. In order to achieve long-term drug treatment, it is difficult to gradually control the release of different drugs, prolong the efficacy, avoid frequent use of drugs, and improve the efficacy.

[0006] To achieve the above objectives, the present invention is implemented by the following technical solutions: a drug release system for delaying a water-soluble drug in a hydrogel, comprising a hydrogel body, wherein the hydrogel body contains EGCG, silver ions and NSAIDs;

[0007] The concentration range of the EGCG is 2-3%, and the dosage per 10 ml is 0.2-0.3 g; the concentration range of the silver ion is 0.01-0.05%, and the dosage per 10 ml is 0.001-0.005 g; the concentration range of the NSAIDs is 0.05-0.1%, and the dosage per 10 ml is 0.005-0.0.01 g.

[0008] Preferably, the EGCG, silver ions and NSAIDs are released sequentially according to concentration, molecular size, cross-linking and hydrophilicity.

[0009] Preferably, the EGCG has a high concentration and good water solubility and is first released quickly, and the antioxidant and anti-inflammatory properties of the EGCG take effect in the initial stage.

[0010] Preferably, the EGCG cross-links with the oral mucosa to form a stable hydrogel structure.

[0011] Preferably, the silver ions have a low concentration and are released slowly and continuously in the hydrogel. The silver ions are gradually released in a humid environment as the hydrogel absorbs water and swells.

[0012] Preferably, the NSAIDs include diclofenac and ibuprofen.

[0013] Preferably, the hydrogel has a double-layer structure, with an inner layer made of gelatin and an outer layer made of polytetrafluoroethylene material.

[0014] Preferably, the EGCG, silver ions and NSAIDs are gradually dissolved in sequence, the EGCG is an early anti-inflammatory, the silver ions are a mid-term antibacterial, and the NSAIDs are a late analgesic.

[0015] The present invention provides a drug release system for delaying water-soluble drugs in hydrogels. Compared with the prior art, the system has the following beneficial effects:

[0016] 1. This drug release system that delays water-soluble drugs in hydrogels adopts a phased release mechanism for different drugs, and uses concentration, molecular size, cross-linking, hydrophilicity and other characteristics to achieve the timed release of EGCG, silver ions and NSAIDs, ensuring that each ingredient acts within its most effective period.

[0017] 2. In this drug release system that delays the release of water-soluble drugs in hydrogels, high concentrations of EGCG are released first to provide early antioxidant and anti-inflammatory protection and stabilize the hydrogel structure. Silver ions are gradually released at lower concentrations to form a continuous sterile environment, and the stability of the hydrogel is enhanced through the cross-linking effect of EGCG and the oral mucosa.

[0018] 3. The drug release system for delayed water-soluble drugs in hydrogels utilizes the differences in molecular size and water solubility to achieve rapid release of EGCG, medium-term release of silver ions, and late slow release of NSAIDs, thereby achieving staged controlled release. At the same time, the release rate of NSAIDs is regulated by nanoparticle encapsulation or salt form. BRIEF DESCRIPTION OF THE DRAWINGS

[0019] Figure 1 It is a structural diagram of the hydrogel of the present invention;

[0020] Figure 2 The EGCG molecular structure diagram of the present invention;

[0021] Figure 3 The molecular structure diagram of NSAIDs of the present invention;

[0022] Figure 4 This is a table of component concentrations of the present invention.

[0023] In the figure: 1-hydrogel, 5-EGCG, 6-silver ions, 7-NSAIDs. DETAILED DESCRIPTION

[0024] The following will be combined with the drawings in the embodiments of the present invention to clearly and completely describe the technical solutions in the embodiments of the present invention. Obviously, the described embodiments are only part of the embodiments of the present invention, not all of the embodiments. Based on the embodiments of the present invention, all other embodiments obtained by ordinary technicians in this field without creative work are within the scope of protection of the present invention.

[0025] See also Figure 1-Figure 4 , the present invention provides a technical solution:

[0026] A drug release system for delaying a water-soluble drug in a hydrogel, comprising a hydrogel body 1, wherein the hydrogel body 1 contains EGCG, silver ions and NSAIDs;

[0027] The concentration range of EGCG is 2-3%, and the dosage is 0.2-0.3 grams per 10 milliliters. The concentration range of silver ions is 0.01-0.05%, and the dosage is 0.001-0.005 grams per 10 milliliters. The concentration range of NSAIDs is 0.05-0.1%, and the dosage is 0.005-0.0.01 grams per 10 milliliters.

[0028] In this embodiment, EGCG, silver ions and NSAIDs are released sequentially according to concentration, molecular size, cross-linking and hydrophilicity.

[0029] By utilizing the differences in molecular size and water solubility, EGCG is released quickly, silver ions are released in the medium term, and NSAIDs are released slowly at the later stage, thus achieving phased controlled release.

[0030] Each ingredient works at a different stage, which can significantly reduce the frequency of administration and improve the convenience of oral ulcer wound care.

[0031] EGCG (epigallocatechin gallate) is released early, at a relatively high concentration, and is released quickly;

[0032] Release characteristics: EGCG has good water solubility and is quickly released in the hydrogel system. Its antioxidant and anti-inflammatory properties can take effect in the initial stage. At the same time, it cross-links with the oral mucosa to help form a stable hydrogel structure. The ingredients are milder than NSAIDs and are natural extracts.

[0033] Function: The cross-linking effect of EGCG can fix the hydrogel structure, reduce the premature release of other drugs or the destruction of the hydrogel by saliva and tongue movement, and improve the durability and stability of the drug.

[0034] Silver ions (Ag+) are released in the medium term, at a lower concentration and gradually;

[0035] Release characteristics: The concentration of silver ions is low, so the release in the hydrogel is slow and continuous. In a humid environment, as the hydrogel absorbs water and swells, Ag+ is gradually released, providing effective antibacterial effects.

[0036] Function: Through antibacterial function, silver ions can reduce bacteria in the oral cavity, prevent infection, ensure the drug stability of the hydrogel, and make subsequent drug release more effective.

[0037] NSAIDs (nonsteroidal anti-inflammatory drugs) are released slowly in the late stage, have large molecular weight and low water solubility;

[0038] Release characteristics: The low water solubility and large molecular weight of NSAIDs make their release rate slow. The use of special preparations (such as nanoparticles) or salt forms can further delay the release time, allowing NSAIDs to be slowly and continuously released in the later stage of the hydrogel, providing long-lasting anti-inflammatory and analgesic effects.

[0039] In this embodiment, EGCG has a high concentration and good water solubility and is first released quickly, and the antioxidant and anti-inflammatory properties of EGCG take effect in the initial stage.

[0040] High concentrations of EGCG are released first, providing early antioxidant and anti-inflammatory protection and stabilizing the hydrogel structure; silver ions are gradually released at lower concentrations to form a continuous sterile environment.

[0041] In this embodiment, EGCG cross-links with the oral mucosa to form a stable hydrogel structure.

[0042] The stability of the hydrogel is enhanced by the cross-linking of EGCG with the oral mucosa, while the release rate of NSAIDs is regulated by nanoparticle encapsulation or salt form.

[0043] The early cross-linking of EGCG stabilizes the hydrogel, the silver ions provide mid-term antimicrobial protection, and the NSAIDs are released in the late stage, which overall prolongs the duration of drug action.

[0044] In this embodiment, the concentration of silver ions is low and the release in the hydrogel is slow and continuous. The silver ions are gradually released as the hydrogel absorbs water and swells in a humid environment.

[0045] In this embodiment, NSAIDs include diclofenac and ibuprofen.

[0046] In this embodiment, the hydrogel body 1 is a double-layer structure, with an inner layer made of gelatin and an outer layer made of polytetrafluoroethylene material.

[0047] In this embodiment, EGCG, silver ions and NSAIDs are gradually dissolved in sequence, EGCG is an early anti-inflammatory, silver ions are a mid-term antibacterial, and NSAIDs are a late analgesic.

[0048] The gradual action mechanism of early anti-inflammatory, mid-term antibacterial and late analgesia makes the therapeutic effect of oral medications more significant and improves the stability and durability of the drugs.

[0049] Meanwhile, the contents not described in detail in this specification belong to the prior art known to those skilled in the art.

[0050] When working, high concentration of EGCG is released first to provide early antioxidant and anti-inflammatory protection and stabilize the hydrogel structure. Silver ions are gradually released at lower concentrations to form a continuous sterile environment. The stability of the hydrogel is enhanced through the cross-linking effect of EGCG and oral mucosa. Utilizing the differences in molecular size and water solubility, silver ions are released in the middle term and NSAIDs are slowly released in the later stage, achieving staged controlled release.

[0051] It should be noted that, in this article, relational terms such as first and second, etc. are only used to distinguish one entity or operation from another entity or operation, and do not necessarily require or imply any such actual relationship or order between these entities or operations. Moreover, the terms "include", "comprise" or any other variants thereof are intended to cover non-exclusive inclusion, so that a process, method, article or device including a series of elements includes not only those elements, but also other elements not explicitly listed, or also includes elements inherent to such process, method, article or device.

[0052] Although embodiments of the present invention have been shown and described, it will be appreciated by those skilled in the art that various changes, modifications, substitutions and variations may be made to the embodiments without departing from the principles and spirit of the present invention, and that the scope of the present invention is defined by the appended claims and their equivalents.

Claims

1. A drug release system for delaying a water-soluble drug in a hydrogel, characterized in that: It comprises a hydrogel (1), wherein the hydrogel (1) contains EGCG, silver ions and NSAIDs; The concentration range of the EGCG is 2-3%, and the dosage per 10 ml is 0.2-0.3 g; the concentration range of the silver ion is 0.01-0.05%, and the dosage per 10 ml is 0.001-0.005 g; the concentration range of the NSAIDs is 0.05-0.1%, and the dosage per 10 ml is 0.005-0.0.01 g.

2. The drug release system for delayed water-soluble drugs in hydrogel according to claim 1, characterized in that: The EGCG, silver ions and NSAIDs are released sequentially according to concentration, molecular size, cross-linking and hydrophilicity.

3. The drug release system for delayed water-soluble drugs in hydrogel according to claim 1, characterized in that: The EGCG has a high concentration and good water solubility and is first released quickly, and the antioxidant and anti-inflammatory properties of EGCG take effect in the initial stage.

4. The drug release system for delayed water-soluble drugs in hydrogel according to claim 1, characterized in that: The EGCG cross-links with the oral mucosa to form a stable hydrogel structure.

5. The drug release system for delayed water-soluble drugs in hydrogel according to claim 1, characterized in that: The silver ions have a low concentration and are released slowly and continuously in the hydrogel. The silver ions are gradually released in a humid environment as the hydrogel absorbs water and swells.

6. The drug release system for delayed water-soluble drugs in hydrogel according to claim 1, characterized in that: The NSAIDs include diclofenac and ibuprofen.

7. The drug release system for delayed water-soluble drugs in hydrogel according to claim 1, characterized in that: The hydrogel (1) is a double-layer structure, with an inner layer made of gelatin and an outer layer made of polytetrafluoroethylene material.

8. The drug release system for delayed water-soluble drugs in hydrogel according to claim 1, characterized in that: The EGCG, silver ions and NSAIDs are gradually dissolved in sequence, wherein the EGCG is anti-inflammatory in the early stage, the silver ions are antibacterial in the middle stage, and the NSAIDs are analgesic in the late stage.

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