Flurbiprofen-based analgesic spray and preparation method thereof

Abstract

The invention is applicable to the technical field of drug-loaded polymer medical preparations, and provides a flurbiprofen-based analgesic spray and a preparation method thereof, the flurbiprofen-based analgesic spray comprises the following components by weight: 0.5%-10% of flurbiprofen, 5%-15% of a cosolvent, 0.5%-15% of a humectant, 0.01%-1.5% of a preservative, 0.1%-5% of a penetration enhancer, and the balance of purified water; preferably, the analgesic spray comprises the following components in percentage by weight: 1.0%-8.0% of flurbiprofen, 8%-12% of a cosolvent, 5%-10% of a humectant, 0.01%-1.0% of a preservative, 0.5%-3% of a penetration enhancer and the balance of purified water. According to the scheme, the high-dose flurbiprofen spray can release more quickly than a sustained-release patch within the same time, the analgesic spray is more stable in efficacy and more quick in effect, and the analgesic spray is simple in preparation process, moderate in dosage of raw materials and auxiliary materials, stable in efficacy and capable of meeting clinical requirements.

Description

Technical Field

[0001] The invention relates to the technical field of drug-carrying polymer medical preparations, in particular to an analgesic spray based on flurbiprofen and a preparation method thereof. Background Art

[0002] Flurbiprofen is one of the excellent varieties of non-steroidal anti-inflammatory analgesics, mainly used to treat rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, traumatic pain and other pains. Flurbiprofen inhibits the activity of prostaglandin synthase cyclooxygenase to achieve anti-inflammatory and analgesic effects. Flurbiprofen introduces a fluorine atom into its molecular structure. The unique properties caused by the fluorine atom make it more effective among similar drugs and have a small therapeutic dose, thus having strong anti-inflammatory, analgesic and antipyretic functions while minimizing side effects.

[0003] Most of the existing flurbiprofen preparations are oral preparations, which have some limitations, such as a strong irritation to the gastrointestinal tract, which limits the use of patients who cannot take oral medications. In addition, oral medications are absorbed slowly and take a long time to take effect, which cannot meet the needs of patients who need quick pain relief. Summary of the invention

[0004] The object of the present invention is to provide an analgesic spray based on flurbiprofen and a preparation method thereof, so as to solve the problems in the above-mentioned background technology.

[0005] To achieve the above object, the present invention provides the following technical solutions: In a first aspect, the present invention provides an analgesic spray based on flurbiprofen, wherein the components and contents of the analgesic spray are as follows in terms of weight percentage:

[0006] Flurbiprofen 0.5%-10%, cosolvent 5%-15%, moisturizer 0.5%-15%, preservative 0.01%-1.5%, penetration enhancer 0.1%-5%, and the rest is purified water.

[0007] Preferably, the components and contents of the analgesic spray are as follows:

[0008] Flurbiprofen 1.0%-8.0%, cosolvent 8%-12%, moisturizer 5%-10%, preservative 0.01%-1.0%, penetration enhancer 0.5%-3%, and the rest is purified water.

[0009] Preferably, the co-solvent is at least one of ethanol, acetone, propylene glycol, 1,3-butanediol, and isopropanol.

[0010] Preferably, the preservative is one or more of methylparaben, propylparaben, hydroxyacetophenone, sorbic acid, and phenoxyethanol.

[0011] Preferably, the penetration enhancer is at least one of peppermint oil, azone, and propylene glycol.

[0012] Preferably, the moisturizer is at least one of butylene glycol, pentylene glycol, glycerin, polyethylene glycol, cetyl palmitate, and alkyl polymethylsiloxane.

[0013] The second aspect of the present invention provides a method for preparing the analgesic spray according to the first aspect of the present invention, comprising the following steps:

[0014] S1, dissolving flurbiprofen in ethanol, stirring and dissolving to obtain an API solution;

[0015] S2, measure an appropriate amount of purified water, add methylparaben and propylparaben, stir and dissolve at 70-90° C. to obtain a transparent uniform solution, cool to room temperature, and set aside;

[0016] S3, adding the solution in S1 to S2, stirring evenly to obtain a mixed solution;

[0017] S4, adding glycerin and peppermint oil to the mixed solution, stirring evenly, and then adding purified water to the required amount to obtain;

[0018] S5, filter the obtained solution and fill it into a spray bottle according to the required amount, and equip it with a quantitative spray pump.

[0019] The present invention has at least the following beneficial effects:

[0020] The present invention provides an analgesic spray based on flurbiprofen and a preparation method thereof. The high-dose flurbiprofen spray is released faster than a sustained-release patch at the same time, the analgesic spray has a more stable efficacy and exerts an effect faster, and the preparation process of the analgesic spray is simple, the dosage of raw and auxiliary materials is moderate, the efficacy is stable, and clinical needs can be met. BRIEF DESCRIPTION OF THE DRAWINGS

[0021] Figure 1 The in vitro cumulative release results of the flurbiprofen spray and flurbiprofen patch sustained-release preparations in Example 1;

[0022] Figure 2 The in vitro cumulative release results of the flurbiprofen spray and the flurbiprofen sustained-release preparation in Example 2;

[0023] Figure 3 The in vitro cumulative release results of the flurbiprofen spray and the flurbiprofen sustained-release preparation in Example 3 are shown. DETAILED DESCRIPTION

[0024] The technical solutions in the embodiments of the present invention are described clearly and completely below. 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] The present invention provides a flurbiprofen analgesic spray, the components and weight percentages of which are as follows:

[0026] Flurbiprofen 0.5%-10%, cosolvent 5%-15%, moisturizer 0.5%-15%, preservative 0.01%-1.5%, penetration enhancer 0.1%-5%, and the rest is purified water.

[0027] Furthermore, the analgesic spray comprises 1.0% to 8.0% of flurbiprofen, 8% to 12% of a solubilizing agent, 5% to 10% of a moisturizing agent, 0.01% to 1.0% of a preservative and 0.5% to 3% of a penetration enhancer, and the remainder is purified water.

[0028] The co-solvent is selected from at least one of ethanol, acetone, propylene glycol, 1,3-butanediol and isopropanol; preferably ethanol.

[0029] Among them, the preservative is selected from one or more of methylparaben, propylparaben, hydroxyacetophenone, sorbic acid, and phenoxyethanol; preferably, methylparaben and propylparaben are used in combination.

[0030] Wherein, the penetration enhancer is selected from at least one of peppermint oil, azone and propylene glycol; preferably, the penetration enhancer is peppermint oil.

[0031] The moisturizer is at least one of butylene glycol, pentylene glycol, glycerin, polyethylene glycol, cetyl palmitate, and alkyl polymethylsiloxane; preferably glycerin.

[0032] The preparation method of the analgesic spray comprises the following steps:

[0033] 1) dissolving flurbiprofen in ethanol, stirring and dissolving to obtain an API solution;

[0034] 2) Take an appropriate amount of purified water, add methylparaben and propylparaben, stir and dissolve at 70-90° C. to obtain a transparent uniform solution, cool to room temperature, and set aside;

[0035] 3) adding the solution in 1) to 2), stirring evenly to obtain a mixed solution;

[0036] 4) Add glycerin and peppermint oil to the mixed solution, stir evenly, and then add purified water to the required amount to obtain the product;

[0037] 5) Filter the resulting solution and fill it into a spray bottle according to the required amount, and equip it with a quantitative spray pump.

[0038] Based on the above technical solution, the present invention provides the following partial embodiments:

[0039] Example 1

[0040] Table 1 Prescription composition and dosage in Example 1

[0041] Component name effect Dosage Flurbiprofen Active ingredients 10g Ethanol Solvents 80g glycerin Moisturizer 100g peppermint Penetration enhancers 7g Methylparaben Antibacterial Agents 0.7g Propylparaben Antibacterial Agents 0.35g Purified water Solvents Add to 1000g

[0042] Example 2

[0043] Table 2 Prescription composition and dosage in Example 2

[0044]

[0045]

[0046] Example 3

[0047] Table 3 Prescription composition and dosage in Example 3

[0048] Component name effect Dosage Flurbiprofen Active ingredients 80g Ethanol Solvents 200g glycerin Moisturizer 150g peppermint Penetration enhancers 9g Methylparaben Antibacterial Agents 0.7g Propylparaben Antibacterial Agents 0.35g Purified water Solvents Add to 1000g

[0049] The products prepared in Examples 1-3 above were used to verify the in vitro cumulative release of the same dose of flurbiprofen analgesic spray and flurbiprofen patch, and the results were as follows: Figure 1-3 As shown:

[0050] Depend on Figure 1 , 2 It can be seen that the same dose of flurbiprofen analgesic spray and flurbiprofen sustained-release preparation have almost the same efficacy at the same time; Figure 3 It can be seen that the high-dose flurbiprofen spray releases faster than the sustained-release patch at the same time, and the analgesic spray has a more stable efficacy and a faster effect. In addition, the analgesic spray has a simple preparation process, a moderate amount of raw materials and auxiliary materials, and a stable efficacy, which meets clinical needs.

[0051] The above shows and describes the basic principles, main features and advantages of the present invention. It is obvious to those skilled in the art that the present invention is not limited to the details of the above exemplary embodiments, and that the present invention can be implemented in other specific forms without departing from the spirit or basic features of the present invention. Therefore, no matter from which point of view, the embodiments should be regarded as exemplary and non-restrictive. The scope of the present invention is defined by the appended claims rather than the above description, and it is intended that all changes falling within the meaning and scope of the equivalent elements of the claims are included in the present invention.

[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 flurbiprofen-based analgesic spray, characterized in that: In terms of weight percentage, the components and contents of the analgesic spray are as follows: Flurbiprofen 0.5%-10%, cosolvent 5%-15%, moisturizer 0.5%-15%, preservative 0.01%-1.5%, penetration enhancer 0.1%-5%, and the rest is purified water.

2. The analgesic spray based on flurbiprofen according to claim 1, characterized in that: The components and contents of the analgesic spray are as follows: Flurbiprofen 1.0%-8.0%, cosolvent 8%-12%, moisturizer 5%-10%, preservative 0.01%-1.0%, penetration enhancer 0.5%-3%, and the rest is purified water.

3. A flurbiprofen-based analgesic spray according to claim 1, characterized in that: The co-solvent is at least one of ethanol, acetone, propylene glycol, 1,3-butanediol, and isopropanol.

4. The analgesic spray based on flurbiprofen according to claim 1, characterized in that: The preservative is one or more of methylparaben, propylparaben, hydroxyacetophenone, sorbic acid and phenoxyethanol.

5. The analgesic spray based on flurbiprofen according to claim 1, characterized in that: The penetration enhancer is at least one of peppermint oil, azone and propylene glycol.

6. The analgesic spray based on flurbiprofen according to claim 1, characterized in that: The moisturizing agent is at least one of butylene glycol, pentylene glycol, glycerin, polyethylene glycol, cetyl palmitate, and alkyl polymethylsiloxane.

7. The method for preparing the analgesic spray according to any one of claims 1 to 6, characterized in that: The following steps are involved: S1, dissolving flurbiprofen in ethanol, stirring and dissolving to obtain an API solution; S2, measure an appropriate amount of purified water, add methylparaben and propylparaben, stir and dissolve at 70-90° C. to obtain a transparent uniform solution, cool to room temperature, and set aside; S3, adding the solution in S1 to S2, stirring evenly to obtain a mixed solution; S4, adding glycerin and peppermint oil to the mixed solution, stirring evenly, and then adding purified water to the required amount to obtain; S5, filter the obtained solution and fill it into a spray bottle according to the required amount, and equip it with a quantitative spray pump.

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