Mupirocin ointment easy to smear and good in stability and preparation method of mupirocin ointment

Mupirocin ointment was prepared by forming a supramolecular system with citric acid and glycerin and mixing it with polyethylene glycol. This solved the problems of uneven application and poor stability, resulting in an easy-to-apply and stable mupirocin ointment suitable for large-scale promotion.

CN121243059APending Publication Date: 2026-01-02JIANGSU SEMPOLL PHARMA
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Patent Information

Application Number
CN202511610396.6
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Filing Date
2025-11-05
Publication Date
2026-01-02

AI Technical Summary

Technical Problem

Mupirocin ointment is difficult to apply evenly, has poor stability, and some preparation methods are complex and costly.

Method used

A supramolecular system soluble in alcohol is formed by citric acid and glycerin. After adding mupirocin, it is mixed with polyethylene glycol 3350, polyethylene glycol 400 and propylene glycol to form a matrix solution. Finally, the mixture is stirred and condensed to obtain mupirocin ointment.

Benefits of technology

The prepared mupirocin ointment has good application uniformity, high stability, high mupirocin content, good storage stability, reduced side effects, and low cost.

✦ Generated by Eureka AI based on patent content.

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Abstract

The invention discloses mupirocin ointment easy to smear and good in stability and a preparation method of the mupirocin ointment, and belongs to the technical field of medicine preparation. The preparation method comprises the following steps: firstly, forming an alcohol-soluble supramolecular system by adopting citric acid and glycerol, and then adding mupirocin into the supramolecular system to form a mixed solution; uniformly mixing polyethylene glycol 3350, polyethylene glycol 400 and propylene glycol to obtain a matrix solution; finally, mixing, stirring and condensing the mixed solution and the matrix solution to obtain the mupirocin ointment. The mupirocin ointment prepared by the invention is easy to smear and good in stability, and has a wider application prospect.
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Description

TECHNICAL FIELD

[0001] The present application relates to a mupirocin ointment with good spreadability and stability and a preparation method thereof, belonging to the technical field of drug preparation. BACKGROUND

[0002] Mupirocin is a broad-spectrum antibiotic, mainly used for the treatment of skin infections caused by gram-positive cocci, such as impetigo, furuncles, folliculitis, etc. Its mechanism of action is to inhibit the isoleucine transferase in the process of bacterial protein synthesis, thereby preventing bacterial growth and reproduction. Mupirocin ointment, as one of its main dosage forms, has the advantages of convenient use, good local absorption, etc., and is favored by clinicians and patients.

[0003] Although mupirocin ointment has significant efficacy in the treatment of skin infections, the existing mupirocin ointment still has some problems in actual use, which to some extent limits its clinical application in a wide range and convenience. Specifically as follows: (1) Uneven spreading Traditional mupirocin ointment usually has a relatively viscous texture. This viscous texture requires a large external force to be evenly spread on the skin surface when applying, which not only brings inconvenience to patients, but also may cause uneven distribution of drugs, affecting the treatment effect. Especially in the treatment of large-area skin infection, the difficulty of application is greater, which is easy to cause drug waste. In addition, the viscous ointment may adhere to the skin surface during use, causing discomfort to the patient, and even may affect the patient's daily activities.

[0004] (2) Poor stability Mupirocin ointment is easily affected by external environmental factors such as temperature, humidity, light, etc. during storage, leading to degradation of the active ingredients of the drug, thereby reducing the drug efficacy. For example, in a high-temperature environment, the oil component in the ointment may be oxidized, making the texture of the ointment hard, and also accelerating the degradation of mupirocin, shortening its shelf life.

[0005] With the continuous improvement of people's attention to skin health, the performance requirements of skin external use drugs are also getting higher and higher. There is an urgent need in the market for a mupirocin ointment that is easy to spread and has good stability to meet the needs of patients for convenient and efficient treatment. However, it is not easy to develop such an ointment.

[0006] At present, many researchers have improved the texture of the ointment by adding different adjuvants, such as adding moisturizers, lubricants, etc., but these methods can only improve the application performance to a certain extent, and have limited effect on stability; some researchers have optimized the preparation process of the ointment, such as using different emulsifiers, controlling different reaction temperatures, etc., but these methods are complex in operation, high in cost, and difficult to realize large-scale promotion.

[0007] Therefore, there is an urgent need for a method for preparing mupirocin ointment with easy application and good stability, which is simple in operation and low in cost, to meet the market demand. SUMMARY

[0008] [TECHNICAL PROBLEM] Mupirocin ointment is not uniform in application, has poor stability, and some preparation methods are complex in operation and high in cost.

[0009] [TECHNICAL SCHEME] In order to solve the above problems, the present application provides a mupirocin ointment with easy application and good stability and a preparation method thereof. Specifically, the present application first forms an alcohol-soluble supramolecular system with citric acid and glycerol, then adds mupirocin to the supramolecular system to form a mixed solution; polyethylene glycol 3350, polyethylene glycol 400 and propylene glycol are mixed uniformly to obtain a base solution; finally, the mixed solution and the base solution are mixed, stirred and condensed to obtain the mupirocin ointment. The mupirocin ointment prepared by the present application has easy application and good stability, and has a more extensive application prospect.

[0010] The first object of the present application is to provide a method for preparing a mupirocin ointment with easy application and good stability, comprising the following steps: (1) Citric acid and glycerol are mixed uniformly at a molar ratio of 0.1-0.5:1 at 300-800 rpm and 70-80℃ to form a supramolecular system; then mupirocin is added to the supramolecular system and mixed uniformly at 500-800 rpm and 70-80℃ to obtain a mixed system; (2) Polyethylene glycol 3350, polyethylene glycol 400 and propylene glycol are dissolved and mixed uniformly to obtain a base solution; (3) The mixed solution and the base solution are mixed, stirred and condensed to obtain the mupirocin ointment.

[0011] In an embodiment of the present application, the molar ratio of citric acid to glycerol in step (1) is 0.2-0.4:1, for example, the molar ratio of citric acid to glycerol is 0.2:1, 0.3:1, 0.4:1, and specific point values between the above point values, limited by the length and for the sake of simplicity, the present application does not enumerate the specific point values included in the range.

[0012] In an embodiment of the present application, the rotation speed for forming the supramolecular system in step (1) can be 300, 400, 500, 600, 700, 800 rpm, and specific point values between the above-mentioned point values. Due to the limited space and for the sake of simplicity, the present application will not list the specific point values included in the range.

[0013] In an embodiment of the present application, the temperature for forming the supramolecular system in step (1) can be 70, 71, 72, 73, 74, 75, 76, 77, 78, 79, 80°C, and specific point values between the above-mentioned point values. Due to the limited space and for the sake of simplicity, the present application will not list the specific point values included in the range.

[0014] In an embodiment of the present application, the rotation speed for forming the mixed system in step (1) can be 500, 600, 700, 800 rpm, and specific point values between the above-mentioned point values. Due to the limited space and for the sake of simplicity, the present application will not list the specific point values included in the range.

[0015] In an embodiment of the present application, the temperature for forming the mixed system in step (1) can be 70, 71, 72, 73, 74, 75, 76, 77, 78, 79, 80°C, and specific point values between the above-mentioned point values. Due to the limited space and for the sake of simplicity, the present application will not list the specific point values included in the range.

[0016] In an embodiment of the present application, the mass ratio of mupirocin to the supramolecular system in step (1) is 10-20:100; for example, the mass ratio of mupirocin to the supramolecular system is 10:100, 15:100, 20:100, and specific point values between the above-mentioned point values. Due to the limited space and for the sake of simplicity, the present application will not list the specific point values included in the range.

[0017] In an embodiment of the present application, the mass ratio of polyethylene glycol 3350, polyethylene glycol 400, and propylene glycol in step (2) is 50:30-50:1-5; for example, the mass ratio of polyethylene glycol 3350, polyethylene glycol 400, and propylene glycol is 50:30:1, 50:30:2, 50:30:3, 50:30:4, 50:30:5, 50:40:1, 50:40:2, 50:40:3, 50:40:4, 50:40:5, 50:50:1, 50:50:2, 50:50:3, 50:50:4, 50:50:5, and specific point values between the above-mentioned point values. Due to the limited space and for the sake of simplicity, the present application will not list the specific point values included in the range.

[0018] In one embodiment of the present application, the mass ratio of the mixed solution and the substrate solution in step (2) is 100-120:800-1100; for example, the mass ratio of the mixed solution and the substrate solution is 100:800, 100:900, 100:1000, 110:800, 110:900, 110:1000, 110:1100, 120:800, 120:800, 120:900, 120:1000, 120:1100, and specific point values between the above-mentioned point values. Due to the limitation of the length and for the sake of simplicity, the present application will not list the specific point values included in the range.

[0019] In one embodiment of the present application, the dissolution in step (2) is 500-800 rpm, 80-90°C, and the mixed solution is dissolved uniformly; for example, the rotation speed of the dissolution can be 500, 600, 700, 800 rpm, and specific point values between the above-mentioned point values. Due to the limitation of the length and for the sake of simplicity, the present application will not list the specific point values included in the range; the temperature of the dissolution can be 80, 81, 82, 83, 84, 85, 86, 87, 88, 89, 90°C, and specific point values between the above-mentioned point values. Due to the limitation of the length and for the sake of simplicity, the present application will not list the specific point values included in the range.

[0020] In one embodiment of the present application, the stirring in step (3) is 50-100 rpm, 50-60°C, and the stirring is performed for 30-60 min; for example, the rotation speed of the stirring can be 50, 60, 70, 80, 90, 100 rpm, and specific point values between the above-mentioned point values. Due to the limitation of the length and for the sake of simplicity, the present application will not list the specific point values included in the range; the temperature of the stirring can be 50, 51, 52, 53, 54, 55, 56, 57, 58, 59, 60°C, and specific point values between the above-mentioned point values. Due to the limitation of the length and for the sake of simplicity, the present application will not list the specific point values included in the range; the stirring time is 30, 35, 40, 45, 50, 55, 60 min, and specific point values between the above-mentioned point values. Due to the limitation of the length and for the sake of simplicity, the present application will not list the specific point values included in the range.

[0021] In one embodiment of the present application, the condensation in step (3) is to stop heating, and the stirring is continued at 50-100 rpm until the ointment is formed; for example, the rotation speed of the stirring can be 50, 60, 70, 80, 90, 100 rpm, and specific point values between the above-mentioned point values. Due to the limitation of the length and for the sake of simplicity, the present application will not list the specific point values included in the range.

[0022] The second object of the present application is the mupirocin ointment prepared by the method of the present application, which is easy to apply and has good stability.

[0023] A third object of the present application is to provide a method for improving the uniformity and stability of mupirocin ointment, comprising the following steps: (1) mixing citric acid and glycerol uniformly at a molar ratio of 0.1-0.5:1, 300-800 rpm, and 70-80℃ to form a supramolecular system; then adding mupirocin into the supramolecular system, mixing uniformly at 500-800 rpm and 70-80℃ to obtain a mixed system; (2) dissolving and mixing polyethylene glycol 3350, polyethylene glycol 400, and propylene glycol uniformly to obtain a base solution; (3) mixing and stirring the mixed solution and the base solution, and condensing to obtain mupirocin ointment.

[0024] In an embodiment of the present application, the molar ratio of citric acid and glycerol in step (1) is 0.2-0.4:1, for example, the molar ratio of citric acid and glycerol is 0.2:1, 0.3:1, 0.4:1, and specific point values between the above-mentioned point values. Due to the limitation of length and for the sake of simplicity, the present application will not exhaustively list the specific point values included in the range.

[0025] In an embodiment of the present application, the rotation speed for forming the supramolecular system in step (1) can be 300, 400, 500, 600, 700, 800 rpm, and specific point values between the above-mentioned point values. Due to the limitation of length and for the sake of simplicity, the present application will not exhaustively list the specific point values included in the range.

[0026] In an embodiment of the present application, the temperature for forming the supramolecular system in step (1) can be 70, 71, 72, 73, 74, 75, 76, 77, 78, 79, 80℃, and specific point values between the above-mentioned point values. Due to the limitation of length and for the sake of simplicity, the present application will not exhaustively list the specific point values included in the range.

[0027] In an embodiment of the present application, the rotation speed for forming the mixed system in step (1) can be 500, 600, 700, 800 rpm, and specific point values between the above-mentioned point values. Due to the limitation of length and for the sake of simplicity, the present application will not exhaustively list the specific point values included in the range.

[0028] In an embodiment of the present application, the temperature for forming the mixed system in step (1) can be 70, 71, 72, 73, 74, 75, 76, 77, 78, 79, 80℃, and specific point values between the above-mentioned point values. Due to the limitation of length and for the sake of simplicity, the present application will not exhaustively list the specific point values included in the range.

[0029] In an embodiment of the present application, the mass ratio of mupirocin and supramolecular system in step (1) is 10-20:100; for example, the mass ratio of mupirocin and supramolecular system is 10:100, 15:100, 20:100, and specific point values between the above-mentioned point values, the specific point values included in the range are not listed exhaustively in view of the length and for the sake of simplicity.

[0030] In an embodiment of the present application, the mass ratio of polyethylene glycol 3350, polyethylene glycol 400, and propylene glycol in step (2) is 50:30-50:1-5; for example, the mass ratio of polyethylene glycol 3350, polyethylene glycol 400, and propylene glycol is 50:30:1, 50:30:2, 50:30:3, 50:30:4, 50:30:5, 50:40:1, 50:40:2, 50:40:3, 50:40:4, 50:40:5, 50:50:1, 50:50:2, 50:50:3, 50:50:4, 50:50:5, and specific point values between the above-mentioned point values, the specific point values included in the range are not listed exhaustively in view of the length and for the sake of simplicity.

[0031] In an embodiment of the present application, the mass ratio of mixed solution and matrix solution in step (2) is 100-120:800-1100; for example, the mass ratio of mixed solution and matrix solution is 100:800, 100:900, 100:1000, 110:800, 110:900, 110:1000, 110:1100, 120:800, 120:800, 120:900, 120:1000, 120:1100, and specific point values between the above-mentioned point values, the specific point values included in the range are not listed exhaustively in view of the length and for the sake of simplicity.

[0032] In an embodiment of the present application, the dissolution in step (2) is 500-800 rpm, 80-90℃, and the mixed solution is dissolved uniformly; for example, the rotation speed of dissolution can be 500, 600, 700, 800 rpm, and specific point values between the above-mentioned point values, the specific point values included in the range are not listed exhaustively in view of the length and for the sake of simplicity; the temperature of dissolution can be 80, 81, 82, 83, 84, 85, 86, 87, 88, 89, 90℃, and specific point values between the above-mentioned point values, the specific point values included in the range are not listed exhaustively in view of the length and for the sake of simplicity.

[0033] In an embodiment of the present application, the stirring in step (3) is stirring at 50-100 rpm, 50-60℃ for 30-60 min; for example, the stirring speed can be 50, 60, 70, 80, 90, 100 rpm, and specific point values between the above-mentioned point values, the present application does not list the specific point values included in the range for the sake of brevity and conciseness, and the present application does not list the specific point values included in the range for the sake of brevity and conciseness; the stirring temperature can be 50, 51, 52, 53, 54, 55, 56, 57, 58, 59, 60℃, and specific point values between the above-mentioned point values, the present application does not list the specific point values included in the range for the sake of brevity and conciseness, and the present application does not list the specific point values included in the range for the sake of brevity and conciseness; the stirring time is 30, 35, 40, 45, 50, 55, 60 min, and specific point values between the above-mentioned point values, the present application does not list the specific point values included in the range for the sake of brevity and conciseness, and the present application does not list the specific point values included in the range for the sake of brevity and conciseness.

[0034] In an embodiment of the present application, the condensation in step (3) is stopping heating and continuing stirring at 50-100 rpm until the ointment is formed; for example: the stirring speed can be 50, 60, 70, 80, 90, 100 rpm, and specific point values between the above-mentioned point values, the present application does not list the specific point values included in the range for the sake of brevity and conciseness.

[0035] [Beneficial effects] (1) The mupirocin ointment prepared by the present application has high mupirocin content, and the content on the 20th day is >95%; that is, the content change is small at 40℃ for 20 days.

[0036] (2) The mupirocin ointment prepared by the present application has a kinematic viscosity of 37-38 mm 2 / s and a rotational viscosity of 4000-5000 mPa·s, which is suitable for application and has good uniformity.

[0037] (3) The mupirocin ointment prepared by the present application has a total impurity content of less than 0.25% after being stored for 6 months, and has good stability.

[0038] (4) The mupirocin ointment prepared by the present application is easy to apply uniformly after centrifugal treatment, and has good centrifugal stability.

[0039] (5) The mupirocin ointment prepared by the present application can ensure the effective concentration of mupirocin on the skin surface, thereby enhancing the inhibition of bacteria and reducing possible side effects.

[0040] (6) The preparation method of the present application is simpler and has low cost. DETAILED DESCRIPTION

[0041] The following describes preferred embodiments of the present application, and it should be understood that the embodiments are for better explaining the present application and are not intended to limit the present application.

[0042] Test method: 1. Content test: The mupirocin ointment was placed at 40℃ for 0, 10, 20 days; then 15mg of sample was taken and the content of mupirocin was tested by liquid chromatography.

[0043] 2. Viscosity test: The kinematic viscosity and rotational viscosity were determined according to the method of viscosity determination in General Test Methods of Chinese Pharmacopoeia 2020 edition Part IV 0633.

[0044] 3. Storage stability test: The mupirocin ointment was placed at 45℃ and 75% relative humidity for 6 months, and samples were taken at the end of the first month, the third month and the sixth month during the test period for detection of related substance content.

[0045] Specifically, the test was performed by chromatography: A sample solution with a mass fraction of 30% was prepared using a phosphate buffer with a pH of 6.3; Mobile phase: ammonium acetate solution with a pH of 5.7 Tetrahydrofuran; Column temperature: 30℃; Flow rate: 0.8mL / min; Detection wavelength: 240nm; Injection volume: 20μL; Elution: ammonium acetate solution with a pH of 5.7 and 60% ethanol aqueous solution.

[0046] 4. Centrifugal stability test: The mupirocin ointment was placed at 45℃ for 24h and centrifuged at 5000rpm for 10min, and its smearing performance was determined.

[0047] The mupirocin ointment was placed at 4℃ for 24h and centrifuged at 5000rpm for 10min, and its smearing performance was determined.

[0048] Example 1 A method for preparing a mupirocin ointment with good smearing and stability, comprising the following steps: (1) Citric acid and glycerol were mixed uniformly at a molar ratio of 0.3:1 at 700rpm and 75℃ to form a supramolecular system; then 15mg of mupirocin was added to 100mg of the supramolecular system and mixed uniformly at 500rpm and 70℃ to obtain a mixed system; (2) 500 mg of polyethylene glycol 3350, 400 mg of polyethylene glycol 400, 5 mg of propylene glycol were dissolved and mixed uniformly at 600 rpm and 85°C to obtain a base solution; (3) The mixed solution and the base solution were stirred at 90 rpm and 55°C for 60 min; the heating was stopped, and the stirring was continued at 100 rpm until the ointment was formed to obtain the mupirocin ointment.

[0049] Example 2 A method for preparing a mupirocin ointment with good spreadability and stability comprises the following steps: (1) Citric acid and glycerol were mixed uniformly at a molar ratio of 0.4:1 at 700 rpm and 75°C to form a supramolecular system; then 20 mg of mupirocin was added to 100 mg of the supramolecular system, and mixed uniformly at 500 rpm and 70°C to obtain a mixed system; (2) 500 mg of polyethylene glycol 3350, 500 mg of polyethylene glycol 400, 3 mg of propylene glycol were dissolved and mixed uniformly at 600 rpm and 85°C to obtain a base solution; (3) The mixed solution and the base solution were stirred at 90 rpm and 55°C for 60 min; the heating was stopped, and the stirring was continued at 100 rpm until the ointment was formed to obtain the mupirocin ointment.

[0050] Example 3 A method for preparing a mupirocin ointment with good spreadability and stability comprises the following steps: (1) Citric acid and glycerol were mixed uniformly at a molar ratio of 0.2:1 at 700 rpm and 75°C to form a supramolecular system; then 10 mg of mupirocin was added to 100 mg of the supramolecular system, and mixed uniformly at 500 rpm and 70°C to obtain a mixed system; (2) 500 mg of polyethylene glycol 3350, 300 mg of polyethylene glycol 400, 3 mg of propylene glycol were dissolved and mixed uniformly at 600 rpm and 85°C to obtain a base solution; (3) The mixed solution and the base solution were stirred at 90 rpm and 55°C for 60 min; the heating was stopped, and the stirring was continued at 100 rpm until the ointment was formed to obtain the mupirocin ointment.

[0051] Comparative Example 1 Compared with Example 1, the difference is that the supramolecular system is not used, and the mixing is directly performed; Specifically comprising the following steps: (1) 38 mg of citric acid, 62 mg of glycerol, and 5 mg of mupirocin were mixed uniformly at 700 rpm and 75°C to obtain a mixed system; (2) 500 mg of polyethylene glycol 3350, 400 mg of polyethylene glycol 400, 5 mg of propylene glycol were dissolved and mixed uniformly at 600 rpm and 85°C to obtain a matrix solution; (3) The mixed solution and the matrix solution were stirred at 90 rpm and 55°C for 60 min; heating was stopped, and stirring was continued at 100 rpm until an ointment was formed to obtain the mupirocin ointment.

[0052] Comparative Example 2 Compared with Example 1, the difference is that a one-pot method is directly mixed to prepare: Specifically includes the following steps: 38 mg of citric acid, 62 mg of glycerol, 5 mg of mupirocin, 500 mg of polyethylene glycol 3350, 400 mg of polyethylene glycol 400, and 5 mg of propylene glycol were stirred at 900 rpm and 85°C for 120 min, heating was stopped, and stirring was continued at 100 rpm until an ointment was formed to obtain the mupirocin ointment.

[0053] Comparative Example 3 Compared with Example 1, the difference is that citric acid is replaced by malic acid; Specifically includes the following steps: (1) Malic acid and glycerol were mixed uniformly at a molar ratio of 0.3:1, 700 rpm, and 75°C to form a supramolecular system; then 15 mg of mupirocin was added to 100 mg of the supramolecular system, and mixed uniformly at 500 rpm and 70°C to obtain a mixed system; (2) 500 mg of polyethylene glycol 3350, 400 mg of polyethylene glycol 400, and 5 mg of propylene glycol were dissolved and mixed uniformly at 600 rpm and 85°C to obtain a matrix solution; (3) The mixed solution and the matrix solution were stirred at 90 rpm and 55°C for 60 min; heating was stopped, and stirring was continued at 100 rpm until an ointment was formed to obtain the mupirocin ointment.

[0054] Comparative Example 4 Compared with Example 1, the difference is that glycerol is replaced by propylene glycol; Specifically includes the following steps: (1) Citric acid and propylene glycol were mixed uniformly at a molar ratio of 0.3:1, 700 rpm, and 75°C to form a supramolecular system; then 15 mg of mupirocin was added to 100 mg of the supramolecular system, and mixed uniformly at 500 rpm and 70°C to obtain a mixed system; (2) 500 mg of polyethylene glycol 3350, 400 mg of polyethylene glycol 400, and 5 mg of propylene glycol were dissolved and mixed uniformly at 600 rpm and 85°C to obtain a matrix solution; (3) The mixed solution and the base solution are stirred at 90 rpm and 55°C for 60 min; the heating is stopped, and the stirring is continued at 100 rpm until the ointment is formed to obtain the mupirocin ointment.

[0055] The obtained mupirocin ointment is subjected to performance testing, and the test results are as follows: As can be seen from Table 1, the mupirocin content in the mupirocin ointment prepared in Examples 1-3 is high, and the content on the 20th day is greater than 95%; that is, at high temperature 40°C, the content change in 20 days is small. However, the mupirocin content in the mupirocin ointment prepared in Comparative Examples 1-4 is less than 90% on the 20th day, the content change is large, and the stability is poor.

[0056] Table 1

[0057] As can be seen from Table 2, the kinematic viscosity of the mupirocin ointment prepared in Examples 1-3 is 37-38 mm 2 / s, and the rotational viscosity is 4000-5000 mPa·s, which is suitable for smearing; the kinematic viscosity of the mupirocin ointment prepared in Comparative Examples 1 and 2 is 38-41 mm 2 / s, and the rotational viscosity is 5000-5500 mPa·s, which is difficult to smear; the kinematic viscosity of the mupirocin ointment prepared in Comparative Examples 3 and 4 is 35-38 mm 2 / s, and the rotational viscosity is 3500-4000 mPa·s, which is small in viscosity and is difficult to completely cover the skin surface to play a role. That is, the ointment viscosity is too low, the solution is too dilute, although it is easy to smear, but it is difficult to uniformly cover the skin surface; the viscosity is too high, which may be uneven, too thick, and the uniformity of smearing is reduced.

[0058] Table 2

[0059] As can be seen from Table 3, after being stored for 6 months, the total impurity content in the mupirocin ointment prepared in Examples 1-3 is less than 0.25%, and the stability is good. However, after being stored for 6 months, the content of the mupirocin ointment prepared in Comparative Examples 1-4 is more than 0.30%, and the stability is poor.

[0060] Table 3 Test results of total impurity content in ointment

[0061] As can be seen from Table 4, after being subjected to centrifugal treatment, the mupirocin ointment prepared in Examples 1-3 is easy to smear uniformly; that is, the centrifugal stability is good.

[0062] Table 4 Test results of centrifugal stability

[0063] Although the present application has been disclosed in its preferred embodiments with reference to the accompanying drawings, it is to be understood that the application is not limited to those precise embodiments, and that various changes and modifications can be effected therein by one skilled in the art without departing from the scope or spirit of the application, therefore, the scope of the present application should be limited only by the appended claims.

Claims

1. A method for preparing mupirocin ointment that is easy to apply and has good stability, characterized in that, Includes the following steps: (1) Citric acid and glycerol are mixed evenly at a molar ratio of 0.1-0.5:1 at 300-800 rpm and 70-80℃ to form a supramolecular system; then mupirocin is added to the supramolecular system and mixed evenly at 500-800 rpm and 70-80℃ to obtain a mixed system. (2) Dissolve and mix polyethylene glycol 3350, polyethylene glycol 400 and propylene glycol evenly to obtain a matrix solution; (3) Mix the mixed solution and the matrix solution, stir and condense to obtain mupirocin ointment.

2. The method according to claim 1, characterized in that, In step (1), the molar ratio of citric acid to glycerol is 0.2-0.4:

1.

3. The method according to claim 1, characterized in that, In step (1), the mass ratio of mupirocin to the supramolecular system is 10-20:

100.

4. The method according to claim 1, characterized in that, In step (2), the mass ratio of polyethylene glycol 3350, polyethylene glycol 400, and propylene glycol is 50:30-50:1-5.

5. The method according to claim 1, characterized in that, In step (2), the mass ratio of the mixed solution to the matrix solution is 100-120:800-1100.

6. The method according to claim 1, characterized in that, In step (2), the dissolution is carried out at 500-800 rpm and 80-90℃ to dissolve and mix evenly.

7. The method according to claim 1, characterized in that, In step (3), the stirring is carried out at 50-100 rpm and 50-60℃ for 30-60 minutes.

8. The method according to claim 1, characterized in that, In step (3), condensation means stopping heating and continuing to stir at 50-100 rpm until an ointment is formed.

9. The mupirocin ointment prepared by the method according to any one of claims 1-8 is easy to apply and has good stability.

10. A method for improving the uniformity and stability of mupirocin ointment application, characterized in that, Includes the following steps: (1) Citric acid and glycerol are mixed evenly at a molar ratio of 0.1-0.5:1 at 300-800 rpm and 70-80℃ to form a supramolecular system; then mupirocin is added to the supramolecular system and mixed evenly at 500-800 rpm and 70-80℃ to obtain a mixed system. (2) Dissolve and mix polyethylene glycol 3350, polyethylene glycol 400 and propylene glycol evenly to obtain a matrix solution; (3) Mix the mixed solution and the matrix solution, stir and condense to obtain mupirocin ointment.

Citation Information

Patent Citations

  • Mupirocin ointment and preparation method thereof

    CN102335122A

  • Mupirocin ointment as well as preparation and application methods thereof

    CN119302903A

  • Mupirocin compositions for topical use, an improved process of making same and methods of using same

    US20050123576A1