A composition with solubilizing effect and its preparation method and application
Through the composition of cosolvent, glidant and inclusion, the problems of limited solubility and poor compatibility of antibiotic drugs are solved, and the stability and solubility of the drug under high temperature conditions are improved. It is suitable for drinking water administration preparations in livestock and poultry breeding.
Patent Information
- Application Number
- CN202211054787.0
- Authority / Receiving Office
- CN · China
- Patent Type
- Patents(China)
- Current Assignee / Owner
- Filing Date
- 2022-08-31
- Publication Date
- 2025-08-26
- Estimated Expiration
- 2042-08-31
AI Technical Summary
The solubility of commonly used antibiotic drugs in the prior art is limited, and there is a problem of poor compatibility when mixed with acidic compounds, which leads to the drug being prone to clumping and discoloration under high temperature conditions, affecting the content of the active ingredient of the drug.
The composition with solubilization effect is prepared by spray drying using a cosolvent, a glidant and an inclusion composition. The mass ratio of the cosolvent to the inclusion composition is 1:1-1:20, the mass ratio of the glidant to the inclusion composition is 1:100-3:20, the cosolvent includes acidic compounds and phosphates, the glidant includes sugars and starch, and the inclusion composition includes cyclodextrins.
It improves the solubility and stability of antibiotic drugs, ensures that the drugs do not agglomerate or discolor under high temperature conditions, enhances the compatibility between drugs and excipients, and improves the stability and solubility of drug preparations.
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Abstract
Description
Technical Field
[0001] The present invention relates to the technical field of veterinary chemical preparations, and more particularly to a composition with solubilization effect, a preparation method and application thereof. Background Art
[0002] With the development of intensive animal husbandry, livestock and poultry farming is gradually shifting towards large and super-large herds. The need for convenient, accurate, and uniform group drug delivery is driving increasingly stringent requirements for livestock and poultry pharmaceutical formulations, such as high water solubility, high stability, and high portability, particularly for formulations administered in drinking water. In recent years, group animal husbandry companies have seen increasing demand for water solubility in drinking water, making it a key focus of veterinary chemical formulation research and development.
[0003] Chlortetracycline hydrochloride, tyvalomycin, amoxicillin, florfenicol, tiamulin, tylosin, and oxytetracycline are commonly used antibiotics in livestock and poultry farming. Due to the physical and chemical properties of the drugs themselves, their solubility is limited. To improve the solubility of these drugs, it is often necessary to add cosolvents to the formulation. Acidic compounds such as malic acid, citric acid, and tartaric acid are commonly used cosolvents. These cosolvents have a significant solubility-enhancing effect on some basic compounds, such as chlortetracycline hydrochloride, tyvalomycin, and oxytetracycline hydrochloride. In addition, these acidic compounds are readily available and inexpensive. However, due to the inherent properties of these drugs, direct mixing with acidic compounds has the disadvantage of poor compatibility. For example, after directly mixing the drugs and acidic compounds and leaving them at 60°C for 10 days, clumping, discoloration, and a decrease in the content of the active ingredient of the drug will occur. Although other methods exist in the prior art to improve drug solubility, such as solid dispersion technology, melting technology, or the use of other expensive cosolvents, these methods have disadvantages such as complex processes, high costs, and low production capacity.
[0004] Therefore, those skilled in the art need to develop a composition having an efficient solubilizing effect on commonly used antibiotics and a preparation method thereof. Summary of the Invention
[0005] The present invention overcomes the deficiencies in the prior art and provides a composition with a solubilizing effect, a preparation method thereof, and an application thereof.
[0006] The purpose of the present invention is achieved through the following technical solutions.
[0007] In one aspect, the present invention provides a composition with a solubilizing effect, which is composed of a cosolvent, a flow aid and an inclusion compound, wherein the mass ratio of the components is as follows: the mass ratio of the cosolvent to the inclusion compound is 1:1-1:20, and the mass ratio of the flow aid to the inclusion compound is 1:100-3:20.
[0008] The cosolvent is one or more of acidic compounds such as malic acid, citric acid, tartaric acid, ethylenediaminetetraacetic acid, lactic acid and their salts or sodium phosphates, sodium carbonate, amino acids, vitamins, sodium lauryl sulfate, sodium docusate, poloxamer and polyethylene glycol.
[0009] Preferably, the cosolvent is one or more of malic acid, citric acid, tartaric acid, ethylenediaminetetraacetic acid, sodium phosphate, vitamins, sodium lauryl sulfate, docusate sodium, and polyethylene glycol, wherein the molecular weight of the polyethylene glycol is greater than 1000.
[0010] Preferably, the vitamins are vitamins B2, B6, B 12 , vitamin C or more.
[0011] The glidant is one or more of fructose, lactose, menthol, mannitol, oligoxylose, sodium carboxymethyl starch, soluble starch, water-soluble starch, microcrystalline cellulose, stearic acid, magnesium stearate, calcium stearate, and talc.
[0012] Preferably, the glidant is one or more of fructose, lactose, mannitol, xylo-oligosaccharides, soluble starch, water-soluble starch, sodium carboxymethyl starch, and microcrystalline cellulose.
[0013] The inclusion compound is one or two of beta-cyclodextrin, hydroxypropyl methylcellulose, carboxymethyl cellulose and povidone.
[0014] In another aspect, the present invention provides a method for preparing a composition having a solubilizing effect, the preparation method being as follows:
[0015] S1. Weigh the solvent, glidant and inclusion compound in proportion;
[0016] S2. The cosolvent is dissolved in 20-60 times its weight of water at 20-30 ° C, stirred to fully dissolve, to obtain a cosolvent solution, directly adding a flow aid to the above cosolvent solution to fully dissolve, or after the temperature of the above cosolvent solution is raised to 40-80 ° C, the flow aid is added thereto to fully dissolve to obtain a mixed solution I, directly adding the inclusion compound to the above mixed solution I to fully dissolve, or after the temperature of the above mixed solution I is raised to 60-90 ° C, the inclusion compound is added thereto to fully dissolve to obtain a mixed solution II;
[0017] S3. The mixed solution II prepared in S2 is spray-dried at an inlet air temperature of 110-150°C and a feed frequency of 10-40 Hz, and the resulting powder is collected. The powder is a composition having a solubilizing effect.
[0018] On the other hand, the present invention provides the use of the composition in improving the solubility of macrolides, tetracyclines, diterpenes, and penicillins, wherein the composition is mixed with the above-mentioned drugs in a mass ratio of 1:4-3:1.
[0019] The beneficial effects of the present invention are:
[0020] The composition of the present invention can play a certain role in improving the solubility of drugs such as macrolides (such as erythromycin, tilmicosin, tylosin, florfenicol), tetracyclines (such as chlortetracycline, oxytetracycline, doxycycline), diterpenes (such as valnemulin, tylosin), and penicillins (such as amoxicillin). In addition, the composition of the present invention does not react with the active ingredients of the drugs, and can ensure that the active ingredient content of the drugs is stable after the drugs are mixed with the composition and placed under high temperature conditions for a period of time, and the mixture of the drugs and the composition does not agglomerate or change color. DETAILED DESCRIPTION
[0021] Below in conjunction with specific embodiment, further set forth the present invention.Should be understood that these embodiments are only used to illustrate the present invention and are not used in limiting the scope of the present invention.In addition, should be understood that after reading the content taught by the present invention, those skilled in the art can make various changes or modifications to the present invention, and these equivalent forms fall equally within the scope limited by the appended claims of the application.
[0022] Example 1
[0023] A solubilizing composition is prepared from the following raw materials in a weight ratio of 1:0.3:6 for citric acid, lactose, and β-cyclodextrin. The preparation method comprises the following steps: accurately weighing the citric acid, lactose, and β-cyclodextrin components, dissolving the citric acid in 50 times its weight of water at 20-30°C, and stirring to dissolve the citric acid to obtain a citric acid solution; adding lactose to the citric acid solution and stirring to dissolve the mixture to obtain a mixed solution I; heating the mixed solution I to 80°C, and then adding β-cyclodextrin and stirring to dissolve the mixture to obtain a mixed solution II; spray drying the mixed solution II to obtain a powder, which constitutes the composition. Spray drying conditions are: an inlet air temperature of 110°C and a feed frequency of 20 Hz.
[0024] Example 2
[0025] A solubilizing composition is prepared from the following raw materials in a weight ratio of 1:0.3:3: malic acid, microcrystalline cellulose, and β-cyclodextrin. The preparation method comprises the following steps: accurately weighing the malic acid, microcrystalline cellulose, and β-cyclodextrin components; dissolving the malic acid in 60 times its weight of water at 20-30°C; stirring to dissolve the malic acid; and adding microcrystalline cellulose to the malic acid solution and stirring to dissolve the solution to obtain a mixed solution I. Raising the temperature of the mixed solution I to 80°C, β-cyclodextrin is then added and fully dissolved to obtain a mixed solution II. The mixed solution II is spray-dried to obtain a powder, which constitutes the composition. Spray-drying conditions are: an inlet air temperature of 120°C and a feed frequency of 15 Hz.
[0026] Example 3
[0027] A solubilizing composition is prepared from the following raw materials in a weight ratio of 1:0.3:15: tartaric acid, soluble starch, and β-cyclodextrin. The preparation method comprises the following steps: accurately weighing the tartaric acid, soluble starch, and β-cyclodextrin; dissolving the tartaric acid in 30 times its weight of water at 20-30°C; stirring to dissolve the tartaric acid; heating the tartaric acid solution to 80°C; then adding the soluble starch and stirring to dissolve the tartaric acid solution; obtaining a mixed solution I; adding β-cyclodextrin to the mixed solution I and dissolving it thoroughly; obtaining a mixed solution II; and spray-drying the mixed solution II to obtain a powder, which constitutes the composition. The spray drying conditions are: an inlet air temperature of 130°C and a feed frequency of 25 Hz.
[0028] Example 4
[0029] A solubilizing composition is prepared from the following raw materials in a weight ratio of 1:0.15:1: sodium phosphate, lactose, and β-cyclodextrin. The preparation method comprises the following steps: accurately weighing the sodium phosphate, lactose, and β-cyclodextrin components, dissolving the sodium phosphate in 20 times its weight of water at 20-30°C, stirring to dissolve, to obtain a sodium phosphate solution; adding lactose to the sodium phosphate solution and fully dissolving it to obtain a mixed solution I; heating the mixed solution I to 90°C, and then adding β-cyclodextrin and fully dissolving it to obtain a mixed solution II; spray-drying the mixed solution II to obtain a powder, which constitutes the composition. Spray-drying conditions are: an inlet air temperature of 130°C and a feed frequency of 10 Hz.
[0030] Example 5
[0031] A solubilizing composition is prepared from the following raw materials in a weight ratio of 1:0.05:0.5:6: tartaric acid, disodium EDTA, mannitol, and hydroxypropyl methylcellulose. The preparation method comprises the following steps: accurately weighing the tartaric acid, disodium EDTA, mannitol, and hydroxypropyl methylcellulose; dissolving the tartaric acid and disodium EDTA in 40 times their weight of water at 20-30°C; stirring to dissolve the tartaric acid and disodium EDTA; adding mannitol to the tartaric acid and disodium EDTA mixed solution and dissolving it thoroughly to obtain a mixed solution I; then adding hydroxypropyl methylcellulose to the mixed solution I and dissolving it thoroughly to obtain a mixed solution II; and spray-drying the mixed solution II to obtain a powder, which constitutes the composition. The spray drying conditions are: an inlet air temperature of 150°C and a feed frequency of 30 Hz.
[0032] Example 6
[0033] A solubilizing composition is prepared from the following raw materials in a weight ratio of 1:0.03:3: malic acid, water-soluble starch, and hydroxypropyl methylcellulose. The preparation method comprises the following steps: accurately weighing the malic acid, water-soluble starch, and hydroxypropyl methylcellulose components, dissolving the malic acid in 40 times its weight of water at 20-30°C, stirring to dissolve the malic acid, obtaining a malic acid solution, adding the water-soluble starch to the malic acid solution and fully dissolving it to obtain a mixed solution I, then adding hydroxypropyl methylcellulose to the mixed solution I and fully dissolving it to obtain a mixed solution II, spray-drying the mixed solution II to obtain a powder, which constitutes the composition. The spray-drying conditions are: an inlet air temperature of 130°C and a feed frequency of 30 Hz.
[0034] Example 7
[0035] A solubilizing composition is prepared from the following raw materials in a weight ratio: polyethylene glycol (molecular weight of polyethylene glycol is 6000), docusate sodium, xylooligosaccharides, and povidone in a mass ratio of 1:0.1:0.2:3. The preparation method comprises the following steps: accurately weighing the polyethylene glycol, docusate sodium, xylooligosaccharides, and povidone components; dissolving the polyethylene glycol and docusate sodium in 30 times their weight of water at 20-30°C; stirring to dissolve the polyethylene glycol and docusate sodium mixture; adding xylooligosaccharides to the polyethylene glycol and docusate sodium mixture and fully dissolving them to obtain a mixed solution I; raising the temperature of the mixed solution I to 60°C; then adding povidone and fully dissolving it to obtain a mixed solution II; spray drying the mixed solution II to obtain a powder, which is the composition. The spray drying conditions are: an inlet air temperature of 120°C and a feed frequency of 20 Hz.
[0036] Example 8
[0037] A solubilizing composition is prepared from the following raw materials in a weight ratio of 1:0.3:3: lactic acid, fructose, and hydroxypropyl methylcellulose. The preparation method comprises the following steps: accurately weighing the lactic acid, fructose, and hydroxypropyl methylcellulose components, dissolving the lactic acid in 60 times its weight of water at 20-30°C, stirring to dissolve the lactic acid, obtaining a lactic acid solution; adding fructose to the lactic acid solution and fully dissolving it to obtain a mixed solution I; then adding hydroxypropyl methylcellulose to the mixed solution I and fully dissolving it to obtain a mixed solution II; spray-drying the mixed solution II to obtain a powder, which constitutes the composition. The spray-drying conditions are: an inlet air temperature of 110°C and a feed frequency of 20 Hz.
[0038] Example 9
[0039] A solubilizing composition is prepared from the following raw materials in a weight ratio of 1:0.1:0.1:6: vitamin C, sodium lauryl sulfate, sodium carboxymethyl starch, and hydroxypropyl methylcellulose. The preparation method comprises the following steps: accurately weighing the vitamin C, sodium lauryl sulfate, sodium carboxymethyl starch, and hydroxypropyl methylcellulose; dissolving the vitamin C and sodium lauryl sulfate in 60 times their weight of water at 20-30°C; stirring to dissolve the vitamin C and sodium lauryl sulfate mixture; adding sodium carboxymethyl starch to the vitamin C and sodium lauryl sulfate mixture and dissolving the mixture thoroughly to obtain a mixed solution I; and adding hydroxypropyl methylcellulose to the mixed solution I and dissolving the mixture thoroughly to obtain a mixed solution II. The mixed solution II is spray-dried to obtain a powder, which constitutes the composition. The spray-drying conditions are: an inlet air temperature of 110°C and a feed frequency of 20 Hz.
[0040] Test Example 1
[0041] The composition obtained in Example 2 was mixed with chlortetracycline hydrochloride in a mass ratio of 1:1, with the remainder being anhydrous glucose, to prepare a 20% specification chlortetracycline hydrochloride soluble powder. At the same time, the above materials were directly mixed with the same materials and proportions (i.e., chlortetracycline hydrochloride, malic acid, microcrystalline cellulose, β-cyclodextrin, anhydrous glucose), and the difference in dissolution rate of the two in water and after being placed at a high temperature of 60°C for 10 days was compared. The test results are shown in Table 1:
[0042] Table 1 Stability test results of samples prepared by different preparation methods
[0043]
[0044] Test Example 2
[0045] The composition obtained in Example 6 was mixed with tylvalosin at a mass ratio of 2:5, with the remainder being anhydrous glucose, to prepare a 25% tylvalosin soluble powder. Simultaneously, the same materials and proportions (i.e., tylvalosin, malic acid, water-soluble starch, hydroxypropyl methylcellulose, and anhydrous glucose) were directly mixed, and the dissolution rates of the two materials in water and after exposure to a high temperature of 60°C for 10 days were compared. The test results are shown in Table 2:
[0046] Table 2 Stability test results of samples prepared by different preparation methods
[0047]
[0048] Test Example 3
[0049] The composition obtained in Example 1 was mixed with valnemulin hydrochloride in a mass ratio of 3:10, with the remainder being anhydrous glucose, to prepare a 20% valnemulin hydrochloride soluble powder. Simultaneously, the same materials and proportions (i.e., valnemulin hydrochloride, citric acid, lactose, β-cyclodextrin, and anhydrous glucose) were directly mixed, and the dissolution rates of the two materials in water and after exposure to a high temperature of 60°C for 10 days were compared. The test results are shown in Table 3:
[0050] Table 3 Stability test results of samples prepared by different preparation methods
[0051]
[0052] Test Example 4
[0053] The composition obtained in Example 4 was mixed with amoxicillin at a mass ratio of 1:4, with the remainder being anhydrous glucose, to prepare a 30% amoxicillin soluble powder. Simultaneously, the same materials and proportions (i.e., amoxicillin, sodium phosphate, lactose, β-cyclodextrin, and anhydrous glucose) were directly mixed, and the dissolution rates of the two materials in water and after exposure to a high temperature of 60°C for 10 days were compared. The test results are shown in Table 4:
[0054] Table 4 Stability test results of samples prepared by different preparation methods
[0055]
[0056] Test Example 5
[0057] The composition obtained in Example 5 was mixed with chlortetracycline hydrochloride in a mass ratio of 3:1, with the remainder being anhydrous glucose, to prepare a 20% specification chlortetracycline hydrochloride soluble powder. At the same time, the above materials were directly mixed with the same materials and proportions (i.e., chlortetracycline hydrochloride, tartaric acid, disodium edetate, mannitol, hydroxypropyl methylcellulose, anhydrous glucose), and the difference in dissolution rate of the two in water and after being placed at a high temperature of 60°C for 10 days was compared. The test results are shown in Table 5:
[0058] Table 5 Stability test results of samples prepared by different preparation methods
[0059]
[0060] Test Example 6
[0061] The composition obtained in Example 3 was mixed with tylvalosin at a mass ratio of 1:1, with the remainder being anhydrous glucose, to prepare a 25% tylvalosin soluble powder. Simultaneously, the same materials and proportions (i.e., tylvalosin, tartaric acid, soluble starch, β-cyclodextrin, and anhydrous glucose) were directly mixed, and the dissolution rates of the two materials in water and after exposure to a high temperature of 60°C for 10 days were compared. The test results are shown in Table 6:
[0062] Table 6 Stability test results of samples prepared by different preparation methods
[0063]
[0064] Test Example 7
[0065] The composition obtained in Example 7 was mixed with florfenicol in a mass ratio of 1:3, with the remainder being anhydrous glucose, to prepare a 30% florfenicol soluble powder. At the same time, the same materials and proportions (i.e., florfenicol, polyethylene glycol, docusate sodium, oligoxylose, povidone, anhydrous glucose) were directly mixed, and the dissolution rates of the two materials in water and after being placed at a high temperature of 60°C for 10 days were compared. The test results are shown in Table 7:
[0066] Table 7 Stability test results of samples prepared by different preparation methods
[0067]
[0068]
[0069] Test Example 8
[0070] The composition obtained in Example 8 was mixed with tiamulin fumarate in a mass ratio of 2:1, with the remainder being anhydrous glucose, to prepare a 10% tiamulin fumarate soluble powder. At the same time, the same materials and proportions (i.e., tiamulin fumarate, lactic acid, fructose, hydroxypropyl methylcellulose, anhydrous glucose) were directly mixed, and the dissolution rates of the two materials in water and after being placed at a high temperature of 60°C for 10 days were compared. The test results are shown in Table 8:
[0071] Table 8 Stability test results of samples prepared by different preparation methods
[0072]
[0073] Test Example 9
[0074] The composition obtained in Example 9 was mixed with oxytetracycline hydrochloride in a mass ratio of 1:2, with the remainder being anhydrous glucose, to prepare a 20% specification oxytetracycline hydrochloride soluble powder. At the same time, the above materials were directly mixed according to the same materials and proportions (i.e., oxytetracycline hydrochloride, vitamin C, sodium lauryl sulfate, sodium carboxymethyl starch, hydroxypropyl methylcellulose, anhydrous glucose), and the difference in dissolution rate of the two in water and after being placed at a high temperature of 60°C for 10 days was compared. The test results are shown in Table 9:
[0075] Table 9 Stability test results of samples prepared by different preparation methods
[0076]
[0077]
[0078] The test results of Test Examples 1-9 show that the drug-soluble powder prepared by the composition prepared in Examples 1-9 and chlortetracycline hydrochloride, tyvalomycin, valnemulin hydrochloride, amoxicillin, florfenicol, tyvalomycin fumarate, and oxytetracycline hydrochloride has better solubility and stability than the simple mixture obtained by directly mixing the above-mentioned drugs with solubilizers, glidants and inclusion compounds. Therefore, the composition of the present invention not only improves the compatibility of the excipients and the active ingredients, but also improves the stability and solubility of the drug mixture. At the same time, the composition is more convenient to use during the application process, and the quality of the drug preparation is more guaranteed.
[0079] Finally, it should be noted that the above embodiments are only used to illustrate the technical solutions of the present invention, rather than to limit it. Although the present invention has been described in detail with reference to the above embodiments, those skilled in the art should understand that they can still modify the technical solutions described in the above embodiments, or replace some or all of the technical features therein with equivalents. However, these modifications or replacements do not cause the essence of the corresponding technical solutions to deviate from the scope of the technical solutions of the embodiments of the present invention.
Claims
1. A composition having a solubilizing effect, characterized in that The composition comprises a solubilizer, a glidant, and an inclusion compound, wherein the mass ratios of the components are as follows: the mass ratio of the solubilizer to the inclusion compound is 1:1-1:20, and the mass ratio of the glidant to the inclusion compound is 1:100-3:20; the solubilizer is one or more of malic acid, citric acid, tartaric acid, disodium edetate, sodium phosphate, vitamin C, sodium lauryl sulfate, docusate sodium, and polyethylene glycol 6000; the glidant is one or more of fructose, lactose, mannitol, oligoxylose, sodium carboxymethyl starch, soluble starch, water-soluble starch, and microcrystalline cellulose; and the inclusion compound is one or two of β-cyclodextrin, hydroxypropyl methylcellulose, and povidone; The preparation method of the composition is as follows: S1. Weigh the solvent, glidant and inclusion compound in proportion; S2. The cosolvent is dissolved in 20-60 times its weight of water at 20-30 ° C, stirred to fully dissolve, to obtain a cosolvent solution, directly adding a flow aid to the above cosolvent solution to fully dissolve, or after the temperature of the above cosolvent solution is raised to 40-80 ° C, the flow aid is added thereto to fully dissolve to obtain a mixed solution I, directly adding the inclusion compound to the above mixed solution I to fully dissolve, or after the temperature of the above mixed solution I is raised to 60-90 ° C, the inclusion compound is added thereto to fully dissolve to obtain a mixed solution II; S3. The mixed solution II prepared in S2 is spray-dried at an inlet air temperature of 110-150°C and a feed frequency of 10-40 Hz, and the resulting powder is collected. The powder is a composition having a solubilizing effect.
2. The composition with solubilization according to claim 1, characterized in that The cosolvent is citric acid, the glidant is lactose, and the inclusion compound is β-cyclodextrin; the mass ratio of citric acid, lactose, and β-cyclodextrin in the composition is 1:0.3:6; the composition is used to improve the solubility of valnemulin hydrochloride; the composition is mixed with valnemulin hydrochloride in a mass ratio of 3:10, with the remainder being anhydrous glucose, to prepare a 20% valnemulin hydrochloride soluble powder.
3. The composition with solubilization according to claim 1, characterized in that The cosolvent is malic acid, the flow aid is microcrystalline cellulose, and the inclusion compound is β-cyclodextrin; the mass ratio of malic acid, microcrystalline cellulose, and β-cyclodextrin in the composition is 1:0.3:3; the composition is used to improve the solubility of chlortetracycline hydrochloride, and the composition is mixed with chlortetracycline hydrochloride in a mass ratio of 1:1, with the remainder being anhydrous glucose, to prepare a 20% chlortetracycline hydrochloride soluble powder.
4. The composition with solubilization according to claim 1, characterized in that The cosolvent is tartaric acid, the glidant is soluble starch, and the inclusion compound is β-cyclodextrin; the mass ratio of tartaric acid, soluble starch, and β-cyclodextrin in the composition is 1:0.3:15; the composition is used to improve the solubility of tylvalosin, and the composition is mixed with tylvalosin in a mass ratio of 1:1, with the remainder being anhydrous glucose, to prepare a 25% tylvalosin soluble powder.
5. The composition with solubilization according to claim 1, characterized in that The cosolvent is sodium phosphate, the glidant is lactose, and the inclusion compound is β-cyclodextrin; the mass ratio of sodium phosphate, lactose, and β-cyclodextrin in the composition is 1:0.15:1; the composition is used to improve the solubility of amoxicillin, and the resulting composition is mixed with amoxicillin in a mass ratio of 1:4, with the remainder being anhydrous glucose, to prepare a 30% amoxicillin soluble powder.
6. The composition having a solubilizing effect according to claim 1, characterized in that The cosolvent is tartaric acid and disodium edetate, the flow aid is mannitol, and the inclusion compound is hydroxypropyl methylcellulose; the mass ratio of tartaric acid, disodium edetate, mannitol, and hydroxypropyl methylcellulose in the composition is 1: 0.05:0.5:6; the application of the composition in improving the solubility of chlortetracycline hydrochloride is that the composition is mixed with chlortetracycline hydrochloride in a mass ratio of 3:1, and the balance is anhydrous glucose to prepare a 20% specification of chlortetracycline hydrochloride soluble powder.
7. The composition having a solubilizing effect according to claim 1, characterized in that The cosolvent is malic acid, the glidant is water-soluble starch, and the inclusion compound is hydroxypropyl methylcellulose; the mass ratio of malic acid, water-soluble starch, and hydroxypropyl methylcellulose in the composition is 1:0.03:3; the composition is used to improve the solubility of tylvalosin, and the resulting composition is mixed with tylvalosin at a mass ratio of 2:5, with the remainder being anhydrous glucose, to prepare a 25% tylvalosin soluble powder.
8. The composition having a solubilizing effect according to claim 1, characterized in that The cosolvent is polyethylene glycol 6000 and docusate sodium, the glidant is xylo-oligosaccharide, and the inclusion compound is povidone; the mass ratio of polyethylene glycol 6000, docusate sodium, xylo-oligosaccharide, and povidone in the composition is 1:0.1:0.2:3; the application of the composition in improving the solubility of florfenicol is that the composition is mixed with florfenicol in a mass ratio of 1:3, and the balance is anhydrous glucose to prepare a 30% florfenicol soluble powder.
9. The composition having a solubilizing effect according to claim 1, characterized in that The cosolvent is lactic acid, the glidant is fructose, and the inclusion compound is hydroxypropyl methylcellulose; the mass ratio of lactic acid, fructose, and hydroxypropyl methylcellulose in the composition is 1:0.3:3; the composition is used to improve the solubility of tiamulin fumarate, and the composition is mixed with tiamulin fumarate in a mass ratio of 2:1, with the remainder being anhydrous glucose, to prepare a 10% tiamulin fumarate soluble powder.
10. The composition having a solubilizing effect according to claim 1, characterized in that The cosolvent is vitamin C and sodium lauryl sulfate, the flow aid is sodium carboxymethyl starch, and the inclusion compound is hydroxypropyl methylcellulose; the mass ratio of vitamin C, sodium lauryl sulfate, sodium carboxymethyl starch, and hydroxypropyl methylcellulose in the composition is 1:0.1:0.1:6; the application of the composition in improving the solubility of oxytetracycline hydrochloride is that the composition is mixed with oxytetracycline hydrochloride in a mass ratio of 1:2, and the balance is anhydrous glucose to prepare a 20% specification of oxytetracycline hydrochloride soluble powder.
Citation Information
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Lactose-polyvidone-crospolyvidone premixed agent and preparation method thereof
CN101664556A