CN106727618B - Compound sulfamethoxazole oral suspension and preparation method thereof - Google Patents
Compound sulfamethoxazole oral suspension and preparation method thereof Download PDFInfo
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- CN106727618B CN106727618B CN201710000282.9A CN201710000282A CN106727618B CN 106727618 B CN106727618 B CN 106727618B CN 201710000282 A CN201710000282 A CN 201710000282A CN 106727618 B CN106727618 B CN 106727618B
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/10—Dispersions; Emulsions
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/63—Compounds containing para-N-benzenesulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonyl hydrazide
- A61K31/635—Compounds containing para-N-benzenesulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonyl hydrazide having a heterocyclic ring, e.g. sulfadiazine
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
- A61K47/38—Cellulose; Derivatives thereof
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
- A61K9/0056—Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals
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Abstract
The invention claims a compound sulfamethoxazole oral suspension and a preparation method thereof, wherein each 100ml of the compound sulfamethoxazole oral suspension comprises the following raw materials: 2.0-3.5 g of sulfamethoxazole, 1.0-2.0 g of trimethoprim, 2.0-3.5 g of citric acid and salts thereof, 0.1-0.5 g of sodium carboxymethylcellulose, 0.1-1.5 g of sodium benzoate, 0.1-0.5 g of sodium bisulfite, 0.01-0.1 g of EDTA-2Na, 1-2.5 g of sodium chloride and the balance of purified water. The preparation method is simple, the process is controllable, the compatibility stability of the composition is high, and the preservation degree of the drug effect of the components is high.
Description
Technical Field
The invention relates to the technical field of medicines, in particular to a compound medicinal preparation, and particularly relates to a compound sulfamethoxazole oral suspension.
Background
Sulfonamides are the first chemical class of drugs that are effective in preventing and treating systemic bacterial infections. Although antibiotics and quinolone drugs are mostly used for clinically treating bacterial infection at present, sulfanilamide drugs have good treatment effects on some infectious diseases, epidemic cerebrospinal meningitis and plague, and are still used up to now. In addition, the sulfonamides have the advantages of convenient use, stable property, low price and the like.
The sulfanilamide drug and the sulfanilamide synergist trimethoprim are used together in a ratio of 4:1 or 5: 1. For example, the sulfanilamide drug, namely the Suxianning (French Vickers), is 40 percent of sulfadiazine and 8 percent of trimethoprim, and has obvious clinical synergism. However, the composition still has the problems of compatibility stability and precipitation, and some preparation methods need to be heated to boiling to dissolve components, so that the drug effect and the components are adversely affected. The present invention is directed to solving the above problems.
Disclosure of Invention
The invention aims to provide the compound sulfamethoxazole oral suspension with good stability and good drug dispersibility.
In order to solve the technical problems, the technical scheme of the invention is as follows: the compound sulfamethoxazole oral suspension comprises the following raw materials per 100 ml: 2.0-3.5 g of sulfamethoxazole, 1.0-2.0 g of trimethoprim, 2.0-3.5 g of citric acid and salts thereof, 0.1-0.5 g of sodium carboxymethylcellulose, 0.1-1.5 g of sodium benzoate, 0.1-0.5 g of sodium bisulfite, 0.01-0.1 g of EDTA-2Na, 1-2.5 g of sodium chloride and the balance of purified water.
Preferably, the compound sulfamethoxazole oral suspension comprises the following raw materials per 100 ml: 2.0-3.0 g of sulfamethoxazole, 1-1.5 g of trimethoprim, 2.0-3.0 g of citric acid and salts thereof, 0.2-0.5 g of sodium carboxymethylcellulose, 0.1-1.0 g of sodium benzoate, 0.1-0.3 g of sodium bisulfite, 0.01-0.05 g of EDTA-2Na, 1-1.5 g of sodium chloride and the balance of purified water.
Preferably, the compound sulfamethoxazole oral suspension comprises the following raw materials per 100 ml: 2.5g of sulfamethoxazole, 1g of trimethoprim, 0.78g of citric acid, 1.74g of sodium citrate, 0.4g of sodium carboxymethylcellulose, 0.5g of sodium benzoate, 0.1g of sodium bisulfite, 0.01g of EDTA-2Na, 1g of sodium chloride and the balance of purified water.
Preferably, the citric acid and its salts include citric acid and sodium or potassium citrate.
The second aspect of the invention provides a preparation method of compound sulfamethoxazole oral suspension, which comprises the following steps:
(1) heating purified water to 45-60 ℃, adding citric acid and salts thereof, stirring and dissolving to obtain solution A for later use,
(2) adding sodium carboxymethylcellulose and trimethoprim into the solution A, stirring and dissolving to obtain solution B,
(3) adding sulfamethoxazole, sodium benzoate, sodium bisulfite, EDTA-2Na, and sodium chloride into the solution B, stirring and dissolving to obtain solution C,
(4) and cooling the C liquid to room temperature, adjusting the pH value to be 4.0-6.0 by using organic acid, and adding water to a proper amount to obtain the compound sulfamethoxazole oral suspension.
Preferably, the solutions in the step (2) and the step (3) are both kept at 45-60 ℃.
Preferably, in the step (4), the organic acid is a 20% citric acid solution.
Preferably, in the step (4), the room temperature is 20-25 ℃.
Preferably, the preparation method of the compound sulfamethoxazole oral suspension comprises the following steps:
(1) 70ml of purified water was heated to 55 ℃ and maintained, and 0.78g of citric acid and 1.74g of sodium citrate were added, stirred and dissolved.
(2) 0.4g of sodium carboxymethylcellulose and 1g of trimethoprim are added, stirred well and allowed to dissolve.
(3) 2.5g of sulfamethoxazole, 0.5g of sodium benzoate, 0.1g of sodium bisulfite, 0.01g of EDTA-2 Na0.1 g of sodium chloride are added in sequence, and the mixture is fully stirred and dissolved.
(4) Cooling to room temperature of 25 deg.C, measuring pH, adjusting pH to 4.0-6.0 with 20% citric acid solution, and adding water to 100 ml.
The medicament is mainly used for veterinary use, mainly refers to pet animals, and comprises, but is not limited to, dogs, cats, rabbits and the like.
Compared with the scheme in the prior art, the invention has the advantages that: the sodium benzoate is used as a preservative, the EDTA-2Na is used as a complexing agent, the purpose of inhibiting the autoxidation reaction is achieved, and the sodium benzoate and the sodium bisulfite cooperate to achieve the antioxidation effect. Sodium carboxymethylcellulose (CMC-Na) is used as a suspending agent, so that the fluidity is good, the redispersibility is good, and the wall hanging condition is qualified. The sodium chloride is used as a deflocculant, the sedimentation volume ratio is more than 0.95, the flocculation degree is more than 1.00, no wall is hung, and the fluidity is good. Under the coordination of citric acid and sodium citrate buffer solution, trimethoprim can be rapidly dissolved at a relatively high temperature of 55 ℃, so that other main medicines and auxiliary materials are not agglomerated when being added. The pH value is set to be 4.0-6.0, and each monitoring index is optimal.
The preparation method is simple, the process is controllable, the compatibility stability of the composition is high, and the preservation degree of the drug effect of the components is high.
Detailed Description
The above-described scheme is further illustrated below with reference to specific examples. It should be understood that these examples are for illustrative purposes and are not intended to limit the scope of the present invention. The conditions used in the examples may be further adjusted according to the conditions of the particular manufacturer, and the conditions not specified are generally the conditions in routine experiments.
Example 1
A compound sulfamethoxazole oral suspension is prepared by the following method:
step (1): heating purified water 70ml to 55 deg.C, adding citric acid 0.78g and sodium citrate 1.74g, stirring and dissolving,
step (2): adding 0.4g sodium carboxymethylcellulose and 1g trimethoprim, stirring thoroughly and dissolving,
and (3): 2.5g of sulfamethoxazole, 0.5g of sodium benzoate, 0.1g of sodium bisulfite, 0.01g of EDTA-2 Na0.1 g of sodium chloride are added in sequence, and the mixture is fully stirred and dissolved.
And (4): cooling to room temperature of 25 deg.C, measuring pH, adjusting pH to 4.0-6.0 with 20% citric acid solution, and adding water to 100 ml.
Example 2
A compound sulfamethoxazole oral suspension is prepared by the following steps (1): 70ml of purified water was taken, heated to 50 ℃ and kept there, 0.83g of citric acid and 1.77g of sodium citrate were added, stirred and dissolved.
Step (2): 0.5g of sodium carboxymethylcellulose and 1.5g of trimethoprim are added, stirred well and allowed to dissolve.
And (3): 3.0g of sulfamethoxazole, 0.5g of sodium benzoate, 0.2g of sodium bisulfite, 0.01g of EDTA-2 Na0.5 g of sodium chloride are added in sequence, and the mixture is fully stirred and dissolved.
And (4): cooling to room temperature of 25 deg.C, measuring pH, adjusting pH to 4.0-6.0 with 20% citric acid solution, and adding water to 100 ml.
Example 3
A compound sulfamethoxazole oral suspension is prepared by the following steps (1): 70ml of purified water was taken, heated to 60 ℃ and kept there, and 0.90g of citric acid and 1.50g of sodium citrate were added, stirred and dissolved.
Step (2): 0.3g of sodium carboxymethylcellulose and 1.0g of trimethoprim are added, stirred well and allowed to dissolve.
And (3): 3.5g of sulfamethoxazole, 0.5g of sodium benzoate, 0.3g of sodium bisulfite, 0.05g of EDTA-2Na0.05g and 1.0g of sodium chloride are added in sequence, and the mixture is fully stirred and dissolved.
And (4): cooling to room temperature of 20 ℃, measuring the pH value, adjusting the pH value to 4.0-6.0 by using 20% citric acid solution, and supplementing water to 120 ml.
Example 4
A compound sulfamethoxazole oral suspension is prepared by the following steps (1): 70ml of purified water was taken, heated to 55 ℃ and kept there, and 1.20g of citric acid and 2.00g of sodium citrate were added, stirred and dissolved.
Step (2): 0.2g of sodium carboxymethylcellulose and 1.5g of trimethoprim are added, stirred well and allowed to dissolve.
And (3): 3g of sulfamethoxazole, 0.5g of sodium benzoate, 0.2g of sodium bisulfite, 0.01g of EDTA-2Na0.0 g of sodium chloride are added in sequence, and the mixture is fully stirred and dissolved.
And (4): cooling to room temperature of 20 ℃, measuring the pH value, adjusting the pH value to 4.0-6.0 by using 20% sodium citrate solution, and supplementing water to 100 ml.
Firstly, stability test: the stability of the compound sulfamethoxazole oral suspension is compared
The compound sulfamethoxazole oral suspension of the embodiments 1 to 4 of the invention is respectively placed at the room temperature of 25 ℃ for observation for 6 to 30 months, and the content changes of the solution and the effective substances are compared and detected. The results are shown in table 1:
TABLE 1
The suspension prepared by the invention has high stability, and particularly has small loss of sulfamethoxazole and trimethoprim which are effective components.
The above examples are only for illustrating the technical idea and features of the present invention, and the purpose thereof is to enable those skilled in the art to understand the content of the present invention and implement the present invention, and not to limit the protection scope of the present invention. All equivalent changes and modifications made according to the spirit of the present invention should be covered within the protection scope of the present invention.
Claims (2)
1. The compound sulfamethoxazole oral suspension comprises the following raw materials per 100 ml: 3.0g of sulfamethoxazole, 1.5g of trimethoprim, 1.2g of citric acid, 2.0g of sodium citrate, 0.2g of sodium carboxymethylcellulose, 0.5g of sodium benzoate, 0.2g of sodium bisulfite, 0.01g of EDTA-2Na, 1g of sodium chloride and the balance of purified water;
the preparation method of the compound sulfamethoxazole oral suspension comprises the following steps:
(1) heating purified water to 45-60 ℃, adding citric acid and salts thereof, stirring and dissolving to obtain solution A for later use,
(2) adding sodium carboxymethylcellulose and trimethoprim into the solution A, fully stirring and fully dissolving to obtain a solution B for later use, and keeping the temperature of the solution at 45-60 ℃;
(3) adding sulfamethoxazole, sodium benzoate, sodium bisulfite, EDTA-2Na and sodium chloride into the solution B in sequence, fully stirring and fully dissolving the components to obtain solution C, and keeping the temperature of the solution at 45-60 ℃;
(4) and cooling the C liquid to room temperature, adjusting the pH value to 4.0-6.0 by using a 20% citric acid solution, and supplementing water to a proper amount to obtain the compound sulfamethoxazole oral suspension.
2. The compound sulfamethoxazole oral suspension according to claim 1, wherein the room temperature in step (4) is 20-25 ℃.
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| CN111617030B (en) * | 2020-05-22 | 2021-09-07 | 广东药科大学 | Chitosan oligosaccharide oral liquid and application thereof in preparation of weight-reducing medicine |
| CN113041219A (en) * | 2021-03-31 | 2021-06-29 | 南京日升昌生物技术有限公司 | Compound sulfadiazine suspension and preparation method and application thereof |
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| CA2598668A1 (en) * | 2005-02-25 | 2006-09-08 | Mutual Pharmaceutical Company, Inc. | Dosage forms of antibiotics and combinations of antibiotics and symptomatic relief agents |
| CN100500127C (en) * | 2006-08-04 | 2009-06-17 | 苏州科牧动物药品有限公司 | Compound sulfonamide suspension and its preparing process |
| CN103405463A (en) * | 2012-08-06 | 2013-11-27 | 四川联美生物药业有限公司 | Preparation method of synergistic tylosin tartrate soluble powder compound medicine |
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Denomination of invention: Compound sulfamethoxazole oral suspension and its preparation method Effective date of registration: 20211228 Granted publication date: 20200124 Pledgee: Haimen sub branch of Bank of Nanjing Co.,Ltd. Pledgor: JIANGSU HFQ BIO-TECHNOLOGY Co.,Ltd. Registration number: Y2021320010618 |
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Date of cancellation: 20230329 Granted publication date: 20200124 Pledgee: Haimen sub branch of Bank of Nanjing Co.,Ltd. Pledgor: JIANGSU HFQ BIO-TECHNOLOGY Co.,Ltd. Registration number: Y2021320010618 |