CN114053229B - Sarafloxacin hydrochloride water-soluble granules and preparation method thereof - Google Patents
Sarafloxacin hydrochloride water-soluble granules and preparation method thereof Download PDFInfo
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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
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1629—Organic macromolecular compounds
- A61K9/1652—Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
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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
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
Abstract
The invention provides a sarafloxacin hydrochloride water-soluble granule and a preparation method thereof, which solve the technical problems of poor treatment effect and serious drug residue problem of the existing sarafloxacin hydrochloride drug and are composed of the following raw materials in parts by weight: 15-45 parts of diethylene diamine, 150-220 parts of cyclodextrin-methyl vinyl ether/maleic anhydride copolymer, 100 parts of sarafloxacin hydrochloride, 635-735 parts of anhydrous glucose and a proper amount of water; the invention also discloses a preparation method of the sarafloxacin hydrochloride water-soluble granules, which comprises the following steps: respectively weighing diethylene diamine and cyclodextrin-methyl vinyl ether/maleic anhydride copolymer, adding into hot water, and uniformly mixing to obtain a first mixture; respectively weighing sarafloxacin hydrochloride and anhydrous glucose, and uniformly mixing to obtain a mixture II; putting the mixture II into a three-dimensional fluidized bed, and performing fluidized bed granulation by taking the mixture I as an adhesive; controlling the air inlet temperature and the like during the process, and finally obtaining sarafloxacin hydrochloride particles; can be widely applied to the technical field of veterinary drugs.
Description
Technical Field
The application relates to the technical field of veterinary drugs, and in particular relates to sarafloxacin hydrochloride water-soluble granules and a preparation method thereof.
Background
Sarafloxacin hydrochloride (Sarafloxacin hydrochloride) is a third-generation fluoroquinolone antibacterial drug special for animals, has wide antibacterial spectrum and strong antibacterial activity, and shows good antibacterial action on gram-negative bacteria, gram-positive bacteria and mildews, in particular to enterobacteriums such as escherichia coli, salmonella, klebsiella, proteus, pasteurella multocida and campylobacter. The sarafloxacin hydrochloride has the advantages of quick absorption, quick metabolism, almost no residue, and no cross drug resistance with many antibacterial drugs, and is mainly used for treating digestive system, respiratory system, urinary tract infection and mycoplasmosis of livestock and poultry caused by sensitive bacteria.
The sarafloxacin hydrochloride is a concentration-dependent drug, and can play a drug effect after a certain concentration is required to be reached in an animal body. The sarafloxacin hydrochloride has strong permeability and quick absorption and metabolism in animals, the existing product is made into a sustained release preparation, but the sarafloxacin hydrochloride is not considered to belong to a concentration-dependent drug, the conventional liposome and coating material can reduce the blood concentration of the drug, the good treatment effect cannot be achieved, the drug withdrawal period of the drug can be prolonged, the drug residue problem is serious, and the drug residue condition still exists after 24 hours.
Disclosure of Invention
The invention aims to solve the technical defects and provides sarafloxacin hydrochloride water-soluble granules and a preparation method thereof, which have good treatment effect, no medicine residue problem and no influence on the medicine withdrawal period.
Therefore, the invention provides sarafloxacin hydrochloride water-soluble granules which are prepared from the following raw materials in parts by weight: 15-45 parts of diethylene diamine, 150-220 parts of cyclodextrin-methyl vinyl ether/maleic anhydride copolymer, 100 parts of sarafloxacin hydrochloride, 635-735 parts of anhydrous glucose and a proper amount of water.
Preferably, the feed is prepared from the following raw materials in parts by weight: 15 parts of diethylene diamine, 150 parts of cyclodextrin-methyl vinyl ether/maleic anhydride copolymer, 100 parts of sarafloxacin hydrochloride, 735 parts of anhydrous glucose and a proper amount of water.
Preferably, the feed is prepared from the following raw materials in parts by weight: 30 parts of diethylene diamine, 200 parts of cyclodextrin-methyl vinyl ether/maleic anhydride copolymer, 100 parts of sarafloxacin hydrochloride, 670 parts of anhydrous glucose and a proper amount of water.
Preferably, the feed is prepared from the following raw materials in parts by weight: 45 parts of diethylene diamine, 220 parts of cyclodextrin-methyl vinyl ether/maleic anhydride copolymer, 100 parts of sarafloxacin hydrochloride, 635 parts of anhydrous glucose and a proper amount of water.
Preferably, the anhydrous glucose is sieved through a 80-mesh sieve.
The preparation method of the sarafloxacin hydrochloride water-soluble granules comprises the following steps:
(1) respectively weighing diethylene diamine and cyclodextrin-methyl vinyl ether/maleic anhydride copolymer according to parts by weight, adding the diethylene diamine and the cyclodextrin-methyl vinyl ether/maleic anhydride copolymer into hot water at the temperature of 55-60 ℃, and uniformly stirring and mixing to obtain a first mixture;
(2) respectively weighing sarafloxacin hydrochloride and anhydrous glucose according to the weight parts, and uniformly stirring and mixing to obtain a mixture II;
(3) putting the mixture II obtained in the step (2) into a three-dimensional fluidized bed, and performing fluidized bed granulation by taking the mixture I obtained in the step (1) as an adhesive; during the period, the air inlet temperature, the air inlet quantity and the atomization pressure are controlled, and finally the sarafloxacin hydrochloride particles are obtained.
Preferably, the stirring speed in the step (1) is 150 r/min, and the stirring time is 30 min.
Preferably, the air inlet temperature in the step (3) is 65 ℃, the air inlet volume is 50 cubic meters, and the atomization pressure is 150 kPa.
The invention has the beneficial effects that: the invention provides a sarafloxacin hydrochloride water-soluble granule and a preparation method thereof, wherein a vertical fluidized bed granulation process is adopted, a cyclodextrin-methyl vinyl ether/maleic anhydride copolymer is used as a carrier of a medicament, and the carrier has strong medicament-carrying capacity, so that the sarafloxacin hydrochloride is continuously and stably released in intestinal tracts, higher blood concentration is maintained within a certain time, and the sarafloxacin hydrochloride can be basically eliminated after 12 hours. Compared with the existing products, the traditional Chinese medicine composition has good treatment effect and does not influence the drug withdrawal period.
Drawings
In order to more clearly illustrate the technical solutions in the embodiments of the present application, the drawings needed in the description of the embodiments or the prior art will be briefly described below, and it is obvious that the drawings in the following description are only embodiments of the present application.
FIG. 1 is a drug-time curve of a chicken orally administered formulation of example 1, comparative example 2 sarafloxacin hydrochloride;
FIG. 2 is a drug-time curve of a chicken orally administered example 2, comparative example 1, comparative example 2 sarafloxacin hydrochloride formulation;
fig. 3 is a drug-time curve of the oral administration of the sarafloxacin hydrochloride formulations of example 3, comparative example 1 and comparative example 2 in a chicken.
Detailed Description
In order to make the technical problems, technical solutions and advantageous effects to be solved by the present application clearer, the present application is further described in detail below with reference to the accompanying drawings and embodiments. It should be understood that the specific embodiments described herein are merely illustrative of the present application and are not intended to limit the present application. The method used in the invention is a conventional method if no special provisions are made; the raw materials and the apparatus used are, unless otherwise specified, conventional commercially available products.
Example 1:
the embodiment provides a method for preparing water-soluble sarafloxacin hydrochloride granules, which comprises the following steps:
(1) respectively weighing 15 g of diethylene diamine and 150 g of cyclodextrin-methyl vinyl ether/maleic anhydride copolymer, adding into hot water at 55 ℃, and uniformly stirring and mixing to obtain a first mixture;
(2) respectively weighing 100 g of sarafloxacin hydrochloride and 735 g of anhydrous glucose, and uniformly stirring and mixing to obtain a mixture II;
(3) putting the mixture II obtained in the step (2) into a three-dimensional fluidized bed, and performing fluidized bed granulation by using the mixture I obtained in the step (1) as a binder; during the period, the air inlet temperature, the air inlet quantity and the atomization pressure are controlled, and finally the sarafloxacin hydrochloride particles are obtained.
Example 2:
the embodiment provides a method for preparing water-soluble sarafloxacin hydrochloride granules, which comprises the following steps:
(1) respectively weighing 30g of diethylene diamine and 200 g of cyclodextrin-methyl vinyl ether/maleic anhydride copolymer, adding into hot water at 58 ℃, and uniformly stirring and mixing to obtain a first mixture;
(2) respectively weighing 100 g of sarafloxacin hydrochloride and 670 g of anhydrous glucose, and uniformly stirring and mixing to obtain a mixture II;
(3) putting the mixture II obtained in the step (2) into a three-dimensional fluidized bed, and performing fluidized bed granulation by using the mixture I obtained in the step (1) as a binder; during the period, the air inlet temperature, the air inlet quantity and the atomization pressure are controlled, and finally the sarafloxacin hydrochloride particles are obtained.
Example 3:
the embodiment provides a method for preparing water-soluble sarafloxacin hydrochloride granules, which comprises the following steps:
(1) respectively weighing 45g of diethylene diamine and 220 g of cyclodextrin-methyl vinyl ether/maleic anhydride copolymer, adding the mixture into hot water at the temperature of 60 ℃, and uniformly stirring and mixing to obtain a first mixture;
(2) respectively weighing 100 g of sarafloxacin hydrochloride and 635 g of anhydrous glucose, and uniformly stirring and mixing to obtain a mixture II;
(3) putting the mixture II obtained in the step (2) into a three-dimensional fluidized bed, and performing fluidized bed granulation by using the mixture I obtained in the step (1) as a binder; during the period, the air inlet temperature, the air inlet quantity and the atomization pressure are controlled, and finally the sarafloxacin hydrochloride particles are obtained.
In the above examples 1 to 3, for the convenience of comparative analysis, the stirring speed in the step (1) was 150 r/min and the stirring time was 30 min; anhydrous glucose which is sieved by a sieve of 80 meshes is used in the step (2); the air inlet temperature of the three-dimensional fluidized bed in the step (3) is 65 ℃, the air inlet volume is 50 cubic, the atomization pressure is 150 kPa, the main process is that a heater is used for heating the air inlet, the uniformly mixed mixture II containing the sarafloxacin hydrochloride is added into the three-dimensional fluidized bed, and the heated air enables the mixture II of the three-dimensional fluidized bed to be in a fluidized state; and (3) feeding the first mixture serving as the adhesive aqueous solution into a spray gun pipe by using a peristaltic pump, spraying the first adhesive mixture into a mist by using compressed air, scattering the mist on the surfaces of the second mixture materials, enabling the second mixture materials to collide with each other and agglomerate into granules, and drying after granulation is finished to finally obtain the sarafloxacin hydrochloride granules.
Next, the pharmacokinetic comparison test, the water solubility comparison test, and the stability comparison test were performed on each of the sarafloxacin hydrochloride particles obtained in examples 1 to 3 and the commercial products of comparative example 1 and comparative example 2. Wherein comparative example 1 is a commercially available 10% sarafloxacin hydrochloride soluble powder, made by a manufacturer in Henan, lot number 20210502; comparative example 2 is a commercial 10% sarafloxacin hydrochloride soluble powder, made by a manufacturer of Jiangsu, lot number 20210710.
Pharmacokinetic comparison test
Pharmacokinetic tests were carried out on the sarafloxacin hydrochloride soluble particles prepared in examples 1 to 3 and the commercial products of comparative example 1 and comparative example 2.
Experimental materials: 20 sanhuang chickens with good mental status (half of each male and female, the weight is 2kg +/-0.2), a dosing device, a high performance liquid chromatograph and the like.
The experimental steps are as follows: the Sanhuang chicken is divided into five groups, each group comprises a male and a female, the medicine is administrated by drenching at 10mg/kg body weight, after administration, venous blood collection is carried out respectively at 0min, 15min, 30min, 1h, 2h, 4h, 8h, 12h and 24h, serum is separated, and the medicine is preserved for standby use at minus 20 ℃. And (3) after the serum is treated, taking the supernatant to detect the content of the sarafloxacin hydrochloride by HPLC. The results are shown in Table 1 and FIGS. 1 to 3.
TABLE 1 pharmacokinetic comparison test results
| When taking blood Workshop (h) | Example 1 mean blood drug Concentration (ug/L) | Example 2 mean blood drug Concentration (ug/L) | Example 3 mean blood drug Concentration (ug/L) | Comparative example 1 mean blood drug Concentration (ug/L) | Comparative example 2 mean blood drug Concentration (ug/L) |
| 0 | 0 | 0 | 0 | 0 | 0 |
| 0.25 | 112 | 90 | 121 | 197 | 55 |
| 0.5 | 183 | 210 | 205 | 461 | 78 |
| 1 | 322 | 342 | 313 | 364 | 140 |
| 2 | 482 | 520 | 499 | 256 | 210 |
| 4 | 724 | 691 | 682 | 208 | 301 |
| 8 | 246 | 230 | 302 | 210 | 385 |
| 12 | 56 | 50 | 39 | 172 | 404 |
| 24 | Not detected out | Not detected out | Not detected out | 65 | 255 |
As can be seen from table 1 and fig. 1 to 3: compared with the medicines sold in the comparative examples 1 and 2, the sarafloxacin hydrochloride water-soluble granules prepared in the embodiments 1 to 3 can be continuously and stably released and absorbed, and can maintain higher blood concentration in a certain time, so that the sarafloxacin hydrochloride water-soluble granules can have good treatment effect as concentration-dependent medicines; meanwhile, the granules provided by the invention are relatively fast in metabolism, have no drug residue problem, and do not influence the drug withdrawal period.
On one hand, the cyclodextrin-methyl vinyl ether/maleic anhydride copolymer is used as a carrier of the drug, and the carrier has strong drug-loading capacity, so that the sarafloxacin hydrochloride is continuously and stably released in intestinal tracts, higher blood concentration is maintained within a certain time, and the drug can be basically eliminated after 12 hours. Compared with the existing products, the traditional Chinese medicine composition has good treatment effect and does not influence the drug withdrawal period; on the other hand, the diethylene diamine is a medical intermediate of the medicine, can be used as an antibacterial synergist of the sarafloxacin hydrochloride, improves the antibacterial effect and better exerts the medicine effect.
Water solubility comparison test
The water-soluble granule of sarafloxacin hydrochloride prepared in example 1 to example 3 and the commercially available drugs of comparative example 1 to comparative example 4 were dissolved in tap water at 25 ℃ at different concentrations, and the dissolution states were compared.
Comparative example 3:
the embodiment provides a method for preparing sarafloxacin hydrochloride granules, which comprises the following steps:
(1) weighing 30g of diethylene diamine, adding the diethylene diamine into hot water at the temperature of 58 ℃, and uniformly stirring and mixing to obtain a first mixture;
(2) respectively weighing 100 g of sarafloxacin hydrochloride and 870 g of anhydrous glucose, and uniformly stirring and mixing to obtain a mixture II;
(3) putting the mixture II obtained in the step (2) into a three-dimensional fluidized bed, and performing fluidized bed granulation by using the mixture I obtained in the step (1) as a binder; during the period, the air inlet temperature, the air inlet quantity and the atomization pressure are controlled, and finally the sarafloxacin hydrochloride particles are obtained.
Comparative example 4:
the embodiment provides a method for preparing sarafloxacin hydrochloride granules, which comprises the following steps:
(1) weighing 200 g of cyclodextrin-methyl vinyl ether/maleic anhydride copolymer, adding into hot water at 58 ℃, and uniformly stirring and mixing to obtain a first mixture;
(2) respectively weighing 100 g of sarafloxacin hydrochloride and 700 g of anhydrous glucose, and uniformly stirring and mixing to obtain a mixture II;
(3) putting the mixture II obtained in the step (2) into a three-dimensional fluidized bed, and performing fluidized bed granulation by using the mixture I obtained in the step (1) as a binder; during the period, the air inlet temperature, the air inlet quantity and the atomization pressure are controlled, and finally the sarafloxacin hydrochloride particles are obtained.
The test materials were: beaker, glass, tap water.
The experimental steps are as follows: 100ml of tap water is placed in each beaker, 0.5g, 1.0g, 3.0g and 5.0g of samples are respectively weighed and added into the beaker, then the mixture is stirred for 2min by a glass rod, the dissolution condition of the samples in each beaker is observed, the turbidity is detected, and the record is made. The monitoring results are shown in table 2.
TABLE 2 Water solubility comparison test results
| Sample/addition Input amount | 0.5g | 1.0g | 3.0g | 5.0g |
| Example 1 | Complete dissolution and turbidity 5.4NTU | Complete dissolution and turbidity 10.3NTU | Complete dissolution, turbidity 15.6NTU | Complete dissolution, turbidity 21.5NTU |
| Example 2 | Complete dissolution and turbidity 5.2NTU | Complete dissolution, turbidity 8.2NTU | Complete dissolution, turbidity 11.3NTU | Complete dissolution, turbidity 19.6NTU |
| Example 3 | Complete dissolution and turbidity 3.2NTU | Complete dissolution, turbidity 5.1NTU | Complete dissolution, turbidity 6.2NTU | Complete dissolution, turbidity 9.8NTU |
| Comparative example 1 | Complete dissolution and turbidity 20.5NTU | A small amount of insoluble particles at the bottom, turbidity Degree 35.9NTU | More insoluble particles at the bottom, turbidity 60.3NTU | Bottom large amount of insoluble particles, turbidity 220.7NTU |
| Comparative example 2 | Turbidity of the solution 120.5NTU | Turbidity of the solution 300.2NTU | Severe turbidity of the solution | Severe turbidity of the solution |
| Comparative example 3 | Complete dissolution and turbidity 7.8NTU | Complete dissolution and turbidity 10.1NTU | Complete dissolution, turbidity 13.3NTU | Complete dissolution, turbidity 21.3NTU |
| Comparative example 4 | Turbidity of the solution 125.3NTU | Turbidity of the solution 378.5NTU | Severe turbidity of the solution | Severe turbidity of the solution |
The sarafloxacin hydrochloride is almost slightly soluble in water, most of products in the market at present mostly adopt some conventional cosolvents in the production process in order to improve the solubility of the sarafloxacin hydrochloride, but the solubility of the sarafloxacin hydrochloride is not obviously improved, the actual production requirements cannot be met, the problems of pipeline blockage, uneven administration and the like in the administration process of animal drinking water exist, the treatment and prevention effects cannot be achieved, and the waste of medicines is caused.
The results in table 1 show that the solubility of the sarafloxacin hydrochloride water-soluble granules prepared in the embodiments 1-3 in the invention is about 10 times higher than that of the commercially available medicines in the comparative examples 1 and 2, and the clinical medication requirements are completely met. Comparative analysis of example 2, comparative example 3 and comparative example 4 shows that diethylene diamine is used as a cosolvent to remarkably increase the solubility of sarafloxacin hydrochloride.
Stability comparison test
Accelerated test verification in drug stability was performed on the water-soluble granule of sarafloxacin hydrochloride prepared in example 1 to example 3 and the commercially available drugs of comparative example 1 and comparative example 2, respectively.
The experimental steps are as follows: the sample is placed in an acceleration test box (40 ℃, 75% humidity) for six months, and samples are respectively taken at 1 st, 3 rd and 6 th months after the sample is placed to detect the appearance, the content, the drying weight loss and the like of the sarafloxacin hydrochloride preparation. The examination results at month 6 of the accelerated test are shown in Table 3.
TABLE 3 stability comparison test results
| Item | Example 1 | Example 2 | Example 3 | Comparative example 1 | Comparative example 2 |
| Traits | Light yellow granule, none Trait change | Yellowish granules, genuineness Change of shape | Yellowish granules, genuineness Change of shape | Reddish brown block, severe Denaturation of the material | Light yellowColored powder, genu Change of shape |
| Loss on drying | 2.53% | 3.68% | 3.99% | 8.13% | 5.15% |
| Content (wt.) | 99.2% | 97.5% | 98.7% | 92.5% | 87.3% |
| Whether it is qualified or not | Qualified | Qualified | Qualified | Fail to be qualified | Fail to be qualified |
As can be seen from table 3: indexes of the sarafloxacin hydrochloride granules prepared in the embodiments 1 to 3 of the invention are superior to those of the commercially available medicaments in the comparative examples 1 and 2. The stability of the commercially available drug is poor, the drug is easy to block and discolor in comparative example 1, and the content of the drug in comparative example 2 is obviously reduced. The invention has stable character and content, the content ratio is higher than 5 percent when the test box is placed in an acceleration test box for 6 months, and the test box is not easy to absorb moisture and is easier to store and use.
The above description is only exemplary of the present application and should not be taken as limiting the present application, as any modification, equivalent replacement, or improvement made within the spirit and principle of the present application should be included in the protection scope of the present application.
Claims (8)
1. The sarafloxacin hydrochloride water-soluble granules are characterized by comprising the following raw materials in parts by weight: 15-45 parts of diethylene diamine, 150-220 parts of cyclodextrin-methyl vinyl ether/maleic anhydride copolymer, 100 parts of sarafloxacin hydrochloride, 635-735 parts of anhydrous glucose and a proper amount of water;
the preparation method of the sarafloxacin hydrochloride water-soluble granules comprises the following steps:
(1) respectively weighing diethylene diamine and cyclodextrin-methyl vinyl ether/maleic anhydride copolymer according to parts by weight, adding the diethylene diamine and the cyclodextrin-methyl vinyl ether/maleic anhydride copolymer into hot water at the temperature of 55-60 ℃, and uniformly stirring and mixing to obtain a first mixture;
(2) respectively weighing sarafloxacin hydrochloride and anhydrous glucose according to the weight parts, and uniformly stirring and mixing to obtain a mixture II;
(3) and (3) putting the mixture II obtained in the step (2) into a three-dimensional fluidized bed, performing fluidized bed granulation by taking the mixture I obtained in the step (1) as an adhesive, and controlling the air inlet temperature, the air inlet volume and the atomization pressure during the granulation to finally obtain the sarafloxacin hydrochloride particles.
2. The sarafloxacin hydrochloride water-soluble granule as claimed in claim 1, which is prepared from the following raw materials in parts by weight: 15 parts of diethylene diamine, 150 parts of cyclodextrin-methyl vinyl ether/maleic anhydride copolymer, 100 parts of sarafloxacin hydrochloride, 735 parts of anhydrous glucose and a proper amount of water.
3. The sarafloxacin hydrochloride water-soluble granule as claimed in claim 1, which is prepared from the following raw materials in parts by weight: 30 parts of diethylene diamine, 200 parts of cyclodextrin-methyl vinyl ether/maleic anhydride copolymer, 100 parts of sarafloxacin hydrochloride, 670 parts of anhydrous glucose and a proper amount of water.
4. The sarafloxacin hydrochloride water-soluble granule as claimed in claim 1, which is prepared from the following raw materials in parts by weight: 45 parts of diethylene diamine, 220 parts of cyclodextrin-methyl vinyl ether/maleic anhydride copolymer, 100 parts of sarafloxacin hydrochloride, 635 parts of anhydrous glucose and a proper amount of water.
5. The sarafloxacin hydrochloride water-soluble granules of claim 1, wherein the anhydrous glucose is treated by sieving with a 80-mesh sieve.
6. A process for producing the water-soluble granule of sarafloxacin hydrochloride according to any one of claims 1 to 5, comprising the steps of:
(1) respectively weighing diethylene diamine and cyclodextrin-methyl vinyl ether/maleic anhydride copolymer according to parts by weight, adding the diethylene diamine and the cyclodextrin-methyl vinyl ether/maleic anhydride copolymer into hot water at the temperature of 55-60 ℃, and uniformly stirring and mixing to obtain a first mixture;
(2) respectively weighing sarafloxacin hydrochloride and anhydrous glucose according to the weight parts, and uniformly stirring and mixing to obtain a mixture II;
(3) and (3) putting the mixture II obtained in the step (2) into a three-dimensional fluidized bed, performing fluidized bed granulation by taking the mixture I obtained in the step (1) as an adhesive, and controlling the air inlet temperature, the air inlet volume and the atomization pressure during the granulation to finally obtain the sarafloxacin hydrochloride particles.
7. The method according to claim 6, wherein the stirring speed in the step (1) is 150 r/min and the stirring time is 30 min.
8. The method as claimed in claim 6, wherein the temperature of the inlet air in the step (3) is 65 ℃, the volume of the inlet air is 50 cubic degrees, and the atomization pressure is 150 kPa.
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