CN114010602A - Veterinary glucurolactone soluble powder and preparation method thereof - Google Patents
Veterinary glucurolactone soluble powder and preparation method thereof Download PDFInfo
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- UYUXSRADSPPKRZ-SKNVOMKLSA-N D-glucurono-6,3-lactone Chemical compound O=C[C@H](O)[C@H]1OC(=O)[C@@H](O)[C@H]1O UYUXSRADSPPKRZ-SKNVOMKLSA-N 0.000 title claims abstract description 80
- 229950002441 glucurolactone Drugs 0.000 title claims abstract description 80
- 239000000843 powder Substances 0.000 title claims abstract description 70
- 238000002360 preparation method Methods 0.000 title abstract description 17
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 claims abstract description 101
- 229960004977 anhydrous lactose Drugs 0.000 claims abstract description 23
- GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 claims abstract 5
- 239000000203 mixture Substances 0.000 claims description 27
- 229960004106 citric acid Drugs 0.000 claims description 25
- 239000002245 particle Substances 0.000 claims description 18
- 244000144972 livestock Species 0.000 claims description 16
- 238000000034 method Methods 0.000 claims description 14
- 238000003756 stirring Methods 0.000 claims description 14
- PXRKCOCTEMYUEG-UHFFFAOYSA-N 5-aminoisoindole-1,3-dione Chemical compound NC1=CC=C2C(=O)NC(=O)C2=C1 PXRKCOCTEMYUEG-UHFFFAOYSA-N 0.000 claims description 10
- 229960004543 anhydrous citric acid Drugs 0.000 claims description 10
- 238000007873 sieving Methods 0.000 claims description 6
- 239000003814 drug Substances 0.000 abstract description 18
- 229940079593 drug Drugs 0.000 abstract description 15
- 241001465754 Metazoa Species 0.000 abstract description 12
- 230000000694 effects Effects 0.000 abstract description 9
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 abstract description 9
- GUBGYTABKSRVRQ-DCSYEGIMSA-N Beta-Lactose Chemical compound OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)[C@H](O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-DCSYEGIMSA-N 0.000 description 19
- 230000000052 comparative effect Effects 0.000 description 15
- 239000000243 solution Substances 0.000 description 15
- 238000012360 testing method Methods 0.000 description 10
- 210000004185 liver Anatomy 0.000 description 7
- 244000144977 poultry Species 0.000 description 6
- 235000013594 poultry meat Nutrition 0.000 description 6
- 208000006454 hepatitis Diseases 0.000 description 5
- 238000010521 absorption reaction Methods 0.000 description 4
- 210000001035 gastrointestinal tract Anatomy 0.000 description 4
- 241000282414 Homo sapiens Species 0.000 description 3
- 230000009286 beneficial effect Effects 0.000 description 3
- 238000009395 breeding Methods 0.000 description 3
- 230000001488 breeding effect Effects 0.000 description 3
- 238000005457 optimization Methods 0.000 description 3
- 239000002244 precipitate Substances 0.000 description 3
- 230000008569 process Effects 0.000 description 3
- 238000013441 quality evaluation Methods 0.000 description 3
- 206010008909 Chronic Hepatitis Diseases 0.000 description 2
- 241000287828 Gallus gallus Species 0.000 description 2
- 208000005374 Poisoning Diseases 0.000 description 2
- 230000001154 acute effect Effects 0.000 description 2
- 238000005054 agglomeration Methods 0.000 description 2
- 230000002776 aggregation Effects 0.000 description 2
- 235000013330 chicken meat Nutrition 0.000 description 2
- 244000144992 flock Species 0.000 description 2
- 231100000572 poisoning Toxicity 0.000 description 2
- 230000000607 poisoning effect Effects 0.000 description 2
- 239000000047 product Substances 0.000 description 2
- 239000000126 substance Substances 0.000 description 2
- 239000004382 Amylase Substances 0.000 description 1
- 102000013142 Amylases Human genes 0.000 description 1
- 108010065511 Amylases Proteins 0.000 description 1
- UYUXSRADSPPKRZ-UHFFFAOYSA-N D-glucuronic acid gamma-lactone Natural products O=CC(O)C1OC(=O)C(O)C1O UYUXSRADSPPKRZ-UHFFFAOYSA-N 0.000 description 1
- 102000004190 Enzymes Human genes 0.000 description 1
- 108090000790 Enzymes Proteins 0.000 description 1
- 206010016952 Food poisoning Diseases 0.000 description 1
- 208000019331 Foodborne disease Diseases 0.000 description 1
- 229920002527 Glycogen Polymers 0.000 description 1
- 241000282412 Homo Species 0.000 description 1
- 206010067125 Liver injury Diseases 0.000 description 1
- 231100000678 Mycotoxin Toxicity 0.000 description 1
- NIPNSKYNPDTRPC-UHFFFAOYSA-N N-[2-oxo-2-(2,4,6,7-tetrahydrotriazolo[4,5-c]pyridin-5-yl)ethyl]-2-[[3-(trifluoromethoxy)phenyl]methylamino]pyrimidine-5-carboxamide Chemical compound O=C(CNC(=O)C=1C=NC(=NC=1)NCC1=CC(=CC=C1)OC(F)(F)F)N1CC2=C(CC1)NN=N2 NIPNSKYNPDTRPC-UHFFFAOYSA-N 0.000 description 1
- 206010061481 Renal injury Diseases 0.000 description 1
- 206010070863 Toxicity to various agents Diseases 0.000 description 1
- 241000700605 Viruses Species 0.000 description 1
- 238000009098 adjuvant therapy Methods 0.000 description 1
- 125000003277 amino group Chemical group 0.000 description 1
- 235000019418 amylase Nutrition 0.000 description 1
- 230000003115 biocidal effect Effects 0.000 description 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 description 1
- 238000006555 catalytic reaction Methods 0.000 description 1
- 230000001684 chronic effect Effects 0.000 description 1
- 208000019425 cirrhosis of liver Diseases 0.000 description 1
- 210000002808 connective tissue Anatomy 0.000 description 1
- 230000003247 decreasing effect Effects 0.000 description 1
- 230000007547 defect Effects 0.000 description 1
- 238000011161 development Methods 0.000 description 1
- 238000004090 dissolution Methods 0.000 description 1
- 238000009826 distribution Methods 0.000 description 1
- 239000003651 drinking water Substances 0.000 description 1
- 235000020188 drinking water Nutrition 0.000 description 1
- 230000000857 drug effect Effects 0.000 description 1
- 230000005611 electricity Effects 0.000 description 1
- 238000002474 experimental method Methods 0.000 description 1
- 235000013305 food Nutrition 0.000 description 1
- 239000011521 glass Substances 0.000 description 1
- 150000002303 glucose derivatives Chemical class 0.000 description 1
- 229940096919 glycogen Drugs 0.000 description 1
- 230000004116 glycogenolysis Effects 0.000 description 1
- 230000036541 health Effects 0.000 description 1
- 231100000283 hepatitis Toxicity 0.000 description 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 description 1
- 210000003000 inclusion body Anatomy 0.000 description 1
- 238000002347 injection Methods 0.000 description 1
- 239000007924 injection Substances 0.000 description 1
- 210000000936 intestine Anatomy 0.000 description 1
- 150000002596 lactones Chemical group 0.000 description 1
- 230000007774 longterm Effects 0.000 description 1
- 239000002207 metabolite Substances 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 239000002636 mycotoxin Substances 0.000 description 1
- 231100000252 nontoxic Toxicity 0.000 description 1
- 230000003000 nontoxic effect Effects 0.000 description 1
- 230000001717 pathogenic effect Effects 0.000 description 1
- 239000000825 pharmaceutical preparation Substances 0.000 description 1
- 229940127557 pharmaceutical product Drugs 0.000 description 1
- ISWSIDIOOBJBQZ-UHFFFAOYSA-N phenol group Chemical group C1(=CC=CC=C1)O ISWSIDIOOBJBQZ-UHFFFAOYSA-N 0.000 description 1
- 239000002574 poison Substances 0.000 description 1
- 231100000614 poison Toxicity 0.000 description 1
- 230000000750 progressive effect Effects 0.000 description 1
- 238000012216 screening Methods 0.000 description 1
- 239000007858 starting material Substances 0.000 description 1
- 230000003068 static effect Effects 0.000 description 1
- 238000003860 storage Methods 0.000 description 1
- 238000006467 substitution reaction Methods 0.000 description 1
- 241000701161 unidentified adenovirus Species 0.000 description 1
- 210000002700 urine Anatomy 0.000 description 1
- 238000005303 weighing Methods 0.000 description 1
Classifications
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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
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7048—Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin, digitoxin or digoxin
-
- 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
- A61K9/141—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
- A61K9/145—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with organic compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P39/00—General protective or antinoxious agents
- A61P39/02—Antidotes
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- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Organic Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- Toxicology (AREA)
- Gastroenterology & Hepatology (AREA)
- Molecular Biology (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The invention provides a soluble glucurolactone powder for veterinary use and a preparation method thereof, and relates to the field of preparation of veterinary medicines. The glucurolactone soluble powder comprises the following components in parts by weight: d, glucurolactone: anhydrous lactose: citric acid =3:6.5: 0.5; wherein, the citric acid needs to be crushed, the granularity is controlled to be 170-190 μm, and the pH value of the solution after the glucurolactone soluble powder is dissolved is stabilized to be 4.5-6.0. The glucurolactone soluble powder has the advantages of good water solubility and obvious curative effect, is convenient for the needs of group culture, and provides convenience for clinical medication of animals. The preparation process of the glucurolactone soluble powder is simple and convenient, easy to operate and good in repeatability.
Description
Technical Field
The invention relates to the technical field of veterinary medicine preparation, and particularly relates to soluble glucurolactone powder for veterinary use and a preparation method thereof.
Background
Glucuronolactone, glucurolactone for short, is a naturally occurring chemical substance, is a glucose metabolite produced in the human liver, and is an important component of connective tissue. Clinically, the medicine is used for the adjuvant treatment of acute and chronic hepatitis and liver cirrhosis, is also used for the relief of food or drug poisoning, and has the functions of protecting the liver and detoxifying. After glucurolactone enters a body, a lactone ring is opened under the catalysis of enzyme and is converted into glucurone to play a role, and the glucurone is one of important detoxifying substances in the body and can be combined with metabolites, poisons or medicaments containing phenolic groups, hydroxyl groups, carboxyl groups and amino groups in liver or intestine to form a nontoxic glucurone conjugate which is discharged out of the body along with urine. Meanwhile, glucurolactone can reduce the activity of liver amylase, prevent glycogenolysis, increase liver glycogen and reduce fat storage, thereby realizing the effect of protecting the liver.
The livestock and poultry are easy to feed mildew feed in the breeding process, and long-term consumption of the mildew feed can cause mycotoxin poisoning and form chronic accumulated hepatorenal poisoning; in addition, a large amount of antibiotic drugs can be used for health care of livestock and poultry in the breeding process, so that pathogenic liver and kidney injuries of livestock and poultry organisms can be caused; poultry adenoviruses also often compromise the breeding of flocks of chickens, and flocks of chickens infected with the virus can cause inclusion body hepatitis. The glucurolactone is mainly tablets or powder for injection at present, is mainly used for the auxiliary treatment of acute and chronic hepatitis of human beings, and is rarely reported for commercial livestock, poultry or pets. Therefore, the present invention aims to convert glucurolactone, which is commonly used in humans, into soluble powder for livestock, poultry or pets. In animal administration, drinking water is mostly adopted, so that the drug has high requirements on the solubility of the drug in water on the premise of ensuring the drug effect. Therefore, the development of a veterinary glucurolactone soluble powder with high solubility and stability is urgently needed.
Disclosure of Invention
Technical problem to be solved
Aiming at the defects of the prior art, the invention provides a soluble glucurolactone powder for animals and a preparation method thereof; the soluble glucurolactone powder provided by the invention converts human medicines into veterinary medicines according to the self characteristics of medicines and the absorption characteristics of animal organisms, expands the treatment range of glucurolactone, and has the advantages of simple process, convenience in operation, good repeatability, higher solubility and good stability.
(II) technical scheme
In order to achieve the purpose, the invention is realized by the following technical scheme:
in one aspect, the invention provides a soluble glucurolactone powder for livestock, which is prepared from glucurolactone, anhydrous lactose and citric acid.
Further, as the optimization of the glucurolactone soluble powder for livestock, the soluble powder is prepared from glucurolactone, anhydrous lactose and citric acid according to the mass ratio of 3:6.5: 0.5.
Further, as the optimization of the gulonolide soluble powder for livestock, the citric acid needs to be crushed, and the particle size is controlled to be 170-190 μm.
Further, as the optimization of the soluble glucurolactone powder for livestock, the pH value of a solution obtained after the soluble powder is dissolved is kept between 4.5 and 6.0.
On the other hand, the invention also provides a preparation method of the glucurolactone soluble powder for livestock, which comprises the following steps:
(1) firstly, 0.5 part by weight of glucurolactone is taken, 0.5 part by weight of citric acid with the granularity of 170-190 microns after being crushed is added, and the mixture is mixed and stirred for 10-15 minutes to obtain a mixture 1;
(2) adding 1 part by weight of glucurolactone into the mixture 1, and mixing and stirring for 10-15 minutes to obtain a mixture 2;
(3) adding 1.5 parts by weight of glucurolactone into the mixture 2, and mixing and stirring for 10-15 minutes to obtain a mixture 3;
(4) adding 3.5 parts by weight of anhydrous lactose into the mixture 3, and mixing and stirring for 10-15 minutes to obtain a mixture 4;
(5) adding 3 parts by weight of anhydrous lactose into the mixture 4, mixing and stirring for 10-15 minutes, and sieving by a 80-mesh sieve to obtain the veterinary glucurolactone soluble powder.
(III) advantageous effects
The invention provides a glucurolactone soluble powder suitable for veterinary clinical treatment and application and a preparation method thereof. The glucurolactone soluble powder disclosed by the invention is simple in component and high in solubility and stability, and the pH range of the animal intestinal tract is 5.0-7.0, so that the pH of a solution obtained after the soluble powder is dissolved can be stably kept at 4.5-6.0, the solution is close to the pH environment of the animal intestinal tract, the drug absorption of an animal body is facilitated, and the glucurolactone soluble powder disclosed by the invention is simple and convenient in preparation process, easy to operate and good in repeatability.
Detailed Description
In order to make the objects, technical solutions and advantages of the embodiments of the present invention clearer, the technical solutions in the embodiments of the present invention will be clearly and completely described below with reference to the embodiments of the present invention, and it is obvious that the described embodiments are some embodiments of the present invention, but not all embodiments. All other embodiments, which can be derived by a person skilled in the art from the embodiments given herein without making any creative effort, shall fall within the protection scope of the present invention.
Example 1
A veterinary glucurolactone soluble powder is prepared by the following method:
(1) firstly, 0.5 part by weight of glucurolactone is taken, 0.5 part by weight of citric acid with the granularity of 170-190 microns after being crushed for 30 seconds is added, and the mixture is mixed and stirred for 10-15 minutes to obtain a mixture 1;
(2) adding 1 part by weight of glucurolactone into the mixture 1, and mixing and stirring for 10-15 minutes to obtain a mixture 2;
(3) adding 1.5 parts by weight of glucurolactone into the mixture 2, and mixing and stirring for 10-15 minutes to obtain a mixture 3;
(4) adding 3.5 parts by weight of anhydrous lactose into the mixture 3, and mixing and stirring for 10-15 minutes to obtain a mixture 4;
(5) adding 3 parts by weight of anhydrous lactose into the mixture 4, mixing and stirring for 10-15 minutes, and sieving by a 80-mesh sieve to obtain the veterinary glucurolactone soluble powder.
Example 2
The difference between the present example and example 1 is that the mass ratio of glucurolactone, anhydrous lactose and citric acid is 3:6: 1.
Example 3
The difference between the present example and example 1 is that the mass ratio of glucurolactone, anhydrous lactose, and citric acid is 3:5.5: 1.5.
Example 4
This example differs from example 1 in that citric acid was crushed for 15 seconds and after crushing had a particle size of greater than 190 μm and failed to pass completely through a 80 mesh sieve.
Example 5
This example differs from example 1 in that citric acid was crushed for 45 seconds and the particle size after crushing was less than 170 μm.
Comparative example 2
The veterinary glucurolactone is prepared by the following steps:
mixing and stirring 3 parts by weight of glucurolactone, 6.5 parts by weight of anhydrous lactose and 0.5 part by weight of citric acid for 15 minutes to obtain the finished product.
Comparative example 3
The veterinary glucurolactone is prepared by the following steps:
crushing 0.5 part by weight of citric acid, and controlling the particle size to be 170-190 microns for later use; and then mixing and stirring 3 parts by weight of glucurolactone and 6.5 parts by weight of anhydrous lactose with the crushed citric acid for 15 minutes, and sieving by a 80-mesh sieve to obtain the product.
Test example 1
Effect of different mass ratios of glucurolactone, anhydrous lactose and citric acid on soluble powder
Table 1 shows the pH of the solution after dissolving soluble powders of glucurolactone, anhydrous lactose and citric acid in different mass ratios in water. Because the pH value of the soluble powder dissolved in water is within the range of 5.0-7.0, the pH value of the soluble powder dissolved in water is close to the pH environment of the animal intestinal tract, and the soluble powder is more beneficial to the absorption of animal organisms to medicines. The pH of the soluble powders prepared in examples 2 and 3 is outside the range of 5.0 to 7.0, and the pH of the soluble powder prepared in example 1 is 5.17, which is closer to the pH environment of animal intestinal tract, so the glucurolactone used in example 1: anhydrous lactose: citric acid =3:6.5:0.5 is the optimal ratio.
TABLE 1 Effect of different mass ratios of glucurolactone, lactose anhydrous and citric acid on soluble powders
| Sample (I) | D, glucurolactone: anhydrous lactose: citric acid | pH |
| Example 1 | 3:6.5:0.5 | 5.17 |
| Example 2 | 3:6:1 | 4.55 |
| Example 3 | 3:5.5:1.5 | 4.03 |
Test example 2
Effect of different citric acid particle sizes on soluble powders
Table 2 shows the effect of different particle sizes of citric acid on the soluble powder during the preparation process. Crushing the citric acid for 30 seconds to obtain fine powder with the particle size range of 170-190 microns, wherein the fine powder can pass through a 80-mesh sieve; crushing the citric acid for 15 seconds, wherein small particles which are not completely crushed exist in the obtained fine powder, and part of the fine powder cannot pass through a 80-mesh sieve, so that the fine powder is not beneficial to mixing; the citric acid is crushed for 45 seconds, and the obtained fine powder is excessively fine and pulverized, so that static electricity is easy to generate, and the agglomeration phenomenon is generated, and the mixing is not facilitated. Therefore, the optimum condition is to pulverize citric acid for 30s to obtain a particle size of 170 μm to 190 μm.
TABLE 2 Effect of different citric acid particle sizes on soluble powders
| Sample (I) | Citric acid crushing time | Citric acid particle size | Phenomenon of preparation process |
| Example 1 | 30s | 170μm~190μm | Mixing, and sieving with 80 mesh sieve |
| Example 4 | 15s | Greater than 190 μm | Mixing, sieving with 80 mesh sieve |
| Example 5 | 45s | Less than 170 μm | Uneven mixing, electrostatic and agglomeration phenomena |
Test example 3
The quality of the drugs prepared in example 1 and comparative examples 1-2 was evaluated.
Quality evaluation indexes and methods:
1. the characteristics are as follows: should be a white powder;
2. appearance uniformity: checking according to a method specified in 0108 powder of appendix of the first part of Chinese animal pharmacopoeia (2015 year edition);
3. granularity: checking according to the second method (screening method) in the particle size and particle size distribution determination method of appendix 0982 of the Chinese veterinary pharmacopoeia (2015 edition);
4. angle of repose: adopt fixed funnel method, fix the glass funnel in the white paper top 1cm eminence of level placement, pour veterinary glucurolactone soluble powder into the funnel along the funnel wall, make it leave naturally, the powder cone point that forms on flowing to the white paper contacts the flare opening till, measures diameter (2R) of cone bottom with the ruler, calculates the angle of repose: a = arctg (H/R) was repeated 3 times and the average value was calculated;
5. pH value: taking a proper amount of sample, adding water to obtain 50ml solution (with concentration being high dose concentration in clinical application), shaking at room temperature to dissolve completely, standing for 30min to prevent turbidity or precipitate, and measuring pH value of the solution.
The quality of the pharmaceutical products obtained in example 1 and comparative examples 1 to 2 was evaluated according to the above quality evaluation method, and the results are shown in Table 1.
TABLE 1 quality evaluation results of glucurolactone for animals prepared by different preparation methods
| Sample (I) | Comparative example 1 | Comparative example 2 | Example 1 |
| Traits | White powder | White powder | White powder |
| Uniformity of appearance | Has a little pattern | Has a little pattern | Uniform color, no pattern and color spot |
| Particle size | Part of the powder passes through a 80-mesh sieve | All pass through a 80-mesh sieve | All pass through a 80-mesh sieve |
| Angle of repose | 46° | 35° | 33° |
| pH | 7.83 | 6.43 | 5.16 |
As can be seen from Table 1: comparative example 1 glucurolactone, anhydrous lactose and citric acid were directly mixed, and although the operation was simple, the mixing was not uniform, the uniformity of the powder appearance did not meet the specification, the particle size was too large, and too large angle of repose indicated that the powder flowability was not good, and the pH of the solution prepared from the soluble powder was alkaline. Comparative example 2 citric acid was crushed and controlled to a particle size of 170-190 μm and mixed with glucurolactone and anhydrous lactose, the particle size of the powder was able to pass through a 80 mesh sieve, the angle of repose also decreased, indicating that the powder flowability became good, but the uniformity of appearance was still unsatisfactory, or due to uneven mixing. In the embodiment 1, citric acid is crushed, the granularity is controlled to be 170-190 mu m, and the citric acid is mixed with glucurolactone and anhydrous lactose in an equivalent progressive mode, so that the problem of uneven mixing of glucurolactone, anhydrous lactose and citric acid is solved, and all indexes of the obtained powder meet the regulations. Therefore, the preparation method of the glucurolactone soluble powder for livestock is preferably the method described in the embodiment 1.
Test example 2
Solubility test of the drugs prepared in example 1 and comparative examples 1-2. In order to verify the advantages of the glucurolactone soluble powder prepared by the invention, particularly the solubility in water at normal temperature, the following samples are selected for a comparative test, and the comparative test comprises the following steps: the soluble powder of glucurolactone prepared in the preparation example 1, the glucurolactone for livestock prepared in the comparative examples 1-2 and the glucurolactone bulk drug.
Experimental methods and conditions: weighing a proper amount of test sample, respectively placing the test sample in 100ml of water solution at normal temperature, shaking for 30S every 5min, observing the dissolution condition after 30min, continuously adding the test sample if no precipitate exists until the precipitate exists, taking the final completely dissolved amount as the maximum solubility, calculating the apparent solubility of each sample according to the maximum solubility, and determining the solubility of the solution. The results are shown in Table 2.
TABLE 2 solubility in water and pH of glucurolactone for veterinary use prepared by different preparation methods
| Name (R) | Solubility (g/ml) | pH |
| Glucurolactone starting material | 0.020 | 6.22 |
| COMPARATIVE EXAMPLE 1 sample (calculated as glucurolactone) | 0.025 | 7.86 |
| COMPARATIVE EXAMPLE 2 samples (based on glucurolactone) | 0.032 | 6.12 |
| EXAMPLE 1 samples (calculated as glucurolactone) | 0.035 | 5.17 |
As can be seen from table 3, the solubility of the glucurolactone soluble powder obtained in example 1 is greatly improved compared to comparative examples 1 and 2 and glucurolactone bulk drug, and the acidity of the solution is maintained, which is beneficial to the absorption of the drug in the body.
The above examples are only intended to illustrate the technical solution of the present invention, but not to limit it; although the present invention has been described in detail with reference to the foregoing embodiments, it will be understood by those of ordinary skill in the art that: the technical solutions described in the foregoing embodiments may still be modified, or some technical features may be equivalently replaced; and such modifications or substitutions do not depart from the spirit and scope of the corresponding technical solutions of the embodiments of the present invention.
Claims (5)
1. The veterinary glucurolactone soluble powder is characterized by consisting of glucurolactone, anhydrous lactose and citric acid.
2. The soluble powder of glucurolactone for livestock according to claim 1, wherein the soluble powder is prepared from glucurolactone, anhydrous lactose and citric acid according to a mass ratio of 3:6.5: 0.5.
3. The soluble powder of glucurolactone for livestock according to claim 1, wherein the citric acid needs to be crushed, and the particle size is controlled to be 170-190 μm.
4. The soluble powder of glucurolactone for livestock according to claim 1, wherein the pH of a solution obtained after the soluble powder is dissolved is kept between 4.5 and 6.0.
5. The method for preparing the glucurolactone soluble powder for livestock as claimed in any one of claims 1 to 4, wherein the method comprises the following steps:
(1) firstly, 0.5 part by weight of glucurolactone is taken, 0.5 part by weight of citric acid with the granularity of 170-190 microns after being crushed is added, and the mixture is mixed and stirred for 10-15 minutes to obtain a mixture 1;
(2) adding 1 part by weight of glucurolactone into the mixture 1, and mixing and stirring for 10-15 minutes to obtain a mixture 2;
(3) adding 1.5 parts by weight of glucurolactone into the mixture 2, and mixing and stirring for 10-15 minutes to obtain a mixture 3;
(4) adding 3.5 parts by weight of anhydrous lactose into the mixture 3, and mixing and stirring for 10-15 minutes to obtain a mixture 4;
(5) and adding 3 parts by weight of anhydrous lactose into the mixture 4, mixing and stirring for 10-15 minutes, and sieving by using a 80-mesh sieve to obtain the veterinary glucurolactone soluble powder.
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