CN117582422A - Coenzyme Q10 composition containing sunflower seed oil and preparation process thereof - Google Patents
Coenzyme Q10 composition containing sunflower seed oil and preparation process thereof Download PDFInfo
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- CN117582422A CN117582422A CN202311424432.0A CN202311424432A CN117582422A CN 117582422 A CN117582422 A CN 117582422A CN 202311424432 A CN202311424432 A CN 202311424432A CN 117582422 A CN117582422 A CN 117582422A
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- ACTIUHUUMQJHFO-UPTCCGCDSA-N coenzyme Q10 Chemical compound COC1=C(OC)C(=O)C(C\C=C(/C)CC\C=C(/C)CC\C=C(/C)CC\C=C(/C)CC\C=C(/C)CC\C=C(/C)CC\C=C(/C)CC\C=C(/C)CC\C=C(/C)CCC=C(C)C)=C(C)C1=O ACTIUHUUMQJHFO-UPTCCGCDSA-N 0.000 title claims abstract description 89
- 235000017471 coenzyme Q10 Nutrition 0.000 title claims abstract description 88
- ACTIUHUUMQJHFO-UHFFFAOYSA-N Coenzym Q10 Natural products COC1=C(OC)C(=O)C(CC=C(C)CCC=C(C)CCC=C(C)CCC=C(C)CCC=C(C)CCC=C(C)CCC=C(C)CCC=C(C)CCC=C(C)CCC=C(C)C)=C(C)C1=O ACTIUHUUMQJHFO-UHFFFAOYSA-N 0.000 title claims abstract description 86
- 229940110767 coenzyme Q10 Drugs 0.000 title claims abstract description 82
- 235000019198 oils Nutrition 0.000 title claims abstract description 58
- 235000020238 sunflower seed Nutrition 0.000 title claims abstract description 58
- 239000000203 mixture Substances 0.000 title claims abstract description 40
- 238000002360 preparation method Methods 0.000 title abstract description 10
- 235000019156 vitamin B Nutrition 0.000 claims abstract description 40
- 239000011720 vitamin B Substances 0.000 claims abstract description 40
- 239000004005 microsphere Substances 0.000 claims abstract description 28
- 229930003270 Vitamin B Natural products 0.000 claims description 11
- 238000001816 cooling Methods 0.000 claims description 10
- 238000000034 method Methods 0.000 claims description 9
- 238000003756 stirring Methods 0.000 claims description 7
- 238000010438 heat treatment Methods 0.000 claims description 5
- 239000003921 oil Substances 0.000 claims description 5
- 239000008194 pharmaceutical composition Substances 0.000 claims description 2
- 238000004519 manufacturing process Methods 0.000 claims 1
- 230000000694 effects Effects 0.000 abstract description 14
- 241000700159 Rattus Species 0.000 abstract description 9
- 208000010125 myocardial infarction Diseases 0.000 abstract description 8
- 208000031225 myocardial ischemia Diseases 0.000 abstract description 6
- 208000027418 Wounds and injury Diseases 0.000 abstract description 4
- 230000006378 damage Effects 0.000 abstract description 4
- 208000014674 injury Diseases 0.000 abstract description 4
- 210000002966 serum Anatomy 0.000 abstract description 4
- 230000008439 repair process Effects 0.000 abstract description 2
- 239000003814 drug Substances 0.000 description 14
- 229940079593 drug Drugs 0.000 description 9
- NPCOQXAVBJJZBQ-UHFFFAOYSA-N reduced coenzyme Q9 Natural products COC1=C(O)C(C)=C(CC=C(C)CCC=C(C)CCC=C(C)CCC=C(C)CCC=C(C)CCC=C(C)CCC=C(C)CCC=C(C)CCC=C(C)C)C(O)=C1OC NPCOQXAVBJJZBQ-UHFFFAOYSA-N 0.000 description 4
- 229940035936 ubiquinone Drugs 0.000 description 4
- AZQWKYJCGOJGHM-UHFFFAOYSA-N para-benzoquinone Natural products O=C1C=CC(=O)C=C1 AZQWKYJCGOJGHM-UHFFFAOYSA-N 0.000 description 3
- 229920001195 polyisoprene Polymers 0.000 description 3
- 238000013268 sustained release Methods 0.000 description 3
- 239000012730 sustained-release form Substances 0.000 description 3
- 230000002708 enhancing effect Effects 0.000 description 2
- 230000002107 myocardial effect Effects 0.000 description 2
- 230000003647 oxidation Effects 0.000 description 2
- 238000007254 oxidation reaction Methods 0.000 description 2
- -1 quinone compound Chemical class 0.000 description 2
- 206010002383 Angina Pectoris Diseases 0.000 description 1
- 206010003210 Arteriosclerosis Diseases 0.000 description 1
- 208000024172 Cardiovascular disease Diseases 0.000 description 1
- 206010011086 Coronary artery occlusion Diseases 0.000 description 1
- 229940123457 Free radical scavenger Drugs 0.000 description 1
- 206010019280 Heart failures Diseases 0.000 description 1
- 208000007536 Thrombosis Diseases 0.000 description 1
- 230000002159 abnormal effect Effects 0.000 description 1
- 230000032683 aging Effects 0.000 description 1
- 239000003963 antioxidant agent Substances 0.000 description 1
- 230000003078 antioxidant effect Effects 0.000 description 1
- 235000006708 antioxidants Nutrition 0.000 description 1
- 208000011775 arteriosclerosis disease Diseases 0.000 description 1
- 230000003796 beauty Effects 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 210000004369 blood Anatomy 0.000 description 1
- 239000008280 blood Substances 0.000 description 1
- 230000036772 blood pressure Effects 0.000 description 1
- 230000005189 cardiac health Effects 0.000 description 1
- 208000015606 cardiovascular system disease Diseases 0.000 description 1
- 238000006243 chemical reaction Methods 0.000 description 1
- 239000002537 cosmetic Substances 0.000 description 1
- 235000013373 food additive Nutrition 0.000 description 1
- 239000002778 food additive Substances 0.000 description 1
- 230000006870 function Effects 0.000 description 1
- 230000036541 health Effects 0.000 description 1
- 208000019622 heart disease Diseases 0.000 description 1
- 230000005986 heart dysfunction Effects 0.000 description 1
- 230000004217 heart function Effects 0.000 description 1
- 230000036039 immunity Effects 0.000 description 1
- 230000006872 improvement Effects 0.000 description 1
- 238000004811 liquid chromatography Methods 0.000 description 1
- 230000007257 malfunction Effects 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 238000012544 monitoring process Methods 0.000 description 1
- 230000001681 protective effect Effects 0.000 description 1
- 239000002516 radical scavenger Substances 0.000 description 1
- 238000011084 recovery Methods 0.000 description 1
- 238000001356 surgical procedure Methods 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 210000003462 vein Anatomy 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
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
- A61K9/5005—Wall or coating material
- A61K9/5021—Organic macromolecular compounds
- A61K9/5031—Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, poly(lactide-co-glycolide)
-
- 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
- A61K31/12—Ketones
- A61K31/122—Ketones having the oxygen directly attached to a ring, e.g. quinones, vitamin K1, anthralin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
- A61K36/18—Magnoliophyta (angiosperms)
- A61K36/185—Magnoliopsida (dicotyledons)
- A61K36/28—Asteraceae or Compositae (Aster or Sunflower family), e.g. chamomile, feverfew, yarrow or echinacea
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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- Natural Medicines & Medicinal Plants (AREA)
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- Bioinformatics & Cheminformatics (AREA)
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- Alternative & Traditional Medicine (AREA)
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- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
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Abstract
The invention provides a coenzyme Q10 composition containing sunflower seed oil and a preparation process thereof. The invention adopts the degradable polyglycolide-lactide slow release microsphere as the shell to comprise sunflower seed oil dissolved with coenzyme Q10 and B vitamins, improves the treatment effect of the coenzyme Q10 by slow release effect, can obviously reduce the myocardial infarction area of rats, improves SOD activity in the serum of the rats, inhibits MDA generation, and has good protection and repair effects on myocardial ischemia injury.
Description
Technical Field
The invention relates to the technical field of heart treatment, in particular to a coenzyme Q10 composition containing sunflower seed oil and a preparation process thereof.
Background
Ubiquinone (UQ), also known as Coenzyme Q (Coenzyme Q), is a naturally occurring fat-soluble quinone compound, and the Ubiquinone molecule contains a side chain composed of a plurality of polyisoprene units and linked to a p-benzoquinone parent nucleus, the length of the side chain varies depending on the source of Ubiquinone, and the length of the side chain is determined by the reaction catalyzed by polyisoprene pyrophosphorosynthetase. Typically containing n=6-10 polyisoprene units. Mammalian n=10, and human and mammalian are 10 isopentenyl units, so are called Coenzyme Q10 (Coenzyme Q10, coQ 10).
Co Q10 has the functions of improving human immunity, enhancing oxidation resistance, delaying aging, enhancing human vitality and the like, is the most effective oxidation resistant component for preventing arteriosclerosis from forming, is widely used for preventing and controlling cardiovascular system diseases in medicine, can prevent and control myocardial infarction, thrombus from forming, heart failure, angina pectoris, abnormal heart beat and the like, can simultaneously reduce blood pressure, reduce blood fat, assist treatment and recovery after heart disease surgery, help athletes to avoid heart malfunction caused by excessive myocardial burden, effectively improve myocardial weakness, heart dysfunction and the like, and is widely used as a natural antioxidant and free radical scavenger for medical health products, beauty cosmetics and food additives at home and abroad. Is being pushed to be the most effective heart health care product in Europe and America and Japan.
However, the therapeutic effect of the currently clinically used coenzyme Q10 drugs is to be improved, and particularly, how to protect the heart function of patients for a long time, and avoiding the additional burden caused by myocardial infarction is the current mainstream research direction.
Disclosure of Invention
Aiming at the technical problems existing in the prior art, the invention provides a coenzyme Q10 composition containing sunflower seed oil and a preparation process thereof. The preparation process flow of the coenzyme Q10 composition containing sunflower seed oil is simpler, more convenient and efficient, has excellent slow release effect, can effectively control the release rate of coenzyme Q10 in a patient, and achieves more efficient treatment effect.
Specifically, the invention firstly provides a coenzyme Q10 composition containing sunflower seed oil, which is characterized in that the pharmaceutical composition comprises: sunflower seed oil, B vitamins, coenzyme Q10 and degradable polyglycolide-lactide slow release microspheres.
Preferably, the composition comprises 20-30 parts of sunflower seed oil, 10-20 parts of B vitamins, 40-60 parts of coenzyme Q10 and 15-25 parts of degradable polyglycolide-lactide slow release microspheres.
Preferably, the composition comprises 20 parts of sunflower seed oil, 10 parts of B vitamins, 40 parts of coenzyme Q10, and 15 parts of degradable polyglycolide-lactide slow release microspheres.
Preferably, the composition comprises 25 parts of sunflower seed oil, 15 parts of B vitamins, 45 parts of coenzyme Q10 and 20 parts of degradable polyglycolide-lactide slow release microspheres.
Preferably, the composition comprises 30 parts of sunflower seed oil, 20 parts of B vitamins, 60 parts of coenzyme Q10 and 25 parts of degradable polyglycolide-lactide slow release microspheres.
Another object of the present invention is to provide a method for preparing the coenzyme Q10 composition, characterized in that the method comprises the steps of:
s1: adding coenzyme Q10 and B vitamins into sunflower seed oil, and stirring to dissolve the coenzyme Q10 and B vitamins into the sunflower seed oil;
s2: adding the degradable polyglycolide-lactide slow-release microsphere into the sunflower seed oil dissolved with the coenzyme Q10 and the vitamin B obtained in the step S1, heating and cooling, and standing the mixture to obtain the degradable polyglycolide-lactide slow-release microsphere containing the coenzyme Q10, the vitamin B and the sunflower seed oil.
Preferably, the operation of adding the coenzyme Q10 and the B vitamins into the sunflower seed oil is performed under the conditions of normal temperature and light shielding.
Preferably, the coenzyme Q10 is dissolved in the sunflower seed oil at a stirring rate of 200-600 rpm.
Preferably, step s2 is performed at 60-90deg.C for 0.5-1.5h, at a cooling rate of 1-10deg.C/min, and cooling to 4-25deg.C.
Preferably, the mixture should be left to stand for 12-24 hours.
The invention has the following advantages: the invention provides a coenzyme Q10 composition containing sunflower seed oil for the first time, and the medicine adopts degradable polyglycolide-lactide slow release microspheres as a shell and comprises the sunflower seed oil dissolved with coenzyme Q10 and B vitamins, so as to improve the treatment effect of the coenzyme Q10 with slow release effect. The result shows that under the treatment of the coenzyme Q10 composition containing sunflower seed oil, the myocardial infarction area of the rat can be obviously reduced, the myocardial ischemia injury is well protected and repaired, and the SOD activity in the serum of the rat can be improved and the MDA generation can be inhibited after the treatment of the sustained release drug. Compared with the traditional slow release medicine, the preparation process flow of the coenzyme Q10 composition containing the sunflower seed oil is simpler, more convenient and efficient, the slow release effect is excellent, the release rate of the coenzyme Q10 in a patient can be effectively controlled, and the more efficient treatment effect is achieved.
Detailed Description
The present invention will be described in further detail with reference to specific examples so as to more clearly understand the present invention by those skilled in the art.
Example 1
A coenzyme Q10 composition comprising sunflower seed oil comprising: sunflower seed oil, B vitamins, coenzyme Q10 and degradable polyglycolide-lactide slow release microspheres, wherein the sunflower seed oil accounts for 20 parts, the B vitamins account for 10 parts, the coenzyme Q10 accounts for 40 parts and the degradable polyglycolide-lactide slow release microspheres account for 15 parts.
The preparation method of the coenzyme Q10 composition comprises the following steps:
s1: under the conditions of normal temperature and light shielding, adding coenzyme Q10 and B vitamins into sunflower seed oil, and dissolving the coenzyme Q10 and B vitamins into the sunflower seed oil by stirring at 200-600 rpm;
s2: adding the degradable polyglycolide-lactide slow release microsphere into the sunflower seed oil dissolved with the coenzyme Q10 and the vitamin B obtained in the step S1, heating at the temperature of 60-90 ℃ at the cooling rate of 1-10 ℃/min, cooling to the temperature of 4-25 ℃, and standing the mixture for 12-24 hours to obtain the degradable polyglycolide-lactide slow release microsphere loaded with the coenzyme Q10, the vitamin B and the sunflower seed oil.
Example 2
A coenzyme Q10 composition comprising sunflower seed oil comprising: sunflower seed oil, B vitamins, coenzyme Q10 and degradable polyglycolide-lactide slow release microspheres, wherein the sunflower seed oil accounts for 25 parts, the B vitamins account for 15 parts, the coenzyme Q10 accounts for 45 parts and the degradable polyglycolide-lactide slow release microspheres account for 20 parts.
The preparation method of the coenzyme Q10 composition comprises the following steps:
s1: under the conditions of normal temperature and light shielding, adding coenzyme Q10 and B vitamins into sunflower seed oil, and dissolving the coenzyme Q10 and B vitamins into the sunflower seed oil by stirring at 200-600 rpm;
s2: adding the degradable polyglycolide-lactide slow release microsphere into the sunflower seed oil dissolved with the coenzyme Q10 and the vitamin B obtained in the step S1, heating at the temperature of 60-90 ℃ at the cooling rate of 1-10 ℃/min, cooling to the temperature of 4-25 ℃, and standing the mixture for 12-24 hours to obtain the degradable polyglycolide-lactide slow release microsphere loaded with the coenzyme Q10, the vitamin B and the sunflower seed oil.
Example 3
A coenzyme Q10 composition comprising sunflower seed oil comprising: sunflower seed oil, B vitamins, coenzyme Q10 and degradable polyglycolide-lactide slow release microspheres, wherein the sunflower seed oil accounts for 30 parts, the B vitamins account for 20 parts, the coenzyme Q10 accounts for 60 parts and the degradable polyglycolide-lactide slow release microspheres account for 25 parts.
The preparation method of the coenzyme Q10 composition comprises the following steps:
s1: under the conditions of normal temperature and light shielding, adding coenzyme Q10 and B vitamins into sunflower seed oil, and dissolving the coenzyme Q10 and B vitamins into the sunflower seed oil by stirring at 200-600 rpm;
s2: adding the degradable polyglycolide-lactide slow release microsphere into the sunflower seed oil dissolved with the coenzyme Q10 and the vitamin B obtained in the step S1, heating at the temperature of 60-90 ℃ at the cooling rate of 1-10 ℃/min, cooling to the temperature of 4-25 ℃, and standing the mixture for 12-24 hours to obtain the degradable polyglycolide-lactide slow release microsphere loaded with the coenzyme Q10, the vitamin B and the sunflower seed oil.
Example 4
In order to evaluate the sustained release efficacy of the sunflower seed oil-containing coenzyme Q10 composition prepared in the present invention. 10mg of the coenzyme Q10 slow-release drug prepared in the invention obtained in the examples 1-3 is respectively dissolved in 10mL of PBS solution, the solution is placed in a constant temperature shaking table at 37 ℃ and is shaken at a constant speed of 150r/min, samples are taken at intervals, and the release amount of the coenzyme Q10 in the sample is analyzed by a liquid chromatography. The results show that: the release rates of the coenzyme Q10 slow-release drugs respectively reach 8.2+/-0.3%, 8.1+/-0.4% and 8.5+/-0.2% in 1 day, and then release at a relatively slow speed until the release rate reaches 10 days, and the coenzyme Q10 slow-release drugs of examples 1-3 respectively reach 94.5+/-1.1%, 94.8+/-1.3% and 95.6+/-0.5%, which indicates that the coenzyme Q10 slow-release drugs prepared by the invention have good slow-release effects.
Example 5
Taking example 1 as an example, the protective effect of the medicament of the invention on myocardial ischemia is further demonstrated. Specifically, a plurality of SD rats with the weight of about 200g are selected, a coronary artery occlusion method is adopted to prepare myocardial ischemia injury model rats, rats with successful modeling are selected and evenly divided into a blank group, a control group and a treatment group, wherein 8 rats are selected from each group, the blank group is not treated by any medicine in a monitoring period, the control group is administered with 0.5mg/kg of coenzyme Q10 daily, the treatment group is administered with 0.5mg/kg of coenzyme Q10 composition containing sunflower seed oil daily, and the treatment group is continuously administered for one week. After the administration is finished, counting the myocardial infarction range after vein ligation and the SOD and MDA content in serum. As shown in the table below, the coenzyme Q10 slow-release drug can obviously reduce myocardial infarction area, has good protection and repair effects on myocardial ischemia injury, can improve SOD activity in rat serum after being treated by the slow-release drug, inhibits MDA generation, and is beneficial to myocardial infarction.
TABLE 1 protection of coenzyme Q10 sustained release drug against myocardial ischemia
| Group of | Myocardial infarction area (%) | SOD(NU/ml) | MDA(nmol/ml) |
| Blank group | 18.96±1.52 | 195.45±10.25 | 8.93±0.98 |
| Control group | 10.23±1.08 | 245.25±8.66 | 5.12±0.56 |
| Treatment group | 4.25±1.23 | 312.26±10.63 | 1.98±0.33 |
It should be noted that the above examples are only for further illustrating and describing the technical solution of the present invention, and are not intended to limit the technical solution of the present invention, and the method of the present invention is only a preferred embodiment and is not intended to limit the scope of the present invention. Any modification, equivalent replacement, improvement, etc. made within the spirit and principle of the present invention should be included in the protection scope of the present invention.
Claims (10)
1. A coenzyme Q10 composition comprising sunflower seed oil, wherein the pharmaceutical composition comprises: sunflower seed oil, B vitamins, coenzyme Q10 and degradable polyglycolide-lactide slow release microspheres.
2. The coenzyme Q10 composition of claim 1, wherein the composition comprises 20-30 parts of sunflower seed oil, 10-20 parts of B-vitamin, 40-60 parts of coenzyme Q10 and 15-25 parts of degradable polyglycolide-lactide slow release microsphere.
3. The coenzyme Q10 composition of claim 1, wherein the composition comprises 20 parts sunflower seed oil, 10 parts B vitamins, 40 parts coenzyme Q10 and 15 parts degradable polyglycolide-lactide slow release microspheres.
4. The coenzyme Q10 composition of claim 1, wherein the composition comprises 25 parts sunflower seed oil, 15 parts B vitamins, 45 parts coenzyme Q10 and 20 parts degradable polyglycolide-lactide slow release microspheres.
5. The coenzyme Q10 composition of claim 1, wherein the composition comprises 30 parts sunflower seed oil, 20 parts B vitamins, 60 parts coenzyme Q10 and 25 parts degradable polyglycolide-lactide slow release microspheres.
6. The method for producing the coenzyme Q10 composition according to any one of claims 1 to 5, characterized in that the method comprises the steps of:
s1: adding coenzyme Q10 and B vitamins into sunflower seed oil, and stirring to dissolve the coenzyme Q10 and B vitamins into the sunflower seed oil;
s2: adding the degradable polyglycolide-lactide slow-release microsphere into the sunflower seed oil dissolved with the coenzyme Q10 and the vitamin B obtained in the step S1, heating and cooling, and standing the mixture to obtain the degradable polyglycolide-lactide slow-release microsphere containing the coenzyme Q10, the vitamin B and the sunflower seed oil.
7. The method according to claim 6, wherein the step of adding the coenzyme Q10 and the vitamin B to the sunflower seed oil is performed at room temperature under a dark condition.
8. The method according to claim 6, wherein the coenzyme Q10 is dissolved in the sunflower seed oil at a stirring rate of 200 to 600 rpm.
9. The process according to claim 6, wherein step s2 is carried out at 60-90℃for a period of time of 0.5-1.5h, at a rate of 1-10℃per minute, and to a temperature of 4-25 ℃.
10. The process of claim 6, wherein the mixture is allowed to stand for 12 to 24 hours.
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