CN116966159A - Hypoglycemic preparation containing rehmannia root extract and preparation method thereof - Google Patents
Hypoglycemic preparation containing rehmannia root extract and preparation method thereof Download PDFInfo
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- CN116966159A CN116966159A CN202311097072.8A CN202311097072A CN116966159A CN 116966159 A CN116966159 A CN 116966159A CN 202311097072 A CN202311097072 A CN 202311097072A CN 116966159 A CN116966159 A CN 116966159A
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- rehmannia root
- preparation
- root extract
- hypoglycemic
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- 235000020824 obesity Nutrition 0.000 description 1
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- 229920000136 polysorbate Polymers 0.000 description 1
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- 230000002441 reversible effect Effects 0.000 description 1
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- 239000000126 substance Substances 0.000 description 1
- YROXIXLRRCOBKF-UHFFFAOYSA-N sulfonylurea Chemical class OC(=N)N=S(=O)=O YROXIXLRRCOBKF-UHFFFAOYSA-N 0.000 description 1
- 238000001356 surgical procedure Methods 0.000 description 1
- KNZSXKKCTOYLSV-UHFFFAOYSA-N trigofoenoside A Natural products O1C(CO)C(O)C(O)C(O)C1OCC(C)CCC(C(C1C2(C)CCC3C4(C)CC5)C)(O)OC1CC2C3CC=C4CC5OC1OC(CO)C(O)C(O)C1OC1OC(C)C(O)C(O)C1O KNZSXKKCTOYLSV-UHFFFAOYSA-N 0.000 description 1
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- A61K9/2806—Coating materials
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Abstract
The application belongs to the field of medicines, and in particular relates to a hypoglycemic preparation containing rehmannia root extract and a preparation method thereof. The hypoglycemic preparation of the application is a film coated tablet containing rehmannia root extract, and the preparation method of the hypoglycemic preparation comprises the following steps: dissolving rehmanniae radix extract in organic solvent, spraying onto crosslinked povidone, drying to obtain mixture, mixing with filler and lubricant, and tabletting; spraying coating liquid on the tablet core, and drying to obtain the final product; the prepared film coated tablet has good surface appearance and stability, the coated film is not easy to wear, break and fall off, the medicine storage and the use are facilitated, the film coated tablet also has good blood sugar reducing effect, the blood sugar of a tetraoxypyrimidine diabetic mouse can be obviously reduced, and the effect of reducing the hyperglycemia caused by the injection of epinephrine into a normal mouse is also realized.
Description
Technical Field
The application belongs to the field of medicines, and in particular relates to a hypoglycemic preparation containing rehmannia root extract and a preparation method thereof.
Background
Diabetes is a metabolic disease characterized by hyperglycemia, which is caused by defective insulin secretion or impaired biological action, or both, and which leads to chronic damage and dysfunction of various tissues, especially eyes, kidneys, heart, blood vessels, nerves; clinical data show that about 10 years after diabetes mellitus occurs, 30% -40% of patients have at least one complication, and once the complication occurs, the drug treatment is difficult to reverse; the incidence rate of diabetes mellitus in various countries in the world is in an increasing trend year by year, and according to the related data of world health organization, the global diabetes mellitus patients are over 3.82 hundred million, the diabetes mellitus patients in China are about 1.5 hundred million people, and 3.5 hundred million people are in the early stage of the diabetes mellitus patients, so that the rehabilitation and medical treatment of the diabetes mellitus patients are one of the important contents of medical and health work in China.
The treatment method of diabetes comprises basic treatment (diet control, proper amount of exercise), drug treatment (such as metformin, acarbose, sulfonylurea drugs, etc.), and surgical treatment (suitable for patients with diabetes with obesity). Various chemical western medicines are taken in the early onset of diabetes, although blood sugar can be rapidly reduced, western medicines can generate great side effects on the body, the treatment result of the western medicines can be gradually increased, various medicines are continuously taken instead, the western medicines are adopted to treat the diabetes, the islet functions cannot be fundamentally recovered, the blood sugar is stably reduced, the purpose of treating the diabetes is achieved, and the toxic and side effects of the medicines are accumulated in the body for a long time along with the long-term accumulation of the toxic and side effects of the medicines, so that the body is more damaged, and various complications are caused. Therefore, the development direction of the medicine for treating diabetes is gradually changed from western medicines to traditional Chinese medicine preparations.
Rehmannia root is a fresh or dried root tuber of rehmannia (Rehmannia glutinosa Libosch) belonging to the Scrophulariaceae, and the processing method is different from the processing method of fresh rehmannia root, raw rehmannia root and prepared rehmannia root, and the different processed products have different emphasis. The components found in the rehmannia root comprise catalpol, rehmannia root glycoside A, rehmannia root glycoside D, rehmannia root glycoside E, aucubin, leonurus glycoside, dihydro catalpol, milt glycoside and the like, wherein the catalpol content is higher, and the ingredients are widely applied to the fields of biology, medicine and the like due to good effects of reducing blood sugar, resisting hepatitis virus and the like. The patent with application number 202211576840.3 discloses a rehmannia root functional factor extract and application thereof in preparing antioxidant and/or hypoglycemic drugs, and an in vitro experiment method is adopted to research the inhibition activity of alpha-glucosidase of the rehmannia root functional factor extract, and the rehmannia root functional factor extract is found to have obvious inhibition effect on the alpha-glucosidase; rehmannia is widely distributed and is rich in resources, so that further development of a traditional Chinese medicine preparation containing rehmannia extract is necessary for treating diabetes.
Disclosure of Invention
Aiming at the defects of the prior art, the application provides a hypoglycemic preparation containing rehmannia root extract and a preparation method thereof, and the hypoglycemic preparation provided by the application has good hypoglycemic effect, can obviously reduce blood sugar of mice with tetraoxypyrimidine diabetes, has the effect of reducing hyperglycemia caused by epinephrine injection of normal mice, and has better effects than acarbose.
The technical scheme adopted by the application for achieving the purpose is as follows:
the preparation method of the hypoglycemic preparation containing the rehmannia root extract comprises the following steps of:
s1, 1-2 parts of rehmannia root extract is dissolved in 10-15 parts of organic solvent, uniformly sprayed on 20-30 parts of crosslinked povidone, dried to obtain a mixture, uniformly mixed with 60-70 parts of filler and 1-2 parts of lubricant, and pressed into tablet cores;
s2, preheating the tablet cores in a rotary coating pot, and spraying 5-10 parts of coating liquid into a spray gun to obtain the tablet cores in the rotary coating pot;
further, the preparation method of the rehmannia root extract in the step S1 comprises the following steps: oven drying radix rehmanniae, pulverizing, sieving with 40-70 mesh sieve to obtain radix rehmanniae powder, sequentially adding radix rehmanniae powder, cellulase and Tween 80 into solvent, soaking for 20-30min, microwave extracting for 3-5min, vacuum filtering, and concentrating the filtrate to obtain radix rehmanniae extract;
further, the mass ratio of the rehmannia powder to the solvent is 1:15-20; the dosage of the cellulase is 0.6-1.0g/L solvent; the dosage of the Tween 80 is 1.2-1.5g/L of solvent; the solvent is ethanol and water with the volume ratio of 1:1-2; the microwave extraction power is 400-600W, and the microwave extraction temperature is 60-80 ℃.
Further, in the step S1, the organic solvent is one or more of acetonitrile, dichloromethane, chloroform, methanol and absolute ethanol; the filler is one or more of lactose, mannitol and sucrose; the lubricant is one or more of magnesium stearate, talcum powder and silicon dioxide.
Further, the coating liquid in the step S2 comprises the following components in parts by weight: 8-12% of modified polyvinyl alcohol; 8-12% of modified polyacrylic resin; 1-2% glycyrrhizin disodium; 0.5-0.8% shellac; the balance of deionized water;
further, the preparation method of the modified polyvinyl alcohol comprises the following steps: adding polyvinyl alcohol into dimethyl sulfoxide solution, heating to 95 ℃, stirring until the polyvinyl alcohol is dissolved, adding phthalic anhydride, continuing to react for 4-6 hours, naturally cooling to room temperature after the reaction is finished, filtering, and drying filter residues to obtain modified polyvinyl alcohol; the mass ratio of the polyvinyl alcohol to the phthalic anhydride is 1:0.5-0.6; the reaction process is as follows:
further, the preparation method of the modified polyacrylic resin comprises the following steps:
(1) Adding ethylene glycol and sodium hydride into anhydrous tetrahydrofuran, protecting with nitrogen, heating to 30-40 ℃, reacting for 2-3h, adding chloromethyl vinyl benzene into the reaction solution, continuing to react for 2-3h, adding water for quenching after the reaction is finished, removing tetrahydrofuran, adding dichloromethane for extraction, and concentrating an organic phase under reduced pressure to obtain a diene monomer; the mol ratio of the ethylene glycol to the chloromethyl vinyl benzene to the sodium hydride is 1:1.1-1.2:1.5-1.8, and the reaction process is as follows:
(2) Adding methacrylic acid and diene monomer into 50-60% ethanol solution, heating to 70-80 ℃, dripping 30-40% potassium persulfate aqueous solution, continuing to react for 6-8h after dripping, naturally cooling to room temperature after the reaction is finished, filtering, and drying filter residues to obtain modified polyacrylic resin; the molar ratio of the methacrylic acid to the diene monomer is 1:0.4-0.5; the dosage of the potassium persulfate is 0.6 to 0.8 percent of the mass of the methacrylic acid.
The application provides a hypoglycemic preparation containing rehmannia root extract, which is prepared by the preparation method of the hypoglycemic preparation containing rehmannia root extract.
The application has the following beneficial effects:
according to the application, coating liquid containing modified polyvinyl alcohol and modified polyacrylic resin is used for coating a tablet core, wherein the modified polyvinyl alcohol molecules contain more polar groups of hydroxyl and carboxyl, the modified polyacrylic resin molecules also contain polar groups of carboxyl, and the polar groups can enable the molecules to be more easily distributed through interaction of intramolecular hydrogen bonds or dipole moments, so that the stability of the coating liquid is enhanced, the coating rate is improved, the problem of rough pits after film formation can be avoided, the film formation property of the modified polyvinyl alcohol is better, and the formed coating film surface has glossiness and can not be adhered; and the molecules of the two materials contain rigid benzene ring groups, so that the mechanical property of the coating film is improved, and the coating film is not easy to break under the action of external force, and cracks are generated; the network structure of the modified polyacrylic resin can also improve the mechanical property of the coating liquid after film formation due to the cross-linked structure among chains, so that the coating film has certain mechanical property and is not easy to wear, break and fall off; thus, the film coated tablet with better strong light resistance, high temperature and high humidity performance and better stability is prepared.
The rehmannia root extract is prepared into the film coated tablet, which is beneficial to medicine storage and use; the coating film is an enteric coating film, has the functions of keeping the medicine in the stomach and preventing the medicine from being stimulated in the stomach to be dissolved, ensures that the medicine reaches a specific part of the intestine and releases the medicine, and effectively plays the role of inhibiting alpha-glucosidase, thereby achieving the effect of reducing blood sugar; the hypoglycemic preparation provided by the application has good hypoglycemic effect, can obviously reduce the blood sugar of mice with tetraoxypyrimidine diabetes, has the effect of reducing hyperglycemia caused by epinephrine injection of normal mice, and has better effect than acarbose.
Detailed Description
The technical solutions of the embodiments of the present application will be clearly and completely described below in conjunction with the embodiments of the present application, and it is apparent that the described embodiments are only some embodiments of the present application, not all embodiments. All other embodiments, which can be made by those skilled in the art based on the embodiments of the application without making any inventive effort, are intended to be within the scope of the application.
Crosslinked povidone CAS number 25249-54-1; tween CAS number 809005-65-6; lactose CAS number 63-42-3; mannitol CAS number 87-78-5; sucrose CAS number 57-50-1; magnesium stearate CAS number 557-04-0; talcum powder CAS number 14807-96-6; silica CAS number 14808-60-7; glycyrrhizin disodium CAS number 71277-79-7; shellac CAS number 9000-59-3; ethylene glycol CAS number 107-21-1; sodium hydride CAS number 7646-69-7; chloromethyl vinyl benzene CAS No. 30030-25-2; methacrylic acid CAS No. 79-41-4; potassium persulfate CAS number 7727-21-1; polyvinyl alcohol CAS number 9002-89-5 (1799 type); phthalic anhydride CAS number 85-44-9; dimethyl sulfoxide CAS number 67-68-5; anhydrous tetrahydrofuran CAS number 109-99-9; ethanol CAS number 64-17-5; acetonitrile CAS number 75-05-8; dichloromethane CAS number 75-09-2; chloroform CAS number 67-66-3; methanol CAS number 67-56-1; all chemical reagents are commercially available.
Example 1
A preparation method of a hypoglycemic preparation containing rehmannia root extract, wherein the hypoglycemic preparation is a film coated tablet containing the rehmannia root extract, and comprises the following steps in parts by weight:
s1, dissolving 2 parts of rehmannia root extract in 15 parts of organic solvent, uniformly spraying the mixture onto 30 parts of crospovidone, drying the mixture to obtain a mixture, uniformly mixing the mixture with 70 parts of filler and 2 parts of lubricant, and pressing the mixture into tablet cores, wherein each tablet weighs 0.200g; wherein the organic solvent is acetonitrile; the filler is lactose; the lubricant is magnesium stearate;
s2, placing the tablet cores into a rotary coating pot for preheating, and spraying 10 parts of coating liquid into a spray gun to obtain the tablet cores in the rotary coating pot;
the preparation method of the rehmannia root extract comprises the following steps: oven drying rehmanniae radix, pulverizing, sieving with 70 mesh sieve to obtain rehmanniae radix powder, sequentially adding rehmanniae radix powder, cellulase and Tween 80 into solvent, soaking for 30min, microwave extracting for 5min, vacuum filtering, and concentrating the filtrate to obtain rehmanniae radix extract; wherein the mass ratio of the rehmannia powder to the solvent is 1:20; the dosage of the cellulase is 1.0g/L solvent; the dosage of Tween 80 is 1.5g/L of solvent; the solvent is ethanol and water with the volume ratio of 1:2; the microwave extraction power was 600W and the microwave extraction temperature was 60 ℃.
The coating liquid comprises the following components in parts by weight: 12% modified polyvinyl alcohol; 12% of modified polyacrylic resin; 2% glycyrrhizin disodium; 0.8% shellac; the balance of deionized water.
The preparation method of the coating liquid comprises the following steps: sequentially adding glycyrrhizin disodium, modified polyvinyl alcohol, modified polyacrylic resin and shellac into deionized water, and uniformly mixing to obtain the final product.
The preparation method of the modified polyvinyl alcohol comprises the following steps: adding polyvinyl alcohol into dimethyl sulfoxide solution, heating to 95 ℃, stirring until the polyvinyl alcohol is dissolved, adding phthalic anhydride, continuing to react for 5 hours, naturally cooling to room temperature after the reaction is finished, filtering, and drying filter residues to obtain modified polyvinyl alcohol; the substitution degree of phthalic anhydride was 23.5% by elemental analysis; the prepared modified polyvinyl alcohol has fluorescence absorption under an ultraviolet lamp (254 nm); wherein the mass ratio of the polyvinyl alcohol to the phthalic anhydride is 1:0.6; the dosage of dimethyl sulfoxide is 25 times of the mass of polyvinyl alcohol, and the reaction process is as follows:
the preparation method of the modified polyacrylic resin comprises the following steps:
(1) Adding ethylene glycol and sodium hydride into anhydrous tetrahydrofuran, protecting with nitrogen, heating to 35 ℃, reacting for 3 hours, adding chloromethyl vinyl benzene into the reaction liquid, continuing to react for 2 hours, adding water for quenching after the reaction is completed, removing tetrahydrofuran, adding dichloromethane for extraction, and concentrating an organic phase under reduced pressure to obtain a diene monomer; wherein the mol ratio of the ethylene glycol to the chloromethyl vinyl benzene to the sodium hydride is 1:1.1:1.5, and the reaction process is as follows:
diene monomer: ESI (m/z): 263.2[ M+H ]] + ， 1 H-NMR(600MHz，DMSO-d 6 ，δppm)：7.35-7.43(m，8H)，7.29(t，J＝8.4Hz，2H)，6.30-6.32(m，2H)，4.99-5.04(m，4H)，3.36-3.39(m，2H)，1.58-1.60(m，4H)。
(2) Adding methacrylic acid and diene monomer into 60% ethanol solution, heating to 80 ℃, dropwise adding 40% potassium persulfate aqueous solution by mass fraction, continuing to react for 8 hours after the completion of the dripping, naturally cooling to room temperature, filtering, and drying filter residues to obtain modified polyacrylic resin; wherein the molar ratio of methacrylic acid to diene monomer is 1:0.5; the amount of potassium persulfate was 0.8% by mass of methacrylic acid.
Example 2
A preparation method of a hypoglycemic preparation containing rehmannia root extract, wherein the hypoglycemic preparation is a film coated tablet containing the rehmannia root extract, and comprises the following steps in parts by weight:
s1, 1 part of rehmannia root extract is dissolved in 10 parts of organic solvent, uniformly sprayed onto 20 parts of crospovidone, dried to obtain a mixture, uniformly mixed with 60 parts of filler and 1 part of lubricant, and pressed into tablet cores, wherein each tablet weighs 0.200g; wherein the organic solvent is methylene dichloride; the filler is mannitol; the lubricant is talcum powder;
s2, preheating the tablet cores in a rotary coating pot, and spraying 5 parts of coating liquid into a spray gun to obtain the tablet cores in the rotary coating pot;
the preparation method of the rehmannia root extract comprises the following steps: oven drying radix rehmanniae, pulverizing, sieving with 40 mesh sieve to obtain radix rehmanniae powder, sequentially adding radix rehmanniae powder, cellulase and Tween 80 into solvent, soaking for 20min, microwave extracting for 3min, vacuum filtering, and concentrating the filtrate to obtain radix rehmanniae extract; wherein the mass ratio of the rehmannia powder to the solvent is 1:15; the dosage of the cellulase is 0.6g/L solvent; the dosage of Tween 80 is 1.2g/L of solvent; the solvent is ethanol and water with the volume ratio of 1:1; the microwave extraction power was 400W and the microwave extraction temperature was 80 ℃.
The coating liquid comprises the following components in parts by weight: 8% of modified polyvinyl alcohol; 8% of modified polyacrylic resin; 1% glycyrrhizin disodium; 0.5% shellac; the balance of deionized water.
The preparation methods of the coating liquid, the modified polyvinyl alcohol and the modified polyacrylic resin were the same as in example 1.
Example 3
A preparation method of a hypoglycemic preparation containing rehmannia root extract, wherein the hypoglycemic preparation is a film coated tablet containing the rehmannia root extract, and comprises the following steps in parts by weight:
s1, 1.5 parts of rehmannia root extract is dissolved in 13 parts of organic solvent, uniformly sprayed onto 25 parts of crospovidone, dried to obtain a mixture, uniformly mixed with 65 parts of filler and 1.5 parts of lubricant, and pressed into tablet cores, wherein each tablet has the weight of 0.200g; wherein the organic solvent is chloroform; the filler is sucrose; the lubricant is silicon dioxide;
s2, preheating the tablet cores in a rotary coating pot, and spraying 8 parts of coating liquid into a spray gun to obtain the tablet cores in the rotary coating pot;
the preparation method of the rehmannia root extract comprises the following steps: oven drying radix rehmanniae, pulverizing, sieving with 50 mesh sieve to obtain radix rehmanniae powder, sequentially adding radix rehmanniae powder, cellulase and Tween 80 into solvent, soaking for 25min, microwave extracting for 4min, vacuum filtering, and concentrating the filtrate to obtain radix rehmanniae extract; wherein the mass ratio of the rehmannia powder to the solvent is 1:18; the dosage of the cellulase is 0.8g/L solvent; the dosage of Tween 80 is 1.3g/L of solvent; the solvent is ethanol and water with the volume ratio of 1:1.5; the microwave extraction power was 500W and the microwave extraction temperature was 70 ℃.
The coating liquid comprises the following components in parts by weight: 10% modified polyvinyl alcohol; 10% of modified polyacrylic resin; 1.5% glycyrrhizin disodium; 0.7% shellac; the balance of deionized water.
The preparation methods of the coating liquid, the modified polyvinyl alcohol and the modified polyacrylic resin were the same as in example 1.
Example 4
A preparation method of a hypoglycemic preparation containing rehmannia root extract, wherein the hypoglycemic preparation is a film coated tablet containing the rehmannia root extract, and comprises the following steps in parts by weight:
s1, dissolving 2 parts of rehmannia root extract in 10 parts of organic solvent, uniformly spraying the mixture onto 30 parts of crospovidone, drying the mixture to obtain a mixture, uniformly mixing the mixture with 60 parts of filler and 1 part of lubricant, and pressing the mixture into tablet cores, wherein each tablet weighs 0.200g; wherein the organic solvent is methanol; the filler is sucrose; the lubricant is magnesium stearate;
s2, placing the tablet cores into a rotary coating pot for preheating, and spraying 10 parts of coating liquid into a spray gun to obtain the tablet cores in the rotary coating pot;
the preparation method of the rehmannia root extract comprises the following steps: oven drying radix rehmanniae, pulverizing, sieving with 60 mesh sieve to obtain radix rehmanniae powder, sequentially adding radix rehmanniae powder, cellulase and Tween 80 into solvent, soaking for 20min, microwave extracting for 4min, vacuum filtering, and concentrating the filtrate to obtain radix rehmanniae extract; wherein the mass ratio of the rehmannia powder to the solvent is 1:20; the dosage of the cellulase is 0.8g/L solvent; the dosage of Tween 80 is 1.2g/L of solvent; the solvent is ethanol and water with the volume ratio of 1:2; the microwave extraction power was 600W and the microwave extraction temperature was 70 ℃.
The coating liquid comprises the following components in parts by weight: 12% modified polyvinyl alcohol; 10% of modified polyacrylic resin; 2% glycyrrhizin disodium; 0.5% shellac; the balance of deionized water.
The preparation methods of the coating liquid, the modified polyvinyl alcohol and the modified polyacrylic resin were the same as in example 1.
Comparative example 1
The composition of the coating liquid was different from that of example 1.
A preparation method of hypoglycemic agent containing rehmanniae radix extract, rehmanniae radix extract and modified polyacrylic resin is the same as in example 1.
The coating liquid comprises the following components in parts by weight: 12% polyvinyl alcohol; 12% of modified polyacrylic resin; 2% glycyrrhizin disodium; 0.8% shellac; the balance of deionized water.
The preparation method of the coating liquid comprises the following steps: sequentially adding glycyrrhizin disodium, polyvinyl alcohol, modified polyacrylic resin and shellac into deionized water, and uniformly mixing to obtain the final product.
Comparative example 2
The composition of the coating liquid was different from that of example 1.
A preparation method of hypoglycemic agent containing rehmanniae radix extract, rehmanniae radix extract and modified polyvinyl alcohol is the same as in example 1.
The coating liquid comprises the following components in parts by weight: 12% modified polyvinyl alcohol; 12% of polyacrylic resin; 2% glycyrrhizin disodium; 0.8% shellac; the balance of deionized water.
The preparation method of the coating liquid comprises the following steps: sequentially adding glycyrrhizin disodium, modified polyvinyl alcohol, polyacrylic resin and shellac into deionized water, and uniformly mixing to obtain the final product.
Comparative example 3
The composition of the coating liquid was different from that of example 1.
A preparation method of hypoglycemic agent containing rehmanniae radix extract, rehmanniae radix extract and modified polyacrylic resin is the same as in example 1.
The coating liquid comprises the following components in parts by weight: 12% of modified polyacrylic resin; 2% glycyrrhizin disodium; 0.8% shellac; the balance of deionized water.
The preparation method of the coating liquid comprises the following steps: sequentially adding glycyrrhizin disodium, polyacrylic resin and shellac into deionized water, and mixing uniformly.
Correlation testing
1. Quality detection of film-coated tablets
The coated tablets prepared in examples 1 to 4 and comparative examples 1 to 3 were subjected to detection of coating rate, tablet weight difference and appearance properties, and the results are shown in Table 1.
Table 1 comparison of quality tests of coated tablets
| Group of | Coating rate% | Sheet weight difference | Appearance characteristics |
| Example 1 | 99.61 | ＜±2％ | Smooth and crack-free |
| Example 2 | 99.34 | ＜±2％ | Smooth and crack-free |
| Example 3 | 99.25 | ＜±2％ | Smooth and crack-free |
| Example 4 | 99.18 | ＜±2％ | Smooth and crack-free |
| Comparative example 1 | 97.53 | ＜±2％ | Coarse and crack-free |
| Comparative example 2 | 96.62 | ＜±2％ | Coarse and crack-free |
| Comparative example 3 | 68.46 | ＜±10％ | Coarse and concave spots and adhesion |
As can be seen from Table 1, the coating rates of examples 1 to 4 (film coated tablets) all reached more than 99%, and the prepared film coated tablets were small in tablet weight difference, smooth in tablet surface appearance, free of cracks and good in surface appearance; the coating liquid component used in example 1 contained modified polyvinyl alcohol, modified polyacrylic resin, as compared with comparative examples 1 to 3; the modified polyvinyl alcohol molecule contains more polar groups of hydroxyl and carboxyl, the modified polyacrylic resin molecule also contains polar groups of carboxyl, and the polar groups can lead the molecules to be more easily distributed through the interaction of intramolecular hydrogen bonds or dipole moments, thus enhancing the stability of coating liquid, being beneficial to improving the coating rate, being capable of avoiding the problem of rough pits after film formation, having better film forming property of the modified polyvinyl alcohol, and leading the surface of the formed coating film to have glossiness and not to be sticky.
2. Friability test of film coated tablets
The film-coated tablets prepared in examples 1 to 4 and comparative examples 1 to 3 were measured using a friability tester for 30 minutes, and the results are shown in Table 2.
Table 2 friability comparison of film coated tablets
As is clear from Table 2, the film-coated tablets of examples 1 to 4 (film-coated tablets) were all obtained, which had good appearance, were smooth and free from cracks, and had good surface, and the film-coated film had a certain brittleness resistance, and was not easily worn and dropped off under the action of external force; the coating liquid component used in example 1 contained modified polyvinyl alcohol, modified polyacrylic resin, as compared with comparative examples 1 to 3; the molecules of the two materials contain rigid benzene ring groups, so that the mechanical property of the coating film is improved, and the coating film is not easy to break under the action of external force, and cracks are generated; and the network structure of the modified polyacrylic resin can also improve the mechanical property of the coating liquid after film formation due to the cross-linked structure among chains, so that the coating film has certain mechanical property and is not easy to wear, break and fall off.
3. Stability test of film coated tablets
The film-coated tablets prepared in examples 1 to 4 and comparative examples 1 to 3 were each prepared by subjecting 10 tablets to conditions of intense light (2300 to 3500 LX), high temperature (60 ℃) and high humidity (RH 90%) for 10 days, and further measuring the properties and disintegration time, and comparing with 0 day, and the results are shown in Table 3.
Table 3 comparison of stability of film coated tablets
As can be seen from Table 3, examples 1 to 4 (film-coated tablets) all had good high-light resistance, high-humidity and high-temperature stability, and long disintegration time and continued action; compared with comparative examples 1-3, the coating liquid containing the modified polyvinyl alcohol and the modified polyacrylic resin used in example 1 has good stability, the hydrogen bond bonding between the components of the coating liquid formed by polar groups is more sufficient, and a coating film with good compactness and stability can be formed, so that the coating film has better strong light resistance, high temperature resistance and high humidity resistance.
4. Hypoglycemic experiment of hypoglycemic preparation containing rehmannia root extract
50 healthy Kunming mice are taken, and the mice are used as male and female, have the weight of 26+/-2 g, are randomly divided into 5 groups, and are respectively a physiological saline group, an acarbose group (Bayer medicine health-care Co., ltd., batch number is 101181), a low-dose group, a medium-dose group and a high-dose group of the hypoglycemic agent (film coated tablets prepared in the embodiment 1); tetraoxypyrimidine diabetic mice are subjected to intraperitoneal injection of tetraoxypyrimidine (200 mg/kg) for 72 hours, fasting blood glucose is measured, and when blood glucose values are above 11.0mmol/L, the difference between average blood glucose values of animals in groups is not more than 0.5mmol/L; 1 time a day, continuously irrigating the stomach for 8 days, and fasted for 3 hours after the last administration, and taking blood from the tail vein to measure blood sugar; the results are shown in Table 4.
TABLE 4 Effect of hypoglycemic agents on blood glucose levels in mice with Tetraoxypyrimidine diabetes
| Group of | Dosage (g/Kg) | Blood sugar (mmol/L) |
| Physiological saline group | / | 11.52±0.57 |
| Acarbose group | 0.1 | 7.98±0.74 |
| Low dosage group of hypoglycemic agent | 0.1 | 6.36±0.32 |
| Dosage group in hypoglycemic agent | 0.2 | 5.72±0.45 |
| High dosage group of hypoglycemic agent | 0.4 | 5.04±0.38 |
As shown in Table 4, compared with the physiological saline group, the low, medium and high dose groups of the hypoglycemic preparation provided by the application can obviously reduce the blood sugar of the mice with the tetraoxypyrimidine diabetes, which indicates that the hypoglycemic preparation containing the rehmannia root extract provided by the application has good hypoglycemic effect and has obvious dose-effect relationship on the hypoglycemic effect. Under the same experimental conditions, compared with a physiological saline group, the acarbose group can also reduce the blood sugar value of mice, but the blood sugar reducing effect is obviously inferior to that of the blood sugar reducing preparation containing rehmannia root extract.
60 healthy Kunming mice are taken, the weight of the mice is 26+/-2 g, the mice are randomly divided into 6 groups, and 10 mice in each group are respectively a normal group, a normal saline group, an acarbose group (Bayer medicine health-care Co., ltd., batch number is 101181), a low-dose group, a medium-dose group and a high-dose group of hypoglycemic agents (film coated tablets prepared in example 1); 1 time a day, continuously lavaging for 8 days, and fasted for 3 hours after the last administration, wherein except for the normal group, epinephrine is injected into each group of abdominal cavity for 100 mug/kg, and blood sugar is measured after 30 minutes by tail vein blood sampling; the results are shown in Table 5.
TABLE 5 Effect of hypoglycemic agents on blood glucose levels in mice hyperglycemic with epinephrine
| Group of | Dosage (g/Kg) | Blood sugar (mmol/L) |
| Normal group | / | 7.24±0.43 |
| Physiological saline group | / | 15.46±0.12 |
| Acarbose group | 0.1 | 10.72±0.53 |
| Low dosage group of hypoglycemic agent | 0.1 | 9.17±0.34 |
| Dosage group in hypoglycemic agent | 0.2 | 8.36±0.22 |
| High dosage group of hypoglycemic agent | 0.4 | 7.80±0.45 |
As shown in Table 5, the hypoglycemic agent provided by the application can obviously reduce hyperglycemia caused by epinephrine in low, medium and high dose groups, and the effect is better than that of acarbose, so that the hypoglycemic agent containing rehmannia root extract provided by the application has good hypoglycemic effect, and has obvious dose-effect relationship on the hypoglycemic effect.
It should be noted that, in this document, the terms "comprises," "comprising," or any other variation thereof, are intended to cover a non-exclusive inclusion, such that a process, method, article, or apparatus that comprises a list of elements does not include only those elements but may include other elements not expressly listed or inherent to such process, method, article, or apparatus.
Although embodiments of the present application have been shown and described, it will be understood by those skilled in the art that various changes, modifications, substitutions and alterations can be made therein without departing from the principles and spirit of the application, the scope of which is defined in the appended claims and their equivalents.
Claims (10)
1. The preparation method of the hypoglycemic preparation containing the rehmannia root extract is characterized in that the hypoglycemic preparation is a film coated tablet containing the rehmannia root extract, and comprises the following steps in parts by weight:
s1, 1-2 parts of rehmannia root extract is dissolved in 10-15 parts of organic solvent, uniformly sprayed on 20-30 parts of crosslinked povidone, dried to obtain a mixture, uniformly mixed with 60-70 parts of filler and 1-2 parts of lubricant, and pressed into tablet cores;
s2, preheating the tablet cores in a rotary coating pot, and spraying 5-10 parts of coating liquid into a spray gun to obtain the tablet cores in the rotary coating pot;
the coating liquid consists of the following components in percentage by weight: 8-12% of modified polyvinyl alcohol; 8-12% of modified polyacrylic resin; 1-2% glycyrrhizin disodium; 0.5-0.8% shellac; the balance of deionized water;
the preparation method of the modified polyvinyl alcohol comprises the following steps: and adding polyvinyl alcohol into the dimethyl sulfoxide solution, heating to 95 ℃, stirring until the polyvinyl alcohol is dissolved, adding phthalic anhydride, and continuing to react for 4-6 hours to obtain the modified polyvinyl alcohol.
2. The method for preparing a hypoglycemic agent containing rehmannia root extract as claimed in claim 1, wherein the preparation method of the modified polyacrylic resin is as follows:
(1) Adding ethylene glycol and sodium hydride into anhydrous tetrahydrofuran, heating to 30-40 ℃ under the protection of nitrogen, reacting for 2-3h, adding chloromethyl vinyl benzene into the reaction solution, and continuing to react for 2-3h to obtain diene monomer;
(2) Adding methacrylic acid and diene monomer into 50-60% ethanol solution, heating to 70-80 ℃, dripping 30-40% potassium persulfate aqueous solution, and continuing to react for 6-8h after dripping to obtain the modified polyacrylic resin.
3. The method for preparing a hypoglycemic agent containing rehmannia root extract according to claim 2, wherein the molar ratio of ethylene glycol, chloromethyl vinyl benzene, sodium hydride in step (1) is 1:1.1-1.2:1.5-1.8.
4. The method for preparing a hypoglycemic agent containing rehmannia root extract as claimed in claim 2, wherein the molar ratio of methacrylic acid and diene monomer in the step (2) is 1:0.4-0.5; the dosage of the potassium persulfate is 0.6 to 0.8 percent of the mass of the methacrylic acid.
5. The method for preparing a hypoglycemic agent containing rehmannia root extract according to claim 1, wherein the mass ratio of polyvinyl alcohol to phthalic anhydride is 1:0.5-0.6.
6. The method for preparing a hypoglycemic agent containing rehmannia root extract as claimed in claim 1, wherein the preparation method of the rehmannia root extract in step S1 is as follows: oven drying rehmanniae radix, pulverizing, sieving with 40-70 mesh sieve to obtain rehmanniae radix powder, sequentially adding rehmanniae radix powder, cellulase and Tween 80 into solvent, soaking for 20-30min, microwave extracting for 3-5min, vacuum filtering, and concentrating the filtrate to obtain rehmanniae radix extract.
7. The method for preparing a hypoglycemic agent containing rehmannia root extract as claimed in claim 6, wherein the mass ratio of rehmannia root powder and solvent is 1:15-20; the dosage of the cellulase is 0.6-1.0g/L solvent; the dosage of the Tween 80 is 1.2-1.5g/L of solvent; the solvent is ethanol and water with the volume ratio of 1:1-2.
8. The method for preparing a hypoglycemic agent containing rehmannia root extract as claimed in claim 6, wherein the microwave extraction power is 400-600W, and the microwave extraction temperature is 60-80 ℃.
9. The method for preparing a hypoglycemic agent containing rehmannia root extract according to claim 1, wherein the organic solvent in step S1 is one or a mixture of several of acetonitrile, dichloromethane, chloroform, methanol and absolute ethanol; the filler is one or more of lactose, mannitol and sucrose; the lubricant is one or more of magnesium stearate, talcum powder and silicon dioxide.
10. A hypoglycemic preparation containing rehmannia root extract, characterized by being prepared by the method for preparing a hypoglycemic preparation containing rehmannia root extract according to any one of claims 1-9.
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Citations (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB857864A (en) * | 1956-10-04 | 1961-01-04 | Charles E Frost & Company | Solid dosage units having an enteric coating of a partially esterified polyvinyl alcohol |
| US20010036471A1 (en) * | 2000-03-29 | 2001-11-01 | Maximilian Angel | Hard capsules comprising polymers of vinyl esters and polyethers, their use and production |
| CN1879706A (en) * | 2006-05-16 | 2006-12-20 | 上海中药制药技术有限公司 | 'Shuang Huang Lian' dispersible tablet and preparation method thereof |
| CN104906160A (en) * | 2015-05-25 | 2015-09-16 | 昆明理工大学 | Enteric preparation of erigeron breviscapus extractive |
| CN106667933A (en) * | 2015-11-10 | 2017-05-17 | 天津汉瑞药业有限公司 | Tablet containing topiroxostat and preparation method thereof |
| CN115804802A (en) * | 2022-12-20 | 2023-03-17 | 杭州赫贝科技有限公司 | Application of euphorbia helioscopia volatile oil in medicine for treating bacterial enteritis |
-
2023
- 2023-08-29 CN CN202311097072.8A patent/CN116966159A/en active Pending
Patent Citations (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB857864A (en) * | 1956-10-04 | 1961-01-04 | Charles E Frost & Company | Solid dosage units having an enteric coating of a partially esterified polyvinyl alcohol |
| US20010036471A1 (en) * | 2000-03-29 | 2001-11-01 | Maximilian Angel | Hard capsules comprising polymers of vinyl esters and polyethers, their use and production |
| CN1879706A (en) * | 2006-05-16 | 2006-12-20 | 上海中药制药技术有限公司 | 'Shuang Huang Lian' dispersible tablet and preparation method thereof |
| CN104906160A (en) * | 2015-05-25 | 2015-09-16 | 昆明理工大学 | Enteric preparation of erigeron breviscapus extractive |
| CN106667933A (en) * | 2015-11-10 | 2017-05-17 | 天津汉瑞药业有限公司 | Tablet containing topiroxostat and preparation method thereof |
| CN115804802A (en) * | 2022-12-20 | 2023-03-17 | 杭州赫贝科技有限公司 | Application of euphorbia helioscopia volatile oil in medicine for treating bacterial enteritis |
Non-Patent Citations (1)
| Title |
|---|
| 王泽溟等: "侧链PEG基聚合物的制备及其催化酯化反应性能", 《化学通报》, vol. 82, no. 6, pages 542 - 548 * |
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