CN112843009B - Method for preparing phlorizin mixed hypoglycemic preparation - Google Patents
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Abstract
The invention discloses a method for preparing a phlorizin mixed hypoglycemic preparation, which comprises the steps of microencapsulating phlorizin and trilobatin, adding xylitol, microcrystalline cellulose, maltodextrin and magnesium stearate as auxiliary materials, and preparing tablets or capsules; the mass ratio of the phlorizin, the trilobatin, the xylitol, the microcrystalline cellulose, the maltodextrin and the magnesium stearate is 0.1:0.15-0.2:1-2:0.2-0.4:2-3: 0.2-0.5. The invention mixes the phlorizin and the trilobatin in an optimal proportion, and prepares an oral tablet or capsule administration preparation by combining a microcapsule process, plays the protection role of the trilobatin on the phlorizin, enables the phlorizin to be absorbed through intestinal tracts, inhibits SGLT from improving the medicine of glucose discharged from urine, and thus utilizes the new target point and a new mechanism to treat the type II diabetes.
Description
Technical Field
The invention relates to the technical field of medical health products, in particular to a phlorizin mixed hypoglycemic preparation and a preparation method thereof.
Background
SGLT (sodium-dependent glucose cotransporter) is a family of glucose transporters found in the intestinal mucosa of the small intestine (intestinal cells) and in the proximal tubule of the nephron. SGLT contributes to renal glucose reabsorption. In the kidney, 100% of the filtered glucose in the glomeruli must be reabsorbed along the nephron. In the case of excessive plasma glucose concentration (hyperglycemia), glucose is excreted in the urine because SGLT is saturated with filtered monosaccharides. Inhibition of SGLT2 results in a decrease in blood glucose levels. Therefore, SGLT2 inhibitors are useful for the treatment of type II diabetes.
Phlorizin dihydrate, also known as phloridzin, is known as 1- (2- (beta-D-glucopyranosyloxy) -4, 6-dihydroxyphenyl) -3- (4-hydroxyphenyl) -propanone, formula C21H24O 10) as a novel SGLT2 inhibitor, and prevents the absorption of glucose by the kidney, achieving the effect of lowering blood glucose levels by a non-insulin dependent mechanism. Before this, the medical community at home and abroad has made a lot of scientific research experiments on phlorizin, which has been successful greatly, and has published academic papers. In 2008, phlorizin was subject-specific studies and published in public by 6-person research teams composed of the University of regis (Rutgers University) and the Central University of North Carolina (North Carolina Central University). Professor of south China university points out that Dongfuqiang (root bark glycosides for preventing and treating diabetes mellitus): phlorizin specifically and competitively inhibits the transportation of glucose molecules by SGLT1 and SGTL2, promotes the secretion of glucose, and reduces fasting and postprandial blood glucose levels without hypoglycemic side effects. However, phlorizin, when administered orally, is hydrolyzed into phloretin and glucose by β -glucosidase in the intestinal tract, thereby losing its activity.
Trilobatin, namely Trilobatin, which is a main sweet component of tender leaves of lithocarpus polystachyus rehd, belongs to a natural sweetener with high sweetness and low calorie, and has the sweetness more than 300 times that of cane sugar. Has good inhibition effect on intestinal hydrolytic enzyme, and the safety of the intestinal hydrolytic enzyme is widely accepted.
In the lithocarpus polystachyus rehd plant slice, trilobatin and phlorizin have a certain transformation relation. Firstly, trilobatin is generated, then the content of the trilobatin is gradually reduced, the content of the phlorizin is gradually increased, and the content of the phlorizin is the largest in leaves with the leaf age of more than 6 months, and the content of the trilobatin is zero. Therefore, how to combine the phlorizin and trilobatin to prepare an oral administration preparation provides a new direction for treating the type II diabetes.
Disclosure of Invention
The invention aims to provide a phlorizin mixed hypoglycemic preparation and a preparation method thereof. The invention mixes the phlorizin and the trilobatin in an optimal proportion, and prepares an oral tablet or capsule administration preparation by combining a microcapsule process, plays the protection role of the trilobatin on the phlorizin, enables the phlorizin to be absorbed through intestinal tracts, inhibits SGLT from improving the medicine of glucose discharged from urine, and thus utilizes the new target point and a new mechanism to treat the type II diabetes.
In order to achieve the above purpose, the technical scheme adopted by the invention is as follows:
a method for preparing a phlorizin mixed hypoglycemic preparation comprises the following steps: firstly, carrying out microencapsulation treatment on phlorizin and trilobatin, adding xylitol, microcrystalline cellulose, maltodextrin and magnesium stearate as auxiliary materials, and preparing tablets or capsules; the mass ratio of the phlorizin, the trilobatin, the xylitol, the microcrystalline cellulose, the maltodextrin and the magnesium stearate is 0.1:0.15-0.2:1-2:0.2-0.4:2-3: 0.02-0.05;
the microencapsulation treatment comprises the following steps:
(1) crushing phlorizin and trilobatin into fine powder, adding the fine powder into water, adding mannan oligosaccharide and sucrose fatty acid glyceride into the water, and performing ultrasonic emulsification to prepare a core material system;
(2) uniformly mixing soybean lecithin, linseed gum and chitosan, adding the mixture into a core material system, and uniformly stirring, wherein the mass ratio of the mixture to the core material system is 1:3-5, so as to prepare a microcapsule mixed solution;
(3) and then carrying out reduced pressure concentration on the mixed solution to remove water, ultrasonically dispersing the obtained extract into a PBS buffer solution system containing polyvinylpyrrolidone, carrying out solid-liquid separation, collecting filtrate, carrying out freeze-drying treatment, and carrying out spray drying to finish microencapsulation treatment, thus obtaining the blood sugar reducing microcapsule.
Further, the mass ratio of the mannooligosaccharide to the sucrose fatty acid glyceride is 1:1-2, and the adding amount of the mannooligosaccharide and the sucrose fatty acid glyceride is 1-3% of the mass of the fine powder.
Further, the water is hot water with the temperature of 50-70 ℃, and the adding amount of the water is 5-7 times of the weight of the fine powder.
Further, the mass of the soybean lecithin, the flaxseed gum and the chitosan is 4-8:1-3: 1-3.
Further, the PBS buffer system pH =7.2, 0.3-0.5 mg polyvinylpyrrolidone per 1ml PBS buffer solution was added.
Further, the ultrasonic dispersion is ultrasonic dispersion at 50-70 ℃ for 20-30 min.
Further, the freeze-drying treatment is freeze-drying for 12-48h at the temperature of-10 to-30 ℃.
Another object of the present invention is to provide: the preparation method of the phlorizin hypoglycemic tablet comprises the following steps: mixing the blood sugar lowering microcapsule with magnesium stearate and microcrystalline cellulose, mixing with the rest raw materials in a multi-directional mixer for 10-30min to obtain dry extract powder, sieving, and sealing and packaging the obtained granules with double-layer polyethylene bag to obtain the phlorizin blood sugar lowering tablet.
Another object of the present invention is to provide: the preparation method of the phlorizin hypoglycemic capsule comprises the following steps: mixing the microcapsule with magnesium stearate and microcrystalline cellulose, mixing with the rest materials in a multi-directional mixer for 10-30min to obtain dry extract powder; and filling the dry paste powder into capsules according to the specification of 0.4g +/-10% of each capsule, polishing the filled capsules by using a capsule polishing machine, and wiping the capsules by using gauze and edible silicone oil to increase the surface smoothness to obtain the phlorizin hypoglycemic capsules.
Compared with the prior art, the invention has the advantages and beneficial effects that:
1. the invention mixes the phlorizin and the trilobatin in an optimal proportion, and prepares an oral tablet or capsule administration preparation by combining a microcapsule process, plays the protection role of the trilobatin on the phlorizin, enables the phlorizin to be absorbed through intestinal tracts, inhibits SGLT from improving the medicine of glucose discharged from urine, and thus utilizes the new target point and a new mechanism to treat the type II diabetes.
2. According to the invention, phlorizin and trilobatin are mixed with mannan oligosaccharide and sucrose fatty acid glyceride to prepare a core material system, and then the core material system is uniformly mixed with soybean lecithin, flaxseed gum and chitosan to prepare microcapsules, and the used auxiliary materials not only have the effects of emulsification, solubilization, dispersion, coating and the like, so that the stability, encapsulation rate and uniformity of the medicine are improved, and the quality guarantee period of the medicine is prolonged; the medicine also has a slow release effect, so that the medicine is slowly and stably released, the phlorizin medicine can be prevented from being inactivated in the intestinal tract, and the technical problem that the phlorizin is hydrolyzed into phloretin and glucose by beta-glucosidase in the intestinal tract so as to lose activity is better solved.
3. The method of the invention also disperses the mixed solution of the microcapsule to a PBS buffer solution system added with polyvinylpyrrolidone (PVP) by ultrasonic dispersion to form a better homogeneous system, which is beneficial to forming the microcapsule with good biocompatibility and better stability.
4. In the invention, xylitol, microcrystalline cellulose, maltodextrin and magnesium stearate are also added in the preparation of the phlorizin hypoglycemic tablet or capsule, which is beneficial to improving the uniformity, smoothness and stability of the medicine.
Drawings
FIG. 1 is a graph of hydrogen ion flow rate of beta cell mass of mice treated with different drugs;
FIG. 2 is a graph of potassium ion flow rate of mouse beta cell mass treated with different drugs;
FIG. 3 is a graph of calcium ion flux in mice treated with different drugs;
FIG. 4 is a graph of hydrogen ion flow rate of liver cell clusters of mice treated with different drugs.
In the figure: the mixing group is prepared by mixing phlorizin and trilobatin according to the proportion of 1: 1.5.
Detailed Description
The present invention will be described in further detail with reference to specific embodiments. It should be emphasized that the following description is merely exemplary in nature and is not intended to limit the scope of the invention or its application.
The phlorizin and trilobatin used in the invention are commercially available products, the particle size is 100 meshes, and the purity is more than or equal to 98%.
Example 1
A method for preparing a phlorizin mixed hypoglycemic preparation comprises the following steps: microencapsulating phlorizin and trilobatin, adding xylitol, microcrystalline cellulose, maltodextrin and magnesium stearate as adjuvants, and making into tablet or capsule. The mass ratio of the phlorizin to the trilobatin to the xylitol to the microcrystalline cellulose to the maltodextrin to the magnesium stearate is 0.1:0.15:1.5:0.3:2.7: 0.03.
The microencapsulation treatment comprises the following steps:
(1) crushing phlorizin and trilobatin into fine powder, sieving with a 100-mesh sieve, adding 60 ℃ warm water 5 times of the fine powder, adding mannooligosaccharide 1% of the mass of the fine powder and sucrose fatty acid glyceride 1.5% of the mass of the fine powder, and performing ultrasonic emulsification for 20min to prepare a core material system;
(2) uniformly mixing soybean lecithin, linseed gum and chitosan in a mass ratio of 6:2:1, adding the mixture into a core material system, and uniformly stirring to prepare a microcapsule mixed solution, wherein the mass ratio of the mixture to the core material system is 1: 4;
(3) and then carrying out reduced pressure concentration on the mixed solution to remove water, ultrasonically dispersing the obtained extract into a PBS (phosphate buffer solution) system containing polyvinylpyrrolidone (pH =7.2, 0.5 mg of polyvinylpyrrolidone is added into every 1ml of PBS buffer solution), ultrasonically dispersing for 20min at the temperature of 60 ℃, filtering, carrying out solid-liquid separation, collecting filtrate, freeze-drying the filtrate at the temperature of-25 ℃ for 24h, and carrying out spray drying until the water content is reduced to be below 5%, thus completing microencapsulation treatment and obtaining the blood glucose reducing microcapsule.
Example 2
A method for preparing a phlorizin mixed hypoglycemic preparation comprises the following steps: microencapsulating phlorizin and trilobatin, adding xylitol, microcrystalline cellulose, maltodextrin and magnesium stearate as adjuvants, and making into tablet or capsule. The mass ratio of the phlorizin, the trilobatin, the xylitol, the microcrystalline cellulose, the maltodextrin and the magnesium stearate is 0.1:0.17:2:0.4:2.3: 0.05.
The microencapsulation treatment comprises the following steps:
(1) crushing phlorizin and trilobatin into fine powder, sieving with a 100-mesh sieve, adding warm water at 70 ℃ 6 times of the fine powder, adding mannan-oligosaccharide 0.9% of the mass of the fine powder and sucrose fatty acid glyceride 0.9%, and performing ultrasonic emulsification for 30min to obtain a core material system;
(2) uniformly mixing soybean lecithin, linseed gum and chitosan in a mass ratio of 8:2:2, adding the mixture into a core material system, uniformly stirring, and preparing a microcapsule mixed solution, wherein the mass ratio of the mixture to the core material system is 1: 3;
(3) and then carrying out reduced pressure concentration on the mixed solution to remove water, ultrasonically dispersing the obtained extract into a PBS (phosphate buffer solution) system containing polyvinylpyrrolidone (pH =7.2, 0.4 mg of polyvinylpyrrolidone is added into every 1ml of PBS buffer solution), ultrasonically dispersing for 20min at the temperature of 70 ℃, filtering, carrying out solid-liquid separation, collecting filtrate, freeze-drying the filtrate at the temperature of-15 ℃ for 36h, and carrying out spray drying until the water content is reduced to be below 5%, thus completing microencapsulation treatment and obtaining the blood glucose reducing microcapsule.
Example 3
A method for preparing a phlorizin mixed hypoglycemic preparation comprises the following steps: microencapsulating phlorizin and trilobatin, adding xylitol, microcrystalline cellulose, maltodextrin and magnesium stearate as adjuvants, and making into tablet or capsule. The mass ratio of the phlorizin, the trilobatin, the xylitol, the microcrystalline cellulose, the maltodextrin and the magnesium stearate is 0.1:0.20:1.5:0.5:2.5: 0.04.
The microencapsulation treatment comprises the following steps:
(1) pulverizing phlorizin and trilobatin into fine powder, sieving with 100 mesh sieve, adding 7 times of 70 deg.C warm water, adding 0.5% of mannooligosaccharide and 1.0% of sucrose fatty acid glyceride by weight of fine powder, and ultrasonic emulsifying for 20min to obtain core material system;
(2) uniformly mixing soybean lecithin, linseed gum and chitosan in a mass ratio of 6:3:1, adding the mixture into a core material system, and uniformly stirring to prepare a microcapsule mixed solution, wherein the mass ratio of the mixture to the core material system is 1: 5;
(3) and then carrying out reduced pressure concentration on the mixed solution to remove water, ultrasonically dispersing the obtained extract into a PBS (phosphate buffer solution) buffer solution system containing polyvinylpyrrolidone (pH =7.2, 0.5 mg of polyvinylpyrrolidone is added into every 1ml of PBS buffer solution), carrying out ultrasonic dispersion at the temperature of 60 ℃ for 30min, filtering, carrying out solid-liquid separation, collecting filtrate, freeze-drying the filtrate at the temperature of-20 ℃ for 36h, and carrying out spray drying until the water content is reduced to below 5%, thus completing microencapsulation treatment and obtaining the blood sugar reducing microcapsule.
The blood sugar reducing microcapsules prepared in the embodiments 1-3 are used for preparing phlorizin blood sugar reducing tablets, and the preparation method comprises the following steps: mixing the blood sugar lowering microcapsule with magnesium stearate and microcrystalline cellulose, mixing with the rest raw materials in a multi-directional mixer for 20min to obtain dry extract powder, sieving, and packaging the obtained granules with a double-layer polyethylene bag to obtain phlorizin blood sugar lowering tablet with content of 0.3 g.
The blood sugar reducing microcapsules prepared in the embodiments 1 to 3 are used for preparing the phlorizin blood sugar reducing capsules, and the preparation method comprises the following steps: mixing the microcapsule with magnesium stearate and microcrystalline cellulose, mixing with the rest materials in a multi-directional mixer for 20min to obtain dry extract powder; and filling the dry paste powder into capsules according to the specification of 0.4g +/-10% of each capsule, polishing the filled capsules by using a capsule polishing machine, and wiping the capsules by using gauze and edible silicone oil to increase the surface smoothness to obtain the phlorizin hypoglycemic capsules.
Comparative example 1
Weighing phlorizin, trilobatin, xylitol, microcrystalline cellulose, maltodextrin and magnesium stearate in a mass ratio of 0.1:0.17:2:0.4:2.3:0.05, uniformly mixing the phlorizin and the trilobatin with the magnesium stearate and the microcrystalline cellulose, placing the mixture and the rest raw materials in a multidirectional motion mixer, mixing for 20min to obtain dry paste powder, sieving, sealing and packaging the obtained granules by using a double-layer polyethylene bag to obtain the phlorizin hypoglycemic tablet, wherein the content of each tablet is 0.3 g.
Comparative example 2
Weighing phlorizin, trilobatin, xylitol, microcrystalline cellulose, maltodextrin and magnesium stearate in a mass ratio of 0.1:0.17:2:0.4:2.3: 0.05; mixing phlorizin and trilobatin with magnesium stearate and microcrystalline cellulose uniformly, placing the mixture and the rest raw materials in a multidirectional motion mixer, and mixing for 20min to obtain dry paste powder; and filling the dry paste powder into capsules according to the specification of 0.4g +/-10% of each capsule, polishing the filled capsules by using a capsule polishing machine, and wiping the capsules by using gauze and edible silicone oil to increase the surface smoothness to obtain the phlorizin hypoglycemic capsules.
Test for lowering blood sugar
Diabetes mellitus is a complex disease caused by lack of insulin secretion or insulin resistance or combined action, and solving insulin secretion from the root is the expected target of us. The insulin secretion is regulated by various ions, and the NMT technology is used for detecting the beta cell H of the mouse + 、K + 、 Ca 2+ Plasma and liver cells H + The dynamic change process of ions and Glucose and the experimental results are respectively shown in the attached figures 1-4, and it can be seen from the figures that the blood sugar reducing effect of the mixture of phlorizin and trilobatin is obviously higher than that of phlorizin and trilobatin.
Testing of drug Release, encapsulation efficiency and stability
The phlorizin hypoglycemic tablets and phlorizin hypoglycemic capsules prepared in the above examples and comparative examples are tested by a pulp method according to a 2015 release degree measuring method and a second method, wherein the testing conditions are that samples are taken at 37 +/-0.5 ℃ and a rotating speed of 50r/min for 10min, 30min, 60min and 120min respectively, and the measuring results are shown in table 1; and calculating the encapsulation rate according to the content of phlorizin in the tablet or the capsule; the stability test is carried out by placing the tablet or capsule in a stability test chamber, carrying out an accelerated test for 6 months at a temperature of 50 ℃. + -. 2 ℃ and a relative humidity of 75%. + -. 5%, and examining according to the moisture detection method of the appendix of the first part of the 'Chinese pharmacopoeia' 2015 edition, wherein the measurement results are shown in Table 2.
Table 1: the result of measuring the sustained release degree of the phlorizin hypoglycemic preparation
Table 2: encapsulation efficiency and stability determination result of phlorizin hypoglycemic preparation
The determination results show that the phlorizin hypoglycemic preparation prepared by the invention has slow and stable release, can prevent the phlorizin drug from being inactivated in intestinal tracts, has higher encapsulation efficiency and good stability, and can improve the stability and the quality guarantee period of the drug.
The foregoing is a more detailed description of the invention in connection with specific/preferred embodiments and is not intended to limit the practice of the invention to those descriptions. It will be apparent to those skilled in the art that various substitutions and modifications can be made to the described embodiments without departing from the spirit of the invention, and such substitutions and modifications are to be considered as within the scope of the invention.
Claims (4)
1. A method for preparing a phlorizin mixed hypoglycemic preparation is characterized by comprising the following steps: microencapsulating phlorizin and trilobatin, adding xylitol, microcrystalline cellulose, maltodextrin and magnesium stearate as adjuvants, and making into tablet or capsule; the mass ratio of the phlorizin, the trilobatin, the xylitol, the microcrystalline cellulose, the maltodextrin and the magnesium stearate is 0.1:0.15-0.2:1-2:0.2-0.4:2-3: 0.02-0.05;
the microencapsulation treatment comprises the following steps:
(1) crushing phlorizin and trilobatin into fine powder, adding the fine powder into water, adding mannan oligosaccharide and sucrose fatty acid glyceride into the water, and performing ultrasonic emulsification to prepare a core material system;
(2) uniformly mixing soybean lecithin, linseed gum and chitosan, adding the mixture into a core material system, and uniformly stirring, wherein the mass ratio of the mixture to the core material system is 1:3-5, so as to prepare a microcapsule mixed solution;
(3) performing reduced pressure concentration on the mixed solution to remove water, performing ultrasonic dispersion on the obtained extract into a PBS buffer solution system containing polyvinylpyrrolidone, performing solid-liquid separation, collecting filtrate, performing freeze-drying treatment, and performing spray drying to complete microencapsulation treatment to obtain the blood sugar reducing microcapsule;
the mass ratio of the manna oligosaccharide to the sucrose fatty acid glyceride is 1:1-2, and the adding amount of the manna oligosaccharide and the sucrose fatty acid glyceride is 1-3% of the mass of the fine powder;
the water is hot water with the temperature of 50-70 ℃, and the adding amount of the water is 5-7 times of the weight of the fine powder;
the mass of the soybean lecithin, the flaxseed gum and the chitosan is 4-8:1-3: 1-3;
the PBS buffer system had pH =7.2, and 0.3-0.5 mg polyvinylpyrrolidone was added per 1ml PBS buffer.
2. The method for preparing a phlorizin mixed hypoglycemic agent according to claim 1, characterized in that: the ultrasonic dispersion is carried out at 50-70 deg.C for 20-30 min.
3. The method for preparing a phlorizin mixed hypoglycemic agent according to claim 1, characterized in that: the freeze-drying treatment is freeze-drying for 12-48h at the temperature of-10 to-30 ℃.
4. The method for preparing a phlorizin mixed hypoglycemic agent according to any one of claims 1 to 3, characterized in that: the preparation method of the phlorizin hypoglycemic capsule comprises the following steps: mixing the microcapsule with magnesium stearate and microcrystalline cellulose, mixing with the rest materials in a multi-directional mixer for 10-30min to obtain dry extract powder; and filling the dry paste powder into capsules according to the specification of 0.4g +/-10% of each capsule, polishing the filled capsules by using a capsule polishing machine, and wiping the capsules by using gauze and edible silicone oil to increase the surface smoothness to obtain the phlorizin hypoglycemic capsules.
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