CN113476418A - Subcutaneous implanted rod for long-acting blood pressure reduction and preparation method thereof - Google Patents
Subcutaneous implanted rod for long-acting blood pressure reduction and preparation method thereof Download PDFInfo
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
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- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
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- A61K9/2004—Excipients; Inactive ingredients
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- A61K9/2027—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
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Abstract
The invention discloses a subcutaneous implanted rod for long-acting blood pressure reduction and a preparation method thereof, wherein a diblock copolymer is adopted as a carrier, and the formula comprises the following substances in parts by weight: 10-20 parts of polycaprolactone, 5-10 parts of polyethylene glycol, 1-5 parts of polyvinylpyrrolidone and 5-20 parts of bulk drug; the raw material medicine is formed by combining perindopril and amlodipine, wherein the perindopril is as follows by mass ratio: 1-20: 1 of amlodipine; the embedded bar is directly used for treating stable blood pressure by long-term sustained release administration after being implanted under the skin, and the diblock copolymer is used as a carrier, so that the problem of short action time of the existing embedded bar is solved, and the embedded bar has the advantages of simple preparation method, easily obtained materials, simple production process and easy mastering; the embedded bar prepared by the invention is implanted into the subcutaneous part of a human body, has complete degradability according to biological materials, good biocompatibility and nontoxicity, and good subcutaneous comfort degree.
Description
Technical Field
The invention relates to a subcutaneous implanted rod for long-acting blood pressure reduction and a preparation method thereof.
Background
At present, the treatment of primary hypertension at home and abroad depends on the maintenance of normal and balanced blood pressure by oral antihypertensives. The drug has short action time, and the drug is orally taken three times or two times a day. The oral large-dosage antihypertensive drug has large side effect, causes systemic and gastrointestinal reaction and great damage to liver and kidney functions.
The traditional Chinese medicine catgut embedding therapy is adopted for treating hypertension, but the catgut embedding treatment effect is not obvious, and the effect of stabilizing the blood pressure for a long time cannot be achieved.
Disclosure of Invention
Aiming at the technical defects, the invention aims to provide a subcutaneous implanted rod for long-acting blood pressure reduction and a preparation method thereof, so as to solve the problems in the background technology.
In order to solve the technical problems, the invention adopts the following technical scheme:
the invention provides a subcutaneous implanted rod for long-acting blood pressure reduction, which adopts diblock copolymer as a carrier and comprises the following substances in parts by weight:
10-20 parts of Polycaprolactone (PCL),
5-10 parts of polyethylene glycol,
1-5 parts of polyvinylpyrrolidone, namely, polyvinylpyrrolidone,
5-20 parts of raw material medicine;
the raw material medicine is formed by combining perindopril and amlodipine, wherein the mass ratio of perindopril to amlodipine is 1-20: 1.
Preferably, the mass ratio of perindopril to amlodipine is 1: 1.
Preferably, the subcutaneous implanted rod for long-acting blood pressure reduction comprises the following substances in parts by weight:
10 parts of polycaprolactone;
5 parts of polyethylene glycol;
2 portions of polyvinylpyrrolidone
10 parts of raw material medicine;
the raw material medicine comprises the following components:
5 parts of perindopril;
5 parts of amlodipine;
preferably, the diameter of the embedded rod is 1-3mm, and the length of the embedded rod is 25-50 mm.
Preferably, the diameter of the embedded rod is 3mm, and the length of the embedded rod is 50 mm.
A preparation method of a subcutaneous implanted rod for long-acting blood pressure reduction comprises the following steps:
step 1: preparing a PCL-PEG-diblock copolymer micelle: polyethylene glycol (PEG) is used as a macroinitiator, Polycaprolactone (PCL) is used as a monomer, and a toxic metal catalyst is avoided, so that a PCL-PEG-diblock copolymer is prepared;
step 2: preparing a carrier for embedding the rod: heating and melting the diblock copolymer micelle prepared in the step 1 into paste, adding the polyvinyl pioglitazone PVP in parts for hygroscopicity, heating, rotating and stirring for sufficient mixing, adding perindopril and amlodipine serving as raw material medicaments in parts, rotating and stirring for sufficient mixing, encapsulating the copolymer micelle with the raw material medicaments to form a microsphere capsule, cooling to form a solid, crushing the mixture by a crusher in sequence, granulating in a granulator, heating and extruding for molding by an extruder, extruding cylindrical strips with the diameter of 1-3mm, placing and drying the extruded cylindrical strips, cutting the cylindrical strips according to the length of 25-50mm, carrying out vacuum packaging, and carrying out irradiation sterilization by cobalt 60 for later use.
Preferably, in step 1, the step of initiating ring-opening polymerization of PCL by PEG comprises:
adding polycaprolactone and polyethylene glycol into a reaction kettle, sealing the reaction kettle, vacuumizing, heating and stirring for 4-6 hours under the protection of nitrogen, opening a reaction kettle cover, adding polyvinylpyrrolidone PVP according to a certain proportion, continuing heating and stirring for 4-6 hours, stopping heating and stirring, opening the reaction kettle cover, naturally cooling, taking out, and drying to obtain the PCL-PEG-diblock copolymer.
The heating and stirring temperature is 100-150 ℃, and the heating temperature of the extruder is 60-80 ℃.
And packaging the vacuum packages according to 4-6 packages per package.
The use method of the embedded bar of the invention comprises the following steps:
1. the embedding rod is embedded subcutaneously at the acupuncture point of Qingling on the inner side of the upper arm and is used for treating and stabilizing the normal blood pressure of primary hypertension.
2. The dosage is as follows: burying 6-12 subcutaneous tissue at one time, wherein the weight of each burying rod is 0.1-0.3 g.
Maladaptive symptoms: the embedded rod of the invention is not suitable for patients with secondary hypertension.
Compared with the prior art, the invention has the beneficial effects that:
1. the invention adopts diblock copolymer as carrier to solve the problems of short action time and burst release of drug of the prior embedded bar carrier, and has the advantages of simple preparation method, easily obtained materials, simple production process and easy control.
2. The embedded bar prepared by the invention is implanted under the skin of a human body, and the material has complete degradability according to the biodegradation performance, good biocompatibility and nontoxicity, and good subcutaneous comfort level of the human body.
3. The polycaprolactone monomer is heated and vacuumized by polyethylene glycol to initiate ring-opening polymerization under the protection of nitrogen, and graft is generated by in-situ compatibilization, so that the composite mechanical property and the thermal property of the polyester base are improved, the application range of the polyester base is expanded, the polyester base is suitable for being applied to biological tissue engineering, the ring-opening polymerization of polycaprolactone is realized, and the safety and the compatibility of the PCL-PEG copolymer which is used as a biomedical material and acts on a human body are considered.
4. The invention relates to an embedded bar prepared according to the principle of subcutaneous slow-release administration, which is implanted into the subcutaneous part of a human body after being sterilized by cobalt 60 irradiation, and is slowly degraded by taking a diblock copolymer as a carrier to play a role in stabilizing blood pressure for long-term treatment, and the medicament is released after the degradation of a degradation material is finished, and finally is converted into carbon dioxide and water in the body to be absorbed by human tissues and finally discharged out of the body without generating any by-product.
Detailed Description
The present invention will be described in further detail with reference to examples.
The invention discloses a subcutaneous implanted rod for long-acting blood pressure reduction, which is implanted subcutaneously for realizing the purpose of long-term blood pressure stabilization and comprises the following substances in parts by weight: 10-20 parts of polycaprolactone, 5-10 parts of polyethylene glycol, 1-5 parts of polyvinylpyrrolidone and 5-20 parts of bulk drug; the parts herein may be expressed in mg, g, kg, without limitation to the unit. Among them, the polyethylene glycol used preferably has a molecular weight of 400.
The drug substance is formed by combining perindopril and amlodipine, wherein the mass ratio of perindopril to amlodipine is 1: 1, and the ratio is the optimal ratio in the application of the embedded bar.
The specific composition of the embedded rod may be any value within the above range of raw materials, for example, it is preferable that: 10 parts of polycaprolactone, 5 parts of polyethylene glycol and 2 parts of polyvinylpyrrolidone, wherein the raw material medicines comprise 5 parts of perindopril and 5 parts of amlodipine. The above-mentioned ratio is merely a preferable example, but the embedded rod prepared by the present invention is not limited to this formulation.
The invention adopts the micelle of the diblock copolymer to prepare the drug carrier of the embedded rod, in particular to a preparation method of the subcutaneous embedded rod for long-acting blood pressure reduction, which comprises the following steps:
step 1: preparation of polycaprolactone diblock copolymer micelle: the ring-opening polymerization of polycaprolactone is initiated by polyethylene glycol. The ring-opening polymerization of polycaprolactone, and considering the safety and compatibility of the PCL-PEG copolymer as a biomedical material when acting on a human body, the polyethylene glycol PEG is directly used as a macroinitiator and the polycaprolactone PCL is used as a monomer in the laboratory, and the PCL-PEG-diblock copolymer is successfully prepared by avoiding using a toxic metal catalyst due to the application of the PCL-PEG copolymer to the human body. Preparing a PCL-PEG-diblock copolymer micelle: adding polycaprolactone and polyethylene glycol into a reaction kettle, sealing the reaction kettle, vacuumizing, heating and stirring for 4-6 hours under the protection of nitrogen, opening a reaction kettle cover, adding polyvinylpyrrolidone PVP (polyvinyl pyrrolidone) in a certain proportion for moisture absorption, continuously heating and stirring for 4-6 hours, stopping heating and stirring, opening the reaction kettle cover, naturally cooling, taking out, and drying to obtain the PCL-PEG-diblock copolymer.
Step 2: preparing a buried planting rod: heating and melting the diblock copolymer micelle prepared in the step 1 into paste, adding perindopril and amlodipine serving as raw material medicines, rotating and stirring the mixture fully under heating, encapsulating the copolymer micelle with the raw material medicines to form a microsphere capsule, cooling the microsphere capsule to form a solid, crushing the mixture by a crusher in sequence, granulating the mixture in a granulator, heating an extruder to extrude the mixture to form a cylindrical strip with the diameter of 1-3mm, placing and drying the extruded cylindrical strip, cutting the cylindrical strip according to the length of 25-50mm, carrying out vacuum packaging, and carrying out irradiation sterilization by cobalt 60 for later use.
Example 1
The diameter of the embedded bar produced by the formula of the embodiment is 3mm, the length of the embedded bar is 50mm, the weight of each embedded bar is 300mg, and each embedded bar contains 100mg of raw material medicines.
Specifically, the subcutaneous implanted rod for long-acting blood pressure reduction comprises the following components in percentage by weight: 10g of polycaprolactone, 5g of polyethylene glycol, 2g of polyvinylpyrrolidone, 5g of perindopril, 5g of amlodipine, 27g of total weight and 300mg of amlodipine, wherein about 90 pieces are prepared.
The preparation process of the embedded bar comprises the following steps:
step 1: preparation of polycaprolactone diblock copolymer micelle: the ring-opening polymerization of polycaprolactone is initiated by polyethylene glycol. The ring-opening polymerization of polycaprolactone, and considering the safety and compatibility of the PCL-PEG copolymer as a biomedical material when acting on a human body, the polyethylene glycol PEG is directly used as a macroinitiator and the polycaprolactone PCL is used as a monomer in the laboratory, and the PCL-PEG-diblock copolymer is successfully prepared by avoiding using a toxic metal catalyst due to the application of the PCL-PEG copolymer to the human body. Preparing a PCL-PEG-diblock copolymer micelle: adding polycaprolactone and polyethylene glycol into a reaction kettle, sealing the reaction kettle, vacuumizing, heating and stirring for 4-6 hours under the protection of nitrogen, wherein the heating and stirring temperature is 100-150 ℃, opening the cover of the reaction kettle, adding polyvinylpyrrolidone (PVP) according to a certain proportion, continuously heating and stirring for 4-6 hours, stopping heating and stirring, opening the cover of the reaction kettle, naturally cooling, taking out, and drying to obtain the PCL-PEG-diblock copolymer.
Step 2: preparing a buried planting rod: heating and melting the diblock copolymer micelle prepared in the step 1 into paste, adding perindopril and amlodipine serving as raw material medicines according to the weight, heating, rotating and stirring for full mixing, encapsulating the copolymer micelle with the raw material medicines to form a microsphere capsule, cooling to form a solid, sequentially crushing the mixture by a crusher, granulating in a granulator, adding a heating extruder for extrusion molding, extruding cylindrical strips with the diameter of 1-3mm, placing and drying the extruded cylindrical strips, cutting the cylindrical strips according to the length of 25-50mm, vacuum packaging, and irradiating and sterilizing by cobalt 60 for later use.
Example 2
The diameter of the embedded bar is 3mm, the length of the embedded bar is 25mm, the weight of each embedded bar is 15mg, and the content of the raw material medicines in each embedded bar is 50 mg.
The specific formula of the embodiment is as follows: 10g of polycaprolactone, 7g of polyethylene glycol, 3g of polyvinylpyrrolidone, 10g of perindopril, 10g of amlodipine, 40g of total weight and 300mg of amlodipine, wherein the total weight is about 133.
The preparation method of this example is the same as example 1.
Example 3
The diameter of the embedded bar is 3mm, the length of the embedded bar is 50mm, the weight of each embedded bar is 300mg, and the content of the raw material medicines in each embedded bar is 100 mg.
The specific formula of the embodiment is as follows: 20g of polycaprolactone, 10g of polyethylene glycol, 2g of polyvinylpyrrolidone, 10g of perindopril, 10g of amlodipine, 52g of total weight, 300mg of each piece and about 173 pieces of amlodipine.
The preparation method of this example is the same as example 1.
The implementation steps of the embedded rod prepared in the above embodiment are as follows:
1) the patient takes the seat and sits on the upper arm with the acupuncture point on the inner side of the upper arm cleaned for conventional local disinfection and local subcutaneous anesthesia.
2) The needle point of a 34# stainless steel sleeve needle is obliquely penetrated into the subcutaneous part at an angle of 25 degrees, the length of the needle point is equal to the length of an embedding rod when the needle point enters the subcutaneous part, a needle core in a steel sleeve needle is pulled out, then the embedding rod is put into the needle from the tail part of the needle tube along the needle tube, the needle core is pushed to the subcutaneous part to complete an embedding process, 6-12 embedding rods are implanted into the subcutaneous part according to the method, and then an alcohol cotton ball is used for pressing the needle hole and fixing the needle hole by using a band-aid.
The clinical verification of the invention is illustrated by typical cases, the invention is embedded in the subcutaneous tissue of acupuncture points of a human body, and the polycaprolactone is slowly degraded to play the long-term pharmacological action, so as to achieve the aim of stabilizing the blood pressure for a long time.
Typical cases
Case 1: in a certain period, male, 61 years old, people in Zhou Kou City of Henan province suffer from hypertension for 10 years, the blood pressure is 160-.
Case 2: zhang Yi, Man, Han, age, 51 years old, Henan province Zhou kou city people, hypertension for 15 years, taking amlodipine and metoprolol at ordinary times, after implantation blood pressure of 130-80mm/Hg, patients feel good.
Case 3: the hypertension is affected for 10 years by some Wang, male, Han, people of the province Zhou city of Henan, the age of 40 years, the blood pressure is 180 mm/Hg at ordinary times, and the patient feels good after being buried by about 130-80 mm/Hg.
The invention relates to an embedded bar prepared according to the principle of subcutaneous slow-release administration, which is implanted into the subcutaneous part of a human body after being sterilized by cobalt 60 irradiation, and is slowly degraded by taking a diblock copolymer as a carrier to play a role in stabilizing blood pressure for long-term treatment, and the medicament is released after the degradation of a degradation material is finished, and finally is converted into carbon dioxide and water in the body to be absorbed by human tissues and finally discharged out of the body without generating any by-product.
The embedded rod prepared by the invention is detected to have no cytotoxicity and good biocompatibility, and is an ideal human subcutaneous administration carrier implantation material.
The implantation rod prepared by the invention is tested by rats, 12 rats with hypertension are selected, the 12 rats are divided into three groups, each group comprises 4 rats, and the animal numbers corresponding to the three groups of rats are respectively as follows: 1M01, 1M02, 1M03, 1M 04; 2M01, 2M02, 2M03, 2M 04; 3M01, 3M02, 3M03, 3M 04; 4M01, 4M02, 4M03, 4M 04; the treatment experiment was conducted by respectively carrying out the long-term sustained release administration of the drugs to 3 groups of rats according to examples 1 to 3 of the present invention and the corresponding treatment methods, and the systolic pressure and the diastolic pressure of the rats were measured on days 0, 3, 5, 7, 11, 14, 23, 28, 32, 39, 46, 53, 60, 67, 74, 81, and 88 during the treatment, respectively, and the detailed measurement data are shown in tables 1 to 17;
TABLE 1 measurement data of day 0 of blood pressure change after embedding
TABLE 2 measurement data of day 3 of blood pressure change after embedding
TABLE 3 measurement data on day 5 of blood pressure change after embedding
TABLE 4 measurement data on day 7 of blood pressure change after embedding
TABLE 5 measurement data on day 11 of blood pressure change after embedding
TABLE 6 measurement data of 14 th day of blood pressure change after embedding
TABLE 7 measurement data of 23 rd day of blood pressure change after embedding
TABLE 8 measurement data of 28 th day of blood pressure change after embedding
32 nd day measurement data of blood pressure change after being embedded in table 9
Blood pressure change measurement data on day 39 after table 10 is embedded
46 th day measurement data of blood pressure change after table 11 is buried
53 th day measurement data of blood pressure change after table 12 is embedded
60 th day measurement data of blood pressure change after table 13 is embedded
67 th day measurement data of blood pressure change with embedded meter 14
74 th day measurement data of blood pressure change after table 15 is embedded
81 st day measurement data of blood pressure change with embedded table 16
88 th day measurement data of blood pressure change after table 17 is buried
The results are shown in tables 1-17, and the blood pressure of the rats in the three groups is stable and normal after the rats are treated by the long-term sustained release drug. The above experimental results show that the implanted rod of the invention has the function of stabilizing blood pressure after long-term sustained-release drug administration to treat rats.
It will be apparent to those skilled in the art that various changes and modifications may be made in the present invention without departing from the spirit and scope of the invention. Thus, if such modifications and variations of the present invention fall within the scope of the claims of the present invention and their equivalents, the present invention is also intended to include such modifications and variations.
Claims (9)
1. A subcutaneous implanted rod for long-acting blood pressure reduction is characterized in that a diblock copolymer is adopted as a carrier, and comprises the following substances in parts by weight:
10-20 parts of Polycaprolactone (PCL),
5-10 parts of polyethylene glycol,
1-5 parts of polyvinylpyrrolidone, namely, polyvinylpyrrolidone,
5-20 parts of raw material medicine;
the raw material medicine is formed by combining perindopril and amlodipine, and the mass ratio of perindopril to amlodipine in the raw material medicine is 1-20: 1.
2. The subcutaneous implanted rod for long-acting blood pressure reduction according to claim 1,
the mass ratio of perindopril to amlodipine is 1: 1.
3. The subcutaneous implanted rod for long-acting blood pressure reduction according to claim 1, which comprises the following substances in parts by weight:
10 parts of polycaprolactone;
5 parts of polyethylene glycol;
2 portions of polyvinylpyrrolidone
10 parts of raw material medicine;
the raw material medicine comprises the following components:
5 parts of perindopril;
and 5 parts of amlodipine.
4. The subcutaneous implanted rod for long-acting blood pressure reduction according to claim 1, wherein the implanted rod has a diameter of 1-3mm and a length of 25-50 mm.
5. The subcutaneous implanted rod for long-acting blood pressure reduction according to claim 1, wherein the implanted rod has a diameter of 3mm and a length of 50 mm.
6. A preparation method of a subcutaneous implanted rod for long-acting blood reduction is characterized by comprising the following steps:
step 1: preparing a PCL-PEG-diblock copolymer micelle: polyethylene glycol (PEG) is used as a macroinitiator, Polycaprolactone (PCL) is used as a monomer, and a toxic metal catalyst is avoided, so that a PCL-PEG-diblock copolymer is prepared;
step 2: preparing a buried planting rod: heating and melting the diblock copolymer micelle prepared in the step 1 into paste, adding the polyvinyl pioglitazone PVP in parts for hygroscopicity, heating, rotating and stirring for sufficient mixing, adding the raw material medicines perindopril and amlodipine according to the weight parts, rotating and stirring for sufficient mixing, encapsulating the copolymer micelle with the raw material medicines to form a microsphere capsule, cooling to form a solid, crushing the mixture by a crusher in sequence, granulating in a granulator, heating and extruding for molding by an extruder, extruding cylindrical strips with the diameter of 1-3mm, placing and drying the extruded cylindrical strips, cutting the cylindrical strips according to the length of 25-50mm, carrying out vacuum packaging, and carrying out irradiation sterilization by cobalt 60 for later use.
7. The method for preparing the subcutaneous implanted rod for long-acting blood pressure reduction according to claim 6, wherein in the step 1, the ring-opening polymerization reaction of PCL initiated by PEG comprises the following specific steps:
adding polycaprolactone and polyethylene glycol into a reaction kettle, sealing the reaction kettle, vacuumizing, heating and stirring for 4-6 hours under the protection of nitrogen, opening a reaction kettle cover, adding polyvinylpyrrolidone PVP according to a certain proportion, continuing heating and stirring for 4-6 hours, stopping heating and stirring, opening the reaction kettle cover, naturally cooling, taking out, and drying to obtain the PCL-PEG-diblock copolymer.
8. The method as claimed in claim 7, wherein the heating and stirring temperature is 100-150 ℃ and the temperature of the extruder is 60-80 ℃.
9. The method for preparing subcutaneous implanted rod for long-acting blood pressure reduction according to claim 6, wherein the vacuum package is packed by 4-6 pieces per package.
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
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| CN114903861A (en) * | 2022-05-13 | 2022-08-16 | 吕汇川 | Biodegradable subcutaneous implanted rod for long-acting blood fat reduction and preparation method thereof |
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2021
- 2021-08-13 CN CN202110931998.7A patent/CN113476418A/en active Pending
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| Publication number | Priority date | Publication date | Assignee | Title |
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| CN108743955A (en) * | 2018-06-26 | 2018-11-06 | 吕鹏威 | One kind being used for essential hypertension elastomer subdermal implantation stick |
Non-Patent Citations (1)
| Title |
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| 李志良: "《卫生与健康生活忠告》", 30 June 2017, 江西科学技术出版社 * |
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| CN114903861A (en) * | 2022-05-13 | 2022-08-16 | 吕汇川 | Biodegradable subcutaneous implanted rod for long-acting blood fat reduction and preparation method thereof |
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