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CN114601916B - Pegylated hippocampus peptide injection and preparation method thereof - Google Patents

Pegylated hippocampus peptide injection and preparation method thereof Download PDF

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Publication number
CN114601916B
CN114601916B CN202210381804.5A CN202210381804A CN114601916B CN 114601916 B CN114601916 B CN 114601916B CN 202210381804 A CN202210381804 A CN 202210381804A CN 114601916 B CN114601916 B CN 114601916B
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peptide
hippocampus
liquid medicine
preparation
completely dissolved
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CN114601916A (en
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董礼
樊继涛
于婷
宋阳
余俊
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Jiangsu Hansoh Pharmaceutical Group Co Ltd
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Jiangsu Hansoh Pharmaceutical Group Co Ltd
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/16Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/18Growth factors; Growth regulators
    • A61K38/1816Erythropoietin [EPO]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/02Inorganic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0019Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/08Solutions
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06Antianaemics

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Abstract

The invention relates to a pelargonidin hippocampal peptide injection preparation and a preparation method thereof. The invention discloses a pharmaceutical composition taking a cultivated hippocampus peptide as an active ingredient. The pharmaceutical composition contains the physiologically acceptable auxiliary materials of the pelargonidae hippocampus peptide with the pH value of 4.0-7.0. The pharmaceutical composition has good pharmaceutical stability and safety, and the preparation method is simple and convenient, and is suitable for industrial production.

Description

Pegylated hippocampus peptide injection and preparation method thereof
Technical Field
The invention belongs to the field of pharmaceutical preparations, and in particular relates to a pelargonidae western Hippocampus peptide injection preparation and a preparation method thereof.
Background
The cultivated Hippocampus japonicus peptide is artificially synthesized PEG erythropoietin mimetic peptide, and can promote proliferation of bone marrow erythroid directional progenitor cells (BFU-E, CFU-E) and differentiation of precursor cells with identifiable morphology by combining with specific EPO receptor on the cell surface, and can also accelerate proliferation and differentiation of precursor cells and promote release of reticulocytes by bone marrow and promote generation of erythrocytes.
The cultivated hippocampal peptide obviously stimulates proliferation of EPO-dependent blood cells (UT 7/EPO cells) in vitro, inhibits apoptosis and stimulates phosphorylation of cell Stat 5; BFU-E colony formation was stimulated (> 50 cells). EPO-018B significantly stimulated peripheral blood reticulocyte production in vivo, with a significant increase in peripheral blood RBC, hgb, HCT%.
The cultivated Hippocampus japonicus peptide is unstable under alkaline condition, and the fluctuation range of pH value can be greatly reduced by using buffer salt solution as pH regulator, meanwhile, the optimal buffer salt proportion is screened out by research, and the pH environment of the solution after the raw material medicine is added is further ensured, so that the stability of the product is ensured, and the clinical use safety is further improved.
The active carbon is a heat source removing component commonly used in injection, and the raw material sources and the production processes are various, so that the active carbon possibly contains different element impurities, and part of the elements are toxic, including neurotoxicity, nephrotoxicity and the like. Activated carbon is also a potential risk source for insoluble particles in injections, increasing the risk of insoluble particle incorporation. Meanwhile, the activated carbon has a certain adsorption effect on the medicine, and particularly has a great influence on the content of the medicine with low dosage.
The preparation process avoids using active carbon, and can ensure product stability and liquid medicine dissolving speed.
Disclosure of Invention
In view of the above, the invention provides a preparation method of a cultivated Hippocampus peptide injection preparation with simple and convenient process, strong stability and high safety, and the preparation method thereof, which can solve the problems of unstable alkali and low content of main medicine after liquid preparation in the liquid preparation process by enhancing the control of endotoxin in raw materials and auxiliary materials without using active carbon in the preparation process, and reduce the clinical application risk.
The invention provides a cercis hippocampal peptide injection preparation which is characterized by comprising cercis hippocampal peptide or pharmaceutically acceptable buffer salt thereof, an osmotic pressure regulator and a solvent.
The preparation of the pernicious western sea horse peptide is characterized in that the buffer salt is dibasic phosphate and monobasic phosphate, preferably dibasic sodium phosphate and monobasic sodium phosphate.
The pernicious western sea horse peptide preparation is characterized in that the osmotic pressure regulator is one or more of sodium chloride, mannitol, glucose, sorbitol or glycerol, preferably mannitol or sodium chloride.
The preparation of the cultivated hippocampal peptide is characterized in that the phosphate proportion of the buffer solution is disodium hydrogen phosphate: the ratio of the sodium dihydrogen phosphate is 1:10 to 30, preferably 1:10 to 20, more preferably 1:17 to 18.
The solvent is water for injection.
The injection preparation comprises 0.05% -3.0% (W/V) of the cultivated Hippocampus peptide, preferably 0.1% -1.0% (W/V).
The injection preparation of the invention contains 0.05 to 5.0 percent (W/V) of buffer salt, preferably 0.5 to 1.5 percent (W/V).
The injection preparation of the invention contains 0.05 to 4.0 percent (W/V) of isotonic regulator, preferably 0.1 to 1.0 percent (W/V).
The preparation of the cultivated hippocampal peptide is characterized in that the pH adjustment range is selected from 4-7, preferably 5-6.
The invention also provides a method for preparing the injection preparation of the cultivated hippocampal peptide, which comprises the following steps:
1) Adding the osmotic pressure regulator with the prescription amount into water for injection, stirring and dissolving;
2) Adding a prescribed amount of buffer salt into the solution in the step 1), and stirring for dissolution;
3) Adding the cultivated Hippocampus japonicus peptide into the solution in the step 2), stirring for dissolution, and measuring the pH value of the solution;
4) Filtering the liquid medicine in the step 3), sub-packaging the filtered liquid medicine into a penicillin bottle or a clip type bottle or a prefilled syringe, filling nitrogen and plugging;
the preparation method of the pernicious Hippocampus peptide preparation is characterized in that sodium chloride is added first, then disodium hydrogen phosphate is added, and then sodium dihydrogen phosphate is added in the preparation process.
The preparation of the cultivated hippocampus peptide is characterized in that the preparation temperature is 10-50 ℃, preferably 15-25 ℃.
The preparation of the cultivated Hippocampus peptide is characterized in that the temperature needs to be suddenly reduced from 30-50 ℃ to 10-25 ℃ when the preparation is prepared; preferably 30℃is suddenly reduced to 25 ℃.
The preparation is characterized in that the pharmaceutical composition is packaged by a penicillin bottle, a cartridge bottle or a prefilled syringe.
The preparation is characterized in that the split charging container of the pharmaceutical composition is made of medium borosilicate glass.
The invention relates to a cerHippocampus peptide preparation, which is characterized in that the rubber plug used is a chlorinated butyl rubber plug or a brominated butyl rubber plug.
The preparation of the cultivated hippocampal peptide is characterized in that an injection pen device is adopted for administration.
Compared with the prior art, the invention has the following advantages and beneficial effects:
(1) The injection preparation provided by the invention has the advantages that the preparation process is simple, the active carbon adsorption process is not needed, the safety of the product is further ensured, the active carbon treatment is not needed, the production cost is reduced, the environment is not polluted, the active carbon is prevented from introducing new impurities, and the safety risk and the environmental protection pressure are avoided.
(2) Meanwhile, the research shows that the impurity A component is alkali sensitive impurity and temperature sensitive impurity, and the free polyethylene glycol (20 KD,40 KD) is sensitive to the ion concentration change of the liquid medicine system. The phosphate proportion screening and preparation process is examined to find a stable and proper pH environment and preparation process, so that the stability of the product can be effectively ensured.
Detailed Description
The present invention will be described in more detail with reference to examples, but the present invention is not limited to the examples.
Example 1:
(1) weighing 70% of the prescribed amount (100 ml') of purified water into a beaker, wherein the water temperature is less than or equal to 25 ℃;
(2) 59mg of disodium hydrogen phosphate and 1032mg of sodium dihydrogen phosphate are added into the solution, and the mixture is stirred until the mixture is completely dissolved;
(3) adding 400mg (calculated as the cultivated Hippocampus peptide) of the raw material medicine, and magnetically stirring until the raw material medicine is completely dissolved;
(4) and (3) fixing the volume to 100ml, stirring for 45min after fixing the volume, and measuring the pH of the liquid medicine to 5-6.
And measuring the osmotic pressure of the liquid medicine after the volume is fixed.
Example 2:
(1) weighing 70% of the prescribed amount (100 ml') of purified water into a beaker, wherein the water temperature is less than or equal to 25 ℃;
(2) 200mg of sodium chloride is added and stirred magnetically until the sodium chloride is completely dissolved;
(3) 59mg of disodium hydrogen phosphate and 1032mg of sodium dihydrogen phosphate are added into the solution, and the mixture is stirred until the mixture is completely dissolved;
(4) adding 400mg (calculated as the cultivated Hippocampus peptide) of the raw material medicine, and magnetically stirring until the raw material medicine is completely dissolved;
(5) and (3) fixing the volume to 100ml, stirring for 45min after fixing the volume, and measuring the pH of the liquid medicine to 5-6.
And measuring the osmotic pressure of the liquid medicine after the volume is fixed.
Example 3:
(1) weighing 70% of the prescribed amount (100 ml') of purified water into a beaker, wherein the water temperature is less than or equal to 25 ℃;
(2) 350mg of sodium chloride is added and stirred magnetically until the mixture is completely dissolved;
(3) 59mg of disodium hydrogen phosphate and 1032mg of sodium dihydrogen phosphate are added into the solution, and the mixture is stirred until the mixture is completely dissolved;
(4) adding 400mg (calculated as the cultivated Hippocampus peptide) of the raw material medicine, and magnetically stirring until the raw material medicine is completely dissolved;
(5) and (3) fixing the volume to 100ml, stirring for 45min after fixing the volume, and measuring the pH of the liquid medicine to 5-6.
And measuring the osmotic pressure of the liquid medicine after the volume is fixed.
Example 4:
(1) weighing 70% of the prescribed amount (100 ml') of purified water into a beaker, wherein the water temperature is less than or equal to 25 ℃;
(2) 425mg of sodium chloride is added and stirred magnetically until the mixture is completely dissolved;
(3) 59mg of disodium hydrogen phosphate and 1032mg of sodium dihydrogen phosphate are added into the solution, and the mixture is stirred until the mixture is completely dissolved;
(4) adding 400mg (calculated as the cultivated Hippocampus peptide) of the raw material medicine, and magnetically stirring until the raw material medicine is completely dissolved;
(5) and (3) fixing the volume to 100ml, stirring for 45min after fixing the volume, and measuring the pH of the liquid medicine to 5-6.
And measuring the osmotic pressure of the liquid medicine after the volume is fixed.
Study of influence of sodium chloride consumption on osmotic pressure
Sodium chloride dosage (g) Sodium chloride concentration (mg/ml) Osmotic pressure (mOsm/Kg)
0 0 159
0.2 2 226
0.35 3.5 277
0.425 4.25 297
Conclusion: the dosage of sodium chloride as osmotic regulator in the prescription is 4.25mg/ml, which can ensure the quality of the product and meet the clinical administration requirement.
Example 5:
(1) weighing 70% of the prescribed amount (100 ml') of purified water into a beaker, wherein the water temperature is less than or equal to 25 ℃;
(2) 425mg of sodium chloride is added and stirred magnetically until the mixture is completely dissolved;
(3) 59mg of disodium hydrogen phosphate and 295mg of sodium dihydrogen phosphate are added into the solution in the step (2), and the proportion is 1:5, stirring until the mixture is completely dissolved;
(4) adding 400mg (calculated as the cultivated Hippocampus peptide) of the raw material medicine, and magnetically stirring until the raw material medicine is completely dissolved;
(5) adjusting the pH value of the solution to 5.0-6.0 by using 1% sodium dihydrogen phosphate;
(6) and (3) fixing the volume to 100ml, stirring for 45min after fixing the volume, and measuring the pH of the liquid medicine to 5-6.
And (5) placing the liquid medicine with the constant volume at the temperature of less than or equal to 25 ℃ to determine the stability of the liquid medicine within 12 hours.
Example 6:
(1) weighing 70% of the prescribed amount (100 ml') of purified water into a beaker, wherein the water temperature is less than or equal to 25 ℃;
(2) 425mg of sodium chloride is added and stirred magnetically until the mixture is completely dissolved;
(3) 59mg of disodium hydrogen phosphate and 590mg of sodium dihydrogen phosphate are added into the solution in the step (2), and the proportion is 1:10, stirring until the mixture is completely dissolved;
(4) adding 400mg (calculated as the cultivated Hippocampus peptide) of the raw material medicine, and magnetically stirring until the raw material medicine is completely dissolved;
(5) adjusting the pH value of the solution to 5.0-6.0 by using 1% sodium dihydrogen phosphate;
(6) and (3) fixing the volume to 100ml, stirring for 45min after fixing the volume, and measuring the pH of the liquid medicine to 5-6.
And (5) placing the liquid medicine with the constant volume at the temperature of less than or equal to 25 ℃ to determine the stability of the liquid medicine within 12 hours.
Example 7:
(1) weighing 70% of the prescribed amount (100 ml') of purified water into a beaker, wherein the water temperature is less than or equal to 25 ℃;
(2) 425mg of sodium chloride is added and stirred magnetically until the mixture is completely dissolved;
(3) 59mg of disodium hydrogen phosphate and 885mg of sodium dihydrogen phosphate are added into the solution in the step (2), and the proportion is 1:15, stirring until the mixture is completely dissolved;
(4) adding 400mg (calculated as the cultivated Hippocampus peptide) of the raw material medicine, and magnetically stirring until the raw material medicine is completely dissolved;
(5) adjusting the pH value of the solution to 5.0-6.0 by using 1% sodium dihydrogen phosphate;
(6) and (3) fixing the volume to 100ml, stirring for 45min after fixing the volume, and measuring the pH of the liquid medicine to 5-6.
And (5) placing the liquid medicine with the constant volume at the temperature of less than or equal to 25 ℃ to determine the stability of the liquid medicine within 12 hours.
Example 8:
(1) weighing 70% of the prescribed amount (100 ml') of purified water into a beaker, wherein the water temperature is less than or equal to 25 ℃;
(2) 425mg of sodium chloride is added and stirred magnetically until the mixture is completely dissolved;
(3) 59mg of disodium hydrogen phosphate and 1180mg of sodium dihydrogen phosphate are added into the solution in the step (2), and the proportion is 1:20, stirring until the mixture is completely dissolved;
(4) adding 400mg (calculated as the cultivated Hippocampus peptide) of the raw material medicine, and magnetically stirring until the raw material medicine is completely dissolved;
(5) adjusting the pH value of the solution to 5.0-6.0 by using 1% disodium hydrogen phosphate;
(6) and (3) fixing the volume to 100ml, stirring for 45min after fixing the volume, and measuring the pH of the liquid medicine to 5-6.
And (5) placing the liquid medicine with the constant volume at the temperature of less than or equal to 25 ℃ to determine the stability of the liquid medicine within 12 hours.
Example 9:
(1) weighing 70% of the prescribed amount (100 ml') of purified water into a beaker, wherein the water temperature is less than or equal to 25 ℃;
(2) 425mg of sodium chloride is added and stirred magnetically until the mixture is completely dissolved;
(3) 59mg of disodium hydrogen phosphate and 1023mg of sodium dihydrogen phosphate are added into the solution in the step (2), and the proportion is 1:17.5, stirring until the mixture is completely dissolved;
(4) adding 400mg (calculated as the cultivated Hippocampus peptide) of the raw material medicine, and magnetically stirring until the raw material medicine is completely dissolved;
(5) measuring the pH of the solution to be in the range of 5.0-6.0;
(6) and (3) fixing the volume to 100ml, stirring for 45min after fixing the volume, and measuring the pH of the liquid medicine to 5-6.
And (5) placing the liquid medicine with the constant volume at the temperature of less than or equal to 25 ℃ to determine the stability of the liquid medicine within 12 hours.
Conclusion(s)
The ratio of disodium hydrogen phosphate to sodium dihydrogen phosphate is 1: at 17.5, the intermediate liquid medicine has the best stability.
Example 10:
(1) weighing 70% of the prescribed amount (100 ml') of purified water into a beaker, wherein the water temperature is less than or equal to 25 ℃;
(2) 425mg of sodium chloride is added and stirred magnetically until the mixture is completely dissolved;
(3) 59mg of disodium hydrogen phosphate and 1023mg of sodium dihydrogen phosphate are added into the solution in the step (2), and the proportion is 1:17.5, stirring until the mixture is completely dissolved;
(4) adding 400mg (calculated as the cultivated Hippocampus peptide) of the raw material medicine, and magnetically stirring until the raw material medicine is completely dissolved;
(5) adjusting the pH value of the solution to 5.0-6.0 by using 1% sodium dihydrogen phosphate or 1% disodium hydrogen phosphate;
(6) and (3) fixing the volume to 100ml, stirring for 45min after fixing the volume, and measuring the pH of the liquid medicine to 5-6.
And (5) placing the liquid medicine with the constant volume at 35 ℃ to determine the stability of the liquid medicine within 12 hours.
Example 11:
(1) weighing 70% of the prescribed amount (100 ml') of purified water into a beaker, wherein the water temperature is less than or equal to 25 ℃;
(2) 425mg of sodium chloride is added and stirred magnetically until the mixture is completely dissolved;
(3) 59mg of disodium hydrogen phosphate and 1023mg of sodium dihydrogen phosphate are added into the solution in the step (2), and the proportion is 1:17.5, stirring until the mixture is completely dissolved;
(4) adding 400mg (calculated as the cultivated Hippocampus peptide) of the raw material medicine, and magnetically stirring until the raw material medicine is completely dissolved;
(5) adjusting the pH value of the solution to 5.0-6.0 by using 1% sodium dihydrogen phosphate or 1% disodium hydrogen phosphate;
(6) and (3) fixing the volume to 100ml, stirring for 45min after fixing the volume, and measuring the pH of the liquid medicine to 5-6.
And (5) placing the liquid medicine with the constant volume at 30 ℃ to determine the stability of the liquid medicine within 12 hours.
Example 12:
(1) weighing 70% of the prescribed amount (100 ml') of purified water into a beaker, wherein the water temperature is less than or equal to 25 ℃;
(2) 425mg of sodium chloride is added and stirred magnetically until the mixture is completely dissolved;
(3) 59mg of disodium hydrogen phosphate and 1023mg of sodium dihydrogen phosphate are added into the solution in the step (2), and the proportion is 1:17.5, stirring until the mixture is completely dissolved;
(4) adding 400mg (calculated as the cultivated Hippocampus peptide) of the raw material medicine, and magnetically stirring until the raw material medicine is completely dissolved;
(5) adjusting the pH value of the solution to 5.0-6.0 by using 1% sodium dihydrogen phosphate or 1% disodium hydrogen phosphate;
(6) and (3) fixing the volume to 100ml, stirring for 45min after fixing the volume, and measuring the pH of the liquid medicine to 5-6.
And (5) placing the liquid medicine with the constant volume at 25 ℃ to determine the stability of the liquid medicine within 12 hours.
Example 13:
(1) weighing 70% of the prescribed amount (100 ml') of purified water into a beaker, wherein the water temperature is less than or equal to 25 ℃;
(2) 425mg of sodium chloride is added and stirred magnetically until the mixture is completely dissolved;
(3) 59mg of disodium hydrogen phosphate and 1023mg of sodium dihydrogen phosphate are added into the solution in the step (2), and the proportion is 1:17.5, stirring until the mixture is completely dissolved;
(4) adding 400mg (calculated as the cultivated Hippocampus peptide) of the raw material medicine, and magnetically stirring until the raw material medicine is completely dissolved;
(5) adjusting the pH value of the solution to 5.0-6.0 by using 1% sodium dihydrogen phosphate or 1% disodium hydrogen phosphate;
(6) and (3) fixing the volume to 100ml, stirring for 45min after fixing the volume, and measuring the pH of the liquid medicine to 5-6.
And (5) placing the liquid medicine with the constant volume at 20 ℃ to determine the stability of the liquid medicine within 12 hours.
Conclusion: the intermediate liquid medicine is sensitive to temperature, and the preparation temperature is stable below 25 ℃.
Meanwhile, the research on the destruction experiments of the bulk drugs is carried out by the company, the results are shown in the following table, and the cultivated Hippocampus japonicus peptide is sensitive to alkali, high temperature and oxygen.
Note that: (1) N/D represents undetected.
Example 14:
(1) weighing 70% of the prescribed amount (100 ml') of purified water into a beaker, wherein the water temperature is less than or equal to 25 ℃;
(2) 425mg of sodium chloride is added and stirred magnetically until the mixture is completely dissolved;
(3) 59mg of disodium hydrogen phosphate and 1023mg of sodium dihydrogen phosphate are added into the solution in the step (2), and the proportion is 1:17.5, stirring until the mixture is completely dissolved;
(4) adding 400mg (calculated as the cultivated Hippocampus peptide) of the raw material medicine, and magnetically stirring until the raw material medicine is completely dissolved;
(5) adjusting the pH value of the solution to 5.0-6.0 by using 1% sodium dihydrogen phosphate or 1% disodium hydrogen phosphate;
(6) and (3) fixing the volume to 100ml, stirring for 45min after fixing the volume, and measuring the pH of the liquid medicine to 5-6.
And (3) placing the liquid medicine with the constant volume at 25 ℃, and measuring the stability of the liquid medicine within 24 hours under the conditions of no light shielding and no nitrogen charging.
Example 15:
(1) weighing 70% of the prescribed amount (100 ml') of purified water into a beaker, wherein the water temperature is less than or equal to 25 ℃;
(2) 425mg of sodium chloride is added and stirred magnetically until the mixture is completely dissolved;
(3) 59mg of disodium hydrogen phosphate and 1023mg of sodium dihydrogen phosphate are added into the solution in the step (2), and the proportion is 1:17.5, stirring until the mixture is completely dissolved;
(4) adding 400mg (calculated as the cultivated Hippocampus peptide) of the raw material medicine, and magnetically stirring until the raw material medicine is completely dissolved;
(5) adjusting the pH value of the solution to 5.0-6.0 by using 1% sodium dihydrogen phosphate or 1% disodium hydrogen phosphate;
(6) and (3) fixing the volume to 100ml, stirring for 45min after fixing the volume, and measuring the pH of the liquid medicine to 5-6.
And (3) placing the liquid medicine with the constant volume at 25 ℃, and measuring the stability of the liquid medicine within 24 hours under the condition of no light shielding and nitrogen charging.
Example 16:
(1) weighing 70% of the prescribed amount (100 ml') of purified water into a beaker, wherein the water temperature is less than or equal to 25 ℃;
(2) 425mg of sodium chloride is added and stirred magnetically until the mixture is completely dissolved;
(3) 59mg of disodium hydrogen phosphate and 1023mg of sodium dihydrogen phosphate are added into the solution in the step (2), and the proportion is 1:17.5, stirring until the mixture is completely dissolved;
(4) adding 400mg (calculated as the cultivated Hippocampus peptide) of the raw material medicine, and magnetically stirring until the raw material medicine is completely dissolved;
(5) adjusting the pH value of the solution to 5.0-6.0 by using 1% sodium dihydrogen phosphate or 1% disodium hydrogen phosphate;
(6) and (3) fixing the volume to 100ml, stirring for 45min after fixing the volume, and measuring the pH of the liquid medicine to 5-6.
And (3) placing the liquid medicine with the constant volume at 25 ℃, avoiding light, and measuring the stability of the liquid medicine within 24 hours under the condition of no nitrogen filling.
Example 17:
(1) weighing 70% of the prescribed amount (100 ml') of purified water into a beaker, wherein the water temperature is less than or equal to 25 ℃;
(2) 425mg of sodium chloride is added and stirred magnetically until the mixture is completely dissolved;
(3) 59mg of disodium hydrogen phosphate and 1023mg of sodium dihydrogen phosphate are added into the solution in the step (2), and the proportion is 1:17.5, stirring until the mixture is completely dissolved;
(4) adding 400mg (calculated as the cultivated Hippocampus peptide) of the raw material medicine, and magnetically stirring until the raw material medicine is completely dissolved;
(5) adjusting the pH value of the solution to 5.0-6.0 by using 1% sodium dihydrogen phosphate or 1% disodium hydrogen phosphate;
(6) and (3) fixing the volume to 100ml, stirring for 45min after fixing the volume, and measuring the pH of the liquid medicine to 5-6.
And (3) placing the liquid medicine with the constant volume at 25 ℃, and measuring the stability of the liquid medicine within 24 hours under the condition of light shielding and nitrogen charging.
Natural light, temperature and nitrogen influence result on liquid medicine stability
Conclusion: the intermediate liquid medicine is stable under 24 hours, and the short-time influence of light and oxygen on the intermediate liquid medicine is small.
Example 18:
(1) weighing 70% of the prescription amount (2L) of purified water into a beaker, wherein the water temperature is less than or equal to 25 ℃;
(2) 8.5g of sodium chloride is added and stirred magnetically until the sodium chloride is completely dissolved;
(3) 1.18g of disodium hydrogen phosphate and 20.46g of sodium dihydrogen phosphate are added into the solution in the step (2), and the proportion is 1:17.5, stirring until the mixture is completely dissolved;
(4) adding 8.0g (calculated as the cultivated Hippocampus peptide) of the crude drug, and magnetically stirring until the crude drug is completely dissolved;
(5) adjusting the pH value of the solution to 5.0-6.0 by using 1% sodium dihydrogen phosphate or 1% disodium hydrogen phosphate;
(6) constant volume to 2L, stirring for 45min after constant volume, and measuring the pH of the liquid medicine to 5-6.
Filtering the liquid medicine with a 0.22 μm filter membrane, filling 1.5ml into a prefilled syringe after filtering, and respectively performing nitrogen filling protection and plugging.
And (5) respectively carrying out lofting investigation on the split-packed samples to the conditions of the influencing factors. The results are shown in Table 1.
Example 19:
(1) weighing 70% of the prescription amount (2L) of purified water into a beaker, wherein the water temperature is less than or equal to 25 ℃;
(2) 8.5g of sodium chloride is added and stirred magnetically until the sodium chloride is completely dissolved;
(3) 1.18g of disodium hydrogen phosphate and 20.46g of sodium dihydrogen phosphate are added into the solution in the step (2), and the proportion is 1:17.5, stirring until the mixture is completely dissolved;
(4) adding 8.0g (calculated as the cultivated Hippocampus peptide) of the crude drug, and magnetically stirring until the crude drug is completely dissolved;
(5) adjusting the pH value of the solution to 5.0-6.0 by using 1% sodium dihydrogen phosphate or 1% disodium hydrogen phosphate;
(6) constant volume to 2L, stirring for 45min after constant volume, and measuring the pH of the liquid medicine to 5-6.
The liquid medicine after volume fixing was filtered with a 0.22 μm filter membrane, and 1.5ml (6.0 mg specification) was filled into a prefilled syringe after filtration.
And (5) respectively carrying out lofting investigation on the conditions of the influencing factors. The results are shown in Table 2.

Claims (4)

1. An injection preparation of the cercis hippocampus peptide is characterized by comprising the cercis hippocampus peptide, buffer salt, osmotic pressure regulator and solvent;
the injection preparation comprises 0.1 to 1.0 percent (W/V) of the cultivated hippocampus peptide, 0.5 to 1.5 percent (W/V) of buffer salt and 0.1 to 1.0 percent (W/V) of osmotic pressure regulator;
the osmotic pressure regulator is sodium chloride, and the solvent is water for injection;
the pH range of the pharmaceutical composition is 5.0-6.0;
the buffer salt is selected from disodium hydrogen phosphate and sodium dihydrogen phosphate, and the ratio of the disodium hydrogen phosphate to the sodium dihydrogen phosphate is 1:17-18.
2. A method of preparing the pernicious western hippocampal peptide injection formulation of claim 1, comprising the steps of:
1) Adding the osmotic pressure regulator with the prescription amount into water for injection, stirring and dissolving;
2) Adding a prescribed amount of buffer salt into the solution in the step 1), and stirring for dissolution;
3) Adding the cultivated Hippocampus japonicus peptide into the solution in the step 2), stirring for dissolution, and measuring the pH value of the solution;
4) Filtering the liquid medicine in the step 3), sub-packaging the filtered liquid medicine into a penicillin bottle or a card bottle or a prefilled syringe, and plugging.
3. The method according to claim 2, wherein the preparation temperature is 10-30 ℃, and the liquid medicine is packaged into penicillin bottles or card bottles or prefilled syringes and is protected by nitrogen filling.
4. A method according to claim 3, characterized in that the preparation temperature is 10-25 ℃.
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Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101456911A (en) * 2007-12-12 2009-06-17 江苏豪森药业股份有限公司 Erythrocyte-stimulating factor mimic peptide derivative, medical salts thereof, preparation method and use thereof
CN103536900A (en) * 2012-07-16 2014-01-29 江苏豪森药业股份有限公司 Erythrogenin mimetic peptide-containing pharmaceutical composition
CN103570834A (en) * 2012-07-19 2014-02-12 江苏豪森药业股份有限公司 Methoxy polyethylene glycol-modified erythropoietin mimic peptide derivative
CN108606955A (en) * 2016-12-09 2018-10-02 江苏豪森药业集团有限公司 The Pharmaceutical composition and preparation method thereof of trainingization Xihai sea horse peptide
WO2019129278A1 (en) * 2017-12-29 2019-07-04 江苏豪森药业集团有限公司 Pharmaceutical composition of pegol-sihematide and preparation method therefor

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101456911A (en) * 2007-12-12 2009-06-17 江苏豪森药业股份有限公司 Erythrocyte-stimulating factor mimic peptide derivative, medical salts thereof, preparation method and use thereof
CN103536900A (en) * 2012-07-16 2014-01-29 江苏豪森药业股份有限公司 Erythrogenin mimetic peptide-containing pharmaceutical composition
CN103570834A (en) * 2012-07-19 2014-02-12 江苏豪森药业股份有限公司 Methoxy polyethylene glycol-modified erythropoietin mimic peptide derivative
CN108606955A (en) * 2016-12-09 2018-10-02 江苏豪森药业集团有限公司 The Pharmaceutical composition and preparation method thereof of trainingization Xihai sea horse peptide
WO2019129278A1 (en) * 2017-12-29 2019-07-04 江苏豪森药业集团有限公司 Pharmaceutical composition of pegol-sihematide and preparation method therefor
CN109985232A (en) * 2017-12-29 2019-07-09 江苏豪森药业集团有限公司 The pharmaceutical composition and preparation method thereof of trainingization Xihai sea horse peptide
CN110214019A (en) * 2017-12-29 2019-09-06 江苏豪森药业集团有限公司 The pharmaceutical composition and preparation method thereof of trainingization Xihai sea horse peptide

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
POS-606 PEGMOLESATIDE FOR THE TREATMENT OF ANEMIA IN CKD PATIENTS UNDERGOING DIALYSIS: INTERIM ANALYSIS OF A MULTICENTER PHASE III TRIAL;CHEN, J等;Kidney International Reports;第7卷(第2期);第S260页 *

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