Piracetam composition injection and preparation method thereof

Abstract

The invention relates to the technical field of injections, in particular to a piracetam composition injection, which is prepared from the following components in percentage by mass: 3 to 4 percent of piracetam, 0.8 to 1 percent of sodium chloride, 0.5 to 0.6 percent of cerebroprotein hydrolysate, 0.1 to 0.2 percent of glutamic acid, 0.05 to 0.1 percent of sodium ethacryate, 0.04 to 0.08 percent of anisodamine, 0.02 to 0.035 percent of injection activated carbon and the balance of water for injection. According to the invention, adverse reactions caused by the injection are improved, digestive tract symptoms and central nervous system symptoms are avoided or reduced, side effects of the injection are reduced, the safety of the injection is higher, the injection is prepared in a mode of matching concentrated preparation and diluted preparation, and the injection quality is improved under the condition of ensuring the uniformity of the injection. The preparation speed and precision are greatly improved, the large-batch preparation requirement is met, the filtering step is added after concentrated preparation and diluted preparation, the clarity of the injection can be guaranteed through filtering, injection activated carbon is further added into the injection, and filter holes are prevented from being blocked by sediment in the injection.

Description

Technical Field

[0001] The invention relates to the technical field of injections, and in particular to a piracetam composition injection and a preparation method thereof. Background Art

[0002] Piracetam is mainly used to treat brain diseases such as Alzheimer's disease, brain trauma, cerebral ischemia, lack of attention, etc. The production of piracetam composition injection must first determine the raw materials, and then go through the steps of solvent preparation, drug preparation, sterilization, filling, etc. to ensure the stability and safety of the quality of the produced injection.

[0003] The main drug ingredients of piracetam injection are pyrrolidine and acetamide, and the auxiliary materials are sodium bisulfite and polyhydrogen salt. The drug may cause adverse reactions during its use, among which the more obvious ones may cause gastrointestinal symptoms and central nervous system symptoms, and some may cause abnormal liver function. In addition, the existing piracetam composition injection directly dilutes all components into the raw materials with solvents, which is not suitable for large-scale preparation, and has high requirements on the weight of the raw materials, which easily causes uneven injection.

[0004] Therefore, in order to solve the above-mentioned problems of large side effects and unsuitability for large-scale preparation, a piracetam composition injection and a preparation method thereof can be designed. Summary of the invention

[0005] In order to overcome the problem of large side effects and unsuitability for large-scale configuration.

[0006] The technical scheme of the present invention is: a piracetam composition injection, which comprises the following components by mass percentage: 3-4% of piracetam, 0.8-1% of sodium chloride, 0.5-0.6% of brain protein hydrolysate, 0.1-0.2% of glutamic acid, 0.05-0.1% of sodium ethacrynate, 0.04-0.08% of anisodamine, 0.02-0.035% of activated carbon for injection, and the balance is water for injection.

[0007] Preferably, the following components are included, in percentage by mass: piracetam: 3%, sodium chloride: 0.8%, brain protein hydrolysate: 0.5%, glutamic acid: 0.1%, ethacrynic acid sodium: 0.05%, scopolamine: 0.04%, activated carbon for injection: 0.02%, and the balance is water for injection.

[0008] Preferably, the following components are included, in percentage by mass: piracetam: 4%, sodium chloride: 1%, brain protein hydrolysate: 0.6%, glutamic acid: 0.2%, ethacrynic acid sodium: 0.1%, scopolamine: 0.08%, activated carbon for injection: 0.02-0.035%, and the remainder is water for injection.

[0009] Preferably, the purity of piracetam is not less than 99%; the purity of sodium chloride is not less than 99.5%.

[0010] A method for preparing a piracetam composition injection, comprising the piracetam composition injection as described above, and the steps are as follows:

[0011] Step 1: Weigh the required weight of raw materials according to the proportion and set aside;

[0012] Step 2: Sodium chloride is put into a concentrated preparation tank containing water for injection, and after sufficient stirring, piracetam is added, stirred to dissolve, and 65-75% of the formula amount of activated carbon for injection is added, and stirring is continued. The mixture is boiled for 10-25 minutes, cooled naturally for 10 minutes, and then circulated internally for 10 minutes, and then filtered under pressure with a filter. The filtered solution is pumped into a dilute preparation tank;

[0013] Step 3: Add water for injection to 78-82% of the total amount in the dilution tank, add the remaining activated carbon for injection, stir well, add water for injection to the full amount, stir and reflux for 15 minutes, measure the pH value, cool to 40-50℃, filter under pressure with a filter and a 0.22μm membrane filter element in turn, and the injection solution enters the filling process;

[0014] Step 4: The empty bag is sent into the fixture of the filling equipment with a fixture, and the filling volume is set in the filling equipment. The filling hose is centered by the center positioning device. When the filling nozzle reaches the lowest limit position, the length of the tube is checked, and whether there is a mouth tube. If an error signal appears, the corresponding filling position will not perform filling of this bag. When the station moves down, the filling nozzle is inserted into the mouth tube of the bag, and the filling valve is opened immediately to fill the liquid medicine into the bag. When the filling volume is reached, the mass flow meter gives a signal to close the filling valve through the control system, and the filling head moves upward under the drive mechanism to end the filling;

[0015] Step 5: Then cover and take out the bag for wet heat sterilization;

[0016] Step 6: Quality inspection;

[0017] Step 7: Packing and storage.

[0018] Preferably, in step 2, the mass ratio of sodium chloride to water for injection is 1:8-10; and the temperature of the water for injection is 70-85°C.

[0019] Preferably, the pH value requirement in step three is 5.0-6.0. If it does not meet the requirement, it can be adjusted with dilute hydrochloric acid or 1M sodium hydroxide.

[0020] Preferably, the moist heat sterilization treatment in step 5 adopts any one of boiling sterilization, pasteurization, high-pressure steam sterilization, circulating steam sterilization or intermittent steam sterilization; the conditions of moist heat sterilization are: 120-123°C, time 12-20min, F0 value ≥12.

[0021] Beneficial effects of the present invention:

[0022] 1. Improve the adverse reactions caused by the injection, avoid or reduce the symptoms of the digestive tract and the central nervous system, reduce the side effects of the injection, and make the injection safer. Brain protein hydrolysate, glutamic acid, sodium ethacrynate and scopolamine are also added to the injection. Brain protein hydrolysate can act on the central nervous system, regulate and improve the metabolism of neurons, improve the energy metabolism in the brain, provide neurotransmitters, peptide hormones and coenzyme precursors, and protect nerve cells from hypoxia and neurotoxin damage. Glutamic acid has the effects of protecting the liver, improving brain function and improving the body's immunity. Sodium ethacrynate has diuretic, anti-hypertension, anti-heart failure, anti-cerebral edema, anti-inflammatory and other effects and functions. The role of scopolamine is to relieve smooth muscle spasms and bile duct spasms;

[0023] 2. The injection solution is prepared by combining concentrated and diluted preparations. While ensuring the uniformity of the injection solution, the preparation speed and accuracy are greatly improved, which is suitable for large-scale preparation requirements. In addition, a filtration step is added after concentrated and diluted preparations. The filtration can ensure the clarity of the injection solution. At the same time, activated carbon for injection is added to the injection solution to prevent the precipitation in the injection solution from clogging the filter pores. DETAILED DESCRIPTION

[0024] The present invention will be further described below in conjunction with the embodiments.

[0025] Example 1

[0026] The present invention provides an embodiment: a piracetam composition injection, which comprises the following components, measured by mass percentage: 3% of piracetam, 0.8% of sodium chloride, 0.5% of brain protein hydrolysate, 0.1% of glutamic acid, 0.05% of sodium ethacrynate, 0.04% of anisodamine, 0.02% of activated carbon for injection, and the balance is water for injection.

[0027] A method for preparing a piracetam composition injection, comprising the piracetam composition injection as described above, and the steps are as follows:

[0028] Step 1: Weigh the required weight of raw materials according to the proportion and set aside;

[0029] Step 2: Sodium chloride is put into a concentrated preparation tank containing water for injection. The mass ratio of sodium chloride to water for injection is 1:8. The temperature of the water for injection is 70°C. After sufficient stirring, piracetam is added and stirred to dissolve. 65% of the formula amount of activated carbon for injection is added and continued stirring. The mixture is boiled for 10 minutes, cooled naturally for 10 minutes, and then circulated internally for 10 minutes. The mixture is then filtered under pressure with a filter and the filtered solution is pumped into a dilute preparation tank.

[0030] Step 3: Add water for injection to 78% of the total amount in the dilution tank, add the remaining activated carbon for injection, stir well, add water for injection to the full amount, stir and reflux for 15 minutes, measure the pH value, the pH value is required to be 5.0-6.0, if it does not meet the requirements, adjust it with dilute hydrochloric acid or 1M sodium hydroxide, cool to 40°C, filter with a filter and a 0.22μm membrane filter element in turn, and the injection solution enters the filling process;

[0031] Step 4: The empty bag is sent into the fixture of the filling equipment with a fixture, and the filling volume is set in the filling equipment. The filling hose is centered by the center positioning device. When the filling nozzle reaches the lowest limit position, the length of the tube is checked, and whether there is a mouth tube. If an error signal appears, the corresponding filling position will not perform filling of this bag. When the station moves down, the filling nozzle is inserted into the mouth tube of the bag, and the filling valve is opened immediately to fill the liquid medicine into the bag. When the filling volume is reached, the mass flow meter gives a signal to close the filling valve through the control system, and the filling head moves upward under the drive mechanism to end the filling;

[0032] Step 5: Then cover and take out the bag for wet heat sterilization. The conditions for wet heat sterilization are: 121℃, time 12min, F0 value ≥12;

[0033] Step 6: Quality inspection;

[0034] Step 7: Packing and storage.

[0035] Example 2

[0036] The present invention provides an embodiment: a piracetam composition injection, which comprises the following components, by mass percentage: 4% of piracetam, 1% of sodium chloride, 0.6% of brain protein hydrolysate, 0.2% of glutamic acid, 0.1% of sodium ethacrynate, 0.08% of anisodamine, 0.02-0.035% of activated carbon for injection, and the balance is water for injection.

[0037] A method for preparing a piracetam composition injection, comprising the piracetam composition injection as described above, and the steps are as follows:

[0038] Step 1: Weigh the required weight of raw materials according to the proportion and set aside;

[0039] Step 2: Sodium chloride is put into a concentrated preparation tank containing water for injection. The mass ratio of sodium chloride to water for injection is 1:10. The temperature of the water for injection is 85°C. After sufficient stirring, piracetam is added and stirred to dissolve. 75% of the formula amount of activated carbon for injection is added and continued stirring. The mixture is boiled for 25 minutes, cooled naturally for 10 minutes, and then circulated for 10 minutes. The mixture is then filtered under pressure with a filter and the filtered solution is pumped into a diluted preparation tank.

[0040] Step 3: Add water for injection to 82% of the total amount in the dilution tank, add the remaining activated carbon for injection, stir well, add water for injection to the full amount, stir and reflux for 15 minutes, measure the pH value, the pH value is required to be 5.0-6.0, if it does not meet the requirements, adjust it with dilute hydrochloric acid or 1M sodium hydroxide, cool to 50°C, filter with a filter and a 0.22μm membrane filter element in turn, and the injection solution enters the filling process;

[0041] Step 4: The empty bag is sent into the fixture of the filling equipment with a fixture, and the filling volume is set in the filling equipment. The filling hose is centered by the center positioning device. When the filling nozzle reaches the lowest limit position, the length of the tube is checked, and whether there is a mouth tube. If an error signal appears, the corresponding filling position will not perform filling of this bag. When the station moves down, the filling nozzle is inserted into the mouth tube of the bag, and the filling valve is opened immediately to fill the liquid medicine into the bag. When the filling volume is reached, the mass flow meter gives a signal to close the filling valve through the control system, and the filling head moves upward under the drive mechanism to end the filling;

[0042] Step 5: Then cover and take out the bag, and carry out moist heat sterilization. The conditions for moist heat sterilization are: 123℃, time 20min, F0 value ≥12;

[0043] Step 6: Quality inspection;

[0044] Step 7: Packing and storage.

[0045] Example 3

[0046] The present invention provides an embodiment: a piracetam composition injection, which comprises the following components, by mass percentage: 3.2% of piracetam, 0.85% of sodium chloride, 0.5% of brain protein hydrolysate, 0.1% of glutamic acid, 0.08% of sodium ethacrynate, 0.06% of anisodamine, 0.025% of activated carbon for injection, and the balance is water for injection.

[0047] A method for preparing a piracetam composition injection, comprising the piracetam composition injection as described above, and the steps are as follows:

[0048] Step 1: Weigh the required weight of raw materials according to the proportion and set aside;

[0049] Step 2: Sodium chloride is put into a concentrated preparation tank containing water for injection. The mass ratio of sodium chloride to water for injection is 1:8.5. The temperature of the water for injection is 75°C. After sufficient stirring, piracetam is added and stirred to dissolve. 68% of the formula amount of activated carbon for injection is added and continued stirring. The mixture is boiled for 20 minutes, cooled naturally for 10 minutes, and then circulated for 10 minutes. The mixture is then filtered under pressure with a filter and the filtered solution is pumped into a diluted preparation tank.

[0050] Step 3: Add water for injection to 80% of the total amount in the dilution tank, add the remaining activated carbon for injection, stir well, add water for injection to the full amount, stir and reflux for 15 minutes, measure the pH value, the pH value is required to be 5.0-6.0, if it does not meet the requirements, adjust it with dilute hydrochloric acid or 1M sodium hydroxide, cool to 40°C, filter with a filter and a 0.22μm membrane filter element in turn, and the injection solution enters the filling process;

[0051] Step 4: The empty bag is sent into the fixture of the filling equipment with a fixture, and the filling volume is set in the filling equipment. The filling hose is centered by the center positioning device. When the filling nozzle reaches the lowest limit position, the length of the tube is checked, and whether there is a mouth tube. If an error signal appears, the corresponding filling position will not perform filling of this bag. When the station moves down, the filling nozzle is inserted into the mouth tube of the bag, and the filling valve is opened immediately to fill the liquid medicine into the bag. When the filling volume is reached, the mass flow meter gives a signal to close the filling valve through the control system, and the filling head moves upward under the drive mechanism to end the filling;

[0052] Step 5: Then cover and take out the bag, and carry out moist heat sterilization. The conditions for moist heat sterilization are: 121℃, time 15min, F0 value ≥12;

[0053] Step 6: Quality inspection;

[0054] Step 7: Packing and storage.

[0055] Table 1 is a table of performance indicators of the injection solutions of Example 1, Example 2 and Example 3.

[0056]

[0057] The embodiments of the present invention are described in detail above, but the present invention is not limited to the above embodiments, and various changes can be made within the knowledge scope of those skilled in the art without departing from the spirit of the present invention.

Claims

1. A piracetam composition injection, characterized in that: The invention comprises the following components in percentage by mass: 3-4% of piracetam, 0.8-1% of sodium chloride, 0.5-0.6% of brain protein hydrolysate, 0.1-0.2% of glutamic acid, 0.05-0.1% of sodium ethacrynate, 0.04-0.08% of scopolamine, 0.02-0.035% of activated carbon for injection, and the balance is water for injection.

2. The piracetam composition injection according to claim 1, characterized in that: The composition includes the following components in percentage by mass: 3% of piracetam, 0.8% of sodium chloride, 0.5% of brain protein hydrolysate, 0.1% of glutamic acid, 0.05% of sodium ethacrynate, 0.04% of anisodamine, 0.02% of activated carbon for injection, and the balance is water for injection.

3. The piracetam composition injection according to claim 1, characterized in that: The composition comprises the following components in percentage by mass: 4% of piracetam, 1% of sodium chloride, 0.6% of brain protein hydrolysate, 0.2% of glutamic acid, 0.1% of sodium ethacrynate, 0.08% of scopolamine, 0.02-0.035% of activated carbon for injection, and the balance is water for injection.

4. The piracetam composition injection according to claim 1, characterized in that: The purity of piracetam is not less than 99%; the purity of sodium chloride is not less than 99.5%.

5. A method for preparing a piracetam composition injection, characterized in that The method comprises the piracetam composition injection according to claim 1, wherein the steps are as follows: Step 1: Weigh the required weight of raw materials according to the proportion and set aside; Step 2: Sodium chloride is put into a concentrated preparation tank containing water for injection, and after sufficient stirring, piracetam is added, stirred to dissolve, and 65-75% of the formula amount of activated carbon for injection is added, and stirring is continued. The mixture is boiled for 10-25 minutes, cooled naturally for 10 minutes, and then circulated internally for 10 minutes, and then filtered under pressure with a filter. The filtered solution is pumped into a dilute preparation tank; Step 3: Add water for injection to 78-82% of the total amount in the dilution tank, add the remaining activated carbon for injection, stir well, add water for injection to the full amount, stir and reflux for 15 minutes, measure the pH value, cool to 40-50℃, filter under pressure with a filter and a 0.22μm membrane filter element in turn, and the injection solution enters the filling process; Step 4: The empty bag is sent into the fixture of the filling equipment with a fixture, and the filling volume is set in the filling equipment. The filling hose is centered by the center positioning device. When the filling nozzle reaches the lowest limit position, the length of the tube is checked, and whether there is a mouth tube. If an error signal appears, the corresponding filling position will not perform filling of this bag. When the station moves down, the filling nozzle is inserted into the mouth tube of the bag, and the filling valve is opened immediately to fill the liquid medicine into the bag. When the filling volume is reached, the mass flow meter gives a signal to close the filling valve through the control system, and the filling head moves upward under the drive mechanism to end the filling; Step 5: Then cover and take out the bag for wet heat sterilization; Step 6: Quality inspection; Step 7: Packing and storage.

6. The method for preparing the piracetam composition injection according to claim 5, characterized in that: In step 2, the mass ratio of sodium chloride to water for injection is 1:8-10; the temperature of the water for injection is 70-85°C.

7. The method for preparing the piracetam composition injection according to claim 5, characterized in that: The pH value requirement in step 3 is 5.0-6.

0. If it does not meet the requirement, adjust it with dilute hydrochloric acid or 1M sodium hydroxide.

8. The method for preparing the piracetam composition injection according to claim 5, characterized in that: In step 5, the moist heat sterilization treatment adopts any one of boiling sterilization, pasteurization, high-pressure steam sterilization, circulating steam sterilization or intermittent steam sterilization; the conditions of moist heat sterilization are: 120-123°C, time 12-20min, F0 value ≥12.

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