A kind of injection containing piracetam and preparation method thereof

Abstract

The present invention relates to the technical field of drug improvement, and specifically provides an injection containing piracetam and a preparation method thereof, wherein the injection containing piracetam comprises the following raw materials: 14-21% piracetam by mass, 3-5% sterile porcine brain peptide by mass, 25-33% Chinese medicine extract by mass, and normal saline to make up the remaining mass fraction. Musk, antler powder, Korean red ginseng, cassia twig and chuanxiong in the injection containing piracetam and the preparation method thereof are extracted by using the unique extraction process parameters of the present invention to obtain a Chinese medicine extract of piracetam and sterile porcine brain peptide.

Description

Technical Field

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

[0002] Piracetam, also known as brain rehabilitation in Chinese, is a kind of medicine that promotes thinking and memory. It has a protective effect on brain damage and can promote the recovery of damaged brain. Brain damage includes damage to the structure and function of the brain caused by various reasons, including cerebrovascular disease, tumors, inflammation and trauma. After surgery, piracetam and other drugs are needed for further damage repair treatment. The values ​​of human high mobility group protein B1 (HMGB-1) and human insulin-like growth factor 1 (IGF-1) in serum are often used in clinical practice to evaluate the therapeutic rehabilitation effect. The lower the HMGB-1 value and the higher the IGF-1 value, the better the therapeutic rehabilitation effect.

[0003] In order to enhance the therapeutic effect, a number of studies on the combined use of piracetam and traditional Chinese medicine have been carried out, such as Mu Jinlin's "Observation on the Efficacy of Shuxuening Injection Combined with Piracetam Injection in the Treatment of Cerebral Infarction", Xie Xiaoyong et al.'s "Observation on the Efficacy of Breviscapine Combined with Piracetam in the Treatment of Moderate Traumatic Brain Injury" and Long Yubo's "Effects of Tongfu Xingshen Decoction Combined with Piracetam Injection on Neurological Function and Serum hs-CRP, NSE, and IL-6 in Patients with Cerebral Hemorrhage", all of which provide directions for the combined use of piracetam and traditional Chinese medicine to treat brain injury.

[0004] Therefore, how to combine traditional Chinese medicine to improve the brain injury treatment effect of piracetam injection has become a hot research direction and an issue that needs to be explored urgently. Summary of the invention

[0005] In order to solve the above problems, the object of the present invention is to provide an injection containing piracetam and a preparation method thereof.

[0006] In one aspect, the present invention provides an injection containing piracetam, wherein the injection containing piracetam comprises the following raw materials:

[0007] 14-21% piracetam by mass, 3-5% sterile porcine brain peptide by mass, 25-33% Chinese herbal medicine extract by mass and normal saline to make up the rest.

[0008] Furthermore, the mass fraction of the piracetam is 17%.

[0009] Furthermore, the mass fraction of the sterile porcine brain peptide is 4%.

[0010] Furthermore, the mass fraction of the traditional Chinese medicine extract is 30%.

[0011] On the other hand, the present invention provides a method for preparing the above-mentioned piracetam-containing injection, comprising the following steps:

[0012] Step 1: prepare the Chinese medicine extract, take 0.8-1.3% of musk, 2.1-3.4% of antler powder, 5-8% of Korean red ginseng, 28-36% of cassia twig, 32-44% of Chuanxiong and make up the balance of pure water, add 80% ethanol with a mass of 13 times the mass of the above medicinal materials, soak at 40°C for 15h, then add to a flash extractor, extract at a speed of 6000r / min for 30s, and then filter through 200 mesh to obtain a coarse filtrate extract; distill the coarse filtrate extract under reduced pressure at 62°C and a vacuum degree of 800mbar until no liquid drips continuously, collect the distillation residue, add activated carbon for injection at 0.005g / mL, sterilize at 115°C for 30min, and filter through a titanium rod filter when cooled to 30°C to obtain the Chinese medicine extract;

[0013] Step 2: Mix 14-21% of the piracetam by mass, 3-5% of the sterile porcine brain peptide by mass, 25-33% of the traditional Chinese medicine extract by mass and normal saline to make up the rest to obtain the piracetam-containing injection.

[0014] Furthermore, the mass fraction of the musk is 1.1%.

[0015] Furthermore, the mass fraction of the velvet antler powder is 2.8%.

[0016] Furthermore, the mass fraction of the Korean red ginseng is 7%.

[0017] Furthermore, the mass fraction of the cassia twig is 32%.

[0018] Furthermore, the mass fraction of the Rhizoma Chuanxiong is 39%.

[0019] The present invention can bring the following beneficial effects:

[0020] The present invention further experiments on the combination of piracetam and traditional Chinese medicine mentioned in the background technology, expands the types of traditional Chinese medicine that can be used in combination and forms a synergistic compound. Piracetam is a cyclic derivative of γ-aminobutyric acid, which promotes the energy synthesis metabolism of the brain by enhancing the conduction of nerve excitation; sterile porcine brain peptide is beneficial to the protein synthesis of nerve cells and their respiratory chain, and at the same time stimulates the production of related hormones; musk has the effects of opening the mind, anti-inflammatory and improving cerebral blood flow; deer antler powder can not only replenish kidney yang, invigorate qi and produce marrow from the perspective of "kidney-brain mutual assistance" in traditional Chinese medicine, but also increase arteriolar blood flow, enhance immune cell activity and promote metabolism; Korean red ginseng can improve the function of the central nervous system and promote nervous system repair; cinnamon twig can dilate blood vessels and improve microcirculation, and can enhance the effect of promoting blood circulation and unblocking collaterals when used in combination with chuanxiong; the above components can act synergistically under the process and proportion of the present invention to enhance the therapeutic effect on brain damage.

[0021] Musk, pilose antler powder, Korean red ginseng, cassia twig and chuanxiong in the piracetam-containing injection and preparation method thereof of the present invention are extracted by using the unique extraction process parameters of the present invention to obtain a Chinese medicine extract of piracetam and sterile porcine brain peptide. The parameters of the scheme of the present invention are related and should be viewed as a whole. DETAILED DESCRIPTION

[0022] In order to more clearly explain the overall concept of the present invention, the overall scheme of the present invention is described in detail in the form of embodiments below; in the following description, a large number of specific details are given to provide a more thorough understanding of the present invention; however, it is obvious to those skilled in the art that the present invention can be implemented without one or more of these details; in other examples, in order to avoid confusion with the present invention, some technical features known in the art are not described.

[0023] In the present invention, piracetam is purchased from Sichuan Weikeqi Biotechnology Co., Ltd. as a pure product for injection, CAS number: 7491-74-9; sterile porcine brain peptide is purchased from Xi'an Fenghe Biotechnology Co., Ltd., which is a 200-mesh sterile powder with a purity of 98%; deer antler powder is sika deer antler powder from Jilin Wanze Deer Industry Co., Ltd.; musk, Korean red ginseng, cassia twig and Chuanxiong are all purchased from Bozhou Chengyitang Biotechnology Co., Ltd., with a water content of 5%, and Korean red ginseng is a second-level good ginseng; a flash extractor is purchased from Beijing Haifuda Technology Co., Ltd., model: RCXY-JHBE-50V, and is used according to the standard volume of 5L; a titanium rod filter is purchased from Wuxi Fengnuochang Electromechanical Technology Co., Ltd., model: FNCTL-15X-40C; and physiological saline is 0.9% physiological saline for injection.

[0024] Unless otherwise specified, all raw material components in the following examples can be purchased from commercial sources, the experimental instruments used are conventional laboratory experimental instruments, and the performance test methods are known in the art. The overall operating space environment is 25°C and the air humidity is 30%.

[0025] The preferred implementation is as follows:

[0026] Embodiment 1:

[0027] The injection containing piracetam was prepared using the following method and components:

[0028] Step 1: prepare the Chinese medicine extract, take 1.1% of musk, 2.8% of pilose antler powder, 7% of Korean red ginseng, 32% of cassia twig, 39% of chuanxiong and pure water to make up the balance, add 80% ethanol with a mass of 13 times the mass of the above medicinal materials, soak at 40°C for 15h, then add to a flash extractor, extract at a speed of 6000r / min for 30s, and then filter through 200 mesh to obtain a coarse filtrate extract; distill the coarse filtrate extract under reduced pressure at 62°C and a vacuum degree of 800mbar until no liquid drips continuously, collect the distillation residue, add activated carbon for injection at 0.005g / mL, sterilize at 115°C for 30min, and filter through a titanium rod filter when cooled to 30°C to obtain the Chinese medicine extract;

[0029] Step 2: Mix 17% of the piracetam by mass, 4% of the sterile porcine brain peptide by mass, 30% of the traditional Chinese medicine extract by mass and normal saline to make up the rest to obtain the piracetam-containing injection.

[0030] Embodiment 2-17:

[0031] The only difference between Example 2 and Example 1 is that the mass fraction of piracetam is 14%;

[0032] The only difference between Example 3 and Example 1 is that the mass fraction of piracetam is 21%;

[0033] The only difference between Example 4 and Example 1 is that the mass fraction of sterile porcine brain peptide is 3%;

[0034] The only difference between Example 5 and Example 1 is that the mass fraction of sterile porcine brain peptide is 5%;

[0035] The only difference between Example 6 and Example 1 is that the mass fraction of the Chinese herbal medicine extract is 25%;

[0036] The only difference between Example 7 and Example 1 is that the mass fraction of the Chinese herbal medicine extract is 33%;

[0037] The only difference between Example 8 and Example 1 is that the mass fraction of musk is 0.8%;

[0038] The only difference between Example 9 and Example 1 is that the mass fraction of musk is 1.3%;

[0039] The only difference between Example 10 and Example 1 is that the mass fraction of velvet antler powder is 2.1%;

[0040] The only difference between Example 11 and Example 1 is that the mass fraction of velvet antler powder is 3.4%;

[0041] The only difference between Example 12 and Example 1 is that the mass fraction of Korean red ginseng is 5%;

[0042] The only difference between Example 13 and Example 1 is that the mass fraction of Korean red ginseng is 8%;

[0043] The only difference between Example 14 and Example 1 is that the mass fraction of cassia twig is 28%;

[0044] The only difference between Example 15 and Example 1 is that the mass fraction of cassia twig is 36%;

[0045] The only difference between Example 16 and Example 1 is that the mass fraction of Chuanxiong is 32%;

[0046] The only difference between Example 17 and Example 1 is that the mass fraction of Chuanxiong is 44%.

[0047] Comparative Examples 1-28:

[0048] The difference between Comparative Example 1 and Example 1 is that the mass fraction of piracetam is 7%;

[0049] The difference between Comparative Example 2 and Example 1 is only that the mass fraction of piracetam is 35%;

[0050] The only difference between Comparative Example 3 and Example 1 is that the mass fraction of sterilized porcine brain peptide is 1%;

[0051] The difference between Comparative Example 4 and Example 1 is that the mass fraction of sterilized porcine brain peptide is 10%;

[0052] The only difference between Comparative Example 5 and Example 1 is that the mass fraction of the Chinese herbal medicine extract is 15%;

[0053] The only difference between Comparative Example 6 and Example 1 is that the mass fraction of the Chinese herbal medicine extract is 45%;

[0054] The difference between Comparative Example 7 and Example 1 is only that the mass fraction of musk is 0.4%;

[0055] The only difference between Comparative Example 8 and Example 1 is that the mass fraction of musk is 2%;

[0056] The only difference between Comparative Example 9 and Example 1 is that the mass fraction of velvet antler powder is 1%;

[0057] The only difference between Comparative Example 10 and Example 1 is that the mass fraction of velvet antler powder is 5%;

[0058] The only difference between Comparative Example 11 and Example 1 is that the mass fraction of Korean red ginseng is 1%;

[0059] The only difference between Comparative Example 12 and Example 1 is that the mass fraction of Korean red ginseng is 15%;

[0060] The difference between Comparative Example 13 and Example 1 is that the mass fraction of cassia twig is 15%;

[0061] The only difference between Comparative Example 14 and Example 1 is that the mass fraction of cassia twig is 42%;

[0062] The difference between Comparative Example 15 and Example 1 is that the mass fraction of Chuanxiong is 15%;

[0063] The only difference between Comparative Example 16 and Example 1 is that the mass fraction of Chuanxiong is 50%;

[0064] The difference between Comparative Example 17 and Example 1 is that the piracetam and the Chinese herbal medicine extract are replaced with equal mass of normal saline;

[0065] The difference between Comparative Example 18 and Example 1 is that piracetam and sterile porcine brain peptide are replaced with equal mass of normal saline;

[0066] The difference between Comparative Example 19 and Example 1 is that the sterile porcine brain peptide and the Chinese medicine extract are replaced with equal mass of normal saline;

[0067] The difference between Comparative Example 20 and Example 1 is that the sterile porcine brain peptide is replaced with an equal mass of normal saline;

[0068] The difference between Comparative Example 21 and Example 1 is that the Chinese herbal medicine extract is replaced with an equal mass of physiological saline;

[0069] The difference between Comparative Example 22 and Example 1 is that the velvet antler powder, Korean red ginseng, cassia twig and Chuanxiong are replaced with musk of equal mass;

[0070] The difference between Comparative Example 23 and Example 1 is that the musk, Korean red ginseng, cassia twig and Chuanxiong are replaced with antler powder of equal mass;

[0071] The difference between Comparative Example 24 and Example 1 is that the musk, antler powder, cassia twig and Chuanxiong are replaced with Korean red ginseng of equal mass;

[0072] The difference between Comparative Example 25 and Example 1 is that the musk, antler powder, Korean red ginseng and Chuanxiong are replaced with cassia twigs of equal mass;

[0073] The difference between Comparative Example 26 and Example 1 is that the musk, antler powder, Korean red ginseng and cassia twig are replaced with chuanxiong of equal mass;

[0074] The difference between Comparative Example 27 and Example 1 is that Korean red ginseng is replaced with American ginseng of equal mass;

[0075] The only difference between Comparative Example 28 and Example 1 is that Chuanxiong is replaced with an equal mass of Salvia miltiorrhiza.

[0076] A blank sample was prepared, and physiological saline of the same mass as that in Example 1 was used.

[0077] The present invention uses the content of HMGB-1 and IGF-1 in the serum of each volunteer to correspond to the treatment of brain injury. The lower the HMGB-1 value and the higher the IGF-1 value, the better the treatment and rehabilitation effect. 46 male volunteers aged 40 and weighing 80 kg all suffered from similar degrees of brain injury. The entrusted hospital used Shanghai Guyan HMGB-1 detection kit and DRG's IGF-1 detection kit to determine the HMGB-1 content of each volunteer's serum by ELISA method, which was 81 μg / L and 103 μg / L.

[0078] 20 mL of the injection solution of each example above was added to 250 mL of normal saline and intravenously dripped into the corresponding volunteers once a day. 6 hours after the 7th drip, the levels of HMGB-1 and IGF-1 in the serum of each volunteer were measured in μg / L, and the test results were rounded. See Table 1.

[0079] Table 1: Test results of HMGB-1 and IGF-1 content in the serum of volunteers in each example:

[0080]

[0081] It can be seen from the data in Table 1 that under the same treatment cycle, compared with other examples, the HMGB-1 content in the serum of the corresponding volunteers treated with the injection containing piracetam according to the embodiments of the present invention, especially Example 1 of the present invention and the injection prepared by the preparation method thereof is the lowest and the IGF-1 content is the highest; that is, the improved piracetam injection according to the embodiments of the present invention, especially Example 1 of the present invention, has the best therapeutic effect on brain injury.

[0082] The above descriptions are merely embodiments of the present invention and are not intended to limit the present invention. For those skilled in the art, the present invention may be subject to various modifications and changes. Any modifications, equivalent substitutions, improvements, etc. made within the spirit and principles of the present invention should be included in the scope of the claims of the present invention.

Claims

1. An injection containing piracetam, characterized in that: The piracetam-containing injection comprises the following raw materials: 14-21% piracetam by mass, 3-5% sterile porcine brain peptide by mass, 25-33% Chinese herbal medicine extract by mass and normal saline to make up the rest; The preparation method of the Chinese medicine extract is as follows: 0.8-1.3% by weight of musk, 2.1-3.4% by weight of pilose antler powder, 5-8% by weight of Korean red ginseng, 28-36% by weight of cassia twig, 32-44% by weight of chuanxiong and the balance of pure water are taken, 80% ethanol with a mass of 13 times the mass of the above medicinal materials is added, soaked at 40°C for 15 hours, then added into a flash extractor, extracted at a speed of 6000 r / min for 30 seconds, and then filtered through 200 mesh to obtain a coarse filtration extract; the coarse filtration extract is distilled under reduced pressure at 62°C and a vacuum degree of 800 mbar until no liquid drips continuously, the distillation residue is collected, activated carbon for injection is added at 0.005 g / mL, sterilized at 115°C for 30 minutes, and filtered through a titanium rod filter when cooled to 30°C to obtain the Chinese medicine extract.

2. The piracetam-containing injection according to claim 1, characterized in that The mass fraction of the piracetam is 17%.

3. The piracetam-containing injection according to claim 1, characterized in that The mass fraction of the sterile porcine brain peptide is 4%.

4. The piracetam-containing injection according to claim 1, characterized in that The mass fraction of the traditional Chinese medicine extract is 30%.

5. A method for preparing an injection containing piracetam as claimed in any one of claims 1 to 4, characterized in that: The steps include: Step 1: prepare the Chinese medicine extract, take 0.8-1.3% of musk, 2.1-3.4% of antler powder, 5-8% of Korean red ginseng, 28-36% of cassia twig, 32-44% of Chuanxiong and make up the balance of pure water, add 80% ethanol with a mass of 13 times the mass of the above medicinal materials, soak at 40°C for 15h, then add to a flash extractor, extract at a speed of 6000r / min for 30s, and then filter through 200 mesh to obtain a coarse filtrate extract; distill the coarse filtrate extract under reduced pressure at 62°C and a vacuum degree of 800mbar until no liquid drips continuously, collect the distillation residue, add activated carbon for injection at 0.005g / mL, sterilize at 115°C for 30min, and filter through a titanium rod filter when cooled to 30°C to obtain the Chinese medicine extract; Step 2: Mix the piracetam with a mass fraction of 14-21%, the sterile porcine brain peptide with a mass fraction of 3-5%, the traditional Chinese medicine extract with a mass fraction of 25-33% and normal saline to make up the rest to obtain the piracetam-containing injection.

6. The method for preparing the piracetam-containing injection according to claim 5, characterized in that: The mass fraction of the musk is 1.1%.

7. The method for preparing the piracetam-containing injection according to claim 5, characterized in that: The mass fraction of the velvet antler powder is 2.8%.

8. The method for preparing the piracetam-containing injection according to claim 5, characterized in that: The mass fraction of the Korean red ginseng is 7%.

9. The method for preparing the piracetam-containing injection according to claim 5, characterized in that: The mass fraction of the cassia twig is 32%.

10. The method for preparing the piracetam-containing injection according to claim 5, characterized in that: The mass fraction of the Rhizoma Chuanxiong is 39%.

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