An injection containing L-carnitine and a preparation method thereof

Abstract

The present invention relates to the technical field of drug improvement, and specifically provides an injection containing L-carnitine and a preparation method thereof, wherein the injection containing L-carnitine comprises the following raw materials: L-carnitine with a mass fraction of 16-22%, coenzyme Q10 with a mass fraction of 1.7-2.8%, a Chinese medicine extract with a mass fraction of 27-36%, and normal saline to make up the remaining mass fraction. The present invention further experiments on the basis of the combination of L-carnitine and Chinese medicine mentioned in the background technology, on the one hand, expands the types of Chinese medicines that can be used in combination and forms a synergistic compound, and on the other hand, finds that the injection of L-carnitine, coenzyme Q10 and Chinese medicine extract after mixing is better than the injection of each separately, and it is speculated that coenzyme Q10 and Chinese medicine extract improve the stability of L-carnitine, and the coordination effect of the mixed injection is more obvious than the injection of each separately.

Description

Technical Field

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

[0002] L-Carnitine is a natural substance in the body that is essential for mammalian energy metabolism. Its main function is to promote lipid metabolism. It can bring long-chain fatty acids into the mitochondrial matrix and promote their oxidative decomposition to provide energy for cells, and it can also export short-chain fatty acyl groups produced in mitochondria. L-Carnitine is the main energy source for muscle cells, especially myocardial cells. It is the main source of energy for the brain, kidneys and many tissues and organs that rely on fat oxidation. Therefore, L-Carnitine plays a very important role in the body's energy metabolism. In clinical practice, L-Carnitine injection is mainly suitable for long-term dialysis patients with chronic renal failure, and a series of complications caused by secondary carnitine deficiency, such as cardiomyopathy, bone disease, arrhythmia, hyperlipidemia, hypotension and muscle spasm during dialysis.

[0003] The combination of L-carnitine and traditional Chinese medicine is also a direction to improve the therapeutic effect of L-carnitine. Taking pediatric viral myocarditis as an example, Li Bin's "Observation on the Efficacy of Astragalus Injection and L-carnitine in the Treatment of 96 Cases of Acute Viral Myocarditis in Children", Zhang Meifang's "Analysis of the Efficacy of L-carnitine Combined with Astragalus Injection in the Treatment of Acute Viral Myocarditis" and Yang Zhongwen et al.'s "Observation on the Efficacy of L-carnitine and Astragalus in the Treatment of Viral Myocarditis in Children" all gave the possibility of the combination of L-carnitine and traditional Chinese medicine. In order to further enhance the effect of L-carnitine, further improvement of the coordination between L-carnitine and traditional Chinese medicine also needs to be explored.

[0004] Therefore, how to improve the therapeutic effect of L-carnitine injection on myocarditis 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 present invention aims to provide an injection containing L-carnitine and a preparation method thereof.

[0006] The present invention provides an injection containing L-carnitine, wherein the injection containing L-carnitine comprises the following raw materials:

[0007] 16-22% L-carnitine, 1.7-2.8% coenzyme Q10, 27-36% Chinese herbal medicine extract and normal saline to make up the rest;

[0008] The preparation method of the Chinese medicine extract comprises the following steps:

[0009] 13-19% by weight of Codonopsis pilosula, 15-22% by weight of Astragalus membranaceus, 5-12% by weight of Salvia miltiorrhiza, 6-10% by weight of Schisandra chinensis, 11-16% by weight of Panax notoginseng and the balance of pure water are added, 80% ethanol with a mass 10 times the mass of the above medicinal materials is added, soaked at 55°C for 24 hours, then added into a flash extractor, extracted at a speed of 8000 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 70°C and a vacuum degree of 800 mbar until no liquid continuously drips out, 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.

[0010] Furthermore, the mass fraction of the L-carnitine is 19%.

[0011] Furthermore, the mass fraction of the coenzyme Q10 is 2.4%.

[0012] Furthermore, the mass fraction of the traditional Chinese medicine extract is 32%.

[0013] Furthermore, the mass fraction of the Codonopsis pilosula is 16%.

[0014] Furthermore, the mass fraction of the astragalus is 18%.

[0015] Furthermore, the mass fraction of the Salvia miltiorrhiza is 9%.

[0016] Furthermore, the mass fraction of Schisandra chinensis is 8%.

[0017] Furthermore, the mass fraction of Panax notoginseng is 13%.

[0018] The present invention can bring the following beneficial effects:

[0019] L-carnitine can improve the energy supply of tissues and organs by increasing energy production, thereby improving the energy supply of the body; coenzyme Q10 can increase coronary blood flow, promote myocardial contraction, enhance endurance, slow down heart rate, and reduce oxygen consumption, and is suitable for the treatment of viral myocarditis in the recovery period; the present invention further experiments on the basis of the combined use of L-carnitine and traditional Chinese medicine mentioned in the background technology, on the one hand, expands the types of traditional Chinese medicines that can be used in combination and forms a synergistic compound, and on the other hand, it is found that the therapeutic effect of mixing L-carnitine, coenzyme Q10 and traditional Chinese medicine extracts and injecting them is better than injecting them separately. It is speculated that coenzyme Q10 and traditional Chinese medicine extracts improve the stability of L-carnitine, and the synergistic effect of mixed injection is more obvious than that of separate injections.

[0020] The codonopsis pilosula, astragalus, salvia miltiorrhiza, schisandra chinensis and panax notoginseng in the injection containing L-carnitine of the present invention and the preparation method thereof are extracted by using the unique extraction process parameters of the present invention to obtain a Chinese medicine extract containing L-carnitine and coenzyme Q10. The parameters of the scheme of the present invention are related and should be viewed as a whole. DETAILED DESCRIPTION

[0021] 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.

[0022] In the present invention, L-carnitine was purchased from Dandong Yichuang Pharmaceutical Co., Ltd. as a pure product for injection; coenzyme Q10 was purchased from Xi'an Zhengte Biomedicine Technology Co., Ltd. as a 98% powder; Codonopsis pilosula, Astragalus membranaceus, Salvia miltiorrhiza, Schisandra chinensis and Panax notoginseng were all purchased from Yunnan Zhenbutong Agricultural Technology Co., Ltd. with a water content of 10%, and Panax notoginseng was the fleshy root part; the flash extractor was purchased from Beijing Haifuda Technology Co., Ltd., model: RCXY-JHBE-50V, and was used according to the standard volume of 5L; the titanium rod filter was purchased from Wuxi Fengnuochang Electromechanical Technology Co., Ltd., model FNCTL-15X-40C; and the physiological saline was 0.9% physiological saline for injection.

[0023] 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%.

[0024] The preferred implementation is as follows:

[0025] Embodiment 1:

[0026] The injection containing L-carnitine is prepared by mixing the raw materials including the following proportions:

[0027] 19% L-carnitine, 2.4% coenzyme Q10, 32% Chinese herbal medicine extract and the rest of the mass fraction is made up of normal saline;

[0028] The preparation method of the Chinese medicine extract is as follows:

[0029] 16% by mass of Codonopsis pilosula, 18% by mass of Astragalus membranaceus, 9% by mass of Salvia miltiorrhiza, 8% by mass of Schisandra chinensis, 13% by mass of Panax notoginseng and the balance of pure water are added, 80% ethanol with a mass of 10 times the mass of the above medicinal materials is soaked at 55°C for 24 hours, then added into a flash extractor, extracted at a speed of 8000 r / min for 30 seconds, and then filtered through 200 mesh to obtain a coarse filtrate extract; the coarse filtrate extract is distilled under reduced pressure at 70°C and a vacuum degree of 800 mbar until no liquid continuously drips out, 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.

[0030] Embodiment 2-17:

[0031] The only difference between Example 2 and Example 1 is that the mass fraction of L-carnitine is 16%;

[0032] The only difference between Example 3 and Example 1 is that the mass fraction of L-carnitine is 22%;

[0033] The only difference between Example 4 and Example 1 is that the mass fraction of coenzyme Q10 is 1.7%;

[0034] The only difference between Example 5 and Example 1 is that the mass fraction of coenzyme Q10 is 2.8%;

[0035] The only difference between Example 6 and Example 1 is that the mass fraction of the Chinese herbal medicine extract is 27%;

[0036] The only difference between Example 7 and Example 1 is that the mass fraction of the Chinese herbal medicine extract is 36%;

[0037] The only difference between Example 8 and Example 1 is that the mass fraction of Codonopsis pilosula is 13%;

[0038] The only difference between Example 9 and Example 1 is that the mass fraction of Codonopsis pilosula is 19%;

[0039] The only difference between Example 10 and Example 1 is that the mass fraction of Astragalus is 15%;

[0040] The only difference between Example 11 and Example 1 is that the mass fraction of Astragalus is 22%;

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

[0042] The only difference between Example 13 and Example 1 is that the mass fraction of Salvia miltiorrhiza is 12%;

[0043] The only difference between Example 14 and Example 1 is that the mass fraction of Schisandra chinensis is 6%;

[0044] The only difference between Example 15 and Example 1 is that the mass fraction of Schisandra chinensis is 10%;

[0045] The only difference between Example 16 and Example 1 is that the mass fraction of Panax notoginseng is 11%;

[0046] The only difference between Example 17 and Example 1 is that the mass fraction of Panax notoginseng is 16%.

[0047] Comparative Examples 1-27:

[0048] The difference between Comparative Example 1 and Example 1 is that the mass fraction of L-carnitine is 10%;

[0049] The difference between Comparative Example 2 and Example 1 is that the mass fraction of L-carnitine is 30%;

[0050] The only difference between Comparative Example 3 and Example 1 is that the mass fraction of coenzyme Q10 is 0.5%;

[0051] The only difference between Comparative Example 4 and Example 1 is that the mass fraction of coenzyme Q10 is 4%;

[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 50%;

[0054] The difference between Comparative Example 7 and Example 1 is that the mass fraction of Codonopsis pilosula is 6%;

[0055] The difference between Comparative Example 8 and Example 1 is that the mass fraction of Codonopsis pilosula is 30%;

[0056] The only difference between Comparative Example 9 and Example 1 is that the mass fraction of Astragalus is 7%;

[0057] The only difference between Comparative Example 10 and Example 1 is that the mass fraction of Astragalus is 30%;

[0058] The only difference between Comparative Example 11 and Example 1 is that the mass fraction of Salvia miltiorrhiza is 2%;

[0059] The difference between Comparative Example 12 and Example 1 is that the mass fraction of Salvia miltiorrhiza is 20%;

[0060] The difference between Comparative Example 13 and Example 1 is that the mass fraction of Schisandra chinensis is 3%;

[0061] The difference between Comparative Example 14 and Example 1 is that the mass fraction of Schisandra chinensis is 20%;

[0062] The only difference between Comparative Example 15 and Example 1 is that the mass fraction of Panax notoginseng is 5%;

[0063] The only difference between Comparative Example 16 and Example 1 is that the mass fraction of Panax notoginseng is 25%;

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

[0065] The difference between Comparative Example 18 and Example 1 is that L-carnitine and coenzyme Q10 are replaced with equal mass of physiological saline;

[0066] The difference between Comparative Example 19 and Example 1 is that the coenzyme Q10 and the Chinese medicine extract are replaced with equal mass of physiological saline;

[0067] The difference between Comparative Example 20 and Example 1 is that the coenzyme Q10 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 Astragalus, Salvia miltiorrhiza, Schisandra chinensis and Panax notoginseng are replaced with Codonopsis pilosula of equal mass;

[0070] The difference between Comparative Example 23 and Example 1 is that Codonopsis pilosula, Salvia miltiorrhiza, Schisandra chinensis and Panax notoginseng are replaced with Astragalus membranaceus of equal mass;

[0071] The difference between Comparative Example 24 and Example 1 is that Codonopsis pilosula, Astragalus membranaceus, Schisandra chinensis and Panax notoginseng are replaced with Salvia miltiorrhiza of equal mass;

[0072] The difference between Comparative Example 25 and Example 1 is that Codonopsis pilosula, Astragalus membranaceus, Salvia miltiorrhiza and Panax notoginseng are replaced with Schisandra chinensis of equal mass;

[0073] The difference between Comparative Example 26 and Example 1 is that Codonopsis pilosula, Astragalus membranaceus, Salvia miltiorrhiza and Schisandra chinensis are replaced with Panax notoginseng of equal mass;

[0074] The difference between Comparative Example 27 and Example 1 is that Comparative Examples 17 to 19 are used at intervals of 1 hour.

[0075] A blank sample was prepared, and physiological saline of the same mass as that in Example 1 was used.

[0076] The present invention uses the content of cardiac troponin T in the serum of each volunteer to correspond to the treatment of myocarditis, and 0-0.15 is considered to be cured. 45 volunteers are 27-year-old males, all of whom suffer from viral myocarditis of similar degree. The entrusted hospital uses the cTnT detection kit of Su Xie No. 20162400281 to use the immune enhancement turbidimetry method to measure the content of cardiac troponin T, i.e., cTnT, in the serum of each volunteer in vitro, which is 0.63 μg / L;

[0077] 10 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 fifth drip, the content of cardiac troponin T in the serum of each volunteer was measured in μg / L, with 2 decimal places. The test results are shown in Table 1.

[0078] Table 1: Test results of cardiac troponin T content in the serum of volunteers corresponding to each example:

[0079]

[0080] It can be seen from the data in Table 1 that, under the same treatment cycle, compared with other examples, the content of cardiac troponin T in the serum of the corresponding volunteers treated with the injection containing L-carnitine according to the embodiments of the present invention, especially the injection prepared by the preparation method thereof according to Embodiment 1 of the present invention, is the lowest; that is, the L-carnitine injection according to the embodiment of the present invention, especially the improved L-carnitine injection according to Embodiment 1 of the present invention, has the best therapeutic effect on myocarditis.

[0081] The above description is only an embodiment of the present invention and is not intended to limit the present invention. For those skilled in the art, the present invention may have various modifications and changes. Any modification, equivalent substitution, improvement, etc. made within the spirit and principle of the present invention should be included in the scope of the claims of the present invention.

Claims

1. An injection containing L-carnitine, characterized in that: The L-carnitine-containing injection comprises the following raw materials: 16-22% L-carnitine, 1.7-2.8% coenzyme Q10, 27-36% Chinese herbal medicine extract and normal saline to make up the rest; The preparation method of the Chinese medicine extract comprises the following steps: 13-19% by weight of Codonopsis pilosula, 15-22% by weight of Astragalus membranaceus, 5-12% by weight of Salvia miltiorrhiza, 6-10% by weight of Schisandra chinensis, 11-16% by weight of Panax notoginseng and the balance of pure water are added, 80% ethanol with a mass 10 times the mass of the above medicinal materials is added, soaked at 55°C for 24 hours, then added into a flash extractor, extracted at a speed of 8000 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 70°C and a vacuum degree of 800 mbar until no liquid continuously drips out, 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 L-carnitine injection according to claim 1, characterized in that: The mass fraction of the L-carnitine is 19%.

3. The L-carnitine-containing injection according to claim 1, characterized in that: The mass fraction of the coenzyme Q10 is 2.4%.

4. The L-carnitine-containing injection according to claim 1, characterized in that: The mass fraction of the traditional Chinese medicine extract is 32%.

5. The L-carnitine-containing injection according to claim 1, characterized in that: The mass fraction of the Codonopsis pilosula is 16%.

6. The L-carnitine-containing injection according to claim 1, characterized in that: The mass fraction of the astragalus root is 18%.

7. The L-carnitine-containing injection according to claim 1, characterized in that: The mass fraction of the salvia miltiorrhiza is 9%.

8. The L-carnitine-containing injection according to claim 1, characterized in that: The mass fraction of the Schisandra chinensis chinensis is 8%.

9. The L-carnitine-containing injection according to claim 1, characterized in that: The mass fraction of the Panax notoginseng is 13%.

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