CN108498474A - A kind of pharmaceutical composition and its preparation method and application comprising Trimetazidine Hydrochloride - Google Patents
A kind of pharmaceutical composition and its preparation method and application comprising Trimetazidine Hydrochloride Download PDFInfo
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- CN108498474A CN108498474A CN201810685548.2A CN201810685548A CN108498474A CN 108498474 A CN108498474 A CN 108498474A CN 201810685548 A CN201810685548 A CN 201810685548A CN 108498474 A CN108498474 A CN 108498474A
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic agents
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- Organic Chemistry (AREA)
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Abstract
The pharmaceutical composition and its preparation method and application comprising Trimetazidine Hydrochloride that the present invention provides a kind of, belongs to field of medicaments.The pharmaceutical composition includes:Trimetazidine Hydrochloride, cornstarch, mannitol, PVP K30, talcum powder, magnesium stearate.Preparation method includes:It counts in parts by weight, by cornstarch, mannitol, 78~82% PVP K30 and Trimetazidine Hydrochloride after mixing, add remaining PVP K30 and carry out wet granulation, and dried at 55~65 DEG C, whole grain is carried out with 14~18 mesh sieve again, obtains dry particl;Dry particl is mixed with talcum powder and magnesium stearate again, tabletting.The reasonable recipe of this pharmaceutical composition, inventor can be used for preparing and prevent or the drug for the treatment of I metallergy diseases the study found that the effect of pharmaceutical composition is to I metallergy diseases is all good.
Description
Technical field
The present invention relates to drug field, in particular to a kind of pharmaceutical composition comprising Trimetazidine Hydrochloride and its
Preparation method and purposes.
Background technology
Type Ⅰ allergy is also known as allergic reaction, is clinical the most common type, its main feature is that:It is mediated by IgE, it is loose thin
The effector cells such as born of the same parents and basophil participate in reacting in a manner of delivery of biologically active medium;Occur soon, to subside also fast;Normal table
It is now physiological dysfunction, and without serious tissue damage;There are apparent individual difference and genetic predisposition.
After anaphylactogen enters body, induction B cell generates IgE antibody.IgE has the affinity of height with target cell, securely
Ground is adsorbed on mast cell, basophil surface.When identical antigen is again introduced into the body of sensitization, combined with IgE antibody,
The series of biochemical reactions of cell membrane will be caused, start the process of two parallel generations:Degranulation Jie new with synthesis
Matter.1. mast cell generates degranulation variation with basophil, many active mediums are released from particle, such as histamine, egg
White hydrolase, heparin, chemotactic factor (CF) etc.;2. cell membrane phospholipid degradation simultaneously, releases arachidonic acid.It is with two approach generations
It thanks, is respectively synthesized prostaglandin, thromboxane A2 and leukotrienes, platelet activating factor.Various media are disseminated to blood flow
Whole body acts on the effector organs such as skin, mucous membrane, respiratory tract, causes thin vessels and telangiectasis, capillary permeability
Increase, smooth muscle contraction, glandular secretion increase, eosinophilia, infiltration, can cause mucocutaneous allergy (nettle rash,
Eczema, angioneurotic edema), respiratory tract anaphylaxis reacts (allergic rhinitis, bronchial asthma, laryngeal edema), alimentary canal mistake
Quick disease (food allergy gastroenteritis), systemic anaphylaxis (anaphylactic shock) seriously affect patient's physical and mental health.
And currently, product not all good to type Ⅰ allergy curative effect in the market, in consideration of it, special propose this patent.
Invention content
The purpose of the present invention is to provide a kind of pharmaceutical composition and its preparation method and application, which includes
Trimetazidine Hydrochloride, it is all good to type Ⅰ allergy curative effect.
In order to realize that the above-mentioned purpose of the present invention, spy use following technical scheme:
A kind of pharmaceutical composition including Trimetazidine Hydrochloride, the pharmaceutical composition include that Trimetazidine Hydrochloride and seaweed are more
Sugar.
A kind of pharmaceutical composition, the pharmaceutical composition include:Trimetazidine Hydrochloride, cornstarch, mannitol, povidone
K30, talcum powder, magnesium stearate.
A kind of preparation method of aforementioned pharmaceutical compositions comprising:
Count in parts by weight, by cornstarch, mannitol, 78~82% PVP K30 mixed with Trimetazidine Hydrochloride
After uniformly, add remaining PVP K30 and carry out wet granulation, and dried at 55~65 DEG C, then with 14~18 mesh sieve into
Row whole grain, obtains dry particl;
Dry particl is mixed with talcum powder and magnesium stearate again, preparation.
A kind of pharmaceutical composition of above-mentioned offer prepare prevent or the drug for the treatment of I metallergy diseases in use
On the way.
Compared with prior art, beneficial effects of the present invention are:
This pharmaceutical composition provided by the present application, active component mainly have Trimetazidine Hydrochloride, while further including one
A little pharmaceutically acceptable auxiliary materials, such as cornstarch, mannitol, PVP K30, talcum powder, magnesium stearate.This medicine group
Object reasonable recipe is closed, inventor can be used for the study found that the effect of pharmaceutical composition is to I metallergy diseases is all good
The drug for preventing or treating I metallergy diseases is prepared, is had a extensive future.
Specific implementation mode
Embodiment of the present invention is described in detail below in conjunction with embodiment, but those skilled in the art will
Understand, the following example is merely to illustrate the present invention, and is not construed as limiting the scope of the invention.It is not specified in embodiment specific
Condition person carries out according to conventional conditions or manufacturer's recommended conditions.Reagents or instruments used without specified manufacturer is
The conventional products that can be obtained by commercially available purchase.
Present embodiment provides a kind of pharmaceutical composition (first chamber), which includes:Hydrochloric acid Sibutramine Hydrochloride he
Piperazine, algal polysaccharides.
Further, it counts in parts by weight, which is 20 parts, the algal polysaccharides are 300~700 parts.
Further, which further includes pharmaceutically acceptable auxiliary material, and auxiliary material is counted in parts by weight includes:
28~38 parts of cornstarch, 25~35 parts of mannitol, 3~7 parts of PVP K30,0.65~1.15 part of talcum powder,
1.0~1.5 parts of magnesium stearate.
Present embodiment also provides a kind of pharmaceutical composition (second chamber), which includes:Hydrochloric acid Sibutramine Hydrochloride
His piperazine, cornstarch, mannitol, PVP K30, talcum powder, magnesium stearate.
Further, it counts in parts by weight, Trimetazidine Hydrochloride is 20 parts, cornstarch is 28~38 parts, mannitol is
25~35 parts, PVP K30 be 3~7 parts, talcum powder is 0.65~1.15 part, magnesium stearate is 1.0~1.5 parts.
Alternatively, counting in parts by weight, Trimetazidine Hydrochloride is 20 parts, cornstarch is 24~34 parts, mannitol be 28~
33 parts, PVP K30 be 4~6 parts, talcum powder is 0.8~1.1 part, magnesium stearate is 1.1~1.4 parts.
Further, which further includes the algal polysaccharides of 300~700 parts by weight.
Present embodiment also provides a kind of preparation method of above-mentioned first chamber and second chamber comprising:
Step S1:Count in parts by weight, by algal polysaccharides, cornstarch, mannitol, 78~82% PVP K30 with
Trimetazidine Hydrochloride after mixing, adds remaining PVP K30 and carries out wet granulation, and dried at 55~65 DEG C,
Whole grain is carried out with 14~18 mesh sieve again, obtains dry particl.
Further, before this step, further include that Trimetazidine Hydrochloride bulk pharmaceutical chemicals be crushed into 50 mesh sieve, mannitol mistake
80 mesh sieve.
Further, preparation method granulation before mixing step in, mixing speed be 250~350rpm, shear velocity 250~
300rpm, 3~8min of mixing time.
Further, during carrying out wet granulation, mixing speed is 250~350rmp, shear velocity 1300
~1700rmp, shear time are 40~80s.
Further, the moisture in dry particl is 2~5%.
Step S2:Dry particl is mixed with talcum powder and magnesium stearate again, preparation.
Further, which is made tablet:Tabletting, mold 5.0 are carried out using ZP14 type rotary pelleting machines
The round deep recessed punchings of~7.0mm, hardness is 30~50N.
The pharmaceutical composition made from above-mentioned preparation method, to I metallergy diseases the effect of, are all good, can be used for making
The standby drug prevented or treat I metallergy diseases, has a extensive future.
The feature and performance of the present invention are described in further detail with reference to embodiments:
Embodiment 1
The present embodiment provides a kind of pharmaceutical composition, component and proportioning are as shown in the table:
Ingredient | Ratio |
Trimetazidine Hydrochloride | 20 |
Cornstarch | 28 |
Mannitol | 35 |
PVPK30 | 4 |
Talcum powder (additional) | 1.15 |
Magnesium stearate (additional) | 1.0 |
10%PVPK30 (additional) | 11 |
The preparation method of the pharmaceutical composition includes:
1) bulk pharmaceutical chemicals pre-process:Trimetazidine Hydrochloride bulk pharmaceutical chemicals crushed 50 mesh sieve, and mannitol crosses 80 mesh sieve.
2) it premixes:Cornstarch, mannitol, PVP K30 and the Trimetazidine Hydrochloride for weighing recipe quantity are placed in wet method system
It in grain machine, is uniformly mixed, parameter when mixing is:Mixing speed 350rpm, shear velocity 250rpm, mixing time 3min.
3) wet granulation:10%PVPK30 adhesives are added and carry out wet granulation, 16 mesh sieve oscillating granulator granulation, granulation
When parameter be:Mixing speed 350rpm, shear velocity 1300rpm, shear time 40s.
4) it dries:It is dried in air dry oven, 65 DEG C of drying temperature, moisture is controlled 2%~5%.
5) whole grain:Whole grain is carried out with 14 mesh of the types of KCK~60 oscillating granulator sieve.
6) total mixed:Converted according to yield, weigh recipe quantity talcum powder and gained after magnesium stearate, with whole grain it is dry
Particle is uniformly mixed, incorporation time 5min.
7) intermediate sample detection, detection project character, content.
8) tabletting:Tabletting, the round deep recessed punching of mold 7.0mm are carried out using ZP14 type rotary pelleting machines, hardness is 40~
50N。
Embodiment 2
The present embodiment provides a kind of pharmaceutical composition, component and proportioning are as shown in the table:
The preparation method of the pharmaceutical composition includes:
1) bulk pharmaceutical chemicals pre-process:Trimetazidine Hydrochloride bulk pharmaceutical chemicals crushed 50 mesh sieve, and mannitol crosses 80 mesh sieve.
2) it premixes:Cornstarch, mannitol, PVP K30 and the Trimetazidine Hydrochloride for weighing recipe quantity are placed in wet method system
It in grain machine, is uniformly mixed, parameter when mixing is:Mixing speed 250rpm, shear velocity 300rpm, mixing time 8min.
3) wet granulation:10%PVPK30 adhesives are added and carry out wet granulation, 16 mesh sieve oscillating granulator granulation, granulation
When parameter be:Mixing speed 250rpm, shear velocity 1700rpm, shear time 80s.
4) it dries:It is dried in air dry oven, 55 DEG C of drying temperature, moisture is controlled 2%~5%.
5) whole grain:Whole grain is carried out with 18 mesh of the types of KCK~60 oscillating granulator sieve.
6) total mixed:Converted according to yield, weigh recipe quantity talcum powder and gained after magnesium stearate, with whole grain it is dry
Particle is uniformly mixed, incorporation time 5min.
7) intermediate sample detection, detection project character, content.
8) tabletting:Tabletting, the round deep recessed punching of mold 5.0mm are carried out using ZP14 type rotary pelleting machines, hardness is 30~
40N。
Embodiment 3
The present embodiment provides a kind of pharmaceutical composition, component and proportioning are as shown in the table:
Ingredient | Ratio |
Trimetazidine Hydrochloride | 20.0 |
Cornstarch | 32.85 |
Mannitol | 30 |
PVPK30 | 5 |
Talcum powder (additional) | 0.9 |
Magnesium stearate (additional) | 1.26 |
10%PVPK30 (additional) | 9.9 |
The preparation method of the pharmaceutical composition includes:
1) bulk pharmaceutical chemicals pre-process:Trimetazidine Hydrochloride bulk pharmaceutical chemicals crushed 50 mesh sieve, and mannitol crosses 80 mesh sieve.
2) it premixes:Cornstarch, mannitol, PVP K30 and the Trimetazidine Hydrochloride for weighing recipe quantity are placed in wet method system
It in grain machine, is uniformly mixed, parameter when mixing is:Mixing speed 300rpm, shear velocity 283rpm, mixing time 5min.
3) wet granulation:10%PVPK30 adhesives are added and carry out wet granulation, 16 mesh sieve oscillating granulator granulation, granulation
When parameter be:Mixing speed 300rpm, shear velocity 1500rpm, shear time 60s.
4) it dries:It is dried in air dry oven, 60 DEG C of drying temperature, moisture is controlled 2%~5%.
5) whole grain:Whole grain is carried out with 16 mesh of the types of KCK~60 oscillating granulator sieve.
6) total mixed:Converted according to yield, weigh recipe quantity talcum powder and gained after magnesium stearate, with whole grain it is dry
Particle is uniformly mixed, incorporation time 5min.
7) intermediate sample detection, detection project character, content.
8) tabletting:Tabletting, the round deep recessed punching of mold 6.0mm are carried out using ZP14 type rotary pelleting machines, hardness is 30~
50N。
Embodiment 4
The present embodiment provides a kind of pharmaceutical composition, component and proportioning are as shown in the table:
Ingredient | Ratio |
Trimetazidine Hydrochloride | 20.0 |
Cornstarch | 32.85 |
Mannitol | 30 |
PVPK30 | 5 |
Talcum powder (additional) | 0.9 |
Magnesium stearate (additional) | 1.26 |
10%PVPK30 (additional) | 9.9 |
Algal polysaccharides | 300.0 |
The preparation method of the pharmaceutical composition and embodiment 3 are almost the same, the difference is that:
2) it premixes:Algal polysaccharides, cornstarch, mannitol, PVP K30 and the Trimetazidine Hydrochloride for weighing recipe quantity are set
It in wet granulator, is uniformly mixed, parameter when mixing is:Mixing speed 300rpm, shear velocity 283rpm, mixing time
5min。
Embodiment 5
The present embodiment provides a kind of pharmaceutical composition, component and proportioning are as shown in the table:
The preparation method of the pharmaceutical composition is consistent with embodiment 4.
Embodiment 6
The present embodiment provides a kind of pharmaceutical composition, component and proportioning are as shown in the table:
Ingredient | Ratio |
Trimetazidine Hydrochloride | 20.0 |
Cornstarch | 32.85 |
Mannitol | 30 |
PVPK30 | 5 |
Talcum powder (additional) | 0.9 |
Magnesium stearate (additional) | 1.26 |
10%PVPK30 (additional) | 9.9 |
Algal polysaccharides | 700.0 |
The preparation method of the pharmaceutical composition is consistent with embodiment 3.
Experimental example
Influence with reference to animal experiment to pharmaceutical composition provided in an embodiment of the present invention to mouse caused by dimethylbenzene xylene inflammation
It illustrates.
One, experimentation:
18~22g ICR male mices 80 are only randomly divided into 8 groups, respectively model group, Dexamethasone group, reality by weight
Apply 1~6 group of example.7 days, once a day, Dexamethasone group dosage 5mg/kg weight are administered in continuous gavage.Examples 1 to 6 group
It is 20mg/kg weight that dosage, which converts into Trimetazidine Hydrochloride,.After last dose 1h, two sides applies 30 μ L before and after every mouse right ear
Caused by dimethylbenzene xylene is scorching, and left ear, which is not coated with, to be compared, and mouse is put to death after 1h, cuts left and right ear, with 8mm diameters card punch respectively same
One position lays round auricle and weighs, using left and right ear difference as swelling.
Two, experimental result
Experimental result is shown in Table 7:
Influence (x ± SD) of 7 present invention of table to mouse caused by dimethylbenzene xylene inflammation
Left ear (mg) | Auris dextra (mg) | Difference (mg) | Inhibiting rate (%) | |
Model group | 8.0±1.6 | 17.5±2.5 | 9.5±2.8 | ~ |
Dexamethasone group | 8.2±1.3 | 12.6±2.9 | 4.4±2.5 | 53.68 |
1 group of embodiment | 8.2±1.6 | 17.5±3.0 | 9.3±3.2 | 2.11 |
2 groups of embodiment | 7.9±1.5 | 17.3±2.9 | 9.4±2.5 | 1.05 |
3 groups of embodiment | 8.0±1.8 | 17.5±3.1 | 9.5±2.8 | 0 |
4 groups of embodiment | 7.9±1.6 | 15.5±2.8 | 7.6±2.3 | 20.00 |
5 groups of embodiment | 8.1±1.5 | 15.0±2.3 | 6.9±2.5 | 27.37 |
6 groups of embodiment | 8.0±1.8 | 14.8±2.8 | 6.8±2.6 | 28.42 |
By table 7 as it can be seen that compared with model group, other than embodiment 3, the different degrees of inhibition two of energy of other embodiment group
Mice auricle swelling caused by toluene.Compared with Examples 1 to 3, the pharmaceutical composition that the embodiment of the present invention 4~6 provides, due to
The addition of algal polysaccharides makes the ability that the pharmaceutical composition inhibits the mice auricle swelling caused by dimethylbenzene be obviously improved.Explanation
Pharmaceutical composition provided by the invention can prevent I metallergy diseases, can be used for preparing and prevent or treat the metamorphosis of I types instead
The drug of answering property disease.
Although illustrate and describing the present invention with specific embodiment, it will be appreciated that without departing substantially from the present invention's
Many other change and modification can be made in the case of spirit and scope.It is, therefore, intended that in the following claims
Including belonging to all such changes and modifications in the scope of the invention.
Claims (10)
1. a kind of pharmaceutical composition including Trimetazidine Hydrochloride, which is characterized in that described pharmaceutical composition includes hydrochloric acid Sibutramine Hydrochloride
His piperazine and algal polysaccharides.
2. pharmaceutical composition according to claim 1, which is characterized in that count in parts by weight, the Trimetazidine Hydrochloride
It it is 300~700 parts for 20 parts, the algal polysaccharides.
3. pharmaceutical composition according to claim 1, which is characterized in that described pharmaceutical composition further includes that can pharmaceutically connect
The auxiliary material received, the auxiliary material is counted in parts by weight includes:
28~38 parts of cornstarch, 25~35 parts of mannitol, 3~7 parts of PVP K30,0.65~1.15 part of talcum powder, tristearin
1.0~1.5 parts of sour magnesium.
4. a kind of pharmaceutical composition, which is characterized in that described pharmaceutical composition includes:Trimetazidine Hydrochloride, cornstarch, sweet dew
Alcohol, PVP K30, talcum powder, magnesium stearate.
5. according to the pharmaceutical composition described in claims 4, which is characterized in that count in parts by weight, the hydrochloric acid Sibutramine Hydrochloride
His piperazine is 20 parts, the cornstarch is 28~38 parts, the mannitol is 25~35 parts, the PVP K30 is 3~7 parts,
The talcum powder is 0.65~1.15 part, the magnesium stearate is 1.0~1.5 parts.
6. according to the pharmaceutical composition described in claims 5, which is characterized in that described pharmaceutical composition further includes 300~
The algal polysaccharides of 700 parts by weight.
7. a kind of preparation method of such as claim 4~6 any one of them pharmaceutical composition, which is characterized in that it includes:
Count in parts by weight, by the cornstarch, the mannitol, 78~82% the PVP K30 and the hydrochloric acid
Trimetazidine after mixing, adds the remaining PVP K30 and carries out wet granulation, and dried at 55~65 DEG C,
Whole grain is carried out with 14~18 mesh sieve again, obtains dry particl;
The dry particl is mixed with the talcum powder and the magnesium stearate again, preparation.
8. the preparation method of pharmaceutical composition according to claim 7, which is characterized in that in the process for carrying out wet granulation
In, mixing speed is 250~350rmp, and shear velocity is 1300~1700rmp, and shear time is 40~80s.
9. the preparation method of pharmaceutical composition according to claim 7, which is characterized in that further include by 300~700 weight
The algal polysaccharides of number and the cornstarch, the mannitol, 78~82% the PVP K30 and the hydrochloric acid Sibutramine Hydrochloride
The step that his piperazine is uniformly mixed.
10. a kind of as claim 1~6 any one of them pharmaceutical composition is preparing prevention or treatment I metallergies
Purposes in the drug of disease.
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Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN111557922A (en) * | 2020-06-28 | 2020-08-21 | 江苏吴中医药集团有限公司 | Trimetazidine hydrochloride preparation and preparation method thereof |
Citations (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN102065869A (en) * | 2008-07-01 | 2011-05-18 | 玛丽诺姆德生物技术公司 | Antiallergic marine biopolymers |
CN107982231A (en) * | 2018-01-03 | 2018-05-04 | 江苏吴中医药集团有限公司 | A kind of Trimetazidine Hydrochloride Tablets in healthy and preparation method thereof |
-
2018
- 2018-06-28 CN CN201810685548.2A patent/CN108498474A/en active Pending
Patent Citations (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN102065869A (en) * | 2008-07-01 | 2011-05-18 | 玛丽诺姆德生物技术公司 | Antiallergic marine biopolymers |
CN107982231A (en) * | 2018-01-03 | 2018-05-04 | 江苏吴中医药集团有限公司 | A kind of Trimetazidine Hydrochloride Tablets in healthy and preparation method thereof |
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
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CN111557922A (en) * | 2020-06-28 | 2020-08-21 | 江苏吴中医药集团有限公司 | Trimetazidine hydrochloride preparation and preparation method thereof |
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