CN113855638A - Rosemastat pharmaceutical preparation - Google Patents

Rosemastat pharmaceutical preparation Download PDF

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Publication number
CN113855638A
CN113855638A CN202111264283.7A CN202111264283A CN113855638A CN 113855638 A CN113855638 A CN 113855638A CN 202111264283 A CN202111264283 A CN 202111264283A CN 113855638 A CN113855638 A CN 113855638A
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cyclodextrin
rosxastat
parts
roxasistat
pharmaceutical preparation
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CN113855638B (en
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刘营营
杨西邈
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Beijing Fuyuan Pharmaceutical Co ltd
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Beijing Fuyuan Pharmaceutical Co ltd
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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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
    • 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
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • 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
    • A61K9/2027—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
    • 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
    • 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
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • 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
    • A61K9/2095—Tabletting processes; Dosage units made by direct compression of powders or specially processed granules, by eliminating solvents, by melt-extrusion, by injection molding, by 3D printing
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06—Antianaemics
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Abstract

The invention relates to a pharmaceutical preparation of roxasistat, which specifically comprises roxasistat, a cyclodextrin derivative, potassium polacriline, a diluent and a disintegrating agent, wherein the particle size d0.9 of the roxasistat is not more than 30 mu m. The Rosemastat pharmaceutical preparation prepared by the invention has good dissolution rate, and the quality and the curative effect of the medicine are guaranteed.

Description

Rosemastat pharmaceutical preparation
Technical Field
The invention relates to a pharmaceutical preparation of a hypoxia inducible factor prolyl hydroxylase inhibitor, in particular to a roxasistat pharmaceutical preparation and a preparation method thereof.
Background
Renal anemia is anemia caused by the development of various Chronic Kidney Diseases (CKD), is often related to relative or absolute deficiency of erythropoietin secreted from renal interstitium, decreased sensitivity of patients to the erythropoietin, shortened service life of red blood cells, changed microenvironment of bone marrow hematopoietic system, iron deficiency and other reasons, and serious renal anemia can increase the death rate of CKD patients. There are about 1.195 million CKD patients in our country, of which about 40 million receive dialysis (or peritoneal dialysis) and are rapidly increasing in two digits per year, so that there are more and more patients in need of treatment of renal anemia.
Rosxastat (RDXT), an oreochromid (fibrigen), AstraZeneca (AstraZeneca) and Astellas (Astellas), was the first globally developed small molecule hypoxia inducible factor prolyl hydroxylase inhibitor for the treatment of renal anemia (CKD). The roxasistat can activate the transcription of related genes by stabilizing HIF, inhibiting the degradation of the HIF, generating corresponding physiological response, moderately increasing the concentration of erythropoietin, improving the sensitivity of Erythropoietin (EPO) receptors, coordinating the generation of red blood cells, reducing the level of hepcidin, increasing the content and activity of transferrin receptors, promoting the absorption and utilization of iron and having good tolerance. The medicine is the first global original medicine which is hatched in China and approved in China for the first time, and is used for chronic renal failure anemia depending on dialysis.
The chemical name of roxasistat is [ (4-hydroxy-1-methyl-7-phenoxy-isoquinoline-3-carbonyl) -amino ] -acetic acid. The structural formula is as follows:
Figure BDA0003324983670000011
the water solubility of the roxasistat is poor, the solubility of the roxasistat in water is only 1.71mg/L, and the roxasistat is a poorly soluble drug. WO 2004108681a1 discloses a rosxastat compound. WO 2014014835a2 discloses several crystalline forms of rasagile other than amorphous rasagile such as crystalline anhydrate form a, hemihydrate form B, hexafluoropropan 2-ol solvate form C and mixed DMSO/water solvate form D. This application also mentions several crystalline and amorphous salts of roxasistat, for example salts with the alkali metals sodium and potassium, with the alkaline earth metals calcium and magnesium, with the amino acids L-arginine and L-lysine, with the amines ethanolamine, diethanolamine, tromethamine and triethylamine, and with hydrochloric acid, sulfuric acid and methanesulfonic acid. WO2014197660a1 discloses the use of an effective amount of a photostabilizer to increase the stability of a pharmaceutical formulation of rosixatase such that the photolysis product of the pharmaceutical formulation is less than about 0.2% w/w. However, the problem of indissolvability of the roxasistat is not solved, so that how to prepare the roxasistat into a pharmaceutical preparation overcomes the indissolvability problem of the roxasistat, and the good dissolution rate is needed for solving the problem to be solved.
Disclosure of Invention
The invention provides a pharmaceutical preparation of rosmarinic acid, aiming at solving the problems of poor water solubility and poor dissolution effect of rosmarinic acid. The pharmaceutical preparation of the roxasistat prepared by the invention has better dissolution rate. The pharmaceutical preparation specifically comprises roxasistat, cyclodextrin derivatives, polacrilin potassium, a diluent and a disintegrating agent, wherein the particle size d0.9 of the roxasistat is not more than 30 mu m.
In the case of a solid preparation, the dissolution rate of the drug directly affects the absorption rate of the drug, and according to the Noyes-Whitney equation, reducing the particle size of the active ingredient is one of effective methods for increasing the dissolution rate of the drug. In general, a decrease in particle size and an increase in surface area contribute to an increase in dissolution. In order to solve the problems of poor water solubility and low dissolution rate of the preparation of the Rosesarta, the particle size d0.9 of the Rosesarta is reduced to be less than 30 mu m. Although the particle size reduction can increase dissolution, the problem of dissolution of the pharmaceutical preparation of rosxata cannot be solved well, and further research on the prescription for improving the dissolution of the pharmaceutical preparation of rosxata is needed. Through a great deal of research, the inventor unexpectedly discovers that the dissolution problem of the pharmaceutical preparation of the roxasistat can be well solved by reducing the particle size d0.9 of the roxasistat to be below 30 mu m and adding the cyclodextrin derivative and the polacrilin potassium in a matching way, and the quality and the curative effect of the medicine are guaranteed.
In some embodiments, the particle size d0.9 of the rosxastat in the pharmaceutical formulation of rosxastat described above is 10-20 μm.
In the above pharmaceutical preparation of rosxastat, the cyclodextrin derivative is selected from one or more of hydroxyethyl-beta-cyclodextrin, hydroxypropyl-beta-cyclodextrin, dihydroxypropyl-beta-cyclodextrin, methyl-beta-cyclodextrin, glucose-cyclodextrin, maltose-cyclodextrin, maltotriose-cyclodextrin, and carboxymethyl-cyclodextrin; preferably, the cyclodextrin derivative is hydroxypropyl- β -cyclodextrin.
In the Rosesatat pharmaceutical preparation, the disintegrant is one or more of sodium carboxymethyl starch, low-substituted hydroxypropyl cellulose, crospovidone and croscarmellose sodium.
In the roxasistat pharmaceutical preparation, the diluent is one or more of microcrystalline cellulose, mannitol, lactose, pregelatinized starch, sucrose, sorbitol and calcium hydrogen phosphate.
In the Rosesarta pharmaceutical preparation, the pharmaceutical preparation comprises the following components by mass: 20-100 parts of roxasistat, 50-100 parts of cyclodextrin derivative, 3-8 parts of polacrilin potassium, 250 parts of diluent 150 and 3-8 parts of disintegrant.
In some embodiments, the preferred pharmaceutical formulation of rosxastat comprises the following components by mass: 20-100 parts of roxasistat, 50-100 parts of hydroxypropyl-beta-cyclodextrin, 3-8 parts of polacrilin potassium, 200 parts of lactose, 30-50 parts of microcrystalline cellulose and 3-8 parts of croscarmellose sodium.
In some embodiments, the pharmaceutical formulation further comprises a binder and/or a lubricant.
In the roxasistat medicinal preparation, the adhesive is one or more of hydroxypropyl cellulose, hydroxypropyl methylcellulose, sodium carboxymethylcellulose and povidone.
In the roxasistat pharmaceutical preparation, the lubricant is one or more of superfine silica powder, talcum powder, magnesium stearate and sodium stearyl fumarate.
The invention also provides a method for preparing a pharmaceutical preparation of roxasistat, which comprises the following steps:
(1) uniformly mixing the roxasistat, the cyclodextrin derivative, the polacrilin potassium, the diluent and the disintegrant to prepare a mixture;
(2) adding purified water into the mixture obtained in the step (1), granulating, and finishing granules to obtain medicine granules;
(3) tabletting the drug granules.
The step (1) further comprises a step of adding a binder.
The step (3) further comprises the step of uniformly mixing the drug particles with the lubricant.
Compared with the prior art, the invention has the beneficial effects that:
1. the invention reduces the particle size d0.9 of the roxasistat to be below 30 mu m, and adds cyclodextrin derivative and polacrilin potassium auxiliary material, which can solve the problem of poor dissolution effect of the roxasistat.
2. In the Rosesarta pharmaceutical preparation, when the cyclodextrin derivative is further selected to be hydroxypropyl-beta-cyclodextrin, and is matched with potassium polacrilin, and the particle size d0.9 of Rosesarta is controlled to be reduced to be less than 30 mu m, the Rosesarta pharmaceutical preparation with good dissolution can be obtained.
3. Furthermore, in the pharmaceutical preparation of the roxasistat, when the cyclodextrin derivative is further selected to be hydroxypropyl-beta-cyclodextrin, and is matched with potassium polacriline, lactose, microcrystalline cellulose, croscarmellose sodium and the particle size d0.9 of the roxasistat is controlled to be reduced to be below 30 mu m, the better dissolved pharmaceutical preparation of the roxasistat can be obtained.
Detailed Description
Example 1
Composition of Dosage (g)
Rosemat sauce 50
Hydroxypropyl-beta-cyclodextrin 80
Polacrilin potassium 6
Lactose 170
Microcrystalline cellulose 43
Croscarmellose sodium 7
Rosemat d0.9 ═ 18 μm
The preparation method comprises the following steps:
(1) uniformly mixing the roxasistat, the hydroxypropyl-beta-cyclodextrin, the polacrilin potassium, the lactose, the microcrystalline cellulose and the croscarmellose sodium to prepare a mixture;
(2) adding purified water into the mixture obtained in the step (1), granulating, and finishing granules to obtain medicine granules;
(3) tabletting the drug granules.
Example 2
Composition of Dosage (g)
Rosemat sauce 100
Hydroxypropyl-beta-cyclodextrin 50
Polacrilin potassium 8
Lactose 200
Microcrystalline cellulose 30
Croscarmellose sodium 8
Rosemat d0.9 ═ 15 μm
The preparation method is the same as example 1.
Example 3
Composition of Dosage (g)
Rosemat sauce 20
Hydroxypropyl-beta-cyclodextrin 100
Polacrilin potassium 3
Lactose 120
Microcrystalline cellulose 50
Croscarmellose sodium 3
Rosemat d0.9 ═ 20 μm
The preparation method is the same as example 1.
Example 4
Figure BDA0003324983670000041
Figure BDA0003324983670000051
Rosemat d0.9 ═ 25 μm
The preparation method comprises the following steps:
(1) uniformly mixing the roxasistat, hydroxyethyl-beta-cyclodextrin, polacrilin potassium, pregelatinized starch, low-substituted hydroxypropyl cellulose and crospovidone to prepare a mixture;
(2) adding purified water into the mixture obtained in the step (1), granulating, and finishing granules to obtain medicine granules;
(3) tabletting the drug granules.
Example 5
Composition of Dosage (g)
Rosemat sauce 50
Glucose-cyclodextrin 80
Polacrilin potassium 6
Calcium hydrogen phosphate 35
Mannitol 137
Sodium carboxymethyl starch 8
Rosemat d0.9 ═ 16 μm
The preparation method comprises the following steps:
(1) uniformly mixing the roxasistat, the glucose-cyclodextrin, the polacrilin potassium, the calcium hydrophosphate, the mannitol and the sodium carboxymethyl starch to prepare a mixture;
(2) adding purified water into the mixture obtained in the step (1), granulating, and finishing granules to obtain medicine granules;
(3) tabletting the drug granules.
Example 6
Composition of Dosage (g)
Rosemat sauce 50
Maltose-cyclodextrin 55
Polacrilin potassium 8
Microcrystalline cellulose 50
Sorbitol 100
Cross-linked polyvidone 6
Hydroxypropyl cellulose 6
Rosemat d0.9 ═ 10 μm
The preparation method comprises the following steps:
(1) uniformly mixing the roxasistat, the maltose-cyclodextrin, the polacrilin potassium, the microcrystalline cellulose, the sorbitol, the crospovidone and the hydroxypropyl cellulose to obtain a mixture;
(2) adding purified water into the mixture obtained in the step (1), granulating, and finishing granules to obtain medicine granules;
(3) tabletting the drug granules.
Example 7
Composition of Dosage (g)
Rosemat sauce 20
Dihydroxypropyl-beta-cyclodextrin 35
Carboxymethyl-cyclodextrin 45
Polacrilin potassium 7
Sucrose 40
Lactose 125
Cross-linked polyvidone 6
Hydroxypropyl methylcellulose 7
Magnesium stearate 4
Rosemat d0.9 ═ 12 μm
The preparation method comprises the following steps:
(1) uniformly mixing the roxasistat, dihydroxypropyl-beta-cyclodextrin, carboxymethyl-cyclodextrin, polacrilin potassium, sucrose, lactose, crospovidone and hydroxypropyl methyl cellulose to prepare a mixture;
(2) adding purified water into the mixture obtained in the step (1), granulating, and finishing granules to obtain medicine granules;
(3) mixing the medicinal granules with magnesium stearate, and tabletting.
Example 8
Composition of Dosage (g)
Rosemat sauce 100
Maltotriose-cyclodextrin 65
Polacrilin potassium 7
Calcium hydrogen phosphate 30
Lactose 165
Croscarmellose sodium 7
Silica gel micropowder 2
Talcum powder 2
Rosemat d0.9 ═ 10 μm
The preparation method comprises the following steps:
(1) uniformly mixing the roxasistat, the maltotriose-cyclodextrin, the polacrilin potassium, the calcium hydrophosphate, the lactose and the croscarmellose sodium to prepare a mixture;
(2) adding purified water into the mixture obtained in the step (1), granulating, and finishing granules to obtain medicine granules;
(3) mixing the medicinal granules with silica gel micropowder and pulvis Talci, and tabletting.
Example 9
Figure BDA0003324983670000071
Figure BDA0003324983670000081
Rosemat d0.9 ═ 30 μm
The preparation method comprises the following steps:
(1) uniformly mixing the roxasistat, the methyl-beta-cyclodextrin, the polacrilin potassium, the lactose, the sorbitol and the low-substituted hydroxypropyl cellulose to prepare a mixture;
(2) adding purified water into the mixture obtained in the step (1), granulating, and finishing granules to obtain medicine granules;
(3) mixing the medicinal granules with sodium stearyl fumarate, and tabletting.
Example 10
Composition of Dosage (g)
Rosemat sauce 50
Hydroxypropyl-beta-cyclodextrin 90
Polacrilin potassium 6
Microcrystalline cellulose 45
Mannitol 205
Croscarmellose sodium 7
Sodium carboxymethylcellulose 4
Povidone 3
Rosemat d0.9 ═ 5 μm
The preparation method comprises the following steps:
(1) uniformly mixing the roxasistat, the hydroxypropyl-beta-cyclodextrin, the polacrilin potassium, the microcrystalline cellulose, the mannitol, the croscarmellose sodium, the carboxymethylcellulose sodium and the povidone to prepare a mixture;
(2) adding purified water into the mixture obtained in the step (1), granulating, and finishing granules to obtain medicine granules;
(3) tabletting the drug granules.
Comparative examples
Figure BDA0003324983670000082
Figure BDA0003324983670000091
The preparation method is the same as example 1.
Dissolution study
Taking the samples prepared in examples 1-10 and comparative recipes 1-5, taking the dissolution liquid at 5, 10, 15, 20, 30, 45min for HPLC determination according to the dissolution determination method (second method of appendix X C of second part of the 2010 edition of Chinese pharmacopoeia) with pH6.5 phosphate buffer as dissolution medium, the experimental results are as follows:
Figure BDA0003324983670000092
the experimental results show that the dissolution rate of the roxasistat can be improved by the limitation of the particle size of the roxasistat and the addition of the cyclodextrin derivative and the potassium polacrilin in the embodiment of the invention. Particularly, when the cyclodextrin derivative is selected from hydroxypropyl-beta-cyclodextrin, the dissolution effect is better; when the cyclodextrin derivative is selected from hydroxypropyl-beta-cyclodextrin, the diluent is selected from lactose and microcrystalline cellulose, and the disintegrant is selected from croscarmellose sodium, the dissolution effect is optimal. The particle size of the obtained sample is only limited by the comparison formula 1, the comparison formula 2 does not contain cyclodextrin derivatives, the comparison formula 3 does not contain polacrilin potassium, the particle size of the rosixostat in the comparison formula 4 is 40 mu m, the comparison formula 5 does not contain polacrilin potassium, and when the dosage of the cross-linked sodium carboxymethylcellulose serving as the disintegrant is increased, the dissolution effect of the prepared sample is poor.

Claims (14)

1. A pharmaceutical formulation of rosxastat comprising rosxastat, a cyclodextrin derivative, polacrilin potassium, a diluent and a disintegrant, wherein the particle size d0.9 of the rosxastat is not greater than 30 μm.
2. The pharmaceutical formulation of rosxastat according to claim 1, characterized in that the particle size d0.9 of the rosxastat is 10-20 μ ι η.
3. A pharmaceutical formulation of rosxastat according to claim 1 characterized in that the cyclodextrin derivative is selected from one or more of hydroxyethyl- β -cyclodextrin, hydroxypropyl- β -cyclodextrin, dihydroxypropyl- β -cyclodextrin, methyl- β -cyclodextrin, glucose-cyclodextrin, maltose-cyclodextrin, maltotriose-cyclodextrin, carboxymethyl-cyclodextrin.
4. The pharmaceutical formulation of rosxastat according to claim 1, characterized in that the cyclodextrin derivative is selected from hydroxypropyl- β -cyclodextrin.
5. The pharmaceutical preparation of rosmarin according to claim 1, wherein the disintegrant is one or more of sodium carboxymethyl starch, low substituted hydroxypropyl cellulose, crospovidone, croscarmellose sodium.
6. The pharmaceutical formulation of rosxastat according to claim 1, wherein the diluent is one or more of microcrystalline cellulose, mannitol, lactose, pregelatinized starch, sucrose, sorbitol, dibasic calcium phosphate.
7. The pharmaceutical preparation of rosxastat according to claim 1, wherein the pharmaceutical preparation comprises the following components in mass: 20-100 parts of roxasistat, 50-100 parts of cyclodextrin derivative, 3-8 parts of polacrilin potassium, 250 parts of diluent 150 and 3-8 parts of disintegrant.
8. The pharmaceutical preparation of rosxastat according to claim 1, wherein the pharmaceutical preparation comprises the following components in mass: 20-100 parts of roxasistat, 50-100 parts of hydroxypropyl-beta-cyclodextrin, 3-8 parts of polacrilin potassium, 200 parts of lactose, 30-50 parts of microcrystalline cellulose and 3-8 parts of croscarmellose sodium.
9. The pharmaceutical formulation of rosxastat according to claim 1, wherein the pharmaceutical formulation further comprises a binder and/or a lubricant.
10. The pharmaceutical formulation of rosxastat according to claim 9, wherein the binder is one or more of hydroxypropyl cellulose, hydroxypropyl methylcellulose, sodium carboxymethyl cellulose, povidone.
11. The pharmaceutical preparation of rosmarin according to claim 9, wherein the lubricant is one or more of aerosil, talc, magnesium stearate, sodium stearyl fumarate.
12. A process for preparing a pharmaceutical formulation of rosxata according to claim 1, comprising the steps of:
(1) uniformly mixing the roxasistat, the cyclodextrin derivative, the polacrilin potassium, the diluent and the disintegrant to prepare a mixture;
(2) adding purified water into the mixture obtained in the step (1), granulating, and finishing granules to obtain medicine granules;
(3) tabletting the drug granules.
13. The method according to claim 12, wherein the step (1) further comprises a step of adding a binder.
14. The method for preparing a drug according to claim 12, wherein the step (3) further comprises a step of uniformly mixing the drug particles with a lubricant.
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CN116199628A (en) * 2023-04-28 2023-06-02 珐博进(中国)医药技术开发有限公司 Solid [ (4-hydroxy-1-methyl-7-phenoxyisoquinoline-3-carbonyl) amino ] acetic acid
CN116199628B (en) * 2023-04-28 2023-09-01 珐博进(中国)医药技术开发有限公司 Solid [ (4-hydroxy-1-methyl-7-phenoxyisoquinoline-3-carbonyl) amino ] acetic acid

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