WO2020253808A1 - Composition pharmaceutique et son procédé de préparation - Google Patents

Composition pharmaceutique et son procédé de préparation Download PDF

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Publication number
WO2020253808A1
WO2020253808A1 PCT/CN2020/096984 CN2020096984W WO2020253808A1 WO 2020253808 A1 WO2020253808 A1 WO 2020253808A1 CN 2020096984 W CN2020096984 W CN 2020096984W WO 2020253808 A1 WO2020253808 A1 WO 2020253808A1
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WO
WIPO (PCT)
Prior art keywords
pharmaceutical composition
composition according
weight
mannitol
content
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PCT/CN2020/096984
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English (en)
Chinese (zh)
Inventor
潘晓晨
刘宇
张新华
Original Assignee
江苏恒瑞医药股份有限公司
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Priority to CN202080043824.0A priority Critical patent/CN113993505B/zh
Publication of WO2020253808A1 publication Critical patent/WO2020253808A1/fr

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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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A61K47/38—Cellulose; Derivatives thereof
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents

Definitions

  • the present disclosure belongs to the field of pharmaceutical preparations, and relates to a pyridine containing 6-acetyl-8-cyclopentyl-5-methyl-2-((5-(piperidin-4-yl)pyridin-2-yl)amino)pyridine And [2,3-d]pyrimidine-7(8H)-one or a pharmacologically acceptable salt thereof and a combination of mannitol.
  • (8H)-ketone is a CDK inhibitor with excellent CDK4/6 inhibitory activity and high selectivity.
  • CN201780000891.2 and CN201710060548.9 reported the use of disintegrants that do not contain metal elements to solve the dissolution problem of pharmaceutical compositions, and found that lactose is not conducive to the stability of pharmaceutical compositions, providing a pharmaceutical composition (preparation) of the aforementioned compound
  • the prescription is: filler mannitol and microcrystalline cellulose, disintegrant povidone, and binder is pregelatinized starch or hypromellose.
  • a tablet is a common solid preparation, which is formed by uniformly mixing the active ingredient and auxiliary materials and then compressed and has a sheet or special-shaped sheet shape.
  • the wet granulation and tabletting method is a molding process in which the granules prepared by the wet method are dried and added with suitable auxiliary materials and then compressed. Where the drug is relatively stable to heat and humidity, wet granulation and tableting can generally be used.
  • the disclosure provides a pharmaceutical composition containing the active ingredient 6-acetyl-8-cyclopentyl-5-methyl-2-((5-(piperidin-4-yl)pyridine-2 -Yl)amino)pyrido[2,3-d]pyrimidine-7(8H)-one or a pharmaceutically acceptable salt thereof and mannitol, wherein the mannitol is by weight and the content (accounting for the total weight of the pharmaceutical composition) Not more than 20%.
  • researchers have found that reducing the content of mannitol in the pharmaceutical composition can obtain a composition with an excellent tableting rate.
  • the composition has a high tableting rate in industrial production and is more suitable for industrial production.
  • the pharmaceutical composition provided by some embodiments contains mannitol in a content of less than 20% by weight.
  • Non-limiting implementations include: 1%, 2%, 3%, 4%, 5%, 6%, 7%, 8%, 9%, 10%, 11%, 12%, 13%, 14%, 15%, 16%, 17%, 18%, 19%, 19.1%, 19.2%, 19.3%, 19.4%, 19.5%, 19.6% , 19.7%, 19.8%, 19.9% or any value between any two numbers.
  • the content of mannitol in the composition can be reduced by adding pregelatinized starch.
  • pregelatinized starch on the one hand can provide inter-particle fluidity, and at the same time can improve The compressibility of the composition.
  • the weight ratio of the pregelatinized starch to mannitol in the pharmaceutical composition is 5:1 to 1:5, and non-limiting examples include: 5:1, 4:1, 3:1, 2: 1. 1:1, 1:2, 1:3, 1:4, 1:5, or any value between any two numbers, preferably 3:1 to 1:3.
  • the content of the pregelatinized starch accounts for 15%-40% of the total weight of the pharmaceutical composition.
  • Non-limiting examples include: 15%, 16%, 17%, 18%, 19%, 20%, 21%, 22%, 23%, 24%, 25%, 26%, 27%, 28%, 29%, 30%, 31%, 32%, 33%, 34%, 35% , 36%, 37%, 38%, 39%, 40% or any value between any two numbers, preferably 17% to 35%.
  • composition described in the present disclosure may further contain microcrystalline cellulose.
  • the content of the microcrystalline cellulose is 5%-20% by weight.
  • Non-limiting examples include: 5%, 6%, 7%, 8%, 9%, 10%, 11%, 12%, 13%, 14%, 15%, 16%, 17%, 18%, 19%, 20% or any value between any two numbers, preferably 10%-15%.
  • the pharmaceutical composition only contains pregelatinized starch, mannitol and microcrystalline cellulose as fillers.
  • the dissolution of the pharmaceutical composition in the present disclosure is very rapid and complete.
  • purified water is used as the dissolution medium, preferably 1000 ml of purified water, and
  • the dissolution test of the pharmaceutical composition of the present disclosure is carried out at 37 ⁇ 0.5°C with a paddle speed of 50 rpm, and the dissolution rate is greater than or equal to 70% in 15 minutes.
  • the pharmaceutically acceptable salt of the active ingredient in the pharmaceutical composition provided in the present disclosure may be preferably selected from the isethionate of the active ingredient.
  • the active ingredient 6-acetyl-8-cyclopentyl-5-methyl-2-((5-(piperidin-4-yl)pyridin-2-yl )Amino)pyrido[2,3-d]pyrimidin-7(8H)-one accounts for 10-40% of the total weight of the pharmaceutical composition.
  • Non-limiting examples include: 10%, 11%, 12%, 13 %, 14%, 15%, 16%, 17%, 18%, 19%, 20%, 21%, 22%, 23%, 24%, 25%, 26%, 27%, 28%, 29%, 30%, 31%, 32%, 33%, 34%, 35%, 36%, 37%, 38%, 39%, 40% or any value between any two numbers, preferably 15-30%.
  • the pharmaceutical composition provided in the present disclosure may further contain at least one of a binder, a disintegrant and a lubricant.
  • the binder in this disclosure is known or can be confirmed by those skilled in the art, and can be selected from but not limited to at least one of polyvinylpyrrolidone, pregelatinized starch, hypromellose and hydroxypropylcellulose Species;
  • the amount of the adhesive accounts for 0.5-10% of the weight of the pharmaceutical composition, including 0.5%, 0.6%, 0.7%, 0.8%, 0.9%, 1%, 1.5%, 2%, 2.5%, 3%, 3.5%, 4%, 4.5%, 5%, 5.5%, 6%, 6.5%, 7%, 7.5%, 8%, 8.5%, 9%, 9.5%, 10% Or any value between any two numbers, based on the weight of the pharmaceutical composition.
  • the disintegrant in the present disclosure is known or confirmed by those skilled in the art, and can be selected from but not limited to at least one of low-substituted hydroxypropyl cellulose and crospovidone; preferably, the The amount of disintegrant accounts for 8%-15% of the weight of the pharmaceutical composition, and non-limiting embodiments include 8%, 8.5%, 9%, 9.5%, 10%, 11%, 12%, 13%, 14%, 15% or any value between any two numbers, based on the weight of the pharmaceutical composition.
  • the lubricant described in the present disclosure is known or can be confirmed by those skilled in the art, and may be selected from but not limited to at least one of magnesium stearate, stearic acid, and glyceryl behenate; preferably, the present disclosure
  • the amount of the lubricant described in the pharmaceutical composition is 0.5% to 5% by weight, and non-limiting embodiments include 0.1%, 0.2%, 0.3%, 0.4%, 0.5%, 0.6%, 0.7%, 0.8%, 0.9% , 1%, 1.5%, 2%, 2.5%, 3%, 3.5%, 4%, 4.5%, 5% or any value between any two numbers, based on the weight of the pharmaceutical composition.
  • the pharmaceutical composition contains the following ingredients by weight:
  • disintegrant is selected from at least one of low-substituted hydroxypropyl cellulose, povidone and crospovidone,
  • the binder is selected from at least one of polyvinylpyrrolidone, pregelatinized starch and hypromellose, and optionally 0.5%-5% lubricant
  • the lubricant is selected from at least one of magnesium stearate, stearic acid and glyceryl behenate.
  • composition described in the present disclosure may be a solid preparation, including tablets, pills or granules, preferably tablets.
  • the present disclosure also provides another pharmaceutical composition, which contains the active ingredient 6-acetyl-8-cyclopentyl-5-methyl-2-((5-(piperidin-4-yl)pyridin-2-yl )Amino)pyrido[2,3-d]pyrimidine-7(8H)-one or its pharmaceutically acceptable salt and pregelatinized starch, the pregelatinized starch is preferably 15%-40% by weight.
  • the pharmaceutical composition provided by some embodiments also contains mannitol.
  • the content of mannitol is not more than 20%.
  • Non-limiting implementations include: 1%, 2%, 3%, 4%, 5%, 6%, 7%, 8%, 9%, 10%, 11%, 12%, 13%, 14%, 15%, 16%, 17%, 18%, 19%, 19.1%, 19.2%, 19.3%, 19.4%, 19.5%, 19.6%, 19.7%, 19.8%, 19.9% or any value between any two numbers.
  • the pharmaceutical composition may further contain microcrystalline cellulose, and the content of the microcrystalline cellulose accounts for 5% to 20% of the total weight of the pharmaceutical composition.
  • Non-limiting examples include: 5%, 6%, 7 %, 8%, 9%, 10%, 11%, 12%, 13%, 14%, 15%, 16%, 17%, 18%, 19%, 20% or any value between any two numbers, It is preferably 10% to 15%.
  • the pharmaceutical composition further contains at least one of a binder, a disintegrant and a lubricant.
  • the amount of the binder, disintegrant or lubricant is as mentioned above.
  • the present disclosure also provides another pharmaceutical composition, which contains the following ingredients by weight: the active ingredient 6-acetyl-8-cyclopentyl-5-methyl-2-((5-(piperidin-4-yl )Pyridin-2-yl)amino)pyrido[2,3-d]pyrimidin-7(8H)-one or a pharmaceutically acceptable salt thereof, 15%-40% pregelatinized starch and mannitol.
  • the weight ratio of the pregelatinized starch to mannitol in the pharmaceutical composition may be 5:1 to 1:5.
  • the pharmaceutical composition provided by some embodiments further contains microcrystalline cellulose.
  • the content of the microcrystalline cellulose accounts for 5% to 20% of the total weight of the pharmaceutical composition.
  • Non-limiting examples include: 5%, 6%, and 7%. , 8%, 9%, 10%, 11%, 12%, 13%, 14%, 15%, 16%, 17%, 18%, 19%, 20% or any value between any two numbers, preferably 10%-15%.
  • the pharmaceutical composition provided by some embodiments further contains at least one of a binder, a disintegrant and a lubricant.
  • the amount of the binder, disintegrant or lubricant is as mentioned above.
  • the final moisture content of the particles during the granulation period is selected from 1.0% to 6.0%, and the final moisture content of the particles may be 1.0%, 1.1%, 1.2%, 1.3%, 1.4%. %, 1.5%, 1.6%, 1.7%, 1.8%, 1.9%, 2.0%, 2.1%, 2.2%, 2.3%, 2.4%, 2.5%, 2.6%, 2.7%, 2.8%, 2.9%, 3.0%, 3.1%, 3.2%, 3.3%, 3.4%, 3.5%, 3.6%, 3.7%, 3.8%, 3.9%, 4.0%, 4.1%, 4.2%, 4.3%, 4.4%, 4.5%, 4.6%, 4.7% , 4.8%, 4.9%, 5.0%, 5.1%, 5.2%, 5.3%, 5.4%, 5.5%, 5.6%, 5.7%, 5.8%, 5.9%, 6.0% or any value between two numbers.
  • the final moisture content of the particles is 1 to 6%
  • the moisture content of the final obtained/used particles or called the pharmaceutical composition
  • the method for measuring the moisture of particles or compositions involved in the present disclosure is the measurement by an infrared rapid moisture meter (measurement temperature is 105°C). This method is a common method for measuring moisture well known to those skilled in the art, and is widely used in granules and tablets. Determination of moisture content in powders, etc.
  • compositions such as tablets described in the present disclosure may adopt methods common in the art, such as wet granulation, dry granulation, and one-step granulation, preferably wet granulation.
  • the wet granulation may be selected from fluidized bed granulation and high-speed stirring granulation, preferably fluidized bed granulation.
  • the active ingredients, excipients and other pharmaceutical auxiliary materials are mixed, and the mixture can be granulated by spraying the aqueous binder solution on it.
  • a person skilled in the art can appropriately set various parameters of the granulator according to the granulator used, for example, air inlet temperature, spray speed, spray air pressure or air inlet volume.
  • the method of the drying step (if necessary) of the particles or the composition of the present disclosure is not particularly limited, and may be vacuum drying or blast drying or drying or baking. As long as the particles are dried until the final moisture content (dry weight method) is 1.0 to 6.0% or less.
  • the drying temperature is room temperature to 100°C, preferably 70°C to 90°C, and the drying time is tens of minutes to several hours, preferably on the order of 10 minutes to 30 minutes.
  • oral 150 mg of the pharmaceutical composition of the present disclosure has a C max (geometric mean) selected from 50 to 90 ng/ml in mammals such as humans, including but not limited to 50 ng/ml, 55 ng/ml, 60 ng/ml, 65 ng /ml, 70ng/ml, 75ng/ml, 80ng/ml, 85ng/ml, 90ng/ml or any number between.
  • 125 mg of the pharmaceutical composition is taken orally, and the C max in mammals such as humans is 64 ng/ml.
  • oral 150 mg of the pharmaceutical composition of the present disclosure has an AUC 0- ⁇ (geometric mean) selected from 1500 ⁇ 2500h*ng/ml in mammals such as humans, including but not limited to 1500h*ng/ml, 1550h*ng/ml , 1600h*ng/ml, 1650h*ng/ml, 1700h*ng/ml, 1750h*ng/ml, 1800h*ng/ml, 1850h*ng/ml, 1900h*ng/ml, 1950h*ng/ml, 2000h *ng/ml, 2050h*ng/ml, 2100h*ng/ml, 2150h*ng/ml, 2200h*ng/ml, 2250h*ng/ml, 2300h*ng/ml, 2350h*ng/ml, 2400h*ng /ml, 2450h*ng/ml, 2500h*ng/ml or any number between values.
  • AUC 0- ⁇ geometric mean
  • the method for preparing the aforementioned pharmaceutical composition comprises: combining the active ingredient 6-acetyl-8-cyclopentyl-5-methyl-2-((5-(piperidin-4-yl)pyridine -2-yl)amino)pyrido[2,3-d]pyrimidin-7(8H)-one or a pharmaceutically acceptable salt thereof is optionally mixed with the aforementioned pharmaceutical excipients.
  • An optional embodiment provides a method for preparing the aforementioned pharmaceutical composition comprising: combining the active ingredient 6-acetyl-8-cyclopentyl-5-methyl-2-((5-(piperidin-4-yl)pyridine- 2-yl)amino)pyrido[2,3-d]pyrimidine-7(8H)-one or its pharmaceutically acceptable salt is mixed with pregelatinized starch, mannitol and microcrystalline cellulose.
  • tableting is performed under the condition that the final water content of the particles is selected from 1.0% to 6.0%, and the final water content of the particles can be 1.0%, 1.1%, 1.2%, 1.3%, 1.4%, 1.5%, 1.6%, 1.7%, 1.8%, 1.9%, 2.0%, 2.1%, 2.2%, 2.3%, 2.4%, 2.5%, 2.6%, 2.7%, 2.8%, 2.9% , 3.0%, 3.1%, 3.2%, 3.3%, 3.4%, 3.5%, 3.6%, 3.7%, 3.8%, 3.9%, 4.0%, 4.1%, 4.2%, 4.3%, 4.4%, 4.5%, 4.6% %, 4.7%, 4.8%, 4.9%, 5.0%, 5.1%, 5.2%, 5.3%, 5.4%, 5.5%, 5.6%, 5.7%, 5.8%, 5.9%, 6.0% or any two numbers between Numerical value.
  • total weight of the pharmaceutical composition in the present invention is the numerical range of the active ingredient or other types of pharmaceutical excipients calculated from the weight of the tablet core not containing the coating agent.
  • Figure 1 shows the dissolution profile of tablets of prescription 1-3 in purified water.
  • Figure 2 shows the dissolution profile of tablets of prescription 4-6 in purified water.
  • Figure 3 shows the dissolution profile of tablets of prescription 7-9 in purified water.
  • Figure 4 shows the dissolution profile of tablets of prescription 10-11 in purified water.
  • the dissolution of tablets with prescriptions 4 to 6 was measured.
  • the results showed that in prescriptions 4 to 6, compound A was completely dissolved, but the dissolution rate of prescription 6 was too fast, and the bioavailability in the body was expected to be low.
  • the dissolution data are shown in Table 4, and the dissolution curve is shown in Figure 2.
  • the compound A, mannitol, pregelatinized starch, microcrystalline cellulose, and low-substituted hydroxypropyl cellulose were prepared by wet granulation using a high-speed shearing granulator according to the proportions in Table 5, and prepared with hypromellose E5
  • the aqueous solution is a wetting agent, wet and soft materials are wet-sized and dried, and then the dry particles (moisture less than 3%) are dry-sized, and the prescribed amount of magnesium stearate is added and mixed evenly.
  • the obtained total mixed granules are compressed into tablets.
  • the dissolution of tablets in prescriptions 7 to 9 was determined.
  • the results showed that in prescriptions 7-9, compound A was completely dissolved; as the amount of pregelatinized starch increased, the dissolution rate gradually increased.
  • the dissolution data are shown in Table 6 below, and the dissolution curve is shown in Figure 3.
  • the compound A, mannitol, pregelatinized starch, microcrystalline cellulose, low-substituted hydroxypropyl cellulose or cross-linked povidone according to the ratio in Table 7 were used for wet granulation with a high-speed shear granulator.
  • the aqueous solution of propylmethyl cellulose E5 is a wetting agent, wet and soft materials are wet-sized and dried, and then the dry particles (moisture less than 3%) are dried and sized, and the prescribed amount of magnesium stearate is added. well mixed. The obtained total mixed granules are compressed into tablets.
  • the dissolution of the tablets of prescription 10 and 11 was determined.
  • Example 1 With reference to the method of Example 1, the corresponding total mixed particles were prepared according to the prescription amount in Table 9, and the granules with prescriptions 12-15 were compressed using a Chuangbojiawei single punch tablet machine.
  • corn starch and pregelatinized starch have similar properties, poor compressibility, and the excipient has both disintegration properties, which will cause the tablet to dissolve faster.
  • Test drug prepared by the method of parameter embodiment 4, 150mg specification;
  • Dosage regimen 12 subjects took a single fasting (150 mg/tablet ⁇ 1 tablet), and the dose was 150 mg, once in total.
  • LC/MS/MS is used to determine the content of active ingredients in healthy humans.
  • the geometric average data is as follows.

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Abstract

La présente invention concerne une composition pharmaceutique et son procédé de préparation. En particulier, la présente invention concerne une composition pharmaceutique contenant un dérivé de pyridopyrimidine ou un sel de celui-ci et son procédé de préparation. La composition pharmaceutique contient du 6-acétyl-8-cyclopentyl-5-méthyl-2-((5-(pipéridin-4-yl)pyridin-2-yl)amino)pyrido[2,3-d]pyrimidine-7(8H)-one ou un sel pharmacologiquement acceptable et du mannitol, la teneur en mannitol étant inférieure ou égale à 20 % en poids. La composition pharmaceutique présente une bonne stabilité et un taux de dissolution élevé ; en outre, le taux de fabrication de comprimés d'une production de masse industrielle est élevé, et la composition pharmaceutique est plus appropriée pour la production industrielle de masse.
PCT/CN2020/096984 2019-06-20 2020-06-19 Composition pharmaceutique et son procédé de préparation WO2020253808A1 (fr)

Priority Applications (1)

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CN202080043824.0A CN113993505B (zh) 2019-06-20 2020-06-19 一种药物组合物以及其制备方法

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CN201910536727.4 2019-06-20
CN201910536727 2019-06-20

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Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003062236A1 (fr) * 2002-01-22 2003-07-31 Warner-Lambert Company Llc 2-(pyridin-2-ylamino)-pyrido[2,3-d]pyrimidin-7-ones
WO2014183520A1 (fr) * 2013-05-17 2014-11-20 上海恒瑞医药有限公司 Dérivé de miazines de tiophène, son procédé de préparation et ses applications médicales
WO2016169422A1 (fr) * 2015-04-22 2016-10-27 江苏恒瑞医药股份有限公司 Forme cristalline d'un inhibiteur de kinase dépendant des cyclines et procédé de préparation de celle-ci
WO2017133542A1 (fr) * 2016-02-04 2017-08-10 江苏恒瑞医药股份有限公司 Composition pharmaceutique comprenant un dérivé pyridopyrimidine ou un sel de qualité pharmaceutique de ce dernier
CN107028899A (zh) * 2016-02-04 2017-08-11 江苏恒瑞医药股份有限公司 一种含有吡啶并嘧啶类衍生物或其可药用盐的药物组合物

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003062236A1 (fr) * 2002-01-22 2003-07-31 Warner-Lambert Company Llc 2-(pyridin-2-ylamino)-pyrido[2,3-d]pyrimidin-7-ones
WO2014183520A1 (fr) * 2013-05-17 2014-11-20 上海恒瑞医药有限公司 Dérivé de miazines de tiophène, son procédé de préparation et ses applications médicales
WO2016169422A1 (fr) * 2015-04-22 2016-10-27 江苏恒瑞医药股份有限公司 Forme cristalline d'un inhibiteur de kinase dépendant des cyclines et procédé de préparation de celle-ci
WO2017133542A1 (fr) * 2016-02-04 2017-08-10 江苏恒瑞医药股份有限公司 Composition pharmaceutique comprenant un dérivé pyridopyrimidine ou un sel de qualité pharmaceutique de ce dernier
CN107028899A (zh) * 2016-02-04 2017-08-11 江苏恒瑞医药股份有限公司 一种含有吡啶并嘧啶类衍生物或其可药用盐的药物组合物

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