CN110898026A - Pharmaceutical composition containing BPI-7711 and preparation method thereof - Google Patents

Pharmaceutical composition containing BPI-7711 and preparation method thereof Download PDF

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Publication number
CN110898026A
CN110898026A CN201911264353.1A CN201911264353A CN110898026A CN 110898026 A CN110898026 A CN 110898026A CN 201911264353 A CN201911264353 A CN 201911264353A CN 110898026 A CN110898026 A CN 110898026A
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China
Prior art keywords
bpi
pharmaceutical composition
sodium
preparation
microcrystalline cellulose
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CN201911264353.1A
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Inventor
余成武
李欣
汤春
张晓霞
J·彭
D·张
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BETA PHARMA (SHANGHAI) Co.,Ltd.
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Beida Pharmaceutical (suzhou) Co Ltd
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Priority to CN201911264353.1A priority Critical patent/CN110898026A/en
Publication of CN110898026A publication Critical patent/CN110898026A/en
Priority to PCT/CN2020/135660 priority patent/WO2021115425A1/en
Priority to ARP200103449A priority patent/AR120727A1/en
Priority to TW109143982A priority patent/TW202122087A/en
Pending legal-status Critical Current

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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
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4866—Organic macromolecular compounds
    • 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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents

Abstract

The invention discloses a pharmaceutical composition containing BPI-7711 and a preparation method thereof, wherein the pharmaceutical composition containing BPI-7711 comprises sachets and capsule shells, and the sachets comprise the following components in percentage by weight: 15-50% of BPI-7711 main drug, 45-80% of diluent, 2-6% of disintegrating agent and 0.5-4% of lubricant. The preparation method is characterized by adopting a direct powder filling method. The medicine of the invention has the advantages of quick dissolution, high bioavailability, stable quality and suitability for industrial production.

Description

Pharmaceutical composition containing BPI-7711 and preparation method thereof
Technical Field
The invention relates to a pharmaceutical composition containing BPI-7711 and a preparation method thereof, belonging to the technical field of pharmaceutical preparations.
Background
BPI-7711 was developed by the drug industry and is disclosed in international patent number WO2017/218892 EGFR-tki, which belongs to the third generation, epidermal growth factor receptors (EGFR, Her1, ErbB1) are the main members of the ErbB family of 4 structurally related cell surface receptors, the other members being Her2(Neu, ErbB2), Her3(ErbB3) and Her4(ErbB4), EGFR exerts its major cellular function through its intrinsic catalytic tyrosine protein kinase activity, this receptor is activated by binding to growth factor ligands, such as Epidermal Growth Factor (EGF) and transforming growth factor- α (TGF- α), catalytically inactive EGFR monomers are converted into catalytically active homopolymers and heterodimers, these catalytically active dimers then initiate intracellular tyrosine kinase activity, which leads to autophosphorylation of specific EGFR tyrosine residues and leads to downstream activation of signaling proteins.
EGFR is found at abnormally high levels on the surface of many types of cancer cells, and elevated levels of EGFR have been associated with late stage disease, cancer spread, and poor clinical prognosis. Mutations in EGFR can lead to overexpression, permanent activation or persistence of the receptor, leading to uncontrolled cell growth, i.e., cancer. Thus, EGFR mutations have been identified in several types of malignancies, including metastatic lung cancer, head and neck cancer, colorectal cancer, and pancreatic cancer. In brain cancer, mutations occur primarily in exons (exons)18-21, which encode pockets of the kinase domain that bind Adenosine Triphosphate (ATP). The most clinically relevant drug sensitive EGFR mutations are deletions in exon 19 that eliminate a common amino acid motif (LREA) and point mutations in exon 21 that result in the substitution of arginine at position 858(L858R) with leucine. Overall, these two mutations account for nearly 85% of the EGFR mutations observed in lung cancer. Both mutations have permanent tyrosine kinase activity and are therefore carcinogenic. In at least 50% of patients who initially respond to current therapy, progression of the disease is associated with the development of a secondary mutation, T790M (also known as a gatekeeper mutation) in exon 20 of EGFR.
BPI-7711 and its pharmaceutically acceptable salts, having hygroscopic, light sensitive and solubility pH dependent properties.
The hygroscopic nature of the medicament causes the medicament to gradually absorb moisture during storage and use, and excessive moisture content accelerates degradation of the medicament and increases the risk of microbial overrun of the medicament. The photosensitivity of the pharmaceutical preparation usually causes the degradation of the pharmaceutical preparation due to exposure to strong light during the manufacturing, storage and use processes, so that the pharmaceutical preparation is not easy to be industrially produced and stored for a long time.
Generally, after oral administration, the drug is dissolved into the digestive juice and then absorbed in various parts of the gastrointestinal tract (including stomach, duodenum, jejunum, ileum and colon). The digestive juices in different absorption sites have different pH values, such as stomach (pH 1-3.5) and small intestine (pH 4-8). BPI-7711 is a gastric soluble drug, and the dissolution speed of the drug in the stomach has great influence on the bioavailability of the drug.
Disclosure of Invention
The invention aims to provide a pharmaceutical composition containing BPI-7711 and a preparation method thereof. The invention designs a formula and a preparation process suitable for continuous, stable and large-scale industrialization of BPI-7711 aiming at the solubility-pH dependence and the light instability of BPI-7711, and the BPI-7711 capsule produced according to the formula and the preparation process of the invention has the advantages of rapid dissolution, good quality, stable product and good clinical curative effect.
In order to achieve the purpose, the invention adopts the following technical scheme:
the present invention provides a pharmaceutical composition comprising BPI-7711, comprising a sachet and a capsule shell, said sachet comprising, in weight percent:
Figure BDA0002312427880000021
preferably, the main drug BPI-7711, the diluent, the disintegrant and the lubricant are all powder; more preferably, the particle size of the BPI-7711 main drug powder is 5-250 μm, and more preferably 60-200 μm; the particle size of the diluent powder is 100 to 250 μm.
Preferably, the main drug BPI-7711 comprises N- (2- (2- (dimethylamino) ethoxy) -4-methoxy-5- ((4- (1-methyl-1H-indol-3-yl) pyrimidin-2-yl) amino) phenyl) acrylamide pharmaceutically acceptable salt, more preferably N- (2- (2- (dimethylamino) ethoxy) -4-methoxy-5- ((4- (1-methyl-1H-indol-3-yl) pyrimidin-2-yl) amino) phenyl) acrylamide mesylate.
Preferably, the diluent comprises microcrystalline cellulose, lactose, calcium carbonate, calcium phosphate, calcium sulfate, cellulose acetate, erythritol, ethylcellulose, silicified microcrystalline cellulose, fructose, inulin, isomalt, lactitol, magnesium carbonate, magnesium oxide, maltitol, maltodextrin, maltose, mannitol, polydextrose, polyethylene glycol, pullulan, simethicone, sodium bicarbonate, sodium carbonate, sodium chloride, sorbitol, starch, sucrose, trehalose, and xylitol. More preferably one or a combination of both of lactose and microcrystalline cellulose.
More preferably, the lactose selected is lactose monohydrate and the microcrystalline cellulose selected is microcrystalline cellulose PH 102.
Preferably, the disintegrant comprises croscarmellose sodium, sodium carboxymethyl starch, hydroxypropyl cellulose, low-substituted hydroxypropyl cellulose methyl cellulose, povidone, sodium starch glycolate. More preferably croscarmellose sodium.
Preferably, the lubricant comprises magnesium stearate, silicon dioxide, sodium stearyl fumarate, calcium stearate, sodium lauryl sulfate and talcum powder. More preferably one or a combination of both magnesium stearate and colloidal silicon dioxide.
Preferably, the capsule shell comprises a gelatin hollow capsule and a hydroxypropyl cellulose hollow capsule. More preferably a gelatin hollow capsule.
The invention also provides a preparation method of the medicinal composition containing BPI-7711, which comprises the following steps:
1) respectively sieving the BPI-7711, the diluent and the disintegrant in required weight parts, and mixing;
2) adding a lubricant into the material obtained in the step 1), and continuously mixing;
3) filling the materials obtained in the step 2) into capsule shells.
Preferably, a 20-60 mesh sieve is adopted in the step 1), and a 30-45 mesh sieve is more preferable.
Preferably, in step 2), silicon dioxide is added into the material obtained in step 1) and mixed, and then magnesium stearate is added and mixed continuously.
The invention has the following beneficial effects:
the medicinal composition containing BPI-7711 controls the particle size range of BPI-7711 main drug to be 5-250 microns, preferably 60-200 microns, and controls the particle size range of diluent to be 100-250 microns, thereby solving the problem that BPI-7711 is too slowly dissolved in a high pH medium due to the solubility-pH dependency of BPI-7711, and simultaneously avoiding the uneven mixing and the layering in the production process caused by the over-small particle size of BPI-7711. Realizes the balance of quick dissolution and producibility of the BPI-7711 capsule.
The preparation method of the medicinal composition containing BPI-7711 adopts a direct powder filling process, has the characteristics of simple process and accurate filling amount, and greatly reduces the production time and cost. Meanwhile, the production time is short (the exposure to light is reduced), so that the exposure of the medicine to moisture and heat is avoided, and the stability and controllability of the product in the production process are effectively ensured.
Detailed Description
The advantageous effects of the present invention will now be further described by the following examples, which are for illustrative purposes only and do not limit the scope of the present invention, and variations and modifications apparent to those skilled in the art according to the present invention are also included in the scope and the like of the present invention.
In each of the following examples, BPI-7711 was prepared using the mesylate salt of N- (2- (2- (dimethylamino) ethoxy) -4-methoxy-5- ((4- (1-methyl-1H-indol-3-yl) pyrimidin-2-yl) amino) phenyl) acrylamide.
Example 1
The capsule comprises the following components by weight of 1000 capsules:
Figure BDA0002312427880000041
wherein: BPI-7711 particle size D90: 200 μm, microcrystalline cellulose particle size pH 102D90: 204 μm, lactose monohydrate particle size D90：200μm。
The preparation method comprises the following steps:
a. sieving: sieving microcrystalline cellulose with pH102, lactose monohydrate and croscarmellose sodium with 45 mesh sieve; using another 45-mesh sieve to sieve BPI-7711, and weighing BPI-7711 with the prescription amount after sieving;
b. premixing: putting the sieved materials into a 1L hopper mixer, and setting the rotating speed of the mixer to be 20 r/min for mixing for 24 min;
c. mixing: sieving the colloidal silicon dioxide by a 45-mesh sieve, adding the sieved colloidal silicon dioxide into the mixer in the step b, setting the rotating speed of the mixer to be 20 revolutions per minute, and continuously mixing for 14 min;
d. lubrication: sieving magnesium stearate with a 45-mesh sieve, adding into the mixer in the step c, setting the rotating speed of the mixer to be 20 rpm, and continuously mixing for 3 min;
e. the medicinal powder is filled into No. 5 gelatin capsules by a full-automatic capsule filling machine to prepare 1000 capsules.
Example 2
The capsule comprises the following components by weight of 1000 capsules:
Figure BDA0002312427880000051
wherein: BPI-7711 particle size D9060 μm, microcrystalline cellulose particle size D90100 μm, lactose grain diameter D90:105μm。
The preparation method comprises the following steps:
a. sieving: sieving microcrystalline cellulose, lactose monohydrate and croscarmellose sodium with a 45-mesh sieve; using another 45-mesh sieve to sieve BPI-7711, and weighing BPI-7711 with the prescription amount after sieving;
b. premixing: putting the sieved materials into a 500L hopper mixer, and setting the rotating speed of the mixer to be 20 r/min for mixing for 24 min;
c. mixing: sieving the colloidal silicon dioxide by a 45-mesh sieve, adding the sieved colloidal silicon dioxide into the mixer in the step b, setting the rotating speed of the mixer to be 20 revolutions per minute, and continuously mixing for 14 min;
d. lubrication: sieving magnesium stearate with a 45-mesh sieve, adding into the mixer in the step c, setting the rotating speed of the mixer to be 20 rpm, and continuously mixing for 3 min;
e. and (3) filling the mixed powder into a No. 1 capsule by using a full-automatic capsule filling machine to prepare 1000 capsules.
Example 3
The capsule comprises the following components by weight of 1000 capsules:
Figure BDA0002312427880000052
Figure BDA0002312427880000061
wherein: BPI-7711 particle size D90: 120 μm, microcrystalline cellulose pH102 particle size D90: 200 μm, lactose particle size D90：205μm。
The preparation method comprises the following steps:
a. sieving: sieving microcrystalline cellulose PH102, lactose monohydrate, and croscarmellose sodium with 45 mesh sieve; using another 45-mesh sieve to sieve BPI-7711, and weighing BPI-7711 with the prescription amount after sieving;
b. premixing: putting the sieved materials into a 1L hopper mixer, and setting the rotating speed of the mixer to be 20 r/min for mixing for 24 min;
c. mixing: sieving the colloidal silicon dioxide by a 45-mesh sieve, adding the sieved colloidal silicon dioxide into the mixer in the step b, setting the rotating speed of the mixer to be 20 revolutions per minute, and continuously mixing for 14 min;
d. lubrication: sieving magnesium stearate with a 45-mesh sieve, adding into the mixer in the step c, setting the rotating speed of the mixer to be 20 rpm, and continuously mixing for 3 min;
e. the medicinal powder is filled into No. 4 gelatin capsules by a full-automatic capsule filling machine to prepare 1000 capsules.
Example 4
The capsule comprises the following components by weight of 1000 capsules:
Figure BDA0002312427880000062
wherein: BPI-7711 particle size D90: 80 μm, microcrystalline cellulose particle size D90:100 μm, lactose particle size D90：110μm。
The preparation method comprises the following steps:
a. sieving: sieving microcrystalline cellulose, lactose monohydrate and croscarmellose sodium with a 45-mesh sieve; using another 45-mesh sieve to sieve BPI-7711, and weighing BPI-7711 with the prescription amount after sieving;
b. premixing: putting the sieved materials into a 1L hopper mixer, and setting the rotating speed of the mixer to be 20 r/min for mixing for 24 min;
c. lubrication: sieving magnesium stearate with a 45-mesh sieve, adding into the mixer in the step c, setting the rotating speed of the mixer to be 20 rpm, and continuously mixing for 3 min;
d. the medicinal powder is filled into No. 4 gelatin capsules by a full-automatic capsule filling machine to prepare 1000 capsules.
Example 5
The capsule comprises the following components by weight of 1000 capsules:
Figure BDA0002312427880000071
wherein: BPI-7711 particle size D90: 80 μm, microcrystalline cellulose particle size D90:100 μm, lactose monohydrate particle size D90：110μm。
The preparation method comprises the following steps:
a. sieving: sieving microcrystalline cellulose, lactose monohydrate and croscarmellose sodium with a 45-mesh sieve; using another 45-mesh sieve to sieve BPI-7711, and weighing BPI-7711 with the prescription amount after sieving;
b. premixing: putting the sieved materials into a 1L hopper mixer, and setting the rotating speed of the mixer to be 20 r/min for mixing for 24 min;
c. mixing: sieving the colloidal silicon dioxide by a 45-mesh sieve, adding the sieved colloidal silicon dioxide into the mixer in the step b, setting the rotating speed of the mixer to be 20 revolutions per minute, and continuously mixing for 14 min;
d. lubrication: sieving magnesium stearate with a 45-mesh sieve, adding into the mixer in the step c, setting the rotating speed of the mixer to be 20 rpm, and continuously mixing for 3 min;
the medicinal powder is filled into No. 3 gelatin capsules by a full-automatic capsule filling machine to prepare 1000 capsules.
Product effect evaluation
Dissolution test of examples 1 to 5
The experimental method comprises the following steps: reference is made to the dissolution measurement method (second method of 0931, the four general rules of pharmacopoeia 2015, china).
According to the following steps:
the dissolution method is a slurry method; dissolution instrument Distek 6300 dissolution instrument (ADS-DIS-012);
the rotating speed is 50 revolutions per minute;
medium volume 900 ml; the medium temperature is 37 ℃;
the sampling mode is automatic sampling; the sampling volume is 1.5 ml;
sampling time points 5 min, 10 min, 20 min, 30 min, 45 min and 60 min.
The dissolution curves of the samples in hydrochloric acid solution of pH1.2, phosphate buffer solution of pH4.5, phosphate buffer solution of pH6.8 (containing 0.5% Tween 80), and water (containing 0.5% Tween 80) were measured, respectively.
The results are as follows:
table 1: dissolution rate in hydrochloric acid solution with pH of 1.2
Figure BDA0002312427880000081
Table 2: dissolution rate in phosphate buffer solution with pH4.5
Figure BDA0002312427880000082
According to the following steps:
the dissolution method is a slurry method; the dissolution instrument is an Agilent 708-DS dissolution instrument;
the rotating speed is 75 revolutions per minute;
medium volume 900 ml; the medium temperature is 37 ℃;
the sampling mode is automatic sampling; the sampling volume is 5 ml;
sampling time points 5 min, 10 min, 20 min, 30 min, 45 min and 60 min.
The dissolution curves of the samples in water (containing 0.5% tween 80) and ph6.8 buffer (containing 0.5% tween 80) were examined separately.
The results are as follows:
table 3: dissolution profile in water (containing 0.5% Tween 80)
Figure BDA0002312427880000091
Table 4: dissolution rate in phosphate buffer (containing 0.5% Tween 80) with pH of 6.8
Figure BDA0002312427880000092
Second, stability test of examples 1-5
The experimental method comprises the following steps: the samples of examples 1 to 5 were placed in stability chambers of 25. + -. 2 ℃ and 60. + -. 5% RH, respectively, and subjected to a long-term stability test. Samples were taken at 0, 1, 3, 6, 9, and 12 months, respectively, and appearance, content, impurities, moisture, and dissolution rate in hydrochloric acid solution pH1.2 were examined for 30 minutes.
The results are as follows:
table 5: stability data under long-term stability conditions (25 ℃. + -. 2 ℃ 60. + -. 5% RH)
Figure BDA0002312427880000093
Figure BDA0002312427880000101
The experimental result shows that the maximum single impurity of the sample of the embodiment is not more than 0.09% and the total impurity of the sample is not more than 0.13% in the stability experiment for 0 day, which are far lower than the limit requirement, and the sample of the embodiment can keep better stability in the preparation process and avoid degradation caused by hygroscopicity and light instability. Meanwhile, the samples of the embodiment have good quality, and the water content is not more than 5% and the content is 97-103% in a stability experiment for 0 day. The release rate of each sample in hydrochloric acid with pH value of 1.2 in 30 minutes is more than 90% in stability experiment of 0 day and 12 months, which shows that the product has rapid dissolution performance in gastric acid. The stability data for a long period of 12 months shows that the maximum single impurity and total impurity of each sample of the example are not obviously increased in the storage process, and the samples of the example have better stability. In conclusion, the invention has the advantages of quick dissolution of the medicine, high bioavailability of the medicine, stable quality and suitability for industrial production.

Claims (10)

1. A pharmaceutical composition comprising BPI-7711, comprising a sachet and a capsule shell, said sachet comprising, in weight percent:
Figure FDA0002312427870000011
2. the pharmaceutical composition of claim 1 containing BPI-7711 wherein the base, diluent, disintegrant and lubricant are powders of BPI-7711; preferably, the particle size of the BPI-7711 main drug powder is 5-250 μm, more preferably 60-200 μm; the particle size of the diluent and the powder is 100 to 250 μm.
3. The pharmaceutical composition of claim 1 containing BPI-7711 wherein said base of BPI-7711 comprises a pharmaceutically acceptable salt of N- (2- (2- (dimethylamino) ethoxy) -4-methoxy-5- ((4- (1-methyl-1H-indol-3-yl) pyrimidin-2-yl) amino) phenyl) acrylamide; the mesylate salt of N- (2- (2- (dimethylamino) ethoxy) -4-methoxy-5- ((4- (1-methyl-1H-indol-3-yl) pyrimidin-2-yl) amino) phenyl) acrylamide is preferred.
4. The pharmaceutical composition according to claim 1 comprising BPI-7711 wherein said diluent comprises microcrystalline cellulose, lactose, calcium carbonate, calcium phosphate, calcium sulfate, cellulose acetate, erythritol, ethylcellulose, silicified microcrystalline cellulose, fructose, inulin, isomalt, lactitol, magnesium carbonate, magnesium oxide, maltitol, maltodextrin, maltose, mannitol, polydextrose, polyethylene glycol, pullulan, simethicone, sodium bicarbonate, sodium carbonate, sodium chloride, sorbitol, starch, sucrose, trehalose, and xylitol; preferably one or a combination of both lactose and microcrystalline cellulose, more preferably the lactose selected is lactose monohydrate and the microcrystalline cellulose selected is microcrystalline cellulose PH 102.
5. The pharmaceutical composition of claim 1 comprising BPI-7711 wherein said disintegrant comprises croscarmellose sodium, sodium carboxymethyl starch, hydroxypropyl cellulose, low substituted hydroxypropyl cellulose methyl cellulose, povidone, sodium starch glycolate; more preferably croscarmellose sodium.
6. The pharmaceutical composition of claim 1 comprising BPI-7711 wherein said lubricant comprises magnesium stearate, silicon dioxide, sodium stearyl fumarate, calcium stearate, sodium lauryl sulfate, talc; more preferably one or a combination of both magnesium stearate and colloidal silicon dioxide.
7. The pharmaceutical composition of claim 1 comprising BPI-7711 wherein said capsule shell comprises gelatin, hydroxypropyl cellulose, gelatin hollow capsules; more preferably gelatin empty capsules.
8. A process for the preparation of a pharmaceutical composition comprising BPI-7711 according to any of claims 1-7 comprising the steps of:
1) sieving the main drug BPI-7711, the diluent and the disintegrant in required weight percentage respectively, and mixing;
2) adding a lubricant into the material obtained in the step 1), and continuously mixing;
3) filling the materials obtained in the step 2) into capsule shells.
9. The preparation method according to claim 8, wherein the step 1) is carried out by using a 20-60 mesh sieve, more preferably a 30-45 mesh sieve.
10. The preparation method according to claim 8, wherein in the step 2), the silicon dioxide is added to the material obtained in the step 1) and mixed, and then the magnesium stearate is added and mixed continuously.
CN201911264353.1A 2019-12-11 2019-12-11 Pharmaceutical composition containing BPI-7711 and preparation method thereof Pending CN110898026A (en)

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CN110898026A (en) * 2019-12-11 2020-03-24 倍而达药业（苏州）有限公司 Pharmaceutical composition containing BPI-7711 and preparation method thereof

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2021115425A1 (en) * 2019-12-11 2021-06-17 倍而达药业（苏州）有限公司 Pharmaceutical composition containing bpi-7711 and preparation method thereof

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