CN115702900B - RMX2001 preparation composition - Google Patents
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- CN115702900B CN115702900B CN202110906154.7A CN202110906154A CN115702900B CN 115702900 B CN115702900 B CN 115702900B CN 202110906154 A CN202110906154 A CN 202110906154A CN 115702900 B CN115702900 B CN 115702900B
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- 238000002360 preparation method Methods 0.000 title abstract description 38
- 239000000203 mixture Substances 0.000 title abstract description 35
- 239000013022 formulation composition Substances 0.000 claims abstract description 19
- 239000002245 particle Substances 0.000 claims abstract description 15
- 239000003795 chemical substances by application Substances 0.000 claims abstract description 13
- 239000008186 active pharmaceutical agent Substances 0.000 claims abstract description 12
- 239000000945 filler Substances 0.000 claims abstract description 12
- 239000000314 lubricant Substances 0.000 claims abstract description 10
- 239000000853 adhesive Substances 0.000 claims abstract description 8
- 230000001070 adhesive effect Effects 0.000 claims abstract description 7
- 229920002785 Croscarmellose sodium Polymers 0.000 claims abstract description 6
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical group [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 claims abstract description 6
- 229960001681 croscarmellose sodium Drugs 0.000 claims abstract description 6
- 235000010947 crosslinked sodium carboxy methyl cellulose Nutrition 0.000 claims abstract description 6
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 claims description 11
- 229960001375 lactose Drugs 0.000 claims description 11
- 239000008101 lactose Substances 0.000 claims description 11
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims description 9
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims description 9
- 239000008108 microcrystalline cellulose Substances 0.000 claims description 9
- 229940016286 microcrystalline cellulose Drugs 0.000 claims description 9
- 238000005550 wet granulation Methods 0.000 claims description 9
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical group [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims description 8
- WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical group C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 claims description 5
- 229920003081 Povidone K 30 Polymers 0.000 claims description 5
- WSVLPVUVIUVCRA-KPKNDVKVSA-N Alpha-lactose monohydrate Chemical group O.O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O WSVLPVUVIUVCRA-KPKNDVKVSA-N 0.000 claims description 4
- 239000011230 binding agent Substances 0.000 claims description 4
- 229960001021 lactose monohydrate Drugs 0.000 claims description 4
- 235000019359 magnesium stearate Nutrition 0.000 claims description 4
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims description 4
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims description 4
- 229940069328 povidone Drugs 0.000 claims description 4
- 150000001875 compounds Chemical class 0.000 claims description 2
- 238000004090 dissolution Methods 0.000 abstract description 9
- 239000003814 drug Substances 0.000 abstract description 7
- 239000000843 powder Substances 0.000 abstract description 6
- 229940079593 drug Drugs 0.000 abstract description 5
- 238000005457 optimization Methods 0.000 abstract description 2
- 238000009472 formulation Methods 0.000 description 21
- 238000000034 method Methods 0.000 description 9
- 239000000463 material Substances 0.000 description 7
- 239000008194 pharmaceutical composition Substances 0.000 description 6
- 239000007962 solid dispersion Substances 0.000 description 6
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 6
- 239000007884 disintegrant Substances 0.000 description 5
- 238000007922 dissolution test Methods 0.000 description 5
- 230000000694 effects Effects 0.000 description 5
- 230000008569 process Effects 0.000 description 5
- 239000008187 granular material Substances 0.000 description 4
- 239000011812 mixed powder Substances 0.000 description 4
- 238000005469 granulation Methods 0.000 description 3
- 230000003179 granulation Effects 0.000 description 3
- 206010059866 Drug resistance Diseases 0.000 description 2
- 230000009471 action Effects 0.000 description 2
- 238000007908 dry granulation Methods 0.000 description 2
- 239000004615 ingredient Substances 0.000 description 2
- 230000001050 lubricating effect Effects 0.000 description 2
- 238000004519 manufacturing process Methods 0.000 description 2
- 238000005259 measurement Methods 0.000 description 2
- 238000002156 mixing Methods 0.000 description 2
- 238000012986 modification Methods 0.000 description 2
- 230000004048 modification Effects 0.000 description 2
- 201000009671 multidrug-resistant tuberculosis Diseases 0.000 description 2
- 239000000126 substance Substances 0.000 description 2
- 201000008827 tuberculosis Diseases 0.000 description 2
- IZXIZTKNFFYFOF-UHFFFAOYSA-N 2-Oxazolidone Chemical class O=C1NCCO1 IZXIZTKNFFYFOF-UHFFFAOYSA-N 0.000 description 1
- 241000192125 Firmicutes Species 0.000 description 1
- RJQXTJLFIWVMTO-TYNCELHUSA-N Methicillin Chemical compound COC1=CC=CC(OC)=C1C(=O)N[C@@H]1C(=O)N2[C@@H](C(O)=O)C(C)(C)S[C@@H]21 RJQXTJLFIWVMTO-TYNCELHUSA-N 0.000 description 1
- 241000191967 Staphylococcus aureus Species 0.000 description 1
- 241000193998 Streptococcus pneumoniae Species 0.000 description 1
- 108010059993 Vancomycin Proteins 0.000 description 1
- 230000000845 anti-microbial effect Effects 0.000 description 1
- 229940124350 antibacterial drug Drugs 0.000 description 1
- 230000001580 bacterial effect Effects 0.000 description 1
- 230000015572 biosynthetic process Effects 0.000 description 1
- 239000011248 coating agent Substances 0.000 description 1
- 238000000576 coating method Methods 0.000 description 1
- 230000001419 dependent effect Effects 0.000 description 1
- 239000010419 fine particle Substances 0.000 description 1
- 239000012530 fluid Substances 0.000 description 1
- 230000002496 gastric effect Effects 0.000 description 1
- 238000000338 in vitro Methods 0.000 description 1
- 208000015181 infectious disease Diseases 0.000 description 1
- 230000002401 inhibitory effect Effects 0.000 description 1
- 238000005304 joining Methods 0.000 description 1
- 238000000691 measurement method Methods 0.000 description 1
- 230000007246 mechanism Effects 0.000 description 1
- 229960003085 meticillin Drugs 0.000 description 1
- 238000001243 protein synthesis Methods 0.000 description 1
- 238000011084 recovery Methods 0.000 description 1
- 239000011343 solid material Substances 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
- 229940031000 streptococcus pneumoniae Drugs 0.000 description 1
- 230000014616 translation Effects 0.000 description 1
- MYPYJXKWCTUITO-LYRMYLQWSA-N vancomycin Chemical compound O([C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@H]1OC1=C2C=C3C=C1OC1=CC=C(C=C1Cl)[C@@H](O)[C@H](C(N[C@@H](CC(N)=O)C(=O)N[C@H]3C(=O)N[C@H]1C(=O)N[C@H](C(N[C@@H](C3=CC(O)=CC(O)=C3C=3C(O)=CC=C1C=3)C(O)=O)=O)[C@H](O)C1=CC=C(C(=C1)Cl)O2)=O)NC(=O)[C@@H](CC(C)C)NC)[C@H]1C[C@](C)(N)[C@H](O)[C@H](C)O1 MYPYJXKWCTUITO-LYRMYLQWSA-N 0.000 description 1
- 229960003165 vancomycin Drugs 0.000 description 1
- MYPYJXKWCTUITO-UHFFFAOYSA-N vancomycin Natural products O1C(C(=C2)Cl)=CC=C2C(O)C(C(NC(C2=CC(O)=CC(O)=C2C=2C(O)=CC=C3C=2)C(O)=O)=O)NC(=O)C3NC(=O)C2NC(=O)C(CC(N)=O)NC(=O)C(NC(=O)C(CC(C)C)NC)C(O)C(C=C3Cl)=CC=C3OC3=CC2=CC1=C3OC1OC(CO)C(O)C(O)C1OC1CC(C)(N)C(O)C(C)O1 MYPYJXKWCTUITO-UHFFFAOYSA-N 0.000 description 1
Abstract
The invention relates to the field of medicines, in particular to an RMX2001 preparation composition. The invention provides an RMX2001 preparation composition, which comprises the following components in percentage by weight: 2001 40 to 60 percent of RMX; 22-38% of filler; 2-10% of disintegrating agent; 3-17% of adhesive; 0.5 to 6.5 percent of lubricant; the disintegrating agent is selected from croscarmellose sodium; in the RMX2001 formulation composition, the API particle size meets the following conditions: d (D) 90 Is 60-120 mu m, D 50 20-50 mu m, D 10 And < 10 μm. The RMX2001 preparation composition provided by the invention has good powder property and good dissolution rate through the selection of the disintegrating agent, reasonable particle size and optimization of the preparation process, and has wide industrialization prospect.
Description
Technical Field
The invention relates to the field of medicines, in particular to an RMX2001 preparation composition.
Background
RMX2001 is a novel oxazolidinone derivative, mainly used for the treatment of drug-resistant gram-positive bacteria including MRSA (methicillin-resistant staphylococcus aureus), VRE (vancomycin-resistant enterococci), s.penumonia (streptococcus pneumoniae) caused infections and MDR-TB (multi-drug resistant tuberculosis). Because of the unique action mechanism, the drug is not easy to cross drug resistance with other antibacterial drugs inhibiting protein synthesis, and the generation of bacterial drug resistance is not easy to induce in vitro.
The structure of RMX2001 (compound 94) and the method of preparation have been disclosed in prior patent CN102171207B and are broadly mentioned as being able to be made into a form suitable for oral administration, but formulation compositions suitable for RMX2001 are not disclosed. In view of the excellent antimicrobial effect of RMX2001, there is an urgent clinical need to develop new formulations for better application to patients, meeting clinical needs.
Disclosure of Invention
In view of the above-described drawbacks of the prior art, an object of the present invention is to provide an RMX2001 formulation composition for solving the problems of the prior art.
To achieve the above and other related objects, in one aspect, the present invention provides an RMX2001 formulation composition, including, in weight percent:
the disintegrating agent is selected from croscarmellose sodium;
in the RMX2001 formulation composition, the API particle size meets the following conditions:
D 90 is 60-120 mu m, D 50 20-50 mu m, D 10 ＜10μm。
In some embodiments of the invention, the filler is selected from microcrystalline cellulose and/or lactose.
In some embodiments of the invention, the filler is selected from the group consisting of microcrystalline cellulose and lactose, the microcrystalline cellulose being 11 to 27% by weight and the lactose being 2 to 18% by weight. .
In some embodiments of the invention, the lactose is selected from lactose monohydrate.
In some embodiments of the invention, the binder is selected from povidone.
In some embodiments of the invention, the binder is selected from povidone K30.
In some embodiments of the invention, the lubricant is selected from magnesium stearate.
In another aspect the invention provides the use of an RMX2001 formulation composition as described above in the manufacture of a pharmaceutical formulation.
In another aspect, the present invention provides a pharmaceutical RMX2001 formulation, prepared from the composition of the RMX2001 formulation described above.
In some embodiments of the invention, the RMX2001 pharmaceutical formulation is prepared by a wet granulation process.
Detailed Description
In order to make the objects, technical solutions and advantageous technical effects of the present invention more apparent, the present invention will be further described in detail with reference to the following examples, and those skilled in the art can easily understand other advantages and effects of the present invention from the disclosure of the present specification.
The present inventors have made extensive practical studies to provide an RMX2001 formulation composition which has good powder properties, and has good dissolution after tabletting, and can have more excellent properties after granulating by a wet process, and have completed the present invention on the basis of this.
The first aspect of the present invention provides an RMX2001 formulation composition, including, in weight percent:
the disintegrating agent is selected from croscarmellose sodium;
in the RMX2001 formulation composition, the API (active pharmaceutical ingredients) particle size meets the following conditions:
D 90 is 60-120 mu m, D 50 20-50 mu m, D 10 ＜10μm。
The RMX2001 preparation composition provided by the invention comprises the following components in percentage by weightRMX2001 may be included in 40-60%, 40-42%, 42-44%, 44-46%, 46-48%, 48-50%, 50-52%, 52-54%, 54-56%, 56-58%, or 58-60%. In the above formulation composition, RMX2001 is a major active pharmaceutical ingredient (API, active pharmaceutical ingredients). As a main effective pharmaceutical ingredient, the API particle size of RMX2001 may generally meet the following conditions: d (D) 90 Can be 60 to 120 μm, 60 to 65 μm, 65 to 70 μm, 70 to 75 μm, 75 to 80 μm, 80 to 85 μm, 85 to 90 μm, 90 to 95 μm, 95 to 100 μm, 100 to 105 μm, 105 to 110 μm, 110 to 115 μm, or 115 to 120 μm, D 50 Can be 20 to 50 μm, 20 to 25 μm, 25 to 30 μm, 30 to 35 μm, 35 to 40 μm, 40 to 45 μm, or 45 to 50 μm, D 10 May be < 10 μm.
The RMX2001 preparation composition provided by the invention can comprise 22-38%, 22-24%, 24-26%, 26-28%, 28-30%, 30-32%, 32-34%, 34-36% and 36-38% of filler by weight percentage. Suitable fillers are generally solid materials that can improve the properties of the material by being added to the material, or can increase the capacity and weight of the material, thereby reducing the cost of the material. For example, the filler may be selected from one or more of microcrystalline cellulose, lactose, etc., preferably from a combination of microcrystalline cellulose and lactose, wherein the proportion of microcrystalline cellulose may be 11 to 27%, 11 to 13%, 13 to 15%, 15 to 17%, 17 to 19%, 19 to 21%, 21 to 23%, 23 to 25%, or 25 to 27%, and the proportion of lactose may be 2 to 18%, 2 to 4%, 4 to 6%, 6 to 8%, 8 to 10%, 10 to 12%, 12 to 14%, 14 to 16%, or 16 to 18% by weight. As another example, lactose may be lactose monohydrate.
The RMX2001 preparation composition provided by the invention can comprise 2-10%, 2-3%, 3-4%, 4-5%, 5-6%, 6-7%, 7-8%, 8-9% or 9-10% of disintegrating agent by weight percent. Suitable disintegrants generally refer to substances that enable a larger volume of the formulation to break up rapidly into fine particles in the gastrointestinal fluid, thereby enabling the functional ingredient to be rapidly dissolved and absorbed, thereby functioning.
The RMX2001 formulation composition provided by the invention can comprise 3-17%, 3-5%, 5-7%, 7-9%, or 9-11%, 11-13%, 13-15%, or 15-17% of adhesive by weight percent. Suitable adhesives are generally tacky substances, typically capable of joining two separate materials together by virtue of their tackiness. For example, the binder may be selected from povidone and the like. For another example, the povidone may be povidone K30.
The RMX2001 preparation composition provided by the invention can comprise 0.5-6.5%, 0.5-1%, 1-1.5%, 1.5-2%, 2-2.5%, 2.5-3%, 3-3.5%, 3.5-4%, 4-4.5%, 4.5-5%, 5-5.5%, 5.5-6%, or 6-6.5% of lubricant by weight percentage. Suitable lubricants are mainly some lubricating media capable of performing a lubricating function. For example, the lubricant may be selected from magnesium stearate and the like.
A second aspect of the invention provides the use of a RMX2001 formulation composition as provided in the first aspect of the invention, in the manufacture of a pharmaceutical formulation.
In a third aspect, the present invention provides a pharmaceutical formulation of RMX2001, prepared from the composition of the RMX2001 formulation provided in the first aspect of the present invention. Suitable methods for obtaining pharmaceutical formulations by preparation of the formulation compositions should be known to those skilled in the art, and preferably, RMX2001 pharmaceutical formulations may be prepared by wet granulation methods of preparation.
The RMX2001 preparation composition provided by the invention has good powder property and good dissolution rate through the selection of the disintegrating agent, reasonable particle size and optimization of the preparation process, and has wide industrialization prospect.
The present application is further illustrated by the following examples, which are not intended to limit the scope of the present application.
Example 1
The names and contents of the components used in the preparation formula 1, the preparation formula 2 and the preparation formula 3 are shown in the table 1, the particle sizes of the APIs in the preparation formula 1, the preparation formula 2 and the preparation formula 3 are shown in the table 2, the formula compositions in the three formulas are the same, and only the particle sizes of the APIs are different (shown in the table 2):
TABLE 1
| Component (A) | mg/tablet | %/tablet | Action |
| RMX2001 | 400 | 56.7 | Main medicine |
| Microcrystalline cellulose M102 | 140 | 19.9 | Filler (B) |
| Lactose monohydrate 200 mesh | 60 | 8.5 | Filler (B) |
| Croscarmellose sodium | 53 | 1.4 | Disintegrating agent |
| Povidone K30 | 40 | 5.7 | Adhesive agent |
| Magnesium stearate | 12 | 1.7 | Lubricant |
| Total weight of tablet core | 705 | 100.0 | NA |
| Opadry 03F180009 | 21.15 | 3％ | Coating material |
| Total weight of coated tablet | 726.15 | NA | NA |
TABLE 2
After the main medicine, the filler, the disintegrating agent, the adhesive and the lubricant are fully mixed, the fluidity, the bulk density of the total mixed powder, the content uniformity of the total mixed powder and other properties of the obtained powder are measured, and the measurement method is shown in table 2 by referring to the measurement results of Chinese pharmacopoeia (2020 edition). From the measurements in Table 2, the overall performance parameters of formulation 1 were poor.
Subsequently, the powder materials of the preparation formula 2 and the preparation formula 3 are subjected to total mixing partial pressure tablet, and the prepared tablet is subjected to dissolution test, wherein in the dissolution test, 4 mediums with different pH values are used, the test result of the preparation formula 2 is shown in the table 3, and the test result of the preparation formula 3 is shown in the table 4:
TABLE 3 Table 3
| Medium (D) | 5min | 10min | 15min | 30min | 45min | 60min |
| Water and its preparation method | 2 | 26 | 53 | 85 | 93 | 97 |
| pH1.2 | 3 | 12 | 40 | 72 | 95 | 95 |
| pH4.0 | 7 | 42 | 67 | 89 | 90 | 91 |
| pH6.8 | 2 | 13 | 45 | 80 | 93 | 95 |
TABLE 4 Table 4
| Medium (D) | 5min | 10min | 15min | 30min | 45min | 60min |
| Water and its preparation method | 1 | 19 | 45 | 72 | 75 | 83 |
| pH1.2 | 2 | 10 | 29 | 52 | 63 | 74 |
| pH4.0 | 5 | 23 | 41 | 61 | 72 | 84 |
| pH6.8 | 1 | 8 | 28 | 58 | 66 | 77 |
From the results of tables 3 and 4, it can be seen that formulation 2 has significantly faster dissolution than formulation 3.
It can be seen that the combination property of formulation 2 has significant advantages in comparison of formulation 1, formulation 2 and formulation 3. Therefore, the preparation formula 2 has reasonable selection of the particle size of the API, and the prepared preparation has excellent effects on dissolution, fluidity, bulk density of total mixed powder, content uniformity of total mixed powder and the like.
Example 2
To further verify the effect of the disintegrant on dissolution, we screened the disintegrant on the premise of determining a reasonable particle size, and specifically, the names and contents of the components used in formulation 2, formulation 4, formulation 5 are shown in table 5, and the particle size of RMX2001 in the three formulations meets the following criteria: d (D) 90 Is 60-120 mu m, D 50 20-50 mu m, D 10 ＜10μm。
TABLE 5
After the main drug, the filler, the disintegrating agent, the adhesive and the lubricant are fully mixed, the powder is subjected to total mixing and tabletting, and the prepared tabletting is subjected to dissolution test, wherein in the dissolution test, 4 mediums with different pH values are used, the paddle method/50 rpm/900 ml/N=6, the test result of the preparation formula 2 is shown in table 3, the test result of the preparation formula 4 is shown in table 4, and the test result of the preparation formula 5 is shown in table 4:
TABLE 6
| Medium (D) | 5min | 10min | 15min | 30min | 45min | 60min |
| Water and its preparation method | 2 | 26 | 53 | 85 | 93 | 97 |
| pH1.2 | 3 | 12 | 40 | 72 | 95 | 95 |
| pH4.0 | 7 | 42 | 67 | 89 | 90 | 91 |
| pH6.8 | 2 | 13 | 45 | 80 | 93 | 95 |
TABLE 7
| Medium (D) | 5min | 10min | 15min | 30min | 45min | 60min |
| Water and its preparation method | 2 | 22 | 47 | 81 | 88 | 92 |
| pH1.2 | 3 | 13 | 36 | 60 | 78 | 82 |
| pH4.0 | 7 | 45 | 65 | 78 | 83 | 90 |
| pH6.8 | 2 | 11 | 42 | 77 | 84 | 93 |
TABLE 8
| Medium (D) | 5min | 10min | 15min | 30min | 45min | 60min |
| Water and its preparation method | 2 | 26 | 53 | 75 | 83 | 87 |
| pH1.2 | 3 | 12 | 40 | 62 | 75 | 85 |
| pH4.0 | 7 | 42 | 67 | 79 | 90 | 91 |
| pH6.8 | 2 | 13 | 45 | 60 | 73 | 85 |
From the results of tables 6, 7 and 8, it can be seen that the formulation dissolution rate of formulation 2 is not pH dependent and is significantly faster than formulation 4 and formulation 5, thus the dissolution rate of the disintegrant, croscarmellose sodium, is significantly better than other disintegrants.
Example 3
After determining the disintegrating agent and particle size, we have also made a search for the preparation process, and the formulation 2 was prepared by wet granulation, dry granulation, and solid dispersion (RMX 2001 and PVP K30 were co-dissolved in water, and then spray-dried to remove the solvent).
During granulation, parameters such as granulation continuity, granule forming rate and recovery rate were observed, and hardness of the prepared tablets was measured, and specific results are shown in table 9:
TABLE 9
As can be seen from Table 9, the yield of the product obtained by the dry granulation process did not meet the industrial requirements, while the wet granulation and solid dispersion preparation processes had good results in granulation continuity, granule formation rate, and tablet hardness.
The prepared particles are subjected to dissolution test under the following conditions: the test results of the granules obtained by the two processes of wet granulation and solid dispersion, ph1.2 HCl/paddle/50 rpm/900 ml/n=6, are shown in table 10:
table 10
| 5min | 10min | 15min | 30min | 45min | 60min | |
| Wet granulation | 2 | 26 | 53 | 85 | 93 | 97 |
| Solid dispersion | 3 | 29 | 58 | 89 | 98 | 99 |
As can be seen from table 10, the yields of both wet granulation and solid dispersion processes were substantially the same as the 0 day dissolution.
The effect factor of the obtained particles was studied, and the results of the light test (4500LX+500 LX, 85.+ -. 10. Mu.w/cm 2) with pH1.2 HCl are shown in Table 11:
TABLE 11
The results of the high temperature test (60 ℃ C.) for pH1.2 HCl are shown in Table 12:
table 12
Results of the high humidity test (25 ℃ C./relative humidity 90% + -5%) with pH1.2 HCl are shown in Table 13:
TABLE 13
From the above results, it is clear that the overall properties of the granules obtained by wet granulation are significantly better than those of the solid dispersion process.
In summary, the present invention effectively overcomes the disadvantages of the prior art and has high industrial utility value.
The above embodiments are merely illustrative of the principles of the present invention and its effectiveness, and are not intended to limit the invention. Modifications and variations may be made to the above-described embodiments by those skilled in the art without departing from the spirit and scope of the invention. Accordingly, it is intended that all equivalent modifications and variations of the invention be covered by the claims, which are within the ordinary skill of the art, be within the spirit and scope of the present disclosure.
Claims (4)
1. An RMX2001 formulation composition, comprising, in weight percent:
RMX2001 40~60%；
22-38% of filler;
2-10% of a disintegrating agent;
3-17% of an adhesive;
0.5-6.5% of lubricant;
the disintegrating agent is croscarmellose sodium;
in the RMX2001 formulation composition, the API particle size meets the following conditions:
D 90 is 60-120 mu m, D 50 20-50 μm, D 10 ＜10μm；
The filler is a combination of microcrystalline cellulose and lactose, the weight percentage of the microcrystalline cellulose is 11-27%, and the weight percentage of the lactose is 2-18%;
the adhesive is povidone;
the lubricant is magnesium stearate;
the RMX2001 is a compound of the structure:
。
2. the RMX2001 formulation composition according to claim 1, wherein said lactose is lactose monohydrate.
3. The RMX2001 formulation composition according to claim 1, wherein said binder is povidone K30.
4. The RMX 2001-formulation composition as claimed in claim 1, wherein the RMX 2001-formulation composition is prepared by a wet granulation process.
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| CN116621828A (en) * | 2022-02-10 | 2023-08-22 | 上海纳为生物技术有限公司 | Crystal forms of oxazolidinone derivative, preparation method and application thereof |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| WO2021195594A1 (en) * | 2020-03-26 | 2021-09-30 | San Diego State University (SDSU) Foundation, dba San Diego State University Research Foundation | Compositions and methods for treating or ameliorating infections |
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Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
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