CN102988316A - Efavirenz tablet and preparation method thereof - Google Patents
Efavirenz tablet and preparation method thereof Download PDFInfo
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- CN102988316A CN102988316A CN2012104787731A CN201210478773A CN102988316A CN 102988316 A CN102988316 A CN 102988316A CN 2012104787731 A CN2012104787731 A CN 2012104787731A CN 201210478773 A CN201210478773 A CN 201210478773A CN 102988316 A CN102988316 A CN 102988316A
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- efavirenz
- weight portions
- sheet
- weight
- cellulose
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- XPOQHMRABVBWPR-UHFFFAOYSA-N Efavirenz Natural products O1C(=O)NC2=CC=C(Cl)C=C2C1(C(F)(F)F)C#CC1CC1 XPOQHMRABVBWPR-UHFFFAOYSA-N 0.000 title claims abstract description 81
- 229960003804 efavirenz Drugs 0.000 title claims abstract description 81
- XPOQHMRABVBWPR-ZDUSSCGKSA-N efavirenz Chemical compound C([C@]1(C2=CC(Cl)=CC=C2NC(=O)O1)C(F)(F)F)#CC1CC1 XPOQHMRABVBWPR-ZDUSSCGKSA-N 0.000 title claims abstract description 81
- 238000002360 preparation method Methods 0.000 title claims description 7
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims abstract description 34
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 claims abstract description 22
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 claims abstract description 17
- RCEAADKTGXTDOA-UHFFFAOYSA-N OS(O)(=O)=O.CCCCCCCCCCCC[Na] Chemical compound OS(O)(=O)=O.CCCCCCCCCCCC[Na] RCEAADKTGXTDOA-UHFFFAOYSA-N 0.000 claims abstract description 17
- 239000001863 hydroxypropyl cellulose Substances 0.000 claims abstract description 17
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 claims abstract description 17
- 235000019359 magnesium stearate Nutrition 0.000 claims abstract description 17
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims abstract description 16
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims abstract description 16
- 239000008108 microcrystalline cellulose Substances 0.000 claims abstract description 16
- 229940016286 microcrystalline cellulose Drugs 0.000 claims abstract description 16
- 239000002994 raw material Substances 0.000 claims abstract description 6
- 238000005303 weighing Methods 0.000 claims description 24
- 239000001768 carboxy methyl cellulose Substances 0.000 claims description 20
- 238000004132 cross linking Methods 0.000 claims description 20
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 claims description 20
- 229920001027 sodium carboxymethylcellulose Polymers 0.000 claims description 20
- DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical compound [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 claims description 16
- 239000004141 Sodium laurylsulphate Substances 0.000 claims description 16
- 239000007864 aqueous solution Substances 0.000 claims description 16
- -1 hydroxypropyl Chemical group 0.000 claims description 16
- 235000019333 sodium laurylsulphate Nutrition 0.000 claims description 16
- 239000008187 granular material Substances 0.000 claims description 15
- 239000007779 soft material Substances 0.000 claims description 12
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 10
- 239000000203 mixture Substances 0.000 claims description 10
- 239000000243 solution Substances 0.000 claims description 10
- 239000011248 coating agent Substances 0.000 claims description 5
- 238000000576 coating method Methods 0.000 claims description 5
- 238000005469 granulation Methods 0.000 claims description 5
- 230000003179 granulation Effects 0.000 claims description 5
- 239000003814 drug Substances 0.000 claims description 3
- 238000004090 dissolution Methods 0.000 abstract description 3
- 210000001035 gastrointestinal tract Anatomy 0.000 abstract description 3
- 229920002785 Croscarmellose sodium Polymers 0.000 abstract 2
- 229960001681 croscarmellose sodium Drugs 0.000 abstract 2
- 235000010947 crosslinked sodium carboxy methyl cellulose Nutrition 0.000 abstract 2
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 abstract 1
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 abstract 1
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 abstract 1
- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 abstract 1
- 229940071676 hydroxypropylcellulose Drugs 0.000 abstract 1
- 238000000034 method Methods 0.000 description 6
- 241000282414 Homo sapiens Species 0.000 description 5
- 230000000694 effects Effects 0.000 description 4
- 238000002386 leaching Methods 0.000 description 4
- 239000012738 dissolution medium Substances 0.000 description 3
- 238000002474 experimental method Methods 0.000 description 3
- 238000005070 sampling Methods 0.000 description 3
- 238000010521 absorption reaction Methods 0.000 description 2
- 239000002671 adjuvant Substances 0.000 description 2
- 238000001727 in vivo Methods 0.000 description 2
- 230000000968 intestinal effect Effects 0.000 description 2
- 238000004519 manufacturing process Methods 0.000 description 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 2
- BHQCQFFYRZLCQQ-UHFFFAOYSA-N (3alpha,5alpha,7alpha,12alpha)-3,7,12-trihydroxy-cholan-24-oic acid Natural products OC1CC2CC(O)CCC2(C)C2C1C1CCC(C(CCC(O)=O)C)C1(C)C(O)C2 BHQCQFFYRZLCQQ-UHFFFAOYSA-N 0.000 description 1
- 208000030507 AIDS Diseases 0.000 description 1
- 239000004380 Cholic acid Substances 0.000 description 1
- 241000713772 Human immunodeficiency virus 1 Species 0.000 description 1
- 208000036142 Viral infection Diseases 0.000 description 1
- 241000700605 Viruses Species 0.000 description 1
- 239000011149 active material Substances 0.000 description 1
- 238000007792 addition Methods 0.000 description 1
- 210000000941 bile Anatomy 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 235000019416 cholic acid Nutrition 0.000 description 1
- BHQCQFFYRZLCQQ-OELDTZBJSA-N cholic acid Chemical compound C([C@H]1C[C@H]2O)[C@H](O)CC[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@H]([C@@H](CCC(O)=O)C)[C@@]2(C)[C@@H](O)C1 BHQCQFFYRZLCQQ-OELDTZBJSA-N 0.000 description 1
- 229960002471 cholic acid Drugs 0.000 description 1
- 150000001875 compounds Chemical class 0.000 description 1
- 230000008878 coupling Effects 0.000 description 1
- 238000010168 coupling process Methods 0.000 description 1
- 238000005859 coupling reaction Methods 0.000 description 1
- KXGVEGMKQFWNSR-UHFFFAOYSA-N deoxycholic acid Natural products C1CC2CC(O)CCC2(C)C2C1C1CCC(C(CCC(O)=O)C)C1(C)C(O)C2 KXGVEGMKQFWNSR-UHFFFAOYSA-N 0.000 description 1
- 235000005911 diet Nutrition 0.000 description 1
- 230000037213 diet Effects 0.000 description 1
- 238000007922 dissolution test Methods 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 229940029119 efavirenz 600 mg Drugs 0.000 description 1
- 238000005516 engineering process Methods 0.000 description 1
- 238000000605 extraction Methods 0.000 description 1
- 235000009200 high fat diet Nutrition 0.000 description 1
- 239000004615 ingredient Substances 0.000 description 1
- 230000007774 longterm Effects 0.000 description 1
- 238000010297 mechanical methods and process Methods 0.000 description 1
- 230000005226 mechanical processes and functions Effects 0.000 description 1
- 229940042402 non-nucleoside reverse transcriptase inhibitor Drugs 0.000 description 1
- 239000002726 nonnucleoside reverse transcriptase inhibitor Substances 0.000 description 1
- 230000035699 permeability Effects 0.000 description 1
- 230000036470 plasma concentration Effects 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 230000028327 secretion Effects 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 230000009385 viral infection Effects 0.000 description 1
- 239000002699 waste material Substances 0.000 description 1
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Abstract
The invention discloses an efavirenz tablet which is prepared from the following raw materials in parts by weight: 65-75 parts of efavirenz, 10-15 parts of croscarmellose sodium, 7-9 parts of microcrystalline cellulose and 7-12 parts of lauryl sodium sulfate, hydroxy propyl cellulose, magnesium stearate and hydroxypropyl methyl cellulose in total. The dispersibility of the efavirenz tablet in the intestinal tract is improved and the dissolution speed of efavirenz is improved by increasing the using amount of the croscarmellose sodium, and therefore the efavirenz can be rapidly absorbed and utilized.
Description
Technical field
The present invention relates to the pharmaceutics field, be specifically related to a kind of efavirenz sheet and preparation method thereof.
Background technology
Efavirenz is the non-nucleoside reverse transcriptase inhibitor of anti-HIV-1 virus of new generation, and is alone or be used for the treatment of AIDS viral infection with the other drug coupling clinically.The monolithic tablet 1.2g that weighs of the commercially available efavirenz sheet of tradition wherein contains 50% efavirenz, 5% cross-linking sodium carboxymethyl cellulose, 20% microcrystalline Cellulose, and surplus is ancillary additions.Because the weight of its monolithic tablet is 1.2g, so its volume of producing the efavirenz sheet that obtains is larger, is unfavorable for suffering from the patient and takes, for some young patients, even stop up throat, cause security incident.
The pharmacokinetics experiment shows, healthy volunteer's single oral 100～1600mg tradition efavirenz sheet, peak time (Tmax) is about 5 hours, maximum plasma concentration (Cmax) is 1.6～9.1uM, Cmax and bioavailability (AUC) increase with dosage in 100～1600mg dosage range, but increment rate reduces gradually; The commercially available efavirenz sheet of the oral tradition of HIV-1 infected patient is the result show, is respectively 200,400 at daily dose, during 600mg, and Cmin and AUC increase with the increase of dosage when Tmax and stable state, reach stable state after oral 6～10 days, about 3～5 hours of Tmax.This shows that traditional efavirenz sheet absorbs slowly in vivo, when dosage became large, effective ingredient can not be absorbed fully.
Therefore, being necessary to provide a kind of can be absorbed by the body and efavirenz sheet that tablet is little fast.
Summary of the invention
The purpose of this invention is to provide a kind of efavirenz sheet, be easier to be absorbed by the body.
For achieving the above object, the present invention has adopted following technical scheme:
A kind of efavirenz sheet, comprise following components by weight percent raw material: efavirenz 65～75 weight portions, cross-linking sodium carboxymethyl cellulose 10～15 weight portions, microcrystalline Cellulose 7～9 weight portions, sodium lauryl sulphate, hydroxypropyl cellulose, magnesium stearate and hydroxypropyl emthylcellulose be totally 7～12 weight portions.
Because efavirenz is for having hygroscopic crystalline powder, the about 9ug/ml of dissolubility in water, that is, bad dispersibility in water, but its permeability higher (Log P=5.4), biopharmaceutics is classified and is belonged to the II compounds.Therefore want to improve the dispersibility of efavirenz in gastrointestinal tract so that human body can just absorb efavirenz fast.The applicant finds by long term test, the bile that human body is secreted after diet can increase the assimilation effect to efavirenz, particularly its assimilation effect more is significantly increased after the high fat diet, therefore having surface-active material can improve the dispersibility of efavirenz in intestinal, so that efavirenz is absorbed fast.Therefore among the application, by increasing the consumption of cross-linking sodium carboxymethyl cellulose, thereby improve the dispersibility of efavirenz sheet in intestinal, improve the dissolution rate of efavirenz, thereby so that efavirenz can be absorbed fast and utilize.In the specific implementation, can choose allotment to the ratio of sodium lauryl sulphate, hydroxypropyl cellulose, magnesium stearate and hydroxypropyl emthylcellulose according to practical operation, as according to sodium lauryl sulphate 1～3 weight portion, hydroxypropyl cellulose 3～4 weight portions, magnesium stearate 1～2 weight portion, hydroxypropyl emthylcellulose 2～3 weight portions take by weighing respectively waste efavirenz sheet, to obtain better effect.
Simultaneously, therefore of paramount importance another inventive point is exactly its size that can reduce the tablet tablet among the application, by reducing the consumption of the adjuvants such as microcrystalline Cellulose, thereby so that the tablet that makes is less, being easier to the patient takes, in actual mechanical process, guaranteeing that the efavirenz sheet has under the prerequisite of good therapeutic effect, that is in the monolithic tablet under the satisfactory prerequisite of efavirenz content, monolithic tablet weight that can the efavirenz sheet is set to 0.80～0.93g, reduce the consumption of adjuvant, reduce production cost, improve the productivity effect of efavirenz sheet.
Another purpose of the application is to provide the preparation method of foregoing efavirenz sheet, and its scheme of taking is that a kind of preparation method of efavirenz sheet may further comprise the steps:
S1: the medicine that accurately takes by weighing parts by weight as claimed in claim 1 is for subsequent use:
S2: will weigh up the sodium lauryl sulphate of getting and be made into lauryl sodium sulfate aqueous solution; The efavirenz that then will take by weighing, microcrystalline Cellulose, hydroxypropyl cellulose and 3/10～6/10 cross-linking sodium carboxymethyl cellulose add to configure and mix into soft material in the lauryl sodium sulfate aqueous solution and with the soft material pelletize, and the granule mix homogeneously after the magnesium stearate that will take by weighing again and remaining cross-linking sodium carboxymethyl cellulose and the pelletize also carries out tabletting and makes tablet;
S3: the hydroxypropyl emthylcellulose that will take by weighing is mixed with 5% solution with 85% ethanol, adopts this solution that the tablet for preparing among the S2 is carried out coating, can obtain finished product efavirenz sheet.
The soft material of producing among the described step S2 carries out pelletize through 18～24 order granulation screen clothes, and the granule after the pelletize needs to carry out granulate through 18～24 purpose screen clothes.
The result of extraction of producing the efavirenz sheet that obtains by such scheme is easier to the absorption of human body more.
In actual production, preferably recently produce the efavirenz sheet according to the weight of defined in three schemes of following A～C, it is with respect to realizing other parameter schemes of the present application purpose, and the dissolving out capability of efavirenz improves 1～2 percentage point approximately, wherein more preferred A scheme:
The A scheme is: efavirenz 75 weight portions, cross-linking sodium carboxymethyl cellulose 10 weight portions, microcrystalline Cellulose 7 weight portions, sodium lauryl sulphate 1 weight portion, hydroxypropyl cellulose 3 weight portions, magnesium stearate 2 weight portions, hydroxypropyl emthylcellulose 2 weight portions.
The B scheme is: efavirenz 65 weight portions, cross-linking sodium carboxymethyl cellulose 15 weight portions, microcrystalline Cellulose 9 weight portions, sodium lauryl sulphate 3 weight portions, hydroxypropyl cellulose 4 weight portions, magnesium stearate 1 weight portion, hydroxypropyl emthylcellulose 3 weight portions.
The C scheme is: efavirenz 71 weight portions, cross-linking sodium carboxymethyl cellulose 12 weight portions, microcrystalline Cellulose 8 weight portions, sodium lauryl sulphate 2 weight portions, hydroxypropyl cellulose 4 weight portions, magnesium stearate 1 weight portion, hydroxypropyl emthylcellulose 2 weight portions.
Description of drawings
Fig. 1 is the stripping curve comparison in 0.5% lauryl sodium sulfate aqueous solution of efavirenz sheet;
Fig. 2 is the stripping curve comparison in 1% lauryl sodium sulfate aqueous solution of efavirenz sheet;
Fig. 3 is the stripping curve comparison in 2% lauryl sodium sulfate aqueous solution of efavirenz sheet.
The specific embodiment
Below come the application is described further by specific embodiment.Wherein embodiment 1～3 is the experiment of producing of efavirenz sheet, and prepared efavirenz sheet contains the 600mg efavirenz by the monolithic agent and produces.Embodiment 4 is the dissolution test comparison with traditional commercially available efavirenz sheet of the efavirenz sheet produced.
Embodiment 1
(1) raw material by each listed in the table 1 weight takes by weighing.
The sodium lauryl sulphate that (2) will take by weighing is water-soluble, is made into lauryl sodium sulfate aqueous solution; The efavirenz that then will take by weighing, microcrystalline Cellulose, hydroxypropyl cellulose add to configure with 3/10 cross-linking sodium carboxymethyl cellulose and mix into soft material in the lauryl sodium sulfate aqueous solution, soft material is carried out pelletize in 18～24 order granulation screen clothes, the granule after the pelletize is carrying out granulate through 18～24 purpose screen clothes.And then the granule mix homogeneously after the magnesium stearate that will take by weighing and remaining cross-linking sodium carboxymethyl cellulose and the pelletize and carry out tabletting and make 1000 tablets of tablets;
The hydroxypropyl emthylcellulose that (3) will take by weighing is mixed with 5% solution with 85% ethanol, adopts this solution that the tablet for preparing among the S2 is carried out coating, can obtain finished product efavirenz sheet, and the average quality that records monolithic efavirenz sheet is 0.800g.
The prescription of table 1 efavirenz sheet forms (A)
Embodiment 2
(1) raw material by each listed in the table 2 weight takes by weighing.
The sodium lauryl sulphate that (2) will take by weighing is water-soluble, is made into lauryl sodium sulfate aqueous solution; The efavirenz that then will take by weighing, microcrystalline Cellulose, hydroxypropyl cellulose add to configure with 1/2 cross-linking sodium carboxymethyl cellulose and mix into soft material in the lauryl sodium sulfate aqueous solution, soft material is carried out pelletize in 18～24 order granulation screen clothes, the granule after the pelletize is carrying out granulate through 18～24 purpose screen clothes.And then the granule mix homogeneously after the magnesium stearate that will take by weighing and remaining cross-linking sodium carboxymethyl cellulose and the pelletize and carry out tabletting and make 1000 tablets of tablets;
The hydroxypropyl emthylcellulose that (3) will take by weighing is mixed with 5% solution with 85% ethanol, adopts this solution that the tablet for preparing among the S2 is carried out coating, can obtain finished product efavirenz sheet, and the average quality that records monolithic efavirenz sheet is 0.845g.
The prescription of table 2 efavirenz sheet forms (B)
Embodiment 3
(1) raw material by each listed in the table 3 weight takes by weighing.
The prescription of table 3 efavirenz sheet forms (C)
The sodium lauryl sulphate that (2) will take by weighing is water-soluble, is made into lauryl sodium sulfate aqueous solution; The efavirenz that then will take by weighing, microcrystalline Cellulose, hydroxypropyl cellulose add to configure with 1/2 cross-linking sodium carboxymethyl cellulose and mix into soft material in the lauryl sodium sulfate aqueous solution, soft material is carried out pelletize in 18～24 order granulation screen clothes, the granule after the pelletize is carrying out granulate through 18～24 purpose screen clothes.And then the granule mix homogeneously after the magnesium stearate that will take by weighing and remaining cross-linking sodium carboxymethyl cellulose and the pelletize and be pressed into 1000 tablets of tablets.
The hydroxypropyl emthylcellulose that (3) will take by weighing is mixed with 5% solution with 85% ethanol, adopts this solution that the tablet for preparing among the S2 is carried out coating, can obtain finished product efavirenz sheet, and the average quality that records monolithic efavirenz sheet is 0.923g.
Embodiment 4
Get efavirenz sheet made among the embodiment 1～3 and traditional commercially available efavirenz sheet (the heavy 1.2g of monolithic contains efavirenz 600mg) and in following leaching condition, carry out respectively the stripping experiment.
Operation (1)
Leaching condition: 0.5% lauryl sodium sulfate aqueous solution, dissolution medium volume 900ml, oar method 50rpm, the UV method is measured.Sampling time point: 10,15,25,35 minutes.Experimental result as shown in Figure 1.
Operation (2)
Leaching condition: 1% lauryl sodium sulfate aqueous solution, dissolution medium volume 900ml, oar method 50rpm, the UV method is measured.Sampling time point: 10,15,25,35 minutes.Experimental result as shown in Figure 2.
Operation (3)
Leaching condition: 2% lauryl sodium sulfate aqueous solution, dissolution medium volume 900ml, oar method 50rpm, the UV method is measured.Sampling time point: 10,15,25,35 minutes.Experimental result as shown in Figure 3.
Interpretation of result: by experimental result in Fig. 1～3 obviously as can be known, the application makes the commercially available efavirenz sheet of efavirenz sheet and tradition and compares and have better dissolution rate, therefore the impact that is subject to gastrointestinal tract environment in the body is less, even also can be dispersed fast absorption in the not enough situation of the secretion such as cholic acid in vivo, can better be absorbed fast by human body.Its tablet is little simultaneously, is easier to take.
Claims (7)
1. efavirenz sheet comprises following components by weight percent raw material:
Efavirenz 65～75 weight portions, cross-linking sodium carboxymethyl cellulose 10～15 weight portions, microcrystalline Cellulose 7～9 weight portions, sodium lauryl sulphate, hydroxypropyl cellulose, magnesium stearate and hydroxypropyl emthylcellulose be totally 7～12 weight portions.
2. efavirenz sheet as claimed in claim 1, it is characterized in that: the monolithic tablet weight of described efavirenz sheet is 0.80～0.93g; Described sodium lauryl sulphate 1～3 weight portion, hydroxypropyl cellulose 3～4 weight portions, magnesium stearate 1～2 weight portion, hydroxypropyl emthylcellulose 2～3 weight portions.
3. efavirenz sheet as claimed in claim 1 or 2, it is characterized in that: efavirenz 75 weight portions, cross-linking sodium carboxymethyl cellulose 10 weight portions, microcrystalline Cellulose 7 weight portions, sodium lauryl sulphate 1 weight portion, hydroxypropyl cellulose 3 weight portions, magnesium stearate 2 weight portions, hydroxypropyl emthylcellulose 2 weight portions.
4. efavirenz sheet as claimed in claim 1 or 2, it is characterized in that: efavirenz 65 weight portions, cross-linking sodium carboxymethyl cellulose 15 weight portions, microcrystalline Cellulose 9 weight portions, sodium lauryl sulphate 3 weight portions, hydroxypropyl cellulose 4 weight portions, magnesium stearate 1 weight portion, hydroxypropyl emthylcellulose 3 weight portions.
5. efavirenz sheet as claimed in claim 1 or 2, it is characterized in that: efavirenz 71 weight portions, cross-linking sodium carboxymethyl cellulose 12 weight portions, microcrystalline Cellulose 8 weight portions, sodium lauryl sulphate 2 weight portions, hydroxypropyl cellulose 4 weight portions, magnesium stearate 1 weight portion, hydroxypropyl emthylcellulose 2 weight portions.
6. preparation method of efavirenz sheet as claimed in claim 1 may further comprise the steps:
S1: the medicine that accurately takes by weighing parts by weight as claimed in claim 1 is for subsequent use:
S2: will weigh up the sodium lauryl sulphate of getting and be made into lauryl sodium sulfate aqueous solution; The efavirenz that then will take by weighing, microcrystalline Cellulose, hydroxypropyl cellulose and 3/10～6/10 cross-linking sodium carboxymethyl cellulose add to configure and mix into soft material in the lauryl sodium sulfate aqueous solution and with the soft material pelletize, and the granule mix homogeneously after the magnesium stearate that will take by weighing again and remaining cross-linking sodium carboxymethyl cellulose and the pelletize also carries out tabletting and makes tablet;
S3: the hydroxypropyl emthylcellulose that will take by weighing is mixed with 5% solution with 85% ethanol, adopts this solution that the tablet for preparing among the S2 is carried out coating, can obtain finished product efavirenz sheet.
7. the preparation method of efavirenz sheet as claimed in claim 6, it is characterized in that: the soft material of producing among the described step S2 carries out pelletize through 18～24 order granulation screen clothes, and the granule after the pelletize needs carry out granulate through 18～24 purpose screen clothes.
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201210478773.1A CN102988316B (en) | 2012-11-22 | 2012-11-22 | Efavirenz tablet and preparation method thereof |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201210478773.1A CN102988316B (en) | 2012-11-22 | 2012-11-22 | Efavirenz tablet and preparation method thereof |
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| CN102988316A true CN102988316A (en) | 2013-03-27 |
| CN102988316B CN102988316B (en) | 2014-11-26 |
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Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107582531A (en) * | 2016-07-06 | 2018-01-16 | 四川科伦药物研究院有限公司 | A kind of razaxaban solid pharmaceutical preparation and preparation method thereof |
| CN114425039A (en) * | 2020-10-29 | 2022-05-03 | 上海迪赛诺药业股份有限公司 | Improved efavirenz quick-release preparation |
| CN114948970A (en) * | 2022-06-07 | 2022-08-30 | 安徽贝克生物制药有限公司 | Efavirenz-containing pharmaceutical composition and preparation method thereof |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2010125572A1 (en) * | 2009-04-29 | 2010-11-04 | Hetero Research Foundation | Compressed tablets and capsules containing efavirenz |
-
2012
- 2012-11-22 CN CN201210478773.1A patent/CN102988316B/en active Active
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2010125572A1 (en) * | 2009-04-29 | 2010-11-04 | Hetero Research Foundation | Compressed tablets and capsules containing efavirenz |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107582531A (en) * | 2016-07-06 | 2018-01-16 | 四川科伦药物研究院有限公司 | A kind of razaxaban solid pharmaceutical preparation and preparation method thereof |
| CN114425039A (en) * | 2020-10-29 | 2022-05-03 | 上海迪赛诺药业股份有限公司 | Improved efavirenz quick-release preparation |
| CN114425039B (en) * | 2020-10-29 | 2023-12-15 | 上海迪赛诺医药集团股份有限公司 | Improved immediate release formulations of efavirenz |
| CN114948970A (en) * | 2022-06-07 | 2022-08-30 | 安徽贝克生物制药有限公司 | Efavirenz-containing pharmaceutical composition and preparation method thereof |
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| Publication number | Publication date |
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| CN102988316B (en) | 2014-11-26 |
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