CN109381440A - A kind of Ai Le replaces nylon 6 combination - Google Patents
A kind of Ai Le replaces nylon 6 combination Download PDFInfo
- Publication number
- CN109381440A CN109381440A CN201811357402.1A CN201811357402A CN109381440A CN 109381440 A CN109381440 A CN 109381440A CN 201811357402 A CN201811357402 A CN 201811357402A CN 109381440 A CN109381440 A CN 109381440A
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- CN
- China
- Prior art keywords
- buddhist nun
- recipe quantity
- calcium sulfate
- fumed silica
- tween
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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Classifications
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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
- A61K9/4858—Organic 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- 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
- A61K9/485—Inorganic compounds
-
- 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 present invention relates to a kind of Ai Le to replace Buddhist nun's oral drugs, belongs to technical field of medicine.Ai Le of the present invention replaces nylon 6 combination, in every thousand unit doses, contain D90Buddhist nun 150g, Tween 80 4-8g, fumed silica 8-26g, calcium sulfate 2-8g, hydroxypropyl cellulose 18-32g, Lactis Anhydrous 20-46g, disodium ethylene diamine tetraacetate 4-8g, magnesium stearate 1.0-1.5g are replaced for 36-55 microns of Ai Le.Technical solution of the present invention is by the reasonable compatibilities of several components, first is that the dissolution of main ingredient is improved, second is that the connection of fumed silica, calcium sulfate, disodium ethylene diamine tetraacetate and effect, improve the anti-moisture absorption property during storage.
Description
Technical field
The present invention relates to a kind of Ai Le to replace Buddhist nun's oral drugs, belongs to technical field of medicine.
Background technique
Lung cancer is one of most common malignant tumour in the world, has become China's urban population Death Cause for Malignant Tumors
1st.Non-small cell type lung cancer includes squamous cell carcinoma (squamous carcinoma), gland cancer, large cell carcinoma, its cancer cell compared with small cell carcinoma
Growth division is slower, and diffusion transfer is relatively late.Non-small cell lung cancer accounts for about the 80% of all lung cancer, when about 75% Finding case
It is in middle and advanced stage, survival rate is very low within 5 years.
Ai Le for Buddhist nun (also known as A Lei replace Buddhist nun, alectinib), be through FDA approval for ALK positive metastatic it is non-small
The first-line treatment of cell lung cancer (NSCLC) patient.The medicine is researched and developed by Roche group.
The ALEX test discovery Ai Le for being tested by ALUR and being mentioned before can be very good to control for Buddhist nun's (A Lei replaces Buddhist nun)
The state of an illness of the advanced Non-small cell lung brain metastes of ALK mutation can rise either in first-line treatment or second line treatment
To good effect.
Ai Le is had found in storing process for Buddhist nun's capsule, and with the extension of resting period, capsule is easy moisture absorption, in cause
Tolerant agglomeration, and dissolution rate declines.
Summary of the invention
For the deficiency during storage of existing capsule, a kind of stable Ai Le is provided for Buddhist nun's capsule.
By testing several times, applicants have invented technical solution of the present invention.
The technical scheme is that a kind of Ai Le replaces nylon 6 combination, in every thousand unit doses, contain D90For 36-55
The Ai Le of micron replaces Buddhist nun 150g, Tween 80 4-8g, fumed silica 8-26g, calcium sulfate 2-8g, hydroxypropyl cellulose 18-
32g, Lactis Anhydrous 20-46g, disodium ethylene diamine tetraacetate 4-8g, magnesium stearate 1.0-1.5g.
In technical solution of the present invention, Ai Le replaces Buddhist nun D90It is 36-55 microns, is lower than 36 microns, to the promotion of solubility without bright
Aobvious effect, and will increase the loss of the main ingredient dust in crushing process；Higher than 55 microns, in the technical solution of the present invention, will affect
The dissolution of main ingredient.
The solubility that Ai Le replaces Buddhist nun can be improved as cosolvent in Tween 80.Fumed silica, calcium sulfate, ethylenediamine
The anti-moisture absorption property during storage can be improved in the connection of tetraacethyl disodium and effect.
Preferably, Ai Le of the present invention replaces nylon 6 combination, in every thousand unit doses, contain D90It is 40-48 microns
Ai Le replaces Buddhist nun 150g, Tween 80 5-7g, fumed silica 15-20g, calcium sulfate 4-7g, hydroxypropyl cellulose 22-30g, nothing
Water and milk sugar 28-42g, disodium ethylene diamine tetraacetate 5-6.5g, magnesium stearate 1.0-1.5g.
Preferably, Ai Le of the present invention replaces nylon 6 combination, in every thousand unit doses, contain D90For 45 microns of Ai Le
For Buddhist nun 150g, Tween 80 6g, fumed silica 18g, calcium sulfate 6g, hydroxypropyl cellulose 28g, Lactis Anhydrous 30g, second two
Amine tetraacethyl disodium 6g, magnesium stearate 1.2g.
Ai Le of the present invention replaces the preparation method of nylon 6 combination, comprising the following steps:
Ai Le is crushed to D for Buddhist nun by first step air-flow crushing90It is 36-55 microns；Other auxiliary materials cross 60 meshes；
The Ai Le of second step recipe quantity is uniformly mixed for Buddhist nun with the fumed silica of recipe quantity, and the Tween 80 of recipe quantity is added
It is uniformly mixed；Calcium sulfate, hydroxypropyl cellulose, Lactis Anhydrous, the disodium ethylene diamine tetraacetate that recipe quantity is added are uniformly mixed；
Obtained by third step second step, the magnesium stearate of recipe quantity is added, is uniformly mixed, it is encapsulated.
The utility model has the advantages that in technical solution of the present invention, by the reasonable compatibility of several components, first is that improving the molten of main ingredient
Out, second is that fumed silica, calcium sulfate, the connection of disodium ethylene diamine tetraacetate and effect, improve the anti-suction during storage
Wet performance.Preparation method of the present invention allows Ai Le to be mixed with the fumed silica of recipe quantity for Buddhist nun first, allows gas phase dioxy
SiClx adequately coats Ai Le and replaces Buddhist nun, can be to avoid the moisture absorption of main ingredient.
1. D of embodiment90Buddhist nun 150g, Tween 80 4g, fumed silica 26g, calcium sulfate 2g are replaced for 36 microns of Ai Le,
Hydroxypropyl cellulose 32g, Lactis Anhydrous 20g, disodium ethylene diamine tetraacetate 8g, magnesium stearate 1.0g, by specification technical solution
Described preparation method prepares 1000 capsules.
2. D of embodiment90Buddhist nun 150g, Tween 80 8g, fumed silica 8g, calcium sulfate 8g are replaced for 55 microns of Ai Le,
Hydroxypropyl cellulose 18g, Lactis Anhydrous 46g, disodium ethylene diamine tetraacetate 4g, magnesium stearate 1.5g, by specification technical solution
Described preparation method prepares 1000 capsules.
3. D of embodiment90Buddhist nun 150g, Tween 80 6g, fumed silica 18g, calcium sulfate 6g are replaced for 45 microns of Ai Le,
Hydroxypropyl cellulose 28g, Lactis Anhydrous 30g, disodium ethylene diamine tetraacetate 6g, magnesium stearate 1.2g, by specification technical solution
Described preparation method prepares 1000 capsules.
The prescription of 1. embodiment 3 of reference examples, Ai Le replace the D of Buddhist nun9065 microns are adjusted to, other are the same as embodiment 3.
The prescription of 2. embodiment 3 of reference examples, removes disodium ethylene diamine tetraacetate, specific as follows:
D90Buddhist nun 150g, Tween 80 6g, fumed silica 18g, calcium sulfate 6g, hydroxypropyl cellulose are replaced for 45 microns of Ai Le
28g, Lactis Anhydrous 30g, magnesium stearate 1.2g prepare 1000 capsules by following preparation methods.
Ai Le is crushed to D for Buddhist nun by first step air-flow crushing90It is 45 microns；Other auxiliary materials cross 60 meshes；
The Ai Le of second step recipe quantity is uniformly mixed for Buddhist nun with the fumed silica of recipe quantity, and the Tween 80 of recipe quantity is added
It is uniformly mixed；The calcium sulfate, hydroxypropyl cellulose, Lactis Anhydrous that recipe quantity is added are uniformly mixed；
Obtained by third step second step, the magnesium stearate of recipe quantity is added, is uniformly mixed, it is encapsulated.
The prescription of 3. embodiment 3 of reference examples removes calcium sulfate, meteorological silica, and corresponding quality is by microcrystalline cellulose
Supplement, specific as follows:
D90Buddhist nun 150g, Tween 80 6g, microcrystalline cellulose 24g, hydroxypropyl cellulose 28g, anhydrous lactitol are replaced for 45 microns of Ai Le
Sugared 30g, disodium ethylene diamine tetraacetate 6g, magnesium stearate 1.2g prepare 1000 capsules by following preparation methods.
Ai Le is crushed to D for Buddhist nun by first step air-flow crushing90It is 45 microns；Other auxiliary materials cross 60 meshes；
The Ai Le of second step recipe quantity is uniformly mixed for Buddhist nun with the microcrystalline cellulose of recipe quantity, and the Tween 80 that recipe quantity is added is mixed
It closes uniform；The hydroxypropyl cellulose, Lactis Anhydrous, disodium ethylene diamine tetraacetate that recipe quantity is added are uniformly mixed；
Obtained by third step second step, the magnesium stearate of recipe quantity is added, is uniformly mixed, it is encapsulated.
The prescription of 4. embodiment 3 of reference examples, removes meteorological silica, and corresponding quality is supplemented by microcrystalline cellulose, tool
Body is as follows:
D90Buddhist nun 150g, Tween 80 6g, microcrystalline cellulose 18g, calcium sulfate 6g, hydroxypropyl cellulose are replaced for 45 microns of Ai Le
28g, Lactis Anhydrous 30g, disodium ethylene diamine tetraacetate 6g, magnesium stearate 1.2g, the described preparation of by specification technical solution
Method prepares 1000 capsules.
Ai Le is crushed to D for Buddhist nun by first step air-flow crushing90It is 45 microns；Other auxiliary materials cross 60 meshes；
The Ai Le of second step recipe quantity is uniformly mixed for Buddhist nun with the microcrystalline cellulose of recipe quantity, and the Tween 80 that recipe quantity is added is mixed
It closes uniform；Calcium sulfate, hydroxypropyl cellulose, Lactis Anhydrous, the disodium ethylene diamine tetraacetate that recipe quantity is added are uniformly mixed；
Obtained by third step second step, the magnesium stearate of recipe quantity is added, is uniformly mixed, it is encapsulated.
The prescription of 5. embodiment 3 of reference examples, prepares capsule 1000 as follows.
Ai Le is crushed to D for Buddhist nun by first step air-flow crushing90It is 45 microns；Other auxiliary materials cross 60 meshes；
The Ai Le of second step recipe quantity for the Tween 80 of Buddhist nun and recipe quantity, fumed silica, calcium sulfate, hydroxypropyl cellulose,
Lactis Anhydrous is uniformly mixed；
Obtained by third step second step, the magnesium stearate of recipe quantity is added, is uniformly mixed, it is encapsulated.
Test example 1. takes the product of 1-3 of the embodiment of the present invention and reference examples 1-5 each 100 respectively, aluminum-plastic packaged, is placed in
In climatic chamber, 25 DEG C, relative humidity 75% is stored 6 months and is taken out.0 day, the 6th the end of month are observed respectively, capsule 's content
State, and its dissolution rate is measured, data record is in table 1.
The measurement of dissolution rate is measured according to the capsule dissolution determination method of States Pharmacopoeia specifications.
Table 1
The product of 1 data of table explanation, 1-3 of the embodiment of the present invention has good dissolution rate, after helping to improve patient's medication
Bioavilability improves therapeutic effect.
Meanwhile product of the embodiment of the present invention be during storage it is stable, overcome main ingredient be easy moisture absorption characteristic.
Illustrate that prescription of the present invention and preparation method overcome main ingredient and be easy moisture absorption and the bad characteristic of dissolution rate.
Claims (4)
1. a kind of Ai Le replaces nylon 6 combination, which is characterized in that in every thousand unit doses, contain D90For 36-55 microns of Ai Le
For Buddhist nun 150g, Tween 80 4-8g, fumed silica 8-26g, calcium sulfate 2-8g, hydroxypropyl cellulose 18-32g, Lactis Anhydrous
20-46g, disodium ethylene diamine tetraacetate 4-8g, magnesium stearate 1.0-1.5g.
2. Ai Le replaces nylon 6 combination according to claim 1, which is characterized in that in every thousand unit doses, contain D90For 40-
48 microns of Ai Le replaces Buddhist nun 150g, Tween 80 5-7g, fumed silica 15-20g, calcium sulfate 4-7g, hydroxypropyl cellulose
22-30g, Lactis Anhydrous 28-42g, disodium ethylene diamine tetraacetate 5-6.5g, magnesium stearate 1.0-1.5g.
3. Ai Le replaces nylon 6 combination according to claim 1, which is characterized in that in every thousand unit doses, contain D90It is 45
The Ai Le of micron replaces Buddhist nun 150g, Tween 80 6g, fumed silica 18g, calcium sulfate 6g, hydroxypropyl cellulose 28g, anhydrous lactitol
Sugared 30g, disodium ethylene diamine tetraacetate 6g, magnesium stearate 1.2g.
4. the preparation method that Ai Le described in claim 1 replaces nylon 6 combination, which comprises the following steps:
Ai Le is crushed to D for Buddhist nun by first step air-flow crushing90It is 36-55 microns；Other auxiliary materials cross 60 meshes；
The Ai Le of second step recipe quantity is uniformly mixed for Buddhist nun with the fumed silica of recipe quantity, and the Tween 80 of recipe quantity is added
It is uniformly mixed；Calcium sulfate, hydroxypropyl cellulose, Lactis Anhydrous, the disodium ethylene diamine tetraacetate that recipe quantity is added are uniformly mixed；
Obtained by third step second step, the magnesium stearate of recipe quantity is added, is uniformly mixed, it is encapsulated.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201811357402.1A CN109381440A (en) | 2018-11-15 | 2018-11-15 | A kind of Ai Le replaces nylon 6 combination |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201811357402.1A CN109381440A (en) | 2018-11-15 | 2018-11-15 | A kind of Ai Le replaces nylon 6 combination |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN109381440A true CN109381440A (en) | 2019-02-26 |
Family
ID=65428732
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201811357402.1A Withdrawn CN109381440A (en) | 2018-11-15 | 2018-11-15 | A kind of Ai Le replaces nylon 6 combination |
Country Status (1)
| Country | Link |
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| CN (1) | CN109381440A (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2021134647A1 (en) * | 2019-12-31 | 2021-07-08 | 广州帝奇医药技术有限公司 | Sustained release composition and preparation method therefor |
Citations (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2015181739A1 (en) * | 2014-05-29 | 2015-12-03 | Novartis Ag | Ceritinib formulation |
| CN107802608A (en) * | 2017-12-20 | 2018-03-16 | 威海贯标信息科技有限公司 | A kind of atomoxetine tablet composition |
| CN107811983A (en) * | 2017-12-04 | 2018-03-20 | 威海贯标信息科技有限公司 | A kind of tofogliflozin composition |
| CN107890462A (en) * | 2017-11-30 | 2018-04-10 | 威海贯标信息科技有限公司 | A kind of pazopanib tablet composition |
| CN107929250A (en) * | 2017-12-15 | 2018-04-20 | 威海贯标信息科技有限公司 | A kind of revaprzan tablet composition |
| CN107951848A (en) * | 2017-12-12 | 2018-04-24 | 威海贯标信息科技有限公司 | A kind of Afatinib tablet composition |
-
2018
- 2018-11-15 CN CN201811357402.1A patent/CN109381440A/en not_active Withdrawn
Patent Citations (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2015181739A1 (en) * | 2014-05-29 | 2015-12-03 | Novartis Ag | Ceritinib formulation |
| CN107890462A (en) * | 2017-11-30 | 2018-04-10 | 威海贯标信息科技有限公司 | A kind of pazopanib tablet composition |
| CN107811983A (en) * | 2017-12-04 | 2018-03-20 | 威海贯标信息科技有限公司 | A kind of tofogliflozin composition |
| CN107951848A (en) * | 2017-12-12 | 2018-04-24 | 威海贯标信息科技有限公司 | A kind of Afatinib tablet composition |
| CN107929250A (en) * | 2017-12-15 | 2018-04-20 | 威海贯标信息科技有限公司 | A kind of revaprzan tablet composition |
| CN107802608A (en) * | 2017-12-20 | 2018-03-16 | 威海贯标信息科技有限公司 | A kind of atomoxetine tablet composition |
Non-Patent Citations (2)
| Title |
|---|
| ERIN LARKINS,ET AL.,: "FDA Approval: Alectinib for the Treatment of Metastatic, ALK-Positive Non–Small Cell Lung Cancer Following Crizotinib", 《CLIN CANCER RES》 * |
| FOOD AND DRUG ADMINISTRATION: "Chemistry review(s)", 《HTTP://WWW.ACCESSDATA.FDA.GOV/DRUGSATFDA_DOCS/NDA/2015/208434ORIG1S000CHEMR.PDF.》 * |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2021134647A1 (en) * | 2019-12-31 | 2021-07-08 | 广州帝奇医药技术有限公司 | Sustained release composition and preparation method therefor |
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Application publication date: 20190226 |