CN102526000B - Dexibuprofen slow-release capsule and production method thereof - Google Patents
Dexibuprofen slow-release capsule and production method thereof Download PDFInfo
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- CN102526000B CN102526000B CN 201210023257 CN201210023257A CN102526000B CN 102526000 B CN102526000 B CN 102526000B CN 201210023257 CN201210023257 CN 201210023257 CN 201210023257 A CN201210023257 A CN 201210023257A CN 102526000 B CN102526000 B CN 102526000B
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- 239000002775 capsule Substances 0.000 title claims abstract description 96
- HEFNNWSXXWATRW-JTQLQIEISA-N dexibuprofen Chemical compound CC(C)CC1=CC=C([C@H](C)C(O)=O)C=C1 HEFNNWSXXWATRW-JTQLQIEISA-N 0.000 title claims abstract description 93
- 229960003428 dexibuprofen Drugs 0.000 title claims abstract description 55
- 238000004519 manufacturing process Methods 0.000 title claims abstract description 14
- 238000000576 coating method Methods 0.000 claims abstract description 180
- 239000011248 coating agent Substances 0.000 claims abstract description 67
- 239000000203 mixture Substances 0.000 claims abstract description 56
- 239000000463 material Substances 0.000 claims abstract description 19
- 239000008188 pellet Substances 0.000 claims abstract description 19
- 235000021355 Stearic acid Nutrition 0.000 claims abstract description 18
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical group CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 claims abstract description 18
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 claims abstract description 18
- 239000008117 stearic acid Substances 0.000 claims abstract description 18
- 238000013268 sustained release Methods 0.000 claims description 48
- 239000012730 sustained-release form Substances 0.000 claims description 48
- 239000000243 solution Substances 0.000 claims description 39
- 238000007789 sealing Methods 0.000 claims description 33
- 239000012530 fluid Substances 0.000 claims description 18
- WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 claims description 16
- 229920003081 Povidone K 30 Polymers 0.000 claims description 16
- 238000001035 drying Methods 0.000 claims description 9
- 239000002245 particle Substances 0.000 claims description 9
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 9
- 238000005507 spraying Methods 0.000 claims description 9
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 6
- 239000007921 spray Substances 0.000 claims description 5
- 230000001476 alcoholic effect Effects 0.000 claims description 4
- 238000000034 method Methods 0.000 claims description 3
- 239000011259 mixed solution Substances 0.000 claims description 3
- 239000008280 blood Substances 0.000 abstract description 7
- 210000004369 blood Anatomy 0.000 abstract description 7
- 239000003814 drug Substances 0.000 abstract description 7
- 238000010521 absorption reaction Methods 0.000 abstract description 4
- 230000000694 effects Effects 0.000 abstract description 4
- 239000011247 coating layer Substances 0.000 abstract 9
- 239000010410 layer Substances 0.000 abstract 5
- 238000002955 isolation Methods 0.000 abstract 3
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 abstract 1
- 229920000036 polyvinylpyrrolidone Polymers 0.000 abstract 1
- 239000011162 core material Substances 0.000 description 42
- 229920002472 Starch Polymers 0.000 description 9
- 235000019698 starch Nutrition 0.000 description 9
- 239000008107 starch Substances 0.000 description 9
- CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 description 8
- 229930006000 Sucrose Natural products 0.000 description 8
- 229960004793 sucrose Drugs 0.000 description 8
- 239000005720 sucrose Substances 0.000 description 7
- HEFNNWSXXWATRW-UHFFFAOYSA-N Ibuprofen Chemical compound CC(C)CC1=CC=C(C(C)C(O)=O)C=C1 HEFNNWSXXWATRW-UHFFFAOYSA-N 0.000 description 6
- 230000003203 everyday effect Effects 0.000 description 4
- 229960001680 ibuprofen Drugs 0.000 description 3
- 239000000041 non-steroidal anti-inflammatory agent Substances 0.000 description 3
- 229940021182 non-steroidal anti-inflammatory drug Drugs 0.000 description 3
- 238000002360 preparation method Methods 0.000 description 3
- 102000004005 Prostaglandin-endoperoxide synthases Human genes 0.000 description 2
- 108090000459 Prostaglandin-endoperoxide synthases Proteins 0.000 description 2
- 239000002552 dosage form Substances 0.000 description 2
- 238000011160 research Methods 0.000 description 2
- 238000012360 testing method Methods 0.000 description 2
- 208000005171 Dysmenorrhea Diseases 0.000 description 1
- 206010013935 Dysmenorrhoea Diseases 0.000 description 1
- 206010019233 Headaches Diseases 0.000 description 1
- 208000002193 Pain Diseases 0.000 description 1
- 238000013459 approach Methods 0.000 description 1
- 244000144987 brood Species 0.000 description 1
- 230000000052 comparative effect Effects 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 238000005516 engineering process Methods 0.000 description 1
- 238000009472 formulation Methods 0.000 description 1
- 210000001035 gastrointestinal tract Anatomy 0.000 description 1
- 231100000869 headache Toxicity 0.000 description 1
- 238000001727 in vivo Methods 0.000 description 1
- 239000003112 inhibitor Substances 0.000 description 1
- 230000010534 mechanism of action Effects 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
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- 210000003205 muscle Anatomy 0.000 description 1
- 239000000820 nonprescription drug Substances 0.000 description 1
- 230000003285 pharmacodynamic effect Effects 0.000 description 1
- 230000000144 pharmacologic effect Effects 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 239000000829 suppository Substances 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
- 239000003826 tablet Substances 0.000 description 1
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- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
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Abstract
The invention discloses a dexibuprofen slow-release capsule. Pellets are filled in the capsule, each pellet consists of a pellet core and four layers of materials wrapped outside the pellet core, the four layers of materials are sequentially an inner isolation layer, a first coating layer, a second coating layer and a third coating layer from inside to outside, and the pellet core, the inner isolation layer, the first coating layer, the second coating layer and the third coating layer respectively have the following compositions: the pellet core is prepared by medicine auxiliary materials, the inner isolation layer is stearic acid, the first coating layer is a coating mixture, the second coating layer comprises the coating mixture and the stearic acid, the third coating layer is the coating mixture, and the coating mixture consists of dexibuprofen and polyvidone K30. The invention also provides a production method of the dexibuprofen slow-release capsule. Compared with an ordinary capsule, the dexibuprofen slow-release capsule disclosed by the invention has the same absorption degree, but the dexibuprofen blood maximum concentration (Cmax) of the dexibuprofen slow-release capsule disclosed by the invention in human bodies is lower, the maximum time (Tmax) from the administration to the blood Cmax reaching is longer, and a good slow release effect is realized.
Description
Technical field
The present invention relates to a kind of Dexibuprofen sustained-release capsule and production method thereof.
Background technology
(S)-ibuprofen is the S (+)-isomer of ibuprofen, and activity was 160 times of levo form in Austria's listing in 1994,1.6 times of racemic modification.Ibuprofen is comprised of d-isomer and the levo form of equivalent, clinical practice has 30 years history, be one of the most general NSAIDs class medicine of clinical use, be considered to safest nonsteroidal antiinflammatory drug (NSAIDs), 1984 is the OTC medicine by drugs approved by FDA.Clinical data shows that (S)-ibuprofen is faster than racemic ibuprofen onset, the mechanism of action is consistent, but pharmacological action is better, is a kind of non-selective cyclooxygenase (COX) inhibitor, be widely used in the treatment atrophic diseases, and the multiple pain such as articular muscle is felt sorry, headache, dysmenorrhea.
Owing to using (S)-ibuprofen to overcome ibuprofen some shortcomings aspect use pharmacodynamics and pharmacokinetics, the external existing trend that substitutes racemic ibuprofen with (S)-ibuprofen.Clinical research show the dosage of (S)-ibuprofen be racemic ibuprofen 75% the time can reach identical or better clinical efficacy.
At present, the dosage form of (S)-ibuprofen has tablet, suppository, capsule and four kinds of dosage forms of oral suspensions, has not yet to see the research of slow release formulation.Because the half-life of (S)-ibuprofen is about 2 hours, absorbs rapidly through gastrointestinal tract, accretion rate is fast, and the half-life is shorter, whenever takes medicine day by day 3～4 times.Medicining times is many, has not only increased the weight of patient's burden, and the concentration change of (S)-ibuprofen is large in the patient blood, and side effect is also large.
Summary of the invention
Problem to be solved by this invention provides and a kind ofly can reduce medicining times, reduces Dexibuprofen sustained-release capsule and the production method thereof of (S)-ibuprofen blood medicine peak value.
The technical scheme of Dexibuprofen sustained-release capsule of the present invention is: a kind of Dexibuprofen sustained-release capsule, be filled with micropill in the capsule, micropill is made of ball core four layer materials outer with being wrapped in the ball core, four layer materials are followed successively by from inside to outside: separately composed as follows of interior sealing coat, coatings I, coatings II and coatings III, ball core, interior sealing coat, coatings I, coatings II and coatings III: the ball core is pharmaceutic adjuvant; Interior sealing coat is stearic acid; Coatings I is the coating mixture; Coatings II contains coating mixture and stearic acid; Coatings III is the coating mixture; Described coating mixture is comprised of (S)-ibuprofen and PVP K30.
The fine pellet core of Dexibuprofen sustained-release capsule of the present invention is slow releasing capsule a kind of pharmaceutic adjuvant commonly used, and the spheroidal particle that can be made by sucrose and starch as the core material of this preparation, plays carrier function.Cane sugar content is 62.5% ~ 91.5% in the fine pellet core, and all the other are starch.
Dexibuprofen sustained-release capsule of the present invention is suitable with the conventional capsule degree of absorption, still, and Dexibuprofen sustained-release capsule of the present invention (S)-ibuprofen blood medicine peak value (C in vivo
Max) lower, from taking the time (T that reaches blood medicine peak value
Max) longer.
Slow releasing capsule of the present invention and general capsule are carried out clinical bioavailability and bioequivalence relatively, more easily find out the slow release effect of capsule of the present invention, relatively capsule of the present invention is called and is subjected to test preparation, will be called for capsule as a comparison the reference capsule; Comparative approach comprises single-dose relatively and multiple dosing compares.The reference capsule is commercially available conventional capsule, and its composition is (S)-ibuprofen, starch and sugar.
Single-dose compares: behind single-dose 450 mg, and the AUC of tested capsule and reference capsule
0-24Be respectively 87.32ug.h/ml and 76.56 ug.h/ml; AUC
0-∞Be respectively 88.36ug.h/ml and 77.74 ug.h/ml; C
MaxBe respectively 13.93 ug/ml and 19.53 ug/ml; T
MaxBe respectively 3.95h and 1.80h; t
1/2Be respectively 2.75 ± 0.80 h and 2.73 ± 0.92 h.Judge according to the above results, the degree of absorption of tested capsule is higher than the reference capsule, and tested capsule C
MaxObviously reduce T
MaxObviously prolong, thus can judge two preparation bioequivalences, and tested capsule has the slow release dynamic characteristic.
Multiple dosing compares: continuous several times oral test capsule, each 225mg, every day 2 times, totally 7 days; The (S)-ibuprofen capsule, each 150mg, every day 3 times, totally 7 days.Obtain the parameter A UC that tested capsule and reference capsule reach limit
SsBe respectively 74.73ug.h/ml and 75.46 ug.h/ml; AUC
0-∞Be respectively 79.01ug.h/ml and 81.57ug.h/ml; C
MaxBe respectively 6.62ug/ml and 6.78ug/ml; T
MaxBe respectively 4.50 and 2.39h; C
MinBe respectively 1.03ug/ml and 1.12ug/ml; C
SsBe respectively 3.11ug/ml and 3.14ug/ml; DF is respectively 1.83 and 1.81.Judge according to the above results, tested capsule and reference capsule are suitable at the degree of absorption that the continuous several times administration reaches under the limit, and the blood concentration fluctuation degree that tested capsule administration every day 2 times and administration every day of reference capsule are 3 times is comparatively approaching, the T of tested capsule
MaxObviously prolong, thus can judge two brood lac Tibetan household slave's thing equivalences, and tested capsule has the slow release dynamic characteristic.
The weight ratio of coating mixture is (80 ~ 88) among the coatings I of Dexibuprofen sustained-release capsule of the present invention, coatings II and the coatings III: (3 ~ 8): 10.
Coating solution and stearic weight ratio are (1.8 ~ 2.2) among the coatings II of Dexibuprofen sustained-release capsule of the present invention: 1.
The weight ratio of (S)-ibuprofen and PVP K30 is (25 ~ 35) in the coating mixture of Dexibuprofen sustained-release capsule of the present invention: (1).
The weight of (S)-ibuprofen is 209.25 ~ 240.75mg in every Dexibuprofen sustained-release capsule of the present invention.
The particle diameter of the fine pellet core of Dexibuprofen sustained-release capsule of the present invention is 600 ~ 710um.
The present invention also provides a kind of production method of above-mentioned Dexibuprofen sustained-release capsule, and the method comprises the steps:
(1) fine pellet core is added in the fluid bed, start fluid bed, spray sealing coat solution in fluid bed, then dry, the ball core that gained is surrounded by interior sealing coat is called micropill I, and above-mentioned interior sealing coat solution is ethanol and stearic mixed solution;
(2) in the fluid bed that contains micropill I, spray coating solution, must be surrounded by the micropill of coatings I, after drying, cross 16 orders and 24 mesh sieves, collect 16 orders to the micropill between 24 orders, be called micropill II;
(3) spray coating solution and stearic mixture in the fluid bed that contains micropill II, gained is surrounded by the micropill of coatings II, after drying, crosses 14 orders and 24 mesh sieves, collects 14 orders to the micropill between 24 orders, is called micropill III;
(4) in the fluid bed that contains micropill III, spray coating solution, after the coating solution drying, must be surrounded by the micropill of coatings III, be called micropill IV;
(5) gained micropill IV in the step (4) is added Capsules, namely get the Dexibuprofen sustained-release capsule; Above-mentioned coating solution is the alcoholic solution that contains (S)-ibuprofen and PVP K30.
Alcoholic solution in the coating solution can volatilize in dry run, and the remaining solid that contains (S)-ibuprofen and PVP K30 is the coating mixture.
In the production method of above-mentioned Dexibuprofen sustained-release capsule, the composition of each composition and proportioning can be with reference to the Dexibuprofen sustained-release capsules of this aforementioned invention, that is:
The weight ratio of the coating solution that sprays in step (2), (3) and (4) is (80 ~ 88): (3 ~ 8): 10.
Coating solution and stearic weight ratio are (1.8 ~ 2.2) in the step (3): 1.
In the production method of Dexibuprofen sustained-release capsule of the present invention, the weight ratio of (S)-ibuprofen and PVP K30 is (25 ~ 35) in the coating solution: (1).
The weight of (S)-ibuprofen is 209.25 ~ 240.75mg/ capsules in the Dexibuprofen sustained-release capsule that the production method of the Dexibuprofen sustained-release capsule of invention obtains.
The specific embodiment
Embodiment 1:
The Dexibuprofen sustained-release capsule, be filled with micropill in the capsule, micropill is made of ball core four layer materials outer with being wrapped in the ball core, four layer materials are followed successively by from inside to outside: separately composed as follows of interior sealing coat, coatings I, coatings II and coatings III, ball core, interior sealing coat, coatings I, coatings II and coatings III: the ball core is the pharmaceutic adjuvant that is comprised of sucrose and starch; Interior sealing coat is stearic acid; Coatings I is the coating mixture; Coatings II contains coating mixture and stearic acid; Coatings III is the coating mixture; Described coating mixture is that (S)-ibuprofen and the PVP K30 of 25:1 forms by weight ratio, the weight ratio of coating mixture is 85:3:10 among above-mentioned coatings I, coatings II and the coatings III, coating solution and stearic weight ratio are 2:1 among the coatings II, the weight of (S)-ibuprofen is 208mg in every above-mentioned Dexibuprofen sustained-release capsule, and the particle diameter of the fine pellet core of above-mentioned Dexibuprofen sustained-release capsule is 600um.
Embodiment 2:
The Dexibuprofen sustained-release capsule, be filled with micropill in the capsule, micropill is made of ball core four layer materials outer with being wrapped in the ball core, four layer materials are followed successively by from inside to outside: separately composed as follows of interior sealing coat, coatings I, coatings II and coatings III, ball core, interior sealing coat, coatings I, coatings II and coatings III: the ball core is the pharmaceutic adjuvant that is comprised of sucrose and starch; Interior sealing coat is stearic acid; Coatings I is the coating mixture; Coatings II contains coating mixture and stearic acid; Coatings III is the coating mixture; Described coating mixture is that (S)-ibuprofen and the PVP K30 of 30:1 forms by weight ratio, the weight ratio of coating mixture is 80:4:10 among above-mentioned coatings I, coatings II and the coatings III, coating solution and stearic weight ratio are 1.8:1 among the coatings II, the weight of (S)-ibuprofen is 220mg in every above-mentioned Dexibuprofen sustained-release capsule, and the particle diameter of the fine pellet core of above-mentioned Dexibuprofen sustained-release capsule is 680um.
Embodiment 3:
The Dexibuprofen sustained-release capsule, be filled with micropill in the capsule, micropill is made of ball core four layer materials outer with being wrapped in the ball core, four layer materials are followed successively by from inside to outside: separately composed as follows of interior sealing coat, coatings I, coatings II and coatings III, ball core, interior sealing coat, coatings I, coatings II and coatings III: the ball core is the pharmaceutic adjuvant that is comprised of sucrose and starch; Interior sealing coat is stearic acid; Coatings I is the coating mixture; Coatings II contains coating mixture and stearic acid; Coatings III is the coating mixture; Described coating mixture is that (S)-ibuprofen and the PVP K30 of 35:1 forms by weight ratio, the weight ratio of coating mixture is 88:6:10 among above-mentioned coatings I, coatings II and the coatings III, coating solution and stearic weight ratio are 2.2:1 among the coatings II, the weight of (S)-ibuprofen is 241mg in every above-mentioned Dexibuprofen sustained-release capsule, and the particle diameter of the fine pellet core of above-mentioned Dexibuprofen sustained-release capsule is 650um.
Embodiment 4:
The Dexibuprofen sustained-release capsule, be filled with micropill in the capsule, micropill is made of ball core four layer materials outer with being wrapped in the ball core, four layer materials are followed successively by from inside to outside: separately composed as follows of interior sealing coat, coatings I, coatings II and coatings III, ball core, interior sealing coat, coatings I, coatings II and coatings III: the ball core is the pharmaceutic adjuvant that is comprised of sucrose and starch; Interior sealing coat is stearic acid; Coatings I is the coating mixture; Coatings II contains coating mixture and stearic acid; Coatings III is the coating mixture; Described coating mixture is that (S)-ibuprofen and the PVP K30 of 33:1 forms by weight ratio, the weight ratio of coating mixture is 85:6:10 among above-mentioned coatings I, coatings II and the coatings III, coating solution and stearic weight ratio are 2.1:1 among the coatings II, the weight of (S)-ibuprofen is 230mg in every above-mentioned Dexibuprofen sustained-release capsule, and the particle diameter of the fine pellet core of above-mentioned Dexibuprofen sustained-release capsule is 700um.
Embodiment 5:
The Dexibuprofen sustained-release capsule, be filled with micropill in the capsule, micropill is made of ball core four layer materials outer with being wrapped in the ball core, four layer materials are followed successively by from inside to outside: separately composed as follows of interior sealing coat, coatings I, coatings II and coatings III, ball core, interior sealing coat, coatings I, coatings II and coatings III: the ball core is the pharmaceutic adjuvant that is comprised of sucrose and starch; Interior sealing coat is stearic acid; Coatings I is the coating mixture; Coatings II contains coating mixture and stearic acid; Coatings III is the coating mixture; Described coating mixture is that (S)-ibuprofen and the PVP K30 of 31:1 forms by weight ratio, the weight ratio of coating mixture is 82:8:10 among above-mentioned coatings I, coatings II and the coatings III, coating solution and stearic weight ratio are 1.9:1 among the coatings II, the weight of (S)-ibuprofen is 208mg in every above-mentioned Dexibuprofen sustained-release capsule, and the particle diameter of the fine pellet core of above-mentioned Dexibuprofen sustained-release capsule is 710um.
Embodiment 6:
The Dexibuprofen sustained-release capsule, be filled with micropill in the capsule, micropill is made of ball core four layer materials outer with being wrapped in the ball core, four layer materials are followed successively by from inside to outside: separately composed as follows of interior sealing coat, coatings I, coatings II and coatings III, ball core, interior sealing coat, coatings I, coatings II and coatings III: the ball core is the pharmaceutic adjuvant that is comprised of sucrose and starch; Interior sealing coat is stearic acid; Coatings I is the coating mixture; Coatings II contains coating mixture and stearic acid; Coatings III is the coating mixture; Described coating mixture is that (S)-ibuprofen and the PVP K30 of 27:1 forms by weight ratio, the weight ratio of coating mixture is 82:3:10 among above-mentioned coatings I, coatings II and the coatings III, coating solution and stearic weight ratio are 2:1 among the coatings II, the weight of (S)-ibuprofen is 228mg in every above-mentioned Dexibuprofen sustained-release capsule, and the particle diameter of the fine pellet core of above-mentioned Dexibuprofen sustained-release capsule is 670um.
Embodiment 7:
A kind of production method of Dexibuprofen sustained-release capsule, the method comprises the steps:
(1) fine pellet core is added in the fluid bed, start fluid bed, spray sealing coat solution in fluid bed, then dry, the ball core that gained is surrounded by interior sealing coat is called micropill I, and above-mentioned interior sealing coat solution is ethanol and stearic mixed solution;
(2) in the fluid bed that contains micropill I, spray coating solution, must be surrounded by the micropill of coatings I, after drying, cross 16 orders and 24 mesh sieves, collect 16 orders to the micropill between 24 orders, be called micropill II;
(3) spray coating solution and stearic mixture in the fluid bed that contains micropill II, gained is surrounded by the micropill of coatings II, after drying, crosses 14 orders and 24 mesh sieves, collects 14 orders to the micropill between 24 orders, is called micropill III;
(4) in the fluid bed that contains micropill III, spray coating solution, after the coating solution drying, must be surrounded by the micropill of coatings III, be called micropill IV;
(5) gained micropill IV in the step (4) is added Capsules, namely get the Dexibuprofen sustained-release capsule; Above-mentioned coating solution is the alcoholic solution that contains (S)-ibuprofen and PVP K30.
The weight ratio of the coating solution that sprays in step (2), (3) and (4) is (80 ~ 88): (3 ~ 8): 10.
Coating solution and stearic weight ratio are (1.8 ~ 2.2) in the step (3): 1.
In the production method of Dexibuprofen sustained-release capsule of the present invention, the weight ratio of (S)-ibuprofen and PVP K30 is (25 ~ 35) in the coating solution: (1).
The weight of (S)-ibuprofen is 209.25 ~ 240.75mg/ capsules in the Dexibuprofen sustained-release capsule that the production method of the Dexibuprofen sustained-release capsule of invention obtains.
Claims (4)
1. Dexibuprofen sustained-release capsule, be filled with micropill in the capsule, micropill is made of ball core four layer materials outer with being wrapped in the ball core, four layer materials are followed successively by from inside to outside: separately composed as follows of interior sealing coat, coatings I, coatings II and coatings III, ball core, interior sealing coat, coatings I, coatings II and coatings III: the ball core is pharmaceutic adjuvant; Interior sealing coat is stearic acid; Coatings I is the coating mixture; Coatings II contains coating mixture and stearic acid; Coatings III is the coating mixture; Described coating mixture is comprised of (S)-ibuprofen and PVP K30; Among described coatings I, coatings II and the coatings III, the weight ratio of coating mixture is (80 ~ 88): (3 ~ 8): 10; Coating mixture and stearic weight ratio are (1.8 ~ 2.2) among the described coatings II: 1; The weight ratio of (S)-ibuprofen and PVP K30 is (25 ~ 35) in the described total coated mixture: 1.
2. according to Dexibuprofen sustained-release capsule claimed in claim 1, it is characterized in that: the weight of (S)-ibuprofen is 208 ~ 241mg in every capsules.
3. according to the production method of Dexibuprofen sustained-release capsule claimed in claim 1, it is characterized in that: the particle diameter of described fine pellet core is 600 ~ 710um.
4. according to the production method of any one described Dexibuprofen sustained-release capsule in the claims 1 to 3, the method comprises the steps:
(1) fine pellet core is added in the fluid bed, start fluid bed, spray sealing coat solution in fluid bed, then dry, the ball core that gained is surrounded by interior sealing coat is called micropill I, and above-mentioned interior sealing coat solution is ethanol and stearic mixed solution;
(2) spray coating solution in the fluid bed that contains micropill I, gained is surrounded by the micropill of coatings I, after drying, crosses 16 orders and 24 mesh sieves, collects 16 orders to the micropill between 24 orders, is called micropill II;
(3) spray coating solution and stearic mixture in the fluid bed that contains micropill II, gained is surrounded by the micropill of coatings II, after drying, crosses 14 orders and 24 mesh sieves, collects 14 orders to the micropill between 24 orders, is called micropill III;
(4) in the fluid bed that contains micropill III, spray coating solution, after the coating solution drying, must be surrounded by the micropill of coatings III, be called micropill IV;
(5) gained micropill IV in the step (4) is added Capsules, namely get the Dexibuprofen sustained-release capsule; Above-mentioned the coating solution described in steps is the alcoholic solution that contains (S)-ibuprofen and PVP K30.
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| CN104546801B (en) * | 2015-02-03 | 2017-07-18 | 常州市第四制药厂有限公司 | A kind of spansule and its preparation technology containing brufen raceme or d-isomer |
| CN110314152B (en) * | 2018-11-27 | 2021-03-26 | 西安圣雪沙药物开发有限公司 | Ibuprofen sustained-release pellet capsule and preparation method thereof |
| CN109966268A (en) * | 2019-04-04 | 2019-07-05 | 吉林市吴太感康药业有限公司 | A kind of preparation method of ibuprofen sustained release capsules |
| CN110327309B (en) * | 2019-07-17 | 2023-02-10 | 珠海润都制药股份有限公司 | Ibuprofen sustained-release pellet without pill sticking |
| CN110755396B (en) * | 2019-12-06 | 2022-04-08 | 北京悦康科创医药科技股份有限公司 | Ibuprofen sustained-release pellet and preparation method thereof |
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| CN101467989A (en) * | 2007-12-27 | 2009-07-01 | 北京德众万全医药科技有限公司 | Sustained-release pellet containing ibuprofen |
| CN101269041A (en) * | 2008-05-16 | 2008-09-24 | 北京正大绿洲医药科技有限公司 | Dexibuprofen sustained-release dropping pill and preparation method thereof |
-
2012
- 2012-02-02 CN CN 201210023257 patent/CN102526000B/en not_active Expired - Fee Related
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| Publication number | Publication date |
|---|---|
| CN102526000A (en) | 2012-07-04 |
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