CN103536575B - Acetylcysteine composition capsule - Google Patents
Acetylcysteine composition capsule Download PDFInfo
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- CN103536575B CN103536575B CN201310479888.7A CN201310479888A CN103536575B CN 103536575 B CN103536575 B CN 103536575B CN 201310479888 A CN201310479888 A CN 201310479888A CN 103536575 B CN103536575 B CN 103536575B
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Abstract
The invention discloses an acetylcysteine composition capsule, and belongs to the field of medicine and medicine preparation technology. The acetylcysteine composition capsule comprises following ingredients: 10 to 30mg of acetylcysteine, 85 to 105mg of chitosan nanoparticle, 95 to 119mg of microcrystalline cellulose, 9 to 12mg of cross linked sodium carboxymethyl cellulose, 4.7 to 5.7mg of polyvinylpyrrolidone and 3.5 to 4.5mg of magnesium stearate. Beneficial effects of the acetylcysteine composition capsule are that: chitosan nanoparticle is a particle with a particle size less than 100nm, and is capable of promoting dissolving out of acetylcysteine effectively, and increasing bioavailability. Spray-dry granulation technology at 20 to 25 DEG C is employed, so that granulation efficiency is increased, destruction of acetylcysteine caused by high temperature is avoided, and medicine stability is increased. In addition, an internally added disintegrating agent and an externally added disintegrated agent are combined, so that disintegration speed of the acetylcysteine composition capsule is further increased, dissolving out lag and disintegrating lag of common capsules are avoided, and the acetylcysteine composition capsule is more suitable for industrialized large-scaled production compared with capsules prepared by prior art.
Description
Technical field:
The present invention relates to medicine and medicine manufacture technology field, particularly relate to a kind of Acetylcysteine composition capsule.
Background technology:
Acetylcysteine (N-acetylcysteine; NAC) molecular formula is C5H9NO3S, is the acetyl compound of Cys, and it contains active-SH base; for clinical conventional expectorant, be also usually used in the liver toxicity reaction that rescue acetaminophen causes.In recent years many bibliographical information NAC are as a kind of sulfydryl donor, or a kind of antioxidant, there is interference free radical generate, remove the free radical generated, regulate the effect such as metabolic activity of cell, be all widely used in the Clinical and experimental study of breathing, cardiovascular, nervous system and AIDS.The curative of the Acute Fulminant's liver failure (Acute Liver Failure) that it can be used as drug intoxication to cause abroad.Acetylcysteine is expectorant, and because it has active-SH base, stability is very poor, to damp and hot more responsive.
Summary of the invention:
An object of the present invention is to provide a kind of acetylcysteine composition, said composition principal agent is acetylcysteine.
Technical problem to be solved by this invention realizes by the following technical solutions.
The invention provides acetylcysteine composition, the prescription of said composition is by acetylcysteine, chitosan nano, microcrystalline Cellulose, cross-linking sodium carboxymethyl cellulose, polyvidone, magnesium stearate.It is characterized in that: chitosan nano can as diluent, disintegrating agent, binding agent.
Described principal agent and the adjuvant ratio shared by by weight in prescription total amount is:
The invention provides a kind of preparation method of Acetylcysteine composition capsule, comprise the preparation of chitosan nano and the preparation of composition capsule:
The preparation of chitosan nano,
1, sieve through 100 eye mesh screens after Chitosan powder being pulverized;
2, take the Chitosan powder of 100g at room temperature (20 DEG C) add 0.1mol/l acetic acid solution 40L, magnetic agitation, chitosan is dissolved completely, obtains chitosan acetic acid solution (C=2.5g/L);
3, pH=5.0 is regulated with 1%NaOH;
4, add 1% sodium tripolyphosphate 1667g in chitosan acetic acid solution under stirring, make chitosan/sodium tripolyphosphate mass ratio be 6:1, be cross-linked into nanoparticle by the electrostatic interaction of zwitterion;
5, by above-mentioned colloid solution 4 DEG C of high speed centrifugation (18000r/min) 30min, lower sediment is collected, after pure water 3 times, cooling final vacuum drying (less than 30 DEG C) obtains chitosan nano, moisture is lower than 2%, and particle diameter≤100nm, zeta current potential is about 15mv;
The preparation of described composition capsule,
A, by the polyvidone of recipe quantity with 18% alcoholic solution be mixed with 10% PVP solution, then add the acetylcysteine of recipe quantity, make it be uniformly dispersed, obtained pastille binding agent;
B, the chitosan nano of recipe quantity, microcrystalline Cellulose, cross-linking sodium carboxymethyl cellulose are crossed 80 ~ 100 mesh sieves respectively, after mix homogeneously, obtained blank mixed accessories;
C, the pastille binding agent of step a gained to be mixed and dry granulating by the high-pressure sprayer of spray dryer and the blank mixed accessories of step b gained;
D, the granule of step c gained is crossed 18 mesh sieve granulate;
E, steps d gained granule is added magnesium stearate mix homogeneously, encapsulated.
Baking temperature described in step c is 20 ~ 30 DEG C, and pellet moisture is lower than 1.5%, and drying time is 5 ~ 6 minutes.
Described diluent is chitosan nano and microcrystalline Cellulose, and its Main Function is the volume increasing capsule, is beneficial to be shaped, also can promotes the disintegrate of capsule, improve stripping.
Described disintegrating agent is chitosan nano and cross-linking sodium carboxymethyl cellulose, and its Main Function makes quick from capsule, the abundant stripping of active constituents of medicine.
Described binding agent is polyvidone, and its Main Function makes grain forming, improves material fluidity.
Described lubricant is magnesium stearate, and its Main Function makes particle lubrication, increases mobility of particle, improves capsule dress sample compliance.
Beneficial effect of the present invention is:
Chitosan nano is the microgranule that a kind of particle diameter is less than 100nm, effectively can promote the stripping of acetylcysteine, improve bioavailability.Adopt 20-25 DEG C of spray-drying process, improve granulation efficiency, avoid the destruction of high temperature to acetylcysteine, improve the stability of medicine, combined with disintegrating agent and additional disintegrating agent by interior, further increase the disintegration rate of capsule, overcome general capsule stripping and the delayed shortcoming of disintegrate, comparatively prior art is more suitable for industrialized great production.
Detailed description of the invention:
The technological means realized to make the present invention, creation characteristic, reaching object and effect is easy to understand, below in conjunction with specific embodiment, setting forth the present invention further.
Following examples are for illustration of the present invention, but these embodiments do not limit the scope of the invention.
The preparation of embodiment one, Acetylcysteine composition capsule, in 1000
1. prescription:
2. preparation technology
1) by the polyvidone of recipe quantity with 18% alcoholic solution be mixed with 10% PVP solution, then add the acetylcysteine of recipe quantity, make it be uniformly dispersed, obtained pastille binding agent;
2) chitosan nano of recipe quantity, microcrystalline Cellulose, cross-linking sodium carboxymethyl cellulose are crossed 80 ~ 100 mesh sieves respectively, after mix homogeneously, obtained blank mixed accessories;
3) the pastille binding agent of step 1 gained is mixed and dry granulating by the high-pressure sprayer of spray dryer and the blank mixed accessories of step 2 gained;
4) granule of step 3 gained is crossed 18 mesh sieve granulate;
5) step 4 gained granule is added magnesium stearate mix homogeneously, encapsulated.
Wherein, the baking temperature described in step 3 is 25 DEG C, and pellet moisture is lower than 1.5%, and drying time is 5 minutes.
The preparation of embodiment two, Acetylcysteine composition capsule, in 1000
1. prescription:
2. preparation technology
1) by the polyvidone of recipe quantity with 18% alcoholic solution be mixed with 10% PVP solution, then add the acetylcysteine of recipe quantity, make it be uniformly dispersed, obtained pastille binding agent;
2) chitosan nano of recipe quantity, microcrystalline Cellulose, cross-linking sodium carboxymethyl cellulose are crossed 80 ~ 100 mesh sieves respectively, after mix homogeneously, obtained blank mixed accessories;
3) the pastille binding agent of step 1 gained is mixed and dry granulating by the high-pressure sprayer of spray dryer and the blank mixed accessories of step 2 gained;
4) granule of step 3 gained is crossed 18 mesh sieve granulate;
5) step 4 gained granule is added magnesium stearate mix homogeneously, encapsulated.
Wherein, the baking temperature described in step 3 is 24 DEG C, and pellet moisture is lower than 1.3%, and drying time is 6 minutes.
The preparation of embodiment three, Acetylcysteine composition capsule, in 1000
1. prescription:
2. preparation technology
1) by the polyvidone of recipe quantity with 18% alcoholic solution be mixed with 10% PVP solution, then add the acetylcysteine of recipe quantity, make it be uniformly dispersed, obtained pastille binding agent;
2) chitosan nano of recipe quantity, microcrystalline Cellulose, cross-linking sodium carboxymethyl cellulose are crossed 80 ~ 100 mesh sieves respectively, after mix homogeneously, obtained blank mixed accessories;
3) the pastille binding agent of step 1 gained is mixed and dry granulating by the high-pressure sprayer of spray dryer and the blank mixed accessories of step 2 gained;
4) granule of step 3 gained is crossed 18 mesh sieve granulate;
5) step 4 gained granule is added magnesium stearate mix homogeneously, encapsulated.
Wherein, the baking temperature described in step 3 is 26 DEG C, and pellet moisture is lower than 1.2%, and drying time is 5 minutes.
Experimental data
Dissolution contrast test
Get Acetylcysteine composition capsule and each 5 of the commercially available acetylcysteine capsules of the embodiment of the present invention 1 ~ 3 preparation respectively, by the requirement of Chinese Pharmacopoeia version annex XC dissolution test method in 2010, test is compared to the accumulation dissolution of each time point, specific as follows:
With hydrochloric acid solution pH1.0 for medium, rotating speed is 50rpm, through 5,10,15,20,30min samples detection, result is as follows:
1): sample prepared by embodiment 1
2): sample prepared by embodiment 2
3): sample prepared by embodiment 3
4): commercially available acetylcysteine capsules sample
Table-1 dissolution contrast test
Known to table-1,15 minutes time, the average dissolution of Acetylcysteine composition capsule of the present invention reaches 90 ~ 93%, and the dissolution of commercially available acetylcysteine capsules is only 53 ~ 56% of labelled amount, namely the more commercially available acetylcysteine capsules of Acetylcysteine composition capsule of the present invention has the advantage that dissolution rate is faster, dissolution increases.
Stability contrast test
The stability of Acetylcysteine composition capsule of the present invention is investigated with the embodiment of the present invention 1 ~ 3 and commercially available capsule, the Acetylcysteine composition capsule prepare embodiment 1 ~ 3 and commercially available capsule are placed in 40 DEG C of relative humidity 5% accelerated tests 6 months, by high performance liquid chromatography, respectively its content, related substance and 30min dissolution are detected.
1): sample prepared by embodiment 1
2): sample prepared by embodiment 2
3): sample prepared by embodiment 3
4): commercially available acetylcysteine capsules sample
Testing result is as follows:
Table-2 stability contrast tests
Can be found out by table-2, in capsule prepared by the present invention, the content of acetylcysteine is 99.0%-100.3%, the content of related substance is 0.02%-0.20%, and the dissolution of 30 minutes is 94%-100%, is all obviously better than the regulation of Chinese Pharmacopoeia version in 2010 about content and stripping limit; And the content of commercially available product acetylcysteine capsules is 95.2%-99.7%, the content of related substance is the dissolution of 0.15%-0.89%, 30min is 75%-95%.Therefore, Acetylcysteine composition capsule of the present invention is all obviously better than commercially available acetylcysteine capsules on content, related substance, dissolution, has stable in properties, and the second best in quality feature, is more suitable for industrialized great production.
More than show and describe ultimate principle of the present invention, principal character and advantage of the present invention.The technical staff of the industry should understand; the present invention is not restricted to the described embodiments; what describe in above-described embodiment and description is only preference of the present invention; be not used for limiting the present invention; without departing from the spirit and scope of the present invention; the present invention also has various changes and modifications, and these changes and improvements all fall in the claimed scope of the invention.Application claims protection domain is defined by appending claims and equivalent thereof.
Claims (2)
1. a preparation method for Acetylcysteine composition capsule, is characterized in that, comprises the preparation of chitosan nano and the preparation of composition capsule:
The preparation of described chitosan nano,
(1) sieve through 100 eye mesh screens after Chitosan powder being pulverized;
(2) Chitosan powder taking 100g adds 0.1mol/l acetic acid solution 40L, magnetic agitation at 20 DEG C of temperature, chitosan is dissolved completely, obtains chitosan acetic acid solution;
(3) pH=5.0 is regulated with 1%NaOH;
(4) add 1% sodium tripolyphosphate 1667g in chitosan acetic acid solution under stirring, make chitosan/sodium tripolyphosphate mass ratio be 6:1, be cross-linked into nanoparticle by the electrostatic interaction of zwitterion;
(5) by colloid solution 4 DEG C of high speed centrifugation 30min, centrifugal speed is 18000r/min, collects lower sediment, after pure water 3 times, be cooled to less than 30 DEG C vacuum dryings, obtain chitosan nano, moisture is lower than 2%, and particle diameter≤100nm, zeta current potential is 15mv;
The preparation of described composition capsule,
A, by the polyvidone of recipe quantity with 18% alcoholic solution be mixed with 10% PVP solution, then add the acetylcysteine of recipe quantity, make it be uniformly dispersed, obtained pastille binding agent;
B, the chitosan nano of recipe quantity, microcrystalline Cellulose, cross-linking sodium carboxymethyl cellulose are crossed 80 ~ 100 mesh sieves respectively, after mix homogeneously, obtained blank mixed accessories;
C, the pastille binding agent of step a gained to be mixed and dry granulating by the high-pressure sprayer of spray dryer and the blank mixed accessories of step b gained;
D, the granule of step c gained is crossed 18 mesh sieve granulate;
E, steps d gained granule is added magnesium stearate mix homogeneously, encapsulated;
Acetylcysteine composition capsule, be made up of following component:
2. the preparation method of Acetylcysteine composition capsule according to claim 1, it is characterized in that, the baking temperature described in step c is 20 ~ 30 DEG C, and pellet moisture is lower than 1.5%, and drying time is 5 ~ 6 minutes.
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| CN201310479888.7A CN103536575B (en) | 2013-10-15 | 2013-10-15 | Acetylcysteine composition capsule |
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| CN201310479888.7A CN103536575B (en) | 2013-10-15 | 2013-10-15 | Acetylcysteine composition capsule |
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| CN108992476B (en) * | 2018-08-28 | 2021-05-25 | 中国热带农业科学院农产品加工研究所 | Amphiphilic chitosan-macadamia nut oil nano microcapsule and preparation method and application thereof |
| CN110292569B (en) * | 2019-07-15 | 2021-11-02 | 广东人人康药业有限公司 | Acetylcysteine capsule and preparation method thereof |
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Non-Patent Citations (2)
| Title |
|---|
| 乙酰半胱氨酸纳米粒的制备及在小鼠体内的分布;王福根等;《中国医药工业杂志》;20121231;第43卷(第7期);第573页第1行，第576页第3栏 * |
| 乙酰半胱氨酸胶囊的制备及质量控制;代东梅等;《中国医院药学杂志》;20040531;第24卷(第5期);第263页第2.1栏 * |
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