CN101647786B - Aciclovir sustained-release tablet and preparation method thereof - Google Patents
Aciclovir sustained-release tablet and preparation method thereof Download PDFInfo
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- CN101647786B CN101647786B CN2008101183790A CN200810118379A CN101647786B CN 101647786 B CN101647786 B CN 101647786B CN 2008101183790 A CN2008101183790 A CN 2008101183790A CN 200810118379 A CN200810118379 A CN 200810118379A CN 101647786 B CN101647786 B CN 101647786B
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Abstract
The invention aims to provide an aciclovir sustained-release tablet having higher medicament release stability and higher medication security. The aciclovir sustained-release tablet is characterized by consisting of an effectively therapeutic dose of aciclovir, a sustained-release material, a pore-forming agent, an additive and a lubricant, and has the characteristics of convenient administration, lasting effect, stable curative effect, small toxic and side effect and the like.
Description
Technical field
The present invention relates to a kind ofly, belong to field of medicaments with Aciclovir sustained-release tablet and preparation method thereof.
Technical background
Acyclovir has another name called acycloguanosine (Acyclovir is called for short ACV), is the ucleosides antiviral agents, chemistry 9-(2-hydroxyl ethoxymethyl) guanine by name.Wellcome company in 1981 is at first in Britain's these article that gone on the market, trade name: Zovirax.Nineteen eighty-two FDA approval is at the U.S.'s these article of listing.Acyclovir has been one of main medicine salable in the world wide at present.Acyclovir is the isoreagent of acyclic NSC 22837, and the latter is the ingredient of DNA, and acyclovir and its structural similarity have only replaced cyclic sugared structure with an acyclic side chain.
Since the eighties in 20th century, structure, infection mechanism, self-control process and the viral gene of many viruses there has been deep understanding, found that synthetic some link of viral organism is different from host cell.For example the mRNA of virus is different with the mRNA of zooblast, and some virus needs a kind of RNA polymerase that relies on DNA when transcript mRNA from the DNA chain, and this kind of enzyme is that virus is special, does not also need this kind of enzyme in the cellular metabolism.These difference are scientifically set up the target of viral chemotherapy research, for the chemotherapy of virus provides foundation.The research of antiviral drugs has got into the stage of appropriate design new drug, has also obtained progress in the practice.Since particularly idoxuridine comes out, more greatly inspire people, excited people to develop the interest of antiviral drugs.Acyclovir is a second filial generation broad-spectrum antiviral medicament, is the open loop nucleoside medicine of the specific anti herpes-like virus of first listing in the world, has become one of main medicine salable in the world wide.
Summary of the invention
The purpose of this invention is to provide a kind of stability of medicine release and the higher Aciclovir sustained-release tablet of safety of medication, have characteristics such as convenient drug administration, persistent, stable curative effect, toxic and side effects be little.
Aciclovir sustained-release tablet of the present invention is characterized in that being made up of acyclovir, slow-release material, porogen, diluent, binding agent, lubricant.
Aciclovir sustained-release tablet of the present invention, the acyclovir effective dose is 100mg～2000mg, is preferably 100mg～400mg.
Described Aciclovir sustained-release tablet is characterized in that said slow-release material can select one or more in hydroxypropyl methylcellulose, Sulisi aqueous dispersion, ethyl cellulose, methylcellulose, cellulose acetate-phthalate, hydroxypropyl cellulose, carboxymethyl cellulose, sodium carboxymethyl cellulose, hydroxyethyl-cellulose, cellulose acetate, cellulose diacetate, Triafol T, the hydroxy methocel for use.
Described Aciclovir sustained-release tablet is characterized in that said porogen can select one or more in microcrystalline Cellulose, low-substituted hydroxypropyl cellulose, polyvinyl alcohol, Polyethylene Glycol, sodium alginate, chitosan, sucrose, the lactose for use.
Described Aciclovir sustained-release tablet is characterized in that said diluent can select microcrystalline Cellulose, mannitol, low-substituted hydroxypropyl cellulose, polyvinyl alcohol for use, gather in phthalic acid vinyl acetate, Polyethylene Glycol, the ethanol one or more.
Described Aciclovir sustained-release tablet is characterized in that said lubricant can select magnesium stearate, micropowder silica gel, Pulvis Talci, hydrogenated vegetable oil, polyethylene glycols for use, month hang in the pure magnesium sulfate one or more.
Described Aciclovir sustained-release tablet is characterized in that in the optional water of said binding agent, ethanol, dehydrated alcohol, starch slurry, polyvidone, crospolyvinylpyrrolidone, hydroxypropyl methylcellulose and/or other cellulose families one or more.
Described Aciclovir sustained-release tablet; It is characterized in that said slow releasing tablet adopts dissolution method (two appendix XC of Chinese Pharmacopoeia version in 2005) second subtraction unit according to drug release determination method (two appendix XD first methods of Chinese Pharmacopoeia version in 2005); 900ml is a solvent with hydrochloric acid solution (9 → 1000); Rotating speed is that per minute 100 changes, got solution 3ml at 1 hour, 2 hours, 5 hours respectively and filters, and the instant hydrochloric acid solvent that in process container, replenishes with volume.It is an amount of that precision is measured subsequent filtrate respectively, adds phosphate acid buffer (PH6.8) 2ml, is diluted to scale with water, shake up, the photograph spectrophotography (" two appendix IV of Chinese pharmacopoeia version in 2005 A), measure trap respectively in the 252nm wavelength; Press C
8H
11N
5O
3Absorptance (E
1% 1cm) be 622 to calculate the burst size of every different time.Every of these article should should be more than 15%～35%, 35%～55% and 80% of labelled amount at 1 hour, 2 hours respectively with 5 hours burst size mutually.
Described Aciclovir sustained-release tablet; It is characterized in that; Said slow releasing tablet adopts dissolution method (two appendix XC of Chinese Pharmacopoeia version in 2005) second subtraction unit according to drug release determination method (two appendix XD first methods of Chinese Pharmacopoeia version in 2005), is solvent with 0.1mol/L hydrochloric acid solution, pH5.8 phosphate buffer, distilled water respectively; Measured its burst size respectively at 0.5,1,2,3,4,5,6 hour, the releasing trend of described slow releasing tablet in different release medium reaches unanimity.
Described Aciclovir sustained-release tablet is characterized in that counting by weight percentage, and it consists of:
Acyclovir 20～70%
Slow-release material 0～40%
Diluent 0～50%
Binding agent is an amount of
The method for preparing of described Aciclovir sustained-release tablet, it comprises following steps:
(1) preparation of granules
A, will write out a prescription in each component cross 100 mesh sieves respectively, subsequent use.
B, with porogen and mixing diluents evenly back and slow-release material with the abundant mixing of equivalent incremental method, again with the acyclovir mix homogeneously; Prepare soft material with binding agent, cross 20 mesh sieve system wet granulars, 60 ℃ of forced air dryings, 18 mesh sieve granulate add the lubricant mixing, and are subsequent use.
(2) tabletting with 12mm drift tabletting, promptly gets the granule of step (1) gained.
Beneficial effect
Acyclovir is processed slow releasing tablet has following beneficial effect:
1, compare with conventional formulation, the slow releasing preparation rate of releasing drug is steady, near the zero level rate process, can overcome " peak valley " phenomenon that is produced behind the ordinary preparation multiple dose administration.After conventional formulation was taken medicine, drug level rose to maximum rapidly, because metabolism is drained and Degradation, reduced rapidly again then, be controlled between MEC and the maximum safe concentration drug level relatively more difficult;
2, can make in the body effective blood drug concentration length of holding time, and steadily, utilization ratio of drug can reach more than 80%, and the utilization rate of conventional medicine is merely 40～60%;
3, can reduce medicine to the gastrointestinal side effect.Conventional formulation is processed slow releasing preparation and can be reduced side effect because oral back disintegrate stripping in gastrointestinal tract is big to GI irritation;
4, obviously prolonged the medicine constant release time, therefore reduced medicining times, improve patient's compliance, abirritate and untoward reaction are specially adapted to the medicine that the half-life weak point need frequently be taken.
Specific embodiment
Prescription
Acyclovir 200g
Hydroxypropyl methylcellulose K15 18g
Hydroxypropyl methylcellulose K4MK
45g
Microcrystalline Cellulose 140g
Lactose 50g
Magnesium stearate 4g
10% 30 POVIDONE K 30 BP/USP, 30 alcoholic solution are an amount of
Process 1000 altogether
Preparation process
(1) preparation of granules
A, will write out a prescription in each component cross 100 mesh sieves respectively, subsequent use.
B, with behind microcrystalline Cellulose, the lactose mix homogeneously with hydroxypropyl methylcellulose K
15, hydroxypropyl methylcellulose K
4With the abundant mixing of equivalent incremental method, again with the acyclovir mix homogeneously; With 10% 30 POVIDONE K 30 BP/USP
3050% alcoholic solution is a binding agent system soft material, crosses 20 mesh sieve system wet granulars, 60 ℃ of forced air dryings, and 18 mesh sieve granulate add the magnesium stearate mixing, and are subsequent use.
(2) tabletting with 12mm drift tabletting, promptly gets the granule of step (1) gained.
Prescription
Acyclovir 200g
Hydroxypropyl methylcellulose K15 15g
Hydroxypropyl methylcellulose K4MK
45g
Microcrystalline Cellulose 140g
Lactose 50g
Magnesium stearate 4g
10% 30 POVIDONE K 30 BP/USP, 30 alcoholic solution are an amount of
Process 1000 altogether
Preparation process
(1) preparation of granules
A, will write out a prescription in each component cross 100 mesh sieves respectively, subsequent use.
B, with behind microcrystalline Cellulose, the lactose mix homogeneously with hydroxypropyl methylcellulose K
15, hydroxypropyl methylcellulose K
4With the abundant mixing of equivalent incremental method, again with the acyclovir mix homogeneously; With 10% 30 POVIDONE K 30 BP/USP
3050% alcoholic solution is a binding agent system soft material, crosses 20 mesh sieve system wet granulars, 60 ℃ of forced air dryings, and 18 mesh sieve granulate add the magnesium stearate mixing, and are subsequent use.
(2) tabletting with 12mm drift tabletting, promptly gets the granule of step (1) gained.
Prescription
Acyclovir 200g
Hydroxypropyl methylcellulose K15 17g
Hydroxypropyl methylcellulose K4MK
45g
Microcrystalline Cellulose 140g
Lactose 50g
Magnesium stearate 4g
10% 30 POVIDONE K 30 BP/USP, 30 alcoholic solution are an amount of
Process 1000 altogether
Preparation process
(1) preparation of granules
A, will write out a prescription in each component cross 100 mesh sieves respectively, subsequent use.
B, with behind microcrystalline Cellulose, the lactose mix homogeneously with hydroxypropyl methylcellulose K
15, hydroxypropyl methylcellulose K
4With the abundant mixing of equivalent incremental method, again with the acyclovir mix homogeneously; With 10% 30 POVIDONE K 30 BP/USP
3050% alcoholic solution is a binding agent system soft material, crosses 20 mesh sieve system wet granulars, 60 ℃ of forced air dryings, and 18 mesh sieve granulate add the magnesium stearate mixing, and are subsequent use.
(2) tabletting with 12mm drift tabletting, promptly gets the granule of step (1) gained.
In order to investigate release in vitro effect of the present invention; According to drug release determination method (two appendix XD first methods of Chinese Pharmacopoeia version in 2005); Adopt dissolution method (two appendix XC of Chinese Pharmacopoeia version in 2005) second subtraction unit, measured the release in vitro degree of the Aciclovir sustained-release tablet of the present invention's preparation.
900ml is a solvent with hydrochloric acid solution (9 → 1000), and rotating speed is that per minute 100 changes, got solution 3ml at 1 hour, 2 hours, 5 hours respectively and filter, and the instant hydrochloric acid solvent that in process container, replenishes with volume.It is an amount of that precision is measured subsequent filtrate respectively, adds phosphate acid buffer (PH6.8) 2ml, is diluted to scale with water, shake up, the photograph spectrophotography (" two appendix IVA of Chinese pharmacopoeia version in 2005), measure trap respectively in the 252nm wavelength; Press C
8H
11N
5O
3Absorptance (E
1% 1cm) be 622 to calculate the burst size of every different time.Calculate every burst size respectively at different time.Slow releasing tablet of the present invention was 1 hour, 2 hours, 5 hours burst size.
The Aciclovir sustained-release tablet of three embodiment preparations, release characteristic is:
Three embodiment releasing curve diagrams are seen Fig. 1.
In order further to investigate the release degree of slow releasing tablet in different medium of the present invention's preparation; Adopt the slow releasing tablet of embodiment 1 preparation; According to drug release determination method (two appendix XD first methods of Chinese Pharmacopoeia version in 2005); Adopt dissolution method (two appendix XC of Chinese Pharmacopoeia version in 2005) second subtraction unit, in different release medium, discharge mensuration respectively.Adopt different release medium in 3: 0.1mol/L hydrochloric acid solution, pH5.8 phosphate buffer, distilled water, measured its burst size respectively at 0.5,1,2,3,4,5,6 hour.
Slow releasing tablet release profiles of different medium in 3 of embodiment 1 preparation is seen Fig. 2.
Result of the test shows that the releasing trend of Aciclovir sustained-release tablet in different release medium of the present invention's preparation reaches unanimity.
Release degree in 0.1mol/L HCl solution
Release degree in the pH5.8 phosphate buffer
Release degree in distilled water
Description of drawings:
Fig. 1 is three embodiment releasing curve diagrams;
Fig. 2 is the releasing curve diagram of slow releasing tablet different medium in 3 of embodiment 1 preparation.
Claims (3)
1. Aciclovir sustained-release tablet is characterized in that this slow releasing tablet is composed of the following components:
Or
Or
2. the method for preparing of slow releasing tablet as claimed in claim 1, its step is following:
(1) preparation of granules:
A, will write out a prescription in each component cross 100 mesh sieves respectively, subsequent use;
B, with behind microcrystalline Cellulose, the lactose mix homogeneously with hydroxypropyl methylcellulose K15, hydroxypropyl methylcellulose K4 with the abundant mixing of equivalent incremental method, again with the acyclovir mix homogeneously; With 10% 30 POVIDONE K 30 BP/USP, 30 50% alcoholic solution is binding agent system soft material, crosses 20 mesh sieve system wet granulars, 60 ℃ of forced air dryings, and 18 mesh sieve granulate add the magnesium stearate mixing, and are subsequent use;
(2) tabletting with 12mm drift tabletting, promptly gets the granule of step (1) gained.
3. slow releasing tablet as claimed in claim 1; It is characterized in that; Said slow releasing tablet adopts two appendix X of dissolution method Chinese Pharmacopoeia version in 2005 C, second subtraction unit according to two appendix X of drug release determination method Chinese Pharmacopoeia version in 2005 D, first method, is solvent with 0.1mol/L hydrochloric acid solution, pH5.8 phosphate buffer, distilled water respectively; Measured its burst size respectively at 0.5,1,2,3,4,5,6 hour, the releasing trend of described slow releasing tablet in different release medium reaches unanimity.
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| CN2008101183790A CN101647786B (en) | 2008-08-15 | 2008-08-15 | Aciclovir sustained-release tablet and preparation method thereof |
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| CN2008101183790A CN101647786B (en) | 2008-08-15 | 2008-08-15 | Aciclovir sustained-release tablet and preparation method thereof |
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| CN101647786B true CN101647786B (en) | 2012-01-25 |
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| CN102058553B (en) * | 2010-12-28 | 2012-10-10 | 哈药集团三精制药股份有限公司 | Acyclovir sustained release tablet and preparation method thereof |
| CN104666267B (en) * | 2015-03-27 | 2017-08-08 | 康普药业股份有限公司 | A kind of ACV pharmaceutical composition |
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Address after: 100083 Haidian District, Xueyuan Road, No. 30, A building, room No. 15, room, room 15 Patentee after: COSCI MED-TECH Co.,Ltd. Address before: 100190, room 1410, satellite building, No. 63, Zhichun Road, Beijing, Haidian District Patentee before: COSCI MED-TECH Co.,Ltd. |
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Effective date of registration: 20230320 Address after: 8639, Floor 6, Building 3, No. 3, Yongchang North Road, Daxing District, Beijing, 100176 Patentee after: Beijing Kexin Jurun Pharmaceutical Technology Co.,Ltd. Address before: 100083 room 15, 15 / F, block a, Tiangong building, 30 Xueyuan Road, Haidian District, Beijing Patentee before: COSCI MED-TECH Co.,Ltd. |
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