CN102058553B - Acyclovir sustained release tablet and preparation method thereof - Google Patents
Acyclovir sustained release tablet and preparation method thereof Download PDFInfo
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- CN102058553B CN102058553B CN201010608384A CN201010608384A CN102058553B CN 102058553 B CN102058553 B CN 102058553B CN 201010608384 A CN201010608384 A CN 201010608384A CN 201010608384 A CN201010608384 A CN 201010608384A CN 102058553 B CN102058553 B CN 102058553B
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- hypromellose
- acyclovir
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Abstract
The invention relates to an acyclovir sustained release tablet and a preparation method thereof. The acyclovir sustained release tablet comprises the following components in percentage by weight: 60-64 percent of acyclovir, 10-12 percent of hydroxypropyl methylcellulose K100M, 1.2-1.3 percent of hydroxypropyl methylcellulose E5LV, 15-20 percent of microcrystalline cellulose, 5-6 percent of lactose, 2.4-2.6 percent of aerosol and 0.4-0.6 percent of magnesium stearate. The preparation method comprises the following steps of: preparing 1/3-1/5 of the acyclovir, the lactose, 1/5 of the microcrystalline cellulose and a proper quantity of the hydroxypropyl methylcellulose E5LV into quick release particles; preparing 2/3-4/5 of the acyclovir, the hydroxypropyl methylcellulose K100M, 2/5 of the microcrystalline cellulose and a proper quantity of the hydroxypropyl methylcellulose E5LV into sustained release particles; and mixing and laminating the quick release particles, the sustained release particles, 2/5 of the microcrystalline cellulose, the aerosol and magnesium stearate into the sustained release tablet. The release quantities of 1 hour, 4 fours and 10 hours of the sustained release tablet respectively reach 30-45 percent, 50-65 percent and higher than 75 percent; the sustained release table is convenient to take and has a definite curative effect; and the release period of the sustained release tablet can reach 12 hours, thereby the administration numbers of times are reduced.
Description
Technical field
The invention belongs to field of pharmaceutical preparations, relate to a kind of method for preparing of medicine, specifically a kind of Aciclovir sustained-release tablet method for preparing.
Background technology
Acyclovir (Aciclovir) is a second filial generation broad-spectrum antiviral medicament, is the open loop nucleoside medicine of first specific anti herpes-like virus of Initial Public Offering in the world in 1981, has become one of main medicine salable in the world wide.This medicine mainly is applicable to acute herpes zoster, genital herpes and chickenpox.
Because the very short (t of half-life of acyclovir
1/2=2.5 hours), bioavailability low (being merely 10%～20%) is effective disease controlling, takes the acyclovir oral formulations of conventional rapid release, the patient need take medicine 5 every day.Every day, medicining times was too many; And be regardless of evening on daytime; Patient is difficult to follow the doctor's advice, and has to miss more, is unfavorable for very much the control of the state of an illness; Press for the longer sustained-release preparation of a drug effect period ratio acyclovir ordinary preparation on the clinical treatment, thereby significantly reduce medicining times every day, improve the compliance of patient's medication.Aciclovir sustained-release tablet is produced in listing at home at present, and specification 200mg/ sheet is obeyed 3 every day, and each 2, still need multiple dosing every day as " slow release " preparation, be unfavorable for making things convenient for effective control of the administration and the state of an illness.
Acyclovir is insoluble in water; In order to control the rate of release of principal agent, make it reach 12 hours drug release rates stably, select suitable framework material; To make two parts mixed pressuring plate can reach best releasing effect for slow-releasing granules and the suitable adjuvant of this two parts selection of controlled release granule simultaneously.
Summary of the invention
The object of the present invention is to provide and a kind ofly can reduce administration number of times, improve the medication compliance, realize the more effectively Aciclovir sustained-release tablet of disease controlling.The present invention also aims to provide a kind of method for preparing of Aciclovir sustained-release tablet.
The objective of the invention is to realize like this:
The percentage by weight of Aciclovir sustained-release tablet of the present invention consists of acyclovir 60-64%, hypromellose K100M10-12%, hypromellose E5LV 1.2-1.3%, microcrystalline Cellulose 15-20%, lactose 5-6%, micropowder silica gel 2.4-2.6% and magnesium stearate 0.4-0.6%; The acyclovir of 1/3-1/5, lactose and 1/5 microcrystalline Cellulose and an amount of hypromellose E5LV process immediate-release granules; The microcrystalline Cellulose of the acyclovir of 2/3-4/5 amount, hypromellose K100M, 2/5 amount and an amount of hypromellose E5LV process slow-releasing granules; The microcrystalline Cellulose of immediate-release granules, slow-releasing granules, 2/5 amount, micropowder silica gel and magnesium stearate mixing are pressed into slow releasing tablet.
The method for preparing of Aciclovir sustained-release tablet of the present invention is:
The percentage by weight of raw material consists of acyclovir 60-64%, hypromellose K100M 10-12%, hypromellose E5LV 1.2-1.3%, microcrystalline Cellulose 15-20%, lactose 5-6%, micropowder silica gel 2.4-2.6% and magnesium stearate 0.4-0.6%;
Increase progressively the microcrystalline Cellulose of acyclovir, lactose and 1/5 amount of dilution method adding 1/3-1/5 amount by equivalent; Mix homogeneously; Using the depletion of QI spraying system to add an amount of weight ratio concentration is that 5% hypromellose E5LV aqueous solution is processed soft material, and 40 mesh sieves are granulated, 60 ℃ of dryings; 40 mesh sieve granulate obtain immediate-release granules;
Increase progressively the microcrystalline Cellulose of acyclovir, hypromellose K100Mh and 2/5 amount of dilution method adding 2/3-4/5 amount by equivalent; Mix homogeneously; Using the depletion of QI spraying system to add an amount of weight ratio concentration is that 5% hypromellose E5LV aqueous solution is processed soft material, and 40 mesh sieves are granulated, 60 ℃ of dryings; 40 mesh sieve granulate obtain slow-releasing granules;
Add microcrystalline Cellulose, micropowder silica gel and the magnesium stearate of slow-releasing granules, immediate-release granules, 2/5 amount successively, evenly mixed, last machine tabletting obtains Aciclovir sustained-release tablet.
The invention provides a kind of anti-herpesvirus medicament Aciclovir sustained-release tablet preparation, specification is the 600mg/ sheet, and twice administration in a day reduces administration number of times, improves the medication compliance, realizes more effectively disease controlling.Aciclovir sustained-release tablet of the present invention through preparation immediate-release granules, slow-releasing granules and suppress technology in blocks and process, makes the burst size of medicine reach 30-45% respectively at 1 hour, 4 hours and 10 hours, more than the 50%-65% and 75%.
Hypromellose K100M among the present invention is that erodible skeleton body material, microcrystalline Cellulose and lactose are that filler, hypromellose E5LV are that binding agent, micropowder silica gel are that fluidizer, magnesium stearate are lubricant.
The main body of method of the present invention is to adopt wet granulation technology to prepare immediate-release granules, slow-releasing granules respectively, and adds adjuvant compacting such as fluidizer and form Aciclovir sustained-release tablet, and its characteristics are following:
1, manufacturing process: Aciclovir sustained-release tablet of the present invention is used the technology of " rapid release-slow release medicine-containing particle is granulated separately, speed-slow-releasing granules proportional mixing film-making ".
2, drug release characteristics and drug effect characteristic: Aciclovir sustained-release tablet of the present invention (12 hours) has specific fabricating technology, and its drug release characteristics is that medicine is with " combination type that rapid release-slow release combines " kenel control release.
3, Aciclovir sustained-release tablet of the present invention reaches 12 hours deenergized period, and is all longer than the deenergized period of the same veriety that goes on the market, and reduced administration number of times, for the patient provides convenience.
Adopt " rapid release-slow release medicine-containing particle is granulated separately, speed-slow-releasing granules proportional mixing film-making " Aciclovir sustained-release tablet of prepared can reach 12 hours drug release rate; 2 administrations of one day treatment phase; Keep 1 administration of one day phase, its 24 hours doses are less than the acyclovir oral formulations of conventional rapid release greatly, have improved the compliance of patient's medication; Reduced the toxic and side effects of this medicine; Realize more effectively disease controlling, its medical expense reduces 25%--35% than three medications in a day and conventional rapid release drug cost, has reduced the medication expenditure of extensive patients.
Said slow releasing tablet is according to drug release determination method (two appendix XD first methods of Chinese Pharmacopoeia version in 2010); Adopting the device of dissolution method second method, is solvent with pH6.8 phosphate buffer 900ml, and rotating speed is that per minute 75 changes; (diameter 1cm, spacing 0.5cm, high 2.5cm) puts into stripping rotor with the corrosion-resistant coil that sheet is housed; Operation in accordance with the law through 1,4,10 hour, is got solution 5ml respectively; Filter with 0.45 μ m filter membrane, and in time in process container, replenish the pH6.8 phosphate buffer 5ml of uniform temp.Precision is measured 1,4,10 hour sampling subsequent filtrate 1.0ml, puts in the 50ml measuring bottle, is diluted to scale with the pH6.8 phosphate buffer, as need testing solution.Other gets acyclovir reference substance 25mg, accurate claims surely, dissolves and be diluted to solution that every 1ml contains 10 μ g as reference substance solution with the pH6.8 phosphate buffer.Get need testing solution and reference substance solution,, measure trap, calculate every burst size respectively at different time in the 252nm wavelength according to spectrophotography (two appendix IVA of Chinese Pharmacopoeia version in 2000).Every of these article reach 30-45% respectively in the burst size of 1 hour, 4 hours and 10 hours, more than the 50%-65% and 75%.
The specific embodiment
For example the present invention is done in more detail below and describes:
Embodiment one:
Proportioning raw materials:
Acyclovir 600g
Hypromellose K100M 109g
Hypromellose E5LV 12.2g
Microcrystalline Cellulose 150g
Lactose 50g
Micropowder silica gel 24g
Magnesium stearate 4.8g
Method for preparing:
Immediate release section: the microcrystalline Cellulose that increases progressively acyclovir, lactose and 1/5 recipe quantity that dilution method adds 1/3 recipe quantity by equivalent; Mix homogeneously adds an amount of 5% hypromellose E5LV aqueous solution system soft material with the depletion of QI spraying system, and 40 mesh sieves are granulated; 60 ℃ of dryings, 40 mesh sieve granulate.
Slow-released part: the microcrystalline Cellulose that increases progressively acyclovir, hypromellose K100M and 2/5 recipe quantity that dilution method adds 2/3 recipe quantity by equivalent; Mix homogeneously; Add an amount of 5% hypromellose E5 aqueous solution system soft material with the depletion of QI spraying system; 40 mesh sieves are granulated, 60 ℃ of dryings, 40 mesh sieve granulate.
Tabletting: add microcrystalline Cellulose, micropowder silica gel and the magnesium stearate of Aciclovir sustained-release granule, acyclovir immediate-release granules, 2/5 recipe quantity successively, evenly mixed, be pressed into 1000, promptly get Aciclovir sustained-release tablet.
Embodiment two:
Proportioning raw materials:
Acyclovir 600g
Hypromellose K100M 109g
Hypromellose E5LV 12.2g
Microcrystalline Cellulose 175g
Lactose 50g
Micropowder silica gel 24g
Magnesium stearate 4.8g
Method for preparing:
Immediate release section: the microcrystalline Cellulose that increases progressively acyclovir, lactose and 1/5 recipe quantity that dilution method adds 1/4 recipe quantity by equivalent; Mix homogeneously adds an amount of 5% hypromellose E5LV aqueous solution system soft material with the depletion of QI spraying system, and 40 mesh sieves are granulated; 60 ℃ of dryings, 40 mesh sieve granulate.
Slow-released part: the microcrystalline Cellulose that increases progressively acyclovir, hypromellose K100M and 2/5 recipe quantity that dilution method adds 3/4 recipe quantity by equivalent; Mix homogeneously; Add an amount of 5% hypromellose E5 aqueous solution system soft material with the depletion of QI spraying system; 40 sieve series grains, 60 ℃ of dryings, 40 mesh sieve granulate.
Tabletting: add microcrystalline Cellulose, micropowder silica gel and the magnesium stearate of Aciclovir sustained-release granule, acyclovir immediate-release granules, 2/5 recipe quantity successively, evenly mixed, be pressed into 1000, promptly get Aciclovir sustained-release tablet.
Embodiment three:
Proportioning raw materials:
Acyclovir 600g
Hypromellose K100M 109g
Hypromellose E5LV 12.2g
Microcrystalline Cellulose 200g
Lactose 50g
Micropowder silica gel 24g
Magnesium stearate 4.8g
Method for preparing:
Immediate release section: the microcrystalline Cellulose that increases progressively acyclovir, lactose and 1/5 recipe quantity that dilution method adds 1/5 recipe quantity by equivalent; Mix homogeneously adds an amount of 5% hypromellose E5LV aqueous solution system soft material with the depletion of QI spraying system, and 40 mesh sieves are granulated; 60 ℃ of dryings, 40 mesh sieve granulate.
Slow-released part: the microcrystalline Cellulose that increases progressively acyclovir, hypromellose K100M and 2/5 recipe quantity that dilution method adds 4/5 recipe quantity by equivalent; Mix homogeneously; Add an amount of 5% hypromellose E5 aqueous solution system soft material with the depletion of QI spraying system; 40 mesh sieves are granulated, 60 ℃ of dryings, 40 mesh sieve granulate.
Tabletting: add microcrystalline Cellulose, micropowder silica gel and the magnesium stearate of Aciclovir sustained-release granule, acyclovir immediate-release granules, 2/5 recipe quantity successively, evenly mixed, be pressed into 1000, promptly get Aciclovir sustained-release tablet.
The Aciclovir sustained-release tablet and the commercially available Aciclovir sustained-release tablet of three embodiment preparations, release characteristic is:
Claims (2)
1. Aciclovir sustained-release tablet, it is characterized in that: percentage by weight consists of acyclovir 60-64%, hypromellose K100M 10-12%, hypromellose E5LV 1.2-1.3%, microcrystalline Cellulose 15-20%, lactose 5-6%, micropowder silica gel 2.4-2.6% and magnesium stearate 0.4-0.6%; The acyclovir of 1/5-1/3, lactose and 1/5 microcrystalline Cellulose and an amount of hypromellose E5LV process immediate-release granules; The microcrystalline Cellulose of the acyclovir of 2/3-4/5 amount, hypromellose K100M, 2/5 amount and an amount of hypromellose E5LV process slow-releasing granules; The microcrystalline Cellulose of immediate-release granules, slow-releasing granules, 2/5 amount, micropowder silica gel and magnesium stearate mixing are pressed into slow releasing tablet.
2. the method for preparing of an Aciclovir sustained-release tablet is characterized in that:
The percentage by weight of raw material consists of acyclovir 60-64%, hypromellose K100M 10-12%, hypromellose E5LV 1.2-1.3%, microcrystalline Cellulose 15-20%, lactose 5-6%, micropowder silica gel 2.4-2.6% and magnesium stearate 0.4-0.6%;
Increase progressively the microcrystalline Cellulose of acyclovir, lactose and 1/5 amount of dilution method adding 1/5-1/3 amount by equivalent; Mix homogeneously; Using the depletion of QI spraying system to add an amount of weight ratio concentration is that 5% hypromellose E5LV aqueous solution is processed soft material, and 40 mesh sieves are granulated, 60 ℃ of dryings; 40 mesh sieve granulate obtain immediate-release granules;
Increase progressively the microcrystalline Cellulose of acyclovir, hypromellose K100M and 2/5 amount of dilution method adding 2/3-4/5 amount by equivalent; Mix homogeneously; Using the depletion of QI spraying system to add an amount of weight ratio concentration is that 5% hypromellose E5LV aqueous solution is processed soft material, and 40 mesh sieves are granulated, 60 ℃ of dryings; 40 mesh sieve granulate obtain slow-releasing granules;
Add microcrystalline Cellulose, micropowder silica gel and the magnesium stearate of slow-releasing granules, immediate-release granules, 2/5 amount successively, evenly mixed, last machine tabletting obtains Aciclovir sustained-release tablet.
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| Application Number | Priority Date | Filing Date | Title |
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| CN201010608384A CN102058553B (en) | 2010-12-28 | 2010-12-28 | Acyclovir sustained release tablet and preparation method thereof |
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| CN201010608384A CN102058553B (en) | 2010-12-28 | 2010-12-28 | Acyclovir sustained release tablet and preparation method thereof |
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| CN102058553B true CN102058553B (en) | 2012-10-10 |
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Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2007000779A2 (en) * | 2005-06-29 | 2007-01-04 | Panacea Biotec Ltd. | Pharmaceutical sustained release compositions and processes thereof |
| CN101502522A (en) * | 2008-09-04 | 2009-08-12 | 山东淄博新达制药有限公司 | Acyclovir enteric sustained-release preparation composition and method for preparing the same |
| CN101502521A (en) * | 2008-09-04 | 2009-08-12 | 山东淄博新达制药有限公司 | Acyclovir sustained-release preparation composition and method for preparing the same |
| CN101647786A (en) * | 2008-08-15 | 2010-02-17 | 北京科信必成医药科技发展有限公司 | Aciclovir sustained-release tablet and preparation method thereof |
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2010
- 2010-12-28 CN CN201010608384A patent/CN102058553B/en active Active
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2007000779A2 (en) * | 2005-06-29 | 2007-01-04 | Panacea Biotec Ltd. | Pharmaceutical sustained release compositions and processes thereof |
| CN101647786A (en) * | 2008-08-15 | 2010-02-17 | 北京科信必成医药科技发展有限公司 | Aciclovir sustained-release tablet and preparation method thereof |
| CN101502522A (en) * | 2008-09-04 | 2009-08-12 | 山东淄博新达制药有限公司 | Acyclovir enteric sustained-release preparation composition and method for preparing the same |
| CN101502521A (en) * | 2008-09-04 | 2009-08-12 | 山东淄博新达制药有限公司 | Acyclovir sustained-release preparation composition and method for preparing the same |
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Owner name: SANJING PHARMACEUTICAL CO., LTD., HAYAO GROUP Free format text: FORMER OWNER: HARBIN PHARMACEUTICAL GROUP SANJING PHARMACEUTICAL CO., LTD. Effective date: 20150619 |
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Effective date of registration: 20150619 Address after: 150000 No. 76, Nangang concentration area, Hengshan Road District, Harbin, Heilongjiang Patentee after: Sanjing Pharmaceutical Co., Ltd., Hayao Group Address before: 150069 Heilongjiang Province, Harbin city Xiangfang District haping Road No. 233 Patentee before: Harbin Pharmaceutical Group, Sanjing Pharmaceutical Co., Ltd. |
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Effective date of registration: 20160127 Address after: Industrial Park Suihua city Heilongjiang province 150000 Sanjing pharmaceutical Mingshui County Patentee after: HARBIN PHARM. GROUP SANJING MINGSHUI PHARMACEUTICAL CO., LTD. Address before: 150000 No. 76, Nangang concentration area, Hengshan Road District, Harbin, Heilongjiang Patentee before: Sanjing Pharmaceutical Co., Ltd., Hayao Group |