CN103462917A - Antiviral acyclovir tablet and preparation method thereof - Google Patents
Antiviral acyclovir tablet and preparation method thereof Download PDFInfo
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- CN103462917A CN103462917A CN2013104146690A CN201310414669A CN103462917A CN 103462917 A CN103462917 A CN 103462917A CN 2013104146690 A CN2013104146690 A CN 2013104146690A CN 201310414669 A CN201310414669 A CN 201310414669A CN 103462917 A CN103462917 A CN 103462917A
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Abstract
The invention discloses an antiviral acyclovir tablet. The preparation is prepared by utilizing an aqueous solution of acyclovir and sodium bicarbonate as a wetting agent, and carrying out wet granulating and tabletting on the following components in parts by weight: 100 parts of acyclovir, 40-65 parts of sodium bicarbonate, 80-200 parts of fillers and a proper amount of lubricant. Compared with the prior art, the antiviral acyclovir tablet disclosed by the invention can be quickly disintegrated and dissolved out without adding a disintegrating agent, and meanwhile, the preparation process is simple and is suitable for the requirements of mass production.
Description
Technical field
The invention belongs to the pharmaceutical preparations technology field, in particular to a kind of for antiviral Acyclovir Tablet and preparation method thereof.
Background technology
Acyclovir (Aciclovir) is to suppress DNA type antiviral drugs, is mainly used in clinically skin and mucosa infection that hepatitis B and chickenpox, herpes zoster, herpes simplex virus cause, has become one of main medicine salable in world wide.This medicine is slightly molten in glacial acetic acid or hot water, and almost insoluble in ether or dichloromethane, its structural formula is as follows:
CN101804037A discloses a kind of Acyclovir dispersible tablet and preparation method thereof.Due to acyclovir soluble,very slightly in water, this technology has only prepared a kind of dispersible tablet, has just shortened disintegration time, and not mentionedly how to improve drug dissolution, and quickly disintegrated slice, thin piece, its stripping is not necessarily fast.
By retrieval, find, prior art does not all provide corresponding technical scheme to the dissolution that how to improve acyclovir, and the inventor considers that drug-eluting affects drug effect, therefore intends the Acyclovir Tablet of a kind of Fast Stripping of exploitation.
Summary of the invention
In view of the deficiencies in the prior art, the inventor is creationary by acyclovir and sodium bicarbonate salify, utilize the character of sodium bicarbonate and hydrochloric acid reaction simultaneously, appropriate sodium bicarbonate has been used as effervescent materials, obtained a kind of Acyclovir Tablet of Fast Stripping.
In order to realize purpose of the present invention, the inventor is studied and is explored preparation prescription and technique by lot of experiments, has finally obtained following technical scheme:
A kind of for antiviral Acyclovir Tablet, said preparation is to using the aqueous solution of acyclovir and sodium bicarbonate as wetting agent, by the component that comprises following weight portion (also can contain the pharmaceutically acceptable adjuvants such as correctives in prescription), by wet granulation tabletting, is formed:
Preferably, above-mentioned Acyclovir Tablet, wherein: using the aqueous solution of acyclovir and sodium bicarbonate as wetting agent, formed by wet granulation tabletting by the component of following weight portion:
Further preferably, in above-mentioned Acyclovir Tablet, the weight ratio of acyclovir and sodium bicarbonate is 1:0.5-0.6.
Further preferably, above-mentioned Acyclovir Tablet, wherein said filler is selected from one or more in microcrystalline Cellulose, lactose, mannitol, starch and pregelatinized Starch.
Further preferably, above-mentioned Acyclovir Tablet, wherein said lubricant is one or more in magnesium stearate, micropowder silica gel and sodium stearyl fumarate.
The present invention also provides the preparation technology of above-mentioned Acyclovir Tablet, can prepare the Acyclovir Tablet of Fast Stripping by this technique.Concrete technical scheme is as follows:
A kind of preparation method of Acyclovir Tablet, the method comprises the steps: acyclovir is dissolved in sodium bicarbonate aqueous solution, take this solution as wetting agent, on filler, granulate, drying, then even with mix lubricant, tabletting.
Preferably, the preparation method of above-mentioned Acyclovir Tablet, wherein the weight ratio of acyclovir and sodium bicarbonate is 1:0.5-0.6.
The preparation method of Acyclovir Tablet of the present invention, wherein said filler is selected from one or more in microcrystalline Cellulose, lactose, mannitol, starch and pregelatinized Starch; Described lubricant is one or more in magnesium stearate, micropowder silica gel and sodium stearyl fumarate.
The inventor is dissolved in acyclovir in sodium bicarbonate aqueous solution, then usings this aqueous solution as wetting agent, pharmaceutically on acceptable adjuvant, granulate, and drying, tabletting.When carrying out dissolution determination, because sodium bicarbonate and acyclovir have become sodium salt, therefore dissolubility is good, the inventor has added a part of sodium bicarbonate in right amount simultaneously, the sodium bicarbonate of this part reacts rapidly with the hydrochloric acid in gastric juice, effervescent effect helps the quick disintegrate of tablet, thus tablet of the present invention not only disintegrate is fast, stripping is also very fast.Compared with prior art, the present invention is without adding disintegrating agent, and tablet is disintegrate stripping rapidly, and preparation technology is simple simultaneously, is applicable to large production requirement.
The specific embodiment
Following examples further describe preparation process of the present invention and beneficial effect, embodiment is only for the purpose of illustration, do not limit the scope of the invention, within the apparent change that those of ordinary skills make according to the present invention simultaneously and modification are also contained in the scope of the invention.
Embodiment 1 Acyclovir Tablet and preparation method thereof
Preparation method:
Recipe quantity takes acyclovir, sodium bicarbonate, joins in pure water, is stirred to dissolve, using this aqueous solution as wetting agent, join recipe quantity and cross on the microcrystalline Cellulose of 100 mesh sieves, granulate, 60 ℃ of dryings, 18 mesh sieve granulate, dry granule is mixed homogeneously with magnesium stearate, tabletting.
Embodiment 2 Acyclovir Tablets and preparation method thereof
Preparation method:
Recipe quantity takes acyclovir, sodium bicarbonate, joins in pure water, is stirred to dissolve, using this aqueous solution as wetting agent, join recipe quantity and cross on the lactose of 100 mesh sieves, granulate, 50 ℃ of dryings, 20 mesh sieve granulate, dry granule is mixed homogeneously with magnesium stearate, tabletting.
Embodiment 3 Acyclovir Tablets and preparation method thereof
Preparation method:
Recipe quantity takes acyclovir, sodium bicarbonate, joins in pure water, is stirred to dissolve, using this aqueous solution as wetting agent, join recipe quantity and cross on the microcrystalline Cellulose of 100 mesh sieves, granulate, 55 ℃ of dryings, 18 mesh sieve granulate, dry granule is mixed homogeneously with magnesium stearate, tabletting.
Comparative example's 1 Acyclovir Tablet and preparation method thereof
Preparation method:
Acyclovir, sodium bicarbonate, microcrystalline Cellulose are all crossed 100 mesh sieves, after recipe quantity takes, mix, and add pure water appropriate, 55 ℃ of dryings, and 18 mesh sieve granulate, dry granule is mixed homogeneously with magnesium stearate, tabletting.
Comparative example's 2 Acyclovir Tablets and preparation method thereof
Preparation method:
Acyclovir was pulverized 100 mesh sieves, recipe quantity takes microcrystalline Cellulose and the low-substituted hydroxypropyl cellulose mix homogeneously of acyclovir, lactose, half amount, using 5% PVP K30 50% alcoholic solution as binding agent, granulate, 65 ℃ of dryings, 30 mesh sieve granulate, then mix homogeneously with magnesium stearate and the Aspartane of the microcrystalline Cellulose of surplus and low-substituted hydroxypropyl cellulose, proportional quantities, tabletting.
Comparative example's 3 Acyclovir Tablets and preparation method thereof
Preparation method:
Recipe quantity takes acyclovir, sodium bicarbonate, joins in pure water, is stirred to dissolve, using this aqueous solution as wetting agent, join recipe quantity and cross on the microcrystalline Cellulose of 100 mesh sieves, granulate, 55 ℃ of dryings, 18 mesh sieve granulate, dry granule is mixed homogeneously with magnesium stearate, tabletting.
Dissolution and the assay of embodiment 4 acyclovir slices
1, dissolution.Get respectively acyclovir slice prepared by embodiment 1-3 and comparative example 1-3, according to dissolution method (appendix X C the second method), the 0.1mol/L hydrochloric acid solution 900ml of take is dissolution medium, rotating speed is per minute 50 to turn, and operation in accordance with the law, in the time of 15 minutes, get solution 10ml, filter, it is appropriate that precision measures subsequent filtrate, with the 0.1mol/L hydrochloric acid solution, quantitatively dilutes and make the solution that approximately contains 10 μ g in every 1ml.According to UV-VIS spectrophotometry (appendix IV A), measure absorbance at the wavelength place of 254nm immediately; Separately get the acyclovir reference substance appropriate, accurately weighed, make with 0.1mol/L dissolve with hydrochloric acid solution quantitative dilution the solution that approximately contains 10 μ g in every 1ml, be measured in the same method the stripping quantity that the meter grate is every.Limit is 80% of labelled amount, should be up to specification.
2, assay.According to high performance liquid chromatography (appendix V D), measure, chromatographic condition and system suitability octadecylsilane chemically bonded silica are filler; Methanol-water (10:90) is mobile phase; The detection wavelength is 254nm, gets acyclovir reference substance solution 5ml, adds the guanine reference substance stock solution 1ml under human guanine and other related substance items, shake up, get 20 μ l and annotate people's chromatograph of liquid, record chromatogram, the separating degree at acyclovir peak and guanine peak should meet the requirements.
Algoscopy: get respectively acyclovir agreement that contracts a film or TV play to an actor or actress 50mg prepared by embodiment 1-3 and comparative example 1-3, accurately weighed, put in the 50ml measuring bottle, adding 0.4% sodium hydroxide solution 5ml makes to dissolve, be diluted with water to scale, shake up, precision measures 2ml, put in the 100ml measuring bottle, be diluted with water to scale, shake up, precision measures 20 μ l, annotate people's chromatograph of liquid, record chromatogram; Separately get the acyclovir reference substance appropriate, be measured in the same method.By external standard method, with calculated by peak area, obtain.
The dissolution of table 1 embodiment acyclovir slice, assay result
| Sample source | 5min dissolution (%) | 15min dissolution (%) | Content (%) |
| Embodiment 1 | 94.6 | 99.7 | 99.8 |
| Embodiment 2 | 99.9 | 99.8 | 99.9 |
| Embodiment 3 | 99.0 | 100.1 | 99.8 |
| The comparative example 1 | 32.5 | 78.1 | 99.5 |
| The comparative example 2 | 21.4 | 75.5 | 99.8 |
| The comparative example 3 | 20.6 | 76.4 | 99.7 |
It can be seen from the table, acyclovir slice stripping prepared by embodiment of the present invention 1-3 is quick, the complete stripping of 5min; Comparative example 1 only mixes sodium bicarbonate with acyclovir, acyclovir is salify not, therefore stripping is slow; Comparative example 2 adopts prior art, and stripping is slow; Comparative example 3 has reduced the sodium bicarbonate consumption, although acyclovir and sodium bicarbonate salify, because sodium bicarbonate does not have unnecessary amount, so stripping can not play the effervescent effect while measuring, therefore disintegration of tablet is slow, and the drug slow stripping.
Claims (9)
1. one kind for antiviral Acyclovir Tablet, it is characterized in that: using the aqueous solution of acyclovir and sodium bicarbonate as wetting agent, formed by wet granulation tabletting by the component that comprises following weight portion:
2. Acyclovir Tablet according to claim 1 is characterized in that: using the aqueous solution of acyclovir and sodium bicarbonate as wetting agent, formed by wet granulation tabletting by the component of following weight portion:
3. Acyclovir Tablet according to claim 1 and 2, it is characterized in that: the weight ratio of acyclovir and sodium bicarbonate is 1:0.5-0.6.
4. Acyclovir Tablet according to claim 1 and 2, it is characterized in that: described filler is selected from one or more in microcrystalline Cellulose, lactose, mannitol, starch and pregelatinized Starch.
5. Acyclovir Tablet according to claim 1 and 2, it is characterized in that: described lubricant is one or more in magnesium stearate, micropowder silica gel and sodium stearyl fumarate.
6. the preparation method of an Acyclovir Tablet according to claim 2, is characterized in that comprising the steps: acyclovir is dissolved in sodium bicarbonate aqueous solution, take this solution as wetting agent, on filler, granulate, drying, then even with mix lubricant, tabletting.
7. the preparation method of Acyclovir Tablet according to claim 6, it is characterized in that: the weight ratio of acyclovir and sodium bicarbonate is 1:0.5-0.6.
8. the preparation method of Acyclovir Tablet according to claim 6, it is characterized in that: described filler is selected from one or more in microcrystalline Cellulose, lactose, mannitol, starch and pregelatinized Starch.
9. the preparation method of Acyclovir Tablet according to claim 6, it is characterized in that: described lubricant is one or more in magnesium stearate, micropowder silica gel and sodium stearyl fumarate.
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Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104042576A (en) * | 2014-05-21 | 2014-09-17 | 丽珠医药集团股份有限公司 | Preparation method of acyclovir tablet |
| WO2021186392A1 (en) * | 2020-03-19 | 2021-09-23 | Noel Carroll | Composition |
| CN115212206A (en) * | 2022-08-15 | 2022-10-21 | 江苏知原药业股份有限公司 | Medicinal composition containing pirfenidone and preparation method thereof |
| CN115463102A (en) * | 2022-09-26 | 2022-12-13 | 湖北科益药业股份有限公司 | Acyclovir tablet and preparation method thereof |
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| JP2003506400A (en) * | 1999-08-04 | 2003-02-18 | ランバクシー ラボラトリーズ リミテッド | Hydrodynamically balanced oral dosage form |
| CN1630513A (en) * | 2002-02-04 | 2005-06-22 | 兰贝克赛实验室有限公司 | Hydrodynamically balancing oral drug delivery system with biphasic release |
| EP2133071A1 (en) * | 2008-06-09 | 2009-12-16 | Université de la Méditerranée | Process for making gastroretentive dosage forms |
| CN101961337A (en) * | 2009-07-24 | 2011-02-02 | 北京润德康医药技术有限公司 | Medicinal composition with aciclovir sodium as active ingredient |
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- 2013-09-12 CN CN2013104146690A patent/CN103462917A/en active Pending
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2003506400A (en) * | 1999-08-04 | 2003-02-18 | ランバクシー ラボラトリーズ リミテッド | Hydrodynamically balanced oral dosage form |
| CN1630513A (en) * | 2002-02-04 | 2005-06-22 | 兰贝克赛实验室有限公司 | Hydrodynamically balancing oral drug delivery system with biphasic release |
| EP2133071A1 (en) * | 2008-06-09 | 2009-12-16 | Université de la Méditerranée | Process for making gastroretentive dosage forms |
| CN101961337A (en) * | 2009-07-24 | 2011-02-02 | 北京润德康医药技术有限公司 | Medicinal composition with aciclovir sodium as active ingredient |
Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104042576A (en) * | 2014-05-21 | 2014-09-17 | 丽珠医药集团股份有限公司 | Preparation method of acyclovir tablet |
| WO2021186392A1 (en) * | 2020-03-19 | 2021-09-23 | Noel Carroll | Composition |
| CN115212206A (en) * | 2022-08-15 | 2022-10-21 | 江苏知原药业股份有限公司 | Medicinal composition containing pirfenidone and preparation method thereof |
| CN115212206B (en) * | 2022-08-15 | 2023-04-18 | 江苏知原药业股份有限公司 | Medicinal composition containing pirfenidone and preparation method thereof |
| CN115463102A (en) * | 2022-09-26 | 2022-12-13 | 湖北科益药业股份有限公司 | Acyclovir tablet and preparation method thereof |
| CN115463102B (en) * | 2022-09-26 | 2023-11-24 | 湖北科益药业股份有限公司 | Acyclovir tablet and preparation method thereof |
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Application publication date: 20131225 |