CN103462926A - Famciclovir tablet and preparation method thereof - Google Patents
Famciclovir tablet and preparation method thereof Download PDFInfo
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- CN103462926A CN103462926A CN2013104323943A CN201310432394A CN103462926A CN 103462926 A CN103462926 A CN 103462926A CN 2013104323943 A CN2013104323943 A CN 2013104323943A CN 201310432394 A CN201310432394 A CN 201310432394A CN 103462926 A CN103462926 A CN 103462926A
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Abstract
The invention discloses an antivirus famciclovir tablet. According to the tablet, an aqueous solution of famciclovir and sodium bicarbonate serves as a wetting agent. The tablet is prepared through the wet granulating and tabletting of the following ingredients in parts by weight: 100 parts of famciclovir, 40-65 parts of sodium bicarbonate, 80-200 parts of bulking agent and an appropriate amount of lubricant. Compared with the prior art, the tablet and the preparation method thereof have the advantages that the tablet can be rapidly disintegrated and dissolved without adding a disintegrant, and meanwhile, the preparation method is simple and is suitable for the requirements for large-scale production.
Description
Technical field
The invention belongs to the pharmaceutical preparations technology field, in particular to a kind of for antiviral famciclovir tablet and preparation method thereof.
Background technology
Famciclovir (Famciclovir) is the diethyl acyl fat of the 6-deoxidation derivative of penciclovir (penciclovir), molecular formula is C14H19N5O4, chemistry 2-[2-(2-amino-9H-purine-9-yl) ethyl by name]-1, ammediol-diethylester, be applicable to treat herpes zoster and primary genitalia herpes, become one of main medicine salable in world wide.Structural formula is:
CN101904825A discloses a kind of Falacyclovir dispersion piece and preparation method thereof.This technology has only prepared a kind of dispersible tablet, has just shortened disintegration time, 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 famciclovir, and the inventor considers that drug-eluting affects drug effect, therefore intends the famciclovir 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 famciclovir 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 famciclovir 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 famciclovir tablet, said preparation is to using the aqueous solution of famciclovir 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 famciclovir tablet, wherein: using the aqueous solution of famciclovir and sodium bicarbonate as wetting agent, formed by wet granulation tabletting by the component of following weight portion:
Further preferably, in above-mentioned famciclovir tablet, the weight ratio of famciclovir and sodium bicarbonate is 1:0.5-0.6.
Further preferably, above-mentioned famciclovir tablet, wherein said filler is selected from one or more in microcrystalline Cellulose, lactose, mannitol, starch and pregelatinized Starch.
Further preferably, above-mentioned famciclovir 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 famciclovir tablet, can prepare the famciclovir tablet of Fast Stripping by this technique.Concrete technical scheme is as follows:
A kind of preparation method of famciclovir tablet, the method comprises the steps: famciclovir 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 famciclovir tablet, wherein the weight ratio of famciclovir and sodium bicarbonate is 1:0.5-0.6.
The preparation method of famciclovir 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 famciclovir 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 famciclovir 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 famciclovir tablet and preparation method thereof
Preparation method:
Recipe quantity takes famciclovir, 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 famciclovir tablets and preparation method thereof
Preparation method:
Recipe quantity takes famciclovir, 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 famciclovir tablets and preparation method thereof
Preparation method:
Recipe quantity takes famciclovir, 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 famciclovir tablet and preparation method thereof
Preparation method:
Famciclovir, 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 famciclovir tablets and preparation method thereof
Preparation method:
Famciclovir was pulverized 100 mesh sieves, recipe quantity takes microcrystalline Cellulose and the low-substituted hydroxypropyl cellulose mix homogeneously of famciclovir, 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 famciclovir tablets and preparation method thereof
Preparation method:
Recipe quantity takes famciclovir, 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 Famciclovir Tablets
1, dissolution.Get respectively Famciclovir Tablet prepared by embodiment 1-3 and comparative example 1-3, according to dissolution method (appendix X C the second method), the 0.lmol/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.lmol/L hydrochloric acid solution, quantitatively dilutes and make the solution that approximately contains 10 μ g in every lml.According to UV-VIS spectrophotometry (appendix IV A), measure absorbance at the wavelength place of 254nm immediately; Separately get the famciclovir 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 lml, 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 famciclovir reference substance solution 5ml, adds the guanine reference substance stock solution lml 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 famciclovir peak and guanine peak should meet the requirements.
Algoscopy: get respectively famciclovir 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 famciclovir 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 Famciclovir Tablet, assay result
| Sample source | 5min dissolution (%) | 15min dissolution (%) | Content (%) |
| Embodiment 1 | 94.2 | 99.8 | 99.3 |
| Embodiment 2 | 99.6 | 99.2 | 99.7 |
| Embodiment 3 | 99.1 | 100.0 | 99.7 |
| The comparative example 1 | 37.9 | 74.4 | 98.4 |
| The comparative example 2 | 25.2 | 78.2 | 99.8 |
| The comparative example 3 | 26.9 | 72.5 | 99.2 |
It can be seen from the table, Famciclovir Tablet 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 famciclovir, famciclovir 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 famciclovir 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. a famciclovir tablet is characterized in that: using the aqueous solution of famciclovir and sodium bicarbonate as wetting agent, formed by wet granulation tabletting by the component that comprises following weight portion:
2. famciclovir tablet according to claim 1 is characterized in that: using the aqueous solution of famciclovir and sodium bicarbonate as wetting agent, formed by wet granulation tabletting by the component of following weight portion:
3. famciclovir tablet according to claim 1 and 2, it is characterized in that: the weight ratio of famciclovir and sodium bicarbonate is 1:0.5-0.6.
4. famciclovir 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. famciclovir 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 a famciclovir tablet according to claim 2, is characterized in that comprising the steps: famciclovir 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 famciclovir tablet according to claim 6, it is characterized in that: the weight ratio of famciclovir and sodium bicarbonate is 1:0.5-0.6.
8. the preparation method of famciclovir 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 famciclovir 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 |
|---|---|---|---|---|
| CN106511286A (en) * | 2016-10-27 | 2017-03-22 | 四川省百草生物药业有限公司 | High-stability famciclovir tablet and preparation method thereof |
| CN112057430A (en) * | 2020-10-17 | 2020-12-11 | 迪沙药业集团有限公司 | Famciclovir pharmaceutical composition |
| CN112168829A (en) * | 2020-09-24 | 2021-01-05 | 华南理工大学 | Application of antiviral drug in preparation of drug for treating myelodysplastic syndrome and prepared myelodysplastic syndrome drug |
| CN112587491A (en) * | 2021-01-03 | 2021-04-02 | 迪沙药业集团有限公司 | Famciclovir tablet composition |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101156856A (en) * | 2007-09-29 | 2008-04-09 | 刘全胜 | Falacyclovir dispersion piece and its preparation method |
| 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 |
-
2013
- 2013-09-23 CN CN201310432394.3A patent/CN103462926B/en not_active Expired - Fee Related
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101156856A (en) * | 2007-09-29 | 2008-04-09 | 刘全胜 | Falacyclovir dispersion piece and its preparation method |
| 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 (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106511286A (en) * | 2016-10-27 | 2017-03-22 | 四川省百草生物药业有限公司 | High-stability famciclovir tablet and preparation method thereof |
| CN106511286B (en) * | 2016-10-27 | 2019-12-20 | 四川省百草生物药业有限公司 | Famciclovir tablet with high stability and preparation method thereof |
| CN112168829A (en) * | 2020-09-24 | 2021-01-05 | 华南理工大学 | Application of antiviral drug in preparation of drug for treating myelodysplastic syndrome and prepared myelodysplastic syndrome drug |
| CN112057430A (en) * | 2020-10-17 | 2020-12-11 | 迪沙药业集团有限公司 | Famciclovir pharmaceutical composition |
| CN112587491A (en) * | 2021-01-03 | 2021-04-02 | 迪沙药业集团有限公司 | Famciclovir tablet composition |
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