CN103462918B - A kind of Valaciclovir hydrochloride tablet and preparation method thereof - Google Patents
A kind of Valaciclovir hydrochloride tablet and preparation method thereof Download PDFInfo
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- CN103462918B CN103462918B CN201310430502.3A CN201310430502A CN103462918B CN 103462918 B CN103462918 B CN 103462918B CN 201310430502 A CN201310430502 A CN 201310430502A CN 103462918 B CN103462918 B CN 103462918B
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- valaciclovir
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- hydrochloride tablet
- sodium bicarbonate
- hydrochlordide
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Abstract
The invention discloses a kind of for antiviral Valaciclovir hydrochloride tablet, said preparation is using the aqueous solution of valaciclovir hydrochlordide and sodium bicarbonate as wetting agent, by the component comprising following weight portion by wet granulation and tabletting form: valaciclovir hydrochlordide 100 parts, sodium bicarbonate 40-65 part, filler 80-200 part, lubricant is appropriate.Compared with prior art, the present invention is without the need to adding disintegrating agent, and tablet can disintegrate stripping rapidly, and preparation technology is simple simultaneously, is applicable to large production requirement.
Description
Technical field
The invention belongs to pharmaceutical preparations technology field, be used for antiviral Valaciclovir hydrochloride tablet and preparation method thereof in particular to one.
Background technology
Valaciclovir hydrochlordide suppresses DNA type antiviral drugs, and clinical being mainly used in treats varicella zoster and the viral infection such as I type, II type herpes simplex, has become one of key agents salable in world wide.Chemistry Valine-2-by name [amino-1, the 6 dihydro-9H-purine-9-bases of 6-2-] ester hydrochloride.This medicine this product is easily molten in water, dissolves in methanol.
CN1513454A discloses a kind of dispersion tablet of vasilowy hydrochlaride and preparation method thereof.This technology has only prepared a kind of dispersible tablet, just shortens disintegration time, and quickly disintegrated slice, thin piece, its stripping is not necessarily fast.
Found by retrieval, prior art does not all provide corresponding technical scheme to the dissolution how improving valaciclovir hydrochlordide, and inventor considers that drug-eluting affects drug effect, therefore intends the Valaciclovir hydrochloride tablet of a kind of Fast Stripping of exploitation.
Summary of the invention
In view of the deficiencies in the prior art, the present inventor is creationary by valaciclovir hydrochlordide and sodium bicarbonate salify, make use of the character of sodium bicarbonate and hydrochloric acid reaction simultaneously, appropriate sodium bicarbonate is used as effervescent materials, obtain a kind of Valaciclovir hydrochloride tablet of Fast Stripping.
In order to realize object of the present invention, inventor is studied by lot of experiments preparation prescription and technique and explores, and finally obtains following technical scheme:
A kind of Valaciclovir hydrochloride tablet, said preparation is using the aqueous solution of valaciclovir hydrochlordide and sodium bicarbonate as wetting agent, by the component (in prescription also can containing pharmaceutically acceptable adjuvants such as correctivess) comprising following weight portion by wet granulation and tabletting form:
Preferably, above-mentioned Valaciclovir hydrochloride tablet, wherein: using the aqueous solution of valaciclovir hydrochlordide and sodium bicarbonate as wetting agent, by the component of following weight portion by wet granulation and tabletting form:
Further preferably, in above-mentioned Valaciclovir hydrochloride tablet, the weight ratio of valaciclovir hydrochlordide and sodium bicarbonate is 1:0.5-0.6.
Further preferably, above-mentioned Valaciclovir hydrochloride tablet, wherein said filler be selected from microcrystalline Cellulose, lactose, mannitol, starch and pregelatinized Starch one or more.
Further preferably, above-mentioned Valaciclovir hydrochloride tablet, wherein said lubricant is one or more in magnesium stearate, micropowder silica gel and sodium stearyl fumarate.
Present invention also offers the preparation technology of above-mentioned Valaciclovir hydrochloride tablet, the Valaciclovir hydrochloride tablet of Fast Stripping can be prepared by this technique.Concrete technical scheme is as follows:
A preparation method for Valaciclovir hydrochloride tablet, the method comprises the steps: valaciclovir hydrochlordide to be dissolved in sodium bicarbonate aqueous solution, with this solution for wetting agent, filler is granulated, dry, then even with mix lubricant, tabletting.
Preferably, the preparation method of above-mentioned Valaciclovir hydrochloride tablet, wherein the weight ratio of valaciclovir hydrochlordide and sodium bicarbonate is 1:0.5-0.6.
The preparation method of Valaciclovir hydrochloride tablet of the present invention, wherein said filler be selected from microcrystalline Cellulose, lactose, mannitol, starch and pregelatinized Starch one or more; Described lubricant is one or more in magnesium stearate, micropowder silica gel and sodium stearyl fumarate.
Valaciclovir hydrochlordide is dissolved in sodium bicarbonate aqueous solution by the present inventor, then using this aqueous solution as wetting agent, pharmaceutically acceptable adjuvant is granulated, dry, tabletting.When carrying out dissolution determination, because sodium bicarbonate and valaciclovir hydrochlordide become sodium salt, therefore dissolubility is good, inventor has added a part of sodium bicarbonate in appropriate amount simultaneously, hydrochloric acid in the sodium bicarbonate of this part and gastric juice reacts rapidly, effervescent effect helps tablet fater disintegration, and therefore not only disintegrate is fast for Tablets, and stripping is also very fast.Compared with prior art, the present invention is without the need to adding disintegrating agent, and tablet can disintegrate stripping rapidly, and preparation technology is simple simultaneously, is applicable to large production requirement.
Detailed description of the invention
Following examples further describe preparation process of the present invention and beneficial effect, embodiment is only for the object of illustration, do not limit the scope of the invention, the simultaneously apparent change made according to the present invention of those of ordinary skill in the art and modification are also contained within the scope of the invention.
Embodiment 1 Valaciclovir hydrochloride tablet and preparation method thereof
Preparation method:
Recipe quantity takes valaciclovir hydrochlordide, sodium bicarbonate, joins in pure water, is stirred to dissolve, using this aqueous solution as wetting agent, joining recipe quantity crosses on the microcrystalline Cellulose of 100 mesh sieves, granulates, 60 DEG C of dryings, 18 mesh sieve granulate, dry granule is mixed homogeneously with magnesium stearate, tabletting.
Embodiment 2 Valaciclovir hydrochloride tablet and preparation method thereof
Preparation method:
Recipe quantity takes valaciclovir hydrochlordide, sodium bicarbonate, joins in pure water, is stirred to dissolve, using this aqueous solution as wetting agent, joining recipe quantity crosses on the lactose of 100 mesh sieves, granulates, 50 DEG C of dryings, 20 mesh sieve granulate, dry granule is mixed homogeneously with magnesium stearate, tabletting.
Embodiment 3 Valaciclovir hydrochloride tablet and preparation method thereof
Preparation method:
Recipe quantity takes valaciclovir hydrochlordide, sodium bicarbonate, joins in pure water, is stirred to dissolve, using this aqueous solution as wetting agent, joining recipe quantity crosses on the microcrystalline Cellulose of 100 mesh sieves, granulates, 55 DEG C of dryings, 18 mesh sieve granulate, dry granule is mixed homogeneously with magnesium stearate, tabletting.
Comparative example 1 Valaciclovir hydrochloride tablet and preparation method thereof
Preparation method:
Valaciclovir hydrochlordide, sodium bicarbonate, microcrystalline Cellulose all cross 100 mesh sieves, and recipe quantity takes rear mixing, and add pure water in right amount, 55 DEG C of dryings, 18 mesh sieve granulate, dry granule is mixed homogeneously with magnesium stearate, tabletting.
Comparative example 2 Valaciclovir hydrochloride tablet and preparation method thereof
Preparation method:
Valaciclovir hydrochlordide pulverized 100 mesh sieves, recipe quantity takes valaciclovir hydrochlordide, lactose, the microcrystalline Cellulose of half amount and low-substituted hydroxypropyl cellulose mix homogeneously, using 5% PVP K30 50% alcoholic solution as binding agent, granulate, 65 DEG C of dryings, 30 mesh sieve granulate, then mix homogeneously with the magnesium stearate of the microcrystalline Cellulose of surplus and low-substituted hydroxypropyl cellulose, proportional quantities and Aspartane, tabletting.
Comparative example 3 Valaciclovir hydrochloride tablet and preparation method thereof
Preparation method:
Recipe quantity takes valaciclovir hydrochlordide, sodium bicarbonate, joins in pure water, is stirred to dissolve, using this aqueous solution as wetting agent, joining recipe quantity crosses on the microcrystalline Cellulose of 100 mesh sieves, granulates, 55 DEG C of dryings, 18 mesh sieve granulate, dry granule is mixed homogeneously with magnesium stearate, tabletting.
The dissolution of embodiment 4 tablets of vacyclovir hydrochloride and assay
1, dissolution.The tablets of vacyclovir hydrochloride prepared of Example 1-3 and comparative example 1-3 respectively, according to dissolution method (annex XC second method), with 0.lmol/L hydrochloric acid solution 900ml for dissolution medium, rotating speed is 50 turns per minute, operates in accordance with the law, through 15 minutes time, get solution 10ml, filter, it is appropriate that precision measures subsequent filtrate, quantitatively dilutes the solution made about containing 10 μ g in every lml with 0.lmol/L hydrochloric acid solution.According to UV-VIS spectrophotometry (annex IVA), measure absorbance at the wavelength place of 254nm immediately; Separately get valaciclovir hydrochlordide reference substance appropriate, accurately weighed, also quantitatively dilute the solution made about containing 10 μ g in every lml with 0.1mol/L dissolve with hydrochloric acid solution, be measured in the same method, the stripping quantity of the every sheet of meter grate.Limit is 80% of labelled amount, should conform with the regulations.
2, assay.Measure according to high performance liquid chromatography (annex VD), chromatographic condition and system suitability octadecylsilane chemically bonded silica are filler; Methanol-water (10:90) is mobile phase; Determined wavelength is 254nm, gets valaciclovir hydrochlordide 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 note people's chromatograph of liquid, record chromatogram, the separating degree at valaciclovir hydrochlordide peak and guanine peak should meet the requirements.
Algoscopy: the tablets of vacyclovir hydrochloride that respectively prepared by Example 1-3 and comparative example 1-3 is about 50mg, accurately weighed, puts in 50ml measuring bottle, add 0.4% sodium hydroxide solution 5ml and make dissolving, be diluted with water to scale, shake up, precision measures 2ml, put in 100ml measuring bottle, be diluted with water to scale, shake up, precision measures 20 μ l, note people chromatograph of liquid, record chromatogram; Separately get valaciclovir hydrochlordide reference substance appropriate, be measured in the same method.By external standard method with calculated by peak area, to obtain final product.
The dissolution of table 1 embodiment tablets of vacyclovir hydrochloride, assay result
| Sample source | 5min dissolution (%) | 15min dissolution (%) | Content (%) |
| Embodiment 1 | 93.8 | 99.3 | 99.5 |
| Embodiment 2 | 99.1 | 99.6 | 99.8 |
| Embodiment 3 | 99.4 | 100.3 | 99.9 |
| Comparative example 1 | 37.3 | 72.9 | 99.1 |
| Comparative example 2 | 22.8 | 75.8 | 99.3 |
| Comparative example 3 | 25.9 | 76.2 | 99.4 |
It can be seen from the table, tablets of vacyclovir hydrochloride stripping prepared by embodiment of the present invention 1-3 is quick, the complete stripping of 5min; Sodium bicarbonate only mixes with valaciclovir hydrochlordide by comparative example 1, the non-salify of valaciclovir hydrochlordide, therefore stripping is slow; Comparative example 2 adopts prior art, and stripping is slow; Comparative example 3 decreases sodium bicarbonate consumption, although valaciclovir hydrochlordide and sodium bicarbonate salify, because sodium bicarbonate does not have unnecessary amount, when therefore stripping measures, can not play effervescent effect, therefore disintegration of tablet is slow, drug slow stripping.
Claims (7)
1. a Valaciclovir hydrochloride tablet, is characterized in that: using the aqueous solution of valaciclovir hydrochlordide and sodium bicarbonate as wetting agent, by the component of following weight portion by wet granulation and tabletting form:
Described filler be selected from microcrystalline Cellulose, lactose, mannitol, starch and pregelatinized Starch one or more.
2. Valaciclovir hydrochloride tablet according to claim 1, is characterized in that: the weight ratio of valaciclovir hydrochlordide and sodium bicarbonate is 1:0.5-0.6.
3. Valaciclovir hydrochloride tablet according to claim 1, is characterized in that: described lubricant is one or more in magnesium stearate, micropowder silica gel and sodium stearyl fumarate.
4. a preparation method for Valaciclovir hydrochloride tablet according to claim 1, is characterized in that comprising the steps: to be dissolved in sodium bicarbonate aqueous solution by valaciclovir hydrochlordide, with this solution for wetting agent, filler is granulated, drying, then even with mix lubricant, tabletting.
5. the preparation method of Valaciclovir hydrochloride tablet according to claim 4, is characterized in that: the weight ratio of valaciclovir hydrochlordide and sodium bicarbonate is 1:0.5-0.6.
6. the preparation method of Valaciclovir hydrochloride tablet according to claim 4, is characterized in that: described filler be selected from microcrystalline Cellulose, lactose, mannitol, starch and pregelatinized Starch one or more.
7. the preparation method of Valaciclovir hydrochloride tablet according to claim 4, is characterized in that: described lubricant is one or more in magnesium stearate, micropowder silica gel and sodium stearyl fumarate.
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Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
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| CN104188928B (en) * | 2014-09-17 | 2017-07-28 | 山东新时代药业有限公司 | A kind of Valaciclovir hydrochloride tablet and preparation method thereof |
| CN110279667B (en) * | 2019-07-30 | 2023-02-10 | 珠海润都制药股份有限公司 | Valaciclovir hydrochloride tablet and preparation method thereof |
| CN112168791B (en) * | 2020-09-23 | 2022-04-22 | 药大制药有限公司 | Valacyclovir hydrochloride liposome tablet and preparation method thereof |
| CN113274356A (en) * | 2021-05-25 | 2021-08-20 | 丽珠集团丽珠制药厂 | Valaciclovir hydrochloride granules and preparation method thereof |
| CN114621227A (en) * | 2022-02-28 | 2022-06-14 | 海南久常制药有限公司 | Valaciclovir hydrochloride, preparation 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 |
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| CN1513454A (en) * | 2003-08-19 | 2004-07-21 | 湖北丽益医药科技有限公司 | Dispersion tablet of vasilowy hydrochlaride and its prepn. method |
| CN1626089A (en) * | 2003-12-11 | 2005-06-15 | 江苏晨牌药业有限公司 | Valaciclovir oral desintegration tablet and preparation method |
| CN101002781A (en) * | 2006-01-19 | 2007-07-25 | 上海秀新臣邦医药科技有限公司 | Tablets of vacyclovir hydrochloride, and its preparing method |
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| CN102552161B (en) * | 2010-12-28 | 2016-06-22 | 上海中西制药有限公司 | The preparation method of a kind of pharmaceutical solid preparation and gained pharmaceutical solid preparation |
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Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1513454A (en) * | 2003-08-19 | 2004-07-21 | 湖北丽益医药科技有限公司 | Dispersion tablet of vasilowy hydrochlaride and its prepn. method |
| CN1626089A (en) * | 2003-12-11 | 2005-06-15 | 江苏晨牌药业有限公司 | Valaciclovir oral desintegration tablet and preparation method |
| CN101002781A (en) * | 2006-01-19 | 2007-07-25 | 上海秀新臣邦医药科技有限公司 | Tablets of vacyclovir hydrochloride, and its preparing method |
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| 盐酸伐昔洛韦泡腾片的制备与质量控制;关延彬等;《医药导报》;20051031;第24卷(第10期);第929-930页 * |
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Effective date of registration: 20151106 Address after: 211200 Lishui Economic Development Zone, Jiangsu, Nanjing No. 1 Shandong Road Applicant after: Nanjing Zhengkuan Pharmaceutical Science and Technology Co., Ltd. Address before: Lishui Economic Development Zone, Nanjing City, Jiangsu province 211200 zhe Ning Road No. 369 Applicant before: Nanjing Zhengliang Medical Technology Co.,Ltd. |
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Inventor after: Zhao Fulu Inventor after: Jia Shutian Inventor after: Ding Fei Inventor after: Shu Zhiling Inventor before: The inventor has waived the right to be mentioned |
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Effective date of registration: 20170615 Address after: No. 9 Qixia Xianlin Avenue District of Nanjing City, Jiangsu province 210023 Co-patentee after: Nanjing Hailing Chinese Medicine Pharmaceutical Technology Research Co., Ltd. Patentee after: Nanjing Hailing Pharmaceutical Co., Ltd. of Yangtze River Pharmaceutical Group Address before: 211200 Lishui Economic Development Zone, Jiangsu, Nanjing No. 1 Shandong Road Patentee before: Nanjing Zhengkuan Pharmaceutical Science and Technology Co., Ltd. |