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Dispersion tablet of vasilowy hydrochlaride and its prepn. method

A technology for valacyclovir hydrochloride and dispersible tablets, applied in the field of antiviral drug valacyclovir hydrochloride dispersible tablets and the preparation thereof, can solve the problems of large single dose and the like, and achieves convenient administration, low production cost and high bioavailability Effect

Active Publication Date: 2004-07-21
湖北科益药业股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Because the single dose of this product is relatively large (150-500mg), its large-volume ordinary tablet can only be swallowed, which brings inconvenience to those who have difficulty swallowing, such as children and elderly patients

Method used

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  • Dispersion tablet of vasilowy hydrochlaride and its prepn. method
  • Dispersion tablet of vasilowy hydrochlaride and its prepn. method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0014] Embodiment 1 per 1000 dosage

[0015] Valacyclovir Hydrochloride 200g

[0016] Microcrystalline Cellulose 530g

[0017] Hypromellose 40

[0018] Croscarmellose Sodium 66g (33g each inside and outside the grain)

[0019] Stevioside 40g

[0020] Polyvinylpyrrolidone (k30) 7g

[0021] Menthol 3g

[0022] Talc powder 11g

[0023] Magnesium Stearate 5g

[0024] Preparation of Valacyclovir Hydrochloride Dispersible Tablets

[0025] Take the prescribed amount of valacyclovir hydrochloride, microcrystalline cellulose, hydroxypropyl cellulose, stevioside and half the amount of croscarmellose sodium, sieve, mix well, and make polyvinylpyrrolidone into a 50 g / liter solvent Add the aqueous solution of the above mixture to make a soft material, pass through a 14-mesh sieve to granulate, dry at 50-60°C for 4 hours, add menthol, talcum powder, magnesium stearate and the remaining croscarmellose sodium, mix evenly, press Slice and serve.

Embodiment 2

[0026] Embodiment 2 per 1000 dosage

[0027] Valacyclovir Hydrochloride 500g

[0028] Microcrystalline Cellulose 200g

[0029] Starch 100g

[0030] Croscarmellose Sodium 70g

[0031] Sodium saccharin 23g

[0032] Hypromellose 2g

[0033] Talc powder 16g

[0034] Magnesium Stearate 4g

[0035] Preparation of Valacyclovir Hydrochloride Dispersible Tablets

[0036] Get the prescribed amount of valacyclovir hydrochloride, microcrystalline cellulose, starch, croscarmellose sodium, and sodium saccharin, sieve, mix evenly, make hypromellose into a 5 g / liter aqueous solution, add the above The soft material is prepared from the mixture, granulated through a 24-mesh sieve, dried at 50-60°C for 4 hours, added with talcum powder and magnesium stearate, mixed evenly, and compressed into tablets.

Embodiment 3

[0037] Embodiment 3 per 1000 dosage

[0038] Valacyclovir Hydrochloride 500g

[0039] Microcrystalline Cellulose 700g

[0040] Cross-linked polyvinylpyrrolidone 64g (added outside the grain)

[0041] Sodium saccharin 23g

[0042] Polyvinylpyrrolidone (k30) 5g

[0043] Menthol 5g

[0044] Micronized silica gel 4g

[0045] Magnesium Stearate 4g

[0046] Note: Polyvinylpyrrolidone is prepared as a 30 g / L solvent ethanol solution, and the solvent is a 50% volume ratio ethanol aqueous solution.

[0047] Preparation of Valacyclovir Hydrochloride Dispersible Tablets

[0048] Get the prescription amount of valacyclovir hydrochloride, microcrystalline cellulose, sodium saccharin, sieve, mix evenly, polyvinylpyrrolidone is made into the ethanol solution of 30 g / liter solvent with 50% ethanol by volume, add in the above-mentioned mixture to prepare The soft material is granulated through a 14-mesh sieve, dried at 50-60°C for 6 hours, added with menthol, micropowder silica gel, ma...

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Abstract

A dispersing tablet of Faxiluowei hydrochloride contains Faxiluowei hydrochloride, the starch, microcrystalline cellulose and / or calcium hydrogen phosphate, the carboxymethyl starch sodium, hydroxypropyl cellulose, polyvinyl pyrrolidone and / or carboxymethyl cellulose sodium, the polyvinyl pyrrolidone or hydroxypropylmethyl cellulose, the sodium saccharin, aspartame, or stevioside, the menthol, the magnesium stearate, and the talc powder or micropowder silica gel. Its advantages are short disintegration time, and high biologic utilization rate.

Description

technical field [0001] The invention relates to an antiviral drug valacyclovir hydrochloride dispersible tablet and a preparation method thereof. Background technique [0002] Valacyclovir hydrochloride is L-valine-2-[(6-oxo-2-amino-1,6-dihydro-9H-purin-9-yl)methoxy]ethyl ester hydrochloride . The English name is Valaciclovir Hydrochloride. [0003] Valacyclovir hydrochloride (VACV) is an antiviral drug with higher bioavailability than its parent drug aciclovir. Lowe (ACV). After ACV enters virus-infected cells, it is phosphorylated by viral thymidine kinase and cellular kinase, and the drug is finally phosphorylated into activated acyclovir triphosphate, which inhibits viral DNA polymerase and blocks viral DNA Synthetic, showing antiviral effects. The oral bioavailability of this product is 3 to 5 times that of ACV. It overcomes the disadvantage of inconvenient taking of ACV (orally, 5 times a day), and only needs to take it 2 times a day. The pharmacokinetic paramet...

Claims

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Application Information

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IPC IPC(8): A61K9/12A61K31/52A61P31/12
Inventor 樊迎春刘洁周利娟
Owner 湖北科益药业股份有限公司
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