Entecavir dispersing tablet and preparing method

Abstract

The present invention discloses an anti-hepatitis B medicine enticavi dispersing tablet preparation and its preparation method. Said preparation adopts proper binding agent and prescription, and the invented enticavi dispersing tablet has high bioavailabity and blood concentration and good disintegration solution effect.

Description

technical field

[0001] The invention relates to an anti-hepatitis B drug entecavir, specifically, the invention relates to an entecavir dispersible tablet preparation and a preparation process thereof. Background technique

[0002] Entecavir (English name entecavir, Baraclude) is a 2′-pentanecyclodeoxyurine nucleoside analogue, which has a strong anti-hepatitis virus ability. Its chemical name is 2-amino-1,9-dihydro-9-[(1S,3R,4S)-4-hydroxy-3-(hydroxymethyl)-2-methylenecyclopentane]-6H - Purin-6-one monohydrate. The target of entecavir is HBV DNA polymerase and reverse transcriptase. By inhibiting this enzyme, it can inhibit the reverse transcription and replication of HBV DNA negative strand of pre-genomic RNA, and then inhibit the synthesis of positive strand to block the assembly and extension of HBV DNA. . After entecavir is orally absorbed into liver cells, it becomes entecavir triphosphate (ETV-TP) through phosphorylation, which is the active form of entecavir that i...

Examples

Embodiment 1

[0031] Prescription: Entecavir 0.5g

[0032] Mannitol 40g

[0033] Lactose 60g

[0034] Microcrystalline Cellulose 60g

[0035] Low-substituted hydroxypropyl cellulose (internal addition) 12.6g

[0036] Crospovidone (extra) 9g

[0037] Micronized silica gel 3.6g

[0038] Magnesium stearate 1.8g

[0039] 20% ethanol solution of hypromellose

[0040] A total of 1000 pieces were made

[0041] Preparation method: first crush the above materials through a 100-mesh sieve, fully mix entecavir, mannitol, lactose, microcrystalline cellulose, and low-substituted hydroxypropyl cellulose, and then add dilute alcohol solution of hypromellose to prepare Soft material, granulate with 20 mesh sieve, dry at 60°C for 1.5-2 hours, granulate with 18 mesh sieve, add disintegrant crospovidone, lubricant micronized silica gel, magnesium stearate, mix well, measure content, adjust tablet weight and make entecavir dispersible table...

Embodiment 2

[0043] Prescription: Entecavir 1.5g

[0044] Mannitol 35g

[0045] Lactose 70g

[0046] Microcrystalline Cellulose 55g

[0047] Low-substituted hydroxypropyl cellulose (internal addition) 14g

[0048] Crospovidone (additional) 8g

[0049] Micronized silica gel 3.7g

[0050] 40% ethanol solution of hypromellose

[0051] A total of 1000 pieces were made

[0052] Preparation method: first crush the above materials through a 100-mesh sieve, fully mix entecavir, mannitol, lactose, microcrystalline cellulose, and low-substituted hydroxypropyl cellulose, and then add hypromellose in 40% ethanol solution Make soft material, granulate with 20-mesh sieve, dry at 60°C for 1.5-2 hours, granulate with 18-mesh sieve, add disintegrating agent cross-linked povidone and lubricant micro-powder silica gel, measure the content after mixing, and adjust the tablet weight , compressed into entecavir dispersible tablets.

Embodiment 3

[0054] Prescription: Entecavir 0.5g

[0055] Xylitol 30g

[0056] 70g pregelatinized starch

[0057] Microcrystalline Cellulose 60g

[0058] Low-substituted hydroxypropyl cellulose (internal and external) 16.2g

[0059] Micronized silica gel 3.6g

[0060] Magnesium stearate 1.8g

[0061] 20% ethanol solution of hypromellose

[0062] A total of 1000 pieces were made

[0063]Preparation method: first crush the above materials through a 100-mesh sieve, fully mix entecavir, xylitol, pregelatinized starch, microcrystalline cellulose, and low-substituted hydroxypropyl cellulose, and then add hypromellose Soft material made from 20% ethanol solution, granulated with a 20-mesh sieve, dried at 60°C for 1.5-2 hours, granulated with a 18-mesh sieve, and disintegrating agent low-substituted hydroxypropyl cellulose and lubricant micro-powdered silica gel, stearic acid added Magnesium, measure the content after mixing, a...

technical field

[0001] The invention relates to an anti-hepatitis B drug entecavir, specifically, the invention relates to an entecavir dispersible tablet preparation and a preparation process thereof. Background technique

[0002] Entecavir (English name entecavir, Baraclude) is a 2′-pentanecyclodeoxyurine nucleoside analogue, which has a strong anti-hepatitis virus ability. Its chemical name is 2-amino-1,9-dihydro-9-[(1S,3R,4S)-4-hydroxy-3-(hydroxymethyl)-2-methylenecyclopentane]-6H - Purin-6-one monohydrate. The target of entecavir is HBV DNA polymerase and reverse transcriptase. By inhibiting this enzyme, it can inhibit the reverse transcription and replication of HBV DNA negative strand of pre-genomic RNA, and then inhibit the synthesis of positive strand to block the assembly and extension of HBV DNA. . After entecavir is orally absorbed into liver cells, it becomes entecavir triphosphate (ETV-TP) through phosphorylation, which is the active form of entecavir that i...

Examples

Embodiment 1

[0031] Prescription: Entecavir 0.5g

[0032] Mannitol 40g

[0033] Lactose 60g

[0034] Microcrystalline Cellulose 60g

[0035] Low-substituted hydroxypropyl cellulose (internal addition) 12.6g

[0036] Crospovidone (extra) 9g

[0037] Micronized silica gel 3.6g

[0038] Magnesium stearate 1.8g

[0039] 20% ethanol solution of hypromellose

[0040] A total of 1000 pieces were made

[0041] Preparation method: first crush the above materials through a 100-mesh sieve, fully mix entecavir, mannitol, lactose, microcrystalline cellulose, and low-substituted hydroxypropyl cellulose, and then add dilute alcohol solution of hypromellose to prepare Soft material, granulate with 20 mesh sieve, dry at 60°C for 1.5-2 hours, granulate with 18 mesh sieve, add disintegrant crospovidone, lubricant micronized silica gel, magnesium stearate, mix well, measure content, adjust tablet weight and make entecavir dispersible table...

Embodiment 2

[0043] Prescription: Entecavir 1.5g

[0044] Mannitol 35g

[0045] Lactose 70g

[0046] Microcrystalline Cellulose 55g

[0047] Low-substituted hydroxypropyl cellulose (internal addition) 14g

[0048] Crospovidone (additional) 8g

[0049] Micronized silica gel 3.7g

[0050] 40% ethanol solution of hypromellose

[0051] A total of 1000 pieces were made

[0052] Preparation method: first crush the above materials through a 100-mesh sieve, fully mix entecavir, mannitol, lactose, microcrystalline cellulose, and low-substituted hydroxypropyl cellulose, and then add hypromellose in 40% ethanol solution Make soft material, granulate with 20-mesh sieve, dry at 60°C for 1.5-2 hours, granulate with 18-mesh sieve, add disintegrating agent cross-linked povidone and lubricant micro-powder silica gel, measure the content after mixing, and adjust the tablet weight , compressed into entecavir dispersible tablets.

Embodiment 3

[0054] Prescription: Entecavir 0.5g

[0055] Xylitol 30g

[0056] 70g pregelatinized starch

[0057] Microcrystalline Cellulose 60g

[0058] Low-substituted hydroxypropyl cellulose (internal and external) 16.2g

[0059] Micronized silica gel 3.6g

[0060] Magnesium stearate 1.8g

[0061] 20% ethanol solution of hypromellose

[0062] A total of 1000 pieces were made

[0063]Preparation method: first crush the above materials through a 100-mesh sieve, fully mix entecavir, xylitol, pregelatinized starch, microcrystalline cellulose, and low-substituted hydroxypropyl cellulose, and then add hypromellose Soft material made from 20% ethanol solution, granulated with a 20-mesh sieve, dried at 60°C for 1.5-2 hours, granulated with a 18-mesh sieve, and disintegrating agent low-substituted hydroxypropyl cellulose and lubricant micro-powdered silica gel, stearic acid added Magnesium, measure the content after mixing, a...

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