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Brovudine medicine absorbed through oral mucosa

A technology of oral mucosa and brivudine, applied in the field of brivudine absorbed through oral mucosa, can solve problems such as low bioavailability, and achieve the effects of good therapeutic effect, fast blood flow rate and strong tolerance

Inactive Publication Date: 2021-11-30
重庆市力扬医药开发有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The only dosage form of brivudine on the market is oral tablets with a specification of 125 mg. After administration, due to the first-pass effect caused by the degradation of liver enzymes, the bioavailability is low, only 30%.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Example 1 (buccal tablet, 130~160mg / tablet)

[0031] composition:

[0032] Brovudine (crushed to D 90 =5~15µm) 130g~160g

[0033] Starch 30g

[0034] Pregelatinized starch 50g

[0035] Aspartame 2g

[0036] 5% povidone aqueous solution appropriate amount

[0037] Magnesium Stearate 2g

[0038] Made into 1000 pieces

[0039] Preparation method: carry out micronization pretreatment of brovudine to D 90 =5~15µm, after the raw materials are mixed evenly with auxiliary ingredients such as starch and pregelatinized starch, 5% povidone aqueous solution is added to granulate, the fluidized bed is dried, granulated, magnesium stearate is added, mixed evenly, and tabletted. Instantly. Dissolution test: Disintegrate and dissolve in 15 minutes to 23 minutes. When taking it, put it on the buccal area and dissolve it.

Embodiment 2

[0040] Example 2 (buccal tablet, 100mg / tablet)

[0041] composition:

[0042] Brovudine (crushed to D 90 =10~25µm) 100g

[0043] Ludipress LCE 33g

[0044] Microcrystalline Cellulose 16g

[0045] Cyclamate 5g

[0046] Sodium stearyl fumarate 2g

[0047] Made into 1000 pieces

[0048] Preparation method: carry out micronization pretreatment of brovudine to D 90 =10~25μm, after mixing with Ludipress LCE, microcrystalline cellulose and other auxiliary ingredients, add magnesium stearate, mix evenly, and directly compress the tablet. Dissolution test: Disintegrate and dissolve in 15 minutes to 20 minutes. When taking it, put it on the buccal area and dissolve it.

Embodiment 3

[0049] Example 3 (buccal tablet, 70mg / tablet)

[0050] composition:

[0051] Brovudine (crushed to D 90 =10~20µm) 70g

[0052] 35g pregelatinized starch

[0053] Starch 20g

[0054] Fructose 10g

[0055] Stearic acid 3g

[0056] Made into 1000 pieces

[0057] Preparation method: carry out micronization pretreatment of brovudine to D 90 =10~20μm, after mixing with pregelatinized starch, starch and other auxiliary ingredients, put it in a fluidized bed, granulate with purified water, dry, granulate, add stearic acid, mix evenly, and compress into tablets. Dissolution test: Disintegrate and dissolve in 13 minutes to 16 minutes. When taking it, put it on the buccal area and dissolve it.

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PUM

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Abstract

The invention provides a bromvudine medicine absorbed through oral mucosa. The bromvudine medicine is prepared from bromvudine serving as an effective medicinal component and acceptable auxiliary components in oral mucosa medicines. The medicine has no irritation to oral cavity, takes effect quickly, has high bioavailability, and ensures that patients have satisfactory compliance.

Description

technical field [0001] The present invention relates to a drug absorbed through the oral mucosa, specifically a brivudine drug that can be absorbed through the oral mucosa, including but not limited to sublingual tablets / granules / pills / film, buccal tablets / granules / pills Pharmaceutical preparations that can be completely or mainly absorbed by oral mucosa such as sublingual mucosa and / or buccal mucosa, etc. Background technique [0002] Varicella-zoster virus (VZV) infection results in two diseases with distinct clinical manifestations. Primary infection with VZV will result in varicella, which is characterized by vesicular lesions of varying stages of progression on the face, trunk, and extremities. Herpes zoster results from reactivation of endogenous latent VZV infection in sensory ganglia. This clinical pattern is characterized by a unilateral painful vesicular eruption, usually in a limited dermatomal distribution. Shingles can occur at any age, but mainly occurs in a...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K47/36A61K47/18A61K47/32A61K31/7072A61P31/22
CPCA61K9/006A61K9/2059A61K9/2027A61K9/2013A61K31/7072A61P31/22
Inventor 刘星刘杰李辽平
Owner 重庆市力扬医药开发有限公司
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