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Tinidazol colon target biology adhesive tablet and preparation method thereof

A technology of tinidazole colon and bioadhesion, applied in the direction of drug delivery, pharmaceutical formulations, medical preparations containing active ingredients, etc., to reduce the incidence of adverse reactions, improve the effect of treatment, and increase the effect of curative effect

Inactive Publication Date: 2009-05-06
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

And making tinidazole into colon-targeting preparation has not been reported yet.

Method used

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  • Tinidazol colon target biology adhesive tablet and preparation method thereof
  • Tinidazol colon target biology adhesive tablet and preparation method thereof
  • Tinidazol colon target biology adhesive tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Tablet prescription:

[0041] Tinidazole 200.0g

[0042] Hypromellose 60.0g

[0043] Sodium alginate 120.0g

[0044] Chitosan 20.0g

[0045] Magnesium Stearate 1.0g

[0046] Made into 1000 pieces

[0047] Coating Solution Prescription:

[0048] EudragitL 100-55: EudragitS100=1:2 60.0g

[0049] Dibutyl phthalate 6.0g

[0050] Talc powder 8.0g

[0051] Acetone 1000ml

[0052] Preparation Process:

[0053] Get the prescribed amount of tinidazole, sodium alginate, hydroxypropyl methylcellulose and chitosan, pass through an 80-mesh sieve and mix evenly, add the prescribed amount of magnesium stearate, mix evenly, and compress the tablet core. Dissolve EudragitL 100-55 and EudragitS100 in the prescribed amount of acetone solution, stir well until clear. Add the talcum powder and dibutyl phthalate in the prescribed amount into the above-mentioned acetone solution, and continue to stir for 1 hour to obtain a coating solution. The t...

Embodiment 2

[0055] Tablet prescription:

[0056] Tinidazole 200.0g

[0057] Hypromellose 60.0g

[0058]Sodium alginate 120.0g

[0059] Chitosan 20.0g

[0060] Magnesium Stearate 1.0g

[0061] Made into 1000 pieces

[0062] Coating Solution Prescription:

[0063] EudragitL 100-55: EudragitS100=1:1 60.0g

[0064] Dibutyl phthalate 6.0g

[0065] Talc powder 8.0g

[0066] Acetone 1000ml

[0067] Preparation Process:

[0068] Get the prescribed amount of tinidazole, sodium alginate, hydroxypropyl methylcellulose and chitosan, pass through an 80-mesh sieve and mix evenly, add the prescribed amount of magnesium stearate, mix evenly, and compress the tablet core. Dissolve EudragitL 100-55 and EudragitS100 in the prescribed amount of acetone solution, stir well until clear. Add the talcum powder and dibutyl phthalate in the prescribed amount into the above-mentioned acetone solution, and continue to stir for 1 hour to obtain a coating solution. The...

Embodiment 3

[0070] Tablet prescription:

[0071] Tinidazole 200.0g

[0072] Hypromellose 60.0g

[0073] Sodium Carboxymethyl Cellulose 120.0g

[0074] Chitosan 20.0g

[0075] Magnesium Stearate 1.0g

[0076] Made into 1000 pieces

[0077] Coating Solution Prescription:

[0078] EudragitL 100-55: EudragitS100=1∶2 60.0g

[0079] Dibutyl phthalate 6.0g

[0080] Talc powder 8.0g

[0081] Acetone 1000ml

[0082] Preparation Process:

[0083] Take the prescribed amount of tinidazole, sodium carboxymethylcellulose, hydroxypropyl methylcellulose and chitosan, respectively pass through an 80-mesh sieve and mix well, add the prescribed amount of magnesium stearate and mix well, and compress the tablet core . Dissolve EudragitL 100-55 and EudragitS100 in the prescribed amount of acetone solution, stir well until clear. Add the talcum powder and dibutyl phthalate in the prescribed amount into the above-mentioned acetone solution, and continue to st...

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Abstract

The invention relates to the technical field of medicament preparation and discloses the composition of a tinidazole colon-targeted bioadhesive tablet. The tinidazole colon-targeted bioadhesive tablet comprises a skeleton tablet core which contains tinidazole, an adhesive accessory and an accessory used for dilution as well as a coat layer which contains polyacrylic resin, an accessory used for plastication, an accessory used for lubricating and a menstruum. The weight percentages (100 tablets) of each component are as follows: the skeleton tablet core contains 10 to 25g of tinidazole, 12 to 20g of the adhesive accessory, 0 to 2g of the accessory used for dilution as well as 0.1g of the accessory used for lubricating; and the coat layer contains 12.0 to 30.0g of the polyacrylic resin, 1.2 to 3.0g of the accessory used for plastication, 2.0 to 4.0g of the accessory used for lubricating and 200 to 500ml of the menstruum. The composition of the tinidazole colon-targeted bioadhesive tablet prolongs the staying time of the tinidazole in the colon, enhances the full contact and absorption between the medicament and the surface of a colonic mucosa, improves the local medicament concentration and reduces the medication use time.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a tinidazole colon-targeting bioadhesive tablet and a preparation method thereof. Background technique [0002] The active ingredient of the present invention is 2-methyl-1-[2-(ethylsulfonyl)ethyl]-5-nitro-1H imidazole, whose common name is tinidazole. [0003] Tinidazole was first developed and marketed by Pfizer of the United States in the 1960s and widely used abroad. Tinidazole tablets, injections, suppositories and capsules have been included in the 2005 edition of the Chinese Pharmacopoeia. [0004] Tinidazole is a derivative of metronidazole, a commonly used anti-anaerobe and anti-protozoal drug. Tinidazole has a strong antibacterial effect on Gram-positive and negative bacteria, and is mainly used clinically for the treatment of pneumonia caused by anaerobic infection, intraperitoneal infection, skin and soft tissue infection, periodontitis, chroni...

Claims

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Application Information

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IPC IPC(8): A61K9/30A61K31/4164A61P31/04
Inventor 聂淑芳李楠潘卫三彭博关津
Owner SHENYANG PHARMA UNIVERSITY
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