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Cefditoren pivoxil tablet and its preparation method

A technology of cefditoren pivoxil and tablet cores, which is applied in pharmaceutical formulations, medical preparations without active ingredients, and medical preparations containing active ingredients, etc., can solve the problems of thermodynamic instability of amorphous materials, decreased oral absorption, Dissolution instability and other problems, to achieve the effect of increased impurities, good bioavailability and high dissolution

Active Publication Date: 2013-03-06
CSPC ZHONGQI PHARM TECH (SHIJIAZHUANG) CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0012] The amorphous formulation with improved bioavailability disclosed in the above-mentioned patent application has a shortcoming: the amorphous material is thermodynamically unstable, and it is easy to change from the amorphous form to the crystalline form, becoming crystalline cefditoren pivoxil, and the dissolution rate is reduced. Decreased absorbency
The patented solid dosage form is dry granulated or directly compressed, which resists the transition from amorphous form to crystalline form, but the dissolution is not stable

Method used

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  • Cefditoren pivoxil tablet and its preparation method
  • Cefditoren pivoxil tablet and its preparation method
  • Cefditoren pivoxil tablet and its preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Embodiment 1: Amorphous cefditoren pivoxil 1

[0040] Element

Dosage

cefditoren pivoxil

40g

hypromellose

1g

0.1mol / L hydrochloric acid

800ml

0.1mol / L sodium hydroxide

Appropriate amount

[0041] making process:

[0042] Dissolve hypromellose in hydrochloric acid, below -5°C, add the prescribed amount of cefditoren pivoxil, stir to dissolve, adjust the pH of the solution to about 7 with sodium hydroxide, filter with suction, and dry in vacuum at 30°C to obtain Amorphous cefditoren pivoxil.

Embodiment 2

[0043] Embodiment 2: amorphous cefditoren pivoxil 2

[0044] Element

Dosage

cefditoren pivoxil

40g

Polyvinylpyrrolidone

1g

0.1mol / L hydrochloric acid

800ml

1mol / L ammonia water

Appropriate amount

[0045] making process:

[0046] Dissolve polyvinylpyrrolidone in hydrochloric acid, below 5°C, add the prescribed amount of cefditoren pivoxil, stir to dissolve, adjust the pH of the solution to about 7 with ammonia water, filter with suction, and dry under vacuum at 30°C to obtain amorphous cefditoren Pixyl.

Embodiment 3

[0047] Embodiment 3: Cefditoren pivoxil tablet (with D-mannitol and β-cyclodextrin as filler)

[0048] Prescription (1000 tablets, specification: 100mg)

[0049]

[0050]

[0051] Note: 130g cefditoren pivoxil is equivalent to 100g cefditoren.

[0052] Preparation Process:

[0053] Grind cefditoren pivoxil, pass through a 200-mesh sieve, dry the prescribed amount of filler and disintegrant at 80°C for 2 hours, then mix the raw and auxiliary materials, dry granulate, and then add the prescribed amount of additional cross-linking Sodium carboxymethyl cellulose and magnesium stearate, mixed evenly and pressed into tablets, tablet weight 280mg, pressure 6-10kg / cm 2 , control the water content of the tablet core to be less than or equal to 5%, then coat the tablet core, control the weight gain of the tablet core to about 3-4%, and dry to obtain the cefditoren pivoxil coated tablet.

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Abstract

The invention relates to a cefditoren pivoxil tablet. The tablet comprises a tablet core and a coating layer, wherein the tablet core contains amorphous cefditoren pivoxil, a filler, a disintegrating agent, a solubilizer and a lubricant, and the filler is a mixture of D-mannitol and beta-cyclodextrin and / or low-substituted hydroxy propyl cellulose. The cefditoren pivoxil tablet avoids the conversion of amorphous cefditoren pivoxil to crystals and has good disintegration and dissolve-out properties under four dissolve-out conditions, and the dissolve-out curve of the cefditoren pivoxil tablet is consistent with the dissolve-out curve of a listed product Meiact.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a cefditoren pivoxil tablet and a preparation method thereof. Background technique [0002] Cefditoren pivoxil is a third-generation cephalosporin antibiotic, a prodrug of cefditoren, and its chemical structure is as shown in formula 1: [0003] [0004] Cefditoren pivoxil has low toxicity and broad antibacterial spectrum, can be absorbed orally, and is used for treating and preventing diseases caused by bacterial infections (US Patent 4839350, European Patent EP175610). [0005] Crystalline cefditoren pivoxil is known to have high purity, high thermal stability and satisfactory stability even in high humidity environments (WO9812200, US Patent 6294669). However, crystalline cefditoren pivoxil has low solubility in water and is thus not suitable for oral administration. [0006] In order to improve the oral absorbability of cefditoren pivoxil, domestic and foreign ...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K9/36A61K31/546A61K47/38A61K47/40A61P31/04
Inventor 吴欢欢陈素锐白敏
Owner CSPC ZHONGQI PHARM TECH (SHIJIAZHUANG) CO LTD
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