Pazufloxacin mesilate medicinal preparation and preparation method thereof

A technology of pazufloxacin mesylate and pharmaceutical preparations, which is applied in the field of pazufloxacin mesylate pharmaceutical preparations and its preparation, and can solve the problems of common preparations such as instability, low dissolution rate, poor stability and bioavailability

Inactive Publication Date: 2012-12-05
CHENGDU JUNXIANG MEDICAL SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Pazufloxacin mesylate is easy to absorb moisture, so it is unstable when made into ordinary preparations, and it will degrade after being placed at room temperature for a certain period of time. At the same time, due to its hygroscopicity and poor fluidity, it is difficult to operate when making preparations. Therefore, Pazufloxacin mesylate preparations currently on the market only have injection preparations, and there is no oral preparation that can be taken conveniently on the market
The literature about pazufloxacin mesylate in the prior art is also mainly its injections and local preparations. For example, Chinese patent application publication CN1490010A discloses a kind of pazufloxacin mesylate injection and its preparation process, and CN1490011A discloses A kind of pazufloxacin mesylate ear drops and its preparation process etc., the literature about its oral preparation only has Chinese patent application publication CN1439373A to disclose a kind of pazufloxacin mesylate oral preparation and its preparation process, This patent application document lists almost all existing oral preparation forms, and lists almost all pharmaceutical excipients that can be used as oral preparations in the prescription of the preparation. The five examples listed in the instructions list tablets and The prescription of granule, this prescription is complicated, and the pharmaceutical excipient that contains is of a great variety, has improved the cost of preparation, and the oral preparation prescription that this document provides is only the small test sample that laboratory provides, and its stability and bioavailability are poor ( Dissolution rate is low), does not meet the requirements of the Chinese Pharmacopoeia for oral preparations, and cannot be industrialized

Method used

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  • Pazufloxacin mesilate medicinal preparation and preparation method thereof
  • Pazufloxacin mesilate medicinal preparation and preparation method thereof
  • Pazufloxacin mesilate medicinal preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Specifications: 200mg tablet (each tablet contains 200mg pazufloxacin)

[0033] prescription:

[0034]

[0035] Process: crush pazufloxacin mesylate, pass through a 100-mesh sieve, take the prescribed amount of pazufloxacin mesylate, mix evenly with the prescribed amount of sodium carboxymethyl starch and pregelatinized starch, add 8% povidone K 30 To make soft materials, pass through a 18-mesh sieve to make granules, and dry at 60°C for 30-45 minutes (hold the dry granules tightly with your hands, loosen your hands so that the granules should not stick together, and there should be no fine powder adhered to the palm or When the index finger and thumb granules are twisted, they should be crushed immediately, without dampness) and granulated, adding magnesium stearate and micro-powder silica gel, mixing well, and pressing into tablets.

Embodiment 2

[0037] Specifications: 300mg capsules (each capsule contains 300mg pazufloxacin)

[0038] prescription:

[0039]

[0040] Process:

[0041] Raw material preparation: Pazufloxacin mesylate and pregelatinized starch are sieved through an 80-mesh sieve for later use; Povidone K30 is prepared into a 10% solution with purified water for later use;

[0042] Weigh the prescription amount of pazufloxacin mesylate and pregelatinized starch, mix well, add 10% povidone K30 aqueous solution to moisten, granulate, dry at 80°C, granulate with 40 mesh, add magnesium stearate, Mix evenly, add silicon dioxide, mix evenly, and after the semi-finished product passes the inspection, fill hollow capsules, pack, and get ready.

Embodiment 3

[0044]Specifications: 100mg tablet (each tablet contains 100mg of pazufloxacin)

[0045] prescription:

[0046]

[0047] Process: crush pazufloxacin mesylate, pass through a 100-mesh sieve, take the prescribed amount of pazufloxacin mesylate, mix evenly with the prescribed amount of hydroxypropylmethylcellulose and microcrystalline cellulose MCC102, add 8% polydimensional Soft material made of ketone aqueous solution, passed through 18-mesh sieve to make granules, and dried at 70°C for 30-45 minutes (hold the dry granules tightly with hands, loosen the hands so that the granules should not stick into agglomerates, and there should be no fine powder adhered to the palm Or rub the granules with your index finger and thumb and crush them immediately, without any damp feeling) and granulate, add magnesium stearate and silicon dioxide, mix well, and press into tablets.

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PUM

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Abstract

The invention provides a pazufloxacin mesilate oral medicinal preparation which comprises the components by weight as follows: 8-15 parts of pazufloxacin mesilate, 0.7-2.0 parts of diluent 0-2.0 parts of a disintegrating agent, 0.03-0.1 parts of lubricant, 0.06-0.2 parts of glidant, 0-0.2 parts of an antisticking agent and 0.18-0.6 parts of adhesive. The preparation is simple in prescription and process, low in production cost, and high in stability and bio-availability, and completely meets the requirements of pharmacopeia. The invention provides a novel pazufloxacin oral medicinal preparation which is more safe and stable and more convenient for being taken.

Description

technical field [0001] The invention relates to a pharmaceutical preparation of pazufloxacin mesilate and a preparation method thereof, in particular to an oral preparation of pazufloxacin mesilate and a preparation method thereof. Background technique [0002] Pazufloxacin mesylate, chemical name: (S)-(-)-10-(1-amino-1-cyclopropyl)-9-fluoro-3-methyl-7-oxo-2,3- Dihydro-7H-pyrido[1,2,3-de][1,4]benzoxazine-6-carboxylic acid methanesulfonate, formula C 16 h 15 FN 2 o 4 ·CH 4 SO 3 , which belongs to the third generation quinolone anti-infective drugs, was created by Toyama Co., Ltd. and jointly developed by Toyama Chemical Industry Co., Ltd. and Mitsubishi Corporation. Its side effects are significantly lower than similar varieties. In vitro antibacterial activity showed: against G - Bacteria, antibacterial activity is greater than ofloxacin, ciprofloxacin, sparfloxacin (2 to 4 times greater than ofloxacin), on G + Bacteria, the antibacterial activity of this product is ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/5383A61P31/04
Inventor 杨方刚罗晓勇何馨唐敏
Owner CHENGDU JUNXIANG MEDICAL SCI & TECH
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