CN109157519B

CN109157519B - Preparation method of ofloxacin tablets

Info

Publication number: CN109157519B
Application number: CN201810597995.2A
Authority: CN
Inventors: 刘登; 朱典成; 王路
Original assignee: Shandong Polytechnic College
Current assignee: Shandong Polytechnic College
Priority date: 2018-06-12
Filing date: 2018-06-12
Publication date: 2021-01-26
Anticipated expiration: 2038-06-12
Also published as: CN109157519A

Abstract

The invention belongs to the field of pharmaceutical preparations, and relates to a method for preparing non-sticking ofloxacin tablets aiming at the defect of sticking of ofloxacin materials. The tablet disclosed by the invention has the advantages of simple preparation method, easiness in industrialization, controllable quality, high production efficiency and the like, can be produced by adopting a conventional preparation method, does not need special equipment, and is obviously improved.

Description

Preparation method of ofloxacin tablets

Technical Field

The invention relates to the field of pharmaceutical preparations, in particular to a tablet containing ofloxacin and a preparation method thereof.

Background

Ofloxacin is a quinolone antibacterial drug, and acts on A subunit of bacterial DNA helicase to inhibit DNA synthesis and replication, so that the bacteria die. Chemical name of ofloxacin: (±) -9-fluoro-2, 3-dihydro-3-methyl-10- (4-methyl-1-piperazinyl) -7-oxo-7H-pyrido [1,2,3-de]-[1,4]Benzoxazine-6-carboxylic acid, formula: c₁₈H₂₀FN₃O₄Molecular weight: 361.38 has the chemical structural formula:

the ofloxacin molecules contain carboxyl, the carboxyl can be tightly combined with stainless steel equipment under the catalysis of moisture to cause sticking, the ofloxacin tablet has the specification of 0.1g and accounts for about 50% of the whole tablet, the sticking phenomenon is serious in the tabletting process, the problem of sticking of the ofloxacin tablet cannot be solved due to the fact that the content of the raw material of the ofloxacin is high, the effect of adding magnesium stearate serving as a lubricant is not large, the problem of sticking of the ofloxacin tablet cannot be solved due to the fact that the type of the lubricant is changed, the traditional production method is to continuously stop equipment to clean a punch, the production efficiency is low, and the product quality cannot be guaranteed.

At present, a patent about solving the sticking problem of the ofloxacin tablet is not found, and a Chinese patent (application number 20131025966.3) discloses a method for solving the sticking problem, and discloses a sticking and punching gap bridge device for a tablet press, which needs to be modified. Other methods for solving the sticking problem of oral solid preparations comprise adopting a special adhesive (CN 2014I 10735866) and treating the raw materials with a special solvent in advance (CN 105380916), and Chinese patent application No. 201410652944.7 discloses an ofloxacin dispersible tablet, which does not mention the method provided by the invention, and treats the materials from the aspect of preparation process to solve the sticking problem.

The invention aims to provide an ofloxacin tablet and a preparation method thereof, which solve the sticking problem in the preparation process, improve the product quality and improve the production efficiency.

Disclosure of Invention

Aiming at the problems, the invention provides a preparation method of an ofloxacin tablet. The ofloxacin tablet provided by the invention contains pharmaceutically acceptable filler, adhesive, disintegrant and lubricant.

Preferably, the pharmaceutical composition provided by the invention consists of ofloxacin, corn starch, sodium carboxymethyl starch, hydroxypropyl methylcellulose and magnesium stearate.

The invention prepares the non-sticking ofloxacin tablet by the following method: mixing ofloxacin raw material and adjuvant, adding adhesive, and mixing. The mixed materials are firstly dried in advance in one step. The granules treated in this step were not sticky during tabletting. The pre-dried material is then granulated in a granulator, finally dried and compressed into tablets.

The invention also provides a preparation method of the oxyfluorsaxate tablet, which comprises the following steps:

adding ofloxacin, corn starch and sodium carboxymethyl starch into a mixing device, and uniformly mixing.

Secondly, adding a water-alcohol mixed solution of hydroxypropyl methylcellulose with certain concentration into the materials obtained in the first step, and uniformly mixing.

Thirdly, the materials obtained in the second step are pre-dried by a fluidized bed, and the end point is 3 to 15 percent (preferably 5 to 8 percent) of the moisture of the materials

And fourthly, granulating the materials which are dried in advance in the third step by using a granulator.

Fifthly, drying the material obtained in the fourth step, and adding magnesium stearate.

Sixthly, tabletting.

The specific implementation content is as follows:

example (b):

prescription:

name (R)	Amount of prescription
		Ofloxacin	1000g
Corn starch	900g
		Sodium starch glycolate	70g
2.5% hydroxypropyl methylcellulose in 50% ethanol	800ml (hydroxypropyl methylcellulose: 20 g)
		Magnesium stearate	30g
Total weight of	2020g
		Amount of preparation	10000 tablets

The preparation process comprises the following steps:

adding prescription dose of ofloxacin, corn starch and sodium carboxymethyl starch into a wet granulator, mixing for 10 minutes at 70rpm, and mixing uniformly.

② adding adhesive with prescription amount, stirring at 70rpm, cutting at 1500rpm, and mixing uniformly.

And thirdly, placing the wet material obtained in the second step into fluidized bed drying equipment, controlling the air inlet temperature to be 75 ℃, setting the frequency of a fan to be 20HZ, drying for about 10 minutes, discharging, taking particles, measuring moisture, controlling the moisture to be 7%, and stopping drying the material.

Fourthly, granulating the materials obtained in the third step by using a 16-mesh sieve, and drying the granules in the fluidized bed again until the water content is 3 percent.

Fifthly, adding the magnesium stearate with the amount of the prescription into the dried material, mixing uniformly and tabletting.

Drug stability study

The ofloxacin tablet prepared by the invention has no sticking problem in the tabletting process, the content of the provided ofloxacin tablet is accelerated for 6 months, the change of related substances is not large, and the product stability is good.

Claims

1. A preparation method of tablets containing ofloxacin is characterized in that: the prescription composition of every ten thousand ofloxacin tablets is as follows: 1000g of ofloxacin, 900g of corn starch, 70g of sodium carboxymethyl starch, 20g of hydroxypropyl methylcellulose and 30g of magnesium stearate;

the preparation method of the oxyfluorsaxate tablet comprises the following steps:

adding prescription dose of ofloxacin, corn starch and sodium carboxymethyl starch into a wet granulator, mixing for 10 minutes at 70rpm, and uniformly mixing;

secondly, dissolving the hydroxypropyl methylcellulose with the prescription amount in 800ml of 50% ethanol solution, adding the solution into the mixed material obtained in the first step, stirring the mixed material at 70rpm, and uniformly mixing the mixed material by a cutter at 1500 rpm;

thirdly, placing the materials obtained in the second step into fluidized bed drying equipment, controlling the air inlet temperature to be 75 ℃ and the frequency of a fan to be 20HZ, and pre-drying the materials until the moisture content of the materials is 3% -15%;

fourthly, after the materials obtained in the third step are granulated by 16 meshes, the granules are put into a fluidized bed again for drying until the moisture content is 3 percent;

fifthly, adding the magnesium stearate with the prescription amount into the material obtained in the fourth step, mixing uniformly and tabletting.

2. The preparation method of claim 1, wherein the predrying end point is that the moisture content of the material is 5% -8%;

3. the method according to claim 1, wherein the predrying end point is a material moisture content of 7%.