Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Prulifloxacin oral solid composition and preparation method thereof

A technology of prulifloxacin and composition, applied in the field of pharmaceutical compositions and preparation thereof, can solve the problems of unfavorable patient medication safety, slow drug dissolution rate, influence on drug absorption, etc., and achieves improved medication safety, good dissolution rate, antibacterial Broad spectrum effect

Active Publication Date: 2013-01-30
SICHUAN KELUN PHARMA CO LTD
View PDF4 Cites 1 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The preparation medicine of existing prulifloxacin has many adjuvants, which is unfavorable for the patient's medication safety; meanwhile, the drug dissolution rate is slow, which affects the absorption of the drug; therefore, it is necessary to develop the medication safety, Prulifloxacin solid oral preparation with good dissolution rate and good stability

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Prulifloxacin oral solid composition and preparation method thereof
  • Prulifloxacin oral solid composition and preparation method thereof
  • Prulifloxacin oral solid composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

experiment example 1

[0041] Experimental Example 1: Dissolution test of prulifloxacin oral solid preparation of the present invention in acid

[0042]Get 6 pieces of samples of the present invention (Example 1), according to the dissolution assay method (Chinese Pharmacopoeia 2010 edition two appendix X C second method) with 0.1mol / L hydrochloric acid solution 900ml as solvent, rotating speed is 50 revolutions per minute, operate according to law After 5 minutes, 10 minutes, 15 minutes, 20 minutes, 30 minutes, and 45 minutes, take 10ml of the solution and filter it, and add 10ml of 0.1mol / L hydrochloric acid solution at the same time, accurately measure 2ml of the filtrate, put it in a 50ml measuring bottle, add 0.1mol / L hydrochloric acid solution, diluted to the mark, shake well, according to spectrophotometry (Chinese Pharmacopoeia 2010 edition two appendix IV A), measure the absorbance at the wavelength of 274nm; in addition, accurately weigh the appropriate amount of prulifloxacin reference sub...

experiment example 2

[0047] Experimental Example 2: Dissolution test of other invented preparations of prulifloxacin in acid

[0048] The sample was prepared according to the method of the patent application No. 200610007557, and the dissolution curve was investigated by the same method as above. The experimental results are shown in Table 2.

[0049] Table 2 Dissolution of Prulifloxacin Dispersible Tablets

[0050]

[0051] According to the above data, with the time (min) as the abscissa and the dissolution rate (%) as the ordinate, draw the dissolution curve (see attached figure 2 ).

[0052] The sample was prepared according to the method of patent application No. 200410037101, and the dissolution curve was investigated by the same method as above. The experimental results are shown in Table 3.

[0053] Table 3 Dissolution study of prulifloxacin tablets

[0054]

[0055] According to the above data, with the time (min) as the abscissa and the dissolution rate (%) as the ordinate, draw...

experiment example 3

[0058] Experimental Example 3: Solubility experiments of prulifloxacin oral solid preparations in different solutions of the present invention

[0059] Get the sample of the present invention (embodiment 1), the sample prepared by the patent No. 200610007557 and 200410037101 and the prulifloxacin raw material respectively, investigate its in water, acetate buffer solution of pH4.5, 0.1mol / L hydrochloric acid aqueous solution, phosphoric acid Solubility in salt buffer (pH 6.8).

[0060] Accurately weigh the raw material and preparation sample powder containing 100mg of prulifloxacin respectively, dissolve it in 100ml of the above-mentioned different solvents, and at the same time sonicate for 20 minutes, filter, take the subsequent filtrate to measure the concentration of the prulifloxacin solution, the results are shown in Table 4.

[0061] Table 4 Solubility Comparison of Different Invention Samples and Raw Materials in Different Solutions

[0062]

[0063] Show accordin...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

The invention discloses a prulifloxacin oral solid composition and a preparation method thereof. The prulifloxacin oral solid composition is prepared from 130 to 135 parts by weight of prulifloxacin, 10 to 30 parts by weight of starch, 30 to 50 parts by weight of microcrystalline cellulose, 20 to 40 parts by weight of lactose, 0.05 to 10 parts by weight of one or more binders, 2 to 15 parts by weight of one or more disintegrants and 0.5 to 10 parts by weight of one or more lubricants. The one or more binders are selected from polyvinylpyrrolidone, lauryl sodium sulfate and polyethylene glycol mixed aqueous solutions or alcoholic solutions. The one or more disintegrants are selected from carboxymethyl starch sodium, polyvinylpolypyrrolidone and hydroxy propyl cellulose. The one or more lubricants are selected from magnesium stearate, calcium stearate and aerosil. The prulifloxacin oral solid composition can be processed into tablets, capsules or granules, has good stability, can effectively improve a dissolution rate, solves the problem that the existing prulifloxacin oral solid preparation has a slow dissolution speed, and improves bioavailability.

Description

technical field [0001] The invention relates to a pharmaceutical composition and a preparation method thereof, in particular to a prulifloxacin oral solid preparation and a preparation method thereof. Background technique [0002] Prulifloxacin (PUFX) is a fourth-generation fluoroquinolone antibacterial drug and a prodrug of the metabolically active substance UFX (codenamed NM394). Nippon Shinyaku (Co., Ltd.) was the first to develop and enter preclinical research, and then Meiji Seika (Co., Ltd.) joined in preclinical and clinical joint research; and Japan Shinyaku (Co., Ltd.) cooperated with Shiquan Chemical Co., Ltd. Carry out research on its raw materials. [0003] After oral administration, prulifloxacin is mainly absorbed by the small intestine, and 5-methyl-2-oxo-1,3-dioxole-4 at the C7 position is removed under the action of dioxygenase in the portal vein and liver - group, became NM394 (AF3013) with antibacterial activity. It has a wide antibacterial spectrum and...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
IPC IPC(8): A61K9/00A61K9/20A61K9/16A61K9/48A61K31/496A61K47/38A61P31/04
Inventor 张永红杨勇陈龙江黄燕萍王利春梁隆
Owner SICHUAN KELUN PHARMA CO LTD
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products