Indometacin and albuterol suppository, preparation method, detection method and application thereof

A technology of indomethacin and salbutamol, which is applied in the direction of suppository delivery, anti-inflammatory agents, measuring devices, etc. It can solve the problems of sedimentation stratification, influence on curative effect and safe medication, patient discomfort, etc., and achieve the effect of ensuring safety

Active Publication Date: 2013-11-20
LIVZON GROUP LIVZON PHARMA FACTORY +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Before 2002, the conventional prescription was produced with a mixture of PEG (polyethylene glycol) 400-PEG6000 as the matrix. Indomethacin and salbutamol were well dissolved and dispersed in the matrix, but PEG400-PEG6000 matrix had a strong dehydration effect and mucosal irritation, discomfort to patients when administered rectally or in the cavity, and a high incidence of side effects
In 2003, with the renewal of the document number and the completion of the national standard upgrade, the new national standard requires the use of "fatty matrix" based on mixed fatty acid glycerides as a molding agent. The existing process is mostly produced by fine powder suspension method, and the product is stable. There is a big problem with the stability. When transportation or storage encounters high temperature (such as 40 ℃), sedimentation and stratification often occur, which affects the curative effect and safe drug use.
In view of the fact that the existing mixed fatty acid glycerides cannot adapt to the production of indomethacin salbutamol suppositories, the drug and the matrix cannot form a stable and uniform system, and are prone to brittle cracks, delamination, and inhomogeneity, it is necessary to screen for new prescriptions and processes To ensure the stability and uniformity of the product, to achieve the purpose of high bioavailability, no stimulation, smooth production and stable quality

Method used

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  • Indometacin and albuterol suppository, preparation method, detection method and application thereof
  • Indometacin and albuterol suppository, preparation method, detection method and application thereof
  • Indometacin and albuterol suppository, preparation method, detection method and application thereof

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Experimental program
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Effect test

Embodiment 1

[0033] This embodiment is used to illustrate the preparation method of the indomethacin salbutamol suppository provided by the present invention.

[0034] Prepare a suppository with a specification of 1.7 g / capsule, prepare 1000 capsules and add 70 g of indomethacin, and the total weight of the matrix is ​​1630 g. According to the test, to meet the requirements of preparation melting time limit, hardness, and delamination resistance, the matrix composition is formulated as follows: (the total weight of the matrix=the weight of 1000 suppositories-medicine powder weight, i.e. 1630g)

[0035]

[0036] 1) Mix fatty acid glycerides, polyoxyethylene sorbitol beeswax derivatives, glyceryl behenate, and methylparaben according to the recipe and melt to 75°C; 2) Heat polyoxyethylene (25) stearate to 70°C, add indomethacin and albuterol to melt for later use; 3) Mix the result of step 1) and step 2), homogeneously emulsify at 2000-6000rpm for 5-20min, cool the interlayer cooling wate...

Embodiment 2

[0038] This embodiment is used to illustrate the preparation method of the indomethacin salbutamol suppository provided by the present invention.

[0039] Prepare a suppository with a specification of 1.7 g / capsule, prepare 1000 capsules and add 70 g of indomethacin, and the total weight of the matrix is ​​1630 g. According to the test, to meet the requirements of preparation melting time limit, hardness, and delamination resistance, the matrix composition is formulated as follows: (the total weight of the matrix=the weight of 1000 suppositories-medicine powder weight, i.e. 1630g)

[0040]

[0041]

[0042] 1) Mix fatty acid glycerides, polyglyceryl isostearate, glyceryl behenate, and ethyl paraben according to the prescription amount and melt to 75°C; 2) Heat polyoxyethylene (40) stearate to 70°C ℃, add indomethacin and salbutamol for later use; 3) mix the result of step 1) and step 2), homogeneously emulsify at 2000-6000rpm for 5-20min, cool the interlayer cooling wate...

Embodiment 3

[0044] This embodiment is used to illustrate the detection of the indomethacin salbutamol suppository provided by the present invention.

[0045] In the suppository prepared by the prescription process of the present invention, the main drug is uniformly dispersed, and the auxiliary materials do not affect the content determination.

[0046] 1. The quality control detection method of albuterol is as follows:

[0047]1) Liquid chromatography column: use octadecylsilane bonded silica gel as filler (4.6mm×150mm, 5μm), use phosphate buffer (take 9.77g sodium dihydrogen phosphate, add water to dissolve and dilute to 1000ml, use Phosphoric acid to adjust the pH value to 3.10±0.05)-methanol (85:15) as the mobile phase, the detection wavelength is 276nm, the number of theoretical plates should not be less than 2000 based on the calculation of the salbutamol sulfate peak, the flow rate is 1.0mL / min, and the detection wavelength is 276nm , the injection volume is 100 μl;

[0048] 2) D...

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Abstract

The invention provides an indometacin and albuterol suppository and a preparation method of the suppository; the suppository comprises effective dose of indometacin, effective dose of albuterol, a dispersing agent, emulsifier and a molding agent. The preparation method comprises the steps of dissolving the indometacin and the albuterol in the dispersing agent, then mixing with the molten molding agent and the emulsifier, and homogenizing to obtain the suppository. The suppository provided by the invention is featured with smooth production and uniform quality; and auxiliary materials do not influence content detection; wherein content detection recovery rate of the albuterol reaches 97%, and content uniformity A+1.8S is less than 10, and is superior to a requirement that content uniformity A+1.8S of a suppository is less than 25 (Department 2 of Chinese Pharmacopoeia 2005 edition, Page 75 of Appendix XE); and layering and precipitation do not appear after the suppository is subjected to a challenge test at 45 degrees centigrade for 72 hr.

Description

technical field [0001] The invention relates to an indomethacin salbutamol suppository, its preparation method, detection method and application. Background technique [0002] Indomethacin salbutamol suppository has a significant curative effect on both primary dysmenorrhea and secondary dysmenorrhea; it also has outstanding curative effect on pain caused by abortion, post-operation, and urinary stones. Before 2002, the conventional prescription was produced with a mixture of PEG (polyethylene glycol) 400-PEG6000 as the matrix. Indomethacin and salbutamol were well dissolved and dispersed in the matrix, but PEG400-PEG6000 matrix had a strong dehydration effect And mucous membrane irritation, rectal or cavity administration brings discomfort to patients, and the incidence of side effects is high. In 2003, with the renewal of the document number and the completion of the national standard upgrade, the new national standard requires the use of "fatty matrix" based on mixed fat...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/405A61K31/137A61K9/02A61P29/00A61P15/00A61P13/04G01N30/02G01N21/33
Inventor 郭国领周俊刘和平孙朗赵淑媛桑梓福
Owner LIVZON GROUP LIVZON PHARMA FACTORY
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