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Muscone suppository and preparation method and application thereof

A kind of muscone suppository, muscone technology, applied in the direction of suppository delivery, medical formula, non-active ingredient medical preparations, etc., can solve the problems of poor curative effect, slow onset, etc., shorten the bleeding time and coagulation time, absorb Fast, stable performance results

Inactive Publication Date: 2018-04-24
山东宏济堂制药集团股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Aiming at the problems of slow onset and poor curative effect of commonly used oral preparations, it is the technology to be solved in the present invention to develop a new dosage form of muscone that can directly act on the affected area, has a quick onset, and can avoid the first-pass effect of the liver at the same time and improve its bioavailability. question

Method used

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  • Muscone suppository and preparation method and application thereof
  • Muscone suppository and preparation method and application thereof
  • Muscone suppository and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Weigh 7.0g of PEG4000, 6.0g of PEG400 and 6.0g of distilled water, heat in a water bath (75-85°C) to melt, stir evenly, and make a water-soluble matrix. Heat 8.0g glyceryl monostearate in a water bath at 75-85°C to melt and stir evenly, add the above water-soluble matrix and mix evenly, accurately weigh 26.0mg muscone and slowly add it to the molten matrix, add 0.3g Tween- 80, add while stirring, stir well. Pour the above homogeneous mixture into the suppository mold coated with liquid paraffin, cool down to room temperature, cool at -20°C for 0.5h, take it out, cut off the overflowing part, and demould. The total number of suppositories to be prepared is 100 capsules .

Embodiment 2

[0023] Weigh 7.0g of PEG4000, 6.0g of PEG400 and 6.0g of distilled water, heat in a water bath (75-85°C) to melt, stir evenly, and make a water-soluble matrix. Heat 8.0g glyceryl monostearate in a water bath at 75-85°C to melt and stir evenly, add the above water-soluble matrix and mix evenly, accurately weigh 52.5mg muscone and slowly add it to the molten matrix, add 0.3g Tween- 80, add while stirring, stir well. Pour the above homogeneous mixture into the suppository mold coated with liquid paraffin, cool down to room temperature, cool at -20°C for 0.5h, take it out, cut off the overflowing part, and demould. The total number of suppositories to be prepared is 100 capsules .

Embodiment 3

[0025] The drug effect animal experiment result of the muscone suppository prepared by the present invention is as follows:

[0026] Experiment 1: Effects of Muscone Hemorrhoid Suppository on a Rat Hemorrhoid Acute Attack Model

[0027] 70 Wistar rats were taken to prepare a similar model of rat hemorrhoid acute attack. The method of modeling was to disinfect the perianal skin with iodophor cotton balls, and then inject 0.05ml of 75% glacial acetic acid into each rat's anal pericutaneous subcutaneously. Ulcers formed in the anus 24 hours after injection, accompanied by redness, swelling and inflammatory exudation. Refer to the four-level scoring standard for local symptoms (see Table 1), and score according to the standard. Animals with a score below 4 are excluded from the experiment, and other animals are considered successful in modeling. Animals with successful modeling were selected and weighed and randomly divided into 5 groups: model group, Mayinglong hemorrhoid suppos...

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Abstract

The invention discloses a muscone suppository and a preparation method and application thereof. The muscone suppository is prepared from distilled water, PEG 4000, PEG 400, Tween-80, glyceryl monostearate and muscone. The muscone suppository is used for treating haemorrhoids, directly acts on an affected area and takes effect quickly, the first-pass effect of the liver is avoided at the same time,and the bioavailability of the muscone suppository is improved.

Description

technical field [0001] The invention relates to the technical field of muskone medicine and its application, in particular to a muscone suppository and its preparation method and application. Background technique [0002] Hemorrhoids are soft venous masses formed by enlarged and varicose rectal vein filaments under the mucous membrane of the end of the rectum and under the skin of the anal canal. Clinically divided into internal hemorrhoids, external hemorrhoids and mixed hemorrhoids. It is a common anorectal disease. Its clinical manifestations are bleeding during defecation, rectal prolapse, swelling and pain as the main symptoms. [0003] The medicine for the treatment of hemorrhoids mostly adopts capsules and tablets for oral administration now, and the onset of effect is slow. Drugs go through the first pass of the liver, which reduces the efficacy of the drug and may cause damage to the liver. [0004] Muscone is one of the main active ingredients in musk, which ha...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/02A61K31/122A61P9/14
CPCA61K9/0034A61K9/02A61K31/122A61K47/10
Inventor 谭乐俊魏永恒李利芬张塞战旗李樱孟兆青
Owner 山东宏济堂制药集团股份有限公司
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