Paracetamol temperature sensitive gel and preparation method and application thereof

A paracetamol and temperature-sensitive gel technology, applied in the field of pharmaceutical preparations, can solve the problems of no bioadhesion, reduced drug efficacy, adverse consequences, etc., and achieve the effects of avoiding first-pass effect, high bioavailability, and simple production process

Inactive Publication Date: 2010-05-12
LOGISTICS UNIV OF CAPF
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Nevertheless, its use is still subject to certain restrictions, such as tablets are not conducive to swallowing by the elderly, oral preparations have certain irritation to the gastrointestinal tract, and injections are inconvenient to use; in addition, pediatric medication also has great particularity, and its compliance Very poor, if only oral preparations are used, a little carelessness will easily lead to children being choked or the medicine being spit out, which not only fails to achieve the purpose of treatment, but sometimes even backfires, leading to other adverse consequences
Therefore, rectal administration has attracted attention, but the only paracetamol suppository for children currently on the market is semi-solid, which will produce an obvious foreign body sensation when used, softens after use and has no bioadhesive effect, and the suppository may go up to the top of the rectum or from Rectal outflow causes leakage, so the first-pass effect reduces the efficacy of the drug; in addition, the dosage of ordinary suppositories is fixed, and the dosage cannot be adjusted in children, so the use is limited
Although the enema preparation overcomes these problems to a certain extent, there is the problem of easy leakage

Method used

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  • Paracetamol temperature sensitive gel and preparation method and application thereof
  • Paracetamol temperature sensitive gel and preparation method and application thereof
  • Paracetamol temperature sensitive gel and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Example 1: Pass paracetamol through a 200-mesh sieve, mix it with Poloxamer 188 and a viscosity modifier, add it to PBS 6.8 buffer to form a uniform solution, add Poloxamer 407 solid particles, make up the water phase to the full amount, and stir Place at 0-4°C until a uniform solution without bubbles is formed.

Embodiment 2

[0032] Example 2: Pass paracetamol through a 200-mesh sieve, mix it with Poloxamer 188, and dissolve it in PBS 6.8 buffer solution. After it is completely swollen, stir and mix evenly, and then add the pre-prepared Poloxamer 407 gel under stirring For the stock solution, make up the water phase to the full amount, stir and place at 0-4°C until a uniform solution without bubbles is formed.

[0033] Table 1

[0034]

[0035] Embodiment 3~10 add the paracetamol thermosensitive gel of regulator

[0036] The phase transition temperature measurement method is the same as in Examples 1-2.

[0037] The preparation method is the same as in Example 2.

[0038] Table 2

[0039]

[0040] Examples 12-19 Paracetamol Thermosensitive Gel Added Other Components

[0041] The phase transition temperature measurement method is the same as in Examples 1-3. The preparation method is the same as in Example 3.

[0042] table 3

[0043]

[0044] Examples 20-27 Paracetamol temperature-s...

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PUM

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Abstract

The invention relates to a paracetamol temperature sensitive gel and a preparation method thereof. The preparation is prepared by paracetamol, poloxamer solution and preservative and the like. The preparation of the thermosensitive gel is sensitive to the temperature, is flowable liquid at normal temperature, has reversible phase change closing to 33-37 DEG C of body temperature to form gel to directly act on administration position, thus not only being capable of being used for local administration, but also giving play to the function of treating the whole body through mucous membrane absorption; in addition, the preparation can conveniently and effectively be applied to body cavity mucous membranes and skin surfaces such as oral cavity, nasal cavity, rectum and vagina and the like, thus having antipyretic and analgesic functions. As the use dosage can be conveniently adjusted according to the needs of the patients, the preparation is suitable for bringing down a fever of infants rapidly, thus avoiding the problems of inconvenient administration by using the common formulations, such as paracetamol tabella and paracetamol turunda and difficult adjusting of dosage according to the needs of the patients.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a paracetamol temperature-sensitive gel and a preparation method and application of the gel. Background technique [0002] Paracetamol, also known as acetaminophen, belongs to aniline derivatives. By inhibiting the synthesis of prostaglandins in the central nervous system, it produces antipyretic and analgesic effects, and has no obvious effect on COX in peripheral tissues. Its antipyretic and analgesic effects are similar to aspirin, but have no obvious anti-inflammatory effects. Oral administration is easy to absorb, and the blood concentration reaches the peak within 0.5-1 hour. In the body, 95% is combined with glucuronic acid or sulfuric acid to be inactivated, and 5% is converted into metabolites toxic to the liver by the liver and excreted from the urine. This drug is an over-the-counter drug, mainly used for antipyretic and analgesic. Short-term use has mild adve...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K31/167A61K47/34A61P29/00A61K47/10
Inventor 张莉王晓辉袁园刘晓辉王雪超仲博胡霞陈莉申去非
Owner LOGISTICS UNIV OF CAPF
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