Meptazinol hydrochloride nasal spray and preparation method thereof

A technology of meptanol hydrochloride and meptanol, which is applied in the field of medicine, can solve the problems of poor patient compliance, unsuitable self-medication, difficult analgesic effect, etc., and achieves high drug bioavailability and clinical application. Good outlook, avoiding pain and inconvenience

Active Publication Date: 2017-10-20
YANGTZE RIVER PHARM GRP SICHUAN HAIRONG PHARM CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Similar to most narcotic analgesics containing phenolic hydroxyl groups, meprotamol has a severe first-pass effect in the liver, and its oral bioavailability is only 86.9%. The oral therapeutic dose is large. Although oral administration is convenient to use, the onset of action is often slow , and the bioavailability is low, it is difficult

Method used

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  • Meptazinol hydrochloride nasal spray and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Example Embodiment

[0023] Example 1 Prescription of meptafol hydrochloride nasal spray (calculated in 1000)

[0024] prescription

[0025] Preparation:

[0026] (1) Liquid preparation: at room temperature, 800ml of water for injection is filled with nitrogen until the dissolved oxygen content of the solution is 3%, then 250g of mestatol hydrochloride (calculated as mestatol) is added, stirred, and after dissolving, add 0.25g Acetic acid, stir, mix, add 10g of chitosan, stir, dissolve, add 6g of sodium acetate, stir, dissolve, add water to the full amount, stir and mix;

[0027] (2) Sterilization filtration: use 0.22μm+0.22μm modified PVDF membrane in series to sterilize and filter;

[0028] (3) Nitrogen-filled filling: 2ml / piece is filled in a quantitative spray bottle.

Example Embodiment

[0029] Example 2 Prescription of meptafol hydrochloride nasal spray (calculated in 1000)

[0030] prescription

[0031] Preparation:

[0032] (1) Liquid preparation: at room temperature, 800ml of water for injection, when filled with nitrogen until the dissolved oxygen in the solution is 4%, add 250g of meptafrol hydrochloride (calculated as meptafol), stir, and after dissolving, add 0.5g Acetic acid, stir, mix, add 12g of chitosan, stir, dissolve, add 5g of sodium acetate, stir, dissolve, add water to the full amount, stir and mix;

[0033] (2) Sterilization filtration: use 0.22μm+0.22μm modified PVDF membrane in series to sterilize and filter;

[0034] (3) Nitrogen-filled filling: 2ml / piece is filled in a quantitative spray bottle.

Example Embodiment

[0035] Example 3 Prescription of meptafol hydrochloride nasal spray (calculated in 1000)

[0036] prescription

[0037] Preparation:

[0038] (1) Liquid preparation: at room temperature, 800ml water for injection, when filled with nitrogen until the dissolved oxygen content of the solution is 3%, add 250g of mepratafol hydrochloride (calculated as mepratafol), stir, after dissolving, add 0.8g Acetic acid, stir, mix, add 14g of chitosan, stir, dissolve, add 4g of sodium acetate, stir, dissolve, add water to the full amount, stir and mix;

[0039] (2) Sterilization filtration: use 0.22μm+0.22μm modified PVDF membrane in series to sterilize and filter;

[0040] (3) Nitrogen-filled filling: 2ml / piece is filled in a quantitative spray bottle.

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PUM

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Abstract

The invention discloses meptazinol hydrochloride nasal spray and a preparation method thereof. Each 2000ml of the nasal spray comprises, 200-300g of meptazinol hydrochloride by the weight of meptazinol, 5-30g of chitosan, 0.15-5g of acetic acid, 2-9g of sodium acetate and the balance water for injection. The meptazinol hydrochloride nasal spray has the advantages that the problem that existing orally-taken meptazinol hydrochloride capsules are low in bioavailability, and pain and inconvenience brought by the use of injection to patients are avoided.

Description

technical field [0001] The invention relates to a mabutaol hydrochloride nasal spray and a preparation method thereof, belonging to the field of medicine. Background technique [0002] Meprotamol hydrochloride is a new type of narcotic analgesic, and it is one of the six agonist-antagonist analgesics recommended in many countries. Its chemical structure is similar to that of morphine. Antagonist, clinically used for short-term treatment of moderate or severe pain, such as rheumatoid arthritis, trauma, musculoskeletal pain, postoperative pain, gynecological dysmenorrhea, obstetric pain and renal colic, etc. Most of the analgesics currently used clinically are accompanied by addiction. In contrast, mebutaol has less side effects, no addiction, and milder adverse reactions, especially respiratory depression, constipation, and miosis. Ideal substitutes such as pethidine and tramadol are non-controlled analgesics with very good industrialization market prospects. [0003] Simil...

Claims

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Application Information

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IPC IPC(8): A61K9/12A61K47/36A61K31/55A61P25/04
CPCA61K9/0043A61K9/12A61K31/55A61K47/36
Inventor 邓凤英余永秀李元波周芯宇余静波
Owner YANGTZE RIVER PHARM GRP SICHUAN HAIRONG PHARM CO LTD
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