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Solution agent of antiallergi medicine contg. levocetirizine

A levocetirizine, anti-allergic technology, applied in the field of anti-allergic pharmaceutical compositions, can solve the problems of molecular aggregation, difficult patient acceptance, poor taste of solution preparations, etc., and achieves the effect of comfortable and easy to accept taste

Inactive Publication Date: 2003-05-21
CHONGQING HUAPONT PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Levocetirizine is prone to chemical degradation in water, which will reduce the curative effect and increase toxic and side effects, and molecular aggregation may occur, making the solution turbid
Levocetirizine has stronger bitter taste in addition, and the mouthfeel of solution preparation is poor, is difficult to accept for the patient

Method used

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Examples

Experimental program
Comparison scheme
Effect test

specific Embodiment approach ： Embodiment 1

[0016] The specific embodiment: embodiment 1 levocetirizine hydrochloride oral solution

[0017] formula:

[0018] Levocetirizine Hydrochloride 0.5g

[0019] Sorbitol 250g

[0020] Macrogol 400 150ml

[0021] Polyvinylpyrrolidone 25g

[0022] Poloxamer (model F68) 10g

[0023] Propionic acid 1ml

[0024] Sodium saccharin 0.1g

[0025] Strawberry essence 1ml

[0026] Citric acid - sodium citrate amount

[0027] Distilled water up to 1000ml

[0028] Preparation: Weigh (or measure) the raw and auxiliary materials according to the formula, take an appropriate amount of distilled water, heat slightly and stir to dissolve, use citric acid-sodium citrate buffer (take 30g of citric acid, add 200ml of water, adjust the pH with sodium hydroxide 5.5±0.2, set aside.) Adjust the pH value to 4.5-6.5, add distilled water to dilute to the full amount, filter with a 0.45 μm microporous membrane, fill, stopper, cap, and sterilize (ASM water bath sterilization, 115.5°C, 30min), you can...

Embodiment 2

[0028] Preparation: Weigh (or measure) the raw and auxiliary materials according to the formula, take an appropriate amount of distilled water, heat slightly and stir to dissolve, use citric acid-sodium citrate buffer (take 30g of citric acid, add 200ml of water, adjust the pH with sodium hydroxide 5.5±0.2, set aside.) Adjust the pH value to 4.5-6.5, add distilled water to dilute to the full amount, filter with a 0.45 μm microporous membrane, fill, stopper, cap, and sterilize (ASM water bath sterilization, 115.5°C, 30min), you can. Embodiment 2 levocetirizine hydrochloride oral solution

[0029] formula:

[0030] Levocetirizine hydrochloride lg

[0031] Propylene glycol 100ml

[0032] Sorbitol 250g

[0033] Macrogol 400 100ml

[0034] Polyvinylpyrrolidone 20g

[0035] Poloxamer 5g

[0036] Sorbic acid 2g

[0037] Sodium saccharin 0.1g

[0038] Strawberry essence 1ml

[0039] Citric acid - sodium citrate amount

[0040] Distilled water up to 1000ml

[0041] Preparat...

Embodiment 3

[0041] Preparation: Weigh (or measure) the raw and auxiliary materials according to the formula, take an appropriate amount of distilled water, heat slightly and stir to dissolve, use citric acid-sodium citrate buffer (take 30g of citric acid, add 200ml of water, adjust the pH with sodium hydroxide 5.5±0.2, set aside.) Adjust the pH value to 4.5-6.5, add distilled water to dilute to the full amount, filter with a 0.45 μm microporous membrane, fill, stopper, cap, and sterilize (ASM water bath sterilization, 115.5°C, 30min), you can. Embodiment 3 levocetirizine hydrochloride oral solution

[0042] formula:

[0043] Levocetirizine Hydrochloride 0.5g

[0044] Sorbitol 180g

[0045] Macrogol 400 10ml

[0046] Polyvinylpyrrolidone 100g

[0047] Poloxamer (model F68) 5g

[0048] Sorbic acid 2g

[0049] Sodium saccharin 0.2g

[0050] Apple flavor 1ml

[0051] Citric acid - sodium citrate amount

[0052] Distilled water up to 1000ml

[0053] Preparation: Weigh (or measure) t...

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PUM

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Abstract

The present invention provides an antianaphylactic medicine solution preparation containing Levocetirizine. In 1000 ml of medicine composite solution 0.5-20g of zocetirizine or its pharmacal acceptable salt, 20-100 g of polyvinyl pyrrolidone, 5-50g of poloxamer and 10-250g of polyethylene glycol 400 are contained.

Description

Technical field: [0001] The invention relates to an antiallergic pharmaceutical composition containing levocetirizine, especially a solution suitable for oral administration and drop administration. Background technique: [0002] European patent EP058146 clarified that the chemical name of cetirizine is: 4-(diphenylmethyl) piperazino alkoxy acetic acid derivative, which has anti-allergic and antispasmodic effects. Levocetirizine is the R-isomer of cetirizine. [0003] Levocetirizine hydrochloride was listed in Germany for the first time, and then in the UK. It is clinically used to treat various allergic diseases caused by histamine, such as: allergic rhinitis, urticaria, hay fever, drug eruption, etc. WO9406429 and US5698558 disclose levocetirizine tablet and capsule formulations. [0004] Levocetirizine is prone to chemical degradation in water, which will reduce the curative effect and increase toxic and side effects, and molecular aggregation may occur, making the solu...

Claims

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Application Information

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IPC IPC(8): A61K31/495A61P37/08
Inventor 魏向阳毛启良王永军张颖刘阔
Owner CHONGQING HUAPONT PHARMA
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