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Cetirizine hydrochloride solid preparation and preparation method thereof

A technology of cetirizine hydrochloride and solid preparation, which can be applied to pharmaceutical formulations, medical preparations without active ingredients, and medical preparations containing active ingredients, etc., and can solve problems such as poor compliance, excessive substances, and inconvenience to carry.

Active Publication Date: 2016-12-07
SUNSHINE LAKE PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Because cetirizine has obvious bitter taste, the taste masking effect of traditional tablets is poor; and syrup or drops are liquid preparations, which are inconvenient to carry and easy to be infected when opening the bottle, which brings additional risks. , especially in infants and young children, the compliance of taking it is poor
In order to improve the mouthfeel, it is necessary to further add polyalcohols such as mannitol and sucrose as diluents or flavoring agents in the composition, but cetirizine has poor stability in formulations containing polyalcohol systems, and is prone to occur with polyalcohols. The esterification reaction produces undesired reaction products. In addition, the oxidation reaction of cetirizine itself can also cause related substances to exceed the standard, resulting in a reduction in product quality

Method used

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  • Cetirizine hydrochloride solid preparation and preparation method thereof
  • Cetirizine hydrochloride solid preparation and preparation method thereof
  • Cetirizine hydrochloride solid preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0051] The influence investigation of embodiment 1PH regulator on preparation stability

[0052] (1) See Table 1 for prescriptions 1-12

[0053] (2) Preparation process

[0054] 1) cetirizine hydrochloride, diluent and pH regulator are mixed homogeneously;

[0055] II) wet the mixture obtained in step I) with 40% (w / w) ethanol-water solution;

[0056] III) stirring the wetting mixture obtained in step II) to bring the pH adjuster in intimate / intimate contact with the active substance and the diluent;

[0057] IV) carry out wet sizing by a swing granulator;

[0058] v) drying the stirred wetting mixture of step IV) until the final moisture content in the suspension-modified particles as measured by loss on drying is <2.0% (w / w);

[0059] VI) Sieve the dry granules obtained in step V), and sieve out particles larger than 20 mesh and fine powders smaller than 80 mesh.

[0060] (3) Detection of related substances

[0061] Take the samples prepared from prescription 1-presc...

Embodiment 2

[0068] The investigation of the type of essence of embodiment 2 to preparation stability

[0069] (1) Prescription 13-16

[0070]

[0071] (2) Preparation process

[0072] 1) cetirizine hydrochloride, sucrose, trisodium citrate dihydrate and specific types of essence are mixed evenly;

[0073] II) wet the mixture obtained in step I) with 40% (w / w) ethanol-water solution;

[0074] III) stirring the wetting mixture obtained in step II) to bring the pH adjuster in intimate / intimate contact with the active substance and the diluent;

[0075] IV) carry out wet sizing by a swing granulator;

[0076] v) drying the stirred wetting mixture of step IV) until the final moisture content in the suspension-modified particles as measured by loss on drying is <2.0% (w / w);

[0077] VI) Sieve the dry granules obtained in step V), and sieve out particles larger than 20 mesh and fine powders smaller than 80 mesh.

[0078] (3) Detection of related substances

[0079] Table 2-2. The resu...

Embodiment 3

[0082] The influence of embodiment 3 solvent on preparation process

[0083] For prescriptions 17-22, different concentrations of ethanol and water solvents were used as wetting agents, and the influence on the preparation process was investigated. The results are shown in Table 3.

[0084] Table 3. The influence of different solvents on the preparation process

[0085]

[0086] As can be seen from Table 3, it is difficult to use water as a solvent for wet granulation, and the resistance of the granulator is large; as the proportion of ethanol in the solvent increases, the wet granulation gradually becomes smoother, and the resistance of the granulator is small, but when the proportion of ethanol reaches 80%. , wet particles are easy to stick together. Considering the overall process and cost, when the proportion of ethanol is in the range of 20%-60%, the process effect is better. When the proportion of ethanol is 40%, the wet granulation is smooth and the process effec...

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Abstract

The invention relates to a cetirizine hydrochloride solid preparation and a preparation method thereof, and belongs to the technical field of medicinal preparations. The solid preparation comprises cetirizine and a pH regulator, the pH regulator and the corresponding use amount of the pH regulator make the pH value of a solution obtained by dissolving the prepared solid preparation in water with the weight 10 times the weight of the solid preparation be 5.0-7.2, and the solid preparation meeting the above condition has good stability. The preparation method of the solid preparation has the advantages of simplicity in operation, low cost, and suitableness for industrial production.

Description

technical field [0001] The invention specifically relates to a solid preparation containing cetirizine capable of stabilizing and improving mouthfeel and a preparation method thereof, belonging to the technical field of pharmaceutical preparations. Background technique [0002] Cetirizine or levocetirizine is a selective H1 receptor antagonist, which can quickly bind to the histamine H1 receptor on the target cell membrane and block the activation of target cells by histamine. The drug is not easy to penetrate the blood-brain barrier, has a low affinity to the central H1 receptor, basically has no drowsiness effect, and has no obvious anticholinergic and anti-serotonin effects, so it has few side effects. Cetirizine is a second-generation H1 antihistamine drug, which is a long-acting, highly selective oral and potent anti-allergic substance. The drug has become the second-generation antihistamine because of its significant curative effect and less side effects. The main dru...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/46A61K31/495A61K9/16A61P37/08
Inventor 齐宜广黄芳芳游劲松
Owner SUNSHINE LAKE PHARM CO LTD
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