Preparation method of carbinoxamine maleate sustained-release suspension

A slow-release suspension and slow-release technology, which is applied in the fields of pharmaceutical formulations, digestive system, respiratory system diseases, etc., can solve problems such as low production capacity and technical difficulties, achieve convenient operation, prolong the preparation cycle, and stabilize blood drug concentration Effect

Inactive Publication Date: 2017-07-04
JIANGSU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The cyclohexane coating system also has the problem of low production capacity
[0006] Although the sustained-release suspension has more advantages relative to the common sustained-release preparation and has obtained the great attention of pharmacists and clinicians, it is very important for those skilled in the art to prepare the carbinoxamine maleate sustained-release suspension in batches. technically difficult

Method used

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  • Preparation method of carbinoxamine maleate sustained-release suspension
  • Preparation method of carbinoxamine maleate sustained-release suspension

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] Embodiment 1: the preparation process of carbinoxamine maleate sustained-release suspension

[0047] (1) Preparation of drug resin:

[0048] Dissolve 10 g of carbinoxamine maleate in 1 L of deionized water, stir on a magnetic stirrer at 1000 rpm, add 20 g of Amberlite ® IRP69, regular sampling, determination of the concentration of the drug in the solution. When the drug concentration no longer decreases with time, the equilibrium is reached, and the unbound drug on the surface of the resin is washed away with deionized water, and dried at 60° C. for 2 hours to obtain the carbinoxamine maleate drug-loaded resin.

[0049] (2) Impregnation of drug resin:

[0050] Take 30g of carbinoxamine maleate drug-loaded resin, add it to 1L of 10% PEG4000 aqueous solution, stir for 1 hour, dry at 60° C. for 0.5 hour, and pass through a 100-mesh sieve to obtain impregnated carbinoxamine maleate drug resin.

[0051] (3) Preparation of drug resin microcapsules:

[0052] ① Preparation ...

Embodiment 2

[0066] Embodiment 2: the preparation process of carbinoxamine maleate sustained-release suspension

[0067] (1) Preparation of drug resin:

[0068] Dissolve 10 g of carbinoxamine maleate in 1 L of deionized water, stir on a magnetic stirrer at 1000 rpm, add 20 g of Amberlite ® IRP88, regular sampling, determination of the concentration of the drug in the solution. Equilibrium was reached when the drug concentration no longer decreased with time, and the unbound drug on the surface of the resin was washed away with deionized water, and dried at 40° C. for 2 hours to obtain the carbinoxamine maleate drug-loaded resin.

[0069] (2) Impregnation of drug resin

[0070] Get 30g carbinoxamine maleate drug-loaded resin, join in the aqueous solution of 1L 30% glycerin, stir 1 hour, 60 ℃ dry 0.5 hour, pass through 100 mesh sieves to obtain the carbinoxamine maleate drug resin impregnated.

[0071] (4) Preparation of drug resin microcapsules

[0072] ① Preparation of dispersed phase...

Embodiment 3

[0086] Embodiment 3: the preparation process of carbinoxamine maleate sustained-release suspension

[0087] (1) Preparation of drug resin

[0088] Dissolve 10 g of carbinoxamine maleate in 1 L of deionized water, stir on a magnetic stirrer at 1000 rpm, add 20 g of Amberlite ® IRP69, regular sampling, determination of the concentration of the drug in the solution. When the drug concentration no longer decreases with time, the equilibrium is reached, and the unbound drug on the surface of the resin is washed away with deionized water, and dried at 50° C. for 2 hours to obtain the carbinoxamine maleate drug-loaded resin.

[0089] (2) Impregnation of drug resin

[0090] Take 30g of carbinoxamine maleate drug-loaded resin, add it to 1L of 20% PEG4000 aqueous solution, stir for 1 hour, dry at 60° C. for 0.5 hour, and pass through a 100-mesh sieve to obtain impregnated carbinoxamine maleate drug resin.

[0091] (5) Preparation of drug resin microcapsules

[0092] ① Preparation o...

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Abstract

The invention relates to a preparation method of a carbinoxamine maleate sustained-release suspension, and belongs to the technical field of drug preparation; two techniques of ion exchange and reaction kettle emulsion solvent volatilization drying coating are creatively simultaneously used for controlling drug release, and the carbinoxamine maleate sustained-release suspension which can be sustained-released is obtained, so that the carbinoxamine maleate in-vivo blood drug concentration is more smooth and steady, and the drug effect is more lasting; compared with conventional suspension preparation technologies, the technology greatly reduces the production cost while ensuring the production capacity, moreover, the whole operation process can be operated in a reaction kettle, the utilization rate of equipment is effectively improved, and at the same time, the reaction kettle parameters are convenient to control and are not influenced by external conditions basically.

Description

technical field [0001] The invention relates to a preparation method of carbinoxamine maleate sustained-release suspension, belonging to the technical field of medicine preparation. Background technique [0002] Carbinoxamine Maleate (CAM) is a mild sedative antihistamine drug, which is clinically used to treat seasonal and perennial allergic rhinitis in children. In addition to treating allergic rhinitis, it also has a significant effect on irritating cough, nausea, vomiting, vertigo and even motion sickness. CAM does not inhibit the release of histamine, but competes with histamine for H in the human uterus, gastrointestinal tract, trachea, and bronchial muscles. 1 The binding site of the receptor, so as to achieve the purpose of antagonizing histamine. The appearance of CAM is white crystalline powder, without irritating smell. Relative molecular weight is 406.84, melting point is 116~121°C, easily soluble in water, artificial gastric juice, pH6.8 phosphate buffer, CAM...

Claims

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Application Information

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IPC IPC(8): A61K9/10A61K31/4422A61K47/26A61K9/50A61P11/02A61P37/08A61P11/14A61P1/08A61P25/20
CPCA61K31/4422A61K9/0002A61K9/10A61K9/5026A61K9/5047A61K47/26
Inventor 刘宏飞刘丹陈成朱飞琴
Owner JIANGSU UNIV
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