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Medicament microsphere and preparation method thereof

A technology of microspheres and drugs, applied in the directions of drug combination, drug delivery, pharmaceutical formulation, etc., can solve the problem of no celecoxib sustained-release hollow microspheres and immediate-release microspheres, etc., and achieve low cost and high encapsulation efficiency. , good reproducibility

Inactive Publication Date: 2015-06-24
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] There are no relevant reports on celecoxib sustained-release hollow microspheres and immediate-release microspheres in the prior art

Method used

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  • Medicament microsphere and preparation method thereof
  • Medicament microsphere and preparation method thereof
  • Medicament microsphere and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Preparation: according to the prescription in Table 1, dissolve celecoxib and EC in 20 mL of a mixed solvent of ethyl acetate and ether (3:1) as the dispersed phase; 0.5% poloxamer-188 solution as the continuous phase; Add it into the continuous phase for emulsification under the condition of stirring, raise the temperature to 30°C, stir to remove the organic solvent, filter with suction, wash with distilled water, and dry to obtain celecoxib microspheres.

[0034] Table 1 Preparation of celecoxib microspheres with different EC viscosity formulations

[0035]

[0036] The celecoxib microspheres prepared in Example 1 were evaluated for quality, and the results are shown in Table 2:

[0037] Table 2 Effect of EC viscosity on celecoxib microspheres

[0038]

Embodiment 2

[0040] Preparation: Dissolve celecoxib, release modifier and EC in ethyl acetate and ether (10:

[0041] 1) Use 10mL of the mixed solvent as the dispersed phase; 0.5% poloxamer-188 solution as the continuous phase; add the dispersed phase to the continuous phase for emulsification under stirring conditions, raise the temperature to 30°C, stir to remove the organic solvent, suction filter, Washing with distilled water and drying to obtain celecoxib sustained-release microspheres.

[0042] Table 3 Preparation of different formulations of celecoxib microsphere release modifier

[0043]

[0044]

[0045] The celecoxib sustained-release microspheres prepared in Example 2 were evaluated for quality, and the results are shown in Table 4. Among them, the celecoxib sustained-release microspheres prepared with PPVP as the release regulator had the highest encapsulation efficiency.

[0046] Table 4 Effect of release modifiers on celecoxib microspheres

[0047]

[0048] The cel...

Embodiment 3

[0050] Dissolve EC20, CXB, and PVPP in 40 mL of a mixed solvent of ethyl acetate and ether (5:1) to make corresponding concentrations of 60 mg·mL -1 , 60mg·mL -1 and 2% solution as the dispersed phase; 0.5% poloxamer-188 solution as the continuous phase; add the dispersed phase to the continuous phase for emulsification under high-speed stirring conditions, raise the temperature to 30°C, stir to remove the organic solvent, filter and wash , dry to get celecoxib microspheres. The quality of the celecoxib microspheres prepared in Example 3 was evaluated, and the results are shown in Table 5.

[0051] Table 5 Effect of poloxamer concentration on celecoxib microspheres

[0052]

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Abstract

The invention belongs to the technical field of pharmaceutical preparations, and particularly relates to a medicament microsphere and a preparation method thereof. The medicament microsphere comprises medicinal materials, a high polymer material and a surfactant, wherein the ratio of the medicament to the high polymer material is 1:(1-3); the medicament preferably is celecoxib, ketoprofen, dipyridamole and nimodipine. The medicament microsphere is prepared by adopting an O / W emulsified solvent diffusion-volatilization method. The O / W emulsified solvent diffusion-volatilization method comprises the following steps: respectively weighing the medicinal materials, the high polymer material and a release regulator according to the prescription amount, and then adding the weighted materials to an organic solvent; ultrasonically or mechanically stirring and dissolving as a disperse phase; taking a surfactant solution as a continuous phase; warming and stirring after low-temperature emulsification under an agitation state, so as to remove an organic solvent; and then carrying out solid separation, washing by distilled water, and drying, so as to obtain the medicament microsphere. Thus, the prepared microsphere is high in encapsulation efficiency and high in yield.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a pharmaceutical microsphere and a preparation method thereof. Background technique [0002] Micro-sphere technology was applied in the field of pharmacy in the 1960s. It is a new type of slow and controlled drug release carrier. After the drug is microsphered, it can be further made into other different conventional dosage forms. One of the effective means to improve targeting. The microspheres of the drug can improve the physical state of the drug, mask the smell of the drug, reduce the side effects of the drug, improve the stability of the drug, and adjust and control the release rate of the drug. In short, the microspheres of drugs are of great significance to improving the way of drug delivery and reducing adverse drug reactions. [0003] Microspheres are a multi-unit drug delivery system, which has the following advantages: (1) The drug can...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/16A61K9/10A61K9/22A61K9/52A61K45/00A61K31/635A61K47/38A61K47/34A61K47/32A61P29/00
Inventor 朱澄云冀艳艳王思玲李三鸣徐峰王中彦代婷婷刘凤鸣包志红万书彤张雨萌姜雨萌
Owner SHENYANG PHARMA UNIVERSITY
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