Ibuprofen microemulsion drug delivery system

A drug delivery system and microemulsion technology, which can be used in antipyretics, drug combinations, emulsion delivery, etc., and can solve problems such as common surfactant content

Inactive Publication Date: 2015-07-29
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The ibuprofen microemulsion reported at present, its surfactant content is generally higher

Method used

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  • Ibuprofen microemulsion drug delivery system
  • Ibuprofen microemulsion drug delivery system
  • Ibuprofen microemulsion drug delivery system

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Example 1 Preparation of Microemulsion Pseudo-ternary Phase Diagram

[0022]Weigh a certain amount of surfactant and co-surfactant, and mix thoroughly with a magnetic stirrer for 1 hour to obtain the total surfactant S-Cos. At 25°C, weigh S-Cos 1.8, 1.6, 1.4, 1.2, 1.0, 0.8, 0.6, 0.4, 0.2 g into vials, then add 0.2, 0.4, 0.6, 0.8, 1.0, 1.2, 1.4 , 1.6, 1.8 g oil phase (the oil phase of a is caprylic triglyceride, the oil phase of b is triolein, the oil phase of c is caprylic triglyceride-triolein (1 :1)), mix well, slowly add distilled water dropwise to the mixture under magnetic stirring, take the appearance of "clear and transparent" as an indicator, record the amount of water added, according to the respective mass percentages of oil, total surfactant, and water at the critical point (w / w), draw a pseudo-ternary phase diagram, determine the microemulsion area, which is represented by a black area, and the results are shown in figure 1 a, 1b and 1c.

[0023] Pseudo...

Embodiment 2

[0024] Embodiment 2 The establishment of ibuprofen HPLC assay method

[0025] Chromatographic conditions: GraceSmart C18 column (250×4.6 mm, 5 μm), mobile phase methanol-pH3.0 phosphate buffer (60:40), flow rate 1 mL / min, injection volume 20 μL, detection wavelength λ = 220 nm, column temperature 35 o c.

[0026] Establishment of the standard curve: using methanol as a solvent, prepare a series of ibuprofen solutions with concentrations of 40, 20, 10, 5, 2.5, 1.2, and 0.6 μg / mL, and inject and analyze them respectively according to the predetermined chromatographic conditions. The peak area versus concentration was used as a standard curve. It can be seen that within the range of 0.6-40 μg / mL for ibuprofen, the peak area has a good linear correlation with the concentration (A=57.103C-5.6333, R 2 =0.9997).

Embodiment 3

[0027] Embodiment 3 Solubility of ibuprofen in water

[0028] Take 2 mL of distilled water in a vial, make 3 parallel portions, add an appropriate amount of ibuprofen until precipitation occurs, vortex for 3-5 min to promote the dissolution of the drug in distilled water, and seal it. put in 25 o C in a constant temperature water bath shaker, 100 rpm for 72 h. After centrifugation at 15000 rpm for 5 min, the supernatant was taken, diluted appropriately with methanol, and the drug content was determined by HPLC. The solubility of ibuprofen in water was about 0.07 mg / mL.

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Abstract

The invention provides an ibuprofen microemulsion drug delivery system which comprises a surfactant, a cosurfactant, water, oil and ibuprofen, wherein the oil is mixed oil of GTCC and glycerol trioleate, and the mass ratio of the GTCC to the glycerol trioleate is (6:1)-(1:6). The microemulsion drug delivery system is characterized by adopting the mixed oil as an oil phase. By virtue of the use of the mixed oil, the microemulsion area is remarkably expanded, the drug solubility is greatly increased, and as a result, the absolute use amount of the surfactant required for preparing the drug loading microemulsion is reduced in a double-effect manner, so that the toxic and side effects of the microemulsion caused by overhigh use amount of the surfactant are reduced; A rat pharmacokinetics result shows that the oral bioavailability of ibuprofen is remarkably improved by the optimized drug loading microemulsion containing less surfactant. Compared with other drug loading microemulsions wither higher content of surfactant, the optimized drug loading microemulsion containing less surfactant has the advantage that the influence of less use amount of the surfactant in the microemulsion on the capability of improvement of the oral bioavailability of drugs is avoided.

Description

technical field [0001] The invention relates to an ibuprofen microemulsion drug delivery system and a preparation method thereof. Background technique [0002] Candidate drugs with potential development value obtained through high-throughput screening, more than 40% of the monomers are poorly soluble in water. These monomers often suffer from premature drug development due to poor solubility-related deficiencies such as low oral bioavailability or insurmountable doses (Lipinski, C.A., Lombardo, F., Dominy, B.W., Feeney, P.J., 2001. Experimental and computational approaches to estimate solubility and permeability in drug discovery and development setting. Adv. Drug Deliv. Rev. 46(1-3), 3-26). In the field of pharmacy, many methods can improve the solubility of poorly soluble drugs, such as salt formation, changing the crystal form of drugs, using mixed solvents, co-solvents, solubilizers, forming solid dispersions, clathrates, etc. Or use new drug delivery systems such as m...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K31/192A61P29/00
Inventor 胡海燕黄辉智陈艺贞王可馨罗耀敏文慧刘丹游秀华庹珏蔡婕王亚龙
Owner SUN YAT SEN UNIV
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