Flurbiprofen liposome and preparation method thereof

A technology of flurbiprofen and profen lipid, applied in the field of flurbiprofen liposome and preparation thereof, can solve the problems of low oral bioavailability, adverse reactions in the central nervous system, low solubility in water, etc. Bioavailability, Avoidance of Toxic Side Effects, Ease of Absorption

A technology of flurbiprofen and profen lipid, applied in the field of flurbiprofen liposome and preparation thereof, can solve the problems of low oral bioavailability, adverse reactions in the central nervous system, low solubility in water, etc. Bioavailability, Avoidance of Toxic Side Effects, Ease of Absorption

CN101732255AInactive Publication Date: 2010-06-16TONGJI UNIV
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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Weigh 6.0 mg of flurbiprofen, 15.0 mg of egg yolk lecithin, 3.0 mg of cholesterol, and 3.0 mg of vitamin C, dissolve them with 6.0 g of chloroform / methanol (mass ratio 4:1), and mix them uniformly to obtain a solution. The above solution was placed in a rotary evaporator, and chloroform and methanol were distilled off under reduced pressure to obtain a lipid film. Phosphate buffer solution with a pH of 6 was added to the lipid film, rotated on a rotary evaporator in a warm bath at 20°C for 4 hours, ultrasonicated in a water bath for 5 minutes, and passed through a 0.22 μm filter membrane to prepare flurbiprofen liposomes. The above raw materials are all commercially available.

Embodiment 2

[0022] Weigh 6.0 mg of flurbiprofen, 15.0 mg of egg yolk lecithin, 30.0 mg of cholesterol, and 3.0 mg of vitamin C, dissolve them in 60 g of chloroform / methanol (mass ratio 4:1), and mix well. The above solution was placed in a rotary evaporator, and chloroform and methanol were distilled off under reduced pressure to obtain a lipid film. A phosphate buffer solution with a pH of 7 was added to a lipid film flask, rotated on a rotary evaporator in a 60° C. temperature bath for 1 h, ultrasonicated in a water bath for 30 min, and passed through a 0.45 μm filter membrane to prepare flurbiprofen liposomes.

Embodiment 3

[0024] Weigh 30.0 mg of flurbiprofen, 50.8 mg of egg yolk lecithin, 6.0 mg of cholesterol, and 6.0 mg of vitamin C, dissolve them in 6.0 g of chloroform / methanol (mass ratio 4:1), and mix well. The above solution was placed in a rotary evaporator, and chloroform and methanol were distilled off under reduced pressure to obtain a lipid film. Phosphate buffer solution with a pH of 7 was added to a lipid film flask, rotated in a 30° C. temperature bath on a rotary evaporator for 3 h, ultrasonicated in a water bath for 15 min, and passed through a 0.45 μm filter membrane to prepare flurbiprofen liposomes.

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Abstract

The invention relates to a flurbiprofen liposome and a preparation method thereof. The flurbiprofen liposome is prepared by weighting the following materials in part by weight: 1 to 10 parts of cholesterol, 5 to 40 parts of yolk lecithin, 2 to 50 parts of flurbiprofen and 1 to 10 parts of vitamin C; dissolving the materials with chloroform and methanol in a mass ratio of 4:1; uniformly mixing the materials to obtain mixed solution; putting the solution into a rotary evaporator; distilling the solution under reduced pressure for removing the chloroform and the methanol to obtain a lipid membrane; adding phosphate buffer with pH between 6 and 8 into the lipid membrane; rotating for 1 to 4 h in warm bath at the temperature of between 20 and 60 DEG C on the rotary evaporator; and carrying out water bath ultrasound for 5 to 30 min, and then filtering the mixture with a 0.22 to 0.45 mu m filter membrane to obtain the flurbiprofen liposome. The flurbiprofen liposome prepared by the invention has good stability, targeting property and slow-releasing property, can reduce administration dosage and reduce toxic and side effect of medicaments, is suitable for percutaneous administration and oral administration, and can be widely used for preparing oral liquid, aerosol, spray, and ophthalmic and external liposome administration formulations.

Description

technical field [0001] The invention relates to a flurbiprofen liposome and a preparation method thereof. It belongs to the technical field of pharmaceutical preparations. Background technique [0002] Flurbiprofen is one of the excellent varieties of non-steroidal anti-inflammatory analgesics, mainly used for the treatment of rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, traumatic pain and other pains. Flurbiprofen acts as an anti-inflammatory and analgesic by inhibiting the activity of prostaglandin synthase cyclooxygenase. The drug is effective orally and well tolerated, and long-term use neither promotes nor inhibits its own metabolism. Although flurbiprofen has unique anti-inflammatory and analgesic effects clinically, flurbiprofen is a lipophilic drug with low solubility in water, resulting in low oral bioavailability and serious gastrointestinal and central nervous system damage. Systemic adverse reactions. At present, most of the reports about flu...

Claims

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Application Information

Patent Timeline
16 Jun 2010
Publication
CN101732255A
IPC
A61K9/127; A61K31/192; A61K47/22; A61P29/00
Inventors
甘礼华; 陈柳华