Preparation method of timolol maleate sustained release microspheres

A technology of timolol maleate and microspheres, which is applied in the field of medicine, can solve the problems of decreased drug encapsulation rate, long time consumption, and low yield, and achieve the effect of reducing discomfort in the eye and reducing the number of medications

Active Publication Date: 2014-04-23
广州铂思雅生物医药科技有限公司
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  • Abstract
  • Description
  • Claims
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Problems solved by technology

[0005] The method of preparing microspheres can be divided into single emulsion (O/W type, W/O type, O/O type)-drying method in liquid and There are two types of double emulsion (W/O/W type and O/W/O type)-in-liquid drying method: (1) Single emulsion (O/W)-in-liquid drying method is a common method for hydrophobic drug microspheres , the disadvantage of this method is that the surface of the prepared microspheres is often embedded with drug crystals. In addition, this method is not suitable for encapsulating more water-soluble drugs, because the drugs are easily distributed from the oil-water interface during the process of emulsification and in-liquid drying. The encapsulation efficienc...

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  • Preparation method of timolol maleate sustained release microspheres
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  • Preparation method of timolol maleate sustained release microspheres

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preparation example Construction

[0026] The preparation method of timolol maleate sustained-release microspheres comprises the following steps:

[0027] 5) Disperse timolol maleate, acrylic resin, Tween, plasticizer, and montmorillonite in an organic solvent, so that the concentration of acrylic resin is 30-100g / L, and the concentration of Tween is 20-60g / L. L, the concentration of the plasticizer is 5-20g / L to obtain the inner phase;

[0028] 6) Dissolve Span in vegetable oil so that the concentration of Span is 10-40g / L to obtain the external phase;

[0029] 7) Under stirring, drop the inner phase into the outer phase to form an oil-in-oil emulsion;

[0030] 8) After the emulsion is ultrasonically treated for 5-30 minutes, the inner phase is evaporated under electromagnetic stirring, washed and dried to obtain sustained-release microspheres.

[0031] The emulsifying agent is very important to the stability of the oil-in-oil emulsion, and the emulsifying agent of the present invention is preferably cheap a...

Embodiment 1

[0036] 1) Accurately weigh 30 mg of timolol maleate, 20 mg of sodium montmorillonite, 50 mg of TEC, 50 mg of glycerin, 400 mg of acrylic resin (RSPO: RLPO mass ratio = 2:1), 124 mg of Tween 80, and add 5 ml of acetonitrile , stir to disperse and mix to obtain the inner phase.

[0037] 2) Dissolve 248mg of Span 80 in 10ml of vegetable oil to obtain the external phase.

[0038] 3) At a stirring speed of 600rpm, add 0.3g of the inner phase into 5g of the outer phase dropwise, and disperse evenly to obtain an oil-in-oil emulsion.

[0039] 4) First place the emulsion in an ultrasonic cell disintegrator for 10 minutes of sonication, then evaporate the inner phase with electromagnetic stirring in an ice bath, wash with n-hexane, and dry at room temperature.

Embodiment 2

[0041] 1) Place 500 mg of sodium montmorillonite in 5v / v% sulfuric acid, activate it at 90°C for 2 hours, wash until neutral, and dry to obtain modified montmorillonite.

[0042] 2) Accurately weigh 30mg of timolol maleate, 20mg of modified montmorillonite, 50mg of TEC, 50mg of glycerin, 400mg of acrylic resin (RSPO: RLPO mass ratio = 2:1), 124mg of Tween 80, and add 5ml In acetonitrile, stir to disperse and mix to obtain the inner phase.

[0043] 3) Dissolve 248mg of Span 80 in 10ml of vegetable oil to obtain the external phase.

[0044] 4) At a stirring speed of 600rpm, add 0.3g of the inner phase to 5g of the outer phase dropwise, and disperse evenly to obtain an oil-in-oil emulsion.

[0045] 5) First place the emulsion in an ultrasonic cell disintegrator for 10 minutes of sonication, then evaporate the inner phase with electromagnetic stirring in an ice bath, wash with n-hexane, and dry at room temperature.

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Abstract

The invention discloses a preparation method of timolol maleate sustained release microspheres. The preparation method comprises the following steps: by adopting an oil-in-oil technology, preparing an internal phase from timolol maleate, modified montmorillonite, acrylic resin, tween and a plasticizer and preparing an external phase from vegetable oil and span; carrying out ultrasonic treatment on an obtained oil-in-oil emulsion; then, electromagnetically stirring to evaporate the internal phase to obtain the timolol maleate sustained release microspheres. The grain diameter of the timolol maleate sustained release microspheres can be controlled in a range of 10 mu m, so that the demand of eye-drops preparations is met. The medicine encapsulation rate reaches up to 80-99%, and the in vitro releasing time can be prolonged to 10-12 hours. The timolol maleate sustained release microspheres prepared by the method serving as an ocular hypotensive agent can reduce intraocular discomfort and reduce the medication frequency, so that the purpose of reducing intraocular pressure for a long time by one-time delivery is realized.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a preparation method of water-soluble intraocular pressure-lowering drug slow-release microspheres. Background technique [0002] Timolol maleate (timolol maleate) is a selective β-receptor blocker, which can reduce the formation of aqueous humor and significantly reduce intraocular pressure, and has no effect on pupil size, light response and vision. Timolol maleate eye drops are widely used clinically in the treatment of primary open-angle glaucoma and aphakic glaucoma. The efficacy of ophthalmic drugs depends on the effective concentration and residence time of the drugs in the cornea. The residence time of traditional eye drops in front of the cornea is 30s, and only 5% of the drugs are absorbed by the cornea. Frequent administration is required, and the dosage of eye drops is difficult to control , and most of them enter the blood circulation through the conjun...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K31/5377A61K47/26A61K47/32A61P27/06
Inventor 侯冬枝刘莉桂茹艺潘育方张兰春胡晟宋凤兰
Owner 广州铂思雅生物医药科技有限公司
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