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Precursor suspension of lyotropic liquid crystal and preparation method thereof

A lyotropic liquid crystal and suspension technology, applied in the directions of liquid delivery, emulsion delivery, drug combination, etc., can solve the problems of weak gel strength, insufficient adhesion, and inability to guarantee retention, and achieve slow release and stability. high effect

Active Publication Date: 2014-11-05
GUANGZHOU NEWORLD PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the arrangement of the water channels as the gel skeleton structure is relatively loose, so the strength of the formed gel is weak, and at the same time, its adhesion is insufficient, and it cannot guarantee its stay in some lesions.

Method used

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  • Precursor suspension of lyotropic liquid crystal and preparation method thereof
  • Precursor suspension of lyotropic liquid crystal and preparation method thereof
  • Precursor suspension of lyotropic liquid crystal and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] The precursor suspension of embodiment 1 lyotropic liquid crystal

[0037] Contains the following components:

[0038]

[0039] The preparation method of the precursor suspension of this embodiment is: after mixing glycerol monooleate, oleic acid and 2-pyrrolidone evenly, add micronized doxycycline hydrochloride (1 ~10μm) raw material drug, after mixing evenly, it is ready. Due to the poor stability of doxycycline hydrochloride, it should be used immediately after mixing. The drug loading of the precursor suspension in this embodiment is 10%, and the drug can be released in vitro for up to one week. The strength of the formed lyotropic liquid crystal gel is about 160 g, and the adhesion is 150 g.

Embodiment 2

[0040] The precursor suspension of embodiment 2 lyotropic liquid crystal

[0041] Contains the following components:

[0042]

[0043] The preparation method of the precursor suspension in this example is: dissolving the doxycycline hydrochloride bulk drug in N-methylpyrrolidone to form a uniform and transparent solution, adding glycerol monooleate at a stirring speed of 2500r / min Esters, oleic acid, and drugs are slowly precipitated during the addition of the two, forming smaller particles (1-10 μm) suspended in the entire system, that is. Due to the poor stability of doxycycline hydrochloride, it should be used immediately after mixing. The precursor suspension in this embodiment is released externally for 7-10 days, and the formed lyotropic liquid crystal gel has a strength of about 80 g and an adhesive force of about 20 g. Compared with Example 1, the weight ratio of solute liquid crystal material is reduced, accompanied by the reduction of gel strength and adhesion. ...

Embodiment 3

[0044] The precursor suspension of embodiment 3 lyotropic liquid crystal

[0045] Contains the following components:

[0046]

[0047] The preparation method of the precursor suspension in this embodiment is as follows: after mixing glycerol monooleate, propylene glycol, and soybean oil evenly, add micronized metronidazole raw drug powder (1-10 μm), and mix evenly to obtain . The drug loading amount of the precursor suspension in this embodiment is 25%, the content is uniform, and the drug release in vitro is 2-3 days. The gel strength is less than 80g, and the adhesion is about 20g.

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Abstract

The invention discloses a precursor suspension of a lyotropic liquid crystal. The precursor suspension comprises lyotropic liquid crystal material, organic solvent, oil phase and a drug, wherein the weight percentage of the oil phase in the precursor suspension is 2-50 percent, the weight percentage of the drug in the precursor suspension is 1-30 percent, and the weight ratio of the lyotropic liquid crystal material and the organic solvent in the precursor suspension is 2-9:1. According to the invention, through the adding of the oil phase into the precursor suspension, the stability of the suspension is improved, the sedimentation rate is reduced, and the strength and the adhesive force of the gel formed are enhanced at the same time; the gel formed in the body is more liable to stay at a lesion location and less liable to be relocated and the shape is less liable to be damaged by the mechanical motion of the body, so that the drug therapy can be located effectively; and the preparation technology is simple and the precursor suspension of the lyotropic liquid crystal is a partial slow-release drug delivering system provided with a favorable perspective.

Description

field of invention [0001] The invention belongs to the field of pharmacy, and more specifically, the invention relates to a precursor suspension of lyotropic liquid crystal and a preparation method thereof. Background of the invention [0002] For some local diseases with long treatment cycle and frequent drug use, such as cancer, mucosal disease, skin disease, etc., the treatment usually adopts traditional systemic drug delivery (oral or injection), and the drug is delivered to the lesion site through blood circulation to exert its drug effect. Although this route of administration is simple and feasible, the inevitable defect is the first-pass effect or systemic adverse reactions. Especially for these patients who need long-term medication, frequent medication is also extremely inconvenient. Compared with systemic administration, local administration can avoid the first-pass effect and adverse reactions to a large extent, which has certain advantages. However, there is no...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/10A61P35/00
Inventor 吴传斌黄心恬覃玲珍潘昕
Owner GUANGZHOU NEWORLD PHARMA CO LTD
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