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Loratadine nasal cavity in situ gel and preparation method thereof

A technology of loratadine and in-situ gel, which is applied in pharmaceutical formulations, medical preparations with non-active ingredients, and medical preparations containing active ingredients, etc., can solve gastrointestinal adverse reactions, liver function, and effective utilization. It can improve bioavailability, reduce toxicity, and improve clearance.

Active Publication Date: 2022-05-20
CHANGZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, because loratadine is almost insoluble in water, its effective utilization rate is low and it is easy to cause gastrointestinal adverse reactions and liver function damage through oral administration, thus limiting its clinical effect

Method used

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  • Loratadine nasal cavity in situ gel and preparation method thereof
  • Loratadine nasal cavity in situ gel and preparation method thereof
  • Loratadine nasal cavity in situ gel and preparation method thereof

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preparation example Construction

[0024] The present invention also provides a preparation method of the loratadine nasal in situ gel, the steps are as follows: according to the formula, gellan gum is placed in a reaction vessel, heated and stirred until completely dissolved, then taken out and allowed to cool, Add sodium alginate, HPMC, Tween 80, and deionized water, and stir until completely dissolved.

[0025] In one embodiment, the temperature of the heating and stirring is 87°C.

Embodiment 1

[0028] The instrument used in the present invention is as follows:

[0029] CL-1A magnetic stirrer (Gongyi Yingyu high-tech instrument factory); DF-Ⅱ digital display heat-collecting magnetic stirrer (Jintan Jerry Electric Co., Ltd.); 85-2 constant temperature magnetic stirrer ( Shanghai Sile Instrument Factory); FA2004B electronic balance (Shanghai Yueping Scientific Instrument (Suzhou) Manufacturing Co., Ltd.); PS-30AL ultrasonic cleaning machine (Shenzhen Shenhuatai Ultrasonic Cleaning Equipment Co., Ltd.); NDJ-1B rotary Viscometer (Shanghai Changji Geological Instrument Co., Ltd.); DHG-9035A blast drying oven (Shanghai Aozhen Instrument Manufacturing Co., Ltd.); s53 UV-Vis spectrophotometer (Shanghai Prism Technology Co., Ltd.); RYJ-12B drug Transdermal diffusion tester; smart phone (Huawei Honor V10 low configuration version).

[0030] The materials used in the present invention are as follows:

[0031] Gellan gum (OPAL Biotech, batch number 18042510); hypromellose (Shan...

Embodiment 2

[0051] Preparation of Loratadine Nasal In Situ Gel: Weigh 0.7624g of Loratadine crude drug, transfer it to a 10mL volumetric flask, add 98% ethanol to the scale line to make up the volume, and ultrasonically dissolve it for later use. Prepare the blank gel according to the prescription in Table 1 and the method described in 2.3.2, take out 10g and put it in a 15mL centrifuge tube, add 1mL of loratadine-ethanol solution into the taken out gel, stir it evenly with a glass rod, and use it as the sample to be tested .

[0052] 1. Determination of loratadine content: It is known that with 50% ethanol aqueous solution as solvent, loratadine has ultraviolet absorption at 247nm, and other substances in the preparation do not absorb under this wavelength, so ultraviolet-visible spectrophotometry can be used Determination of loratadine content.

[0053] Drawing of the standard curve of loratadine solution: Weigh 125.3mg of loratadine, transfer to a 500mL volumetric flask, dilute to the...

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Abstract

The invention discloses a loratadine nasal cavity in situ gel and a preparation method thereof, belonging to the technical field of nasal cavity gel. The loratadine nasal in situ gel includes the following components: loratadine 7.6 mg / mL, gellan gum 3 mg / mL, sodium alginate 2 mg / mL, HPMC 2 mg / mL, Tween 80 1 mg / mL, ethanol 1 mL / mL, and deionized water as the balance. The present invention uses gellan gum and sodium alginate as the gel matrix, and conducts research on the viscosity of the gel, gelation time, gel strength, drug content, adhesion, stability and drug release in vitro, etc., and comprehensively evaluates, To determine an optimal prescription of loratadine nasal in situ gel.

Description

technical field [0001] The invention belongs to the technical field of nasal cavity gel, and in particular relates to a loratadine nasal cavity in situ gel and a preparation method thereof. Background technique [0002] In recent years, as a convenient and reliable systemic drug delivery method, nasal administration has shown its superiority, especially for drugs that are ineffective orally and must be injected. The nasal epithelium has high permeability, and there are only two layers of cells between the nasal cavity and the dense vascular network of the lamina propria. Compared with other systemic drug administration routes, nasal administration has many advantages, including: rapid absorption, avoiding intestinal and liver effects, rapid onset of action, avoiding gastrointestinal membrane irritation, non-invasive drug delivery, and convenient self-administration by patients. Improve patient compliance, etc. These make nasal administration has received extensive attentio...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/06A61K47/36A61K47/38A61K47/26A61K47/10A61K31/4545A61P37/08
CPCA61K9/0043A61K9/06A61K47/36A61K47/38A61K47/26A61K47/10A61K31/4545A61P37/08
Inventor 周舒文王佳炜崔朋飞邱琳崔硕王建浩
Owner CHANGZHOU UNIV
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