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Chitosan derivatives, their preparation and medical composition containing the same as active component

A compound and drug technology, applied in the field of chitosan derivatives, can solve the problems of corneal ulcer and corneal goblet cell differentiation and reduction, and achieve the effects of good chemical property stability, good water solubility, and improved moisturizing performance.

Inactive Publication Date: 2004-03-31
浙江南洋药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] 5. Vitamin A artificial tears and Youlepe artificial tears produced by Novartis Ophthalmology in Switzerland are used for patients who are ineffective in general artificial tears, which will reduce the number of corneal keratinocytes and increase the number of goblet cells, but corneal ulcers and corneal ulcers may occur after discontinuation of use. Abnormal differentiation and reduction of goblet cells
In addition, the stability and corneal residence time of artificial tears need to be improved

Method used

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  • Chitosan derivatives, their preparation and medical composition containing the same as active component

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053] Preparation of Chitosan Lactate

[0054] Chitosan with a viscosity average molecular weight of 50,000-400,000 is 100g, soaked in 1300mL of deionized water for 0.5-1 hour, added 132ml of lactic acid, controlled the reaction temperature at 20°C, and reacted for 4-6 hours. Concentrate by nanofiltration, and the obtained concentrated solution is subjected to vacuum freeze-drying to obtain the final product (purity above 99%, modification rate at 99%, white sheet, easy to dissolve at room temperature).

[0055] NMR analysis results of chitosan lactate

[0056] Hydrogen atom Chemical shift (peak intensity) Number of hydrogen atoms

[0057] H1 4.73725(0.9411) 1

[0058] H2 3.03592(1.000) 1

[0059] H5 3.51608(1.2129) 1

[0060] H3, 4, 6, 6' 3.66585, 3.76325(3.7320) 4

[0061] Ha 1.19985-1.29622(3.5409) 3

[0062] Hb 4.14336-4.16975(1.2697) 1I(Ha) / I(Hb)=3.5409 / 1.2697≈3 conforms to CH in the structural formula 3(a) CH-OH (b) COO - Medium H a / H b Ratio [I(H a ) / 3] / I(...

Embodiment 2

[0097] artificial tears

[0098] Chitosan Lactate 0.5%

[0099] Natural Stabilizer 4%

[0100] NaCl 0.014%

[0101] KCl 0.014%

[0102] CaCl 0.014%

[0103] 1%NaHCOO 3 0.05M

[0104] Preparation method: prepare 1% NaHCO 3 Solution Chitosan lactate, natural stabilizer, NaCl, KCl, CaCl are weighed according to the prescription, dissolved in prepared 1% NaHCO 3 The solution is tested for pH, meets the requirements of artificial tears, and is bottled.

[0105] Artificial tears requirements

[0106] PH: 6-8 (human tears 6.5-7.4)

[0107] Osmotic pressure: 248-370mOsM / kg

[0108] Viscosity: 2.0-6.0mPa.S (human tears 4.0-5.0mPa.S)

[0109] Preservatives: less toxic and side effects (preferably not used)

[0110] Clarity: colorless and transparent

[0111] Safety: The ingredients used are non-toxic, safe and reliable, with good hygroscopicity and moisturizing properties.

Embodiment 3

[0113] Tablets (10,000 pieces):

[0114] Chitosan Lactate 1kg

[0115] Beating starch (10%) 0.5kg

[0116] Starch 200g

[0117] Magnesium Stearate 7.5g

[0118] Preparation method: mix chitosan lactate, beating starch and starch, sieve and dry, add magnesium stearate, and press into tablets.

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Abstract

A new chitosan derivative with the general formula (I), wherein R is CH3(CH2)N-( 0 íœníœ5), or CH3(CH2) n-1CHOH-(1íœníœ5). The invention also relates to the preparation method and pharmaceutical compound containing the derivative as the active component, and the application of the compound in preparing drugs for scheroma.

Description

technical field [0001] The invention relates to a chitosan derivative, a preparation method thereof, a pharmaceutical composition using the compound as an active ingredient, and an application of the compound in preparing medicine for treating dry eye disease. Background technique [0002] Dry eye disease is a general term for a group of diseases in which the eye epithelium dries up due to low tear secretion or abnormal tear film caused by other reasons. The disease is basically caused by low tear secretion or abnormal tear secretion, which leads to ocular surface epithelial dryness. The exact cause and pathogenesis are still unknown, and it may be related to abnormal immune function of endocrine, red blood cells and lymphocytes. SS is a special major disease that causes dry eye, mainly related to lacrimal gland lesions. Furthermore, xerophthalmia, synonymous with vitamin A deficiency, is the typical dry eye due to mucus deficiency. With the prolong...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/722A61P27/02C08B37/08
Inventor 吴绵斌马越峰陈春
Owner 浙江南洋药业有限公司
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