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An ophthalmic preparation, the technology of ligustrazine, which is applied in the field of ligustrazine ophthalmic preparations, can solve the problems of affecting the curative effect, application limitation, and short duration of drug efficacy.
Inactive Publication Date: 2010-08-18
ZHONGSHAN OPHTHALMIC CENT SUN YAT SEN UNIV
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Problems solved by technology
Preliminary studies have shown that ligustrazine can penetrate the blood-aqueous humor barrier and the blood-retinal barrier after intraperitoneal injection or intravenous infusion, and enter the aqueous humor, vitreous body and retinal tissue, but it is quickly eliminated in the intraocular tissue and the drug effect is maintained. The time is short, affecting the curative effect
The frequency of systemic medication is affected by factors such as patient compliance and adverse drug reactions, which limits its application in ophthalmology.
Method used
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Embodiment 1
[0133] Embodiment 1, the preparation of ligustrazine ophthalmic preparation-eye drops, formula is as follows:
[0142] Take 0.3g of ethylparaben and add appropriate amount of water for injection, heat and stir to dissolve it, and set aside; dissolve 0.5g of ligustrazine hydrochloride in appropriate amount of water for injection, then gradually add 0.1g of disodium edetate and 8g of sodiumchloride and make it Dissolve; add the above-mentioned ethylparaben solution, stir well, add water for injection to the full amount, adjust the pH value with 1mol / L sodium hydroxide, filter, and sterilize by circulating steam at 100°C, and use aseptically dispensed. ...
Embodiment 2
[0143] Embodiment two, the preparation of ligustrazine ophthalmic preparation-eye drops, formula is as follows:
[0152] Take 0.3g of ethylparaben and add appropriate amount of water for injection, heat and stir to dissolve it, and set aside; dissolve 1g of ligustrazine hydrochloride in appropriate amount of water for injection, then gradually add 0.1g of edetate disodium and 8g of sodium chloride to dissolve Add the above-mentioned ethylparaben solution, stir well, add water for injection to the full amount, adjust the pH value with 1mol / L sodium hydroxide, filter, steam sterilization at 100°C, and aseptically dispense for use.
Embodiment 3
[0153] Embodiment three, the preparation of ligustrazine ophthalmic preparation-eye drops, formula is as follows:
[0159] 1mol / L sodium hydroxide appropriate amount
[0160] Add water for injection to 1000ml
[0161]
[0162] Take 0.3g of ethylparaben and add appropriate amount of water for injection, heat and stir to dissolve it, and set aside; dissolve 2g of ligustrazine hydrochloride in appropriate amount of water for injection, then gradually add 0.1g of edetate disodium and 8g of sodium chloride to dissolve ; Add the above-mentioned ethylparaben solution, stir well, add water for injection to the full amount, adjust the pH value with 1mol / L sodium hydroxide, filter; sterilize by circulating steam at 100°C, and use aseptically dispensed.
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Abstract
The invention discloses a chuangxionzine ophthalmic preparation with good curative effect, low toxic and side effect, stable pesticide effect and small irritation. The preparation is composed of effective quantity of chuangxionzine or chuangxionzine officinal salt and auxiliary material. Preferably, by mass percent of 100%, the content of the chuangxionzine or chuangxionzine officinal salt in the chuangxionzine ophthalmic preparation is 0.05-0.2%, and more preferably, the content of the chuangxionzine or chuangxionzine officinal salt is 0.1%. Experiment proves that the chuangxionzine ophthalmic preparation of the invention is safe and non-toxic, is resistant to rat crystalline lens oxidative damage caused by hydrogenperoxide and can delaysodium selenite to induce rat crystalline lens turbidness, curative effect is obvious, pharmacological action is strong, thus the preparation can be used for preventing and treating age-related cataract and can be made into eye drops or ophthalmic gel for use.
Description
technical field [0001] The invention belongs to the field of medicines, in particular to a ligustrazine ophthalmic preparation. Background technique [0002] Ligustrazine (ligustrazine) is an active ingredient extracted from the rhizome of Umbelliferae Ligusticum Chuanxiong, chemical name is 2,3,5,6-tetramethylpyrazine (tetramethylpyrazine, TMP), molecular formula C 8 h 12 N 2 , the structural formula is shown in Formula 1, and the molecular weight is 136.20. It has pharmacological effects such as dilating blood vessels, anti-platelet aggregation, improving tissue microcirculation, regulating lipid metabolism, anti-lipid oxidation, inhibiting proliferation of smooth muscle cells and fibroblasts, anti-tissue fibrosis and regulating immunity. At present, ligustrazine is mainly used clinically to treat ischemic cardiovascular and cerebrovascular diseases, ischemic limb vascular diseases, some diseases of the immune system, digestive system, urinary system and respiratory sys...
Claims
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Application Information
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