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A kind of sustained release type forsythin eye drops and preparation method thereof

A technology of forsythin eye drops and slow-release type, which is applied in the directions of pharmaceutical formulation, liquid transportation, emulsion transportation, etc., can solve the problems of restricting wide application, difficulty in reaching effective concentration, difficulty in forsythin, etc., and achieve easy raw material The production process is simple and feasible, and the effect of significant economic benefits

Active Publication Date: 2019-02-05
GUANGDONG LEWWIN PHARM RES INST CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The best way of topical administration in ophthalmology is eye drops, but because forsythin is insoluble in water, the solubility in water is 0.1mg / ml, it is difficult to reach its effective concentration, which limits its clinical application, especially in ophthalmology. widely used

Method used

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  • A kind of sustained release type forsythin eye drops and preparation method thereof
  • A kind of sustained release type forsythin eye drops and preparation method thereof
  • A kind of sustained release type forsythin eye drops and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1-3

[0035] Prepare raw materials according to the formula shown in table 1,

[0036] Step 1), the full amount of sodium hyaluronate was swelled for 2 hours, polycarbophil was added and stirred to dissolve, and then the full amount of forsythin was dissolved;

[0037] Step 2), disperse the thickener with water for injection and let it cool, and dissolve the pH regulator, osmotic pressure regulator, and bacteriostat with water for injection, stir well and filter, and combine the above two parts of the mixed solution;

[0038] Step 3), add dissolved forsythin to the mixed solution obtained in step 2), add water for injection to the full amount, filter, sub-package, and obtain, the pH value of the obtained eye drops is 5.5-7.5, drop The osmolality of the eye solution is 250-350 mOsmol / kg.

[0039] Table 1 Preparation of sustained release type forsythin eye drops raw material components and dosage

[0040]

[0041]

experiment example 2

[0042] Pharmacokinetic test of experimental example 2 forsythin sustained-release eye drops

experiment example 3

[0067] Experimental Example 3 Eye Irritation Test of Sustained-release Forsythin Eye Drops with Different Concentrations

[0068] The eye drops prepared by the method of Example 1-3 of the present invention were used for eye irritation test.

[0069] Comparative Example 2: Dexamethasone Eye Drops (0.1%)

[0070] 24 healthy New Zealand rabbits (half male and half female) (provided by Qingdao Kangda Biotechnology Co., Ltd.). The eyes of the animals were checked 24 hours before the experiment, and animals with normal eyes, no inflammation, no defects, and no old corneal damage were selected for the experiment. The self-comparison method was used to measure the left and right sides of the same body. Drugs were given to the left eye, 0.9% sodium chloride injection was given to the left eye of the negative group, and the right eye was used as a negative control. 100 μL per eye, once a day, for 7 consecutive days. Before administration every day and 1, 2, 4, 24, 48 and 72 hours aft...

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Abstract

The invention relates to slowly-released forsythin eye drops, and a preparation method thereof. According to the preparation method, forsythin is taken as a drug effect raw material, polycarbophil and sodium hyaluronate are used for forming a mucous adhesive-type polymer drug release system, and the slowly-released forsythin eye drops are prepared from the above raw materials and eye acceptable pharmaceutically acceptable auxiliary materials. The weight ratio of forsythin: polycarbophil : sodium hyaluronate is controlled to be 1:0.5-2:0.5-5. The dosage form is eye drops. The slowly-released forsythin eye drops are used for local external use, is capable of preventing inflammation, oxidation, bacteria, and cancer, is capable of protecting nerves, can be used for treating different eye inflammations, can be used for postoperative recovery of ophthalmologic operation such as cataract operation, is wide in application range, possesses excellent eye penetrability, and is relatively high in bioavailability in eyes.

Description

technical field [0001] The invention belongs to the field of medicines, and more specifically relates to a sustained-release forsythin eye drop and a preparation method thereof. Background technique [0002] Forsythin (Forsythin) is extracted and refined from the dried leaves of Forsythia suspense (Thunb.) Vahl., a plant of Oleaceae. , is also the quality control index component of Forsythia medicinal materials stipulated in the National Pharmacopoeia. Its pharmacological activities are mainly manifested as antioxidant activity, antibacterial activity, anti-inflammatory activity, antiviral activity, antitumor activity and antipyretic and analgesic activity. [0003] Cataract is the leading cause of blindness in the world, and its etiology has not yet been clarified. Studies have shown that oxygen free radical damage is the first risk factor for senile cataract. If free radicals are generated too much or scavenged too little, free radicals will gather to produce crystal cel...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/06A61K31/7048A61K47/36A61K47/32A61P27/02A61P29/00
CPCA61K9/0048A61K9/06A61K31/7048A61K47/32A61K47/36
Inventor 郭健敏杨威林俊粒文冬梅
Owner GUANGDONG LEWWIN PHARM RES INST CO LTD
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