阅读说明：本技术 一种高效草本滴眼液 (High-efficiency herbal eye drops ) 是由 李达欣 于 2018-08-31 设计创作，主要内容包括：本发明了公开一种高效草本滴眼液,属于医药化学品领域,包含以下组分及重量比：水80-100、聚卡波菲AA 50-60、土霉素30-40、他氟前列素25-30、马来酸噻吗洛尔20-25、鱼腥草精华18-23、金银花精华16-21、决明子精华13-18、黄连精华11-16、氯化钠9-13、依地酸二钠6-11、泊洛沙姆6-9、泰洛沙泊5-8、马来酸噻吗洛尔4-8、布林佐胺4-6、甘露醇2-5、柠檬酸2-5、柠檬酸钠2-4、苯1-3、防腐剂1-3,解决传统草本药水吸收差、效果差,化学制剂滴眼液又伤害眼睛的问题。(The invention discloses a high-efficiency herbal eye drop, which belongs to the field of medicinal chemicals and comprises the following components in parts by weight: 80-100 parts of water, 50-60 parts of polycarbophil AA, 30-40 parts of oxytetracycline, 25-30 parts of tafluprost, 20-25 parts of timolol maleate, 18-23 parts of houttuynia cordata essence, 16-21 parts of honeysuckle essence, 13-18 parts of cassia seed essence, 11-16 parts of coptis chinensis essence, 9-13 parts of sodium chloride, 6-11 parts of edetate disodium, 6-9 parts of poloxamer, 5-8 parts of tyloxapol, 4-8 parts of timolol maleate, 4-6 parts of brinzolamide, 2-5 parts of mannitol, 2-5 parts of citric acid, 2-4 parts of sodium citrate, 1-3 parts of benzene and 1-3 parts of a herbal preservative, and the problems that the traditional liquid medicine is poor in absorption and effect, and the eye drops of chemical preparations damage eyes are solved.)

1. The high-efficiency herbal eye drops are characterized by comprising the following components in parts by weight: 80-100 parts of water, 80-60 parts of polycarbophil AA50, 30-40 parts of oxytetracycline, 25-30 parts of tafluprost, 20-25 parts of timolol maleate, 18-23 parts of houttuynia cordata essence, 16-21 parts of honeysuckle essence, 13-18 parts of cassia seed essence, 11-16 parts of coptis chinensis essence, 9-13 parts of sodium chloride, 6-11 parts of edetate disodium, 6-9 parts of poloxamer, 5-8 parts of tyloxapol, 4-8 parts of timolol maleate, 4-6 parts of brinzolamide, 2-5 parts of mannitol, 2-5 parts of citric acid, 2-4 parts of sodium citrate, 1-3 parts of benzene and 1-3 parts of preservative.

2. The super-potent herbal eye drop as claimed in claim 1, which comprises the following components in weight ratio: water 91, polycarbophil AA 56, oxytetracycline 34, tafluprost 27, timolol maleate 23, houttuynia cordata essence 21, honeysuckle essence 18, cassia seed essence 16, coptis chinensis essence 13, sodium chloride 11, edetate disodium 9, poloxamer 8, tyloxapol 7, timolol maleate 5, brinzolamide 5, mannitol 4, citric acid 4, sodium citrate 3, benzene 2 and preservative 2.

3. The super-potent herbal eye drops as claimed in claim 1 or 2, wherein the preservative comprises one or more of benzalkonium chloride, and sorbitol.

Technical Field

The invention relates to the field of medicinal chemicals, and in particular relates to high-efficiency herbal eye drops.

Background

The existing dosage form on the market is aqueous eye drops, and the solution type eye drops have the advantages of simple production process, convenient operation and the like, but have the following defects and aspects: 1) the dosage is inaccurate, and the dripping amount of each time of a patient is different, so that the outflow effect of aqueous humor of a uvea sclera is different, the intraocular pressure reducing effect is unstable, and the safety risk exists; 2) the tafluprost eye drops have high elimination speed, and the average blood concentration of the tafluprost acid is lower than the detection limit (10pg/mL) in a biological analysis test after eye instillation for 30 min; 3) during the process of continuous blinking of eyelids and continuous secretion of tears in conjunctiva, more than 95% of liquid medicine is taken away by tears through nasolacrimal duct, so that the bioavailability is extremely low (less than 1%), and a large amount of medicine enters nasal cavity or digestive tract through nasolacrimal duct and is finally absorbed by the whole body, thereby increasing the risk of inducing toxic and side effects 4). Therefore, in order to solve the above problems, it is necessary to develop and search an ophthalmic drug delivery formulation having a long retention time in the eye and a sustained/controlled release capability to compensate for the inherent deficiency in the therapeutic effect of an ophthalmic liquid preparation.

Oxytetracycline (oxytetracycline) is a broad-spectrum antibiotic found in the culture broth of Streptomyces rimosus (actinomycetes) by Fenli (A.C Finlay) and the like (1950). Can inhibit the development of various bacteria, rickettsia and chlamydia, and can be widely used for treatment. The action mechanism of terramycin is that the medicine can be specifically combined with A position of bacterial ribosome 30S subunit, and can inhibit growth of peptide chain and affect synthesis of bacterial protein. The existing oxytetracycline preparations comprise tablets, capsules, ointments, eye ointments and the like. Can be used for treating dysentery, trachoma, conjunctivitis, pneumonia, otitis media, dermatitis, amoebic enteritis, and intestinal infection. .

Disclosure of Invention

The invention aims to solve the problems that the traditional herbal liquid medicine is poor in absorption and effect and chemical preparation eye drops injure eyes and provide the high-efficiency herbal eye drops.

In order to solve the technical problems, the invention adopts the following technical scheme:

an efficient herbal eye drop comprises the following components in parts by weight: 80-100 parts of water, 80-60 parts of polycarbophil AA50, 30-40 parts of oxytetracycline, 25-30 parts of tafluprost, 20-25 parts of timolol maleate, 18-23 parts of houttuynia cordata essence, 16-21 parts of honeysuckle essence, 13-18 parts of cassia seed essence, 11-16 parts of coptis chinensis essence, 9-13 parts of sodium chloride, 6-11 parts of edetate disodium, 6-9 parts of poloxamer, 5-8 parts of tyloxapol, 4-8 parts of timolol maleate, 4-6 parts of brinzolamide, 2-5 parts of mannitol, 2-5 parts of citric acid, 2-4 parts of sodium citrate, 1-3 parts of benzene and 1-3 parts of preservative.

Preferably, the composition comprises the following components in percentage by weight: water 91, polycarbophil AA 56, oxytetracycline 34, tafluprost 27, timolol maleate 23, houttuynia cordata essence 21, honeysuckle essence 18, cassia seed essence 16, coptis chinensis essence 13, sodium chloride 11, edetate disodium 9, poloxamer 8, tyloxapol 7, timolol maleate 5, brinzolamide 5, mannitol 4, citric acid 4, sodium citrate 3, benzene 2 and preservative 2.

Preferably, the preservative comprises one or more of benzalkonium chloride, and sorbitol.

The implementation of the invention has the following beneficial effects:

the inventor discovers in research that hydrophilic polymer polycarbophil AA-1 or carbomer is used as an eye drop slow-release material, the eye drop slow-release material is in a water solution form in an in vitro environment, when the eye drop is dripped into a conjunctival sac, the eye drop fast forms gel to be attached to the surface of an eyeball under the influence of the temperature, the pH value or the ionic strength of the eye, and an extremely thin drug reservoir is formed, so that the time of the drug staying at the eye using part can be prolonged, the fast loss of the drug is avoided, the formed drug reservoir has the function of slowly releasing the drug, the fast elimination of the drug is avoided, and the bioavailability is improved. The eye drop can be closely contacted with eyes for a long time, has better biological adhesion, and overcomes the defect that the aqueous solution type eye drop can be quickly washed by tears and cannot reach the effective drug concentration or maintain the long-time intraocular pressure reduction effect; the eye gel has good compatibility with eyeball tissues, is convenient to use, and improves the compliance of patients; the hydrophilic polymer is highly hydrophilic, can bind the medicine in a net structure, slowly control the medicine release, improve the bioavailability, reduce the administration frequency and improve the economic benefit of the medicine; the dosage is accurate, and the adverse reaction of the whole body is avoided being difficult to cause by long-term administration; has special physical and chemical properties, is easy to fill and is easy for industrial production.

Detailed Description

In order to make the objects, technical solutions and advantages of the present invention more apparent, the present invention will be further described in detail with reference to specific embodiments.