Decumbent corydalis tuber eye drop and preparation method thereof

Abstract

The invention relates to a decumbent corydalis tuber eye drop and a preparation method thereof. According to the decumbent corydalis tuber eye drop, the pH value is 4.6 to 6.5, and the permeation pressure is between 0.24 and 0.360 smol / kg; each 1,000 milliliters of decumbent corydalis tuber eye drop is prepared from the following substances: a decumbent corydalis tuber extract containing 0.32 to 0.43 gram of protopine, 0.0036 to 0.0048 mol of diluted phosphoric acid solution, and 0.1 to 3.0 grams of sodium dihydrogen phosphate, 3 to 8 grams of solubilizer, 0.2 to 0.8 gram of disodium edentate, 0.1 to 0.8 gram of bacteriostatic agent, 0 to 2.0 grams of thickening agent, 0 to 4 grams of medicinal ethanol solution of freshener, disodium hydrogen phosphate and glycerol which serve as auxiliary materials and the balance of water for injection, wherein the concentration of the diluted phosphoric acid solution is less than or equal to 0.5 mol / L, and a mass ratio of the freshener to medicinalethanol is 1:(1-15); the amount of the disodium hydrogen phosphate is used for regulating the pH value of the decumbent corydalis tuber eye drop; and the amount of the glycerol is used for regulatingthe permeation pressure of the decumbent corydalis tuber eye drop. The decumbent corydalis tuber eye drop has a mild effect, and the compliance of patients is improved greatly, so the decumbent corydalis tuber eye drop is an eye drop which is small in irritation and high in stability.

Description

technical field [0001] The invention belongs to the technical field of ophthalmic medication of pharmaceutical preparations, and in particular relates to a summer-free eye drop with minimal irritation and good stability and a preparation method. Background technique [0002] Summer Wuwei Papaveraceae Corydalis Corydalis Corydalis decumhens (Thunb.) Pers. The main components of its extract are alkaloids, including protropine (original opioid), allocryptopine, cryptophyrine, cryptopin palmatine, tetrahydropalmatine, and corydalis monophenol alkali, dihydropalmatine, palmatine, jatrorrhizine, etc. Xia Tian Wu Eye Drops is an eye drop prepared from Xia Tian Wu extract as the main raw material. Its main active ingredient, protropine (formerly opioid), can directly relax smooth muscle, and can also antagonize the effects of acetylcholine and barium chloride on eye muscles. Spasmodic contraction. Xia Wu Eye Drops has the functions of promoting blood circulation, improving eyesig...

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Problems solved by technology

[0003] Xia Tian Wu Eye Drops is a new drug developed in the 1970s. Due to the limitations of the environment and conditions at that time, the excipients in the original prescription were not perfect, and there were obvious irritations; After continuous exploration, the prescription process of Xia Tian Wu Eye Drops was gradually improved; the Xia Tian Wu Eye Drops currently on the market are produced according to the standards of this product in the 2010 edition of the Chinese Pharmacopoeia, and their irritation is significantly higher than that of the original product. Improved, but still difficult to eliminate transient irritation with use

[0004] When no eye drops are used in summer, when they are instilled into the eyes, most patients report a transient irritation (stinging pain), especially for children and adolescents who are particularly sensitive to pain, it is difficult to accept, and even stop the medication subjectively; Afterwards, the strong irritation causes increased tear secretion, which seriously reduces the bioavailability of the drug and affects the curative effect.

The above deficiencies limit the popularization and application of this product, so that it cannot give full play to its due social and economic benefits; therefore, further reducing the irritation of summer eye drops is the key to improving patient compliance and curative effect

[0005] Since the Xiawu eye drops contain a variety of alkaloids, the original prescription and its preparation method need to be dissolved with a strong acid-hydrochloric acid solution, resulting in a low pH of the eye drops and a relatively strong transient irritation; however, once Reduce the amount of acid or increase the pH of the system, although the transient irritation is reduced, but the stability of the system is greatly reduced, and it is easy to produce foggy precipitation during the storage process

In order to obtain a stable product, Xia Tian Wu Eye Drops (original prescription) adopts a lower pH range (3-4.5), usually it needs to be controlled below 3.5 to be stable, which is beyond the normal tolerance range of human eyes (5-8 ), so the irritating

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