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CN-121971385-A - Gel eye drops containing bromfenac sodium and moxifloxacin hydrochloride, and preparation method and application thereof

CN121971385ACN 121971385 ACN121971385 ACN 121971385ACN-121971385-A

Abstract

The invention discloses gel eye drops containing bromfenac sodium and moxifloxacin hydrochloride, and a preparation method and application thereof, and belongs to the technical field of medicines. The water-based gel comprises, by weight, 0.8-1.2 parts of bromfenac sodium, 0.8-6 parts of moxifloxacin hydrochloride, 15-30 parts of a gel matrix, 3-15 parts of sodium hyaluronate, 8-12 parts of an osmotic pressure regulator, 7.0-9.0 parts of citric acid, 0.02-0.05 part of sodium citrate and 950-1050 parts of purified water. The invention realizes the compound gel eye drops which have no preservative, low stimulation, good stability, improved bioavailability of medicines, anti-inflammatory and antibacterial synergism and can effectively treat the ocular inflammation through the combination of the bromfenac sodium and the moxifloxacin hydrochloride and the combination of the gel matrix, the sodium hyaluronate, the osmotic pressure regulator, the citric acid, the sodium citrate and the purified water.

Inventors

  • LIU WENFEI
  • LIU SHAOCHAO
  • WANG NA

Assignees

  • 但丁生物科技(山东)有限公司

Dates

Publication Date
20260505
Application Date
20260318

Claims (10)

  1. 1. The gel eye drops containing the bromfenac sodium and the moxifloxacin hydrochloride are characterized by comprising, by weight, 0.8-1.2 parts of bromfenac sodium, 0.8-6 parts of moxifloxacin hydrochloride, 15-30 parts of gel matrix, 3-15 parts of sodium hyaluronate, 8-12 parts of osmotic pressure regulator, 7.0-9.0 parts of citric acid, 0.02-0.05 part of sodium citrate and 950-1050 parts of purified water.
  2. 2. The gel eye drop containing sodium bromfenac and moxifloxacin hydrochloride according to claim 1, wherein the gel matrix is selected from one or more of hypromellose, carbomer, xanthan gum, hydroxyethyl cellulose.
  3. 3. The gel eye drop containing bromfenac sodium and moxifloxacin hydrochloride according to claim 1, wherein the weight ratio of bromfenac sodium to moxifloxacin hydrochloride is 1:1-1:5; the weight ratio of the bromfenac sodium to the moxifloxacin hydrochloride is 1:1, 1:2, 1:3, 1:4 or 1:5.
  4. 4. The gel eye drop containing sodium bromfenac and moxifloxacin hydrochloride according to claim 1, wherein the osmotic pressure regulator is one or more selected from sorbitol, glycerin, propylene glycol, mannitol.
  5. 5. A method for preparing the gel eye drops containing bromfenac sodium and moxifloxacin hydrochloride according to any one of claims 1 to 4, which is characterized by comprising the following steps: (1) Dispersing and dissolving the gel matrix and sodium hyaluronate in part of purified water, fully swelling, and sterilizing at high temperature to obtain gel matrix dispersion liquid; (2) Dissolving sodium bromfenac and moxifloxacin hydrochloride in part of purified water, adding citric acid, sodium citrate and osmotic pressure regulator, uniformly stirring, filtering and sterilizing to obtain a second solution; (3) Mixing the second solution obtained in the step (2) with the gel matrix dispersion liquid obtained in the step (1), adding purified water to a sufficient amount, stirring, and filling into a single-dose packaging container.
  6. 6. The process according to claim 5, wherein in step (1), the high temperature is 120 to 130 ℃.
  7. 7. The method of claim 5, wherein in step (2), 0.22 μm PVDF filter is used for sterilization.
  8. 8. The process according to claim 5, wherein in the step (3), the stirring speed is 1000 to 2000rpm, the stirring temperature is 30 to 40℃and the stirring time is 30 to 40 minutes.
  9. 9. The method according to claim 5, wherein in the step (3), the filling amount is 0.4ml to 1.5ml.
  10. 10. The application of the gel eye drops containing sodium bromfenac and moxifloxacin hydrochloride prepared by any one of claims 1-4 or the gel eye drops containing sodium bromfenac and moxifloxacin hydrochloride prepared by any one of claims 5-9 in the preparation of anti-inflammatory drugs.

Description

Gel eye drops containing bromfenac sodium and moxifloxacin hydrochloride, and preparation method and application thereof Technical Field The invention relates to the technical field of medicines, in particular to gel eye drops containing bromfenac sodium and moxifloxacin hydrochloride, and a preparation method and application thereof. Background The information disclosed in the background of the invention is only for enhancement of understanding of the general background of the invention and is not necessarily to be taken as an admission or any form of suggestion that this information forms the prior art already known to a person of ordinary skill in the art. The eye mucosa tissue is fragile and directly contacts with the outside, is easy to be affected by microorganisms and is physically and chemically stimulated to cause inflammatory diseases, and in clinic, the symptoms such as infectious conjunctivitis, xerophthalmia combined inflammation and the like are high, and the cornea barrier can be damaged to influence the visual function when serious, so that the eye preparation with anti-inflammatory and antibacterial effects is required in clinic. The existing anti-inflammatory eye drops commonly used clinically are represented by bromfenac sodium, the antibacterial eye drops are represented by moxifloxacin hydrochloride, and the two are widely applied to the field of ophthalmology by virtue of excellent drug effects. In the prior art, the bromfenac sodium eye drops and the moxifloxacin hydrochloride eye drops are marketed in a multi-dose solution type, and in order to ensure the storage stability of a multi-dose product, borax is added as a preservative, but the long-term contact of borax with the ocular surface can damage the ocular surface mucosa barrier integrity, so that the tear evaporation rate is accelerated, dryness and foreign body sensation of eyes are induced or aggravated, the applicability to dry eyes and cornea sensitive people is extremely poor, and meanwhile, the single bromfenac sodium preparation needs to be additionally added with an oxidant to ensure the stable drug effect, the oxidant can enhance the ocular administration irritation, and the drug stability is poor. In addition, the two eye drops are combined for use, so that the administration times and inconvenience of patients are increased, and the compound stimulation and burden on the ocular surface are increased because the two preparations possibly contain different pH adjusting systems, osmotic pressure regulators and preservatives. The solution type eye drops are convenient to use and low in cost, but have obvious problems that on one hand, due to an eye protection mechanism, the medicine stays in conjunctival sac for a short time, the local bioavailability is low, the medicine effect is difficult to fully exert, and on the other hand, most of the medicine can reach nasal cavities along with tears and then enter the systemic circulation through mucous membrane absorption, so that the risk of side effects is increased. Although the hydrogel technology has proved to prolong the retention time of the medicine on the ocular surface, the hydrogel eye drops are sticky and are easy to grow microorganisms, so that the problems of eye irritation, dryness and the like caused by adding preservatives are solved. The prior art lacks a bromfenac sodium and moxifloxacin hydrochloride compound eye drop which has no preservative, low irritation, good stability, improves the bioavailability of the medicine and can realize the synergistic effect of anti-inflammatory and antibacterial, and the research and development are urgently needed. Disclosure of Invention In view of the above, the invention provides a gel eye drop containing bromfenac sodium and moxifloxacin hydrochloride, and a preparation method and application thereof. In the first aspect, the invention provides a gel eye drop containing bromfenac sodium and moxifloxacin hydrochloride, which comprises the following raw materials, by weight, 0.8-1.2 parts of bromfenac sodium, 0.8-6 parts of moxifloxacin hydrochloride, 15-30 parts of gel matrix, 3-15 parts of sodium hyaluronate, 8-12 parts of osmotic pressure regulator, 7.0-9.0 parts of sodium citrate, 0.02-0.05 parts of citric acid and 950-1050 parts of purified water. Preferably, the gel matrix comprises one or more of hypromellose, carbomer, xanthan gum, hydroxyethyl cellulose. Preferably, the weight ratio of the bromfenac sodium to the moxifloxacin hydrochloride is 1:1-1:5; the weight ratio of the bromfenac sodium to the moxifloxacin hydrochloride is 1:1, 1:2, 1:3, 1:4 or 1:5. Preferably, the osmotic pressure regulator is selected from one or more of sorbitol, glycerol, propylene glycol and mannitol. In a second aspect, the invention provides a preparation method of the gel eye drops containing bromfenac sodium and moxifloxacin hydrochloride, which comprises the following steps: (1) Dispersing and dissolving the gel matrix and sodium h