CN112656759A - Rudexilvir eye drops and preparation method and application thereof - Google Patents
Rudexilvir eye drops and preparation method and application thereof Download PDFInfo
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- CN112656759A CN112656759A CN202110092173.0A CN202110092173A CN112656759A CN 112656759 A CN112656759 A CN 112656759A CN 202110092173 A CN202110092173 A CN 202110092173A CN 112656759 A CN112656759 A CN 112656759A
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- eye drop
- reed
- seivir
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- virus infection
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- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
Abstract
The invention belongs to the technical field of medicinal preparations, and particularly relates to a Reidesciclovir eye drop, a preparation method and application thereof, which contain 0.1-20.0% (W/V) of Reidesciclovir, 0.1-4.0% (W/V) of osmotic pressure regulator, 0.1-5.0% (W/V) of antioxidant, 0.1-5.0% (W/V) of pH regulator, 0.1-1% (W/V) of bacteriostatic agent and 65.0-99.5% (W/V) of solvent, and are used for treating eyelid virus infection, conjunctival virus infection, corneal virus infection and retinal virus infection.
Description
Technical Field
The invention belongs to the technical field of pharmaceutical preparations, and particularly relates to an eye drop and a preparation method and application thereof.
Background
Reddesivir (Remdesivir) is a viral RNA-dependent RNA polymerase (rdrp) inhibitor developed by Gilidd Science, Inc. and uses the prodrug design of ProTide in its molecular structure. Previously, the clinically developed indications for reicepvir have all surrounded ebola virus infection. The structural formula is as follows:
reed-civir qualifies as an orphan drug for the treatment of ebola virus infection in the us at 9 months 2015 and in europe at 1 month 2016, respectively. The currently marketed RudeSewei preparation is a freeze-dried preparation, can only be used by injection, and has poor stability and easy color change after long-term storage. For patients with eyes infected by virus, the blood brain barrier is difficult to pass through by in vivo injection, and a preparation capable of directly acting on eyes needs to be developed to make up for the clinical medication requirement.
Disclosure of Invention
Currently marketed Rudexiwei preparations have poor stability, are easy to discolor after being stored for a long time and can only be used by injection. The invention provides a novel eye drop containing the Reidesvir and application of the eye drop in treating ocular virus infection by researching the prescription and process of the eye drop containing the Reidesvir.
A Rudexiluwei eye drop comprises main active components of Rudexiluwei, osmotic pressure regulator, antioxidant, PH regulator, bacteriostatic agent and solvent, wherein the content of the Rudexiluwei is 0.1-20.0% (W/V); the content of the osmotic pressure regulator is 0.1-4.0% (W/V), and the content of the antioxidant is 0.1-5.0% (W/V); the content of the PH regulator is 0.1-5.0% (W/V); the content of the bacteriostatic agent is 0.1-1% (W/V); the content of the solvent is 65.0-99.5% (W/V).
The osmotic pressure regulator is any one of glycerol, sodium chloride and potassium chloride, and the dosage of the osmotic pressure regulator is 0.1-4.0% (W/V); preferably glycerol.
The antioxidant is any one of vitamin E, vitamin C, sodium sulfite, sodium metabisulfite, dibutyl phenol, sodium bisulfite, sodium thiosulfate, tert-butyl p-hydroxyanisole (bha) and dibutyl phenol (bhg), and the dosage of the antioxidant is 0.1-5.0% (W/V), preferably vitamin E.
The pH regulator is any one of boric acid, hydrochloric acid, sodium hydroxide, disodium hydrogen phosphate and sodium dihydrogen phosphate, and the dosage of the pH regulator is 0.1-5.0% (W/V), preferably boric acid.
The bacteriostatic agent is any one of benzalkonium chloride, benzyl alcohol, butyl hydroxybenzoate, phenol and chlorobutanol, and the dosage of the bacteriostatic agent is 0.1-1% (W/V), preferably benzalkonium chloride.
The solvent is selected from medium-chain triglyceride and water for injection, and the dosage of the solvent is 65.0-99.5% (W/V), and preferably the medium-chain triglyceride.
The specification of the eye drop is 1 mg-200 mg/ml.
The preparation method of the Rudexiluwei eye drops comprises the following steps:
adding benzalkonium chloride and boric acid into glycerol, heating to 60 ℃, stirring at a speed of 50rpm for 30min to dissolve;
adding vitamin E and Ruidexilvir, stirring and dissolving;
thirdly, diluting the mixture to the full preparation amount by using sterile medium chain triglyceride, adjusting the pH value to 5.0-7.0 by using 0.1mol/L hydrochloric acid solution, filtering the mixture by using a 0.22 mu m microporous filter membrane, and aseptically filling the mixture into an eye drop bottle to obtain the eye drop.
The application of the Rdesavir eye drops is used for treating eyelid virus infection, conjunctival virus infection, corneal virus infection and retinal virus infection.
The active ingredients of the Rudexiluwei eye drops prepared by the invention can be directly absorbed by eyes to focus, and the eye virus infection can be controlled, so that the Rudexiluwei eye drops have the advantages of high bioavailability, good compliance, stable and controllable quality, convenience in carrying and use, suitability for industrial production and the like.
Detailed Description
The following are specific embodiments of the present invention, and the examples are intended to further illustrate the invention and not to limit it. All technical solutions equivalent to the present invention belong to the protection scope of the present invention.
Example 1
Name of ingredient | Weight (D) |
Ruidexiwei (Ridexil) | 3g |
Glycerol | 20g |
Vitamin E | 20g |
Boric acid | 2g |
Benzalkonium chloride | 0.5g |
Medium chain triglycerides | 955ml |
The preparation method comprises the following steps:
adding benzalkonium chloride 0.5g and boric acid 2g into glycerol 20g, heating to 60 deg.C, stirring at 50rpm for 30min to dissolve; then adding 20g of vitamin E and 3g of Reidesvir, stirring at the speed of 100rpm for 30min to dissolve completely; diluting with sterile medium chain triglyceride 955ml to full dose, adjusting pH to 6.0, filtering with 0.22 μm microporous membrane, and aseptically packaging in eye drop bottle. Each bottle is filled with 10ml, and 100 bottles are filled.
Example 2
The preparation method comprises the following steps:
adding benzalkonium chloride 0.5g and boric acid 4g into glycerol 40g, heating to 60 deg.C, stirring at 50rpm for 20min to dissolve; then adding 20g of vitamin E and 1g of Reidesvir, stirring at the speed of 100rpm for 20min to dissolve completely; diluting with 935ml sterile medium chain triglyceride to full dose, adjusting pH to 5.0, filtering with 0.22 μm microporous membrane, and aseptically packaging in eye drop bottle. Each bottle is filled with 10ml, and 100 bottles are filled.
Example 3
Name of ingredient | Weight (D) |
Ruidexiwei (Ridexil) | 10g |
Glycerol | 20g |
Vitamin E | 40g |
Boric acid | 1g |
Benzalkonium chloride | 0.5g |
Medium chain triglycerides | 929 |
The preparation method comprises the following steps:
adding benzalkonium chloride 0.5g and boric acid 1g into glycerol 20g, heating to 60 deg.C, stirring at 50rpm for 30min to dissolve; then adding 40g of vitamin E and 10g of Reidesvir, stirring at the speed of 100rpm for 50min to dissolve completely; diluting with 929ml sterile medium chain triglyceride to full dose, adjusting pH to 7.0, filtering with 0.22 μm microporous membrane, and aseptically packaging in eye drop bottle. Each bottle is filled with 10ml, and 100 bottles are filled.
Experimental example one drop eye drop stability test
The experimental research method is carried out according to the relevant requirements of Chinese pharmacopoeia, and the stability of the eye drops is tested. The RudeSewei eye drops in the embodiments 1, 2 and 3 are stored for 6 months at 40 +/-2 ℃, and indexes such as properties, osmotic pressure, pH value, related substances, content and the like of the sample are examined at 0 month, 1 month, 2 months, 3 months and 6 months. The relevant parameters were sampled and determined to obtain the corresponding data, as shown in the following table:
TABLE 1 sample test data
The detection data result of the test example proves that the sample prepared by the method has good stability, and the indexes of characters, osmotic pressure, pH value, related substances, content and the like are basically not obviously changed in the placing process, so that the quality of a patient in the using process can be ensured.
Experimental example two
The safety of the ophthalmic formulation of ridciclovir was examined using the samples prepared in example 1. The irritation test of the rabbit eyes by single administration and multiple administrations is observed. Before the test, both eyes of each rabbit were examined, rabbits without eye irritation symptom, corneal defect and conjunctival injury were selected, and 24 healthy rabbits were selected, half of them were divided into 8 groups at random. The ophthalmic solution of Ready-Wevir was dropped into the left eye, and the same amount of sterile water for injection was dropped into the right eye, followed by gentle palpebral closure for 20 seconds. The eye local reaction conditions of 0h, 12h, 24h, 48h and 72h after the administration are observed by taking corneal opacity, iris congestion, conjunctival swelling, conjunctival congestion and conjunctival secretion as the investigation indexes. The results are as follows:
the test result shows that the Rudexilawi eye drop product has no stimulation to eyes and is applied to ocular virus infection. Can improve the life quality of patients and has wide application value.
Claims (9)
1. A Rudesiwei eye drop is characterized in that: comprises the main active ingredients of Reidesciclovir, osmotic pressure regulator, antioxidant, PH regulator, bacteriostatic agent and solvent, wherein the content of Reidesciclovir is 0.1-20.0% (W/V); the content of the osmotic pressure regulator is 0.1-4.0% (W/V), and the content of the antioxidant is 0.1-5.0% (W/V); the content of the PH regulator is 0.1-5.0% (W/V); the content of the bacteriostatic agent is 0.1-1% (W/V); the content of the solvent is 65.0-99.5% (W/V).
2. A reed-seivir eye drop according to claim 1 characterized in that: the osmotic pressure regulator is any one of glycerol, sodium chloride and potassium chloride.
3. A reed-seivir eye drop according to claim 1 characterized in that: the antioxidant is selected from one of vitamin E, vitamin C, sodium sulfite, sodium pyrosulfite, dibutylphenol, sodium bisulfite, sodium thiosulfate, tert-butyl p-hydroxyanisole (bha) and dibutylphenol (bhg).
4. A reed-seivir eye drop according to claim 1 characterized in that: the pH regulator is any one of boric acid, hydrochloric acid, sodium hydroxide, disodium hydrogen phosphate and sodium dihydrogen phosphate.
5. A reed-seivir eye drop according to claim 1 characterized in that: the bacteriostatic agent is any one of benzalkonium chloride, benzyl alcohol, butyl hydroxybenzoate, phenol and chlorobutanol.
6. A reed-seivir eye drop according to claim 1 characterized in that: the solvent is any one of medium-chain triglyceride and water for injection.
7. A ridciclovir eye drop as claimed in any one of claims 1-6 wherein: the specification of the eye drop is 1 mg-200 mg/ml.
8. A method for preparing a reed-seivir eye drop according to claim 1, characterized in that: the method comprises the following steps:
adding benzalkonium chloride and boric acid into glycerol, heating and stirring for dissolving;
adding vitamin E and Ruidexilvir, stirring and dissolving;
and thirdly, diluting the mixture to the full preparation amount by using sterile medium-chain triglyceride, adjusting the pH value to 5.0-7.0, filtering the mixture through a 0.22 mu m microporous filter membrane, and aseptically filling the mixture into eyedrops to obtain the eyedrops.
9. Use of ophthalmic reed-seivir drops according to claim 1, characterized in that: can be used for treating eyelid virus infection, conjunctival virus infection, corneal virus infection, and retinal virus infection.
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Cited By (1)
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WO2022047441A1 (en) * | 2020-08-28 | 2022-03-03 | Emphascience, Inc. | Formulations of anti-viral compounds |
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CN107929235A (en) * | 2016-10-13 | 2018-04-20 | 沈阳兴齐眼药股份有限公司 | A kind of ophthalmically acceptable preparation of tacrolimus and preparation method thereof |
US20190083525A1 (en) * | 2017-07-11 | 2019-03-21 | Gilead Sciences, Inc. | Compositions comprising an rna polymerase inhibitor and cyclodextrin for treating viral infections |
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CN111991375A (en) * | 2020-09-25 | 2020-11-27 | 中国药科大学 | Reed-ciclovir liposome for aerosol inhalation and preparation method thereof |
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Patent Citations (5)
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CN107929235A (en) * | 2016-10-13 | 2018-04-20 | 沈阳兴齐眼药股份有限公司 | A kind of ophthalmically acceptable preparation of tacrolimus and preparation method thereof |
US20190083525A1 (en) * | 2017-07-11 | 2019-03-21 | Gilead Sciences, Inc. | Compositions comprising an rna polymerase inhibitor and cyclodextrin for treating viral infections |
US20200237689A1 (en) * | 2018-11-15 | 2020-07-30 | Bluewillow Biologics, Inc. | Prevention and treatment of coronavirus and other respiratory infections using nanoemulsion compositions |
CN111956630A (en) * | 2020-08-20 | 2020-11-20 | 大连理工大学 | Liquid preparation for atomizer of Reidesciclovir, preparation method and application thereof |
CN111991375A (en) * | 2020-09-25 | 2020-11-27 | 中国药科大学 | Reed-ciclovir liposome for aerosol inhalation and preparation method thereof |
Non-Patent Citations (2)
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BRANDI N. WILLIAMSON ET AL.: "Clinical benefit of remdesivir in rhesus macaques infected with SARS-CoV-2", 《NATURE》 * |
SAWITTREE SAHAKIJPIJARN ET AL.: "Development of Remdesivir as a Dry Powder for Inhalation by Thin Film Freezing", 《PHARMACEUTICS》 * |
Cited By (2)
Publication number | Priority date | Publication date | Assignee | Title |
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WO2022047441A1 (en) * | 2020-08-28 | 2022-03-03 | Emphascience, Inc. | Formulations of anti-viral compounds |
GB2613516A (en) * | 2020-08-28 | 2023-06-07 | Sayvaa Pharmaceuticals Inc | Formulations of anti-viral compounds |
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