CN112263545A - Ophthalmic composition and preparation method and application thereof - Google Patents
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Abstract
The present invention relates to an ophthalmic composition comprising chondroitin sulfate and olopatadine hydrochloride. The invention also relates to a preparation method of the ophthalmic composition, which comprises the following steps: s1, mixing the pH regulator, the osmotic pressure regulator and water for injection to obtain a mixed solution I; s2, homogenizing, stirring and mixing chondroitin sulfate, olopatadine hydrochloride and water for injection at 3000-4500r/min for 10-15min to obtain a mixed solution II; s3, mixing the mixed solution I and the mixed solution II with water for injection, and filtering to obtain the ophthalmic composition. In addition, the invention also relates to the application of the ophthalmic composition in preparing a medicament for improving eye irritation symptoms caused by treating corneal diseases. The ophthalmic composition provided by the invention can effectively relieve eye irritation caused by conventional dose of chondroitin sulfate in treatment of corneal diseases as eye drops, thereby increasing the medication compliance of patients and effectively shortening the treatment time of patients.
Description
Technical Field
The invention belongs to the technical field of medicines, and particularly relates to an ophthalmic composition, and a preparation method and application thereof.
Background
Chondroitin sulfate is an acidic mucopolysaccharide substance extracted and purified from animal tissues, is a main component forming intercellular substance, can accelerate wound healing, reduce scar tissue generation, is beneficial to migration of corneal epithelial cells, thereby promoting healing of corneal wound, is commonly used for treating keratitis, corneal ulcer and corneal injury, but in the treatment process, patients often complain about using chondroitin sulfate eye drops, and have eye stinging sensation, so that medication compliance is influenced, and the treatment time of the patients is prolonged, even fails.
Therefore, the problem at present is to provide an ophthalmic composition capable of reducing eye irritation symptoms (such as eye stinging sensation) caused when patients use chondroitin sulfate eye drops to treat corneal diseases, and a preparation method and application thereof, so as to increase the medication compliance of patients and effectively shorten the time for treating and recovering eyes.
Disclosure of Invention
Aiming at the defects in the prior art, the invention aims to provide an ophthalmic composition, and a preparation method and application thereof. The ophthalmic composition comprises chondroitin sulfate and olopatadine hydrochloride. The ophthalmic composition provided by the invention can reduce eye irritation symptoms (such as eye sting) caused by using chondroitin sulfate eye drops to treat corneal diseases for patients as eye drops, thereby increasing the medication compliance of the patients and effectively shortening the time for treating and recovering eyes.
To achieve the above object, the present invention provides, in a first aspect, an ophthalmic composition comprising chondroitin sulfate and olopatadine hydrochloride.
In some embodiments of the invention, the mass ratio of chondroitin sulfate to olopatadine hydrochloride is (0.28-0.57): 1.
According to the present invention, the ophthalmic composition further comprises an adjuvant; the auxiliary materials comprise an osmotic pressure regulator, a pH regulator and water for injection.
In some specific embodiments of the present invention, the ophthalmic composition comprises, based on the total weight of the ophthalmic composition:
Water for injection.
In some preferred embodiments of the present invention, the ophthalmic composition comprises, based on the total weight of the ophthalmic composition:
Water for injection.
According to the present invention, the osmotic pressure regulator includes at least one of sodium chloride, mannitol, potassium chloride, glycerin, sorbitol, glucose, and propylene glycol.
According to the invention, the pH regulator comprises at least one of citric acid, sodium citrate, sodium hydroxide, boric acid and borax.
In a second aspect, the present invention provides a method for preparing an ophthalmic composition according to the first aspect of the present invention, comprising the steps of:
s1, mixing the pH regulator, the osmotic pressure regulator and water for injection to obtain a mixed solution I;
s2, homogenizing, stirring and mixing chondroitin sulfate, olopatadine hydrochloride and water for injection at 3000-4500r/min for 10-15min to obtain a mixed solution II;
s3, mixing the mixed solution I and the mixed solution II with water for injection, and filtering to obtain the ophthalmic composition;
wherein the ratio of the amount of the water for injection in the step S1, the amount of the water for injection in the step S2, and the amount of the water for injection in the step S3 is 3:3:4 or 2:5: 3.
After preparation, the kinematic viscosity of the ophthalmic composition is 5.7-12.4 mm2And/s, so as to ensure the sufficient swelling and dissolution of the chondroitin sulfate.
Because chondroitin sulfate and olopatadine hydrochloride are likely to generate a coagulation phenomenon, the invention adopts proper homogenizing speed and mixing time to realize that two materials can be uniformly dispersed in water.
In a third aspect, the present invention provides the use of an ophthalmic composition according to the first aspect of the present invention or an ophthalmic composition prepared according to the method of the second aspect of the present invention in the manufacture of a medicament for the amelioration of symptoms of ocular irritation caused by the treatment of corneal diseases.
According to the invention, the corneal diseases comprise ocular corner ulcers and/or ocular corner erosions.
According to the invention, the medicament is an eye drop.
In a third aspect, the present invention provides the use of a combination of chondroitin sulfate and olopatadine hydrochloride in the preparation of an ophthalmic composition having a mass ratio of chondroitin sulfate to olopatadine hydrochloride of (0.28-0.57): 1.
In a fourth aspect, the present invention provides the use of an ophthalmic composition comprising olopatadine hydrochloride in the manufacture of a medicament for ameliorating eye irritation symptoms induced by the treatment of corneal diseases, wherein said ophthalmic composition comprises chondroitin sulfate, and wherein olopatadine hydrochloride in said ophthalmic composition is present in an amount sufficient to reduce or inhibit eye irritation symptoms induced by chondroitin sulfate in said ophthalmic composition; preferably, the mass ratio of the chondroitin sulfate to the olopatadine hydrochloride in the ophthalmic composition is (0.28-0.57): 1.
Compared with the prior art, the invention has the beneficial effects that:
the ophthalmic composition provided by the invention contains chondroitin sulfate and olopatadine hydrochloride, and when the ophthalmic composition is used as eye drops for treating corneal diseases, the olopatadine hydrochloride and chondroitin sulfate have a synergistic effect, so that the side effect of the chondroitin sulfate eye drops can be obviously reduced, the stimulation symptom of the chondroitin sulfate in the eye drops to eyes is reduced, the medication comfort of patients is improved, the medication compliance of the patients is increased, and the treatment and recovery time of the patients is effectively shortened.
Detailed Description
In order that the invention may be more readily understood, reference will now be made in detail to the following examples. It is to be understood that these examples are illustrative only and are not intended to limit the present invention.
Examples
Preparation of ophthalmic composition and quality inspection of eye drops
Example 1
(1) Preparation of ophthalmic compositions
Step S1, sodium citrate, sodium chloride and water for injection are mixed evenly to prepare a mixed solution I;
step S2, adding chondroitin sulfate and olopatadine hydrochloride into water for injection, homogenizing and stirring at 3000r/min for 10min to obtain a mixed solution II;
step S3, mixing the mixed solution I and the mixed solution II evenly, adding water for injection, filtering by a 0.22 mu m filter element, and filling to obtain the ophthalmic composition which comprises the following components by the total weight of the ophthalmic composition:
Water for injection;
the mass ratio of the chondroitin sulfate to the olopatadine hydrochloride in the ophthalmic composition is 0.34: 1;
the ratio of the amount of water for injection in step S1, the amount of water for injection in step S2, and the amount of water for injection in step S3 is 3:3: 4.
(2) Performance analysis of eye drops
The ophthalmic composition prepared in example 1 was used as eye drops, and accelerated stability examination was performed according to the principle of stability examination of formulations in "chinese pharmacopoeia" 9001, 2015 edition, and simultaneously, examination was performed according to the standard under the general rule of 0105 ophthalmic formulations, and the results are shown in table 1.
Table 1 test results of ophthalmic composition of example 1 as eye drops
As can be seen from table 1, the ophthalmic composition prepared in example 1 of the present invention can satisfy the basic requirements of pharmacopoeia for ophthalmic preparations as eye drops, and other components have good compatibility with chondroitin sulfate or olopatadine hydrochloride and do not interact with each other.
Example 2
(1) Preparation of ophthalmic compositions
Step S1, mixing borax, potassium chloride and water for injection uniformly to prepare a mixed solution I;
step S2, adding chondroitin sulfate and olopatadine hydrochloride into water for injection, homogenizing and stirring at 4500r/min for 15min to obtain a mixed solution II;
step S3, mixing the mixed solution I and the mixed solution II evenly, adding water for injection, filtering by a 0.22 mu m filter element, and filling to obtain the ophthalmic composition which comprises the following components by the total weight of the ophthalmic composition:
Water for injection;
the mass ratio of the chondroitin sulfate to the olopatadine hydrochloride in the ophthalmic composition is 0.28: 1;
the ratio of the amount of water for injection in step S1, the amount of water for injection in step S2, and the amount of water for injection in step S3 is 2:5: 3.
(2) Performance analysis of eye drops
The ophthalmic composition prepared in example 2 was used as eye drops, and accelerated stability examination was performed according to the principle of stability examination of formulations in "chinese pharmacopoeia" 9001, 2015 edition, and simultaneously, examination was performed according to the general guidelines of 0105 ophthalmic formulations, and the results are shown in table 2.
Table 2 test results of ophthalmic composition of example 2 as eye drops
As can be seen from table 2, the ophthalmic composition prepared in example 2 of the present invention can satisfy the basic requirements of pharmacopoeia for ophthalmic preparations as eye drops, and other components have good compatibility with chondroitin sulfate or olopatadine hydrochloride and do not interact with each other.
Example 3
(1) Preparation of ophthalmic compositions
The ophthalmic composition of this example was prepared as in example 1, except that the osmolality adjusting agent was glycerol and the pH adjusting agent was citric acid, to obtain an ophthalmic composition consisting of, based on the total weight of the ophthalmic composition:
Water for injection;
the mass ratio of the chondroitin sulfate to the olopatadine hydrochloride in the ophthalmic composition is 0.41: 1.
(2) Performance analysis of eye drops
The ophthalmic composition prepared in example 3 was used as eye drops, and accelerated stability examination was performed according to the principle of stability examination of formulations in "chinese pharmacopoeia" 9001, 2015 edition, and simultaneously, examination was performed according to the general guidelines of 0105 ophthalmic formulations, and the results are shown in table 3.
Table 3 test results of ophthalmic composition of example 3 as eye drops
As can be seen from table 3, the ophthalmic composition prepared in example 3 of the present invention can satisfy the basic requirements of pharmacopoeia for ophthalmic preparations as eye drops, and other components have good compatibility with chondroitin sulfate or olopatadine hydrochloride and do not interact with each other.
Example 4
(1) Preparation of ophthalmic compositions
The ophthalmic composition of this example was prepared as in example 1, except that the osmolality adjusting agent was glycerol and the pH adjusting agent was citric acid, to obtain an ophthalmic composition consisting of, based on the total weight of the ophthalmic composition:
Water for injection;
the mass ratio of the chondroitin sulfate to the olopatadine hydrochloride in the ophthalmic composition is 0.57: 1.
(2) Performance analysis of eye drops
The ophthalmic composition prepared in example 4 was used as eye drops, and accelerated stability examination was performed according to the principle of stability examination of formulations in "chinese pharmacopoeia" 9001, 2015 edition, and simultaneously, examination was performed according to the general guidelines of 0105 ophthalmic formulations, and the results are shown in table 4.
Table 4 test results of ophthalmic composition of example 4 as eye drops
As can be seen from table 4, the ophthalmic composition prepared in example 4 of the present invention can satisfy the basic requirements of pharmacopoeia for ophthalmic preparations as eye drops, and other components have good compatibility with chondroitin sulfate or olopatadine hydrochloride and do not interact with each other.
Comparative example 1
(1) Preparation of ophthalmic compositions
Step S1, sodium citrate, sodium chloride and water for injection are mixed evenly to prepare a mixed solution I;
step S2, adding chondroitin sulfate into water for injection, homogenizing and stirring at 3000r/min for 10min to obtain a mixed solution II;
step S3, mixing the mixed solution I and the mixed solution II evenly, adding water for injection, filtering by a 0.22 mu m filter element, and filling to obtain the ophthalmic composition which comprises the following components by the total weight of the ophthalmic composition:
chondroitin sulfate 5.0 wt%;
1.52 wt% of sodium chloride;
2.5 wt% of sodium citrate; and the remainder of
Water for injection;
the ratio of the amount of water for injection in step S1, the amount of water for injection in step S2, and the amount of water for injection in step S3 is 3:3: 4.
(2) Performance analysis of eye drops
The ophthalmic composition prepared in comparative example 1 was used as eye drops, and accelerated stability examination was performed according to the principle of stability examination of formulations in "chinese pharmacopoeia" 9001, 2015 edition, and simultaneously, examination was performed according to the criteria under the general rule of 0105 ophthalmic formulations, and the results are shown in table 5.
TABLE 5 examination results of the ophthalmic composition of comparative example 1 as eye drops
As is apparent from Table 5, the ophthalmic composition prepared in comparative example 1 of the present invention as eye drops can satisfy the basic requirements of pharmacopoeia for ophthalmic preparations.
Comparative example 2
(1) Preparation of ophthalmic compositions
Step S1, sodium citrate, sodium chloride and water for injection are mixed evenly to prepare a mixed solution I;
step S2, adding chondroitin sulfate into water for injection, homogenizing and stirring at 3000r/min for 10min to obtain a mixed solution II;
step S3, mixing the mixed solution I and the mixed solution II evenly, adding water for injection, filtering by a 0.22 mu m filter element, and filling to obtain the ophthalmic composition which comprises the following components by the total weight of the ophthalmic composition:
chondroitin sulfate 3.0 wt%;
0.21 wt% of sodium chloride;
1.1 wt% of sodium citrate; and the remainder of
Water for injection;
the ratio of the amount of water for injection in step S1, the amount of water for injection in step S2, and the amount of water for injection in step S3 is 3:3: 4.
(2) Performance analysis of eye drops
The ophthalmic composition prepared in comparative example 2 was used as eye drops, and accelerated stability examination was performed according to the principle of stability examination of formulations in "chinese pharmacopoeia" 9001, 2015 edition, and simultaneously, examination was performed according to the criteria under the general rule of 0105 ophthalmic formulations, and the results are shown in table 6.
TABLE 6 examination results of the ophthalmic composition of comparative example 2 as eye drops
As is apparent from Table 6, the ophthalmic composition prepared in comparative example 2 of the present invention as eye drops can satisfy the basic requirements of pharmacopoeia for ophthalmic preparations.
Comparative example 3
(1) Preparation of ophthalmic compositions
The ophthalmic composition of this example was prepared as in example 1, except that the osmolality adjusting agent was glycerol and the pH adjusting agent was citric acid, to obtain an ophthalmic composition consisting of, based on the total weight of the ophthalmic composition:
Water for injection;
the mass ratio of the chondroitin sulfate to the olopatadine hydrochloride in the ophthalmic composition is 1: 1.
(2) Performance analysis of eye drops
The ophthalmic composition prepared in comparative example 3 was used as eye drops, and accelerated stability examination was performed according to the principle of stability examination of formulations in "chinese pharmacopoeia" 9001, 2015 edition, and simultaneously, examination was performed according to the criteria under the general rule of 0105 ophthalmic formulations, and the results are shown in table 7.
TABLE 7 examination results of the ophthalmic composition of comparative example 3 as eye drops
As can be seen from table 7, the ophthalmic composition prepared in comparative example 3 of the present invention can satisfy the basic requirements of pharmacopoeia for ophthalmic preparations as eye drops, and other ingredients have good compatibility with chondroitin sulfate or olopatadine hydrochloride, and no interaction occurs.
Comparative example 4
(1) Preparation of ophthalmic compositions
The ophthalmic composition of this example was prepared as in example 1, except that the osmolality adjusting agent was glycerol and the pH adjusting agent was citric acid, to obtain an ophthalmic composition consisting of, based on the total weight of the ophthalmic composition:
Water for injection;
the mass ratio of the chondroitin sulfate to the olopatadine hydrochloride in the ophthalmic composition is 2: 1.
(2) Performance analysis of eye drops
The ophthalmic composition prepared in comparative example 4 was used as eye drops, and accelerated stability examination was performed according to the principle of stability examination of formulations in "chinese pharmacopoeia" 9001, 2015 edition, and simultaneously, examination was performed according to the criteria under the general rule of 0105 ophthalmic formulations, and the results are shown in table 8.
TABLE 8 examination results of the ophthalmic composition of comparative example 4 as eye drops
As can be seen from table 8, the ophthalmic composition prepared in comparative example 4 of the present invention can satisfy the basic requirements of pharmacopoeia for ophthalmic preparations as eye drops, and other ingredients have good compatibility with chondroitin sulfate or olopatadine hydrochloride, and no interaction occurs.
Comparative example 5
(1) Preparation of ophthalmic compositions
The ophthalmic composition of this example was prepared as in example 1, except that the osmolality adjusting agent was glycerol and the pH adjusting agent was citric acid, to obtain an ophthalmic composition consisting of, based on the total weight of the ophthalmic composition:
Water for injection;
the mass ratio of the chondroitin sulfate to the olopatadine hydrochloride in the ophthalmic composition is 0.2: 1.
(2) Performance analysis of eye drops
The ophthalmic composition prepared in comparative example 5 was used as eye drops, and accelerated stability examination was performed according to the principle of stability examination of formulations in "chinese pharmacopoeia" 9001, 2015 edition, and simultaneously, examination was performed according to the criteria under the general rule of 0105 ophthalmic formulations, and the results are shown in table 9.
TABLE 9 examination results of the ophthalmic composition of comparative example 5 as eye drops
As can be seen from table 9, the ophthalmic composition prepared in comparative example 5 of the present invention can satisfy the basic requirements of pharmacopoeia for ophthalmic preparations as eye drops, and other ingredients have good compatibility with chondroitin sulfate or olopatadine hydrochloride, and no interaction occurs.
Animal experiments
Wistar rats 180 in half of male and female and 80-120g in weight are selected and randomly divided into 9 groups of 20 rats. Each group was modeled for conjunctivitis: the mouse head was fixed, the face was pulled down, and 200. mu.l of 10 wt% croton oil-based inflammatory agent was dropped into each eye, and the solution was left in the conjunctival sac for 45 seconds and washed away with physiological saline. According to ocular inflammatory manifestations: the ophthalmic compositions of examples 1 to 4 and comparative examples 1 to 5 were dropped into the experimental group after successful inflammation observation, the ophthalmic compositions of examples 1 to 4 and comparative examples 1 to 5 were dropped into the experimental group at 2 to 3 drops, the blank control group was dropped with an equal volume of physiological saline, and according to "eye irritation response scoring criteria" of new drug research guideline of ministry of health, at different times after administration, the cornea, iris and conjunctiva were observed with naked eyes or with a slit lamp for the presence of eyelid edema, conjunctival hyperemia and burning sensation of pain, and the scoring criteria are shown in table 10, and then the total score was calculated according to the scoring criteria, and the irritation was judged according to the total score, which is shown in table 11, the average score (, total score/20) was calculated, and the evaluation results are shown in table 12.
TABLE 10 Scoring criteria
TABLE 11 irritation test standards
TABLE 12 evaluation results of various ophthalmic compositions
As can be seen from table 12, the eye irritation symptoms of rats with inflammation of conjunctiva of eyes with chondroitin sulfate eye drops containing olopatadine hydrochloride are obviously lower than those of the rat without olopatadine hydrochloride at different times after the drug is applied, and the eye drops composed of each prescription have no obvious difference in eye irritation after the drug is applied for 12 hours.
It can be seen from the comparison between the examples and the comparative examples that, the ophthalmic pharmaceutical composition provided by the examples 1 to 4 of the present invention reduces the conventional dosage of chondroitin sulfate by combining chondroitin sulfate and olopatadine hydrochloride, and can significantly reduce the eye burning stimulation caused by the conventional chondroitin sulfate eye drops, thereby improving the medication comfort of patients, increasing the medication compliance of patients, and further shortening the recovery time.
The present invention is not limited to the above-described embodiments, and it will be apparent to those skilled in the art that various modifications and improvements can be made without departing from the principle of the present invention, and such modifications and improvements are also considered to be within the scope of the present invention. Those not described in detail in this specification are within the skill of the art.
Claims (12)
1. An ophthalmic composition, which comprises chondroitin sulfate and olopatadine hydrochloride, wherein the mass ratio of the chondroitin sulfate to the olopatadine hydrochloride is (0.28-0.57): 1.
2. The ophthalmic composition of claim 1, wherein the ophthalmic composition further comprises an adjuvant; the auxiliary materials comprise an osmotic pressure regulator, a pH regulator and water for injection.
3. The ophthalmic composition of claim 1, wherein the ophthalmic composition comprises, based on the total weight of the ophthalmic composition:
4. the ophthalmic composition of claim 3, wherein the ophthalmic composition comprises, based on the total weight of the ophthalmic composition:
5. the ophthalmic composition according to any one of claims 2 to 4, wherein the tonicity modifier comprises at least one of sodium chloride, mannitol, potassium chloride, glycerin, sorbitol, glucose and propylene glycol.
6. The ophthalmic composition according to any one of claims 2-4, wherein the pH adjusting agent comprises at least one of citric acid, sodium citrate, sodium hydroxide, boric acid and borax.
7. A method of making an ophthalmic composition according to any one of claims 1-6, comprising the steps of:
s1, mixing the pH regulator, the osmotic pressure regulator and water for injection to obtain a mixed solution I;
s2, homogenizing, stirring and mixing chondroitin sulfate, olopatadine hydrochloride and water for injection at 3000-4500r/min for 10-15min to obtain a mixed solution II;
s3, mixing the mixed solution I and the mixed solution II with water for injection, and filtering to obtain the ophthalmic composition;
the kinematic viscosity of the ophthalmic composition is 5.7-12.4 mm2/s。
8. Use of an ophthalmic composition according to any one of claims 1 to 6 or prepared according to the method of claim 7 for the preparation of a medicament for ameliorating symptoms of ocular irritation caused by the treatment of corneal diseases.
9. Use according to claim 8, characterized in that said corneal diseases comprise ocular corner ulcers and/or ocular corner erosions.
10. The use of claim 8, wherein the medicament is an eye drop.
11. Use of a combination of chondroitin sulphate and olopatadine hydrochloride for the preparation of an ophthalmic composition, characterized in that the mass ratio of chondroitin sulphate to olopatadine hydrochloride in the ophthalmic composition is (0.28-0.57): 1.
12. Use of an ophthalmic composition comprising olopatadine hydrochloride in the manufacture of a medicament for ameliorating eye irritation symptoms induced by the treatment of corneal diseases, wherein the ophthalmic composition comprises chondroitin sulfate and the olopatadine hydrochloride in the ophthalmic composition is present in an amount sufficient to reduce or inhibit the eye irritation symptoms induced by chondroitin sulfate in the ophthalmic composition; preferably, the mass ratio of the chondroitin sulfate to the olopatadine hydrochloride in the ophthalmic composition is (0.28-0.57): 1.
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| CN117338787A (en) * | 2023-11-24 | 2024-01-05 | 南京恒道医药科技股份有限公司 | Ophthalmic pharmaceutical composition and preparation method thereof |
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