阅读说明：本技术 防治nitm 的药物组合物及其医药用途 (Pharmaceutical composition for preventing and treating NITM and medical application thereof ) 是由 刘继东 王宁利 郭雷 杨强 高坤 李林蔚 顾红 孙洋 付乐 于 2018-11-05 设计创作，主要内容包括：本发明属于医药领域,涉及一种防治NITM的药物组合物及其医药用途。具体地,所述药物组合物为眼用药物组合物例如眼用制剂。具体地,本发明涉及一种药物组合物,其包含0.001％－0.2％的阿托品或其可药用盐,以及一种或多种药学上可接受的辅料；其中,所述药物组合物的pH值为4.0－6.5；所述药物组合物包含0.5％－5％的pH调节剂,所述pH调节剂选自磷酸二氢钠、磷酸氢二钠、枸橼酸、枸橼酸盐、硼酸和硼酸盐中的任意一种或多种。本发明的药物组合物能够有效地治疗和/或预防NITM,具有良好的应用前景。(The invention belongs to the field of medicines, and relates to a medicinal composition for preventing and treating NITM and medical application thereof. In particular, the pharmaceutical composition is an ophthalmic pharmaceutical composition such as an ophthalmic formulation. Specifically, the invention relates to a pharmaceutical composition, which comprises 0.001-0.2% of atropine or pharmaceutically acceptable salts thereof and one or more pharmaceutically acceptable auxiliary materials; wherein the pH value of the pharmaceutical composition is 4.0-6.5; the pharmaceutical composition comprises 0.5-5% of pH regulator, wherein the pH regulator is selected from one or more of sodium dihydrogen phosphate, disodium hydrogen phosphate, citric acid, citrate, boric acid and borate. The pharmaceutical composition can effectively treat and/or prevent NITM, and has good application prospect.)

A pharmaceutical composition comprising 0.001% -0.2% atropine or a pharmaceutically acceptable salt thereof, and one or more pharmaceutically acceptable excipients;

wherein the content of the first and second substances,

the pH value of the pharmaceutical composition is 4.0-6.5;

the pharmaceutical composition comprises 0.05% -5% of pH regulator, wherein the pH regulator is selected from one or more of sodium dihydrogen phosphate, disodium hydrogen phosphate, citric acid, citrate, boric acid and borate.

The pharmaceutical composition according to claim 1, which is an ophthalmic formulation, such as an ophthalmic liquid formulation (e.g. eye drops, eye washes or intraocular injection solutions), an ophthalmic semi-solid formulation (e.g. eye ointments, eye creams or eye gels) or an ophthalmic solid formulation (e.g. eye films, eye pills or eye inserts); alternatively, the ophthalmic liquid preparation may be packaged in solid form, prepared with a solvent, and prepared as a solution or suspension just before use.

The pharmaceutical composition according to claim 2, wherein the concentration or content of atropine or a pharmaceutically acceptable salt thereof is 0.001% to 0.1%, preferably 0.005% to 0.05%, more preferably 0.005% to 0.02%, further preferably 0.005% to 0.015%, particularly preferably 0.01%; preferably, the pharmaceutically acceptable salt of atropine is atropine sulfate.

The pharmaceutical composition according to any one of claims 1 to 3, wherein the pH of the pharmaceutical composition is 4.0-6.0, preferably 4.5-6.0, more preferably 4.5-5.5.

The pharmaceutical composition according to any one of claims 1 to 3, wherein,

the content of the pH regulator is 0.5% -5%, more preferably 1% -3%, further preferably 1.5% -2.5%, and particularly preferably 1.75% -2.0%;

preferably, the citrate is sodium citrate and/or the borate is sodium tetraborate.

The pharmaceutical composition of any one of claims 1 to 3, wherein the pharmaceutical composition comprises 0.5-3%, 1-3%, 1.5-2.5%, 1.75-2.25%, or 1.75-2% boric acid.

The pharmaceutical composition according to any one of claims 1 to 3, wherein the pharmaceutical composition further comprises any one or more selected from the group consisting of 1) to 5) below:

1) a thickening agent, and the thickening agent is selected from one or more of hypromellose, sodium carboxymethylcellulose and sodium hyaluronate; preferably, the thickener is present in an amount of 0.01% to 5%, preferably 0.5% to 3%, more preferably 0.5% to 1.5%, and particularly preferably 0.8% to 1.2%.

2) An osmotic pressure regulator, for example, any one or more selected from glycerol, mannitol, propylene glycol, sodium chloride, potassium chloride;

3) preservatives, for example, selected from any one or more of benzalkonium chloride, paraben bacteriostatic agents, polyquaternium;

4) a stabilizer, for example, one or more selected from disodium edetate and calcium disodium edetate;

5) an appropriate amount of water.

The pharmaceutical composition according to any one of claims 1 to 3, wherein the components and content of the pharmaceutical composition are selected from any one of the following groups (1) to (8):

(1)

(2)

(3)

(4)

(5)

(6)

(7)

(8)

use of atropine or a pharmaceutically acceptable salt thereof or a pharmaceutical composition comprising atropine or a pharmaceutically acceptable salt thereof for the manufacture of a medicament for the treatment and/or prevention of NITM;

preferably, the pharmaceutically acceptable salt is atropine sulfate;

preferably, the pharmaceutical composition further comprises one or more pharmaceutically acceptable excipients;

preferably, the pharmaceutical composition is the pharmaceutical composition of any one of claims 1 to 8.

Use according to claim 9, wherein the medicament is an ophthalmic formulation, preferably an eye drop.

The use according to claim 10, wherein the eye drop is administered once daily or every other day, 1-2 drops each; preferably, the eye drops are instilled in the conjunctival sac.

The use according to claim 10 or 11, wherein the subject of eye drops is a person with near vision or a person susceptible to myopia;

preferably, the near sighted person is a myopic patient or a non-myopic patient;

preferably, the person susceptible to myopia is a person 6-18 years old;

preferably, the person susceptible to myopia is a myope or a non-myope.

A kit product comprising a medicament and product instructions;

wherein the drug is atropine or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition containing the atropine or the pharmaceutically acceptable salt thereof;

preferably, the pharmaceutically acceptable salt is atropine sulfate;

preferably, the pharmaceutical composition further comprises one or more pharmaceutically acceptable excipients;

preferably, the pharmaceutical composition is a pharmaceutical composition according to any one of claims 1 to 8;

preferably, the medicament is an ophthalmic formulation, preferably an eye drop.

The kit product of claim 11 wherein the product instructions state that the eye drop is administered once daily or every other day, 1-2 drops each time;

preferably, the product instructions further recite that the eye drop is instilled in the conjunctival sac.

The kit product of claim 13 or 14, wherein the product instructions recite that the subject of the eye drops is a myopic or a non-myopic patient;

preferably, the product specification states that the subject of the eye drops is a near-sighted person;

preferably, the product specification states that the subject of the eye drops is a myopic or non-myopic patient with near vision;

preferably, the product specification states that the subject of the eye drops is a person susceptible to myopia;

preferably, the product instructions recite that the subject of the eye drops is a person 6-18 years old, such as a myope 6-18 years old or a non-myope 6-18 years old.

Atropine or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising atropine or a pharmaceutically acceptable salt thereof, for use in the treatment and/or prevention of NITM;

preferably, the pharmaceutically acceptable salt is atropine sulfate;

preferably, the pharmaceutical composition further comprises one or more pharmaceutically acceptable excipients;

preferably, the pharmaceutical composition is the pharmaceutical composition of any one of claims 1 to 8.

Atropine or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising atropine or a pharmaceutically acceptable salt thereof according to claim 16, wherein the pharmaceutical composition is an ophthalmic formulation, preferably an eye drop.

Atropine or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising atropine or a pharmaceutically acceptable salt thereof according to claim 17, wherein the eye drop is administered once daily or every other day, 1-2 drops at a time; preferably, the eye drops are instilled in the conjunctival sac.

Atropine or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising atropine or a pharmaceutically acceptable salt thereof according to claim 17 or 18, wherein the subject of eye drops is a person with close or a person susceptible to myopia;

preferably, the near sighted person is a myopic patient or a non-myopic patient;

preferably, the person susceptible to myopia is a person 6-18 years old.

A method for the treatment and/or prevention of NITM comprising the step of administering to a subject in need thereof an effective amount of a drug, wherein the drug is atropine or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising atropine or a pharmaceutically acceptable salt thereof;

preferably, the pharmaceutically acceptable salt is atropine sulfate;

preferably, the pharmaceutical composition further comprises one or more pharmaceutically acceptable excipients;

preferably, the pharmaceutical composition is the pharmaceutical composition of any one of claims 1 to 8.

A method for the treatment and/or prophylaxis of NITM according to claim 20, wherein the pharmaceutical composition is an ophthalmic formulation, preferably eye drops.

The method of treating and/or preventing NITM according to claim 21 wherein the eye drops are administered once daily or every other day, 1-2 drops each; preferably, administration is done before bedtime;

preferably, the eye drops are instilled in the conjunctival sac.

A method of treatment and/or prevention of NITM according to claim 21 or 22 wherein the subject of eye drops is a myopic or non-myopic patient;

preferably, the subject of the eye drops is a short-distance eyeman;

preferably, the subject of the eye drops is a myopic or non-myopic patient who uses the eye at near distance;

preferably, the subject of eye drops is a person susceptible to myopia, for example a person 6-18 years old;

preferably, the person susceptible to myopia is a myope or a non-myope.