CN105935442A - Pharmaceutical composition for treatment of glaucoma - Google Patents
Pharmaceutical composition for treatment of glaucoma Download PDFInfo
- Publication number
- CN105935442A CN105935442A CN201610010468.8A CN201610010468A CN105935442A CN 105935442 A CN105935442 A CN 105935442A CN 201610010468 A CN201610010468 A CN 201610010468A CN 105935442 A CN105935442 A CN 105935442A
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- CN
- China
- Prior art keywords
- pharmaceutical composition
- glaucoma
- intraocular pressure
- treatment
- pharmaceutically acceptable
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- A61K38/39—Connective tissue peptides, e.g. collagen, elastin, laminin, fibronectin, vitronectin, cold insoluble globulin [CIG]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/045—Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
- A61K31/047—Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates having two or more hydroxy groups, e.g. sorbitol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/498—Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
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- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Biomedical Technology (AREA)
- Zoology (AREA)
- Gastroenterology & Hepatology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The invention discloses a pharmaceutical composition for the treatment of glaucoma. The composition includes brimonidine or a pharmaceutically acceptable salt thereof and at least one medicament for lowering intraocular pressure and optionally at least one pharmaceutically acceptable carrier. The active ingredients in all cases are in free form or in the form of pharmaceutically acceptable salt. The composition is for simultaneous, separate or sequential usage; and preferably, the medicament for lowering intraocular pressure is lutein. The invention has the advantage that medicaments with different mechanisms of action area combined to give full play to complementary synergistic effects of the medicaments and to reduce adverse reactions associated with the increase of a certain dose. The pharmaceutical composition can relieve symptoms in a short period of time, and can be effective in the treatment of glaucoma.
Description
Technical field
The present invention relates to pharmaceutical technology field, be specifically related to a kind of pharmaceutical composition treating glaucoma and application thereof.
Background technology
Glaucoma is ophthalmology one commonly encountered diseases, and harm visual function is very big, is also one of modal diseases causing blindness, can bring blind misery to patient for various reasons.The common intraocular pressure of glaucoma increases and with symptoms such as circumcorneal injection, platycoria, visual acuity, headache, nausea and vomiting.When the intraocular pressure of glaucoma has exceeded the limit that eyeball inner tissue, especially retina can bear, then can bring the functional pathological changes of eyes, bring great misery to extensive patients.
Alphagan (brimonidine) is alpha-2 adrenergic receptor agonists, and it has dual mechanism of action: had both reduced the generation of aqueous humor, and had increased again uveoscleral outflow.Betaxolol (betaxolol) is β-1 Adrenergic receptor blocker, and its mechanism of action is to reduce aqueous humor to generate, and does not affect pupil size and regulative mechanism, long action time, and hypotensive effect can maintain 12h.This product has calcium antagonism, the blood vessel that can directly expand, and improves ocular blood supply, thus shields optic nerve.
Although prior art also having the medicine for treating glaucoma, but the therapeutic effect of drug alone being difficult to meet the requirement of patient, so, the pharmaceutical composition developing a kind of effective treatment glaucoma is significant to play synergistic therapeutic effect.
Summary of the invention
The present invention is directed to the deficiencies in the prior art, by drug screening and the clinical verification repeatedly of several years, it is provided that a kind of pharmaceutical composition treating glaucoma, its feature is easy to use, can effectively treat glaucoma.In order to realize the purpose of the present invention, intend adopting the following technical scheme that
One aspect of the present invention relates to a kind of pharmaceutical composition treating glaucoma, wherein comprise brimonidine or its pharmaceutically acceptable salt, at least one albumen, at least one additional reduce medicine and optional at least one pharmaceutically useful carrier of intraocular pressure, active component therein is the most in a free form or presented in officinal salt, described combination is used for simultaneously, uses respectively or successively；Preferably, the described medicine reducing intraocular pressure is phylloxanthin；Described albumen is preferably collagen protein.
In a preferred embodiment of the present invention, described pharmaceutical composition is combination formulations or pharmaceutical composition, it is preferred that described brimonidine or its pharmaceutically acceptable salt are 1-3:1 to reduce the weight proportion of intraocular pressure medicine with another.
In a preferred embodiment of the present invention, described pharmaceutical composition is used for simultaneously, uses respectively or successively with prevention, delay of progression or treatment glaucoma.
The pharmaceutical composition of the present invention, its brimonidine comprising treatment epilepsy effective dose or its pharmaceutically acceptable salt and phylloxanthin (weight proportion is 1-3:1) are as active constituents of medicine and at least one pharmaceutically useful carrier.
The invention still further relates to aforementioned pharmaceutical compositions preparation for preventing, delay of progression or treatment glaucoma medicine in purposes.
Another aspect of the present invention further relates to a kind of commercial packing, and it comprises power aforementioned pharmaceutical compositions, and is used in prevention, delay of progression or treatment glaucoma simultaneously, the operation instructions used respectively or successively.
Term " the associating agent be used for simultaneously, used respectively or successively or pharmaceutical composition " especially refers to one " component bag ", the meaning is component brimonidine or its pharmaceutically acceptable salt and phylloxanthin can be used independently of one another or be used by the different fixed Combination with different component content, i.e. in different time points or uses simultaneously.So, the component of component bag can be used the most simultaneously or interval is used in chronological order, i.e. in different time points and any component of using component bag with identical or different time interval.Preferably, selected time interval should make component effect to treated disease or disease to be used in combination higher than only using any obtained effect of single component.
Term " prevents " to refer to prophylactically use described combination to healthy patients to prevent disease described herein and disease from occurring.Additionally, term " prevents ", the patient that may point to be in disease early stage to be treated is preventative uses described combination.Term used herein " delay of progression " refers to prophylactically use described combination to the patient of the front disease being in disease early stage to be treated, being diagnosed with corresponding disease.
In the present invention combination of therapeutically effective amount, every kind of component can or use with any successively simultaneously, and described component can be used respectively or use as fixed Combination.Single component in combination can be used or with separate or single combining form and use respectively at the different time during treating.Additionally, term administering " also include that use can be converted into the prodrug of any medicine of selected medicine in vivo.Therefore, should invention is construed as including all these scheme either simultaneously or alternately treated, and should be correspondingly to term administering " explain.
The preferred route of administration of dosage form of the present invention is through enteral or preferred oral approach.Owing to using the optimal oral dosage unit form of convenience, tablet and Capsules representative, in this case, it is evident that solid pharmaceutical carriers need to be used.
The effective dose of every kind of active component used in therapeutic alliance can change with the concrete pharmaceutical composition used, occupation mode or the sanatory order of severity of institute.
It is an advantage of the invention that the medicine according to the different mechanism of action of combination, give full play to medicine complementation synergism, and reduce the untoward reaction relevant to the increase of certain dose, take pharmaceutical composition of the present invention, can relief of symptoms at short notice, can effectively treat glaucoma.
Detailed description of the invention
If not specified, that technological means used in embodiment is well known to those skilled in the art conventional means.
Embodiment 1:
Experimental group prescription: brimonidine tartrate 0.2g, collagen protein 0.1g, phylloxanthin 0.1g, polyvinyl alcohol 1.0g, sodium chloride 0.9g, pH adjusting agent sodium hydroxide and hydrochloric acid are adjusted to 5.6-6.6, add water to 100mL.
Matched group prescription: brimonidine tartrate 0.2g, collagen protein 0.1g, polyvinyl alcohol 1.0g, sodium chloride 0.9g, pH adjusting agent sodium hydroxide and hydrochloric acid are adjusted to 5.6-6.6, add water to 100mL.
Technique: weigh recipe quantity polyvinyl alcohol, adds appropriate water for injection and dissolves；
(2) weighing the brimonidine tartrate of recipe quantity, collagen protein, phylloxanthin (matched group does not contains), sodium chloride is placed in sterilized container, adds appropriate water for injection, and stirring makes it dissolve；
(3) step (1) and the mixing of step (2) solution, regulate pH value 6.0 with hydrochloric acid or sodium hydroxide, add to 100ml, filtration sterilization, fill with water for injection, to obtain final product.
By Experiment of Zoology, the pharmaceutical composition of the present invention therapeutical effect to glaucoma will be described below.
Laboratory animal: healthy rabbits 42, male and female do not limit, body weight 1.8-2.2Kg.
Experiment reagent: matched group and test group give the eye drop prepared by embodiment 1 respectively.
Experimental technique: rabbit is randomly divided into 2 groups, often group 21, every eyes are administered once, and are administered volume about 50 microlitre every time.Measure with schiotz indentation tonometers and be administered 0h, 1h, 2h, 3h, 4h intraocular pressure.Calculate the percent change of intraocular pressure before and after being administered, the results are shown in Table 1
(intraocular pressure before intraocular pressure-administration after administration) ÷ is administered front intraocular pressure × 100%
Institute's value is just, after illustrating to be administered, intraocular pressure rises, and institute's value is negative, and after illustrating to be administered, intraocular pressure declines.
The impact on rabbit intraocular pressure of table 1 eye drop
| Group | 0h intraocular pressure (mmHg) | 1h | 2h | 3h | 4h |
| Experimental group | 18.46 | -16.8 | -28.8 | -36.4 | -19.2 |
| Matched group | 18.43 | -12.3 | -18.9 | -20.3 | -15.4 |
As can be seen from the above table, experimental group patient is substantially better than the curative effect of matched group patient.
The above is the preferred embodiments of the present invention; it should be pointed out that, for those skilled in the art, on the premise of without departing from principle of the present invention; can also make some improvements and modifications, these improvements and modifications also should be regarded as protection scope of the present invention.
Claims (6)
1. the pharmaceutical composition treating glaucoma, wherein comprise brimonidine or its pharmaceutically acceptable salt, at least one albumen, at least one additional reduce medicine and optional at least one pharmaceutically useful carrier of intraocular pressure, active component therein is the most in a free form or presented in officinal salt, described combination is used for simultaneously, uses respectively or successively；Preferably, the described medicine reducing intraocular pressure is phylloxanthin；Described albumen is preferably collagen protein.
2. the pharmaceutical composition described in claim 1, it is combination formulations or pharmaceutical composition, it is preferred that described brimonidine or its pharmaceutically acceptable salt are 1-3:1 to reduce the weight proportion of intraocular pressure medicine with another.
3. the pharmaceutical composition described in claim 1 or 2, it is used for simultaneously, uses respectively or successively with prevention, delay of progression or treatment glaucoma.
4. pharmaceutical composition, its combination of any one of claim 1 to 2 comprising treatment epilepsy effective dose and at least one pharmaceutically useful carrier.
5. the combination of any one of claim 1 to 2 in preparation purposes for preventing, in the medicine of delay of progression or treatment glaucoma.
6. a commercial packing, it comprises the pharmaceutical composition described in claim 1 or 2, and in prevention, delay of progression or treatment glaucoma simultaneously, the operation instructions used respectively or successively.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610010468.8A CN105935442A (en) | 2016-01-08 | 2016-01-08 | Pharmaceutical composition for treatment of glaucoma |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610010468.8A CN105935442A (en) | 2016-01-08 | 2016-01-08 | Pharmaceutical composition for treatment of glaucoma |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN105935442A true CN105935442A (en) | 2016-09-14 |
Family
ID=57152831
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201610010468.8A Withdrawn CN105935442A (en) | 2016-01-08 | 2016-01-08 | Pharmaceutical composition for treatment of glaucoma |
Country Status (1)
| Country | Link |
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| CN (1) | CN105935442A (en) |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1950067A (en) * | 2004-04-30 | 2007-04-18 | 阿勒根公司 | Intraocular implants of alpha-2 adrenergic receptor agonists and methods for improving vision |
| CN101347620A (en) * | 2007-07-20 | 2009-01-21 | 天津药业研究院有限公司 | Medicament composition and use thereof in preparing medicament for treating glaucoma |
| CN101648006A (en) * | 2008-08-13 | 2010-02-17 | 北京和润创新医药科技发展有限公司 | Medicinal composition for treating glaucoma and application thereof |
-
2016
- 2016-01-08 CN CN201610010468.8A patent/CN105935442A/en not_active Withdrawn
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1950067A (en) * | 2004-04-30 | 2007-04-18 | 阿勒根公司 | Intraocular implants of alpha-2 adrenergic receptor agonists and methods for improving vision |
| CN101347620A (en) * | 2007-07-20 | 2009-01-21 | 天津药业研究院有限公司 | Medicament composition and use thereof in preparing medicament for treating glaucoma |
| CN101648006A (en) * | 2008-08-13 | 2010-02-17 | 北京和润创新医药科技发展有限公司 | Medicinal composition for treating glaucoma and application thereof |
Non-Patent Citations (2)
| Title |
|---|
| 王璐等: "《生物医用纺织品》", 30 November 2011, 中国纺织出版社 * |
| 蒋幼芹: "青光眼的药物治疗", 《中华眼科杂志》 * |
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| WW01 | Invention patent application withdrawn after publication | ||
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Application publication date: 20160914 |