CN113876702A - Levocetirizine hydrochloride eye drops and preparation method thereof - Google Patents
Levocetirizine hydrochloride eye drops and preparation method thereof Download PDFInfo
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- CN113876702A CN113876702A CN202111300163.8A CN202111300163A CN113876702A CN 113876702 A CN113876702 A CN 113876702A CN 202111300163 A CN202111300163 A CN 202111300163A CN 113876702 A CN113876702 A CN 113876702A
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/08—Solutions
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/32—Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
- A61K47/38—Cellulose; Derivatives thereof
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0048—Eye, e.g. artificial tears
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic agents
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Abstract
The invention relates to levocetirizine hydrochloride eye drops and a preparation method thereof, belonging to the technical field of pharmaceutical preparations and comprising the following components: 0.01-0.5% (w/v) of levocetirizine hydrochloride, 0.1-4.0% (w/v) of thickening agent, 0.1-1.0% (w/v) of buffering agent, 0.1-5.0% (w/v) of osmotic pressure regulator, 0.001-0.3% (w/v) of metal chelating agent, pH regulator and water for injection. The preparation method comprises the following steps: step 1), dissolving a thickening agent, a buffering agent, an osmotic pressure regulator and a metal chelating agent in water for injection, and then adding a main drug for dissolution; step 2) adjusting the pH value to 5.0-8.0 by using a pH regulator; adding the rest water for injection, and stirring uniformly; filtering, sterilizing, and packaging. The pH value of the obtained eye drops is 5.0-8.0, and the osmotic pressure molar concentration is 260-320 m0 sm/kg.
Description
Technical Field
The invention belongs to the technical field of pharmaceutical preparations, and particularly relates to levocetirizine hydrochloride eye drops and a preparation method thereof.
Background
Levocetirizine hydrochloride, is a selective histamine H1 receptor antagonist. The traditional Chinese medicine composition is mainly used for relieving allergic symptoms of allergic diseases, is clinically used for treating skin and mucosa allergic diseases such as allergic rhinitis, urticaria, angioneurotic edema and the like, and is also used for relieving the allergic symptoms during cold. The eye drops taking levocetirizine hydrochloride as a main active ingredient are mainly used for treating eye pruritus related to allergic conjunctivitis. The most common symptom of allergic conjunctivitis is ocular itching, which is present in almost all patients with allergic conjunctivitis, of which vernal keratoconjunctivitis usually appears most pronounced. Other symptoms include tearing, burning sensation, photophobia and increased secretion. The secretion is mostly mucous.
The affinity of levocetirizine for the H1 receptor is twice that of cetirizine and 30 times that of dextrocetirizine for the H1 receptor. In addition, the half-life of levocetirizine is 142 minutes, and that of dextrocetirizine is only 6 minutes, which indicates that the duration of the binding of the levocetirizine and the dextrocetirizine to the H1 receptor is obviously longer than that of the dextrocetirizine. The invention provides a cetirizine hydrochloride eye drop which improves the existing marketed cetirizine hydrochloride eye drops in the United states into levocetirizine hydrochloride eye drops only containing a single chiral enantiomer with pharmacological activity, removes an inactive dextrocetirizine enantiomer, reduces the clinical administration dosage by half, further reduces the possibility of the occurrence of side effects of drugs and the occurrence of drug resistance on the premise of ensuring that the drug effect is not changed, and obviously improves the safety of clinical medication. In addition, the thickening agent in the prescription of the product can obviously prolong the retention time of the levocetirizine in the eyes, and the clinical effects of slow release and long-acting of the medicine are achieved.
Disclosure of Invention
The invention aims to provide levocetirizine hydrochloride eye drops and a preparation method thereof, which are mainly used for treating eye pruritus related to allergic conjunctivitis.
The invention provides levocetirizine hydrochloride eye drops which comprise levocetirizine hydrochloride, a thickening agent, a buffering agent, a wetting agent, a metal chelating agent, a pH regulator and water for injection.
Wherein the content of the levocetirizine hydrochloride is 0.01-0.5% (w/v).
Wherein the thickening agent is one or more of hydroxypropyl methylcellulose, carbomer, methylcellulose, carboxymethyl cellulose, hydroxyethyl cellulose, polycarbophil, polyvinylpyrrolidone, polyallyl alcohol, sodium hyaluronate, chitosan and chondroitin sulfate; the content of the thickening agent is 0.1-4.0% (w/v).
Wherein the buffer is one or more of disodium hydrogen phosphate, sodium dihydrogen phosphate, potassium dihydrogen phosphate and sodium citrate; the content of the buffer is 0.1-1.0% (w/v).
Wherein the osmotic pressure regulator is one or more of ethanol, propylene glycol, glycerol, polyethylene glycol 200-400 and the like, and tween-80; the content of the osmotic pressure regulator is 0.1-5.0% (w/v).
Wherein the metal chelating agent is one or more of triethanolamine, sodium sulfide, glycerol, sodium citrate, sorbitol, sodium gluconate and edetate disodium in any combination; the content of the metal chelating agent is 0.001-0.3% (w/v).
Wherein the pH regulator is one or more of citric acid, sodium citrate, boric acid, borax, disodium hydrogen phosphate, sodium dihydrogen phosphate, acetic acid, sodium acetate, sodium hydroxide and hydrochloric acid; and adjusting the pH value of the levocetirizine hydrochloride eye drops to 5.0-8.0.
A preparation method of levocetirizine hydrochloride eye drops comprises the following steps:
step 1), dissolving a thickening agent, a buffering agent, an osmotic pressure regulator and a metal chelating agent in water for injection, and then adding a main drug for dissolution;
step 2) adjusting the pH value to 5.0-8.0 by using a pH regulator; adding the rest water for injection, and stirring uniformly; filtering, sterilizing, and packaging. The pH value of the obtained eye drops is 5.0-8.0, and the osmotic pressure molar concentration is 260-320 m0 sm/kg.
The invention uses levocetirizine hydrochloride as an active ingredient, reduces the input amount of raw material medicaments, thereby reducing the possibility of side effects of medicaments and medicament resistance.
The invention uses the thickening agent, increases the biological adhesiveness of the eye drops, reduces the fluidity of the medicine, prolongs the detention time of the medicine in the eyes, improves the bioavailability, is beneficial to the medicine to exert the curative effect, has small stimulation to the eyes and can reduce the medicine absorption of the lacrimal sac.
Detailed Description
In order to make the objects, technical solutions and advantages of the present invention more apparent, the present invention is further described in detail with reference to the following embodiments. The specific embodiments described herein are merely illustrative of the invention and do not delimit the invention.
Example 1
A levocetirizine hydrochloride eye drop, 100ml comprises the following components: 0.01% (w/v) of levocetirizine hydrochloride, 0.1% (w/v) of thickening agent, 0.1% (w/v) of buffering agent, 1.2% (w/v) of osmotic pressure regulator, 0.001% (w/v) of metal chelating agent, hydrochloric acid, sodium hydroxide and water for injection. The method comprises the following steps:
step 1), dissolving a thickening agent, a buffering agent, an osmotic pressure regulator and a metal chelating agent in water for injection, and then adding levocetirizine hydrochloride for dissolution;
step 2) adjusting the pH value to 5.0-8.0 by using a pH regulator; adding the rest water for injection, and stirring uniformly; filtering, sterilizing, and packaging. The pH value of the obtained eye drops is 5.0-8.0, and the osmotic pressure molar concentration is 260-320 m0 sm/kg.
Example 2
A levocetirizine hydrochloride eye drop, 100ml comprises the following components: 0.5% (w/v) of levocetirizine hydrochloride, 4.0% (w/v) of thickening agent, 1.0% (w/v) of buffering agent, 5.0% (w/v) of osmotic pressure regulator, 0.3% (w/v) of metal chelating agent, hydrochloric acid, sodium hydroxide and water for injection. The method comprises the following steps:
step 1), dissolving a thickening agent, a buffering agent, an osmotic pressure regulator and a metal chelating agent in water for injection, and then adding levocetirizine hydrochloride for dissolution;
step 2) adjusting the pH value to 5.0-8.0 by using a pH regulator; adding the rest water for injection, and stirring uniformly; filtering, sterilizing, and packaging. The pH value of the obtained eye drops is 5.0-8.0, and the osmotic pressure molar concentration is 260-320 m0 sm/kg.
Example 3
A levocetirizine hydrochloride eye drop, 100ml comprises the following components: 0.14% (w/v) of levocetirizine hydrochloride, 0.25% (w/v) of thickening agent, 0.2% (w/v) of buffering agent, 1.8% (w/v) of osmotic pressure regulator, 0.025% (w/v) of metal chelating agent, hydrochloric acid, sodium hydroxide and water for injection. The method comprises the following steps:
step 1), dissolving a thickening agent, a buffering agent, an osmotic pressure regulator and a metal chelating agent in water for injection, and then adding levocetirizine hydrochloride for dissolution;
step 2) adjusting the pH value to 5.0-8.0 by using a pH regulator; adding the rest water for injection, and stirring uniformly; filtering, sterilizing, and packaging. The pH value of the obtained eye drops is 5.0-8.0, and the osmotic pressure molar concentration is 260-320 m0 sm/kg.
Through comparison of three examples, the best effect is the example 3, so that the selection of the example 3 as the best example, and the specific change of the amount also belongs to the protection scope of the technical scheme.
The eye drop is added with a certain amount of thickening agent, so that the comfort level of the medicine can be obviously improved, and the dryness of eyes can be better relieved; the invention has simple and reliable preparation process, easy implementation, simple components of the eye drops, relatively low cost and convenient preparation.
Although embodiments of the present invention have been shown and described, it will be appreciated by those skilled in the art that changes, modifications, substitutions and alterations can be made in these embodiments without departing from the principles and spirit of the invention, the scope of which is defined in the appended claims and their equivalents.
Claims (8)
1. The levocetirizine hydrochloride eye drops are characterized by comprising the following components: 0.01-0.5% (w/v) of levocetirizine hydrochloride, a thickening agent, a buffering agent, an osmotic pressure regulator, a metal chelating agent, a pH regulator and water for injection.
2. The levocetirizine hydrochloride eye drops as claimed in claim 1, characterized in that: the thickening agent is one or more of hydroxypropyl methylcellulose, carbomer, methylcellulose, carboxymethyl cellulose, hydroxyethyl cellulose, polycarbophil, polyvinylpyrrolidone, polyallyl alcohol, sodium hyaluronate, chitosan and chondroitin sulfate; the content of the thickening agent is 0.1-4.0% (w/v).
3. The levocetirizine hydrochloride eye drops as claimed in claim 1, characterized in that: the buffer is one or more of disodium hydrogen phosphate, sodium dihydrogen phosphate, potassium dihydrogen phosphate and sodium citrate; the content of the buffer is 0.1-1.0% (w/v).
4. The levocetirizine hydrochloride eye drops as claimed in claim 1, characterized in that: the osmotic pressure regulator is one or more of ethanol, propylene glycol, glycerol, polyethylene glycol 200-400 and the like, and tween-80; the content of the osmotic pressure regulator is 0.1-5.0% (w/v).
5. The levocetirizine hydrochloride eye drops as claimed in claim 1, characterized in that: the metal chelating agent is one or more of triethanolamine, sodium sulfide, glycerol, sodium citrate, sorbitol, sodium gluconate and edetate disodium in any combination; the content of the metal chelating agent is 0.001-0.3% (w/v).
6. The levocetirizine hydrochloride eye drops as claimed in claim 1, characterized in that: the pH regulator is one or more of citric acid, sodium citrate, boric acid, borax, disodium hydrogen phosphate, sodium dihydrogen phosphate, acetic acid, sodium acetate, sodium hydroxide and hydrochloric acid; and adjusting the pH value of the levocetirizine hydrochloride eye drops to 5.0-8.0.
7. A method for preparing levocetirizine hydrochloride eye drops as claimed in claim 1, which comprises the following steps:
step 1), dissolving a thickening agent, a buffering agent, an osmotic pressure regulator and a metal chelating agent in water for injection, and then adding a main drug for dissolution;
step 2) adjusting the pH value to 5.0-8.0 by using a pH regulator; adding the rest water for injection, and stirring uniformly; filtering, sterilizing, and packaging;
the pH value of the obtained eye drops is 5.0-8.0, and the osmotic pressure molar concentration is 260-320 m0 sm/kg.
8. Levocetirizine hydrochloride eye drops as claimed in claim 1, mainly for the treatment of ocular itching associated with allergic conjunctivitis.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN202111300163.8A CN113876702A (en) | 2021-11-04 | 2021-11-04 | Levocetirizine hydrochloride eye drops and preparation method thereof |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN202111300163.8A CN113876702A (en) | 2021-11-04 | 2021-11-04 | Levocetirizine hydrochloride eye drops and preparation method thereof |
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| CN113876702A true CN113876702A (en) | 2022-01-04 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN202111300163.8A Pending CN113876702A (en) | 2021-11-04 | 2021-11-04 | Levocetirizine hydrochloride eye drops and preparation method thereof |
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Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1418630A (en) * | 2002-10-09 | 2003-05-21 | 重庆华邦制药股份有限公司 | Solution agent of antiallergi medicine contg. levocetirizine |
| CN107961215A (en) * | 2016-10-20 | 2018-04-27 | 北京科信必成医药科技发展有限公司 | A kind of levocetirizine injection |
| US20200030320A1 (en) * | 2017-02-13 | 2020-01-30 | Nitto Medic Co., Ltd. | Aqueous composition for eye drops and nasal drops |
-
2021
- 2021-11-04 CN CN202111300163.8A patent/CN113876702A/en active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1418630A (en) * | 2002-10-09 | 2003-05-21 | 重庆华邦制药股份有限公司 | Solution agent of antiallergi medicine contg. levocetirizine |
| CN107961215A (en) * | 2016-10-20 | 2018-04-27 | 北京科信必成医药科技发展有限公司 | A kind of levocetirizine injection |
| US20200030320A1 (en) * | 2017-02-13 | 2020-01-30 | Nitto Medic Co., Ltd. | Aqueous composition for eye drops and nasal drops |
Non-Patent Citations (1)
| Title |
|---|
| 高涛等: "《药剂学》", 31 May 2017 * |
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Application publication date: 20220104 |