CN109498569A - A kind of Lortadine syrup and preparation method thereof - Google Patents
A kind of Lortadine syrup and preparation method thereof Download PDFInfo
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- CN109498569A CN109498569A CN201811574375.3A CN201811574375A CN109498569A CN 109498569 A CN109498569 A CN 109498569A CN 201811574375 A CN201811574375 A CN 201811574375A CN 109498569 A CN109498569 A CN 109498569A
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- syrup
- lortadine
- preparation
- added
- glycerol
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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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
-
- 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
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
-
- 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
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/16—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing nitrogen, e.g. nitro-, nitroso-, azo-compounds, nitriles, cyanates
- A61K47/18—Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
- A61K47/183—Amino acids, e.g. glycine, EDTA or aspartame
-
- 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
- A61K9/0087—Galenical forms not covered by A61K9/02 - A61K9/7023
- A61K9/0095—Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
-
- 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
Abstract
The invention belongs to technical field of medicine, and in particular to a kind of Lortadine syrup and preparation method thereof.The Lortadine syrup, it is counted on the basis of 1000ml, the formula of each component are as follows: 0.9~1.1g of Loratadine, 650~750g of sweetener, 80~120ml of propylene glycol, 40~60ml of glycerol, 0.9~1.1g of disodium ethylene diamine tetraacetate, 15~25g of acidity regulator, 2~4g of preservative add water to 1000ml.The present invention prepares gained Lortadine syrup and is able to satisfy the finely dispersed requirement of bulk pharmaceutical chemicals, and effective component can be dispersed in syrup, and the upper layer of syrup, middle layer, lower layer's content are uniform, and quality is uniform；Lortadine syrup is produced using preparation method of the present invention, alcohol solvent is free of in preparation process, no ethyl alcohol remains, and clinical safety is good；The quality that the present invention prepares gained Lortadine syrup is stablized, and validity period was up to 36 months or more.
Description
Technical field
The invention belongs to technical field of medicine, and in particular to a kind of Lortadine syrup and preparation method thereof.
Background technique
Loratadine is the antihistamine drug of the second generation, is usually used in treating allergic symptom.It is compared with first generation antihistamine,
The big characteristic of its one is acted on without drowsiness.Clinic is widely used in allergic rhinitis, acute or chronic nettle rash, anaphylaxis conjunctiva
Scorching, pollinosis and other anaphylaxis dermatosis.
There are Loratadine tablet, capsule, granule, syrup etc. for what is clinically used at present.Wherein syrup pair
In child patient, dose ratio tablet, the capsule of medication are more acurrate, are easier to take, and the mouthfeel with sweet tea also allows child patient
It is more willing to accept, therefore there is greater advantage in terms of compliance medication.Existing Lortadine syrup preparation listing both at home and abroad, but
It is all unstable since Loratadine is not soluble in water, and under alkali, heat condition, it has listed syrup preparation process and has largely used second
Alcohol, not only there are hidden danger for drug safety, but also generally related substance rises very fast, content uniformity after storage 12 months
It is deteriorated, keeping life longest only has 24 months.Therefore when preparing Lortadine syrup, Loratadine is dispersed in sugar
In slurry and it is made to maintain a long-term stability, reaches long term quality first is that preparation difficult point.
Disclosed Chinese patent application (application number: 201510291917.6) is related to a kind of Lortadine syrup agent preparation side
Sugar is made after mainly including Loratadine as inclusion agents using beta-cyclodextrin or gamma-cyclodextrin in method, the method for the patent application again
Slurry.The method is more demanding to clathrate process: syrup must be cooled to 60 DEG C or less row clathrate process again；Inclusion process must be with thread side
The ethanol solution containing main ingredient is added in formula, and thread operation may more difficult grasp；A large amount of ethyl alcohol dissolutions must be first used during inclusion
Main ingredient, ethyl alcohol residual also bring security risks to medication.
Summary of the invention
The present invention is in view of the deficiencies of the prior art, and it is an object of the present invention to provide a kind of Lortadine syrup and preparation method thereof.
For achieving the above object, the technical solution adopted by the present invention are as follows:
A kind of Lortadine syrup, is counted on the basis of 1000ml, the formula of each component are as follows: 0.9~1.1g of Loratadine, sweet tea
650~750g of taste agent, 80~120ml of propylene glycol, 40~60ml of glycerol, 0.9~1.1g of disodium ethylene diamine tetraacetate, acidity adjustment
15~25g of agent, 2~4g of preservative, add water to 1000ml.
In above scheme, the propylene glycol, glycerol, disodium ethylene diamine tetraacetate ratio be 100ml:50ml:1g.
In above scheme, the sweetener is sucrose；The acidity regulator is citric acid；The preservative is benzoic acid
Sodium.
In above scheme, the pH value of the Lortadine syrup is 2.0~3.0.
The preparation method of above-mentioned Lortadine syrup, includes the following steps:
(1) sucrose is weighed, water is added, is dissolved by heating, filter-cloth filtering is used while hot, simple syrup is made；
(2) be added disodium ethylene diamine tetraacetate and Loratadine into glycerol, propylene glycol, stirring be allowed to dissolution and then
It is added in simple syrup made of step (1)；
(3) citric acid, sodium benzoate and suitable quantity of water are continuously added into syrup, is stirred evenly, and are boiled, it is cooling, it is filling up to chlorine
Lei Tading syrup.
Beneficial effects of the present invention are as follows: it is finely dispersed that present invention preparation gained Lortadine syrup is able to satisfy bulk pharmaceutical chemicals
It is required that effective component can be dispersed in syrup, the upper layer of syrup, middle layer, lower layer's content are uniform, and quality is uniform；Using
Preparation method of the present invention produces Lortadine syrup, and alcohol solvent, no ethyl alcohol residual, clinical safety are free of in preparation process
Property is good；The quality that the present invention prepares gained Lortadine syrup is stablized, and validity period up to 36 months or more, keeps sample 36 months for a long time and surveys
Obtain Loratadine degradation < 1.0%, content uniformity RSD < 1%.
Specific embodiment
For a better understanding of the present invention, below with reference to the embodiment content that the present invention is furture elucidated, but it is of the invention
Content is not limited solely to the following examples.
Embodiment 1
A kind of Lortadine syrup, each component formula are as follows: Loratadine 1.0g, sucrose 680g, propylene glycol 100ml, glycerol
50ml, citric acid 20g, sodium benzoate 3g, disodium ethylene diamine tetraacetate 1g add water to 1000ml.
A kind of preparation method of Lortadine syrup, includes the following steps:
(1) sucrose is weighed, water is added, is dissolved by heating, filter-cloth filtering is used while hot, simple syrup is made；
(2) be added disodium ethylene diamine tetraacetate and Loratadine into glycerol, propylene glycol, stirring be allowed to dissolution and then
It is added in simple syrup made of step (1)；
(3) citric acid, sodium benzoate and suitable quantity of water are continuously added into syrup, is stirred evenly, and are boiled, it is cooling, it is filling up to chlorine
Lei Tading syrup.
Embodiment 2
A kind of Lortadine syrup, each component formula are as follows: Loratadine 1.05g, sucrose 750g, propylene glycol 100ml, glycerol
50ml, citric acid 18g, sodium benzoate 2.5g, disodium ethylene diamine tetraacetate 1g add water to 1000ml.
A kind of preparation method of Lortadine syrup, includes the following steps:
(1) sucrose is weighed, water is added, is dissolved by heating, filter-cloth filtering is used while hot, simple syrup is made；
(2) be added disodium ethylene diamine tetraacetate and Loratadine into glycerol, propylene glycol, stirring be allowed to dissolution and then
It is added in simple syrup made of step (1)；
(3) citric acid, sodium benzoate and suitable quantity of water are continuously added into syrup, is stirred evenly, and are boiled, it is cooling, it is filling up to chlorine
Lei Tading syrup.
Embodiment 3
A kind of Lortadine syrup, each component formula are as follows: Loratadine 0.95g, sucrose 650g, propylene glycol 100ml, glycerol
50ml, citric acid 25g, sodium benzoate 3.5g, disodium ethylene diamine tetraacetate 1g add water to 1000ml.
A kind of preparation method of Lortadine syrup, includes the following steps:
(1) sucrose is weighed, water is added, is dissolved by heating, filter-cloth filtering is used while hot, simple syrup is made；
(2) be added disodium ethylene diamine tetraacetate and Loratadine into glycerol, propylene glycol, stirring be allowed to dissolution and then
It is added in simple syrup made of step (1)；
(3) citric acid, sodium benzoate and suitable quantity of water are continuously added into syrup, is stirred evenly, and are boiled, it is cooling, it is filling up to chlorine
Lei Tading syrup.
Influence factor examination is carried out with commercially available Lortadine syrup and the preparation gained Lortadine syrup of the embodiment of the present invention 1
Test, accelerate and long-time stability investigation compare, the results show that syrup quality produced by the present invention is more stable, validity period is longer.
Concrete outcome is as follows:
(1) influence factor is tested, and experimental result is shown in Table 1, table 2, and the result of Tables 1 and 2 illustrates invention formulation than commercially available
Preparation influences temperature and illumination condition smaller, and quality is more stable, in relation to the trend that substance does not increase, content be basically unchanged and
Uniform content.
1 embodiment of the present invention of table preparation gained Lortadine syrup (lot number: 20150424)
2 commercial preparation of table (lot number: 1EISAAD001)
(2) accelerated test 1, experimental result are shown in Table 3,4, and the result of table 3 and table 4 also illustrates invention formulation in 40 DEG C of conditions
Lower more more stable than commercial preparation, related substance growth trend is unobvious, and content is also basically unchanged and uniform content, and commercial preparation
Related substance growth trend is obvious, and content has lamination tendency.
3 embodiment of the present invention of table preparation gained Lortadine syrup (lot number: 20150424, investigation condition: 40 ± 2 DEG C,
RH75 ± 5%)
4 commercial preparation of table (lot number: 1EISAAD001, investigation condition: 40 ± 2 DEG C, RH75 ± 5%)
(3) accelerated test 2, experimental result are shown in Table 5,6, and the result of table 5 and table 6 also illustrates invention formulation in 30 DEG C of conditions
Lower more more stable than commercial preparation, related substance growth trend is more gentle, and content is also basically unchanged and uniform content, and commercial preparation
Related substance growth trend is obvious, and content has lamination tendency.
5 embodiment of the present invention of table preparation gained Lortadine syrup (lot number: 20150424, investigation condition: 30 ± 2 DEG C,
RH65 ± 5%)
6 commercial preparation of table (lot number: 1EISAAD001, investigation condition: 30 ± 2 DEG C, RH65 ± 5%)
(4) long term test, experimental result are shown in Table 7,8, and the result of table 7 and table 8 illustrates invention formulation under the conditions of 25 DEG C
Long-term storage is more more stable than commercial preparation, and related substance growth is much smaller compared with commercial preparation, and changes of contents is also smaller and content
Uniform, shelf life had apparent quality-advantage up to 36 months.
7 embodiment of the present invention of table preparation gained Lortadine syrup (lot number: 20150424, investigation condition: 25 ± 2 DEG C,
RH60 ± 5%)
8 commercial preparation of table (lot number: 1EISAAD001, investigation condition: 25 ± 2 DEG C, RH60 ± 5%)
Obviously, above-described embodiment is only intended to clearly illustrate made example, and is not the limitation to embodiment.It is right
For those of ordinary skill in the art, can also make on the basis of the above description it is other it is various forms of variation or
It changes.There is no necessity and possibility to exhaust all the enbodiments.And the obvious variation or change therefore amplified
It moves within still in the protection scope of the invention.
Claims (5)
1. a kind of Lortadine syrup, is counted on the basis of 1000ml, the formula of each component are as follows: 0.9 ~ 1.1g of Loratadine, sweet taste
650 ~ 750g of agent, 80 ~ 120ml of propylene glycol, 40 ~ 60ml of glycerol, 0.9 ~ 1.1g of disodium ethylene diamine tetraacetate, acidity regulator 15 ~
25g, 2 ~ 4g of preservative, add water to 1000ml.
2. Lortadine syrup according to claim 1, which is characterized in that the propylene glycol, glycerol, ethylenediamine tetra-acetic acid two
The ratio of sodium is 100ml:50ml:1g.
3. Lortadine syrup according to claim 1, which is characterized in that the sweetener is sucrose, the acidity adjustment
Agent is citric acid；The preservative is sodium benzoate.
4. Lortadine syrup according to claim 1, which is characterized in that the pH value of the Lortadine syrup be 2.0 ~
3.0。
5. the preparation method of any Lortadine syrup of claim 1 ~ 4, which comprises the steps of:
(1) sucrose is weighed, water is added, is dissolved by heating, filter-cloth filtering is used while hot, simple syrup is made；
(2) disodium ethylene diamine tetraacetate and Loratadine are added into glycerol, propylene glycol, stirring is allowed to dissolve and then be added
Into simple syrup made of step (1)；
(3) citric acid, sodium benzoate and suitable quantity of water are continuously added into syrup, is stirred evenly, is boiled, it is cooling, it is filling up to chlorine thunder he
Determine syrup.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201811574375.3A CN109498569A (en) | 2018-12-21 | 2018-12-21 | A kind of Lortadine syrup and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201811574375.3A CN109498569A (en) | 2018-12-21 | 2018-12-21 | A kind of Lortadine syrup and preparation method thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN109498569A true CN109498569A (en) | 2019-03-22 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201811574375.3A Pending CN109498569A (en) | 2018-12-21 | 2018-12-21 | A kind of Lortadine syrup and preparation method thereof |
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| Country | Link |
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Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110934823A (en) * | 2019-12-27 | 2020-03-31 | 湖北康源药业有限公司 | Valganciclovir hydrochloride oral solution and preparation method thereof |
| CN113730336A (en) * | 2021-09-27 | 2021-12-03 | 浙江核力欣健药业有限公司 | Loratadine syrup and preparation method thereof |
| CN114767677A (en) * | 2022-05-06 | 2022-07-22 | 成都倍特药业股份有限公司 | Loratadine composition and preparation method thereof |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1082117B1 (en) * | 1998-06-01 | 2004-01-14 | Schering Corporation | A stabilized antihistamine syrup containing aminopolycarboxylic acid as stabilizer |
| CN102670488A (en) * | 2011-12-09 | 2012-09-19 | 东莞达信生物技术有限公司 | Rupatadine syrup composition and preparation method thereof |
| CN104856948A (en) * | 2015-06-01 | 2015-08-26 | 广东华润顺峰药业有限公司 | Loratadine syrup and preparation method thereof |
-
2018
- 2018-12-21 CN CN201811574375.3A patent/CN109498569A/en active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1082117B1 (en) * | 1998-06-01 | 2004-01-14 | Schering Corporation | A stabilized antihistamine syrup containing aminopolycarboxylic acid as stabilizer |
| CN102670488A (en) * | 2011-12-09 | 2012-09-19 | 东莞达信生物技术有限公司 | Rupatadine syrup composition and preparation method thereof |
| CN104856948A (en) * | 2015-06-01 | 2015-08-26 | 广东华润顺峰药业有限公司 | Loratadine syrup and preparation method thereof |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110934823A (en) * | 2019-12-27 | 2020-03-31 | 湖北康源药业有限公司 | Valganciclovir hydrochloride oral solution and preparation method thereof |
| CN113730336A (en) * | 2021-09-27 | 2021-12-03 | 浙江核力欣健药业有限公司 | Loratadine syrup and preparation method thereof |
| CN114767677A (en) * | 2022-05-06 | 2022-07-22 | 成都倍特药业股份有限公司 | Loratadine composition and preparation method thereof |
| CN114767677B (en) * | 2022-05-06 | 2023-11-07 | 成都倍特药业股份有限公司 | Loratadine composition and preparation method thereof |
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| PB01 | Publication | ||
| SE01 | Entry into force of request for substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| RJ01 | Rejection of invention patent application after publication |
Application publication date: 20190322 |
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| RJ01 | Rejection of invention patent application after publication |