CN104546685A - Zidovudine syrup preparation and preparation method thereof - Google Patents
Zidovudine syrup preparation and preparation method thereof Download PDFInfo
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- CN104546685A CN104546685A CN201510005719.9A CN201510005719A CN104546685A CN 104546685 A CN104546685 A CN 104546685A CN 201510005719 A CN201510005719 A CN 201510005719A CN 104546685 A CN104546685 A CN 104546685A
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Abstract
The invention relates to an anti-AIDS drug syrup preparation and a preparation method thereof. The drug comprises zidovudine, a cosolvent, a pH regulator, a corrigent, a stabilizer, a preservative and other pharmaceutically accepted pharmaceutic adjuvants. The anti-AIDS drug syrup preparation is characterized by covering the bitter taste of the zidovudine, and being easier to adjust dosage, suitable for children medication to increase clinic compliance, simple in process and controllable in quality, improving the stability and preferably satisfying the clinic demand.
Description
Technical field
The present invention relates to a kind of syrup preparation containing zidovudine and preparation method thereof, this syrup preparation is mainly used in the treatment of HIV (human immunodeficiency virus) infection patient.
Background technology
Acquired immune deficiency syndrome (AIDS) and acquired immune deficiency syndrome (AIDS), caused by aids infection virus (HIV virus).After HIV enters human body, optionally invade helper T lymphocyte, make it to destroy, cause this cell function serious defect, make human body lose immunologic function.Therefore cause human body to be easy to infect various diseases, and malignant tumor can occur, case fatality rate is higher.Current whole world Epidemic Situation of AIDS is very severe, particularly Africa and Asia, and in recent years, the infection of China's AIDS and number of the infected also increase comparatively fast.
Still do not have at present a kind of method can treatment of AIDS in the world, effective method is " highly active antiretroviral therapy " the most, be commonly called as " cocktail ", zidovudine is the important medicine in effective therapy " cocktail " of the treatment acquired immune deficiency syndrome (AIDS) of international endorsement, and it also has certain effect to hepatitis B virus and Epstein-Barr virus simultaneously.Antiviral dominant mechanism is be combined with the archaeal dna polymerase of virus, stops the growth of DNA chain, thus suppresses copying of virus.
In prior art, CN101199541A discloses a kind of Zidovudine capsule and preparation method thereof, CN101879145A discloses anti-HIV drug zidovudine for injection and preparation technology thereof, the application for a patent for invention of 02139215.3 discloses a kind of inverase zidovudine injectable powder and preparation method thereof, propose technical scheme zidovudine being prepared into lyophilized preparation, zidovudine syrup preparation not yet has patent report.This syrup preparation effectively can cover the bitterness of zidovudine, and compared with zidovudine tablet, capsule, during children, syrup preparation dosage is easier to adjustment and accurately, flavor adjustment, increases patient's compliance.
Summary of the invention
The invention provides a kind of easy adjust dosages containing zidovudine medicine, be applicable to children, the syrup that clinical compliance is good.
Present invention also offers a kind of preparation method effectively can treating the syrup of acquired immune deficiency syndrome (AIDS) containing zidovudine medicine.
Syrup containing neat Fu Duoding disclosed by the invention, is characterized in that described pharmaceutically acceptable pharmaceutic adjuvant is one or more in cosolvent, pH adjusting agent, correctives, antiseptic, stabilizing agent.
Syrup containing neat Fu Duoding disclosed by the invention, is characterized in that described syrup composition weight proportion is: zidovudine is 0.5%-5%; Syrup substrate is 45%-75%; Cosolvent is 1%-5%; PH adjusting agent is 3%-8%; Antiseptic is 0.1-0.5%; Correctives is appropriate; Purified Water q. s.
Syrup containing neat Fu Duoding disclosed by the invention, is characterized in that described cosolvent is the mixture of one or more of glycerol, propylene glycol, sodium benzoate, sodium chloride.
Syrup containing neat Fu Duoding disclosed by the invention, is characterized in that pH scope is 6.0-9.0.
Syrup containing neat Fu Duoding disclosed by the invention, is characterized in that described pH regulator is that the compositions of one or more in fumaric acid, citric acid, sodium citrate, tartaric acid, acetic acid, sodium acetate, sodium hydroxide, sodium bicarbonate, phosphate or other bufferings pharmaceutically acceptable are to solution.
Syrup containing neat Fu Duoding disclosed by the invention, is characterized in that described antiseptic includes but are not limited to benzoic acid and salt, methyl hydroxybenzoate, ethyl hydroxybenzoate, propyl hydroxybenzoate, benzalkonium bromide, benzalkonium chloride, sorbic acid and salt thereof.
Syrup containing neat Fu Duoding disclosed by the invention, is characterized in that described correctives includes but are not limited to steviosin, sorbitol, mannitol, flavoring banana essence, strawberry essence, flavoring pineapple essence, orange essence, peach flavor, apple essence or cherry essence.
Syrup containing neat Fu Duoding disclosed by the invention, is characterized in that its preparation process comprises the following steps; Take sucrose, add purified water and boil dissolving, be cooled to 65-80 DEG C. in above-mentioned solution, add pH regulator, correctives, antiseptic stirs and makes it dissolve completely, is cooled to room temperature for subsequent use; By zidovudine, stabilizing agent is added in cosolvent and stirs, and is added in above-mentioned syrup after mix homogeneously, continues to stir, and adds the boiling water of appropriate room temperature to quantitative after filtration.
Detailed description of the invention
Following examples are to further explanation of the present invention, but the present invention is not limited only to these embodiments, the protection domain that these embodiments do not limit the present invention in any way.
Embodiment 1
The existence form of this embodiment is syrup.(with every 1000mL gauge)
Preparation method:
Take sucrose, add purified water and boil dissolving, be cooled to 65-80 DEG C. in above-mentioned solution, add pH regulator, correctives, antiseptic stirs and makes it dissolve completely, is cooled to room temperature for subsequent use; By zidovudine, stabilizing agent, antioxidant are added in cosolvent and stir, and are added in above-mentioned syrup after mix homogeneously, continue to stir, and add the boiling water of appropriate room temperature to quantitative after filtration.
Embodiment 2
The existence form of this embodiment is syrup.(with every 1000mL gauge)
Preparation method is with embodiment 1.
Embodiment 3
The existence form of this embodiment is syrup.(with every 1000mL gauge)
Preparation method is with embodiment 1.
Embodiment 4
The existence form of this embodiment is syrup.(with every 1000mL gauge)
Preparation method is with embodiment 1.
Embodiment 5
The existence form of this embodiment is syrup.(with every 1000mL gauge)
Preparation method is with embodiment 1.
Embodiment 6
The existence form of this embodiment is syrup.(with every 1000mL gauge)
Preparation method is with embodiment 1.
Embodiment 7
The existence form of this embodiment is syrup.(with every 1000mL gauge)
Preparation method is with embodiment 1.
Embodiment 8
Preparation embodiment 1,4,6 produced is in Acceleration study (temperature 40 ± 2 DEG C, humidity 75% ± 5%) and long-time stability experiment (temperature 25 ± 2 DEG C, humidity 60% ± 5%) place under condition, investigate its character, content, clarity, related substance respectively, concrete outcome is in table 1 and table 2.
Acceleration study result:
Table 1-1 embodiment 1
Table 1-2 embodiment 4
Table 1-3 embodiment 6
Long-time stability experimental result
Table 2-1 embodiment 1
| Standing time | 0 month | 1 month | 2 months | 3 months | 6 months |
| Character | Colourless transparent liquid; Taste is sweet | Colourless transparent liquid; Taste is sweet | Colourless transparent liquid; Taste is sweet | Colourless transparent liquid; Taste is sweet | Colourless transparent liquid; Taste is sweet |
| Content (%) | 99.9 | 99.9 | 100.3 | 100.5 | 101.1 |
| Clarity | Clarification | Clarification | Clarification | Clarification | Clarification |
| Single assorted | 0.04 | 0.06 | 0.07 | 0.05 | 0.09 |
| Total assorted | 0.11 | 0.15 | 0.16 | 0.18 | 0.16 |
Table 2-2 embodiment 4
| Standing time | 0 month | 1 month | 2 months | 3 months | 6 months |
| Character | Colourless transparent liquid; Taste is sweet | Colourless transparent liquid; Taste is sweet | Colourless transparent liquid; Taste is sweet | Colourless transparent liquid; Taste is sweet | Colourless transparent liquid; Taste is sweet |
| Content (%) | 100.3 | 101.3 | 100.5 | 100.9 | 101.0 |
| Clarity | Clarification | Clarification | Clarification | Clarification | Clarification |
| Single assorted | 0.08 | 0.05 | 0.04 | 0.05 | 0.08 |
| Total assorted | 0.13 | 0.11 | 0.12 | 0.15 | 0.16 |
Table 2-3 embodiment 6
| Standing time | 0 month | 1 month | 2 months | 3 months | 6 months |
| Character | Colourless transparent liquid; Taste is sweet | Colourless transparent liquid; Taste is sweet | Colourless transparent liquid; Taste is sweet | Colourless transparent liquid; Taste is sweet | Colourless transparent liquid; Taste is sweet |
| Content (%) | 100.5 | 100.6 | 100.5 | 101.1 | 100.9 |
| Clarity | Clarification | Clarification | Clarification | Clarification | Clarification |
| Single assorted | 0.06 | 0.05 | 0.07 | 0.06 | 0.09 |
| Total assorted | 0.11 | 0.16 | 0.13 | 0.14 | 0.15 |
Therefore, as can be seen from the table, zidovudine syrup prepared by the present invention places a period of time under accelerated test condition He under long term test condition, and investigate result from acceleration and long-term experiment, each investigation project is all without exception, meets quality criteria requirements.Illustrate that zidovudine syrup of the present invention has good stability.
Claims (9)
1. a medical syrup preparation for anti-AIDS, is characterized in that containing active component zidovudine and pharmaceutically acceptable pharmaceutic adjuvant.
2. syrup as claimed in claim 1, is characterized in that described pharmaceutically acceptable pharmaceutic adjuvant is one or more in cosolvent, pH adjusting agent, correctives, antiseptic, stabilizing agent.
3. syrup as claimed in claim 2, is characterized in that described syrup composition weight proportion is: zidovudine is 0.5%-5%; Syrup substrate is 45%-75%; Cosolvent is 1%-5%; PH adjusting agent is 3%-8%; Antiseptic is 0.1-0.5%; Correctives is appropriate; Purified Water q. s.
4. syrup as claimed in claim 2, is characterized in that described cosolvent is the mixture of one or more of glycerol, propylene glycol, sodium benzoate, sodium chloride.
5. syrup as claimed in claim 2, is characterized in that pH scope is 6.0-9.0.
6. syrup as claimed in claim 2, is characterized in that described pH regulator is that the compositions of one or more in fumaric acid, citric acid, sodium citrate, tartaric acid, acetic acid, sodium acetate, sodium hydroxide, sodium bicarbonate, phosphate or other bufferings pharmaceutically acceptable are to solution.
7. syrup as claimed in claim 2, is characterized in that described antiseptic includes but are not limited to benzoic acid and salt, methyl hydroxybenzoate, ethyl hydroxybenzoate, propyl hydroxybenzoate, benzalkonium bromide, benzalkonium chloride, sorbic acid and salt thereof.
8. syrup as claimed in claim 2, is characterized in that described correctives includes but are not limited to steviosin, sorbitol, mannitol, flavoring banana essence, strawberry essence, flavoring pineapple essence, orange essence, peach flavor, apple essence or cherry essence.
9. the syrup as described in any one of claim 1-7, it is characterized in that its preparation process comprises the following steps: take sucrose, add purified water and boil dissolving, be cooled to 65-80 DEG C, pH regulator is added in above-mentioned solution, correctives, antiseptic stirs and makes it dissolve completely, is cooled to room temperature for subsequent use; By zidovudine, stabilizing agent is added in cosolvent and stirs, and is added in above-mentioned syrup after mix homogeneously, continues to stir, and adds the boiling water of appropriate room temperature to quantitative after filtration.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510005719.9A CN104546685A (en) | 2015-01-07 | 2015-01-07 | Zidovudine syrup preparation and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510005719.9A CN104546685A (en) | 2015-01-07 | 2015-01-07 | Zidovudine syrup preparation and preparation method thereof |
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| Publication Number | Publication Date |
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| CN104546685A true CN104546685A (en) | 2015-04-29 |
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| Application Number | Title | Priority Date | Filing Date |
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| CN201510005719.9A Pending CN104546685A (en) | 2015-01-07 | 2015-01-07 | Zidovudine syrup preparation and preparation method thereof |
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Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2013057469A1 (en) * | 2011-10-20 | 2013-04-25 | Cipla Limited | Pharmaceutical antiretroviral compositions |
| CN104095807A (en) * | 2013-04-02 | 2014-10-15 | 万特制药(海南)有限公司 | Desloratadine syrup and preparation method thereof |
-
2015
- 2015-01-07 CN CN201510005719.9A patent/CN104546685A/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2013057469A1 (en) * | 2011-10-20 | 2013-04-25 | Cipla Limited | Pharmaceutical antiretroviral compositions |
| CN104095807A (en) * | 2013-04-02 | 2014-10-15 | 万特制药(海南)有限公司 | Desloratadine syrup and preparation method thereof |
Non-Patent Citations (1)
| Title |
|---|
| RICHARD H. DREW ET AL.: ""Bioequivalence Assessment of Zidovudine (Retrovir) Syrup, Solution, and Capsule Formulations in Patients Infected with Human Immunodeficiency Virus"", 《ANTIMICROBIAL AGENTS AND CHEMOTHERAPY》 * |
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