CN101623252A - Sertraline hydrochloride oral liquid and preparation method thereof - Google Patents
Sertraline hydrochloride oral liquid and preparation method thereof Download PDFInfo
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- CN101623252A CN101623252A CN 200810116330 CN200810116330A CN101623252A CN 101623252 A CN101623252 A CN 101623252A CN 200810116330 CN200810116330 CN 200810116330 CN 200810116330 A CN200810116330 A CN 200810116330A CN 101623252 A CN101623252 A CN 101623252A
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Abstract
The invention discloses a sertraline hydrochloride oral liquid and a preparation method thereof. The sertraline hydrochloride oral liquid has the advantages of convenient administration, steady storage at low temperature or normal temperature, quick absorption, good mouthfeel, more suitability for senile patients, simple process and material conservation.
Description
Technical field
The present invention relates to a kind of sertraline hydrochloride oral liquid and preparation method thereof, particularly a kind of with HYDROXYPROPYL BETA-CYCLODEXTRIN and sucrose monolaurate mixture as oral liquid of solubilizing agent and stabilizing agent and preparation method thereof.
Background technology
It is up-to-date a kind of that Sertraline (Sertraline) is that the selectivity 5-hydroxy tryptamine reclaims in the inhibitor (SSRI) again, can help to improve the ability of body, alleviate patient's depressive symptom effectively, comprise irritated emotion, and can alleviate the fatigue symptom and the anxiety state of persistence, have and remove the characteristics such as the old people takes that are suitable for soon, very much in long-acting, low, the body, in the world extensively in order to treatment depressibility and compulsive disorder hepatotoxicity.
A kind of oral cavity disintegration tablet that contains Sertraline and preparation method thereof is disclosed among the CN1771920A, this oral disintegrated sertraline tablet, the mixture that comprises active constituents of medicine Sertraline and excipient, it is characterized in that described excipient comprises disintegrating agent, filler, solubility polyhydric alcohol and penetrating agent, compare with common solid preparation, it is rapider that oral cavity disintegration tablet has an effect, be suitable for the advantage that the sufferer crowd of dysphagia takes, but compare with oral liquid, the speed of action of oral liquid will be apparently higher than oral cavity disintegration tablet, have good mouthfeel simultaneously, be more suitable for the old people and take.
A kind of sertraline hydrochloride drop pill and preparation method thereof is disclosed among the CN1526382A, this sertraline hydrochloride drop pill is made by using micronizing and drop pill production technology, thereby can mention the molten diffusing speed of disintegrate, onset rapidly, but its production technology is compared with oral liquid, complex operation, cost are higher, simultaneously, compare with drop pill, oral liquid has following advantage: effect rapidly, good effect can reduce the zest of some drugs, avoid stimulation, more be applicable to the gerontal patient the gastrointestinal generation.
Sertraline is white or off-white color crystal formation powder, atomic molten in water, at present commercially available wide in variety based on oral dosage form, how to improve the dissolubility of sertraline hydrochloride in aqueous solution, and guarantee that solution stable in storage process is key and the difficult point place that sertraline hydrochloride is made oral liquid, external like product adopts surface active agent solubilization and cyclodextrin inclusion technique to solve this problem usually, even the adding of surfactant one nonionic surfactant also has certain toxicity zest, and the toxicity zest of cationic and anionic surfactant is more strong; In cyclodextrin inclusion technique, the consumption of cyclodextrin at least should be suitable with the consumption of sertraline hydrochloride, supplementary product consumption is relatively large, and the stability of solution that obtains in the presence of surfactant-free is bad, and storage can be separated out solid sertraline hydrochloride under low temperature or room temperature.Sertraline hydrochloride oral liquid provided by the invention adopts HYDROXYPROPYL BETA-CYCLODEXTRIN and sucrose monolaurate mixture as solubilizing agent and stabilizing agent, consumption is less, and in the presence of surfactant-free, just can obtain being suitable for clinical practice, storage can not separated out solid sertraline hydrochloride oral liquid under low temperature or the room temperature.
Summary of the invention
The purpose of this invention is to provide a kind of oral liquid that contains sertraline hydrochloride and preparation method thereof, have taking convenience, under low temperature or room temperature storage-stable, absorb fast, mouthfeel is good, more be applicable to the gerontal patient, technology is simple, the advantage of saving material.
Oral liquid provided by the present invention comprises active constituents of medicine sertraline hydrochloride and acceptable accessories, and described adjuvant comprises solubilizing agent, stabilizing agent, plasticizer, antiseptic, aromatic.
The invention solves key issue-dissolubility and stability problem on the sertraline hydrochloride oral liquid preparation technology, select for use the HYDROXYPROPYL BETA-CYCLODEXTRIN of almost non-toxic sexual stimulus under using dosage and sucrose monolaurate mixture as solubilizing agent and stabilizing agent, thereby provide a kind of with HYDROXYPROPYL BETA-CYCLODEXTRIN and the sucrose monolaurate mixture sertraline hydrochloride oral liquid as solubilizing agent and stabilizing agent, wherein the weight ratio of HYDROXYPROPYL BETA-CYCLODEXTRIN and sucrose monolaurate is 9: 1.
The present invention is through selection, and plasticizer can be selected from sorbitol, glycerol, propylene glycol in the described adjuvant.
The present invention is through selection, and antiseptic can be selected from methyl hydroxybenzoate, propylparaben, benzoic acid, sodium benzoate in the described adjuvant.
The present invention is through selection, and aromatic can be selected from minty note essence, fragrant citrus essence and strawberry essence in the described adjuvant.
The preparation method of sertraline hydrochloride oral liquid may further comprise the steps: water intaking is an amount of, is heated to boiling, adds solubilizing agent and stabilizing agent and makes dissolving, adds antiseptic again and makes dissolving, puts coldly, gets plasticizer and an amount of aromatic, and solubilizer filters to full dose.
The hydrochloric acid house of prescription of the present invention and method preparation is got the woods oral liquid, adopt HYDROXYPROPYL BETA-CYCLODEXTRIN and sucrose monolaurate mixture as solubilizing agent and stabilizing agent, effectively raise the dissolubility of sertraline hydrochloride, supplementary product consumption is also less relatively, and just can obtain in the presence of the surfactant-free being suitable for clinical practice, storage can not separated out solid sertraline hydrochloride oral liquid under low temperature or the room temperature, thereby guaranteed the curative effect of medicine.
The specific embodiment
Come medical composition of the present invention done further specifying by following examples, but be not limited in following example.
Embodiment 1:
| The hydrochloric acid house is got woods | ?2.00g |
| HYDROXYPROPYL BETA-CYCLODEXTRIN | ?0.90g |
| Sucrose monolaurate | ?0.10g |
| Sorbitol | ?15.0g |
| Methyl hydroxybenzoate | ?15.0mg |
| Fragrant citrus essence | ?9.00mg |
| Pure water | Add to 100ml |
Preparation method:
It is an amount of to get pure water, is heated to boiling, after adding HYDROXYPROPYL BETA-CYCLODEXTRIN and sucrose monolaurate make dissolving, adds the hydrochloric acid house and gets woods, add methyl hydroxybenzoate, put coldly, add sorbitol, stir and make dissolving, add fragrant citrus essence again, by filtering with microporous membrane, promptly.
The comparative example 1:
| The hydrochloric acid house is got woods | ?2.00g |
| HYDROXYPROPYL BETA-CYCLODEXTRIN | ?4.00g |
| Tween 80 | ?0.10g |
| Sorbitol | ?15.0g |
| Methyl hydroxybenzoate | ?15.0mg |
| Fragrant citrus essence | ?9.00mg |
| 0.1MnaOH solution | ?2ml |
| Pure water | Add to 100ml |
Preparation method:
HYDROXYPROPYL BETA-CYCLODEXTRIN made 20% aqueous solution, hydrochloric acid house is got in the aqueous solution that woods adds to HYDROXYPROPYL BETA-CYCLODEXTRIN, and the limit edged stirs, and adds tween 80,50～60 ℃ of heating 10～20min, add the PH regulator after molten entirely and make solution PH to 7.0 ± 0.5, and add sorbitol, methyl hydroxybenzoate, fragrant citrus essence, and be diluted with water to 100ml, 60 ℃ of heating 15～20min, cold slightly, with filtering with microporous membrane, promptly.
Embodiment 2:
| The hydrochloric acid house is got woods | ?1.20g |
| HYDROXYPROPYL BETA-CYCLODEXTRIN | ?0.54g |
| Sucrose monolaurate | ?0.06g |
| Mannitol | ?10.0g |
| Propylparaben | ?14.0mg |
| Strawberry essence | ?5.00mg |
| Pure water | Add to 100ml |
Preparation method:
It is an amount of to get pure water, is heated to boiling, adds HYDROXYPROPYL BETA-CYCLODEXTRIN and sucrose monolaurate and makes dissolving back adding hydrochloric acid house get woods, adds propylparaben, put coldly, add mannitol, stir and make dissolving, add strawberry essence again, by filtering with microporous membrane, promptly.
Embodiment 3:
| The hydrochloric acid house is got woods | ?2.50g |
| HYDROXYPROPYL BETA-CYCLODEXTRIN | ?1.08g |
| Sucrose monolaurate | ?0.12g |
| Propylene glycol | ?25.0g |
| Sodium benzoate | ?20.0mg |
| Strawberry essence | ?10.00mg |
| Pure water | Add to 100ml |
Preparation method:
It is an amount of to get pure water, is heated to boiling, adds HYDROXYPROPYL BETA-CYCLODEXTRIN and sucrose monolaurate and makes dissolving back adding hydrochloric acid house get woods, adds sodium benzoate, put coldly, add propylene glycol, stir and make dissolving, add strawberry essence again, by filtering with microporous membrane, promptly.
We compare embodiment 1 with present common method (comparative example 1):
Among the comparative example 1, added the surfactant tween 80, and the HYDROXYPROPYL BETA-CYCLODEXTRIN consumption is 4g;
Among the embodiment 1, under the essentially identical situation of all the other supplementary material consumptions, sucrose monolaurate with same dose has replaced the surfactant tween 80, its HYDROXYPROPYL BETA-CYCLODEXTRIN consumption is 0.9g, / 4th amounts for HYDROXYPROPYL BETA-CYCLODEXTRIN among the comparative example 1 obviously are better than comparative example 1.
Claims (7)
1. sertraline hydrochloride oral liquid is characterized in that comprising:
Sertraline hydrochloride 1.0～2.8wt%
Mixture 0.5～the 1.4wt% of stabilizing agent and solubilizing agent
Thickening agent 10～30wt%
Antiseptic 0.01～0.5wt%
Aromatic 0.005～0.05wt%
Solvent 66～87wt%.
2. oral liquid according to claim 1, the mixture that it is characterized in that described solubilizing agent and stabilizing agent is the mixture of HYDROXYPROPYL BETA-CYCLODEXTRIN and sucrose monolaurate.
3. according to the described described oral liquid of claim 2, the weight ratio that it is characterized in that HYDROXYPROPYL BETA-CYCLODEXTRIN and sucrose monolaurate is 9: 1.
4. oral liquid according to claim 1 is characterized in that described thickening agent is selected from sorbitol, glycerol or propylene glycol.
5. oral liquid according to claim 1 is characterized in that described antiseptic is selected from methyl hydroxybenzoate, propylparaben, benzoic acid or sodium benzoate.
6. oral liquid according to claim 1 is characterized in that described aromatic is selected from Herba Menthae essence, fragrant citrus essence or strawberry essence.
7. the preparation method of oral liquid according to claim 1, it is characterized in that may further comprise the steps: water intaking is an amount of, be heated to boiling, adding solubilizing agent and stabilizing agent makes the dissolving back add principal agent, add antiseptic again and make dissolving, put coldly, get sweeting agent, plasticizer and an amount of aromatic, solubilizer filters to full dose.
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| Application Number | Priority Date | Filing Date | Title |
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| CN 200810116330 CN101623252A (en) | 2008-07-09 | 2008-07-09 | Sertraline hydrochloride oral liquid and preparation method thereof |
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| Application Number | Priority Date | Filing Date | Title |
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| CN 200810116330 CN101623252A (en) | 2008-07-09 | 2008-07-09 | Sertraline hydrochloride oral liquid and preparation method thereof |
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| CN101623252A true CN101623252A (en) | 2010-01-13 |
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Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104054704A (en) * | 2014-03-26 | 2014-09-24 | 中国人民解放军第三军医大学第一附属医院 | Hydroxypropyl-beta-cyclodextrin supermolecular inclusion complex of methylparaben, preparation method of inclusion complex and use method of inclusion complex |
| CN104971063A (en) * | 2015-06-17 | 2015-10-14 | 天津市聚星康华医药科技有限公司 | Medicinal composition containing tadalafil, and preparation method thereof |
| CN104971066A (en) * | 2015-06-17 | 2015-10-14 | 天津市聚星康华医药科技有限公司 | Medicinal composition containing vardenafil, and preparation method thereof |
| CN109908354A (en) * | 2017-12-12 | 2019-06-21 | 万特制药(海南)有限公司 | Sertraline hydrochloride takes orally concentrate and its preparation process |
-
2008
- 2008-07-09 CN CN 200810116330 patent/CN101623252A/en active Pending
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104054704A (en) * | 2014-03-26 | 2014-09-24 | 中国人民解放军第三军医大学第一附属医院 | Hydroxypropyl-beta-cyclodextrin supermolecular inclusion complex of methylparaben, preparation method of inclusion complex and use method of inclusion complex |
| CN104971063A (en) * | 2015-06-17 | 2015-10-14 | 天津市聚星康华医药科技有限公司 | Medicinal composition containing tadalafil, and preparation method thereof |
| CN104971066A (en) * | 2015-06-17 | 2015-10-14 | 天津市聚星康华医药科技有限公司 | Medicinal composition containing vardenafil, and preparation method thereof |
| CN109908354A (en) * | 2017-12-12 | 2019-06-21 | 万特制药(海南)有限公司 | Sertraline hydrochloride takes orally concentrate and its preparation process |
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Application publication date: 20100113 |