CN102327213A - Triamcinolone acetonaide acetate nano eye drops and preparation method thereof - Google Patents
Triamcinolone acetonaide acetate nano eye drops and preparation method thereof Download PDFInfo
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- CN102327213A CN102327213A CN 201110287454 CN201110287454A CN102327213A CN 102327213 A CN102327213 A CN 102327213A CN 201110287454 CN201110287454 CN 201110287454 CN 201110287454 A CN201110287454 A CN 201110287454A CN 102327213 A CN102327213 A CN 102327213A
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- triamcinolone acetonide
- acetonide acetate
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Abstract
The invention relates to triamcinolone acetonaide acetate nano eye drops and a preparation method thereof, wherein the triamcinolone acetonaide acetate nano eye drops are prepared in the way that the triamcinolone acetonaide acetate and the chitosan nano carrier are prepared into nanoparticles according to the proportion of 1/2 and then are mixed with the distilled water. The invention provides the triamcinolone acetonaide acetate nano eye drops which have simple preparation process, can prevent pain and complication which are caused by local injection, facilitate clinical use and are easy to be accepted by patients and the preparation method of the triamcinolone acetonaide acetate nano eye drops.
Description
Technical field
The invention belongs to field of medicaments, relate to a kind of eye drop and preparation method thereof, relate in particular to a kind of triamcinolone acetonide acetate nano eye drop and preparation method thereof.
Background technology
Triamcinolone acetonide is a kind of long-acting glucocorticoid, and it has powerful antiinflammatory action, and antiinflammatory and allergic effect are strong and lasting, also are the common drugs of ophthalmology simultaneously.It can not only alleviate hyperemia; Reduce the permeability of blood capillary, the inflammation-inhibiting cell moves to inflammation part, can also stop inflammatory mediator such as kassinin kinin class, histamine, slow reacting substance etc. to react; Suppress cytophagous function; Stablize lysosome membrane, stop complement to participate in inflammatory reaction, the reparation of tissue injury etc. behind the inflammation-inhibiting.In addition, it also has immunosuppressant, influences effects such as metabolism and hemopoietic system, is widely used clinically.Triamcinolone acetonide is mainly used in uveitis, macular edema, optic neuritis, ocular injury, glass in field of ophthalmology, and to cut operation auxiliary etc.But because the restriction of the characteristics of glucocorticoid itself and dosage form (triamcinolone acetonide only has injection and non-eye to use unguentum); In clinical use, complication such as high intraocular pressure, endophthalmitis, intraocular hemorrhage, the formation of promotion cataract, retinal toxicity have inevitably appearred.In addition, some ophthalmic diseases often must be repeatedly and long term administration, more increased the incidence rate of complication.Therefore, for the focus that is modified into of triamcinolone acetonide conventional dosage forms and administering mode for Recent study.In clinical ophthalmology medication practice, because advantages such as eye drop is easy to use, better tolerance become the first-selected dosage form of clinical medicine for external use.But reflexive lacrimal secretion or twinkle during topical can't contact medicine with eye list structure composition, can't pass through barrier structure in addition, makes can't reach effective drug level in the eye inner tissue, thereby needs administration frequent, high concentration.Nonetheless, effect is also not satisfactory sometimes, moreover effective drug level also difficulty is kept for a long time, and can not reach the purpose of treatment.Simultaneously, the side effect that conjunctiva absorbs and the nasolacrimal duct drain can produce whole body.The characteristics of administration nano-drug administration system can overcome the shortcoming that the local removing of traditional eye drop is fast, bioavailability is low and systemic absorption has side effects; The nano carrier material of colloidal nature helps prolong drug in the local time that stops of administration; Improve the cornea penetrance of medicine, and then improve bioavailability of medicament, help to keep effective drug level in the part; Reducing complication and side effect, also is puzzlement ophthalmology ophthalmologist's problem.Yet in clinical practice, if long-term whole body uses glucocorticoid can produce some toxic and side effects, during topical application, because that drug metabolism is eliminated is fast, bioavailability is low, drug effect is of short duration, needs multiple dosing etc., usually makes poor effect.And multiple dosing can produce complication such as chemosis when ophthalmic applications, and reduces patient's toleration.Therefore, the improvement of new hormone dosage form has very big using value.
Summary of the invention
In order to solve the above-mentioned technical problem that exists in the background technology, the invention provides a kind of prepare process simple, can avoid misery that local injection brings and complication, make things convenient for clinical use and easily by triamcinolone acetonide acetate nano eye drop that the patient accepted and preparation method thereof.
Technical solution of the present invention is: the invention provides a kind of triamcinolone acetonide acetate nano eye drop, it is characterized in that: said triamcinolone acetonide acetate nano eye drop is become to be mixed with distilled water behind the nanoparticle in ratio preparation in 1: 2 by triamcinolone acetonide acetate, chitosan nano carrier again and forms.
A kind of method for preparing of triamcinolone acetonide acetate nano eye drop, its special character is: the method for preparing of said triamcinolone acetonide acetate nano eye drop may further comprise the steps:
1) preparation chitosan nano carrier;
2) triamcinolone acetonide acetate is wrapped in the resulting chitosan nano carrier of step 1), obtains containing the chitosan nano of triamcinolone acetonide acetate;
3) with step 2) resulting chitosan nano and the distilled water that contains triamcinolone acetonide acetate be hybridly prepared into the triamcinolone acetonide acetate nano eye drop.
Above-mentioned steps 1) concrete implementation is:
In 10-100mg deoxycholic acid chitosan derivatives, add 3-30ml distilled water stirring and dissolving, obtain chitosan nano carrier.
Last step 2) concrete implementation is:
2.1) take by weighing the 5-50mg triamcinolone acetonide acetate and be dissolved in the 0.3-3ml oxolane;
2.2) with step 2.1) resulting drips of solution is added in the resulting chitosan nano carrier of step 1), and dropping distilled water 1-10ml, at room temperature continue to stir;
2.3) make the oxolane volatilization in stirred in water bath;
2.4) with step 2.3) resulting solution carries out centrifugal and collect supernatant, this supernatant is the chitosan nano of load triamcinolone acetonide.
Above-mentioned steps 2.2) in step 2.1) speed of dripping that is added in the resulting chitosan nano carrier of step 1) of resulting drips of solution is not higher than 1ml/min.
Above-mentioned steps 2.2) at room temperature continues to stir in to be not less than 24 hours.
Above-mentioned steps 2.3) temperature of water-bath is not less than 40 ° in.
Above-mentioned steps 2.4) centrifugal condition is 5000r/min in, 5min.
Above-mentioned steps 3) it is 7.5 triamcinolone acetonide acetate nano eye drop that chitosan nano and the distilled water that contains triamcinolone acetonide acetate in is hybridly prepared into pH.
The concentration of above-mentioned triamcinolone acetonide acetate nano eye drop is 1%-3%.
Advantage of the present invention is:
The method for preparing of triamcinolone acetonide acetate nano eye drop provided by the present invention; Triamcinolone acetonide acetate is wrapped in the chitosan nano carrier material; Again itself and distilled water are formulated as eye drop after making nanoparticle; Be that the triamcinolone acetonide acetate preparation is become the nano eyedrop dosage form, compare, use more easy, safety with injection type.
The specific embodiment
The present invention is prepared as nanoparticle with triamcinolone acetonide acetate, and it is formulated as eye drop, is the novel form of triamcinolone acetonide acetate clinical practice.
Principle of the present invention is: triamcinolone acetonide acetate being wrapped in the chitosan nano carrier material, again itself and distilled water being formulated as eye drop after making nanoparticle, is that the triamcinolone acetonide acetate preparation is become the nano eyedrop dosage form.
Embodiment one:
Take by weighing 10mg deoxycholic acid chitosan derivatives and place flask; Add the 3ml distilled water, stirring and dissolving takes by weighing the 5mg triamcinolone acetonide acetate; Be dissolved in the 0.3ml oxolane; Slowly (drip speed) and be added drop-wise in the above-mentioned chitosan solution, and then slowly drip distilled water 1ml, at room temperature continue stirring until few 24h less than 1ml/min.Then be not less than to stir in 40 ℃ and make the oxolane volatilization in water-bath.After treating oxolane volatilization, centrifugal (5000r/min, 5min), the supernatant is the chitosan nano of load triamcinolone acetonide with mixed liquor.At last this nanoparticle and distilled water are formulated as 1% concentration, pH=7.5 eye drop.
Embodiment two:
Take by weighing 8mg deoxycholic acid chitosan derivatives and place flask; Add the 2.7ml distilled water, stirring and dissolving takes by weighing the 10mg triamcinolone acetonide acetate; Be dissolved in the 0.675ml oxolane; Slowly (drip speed) and be added drop-wise in the above-mentioned chitosan solution, and then slowly drip distilled water 0.8ml, at room temperature continue stirring until few 24h less than 1ml/min.Then be not less than to stir in 40 ℃ and make the oxolane volatilization in water-bath.After treating oxolane volatilization, centrifugal (5000r/min, 5min), the supernatant is the chitosan nano of load triamcinolone acetonide with mixed liquor.At last this nanoparticle and distilled water are formulated as 1%-3% concentration, pH=7.5 eye drop.
Embodiment three:
Take by weighing 20mg deoxycholic acid chitosan derivatives and place flask; Add the 8ml distilled water, stirring and dissolving takes by weighing the 10mg triamcinolone acetonide acetate; Be dissolved in the 0.8ml oxolane; Slowly (drip speed) and be added drop-wise in the above-mentioned chitosan solution, and then slowly drip distilled water 2ml, at room temperature continue stirring until few 24h less than 1ml/min.Then be not less than to stir in 40 ℃ and make the oxolane volatilization in water-bath.After treating oxolane volatilization, centrifugal (5000r/min, 5min), the supernatant is the chitosan nano of load triamcinolone acetonide with mixed liquor.At last this nanoparticle and distilled water are formulated as 1%-3% concentration, pH=7.5 eye drop.
Embodiment four:
Take by weighing 40mg deoxycholic acid chitosan derivatives and place flask; Add the 18ml distilled water, stirring and dissolving takes by weighing the 20mg triamcinolone acetonide acetate; Be dissolved in the 1.5ml oxolane; Slowly (drip speed) and be added drop-wise in the above-mentioned chitosan solution, and then slowly drip distilled water 5ml, at room temperature continue stirring until few 24h less than 1ml/min.Then be not less than to stir in 40 ℃ and make the oxolane volatilization in water-bath.After treating oxolane volatilization, centrifugal (5000r/min, 5min), the supernatant is the chitosan nano of load triamcinolone acetonide with mixed liquor.At last this nanoparticle and distilled water are formulated as 1%-3% concentration, pH=7.5 eye drop.
Embodiment five:
Take by weighing 100mg deoxycholic acid chitosan derivatives and place flask; Add the 30ml distilled water, stirring and dissolving takes by weighing the 50mg triamcinolone acetonide acetate; Be dissolved in the 2ml oxolane; Slowly (drip speed) and be added drop-wise in the above-mentioned chitosan solution, and then slowly drip distilled water 8ml, at room temperature continue stirring until few 24h less than 1ml/min.Then be not less than to stir in 40 ℃ and make the oxolane volatilization in water-bath.After treating oxolane volatilization, centrifugal (5000r/min, 5min), the supernatant is the chitosan nano of load triamcinolone acetonide with mixed liquor.At last this nanoparticle and distilled water are formulated as 1%-3% concentration, pH=7.5 eye drop.
Embodiment six:
Take by weighing 60mg deoxycholic acid chitosan derivatives and place flask; Add the 20ml distilled water, stirring and dissolving takes by weighing the 30mg triamcinolone acetonide acetate; Be dissolved in the 2ml oxolane; Slowly (drip speed) and be added drop-wise in the above-mentioned chitosan solution, and then slowly drip distilled water 5ml, at room temperature continue stirring until few 24h less than 1ml/min.Then be not less than to stir in 40 ℃ and make the oxolane volatilization in water-bath.After treating oxolane volatilization, centrifugal (5000r/min, 5min), the supernatant is the chitosan nano of load triamcinolone acetonide with mixed liquor.At last this nanoparticle and distilled water are formulated as 1%-3% concentration, pH=7.5 eye drop.
Embodiment seven:
Take by weighing 80mg deoxycholic acid chitosan derivatives and place flask; Add the 65ml distilled water, stirring and dissolving takes by weighing the 40mg triamcinolone acetonide acetate; Be dissolved in the 7ml oxolane; Slowly (drip speed) and be added drop-wise in the above-mentioned chitosan solution, and then slowly drip distilled water 20ml, at room temperature continue stirring until few 24h less than 1ml/min.Then be not less than to stir in 40 ℃ and make the oxolane volatilization in water-bath.After treating oxolane volatilization, centrifugal (5000r/min, 5min), the supernatant is the chitosan nano of load triamcinolone acetonide with mixed liquor.At last this nanoparticle and distilled water are formulated as 1%-3% concentration, pH=7.5 eye drop.
Claims (10)
1. triamcinolone acetonide acetate nano eye drop is characterized in that: said triamcinolone acetonide acetate nano eye drop is prepared from distilled water after becoming nanoparticle triamcinolone acetonide acetate, chitosan in ratio preparation in 1: 2 again.
2. the method for preparing of a triamcinolone acetonide acetate nano eye drop, it is characterized in that: the method for preparing of said triamcinolone acetonide acetate nano eye drop may further comprise the steps:
1) preparation chitosan nano carrier;
2) triamcinolone acetonide acetate is wrapped in the resulting chitosan nano carrier of step 1), obtains containing the chitosan nano of triamcinolone acetonide acetate;
3) with step 2) the resulting chitosan nano that contains triamcinolone acetonide acetate mixes with distilled water, is mixed with the triamcinolone acetonide acetate nano eye drop.
3. the method for preparing of triamcinolone acetonide acetate nano eye drop according to claim 2 is characterized in that: the concrete implementation of said step 1) is:
In 10-100mg deoxycholic acid chitosan derivatives, add 3-30ml distilled water stirring and dissolving, obtain chitosan nano carrier.
4. the method for preparing of triamcinolone acetonide acetate nano eye drop according to claim 3 is characterized in that: concrete implementation said step 2) is:
2.1) take by weighing the 5-50mg triamcinolone acetonide acetate and be dissolved in the 0.3-3ml oxolane;
2.2) with step 2.1) resulting drips of solution is added in the resulting chitosan nano carrier of step 1), and dropping distilled water 1-10ml, at room temperature continue to stir;
2.3) make the oxolane volatilization in stirred in water bath;
2.4) with step 2.3) resulting solution carries out centrifugal and collect supernatant, this supernatant is the chitosan nano of load triamcinolone acetonide.
5. the method for preparing of triamcinolone acetonide acetate nano eye drop according to claim 4 is characterized in that: said step 2.2) with step 2.1) speed of dripping that is added in the resulting chitosan nano carrier of step 1) of resulting drips of solution is not higher than 1ml/min.
6. the method for preparing of triamcinolone acetonide acetate nano eye drop according to claim 5 is characterized in that: at room temperature continue to stir said step 2.2) to be not less than 24 hours.
7. the method for preparing of triamcinolone acetonide acetate nano eye drop according to claim 6 is characterized in that: the temperature of water-bath is not less than 40 ° said step 2.3).
8. the method for preparing of triamcinolone acetonide acetate nano eye drop according to claim 7 is characterized in that: centrifugal condition is 5000r/min said step 2.4), 5min.
9. according to the method for preparing of the described triamcinolone acetonide acetate nano eye drop of the arbitrary claim of claim 2-8, it is characterized in that: it is 7.5 triamcinolone acetonide acetate nano eye drop that chitosan nano and the distilled water that contains triamcinolone acetonide acetate in the said step 3) is hybridly prepared into pH.
10. the method for preparing of triamcinolone acetonide acetate nano eye drop according to claim 9 is characterized in that: the concentration of said triamcinolone acetonide acetate nano eye drop is 1%-3%.
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN108635340A (en) * | 2018-05-11 | 2018-10-12 | 昆明医科大学第二附属医院 | A kind of novel Triamcinolone acetonide polymer drug long-acting slow-release diaphragm and preparation method thereof |
| CN115444991A (en) * | 2022-09-08 | 2022-12-09 | 沈阳贺麒医疗科技合伙企业(有限合伙) | Drug-loaded matrix and preparation method thereof |
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| CN101332186A (en) * | 2008-04-11 | 2008-12-31 | 广州贝氏药业有限公司 | Medicine composition for injecting triamcinolone acetonide palmitate lipid microsphere and preparation method thereof |
| CN101816627A (en) * | 2010-04-16 | 2010-09-01 | 浙江大学 | Synergistic treatment type multi-material sustained-release eye drop and preparation method |
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2011
- 2011-09-26 CN CN 201110287454 patent/CN102327213A/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101332186A (en) * | 2008-04-11 | 2008-12-31 | 广州贝氏药业有限公司 | Medicine composition for injecting triamcinolone acetonide palmitate lipid microsphere and preparation method thereof |
| CN101816627A (en) * | 2010-04-16 | 2010-09-01 | 浙江大学 | Synergistic treatment type multi-material sustained-release eye drop and preparation method |
Non-Patent Citations (1)
| Title |
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| 《中国组织工程研究与临床康复》 20100716 周怀胜，等 两亲性壳聚糖衍生物负载及缓释醋酸曲安奈德的性能 5371-5374 1-10 第14卷, 第29期 * |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN108635340A (en) * | 2018-05-11 | 2018-10-12 | 昆明医科大学第二附属医院 | A kind of novel Triamcinolone acetonide polymer drug long-acting slow-release diaphragm and preparation method thereof |
| CN115444991A (en) * | 2022-09-08 | 2022-12-09 | 沈阳贺麒医疗科技合伙企业(有限合伙) | Drug-loaded matrix and preparation method thereof |
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Application publication date: 20120125 |