CN103432075A - Desloratadine nanoemulsion and preparation method thereof - Google Patents
Desloratadine nanoemulsion and preparation method thereof Download PDFInfo
- Publication number
- CN103432075A CN103432075A CN2013104209098A CN201310420909A CN103432075A CN 103432075 A CN103432075 A CN 103432075A CN 2013104209098 A CN2013104209098 A CN 2013104209098A CN 201310420909 A CN201310420909 A CN 201310420909A CN 103432075 A CN103432075 A CN 103432075A
- Authority
- CN
- China
- Prior art keywords
- desloratadine
- emulsion
- nano
- surfactant
- ethyl acetate
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
Abstract
The invention discloses a desloratadine nanoemulsion, wherein the grain size of liquid drops is ranged within 10-100nm. The desloratadine nanoemulsion is prepared from the following raw materials in percent by weight: 0.01-0.10% of desloratadine, 6.00-36.00% of ethyl acetate, 14.00-36.00% of a surfactant, 10.00-20.00% of a cosurfactant and 7.90-60.98% of distilled water based on 100% of total components. According to the desloratadine nanoemulsion, the medicine stability of desloratadine in the processing process is improved, the bioavailability is improved, the metabolic time of medicines in emulsion is slowed down, the use level of auxiliary materials is reduced, and the production cost is lowered. The desloratadine nanoemulsion has a wide market prospect in the field of medicine.
Description
Technical field
The invention belongs to field of medicaments, relate to a kind of new formulation of Desloratadine, particularly the Desloratadine nano-emulsion.
Background technology
The long-acting tricyclic antidepressants antihistaminic that Desloratadine is non-sedating, be the active metabolite of loratadine, can pass through optionally antagonism peripheral H1-receptor.In addition, results of in vitro studies, this product can suppress histamine and discharge from people's mastocyte.The zooscopy prompting, be difficult for by blood brain barrier, can be used for treatment seasonality and catarrhus perennialis, anaphylaxis conjunctivitis, urticaria.But Desloratadine is water insoluble, absorbability is poor, has affected curative effect.
Utilize the fabrication technology, take nano-emulsion as carrier, will be prepared into the Desloratadine Nano medication.The new drug of preparing can overcome the shortcoming that dissolubility is low, bioavailability is low, and easy absorption is arranged, the advantage that therapeutic effect improves greatly.Combine with nanotechnology by Desloratadine, develop a kind of efficient, safe new drug, important production and the meaning of applying are arranged.
Summary of the invention
For above-mentioned problems of the prior art and defect, the object of the present invention is to provide that a kind of dissolubility is good, physical property is stable, not volatile, the good preservation, finely dispersed Desloratadine nanometer emulsion oral liquid.
The technical scheme that realizes the foregoing invention purpose is the Desloratadine nano-emulsion, and it is to be made by the raw material of following weight percentage ratio:
Desloratadine 0.01 ﹪～0.10 ﹪, ethyl acetate 6.00 ﹪～36.00 ﹪, surfactant 14.00 ﹪～36.00 ﹪, cosurfactant 10.00 ﹪～20.00 ﹪ and distilled water 7.90%～60.98% form, and total component is 100 ﹪.
A kind of Desloratadine nano-emulsion nanometer emulsion oral liquid, optimization formula is:
Desloratadine 0.02 ﹪～0.10 ﹪, ethyl acetate 7.00 ﹪～36.00 ﹪, surfactant 15.00 ﹪～36.00 ﹪, cosurfactant 10.00 ﹪～20.00 ﹪ and distilled water 7.90%～60.98% form, and total component is 100 ﹪.
A kind of Desloratadine nano-emulsion nanometer emulsion oral liquid, optimum formula is:
A kind of Desloratadine nano-emulsion, it is characterized in that, the size droplet diameter of this nano-emulsion is between 10～100 nm, raw material by following weight percentage ratio is made: Desloratadine 0.10 ﹪, ethyl acetate 18.00 ﹪, surfactant 26.00 ﹪, cosurfactant 10.00 ﹪ and distilled water 45.90% form, and total component is 100 ﹪.
Desloratadine nano-emulsion of the present invention has overcome its poorly soluble shortcoming, and arrives the effect easily absorbed.Desloratadine nano-emulsion of the present invention adopts lower temperature in preparation process, has avoided the loss of principal agent, thus content evenly accurately, steady quality, and prepare easyly, be easy to expanding production.
In the selection of surfactant, the present invention selects the nonionic surfactant of avirulence and good biocompatibility.Nonionic surfactant is more stable in solution, is not subject to the impact of strong electrolyte, inorganic salts, also is not subject to the impact of soda acid, and good with the compatibility of other surfactants, and haemolysis is less.In theory, the preparation of O/W type nanometer emulsion needs the HLB value of surfactant between 8～18, consider preparation technology's simplicity, be the easy formative of nano-emulsion and the stability of the nano-emulsion prepared, the present invention selects the liquid nonionic surfactant of HLB between 10～15.Surfactant is tween 80 or castor oil polyoxyethylene ether.
Hydrophilic and oleophilic value (HLB) for the adjustment form surface-active agent, can further reduce interfacial tension, increase flexibility and the rigidity of film, be inserted in interfacial film, promote the formation of the film that radius of curvature is very little, enlarge nano-emulsion and form zone, the present invention selects bland cosurfactant, mainly contain ethanol, 1,2-PD, glycerol and n-butyl alcohol.
When the present invention is close with surfactant according to the HLB when the required surfactant of emulsifying oil phase, the principle that formed emulsion is stable, the oils and fats of selecting is ethyl acetate.Under this oily room temperature, be in a liquid state.
The preparation method of Desloratadine nano-emulsion of the present invention, comprise the following steps:
(1) preparation of surfactant phase takes surfactant by formula proportion, and helps surface activity composite in proportion, calculates the HLB value of this system, stirs.The HLB value of common emulsifying agent can be found in some chemical industry handbooks, as " the chemical products handbook of chemical industry publishing house.Because hydrophile-lipophile balance (HLB) value of surfactant has additive properties, the available quality averaging method is obtained the HLB value of surfactant.For example, after two kinds of surfactant A, B mix, the hydrophile-lipophile balance HLBAB value of its mixed surfactant is
HLBAB＝（WAHLBA＋WBHLBB）/（WA＋WB）
WA in formula, WB---the quality of blend surfactants A, B;
HLBA, the HLB value of HLBB---surfactant A, B.
(2) preparation of oil phase, according to the HLB value of surfactant phase, is selected oil, adjusts its ratio, makes the required HLB value of its emulsifying close with the HLB of surfactant phase.
(3) change the ratio of surfactant phase and oil phase in rule, add wherein formula proportion, stirring makes it whole dissolvings, at 20 ℃～25 ℃ slow adding distil waters, fully stir, until colourless, the faint yellow or yellow O/W type nanometer emulsion that forms clear, viscosity is little and there is mobility.
Droplet diameter distribution of the present invention is between 10～100nm, and outward appearance is colourless, faint yellow or yellow transparent liquid, has good stability:
Ageing stability refers to when nanometer emulsion oral liquid is preserved under room temperature nature change condition, and outward appearance extends and the degree that changes in time.This Desloratadine nano-emulsion is transparent lastingly, does not find muddy or precipitation, illustrates that ageing stability is good.This is an important indicator estimating nanometer emulsion oral liquid.
Desloratadine nano-emulsion of the present invention compared with prior art, has the following advantages:
1) thermodynamic stability is high.During preparation, operation is fairly simple, not phase-splitting, do not precipitate, and bin stability improves;
2) light transmission is good, and any inhomogeneities or sedimentary existence easily are found, and sensible quality improves;
3) antiseptic property improves, because decentralized photo liquid is smaller, can prevent the intrusion of antibacterial, increases the dissolubility of some active ingredients simultaneously;
4) there is good solubilization, can effectively improve the dissolubility of insoluble drug;
5) can improve the Desloratadine dissolubility, delay the regression time of Desloratadine, thereby improve the bioavailability of Desloratadine;
6) method technique is simple, is applicable to large-scale production.
The specific embodiment
Below the embodiment that provides by the inventor further set forth the preparation method of Desloratadine nano-emulsion of the present invention.
embodiment 1
Accurately take Desloratadine 0.10g, ethyl acetate 18.00g, tween 80 26.00g, n-butyl alcohol 10.00 g, put into beaker, under 20 ℃ of room temperature conditions, hand operated mixing is by its abundant mix homogeneously, stir fully, then slowly add wherein distilled water, adding distil water limit, limit hand operated mixing, during beginning, the system viscosity is less, increase along with the distillation water yield, it is sticky that system can become, continue to drip and constantly stir, when system unexpected when thinning, what now produce is stable yellow transparent Desloratadine nano-emulsion, claims that its gross weight is 100.0g.
embodiment 2
Accurately take Desloratadine 0.01g, ethyl acetate 10.00g, tween 80 20.00g, n-butyl alcohol 10.00 g, put into beaker, under 20 ℃ of room temperature conditions, hand operated mixing is by its abundant mix homogeneously, stir fully, then slowly add wherein distilled water, adding distil water limit, limit hand operated mixing, during beginning, the system viscosity is less, increase along with the distillation water yield, it is sticky that system can become, continue to drip and constantly stir, when system unexpected when thinning, what now produce is stable yellow transparent Desloratadine nano-emulsion, claims that its gross weight is 100.0g.
embodiment 3
Really take Desloratadine 0.01g, ethyl acetate 6.00g, tween 80 36.00g, n-butyl alcohol 20.00 g, put into beaker, under 20 ℃ of room temperature conditions, hand operated mixing is by its abundant mix homogeneously, stir fully, then slowly add wherein distilled water, adding distil water limit, limit hand operated mixing, during beginning, the system viscosity is less, increase along with the distillation water yield, it is sticky that system can become, continue to drip and constantly stir, when system unexpected when thinning, what now produce is stable yellow transparent Desloratadine nano-emulsion, claims that its gross weight is 100.0g.
embodiment 4
Really take Desloratadine 0.02g, ethyl acetate 11.00g, castor oil polyoxyethylene ether 14.00g, ethanol 20.00 g, put into beaker, under 20 ℃ of room temperature conditions, hand operated mixing is by its abundant mix homogeneously, stir fully, then slowly add wherein distilled water, adding distil water limit, limit hand operated mixing, during beginning, the system viscosity is less, increase along with the distillation water yield, it is sticky that system can become, continue to drip and constantly stir, when system unexpected when thinning, what now produce is the stable faint yellow nano-emulsion of loratadine pellucidly, claims that its gross weight is 100.0g.
embodiment 5
Really take Desloratadine 0.02g, ethyl acetate 8.00g, tween 80 24.00g, n-butyl alcohol 11.00 g, put into beaker, under 20 ℃ of room temperature conditions, hand operated mixing is by its abundant mix homogeneously, stir fully, then slowly add wherein distilled water, adding distil water limit, limit hand operated mixing, during beginning, the system viscosity is less, increase along with the distillation water yield, it is sticky that system can become, continue to drip and constantly stir, when system unexpected when thinning, what now produce is stable yellow transparent Desloratadine nano-emulsion, claims that its gross weight is 100.0g.
embodiment 6
Really take Desloratadine 0.03g, ethyl acetate 10.00g, tween 80 18.00g, 1,2-PD 12.00 g, put into beaker, under 20 ℃ of room temperature conditions, hand operated mixing, by its abundant mix homogeneously, stirs fully, then slowly adds wherein distilled water, adding distil water limit, limit hand operated mixing, during beginning, the system viscosity is less, and along with the increase of the distillation water yield, it is sticky that system can become, continue to drip and constantly stir, unexpected when thinning when system, what now produce is stable yellow transparent Desloratadine nano-emulsion, claims that its gross weight is 100.0g.
embodiment 7
Really take Desloratadine 0.045g, ethyl acetate 13.27g, tween 80 29.40g, glycerol 18.00 g, put into beaker, under 20 ℃ of room temperature conditions, hand operated mixing is by its abundant mix homogeneously, stir fully, then slowly add wherein distilled water, adding distil water limit, limit hand operated mixing, during beginning, the system viscosity is less, increase along with the distillation water yield, it is sticky that system can become, continue to drip and constantly stir, when system unexpected when thinning, what now produce is stable yellow transparent Desloratadine nano-emulsion, claims that its gross weight is 100.0g.
embodiment 8
Really take Desloratadine 0.02g, ethyl acetate 7.00g, tween 80 13.00g, glycerol 19.00 g, put into beaker, under 20 ℃ of room temperature conditions, hand operated mixing is by its abundant mix homogeneously, stir fully, then slowly add wherein distilled water, adding distil water limit, limit hand operated mixing, during beginning, the system viscosity is less, increase along with the distillation water yield, it is sticky that system can become, continue to drip and constantly stir, when system unexpected when thinning, what now produce is stable yellow transparent Desloratadine nano-emulsion, claims that its gross weight is 100.0g.
embodiment 9
Really take Desloratadine 0.1g, ethyl acetate 36.00g, tween 80 36.00g, n-butyl alcohol 20.00 g, put into beaker, under 20 ℃ of room temperature conditions, hand operated mixing is by its abundant mix homogeneously, stir fully, then slowly add wherein distilled water, adding distil water limit, limit hand operated mixing, during beginning, the system viscosity is less, increase along with the distillation water yield, it is sticky that system can become, continue to drip and constantly stir, when system unexpected when thinning, what now produce is stable yellow transparent Desloratadine nano-emulsion, claims that its gross weight is 100.0g.
Below the embodiment that provides by the inventor further set forth the efficacy experiment of Desloratadine nano-emulsion of the present invention.
The experimenter 1: female, 58 years old 8 months.After oral this product, allergic symptom disappears rapidly, less than Desloratadine consumption, rapid-action, effective, without any untoward reaction.For the allergic dermatitis on skin, extraordinary curative effect is arranged, can bring into play local antianaphylactic effect by transdermal.
The experimenter 2: female, 30 years old.After oral this product, allergic symptom disappears rapidly, less than Desloratadine consumption, rapid-action, effective, without any untoward reaction.
Claims (3)
1. a Desloratadine nano-emulsion, it is characterized in that, the size droplet diameter of this nano-emulsion is between 10～100 nm, raw material by following weight percentage ratio is made: Desloratadine 0.01 ﹪～0.10 ﹪, ethyl acetate 6.00 ﹪～36.00 ﹪, surfactant 14.00 ﹪～36.00 ﹪, cosurfactant 10.00 ﹪～20.00 ﹪ and distilled water 7.90%～60.98% form, and total component is 100 ﹪; Oils and fats recited above is ethyl acetate; Surfactant is tween 80 or castor oil polyoxyethylene ether; Cosurfactant has ethanol, 1,2-PD, glycerol and n-butyl alcohol.
2. a Desloratadine nano-emulsion, it is characterized in that, the size droplet diameter of this nano-emulsion is between 10～100 nm, raw material by following weight percentage ratio is made: Desloratadine 0.02 ﹪～0.10 ﹪, ethyl acetate 7.00 ﹪～36.00 ﹪, surfactant 15.00 ﹪～36.00 ﹪,, cosurfactant 11.00 ﹪～20.00 ﹪ and distilled water 7.90%～60.98% form, total component is 100 ﹪.
3. a Desloratadine nano-emulsion, it is characterized in that, the size droplet diameter of this nano-emulsion is between 10～100 nm, raw material by following weight percentage ratio is made: Desloratadine 0.10 ﹪, ethyl acetate 18.00 ﹪, surfactant 26.00 ﹪, cosurfactant 10.00 ﹪ and distilled water 45.90% form, and total component is 100 ﹪.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2013104209098A CN103432075A (en) | 2013-09-17 | 2013-09-17 | Desloratadine nanoemulsion and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2013104209098A CN103432075A (en) | 2013-09-17 | 2013-09-17 | Desloratadine nanoemulsion and preparation method thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN103432075A true CN103432075A (en) | 2013-12-11 |
Family
ID=49685863
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN2013104209098A Pending CN103432075A (en) | 2013-09-17 | 2013-09-17 | Desloratadine nanoemulsion and preparation method thereof |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN103432075A (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110354075A (en) * | 2019-04-26 | 2019-10-22 | 沈阳药科大学 | A kind of Loratadine nano suspension and preparation method thereof |
| CN110840833A (en) * | 2019-11-22 | 2020-02-28 | 南京知和医药科技有限公司 | Sugar-free desloratadine oral solution and preparation process thereof |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101390860A (en) * | 2007-09-21 | 2009-03-25 | 北京德众万全药物技术开发有限公司 | Desloratadine syrup and preparation method thereof |
| CN102274178A (en) * | 2011-08-25 | 2011-12-14 | 西北农林科技大学 | Acetyl-isovaleryl tylosin nanoemulsion medicine and preparation method thereof |
| CN102302448A (en) * | 2011-08-25 | 2012-01-04 | 西北农林科技大学 | Oil-in-water furazolidone nano emulsion antibacterial medicament and preparation method thereof |
| CN102579435A (en) * | 2012-02-19 | 2012-07-18 | 西北农林科技大学 | Oil-in-water compound fluconazole nano-emulsion and preparation method thereof |
-
2013
- 2013-09-17 CN CN2013104209098A patent/CN103432075A/en active Pending
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101390860A (en) * | 2007-09-21 | 2009-03-25 | 北京德众万全药物技术开发有限公司 | Desloratadine syrup and preparation method thereof |
| CN102274178A (en) * | 2011-08-25 | 2011-12-14 | 西北农林科技大学 | Acetyl-isovaleryl tylosin nanoemulsion medicine and preparation method thereof |
| CN102302448A (en) * | 2011-08-25 | 2012-01-04 | 西北农林科技大学 | Oil-in-water furazolidone nano emulsion antibacterial medicament and preparation method thereof |
| CN102579435A (en) * | 2012-02-19 | 2012-07-18 | 西北农林科技大学 | Oil-in-water compound fluconazole nano-emulsion and preparation method thereof |
Non-Patent Citations (3)
| Title |
|---|
| NEMANJA KOLASINAC等: "Solubility enhancement of desloratadine by solid dispersion in poloxamers", 《INTERNATIONAL JOURNAL OF PHARMACEUTICS 》 * |
| 李海燕等: "氯雷他定自微乳制剂的体内外评价", 《中国药学杂志》 * |
| 杨祥良: "《纳米药物》", 31 October 2007 * |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110354075A (en) * | 2019-04-26 | 2019-10-22 | 沈阳药科大学 | A kind of Loratadine nano suspension and preparation method thereof |
| CN110840833A (en) * | 2019-11-22 | 2020-02-28 | 南京知和医药科技有限公司 | Sugar-free desloratadine oral solution and preparation process thereof |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CN1931164A (en) | Nanometer miconazole nitrate emulsion medicine and its prepn process | |
| CN104739656B (en) | A kind of nanoemulsions containing anionic Gemini surfactant and preparation method thereof | |
| NZ591205A (en) | Pharmaceutical compositions comprising clevidipine and methods for producing low impurity concentrations of the same | |
| CN1931293A (en) | Oil-in-water type nanometer grassleaved sweetflag oil emulsion oral liquid and its prepn process | |
| CN103393631A (en) | Flurbiprofen axetil pharmaceutical composition | |
| CN103432075A (en) | Desloratadine nanoemulsion and preparation method thereof | |
| CN102048742A (en) | Nano-scale liquid composite vitamin preparation | |
| CN103301038A (en) | Tea tree oil nanoemulsion and preparation method thereof | |
| CN102274178A (en) | Acetyl-isovaleryl tylosin nanoemulsion medicine and preparation method thereof | |
| CN103768103A (en) | Propolis nano emulsion oral solution and preparation method thereof | |
| CN104352510B (en) | A kind of perillaldehyde, citral, nystatin nanoemulsion and preparation method thereof | |
| CN102166257A (en) | Oil-in-water type cinnamon oil nano emulsion oral liquid | |
| CN102166253A (en) | Oil-in-water type elsholtzia oil nano emulsion preparation and method for preparing same | |
| CN104415083A (en) | Rhododendron dauricum oil-blumea oil nanoemulsion and preparation method thereof | |
| CN102397405A (en) | Compound bergamot oil nano-emulsion composition and preparation method thereof | |
| CN1899621A (en) | Nano emulsus micro emulsion composition and method for producing its products | |
| CN102872476A (en) | Compounded freshener, preparation method thereof and disposable sanitary product | |
| CN102302448A (en) | Oil-in-water furazolidone nano emulsion antibacterial medicament and preparation method thereof | |
| CN108813616A (en) | A method of preparing lutein water-soluble microemulsion | |
| WO2020253709A1 (en) | Method for preparing transparent water dispersion of fat-soluble nutritional medicine | |
| CN102379829B (en) | Coenzyme Q10 clear preparation being added into skin caring articles and preparation method thereof | |
| CN103301204B (en) | Compound fructus forsythiae-radix bupleuri oil nanoemulsion and preparation method | |
| CN100490775C (en) | Vitamin E cream and its formulation method | |
| US11439634B2 (en) | Medical skin external preparation | |
| CN105343002B (en) | A kind of Etoricoxib oral microemulsion preparation and preparation method thereof |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination |