CN102836432A - Nasal preparation for treating epilepsy - Google Patents
Nasal preparation for treating epilepsy Download PDFInfo
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- CN102836432A CN102836432A CN2011101685712A CN201110168571A CN102836432A CN 102836432 A CN102836432 A CN 102836432A CN 2011101685712 A CN2011101685712 A CN 2011101685712A CN 201110168571 A CN201110168571 A CN 201110168571A CN 102836432 A CN102836432 A CN 102836432A
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Abstract
The invention relates to a nasal preparation for treating epilepsy. The nasal preparation comprises a liquid preparation (nasal drops, nasal spray, collunarium), a nasal semisolid preparation (nasal smearing paste) and a nasal solid preparation (nasal powder). The nasal preparation comprises a main drug of an M receptor antagonist, such as the substituted hydroxyl phenylacetic acid (N-substituted bicyclic [3, 3, 1] nonane ester) and substituted hydroxyphenyl ethyl (N-substituted bicyclic [3, 3, 1] nonane ether). The nasal drug preparation is convenient to carry and use, and can be effectively treat and prevent seizure disorders.
Description
Technical field
The present invention relates to a kind of nasal formulations of treating epilepsy, comprise nasal liquid preparation (nasal drop, nasal spray, nasal douche), nose with semi-solid preparation (nasal cavity paste agent) and nose with solid preparation (nose is used powder) etc.The main medicine of nasal formulations is the m receptor antagonist, like substituted hydroxyl phenylacetic acid (the substituted dicyclo of N-[3.3.1] nonane ester) and substituted leptodactyline (the substituted dicyclo of N-[3.3.1] nonane ether).Said nasal pharmaceutical formulations carries with easy to use, can effectively treat and prevent the epilepsy disease.
Background technology
Epilepsy is to be a kind of serious neurological disorder of characteristic with the outbreak.The epileptics clinical manifestation is that of short duration sensory disturbance, limbs tic, loss of consciousness, behavior disorder or vegetative nerve function is unusual, is called epilepsy, and dissimilar epileptics clinical symptoms have nothing in common with each other.All ages and classes section epileptic symptom is not quite similar, as the children epilepsy initial stage show as usually dull mind, the point first-class; The adult patients outbreak time can show as tetany, loss of consciousness, spit out white foams etc.The outbreak of twice or repeatedly non-stimulation is defined as epilepsy, and the epilepsy invasion rate of whole world different crowd is estimated to be about 0.3% to 0.5%, estimates that per 1000 philtrums just have 5 to 10 to suffer from epilepsy.
Practical situation during in view of the epileptic patient outbreak, the common oral preparation that waits is difficult to use, and injection should not be preserved and carry.The asal agent type that can effectively treat the epileptic condition medicine is easy to use, carries easily and medication.
Nasal formulations means and directly is used for nasal cavity, the biological product of performance part or whole body therapeutic effect.Nasal formulations can be divided into nasal liquid preparation (nasal drop, nasal douche and nasal spray), nose with semi-solid preparation (nose with ointment, nose with ointment and gel for nose), nose with solid preparation (nose is used stick with powder, powder nose inhalant and nose) etc.Compare with oral administration, nasal-cavity administration can avoid medicine in gastro-intestinal Fluid, to degrade and liver first-pass effect, and bioavailability is high, and the small-molecule drug bioavailability is near quiet notes.Compare with drug administration by injection, nasal-cavity administration is easy to use, medication voluntarily, and the light or nothing to body injury, patient's compliance is good, and fibre-less toxicity and irritating pharmaceutical preparation are suitable for long term administration, and can reduce the propagation of infectious disease.Simultaneously, also be applicable to because a variety of causes and patient that can't oral administration.
Summary of the invention
The present invention relates to a kind of nasal formulations of treating epilepsy, comprise nasal liquid preparation (nasal drop, nasal spray, nasal douche), nose with semi-solid preparation (nasal cavity paste agent) and nose with solid preparation (nose is used powder) nasal drop, nasal spray etc.The main medicine of nasal formulations is the m receptor antagonist, like substituted hydroxyl phenylacetic acid (the substituted dicyclo of N-[3.3.1] nonane ester) and substituted leptodactyline (the substituted dicyclo of N-[3.3.1] nonane ether).
Said nasal pharmaceutical formulations carries with easy to use, can effectively treat and prevent the epilepsy disease.
The nasal spray of solution-type is made up of principal agent, medicinal solvent, cosolvent, fragrant correctives and antibiotic antiseptic.Its preparation process is that principal agent is mixed with various suitable pharmaceutic adjuvants, processes solution and promptly obtains medicinal liquid.
The gel-type nasal spray is made up of principal agent, medicinal solvent, cosolvent, bioadhesion macromolecular material, fragrant correctives and antibiotic antiseptic.Process half hydrophilic gel type nasal spray with polyacrylic acid etc.Can prolong drug and time of contact of nasal membrane, help improving bioavailability, its preparation process is that principal agent is mixed with various suitable pharmaceutic adjuvants, processes hydrophilic gel solution and promptly obtains drug gel liquid.
The suspension type nasal spray is made up of principal agent, medicinal solvent, suspending agent, bioadhesion macromolecular material, fragrant correctives and antibiotic antiseptic.Its preparation process is that principal agent is mixed with various suitable pharmaceutic adjuvants, processes hydrophilic outstanding miscible fluid and promptly obtains spray liquor.
The emulsion-type nasal spray is made up of principal agent, medicinal solvent, suspending agent, bioadhesion macromolecular material, fragrant correctives and antibiotic antiseptic.
Medicinal solvent is that water, Polyethylene Glycol comprise model, ethanol, propylene glycol and glycerol such as 200,300,400, can be wherein one or more.
The bioadhesion macromolecular material comprises: polyacrylic acid, polyvinylpyrrolidone, Polyethylene Glycol, cellulose and derivant; Wherein gather and comprise models such as card pool nurse 394,974,941,981, TR-2 with olefin(e) acid; Cellulose and derivant thereof comprise methylcellulose, Carboxymethyl cellulose sodium, sodium carboxymethyl cellulose, hydroxyethyl-cellulose etc., can be wherein one or more.
The pH regulator agent comprises inorganic acid alkali and organic acids and base, is used for the pH value of regulator solution, and its consumption is few, can add according to actual needs.
Cosolvent is a cyclodextrin, comprises alpha-cyclodextrin, beta-schardinger dextrin-, ethoxy-alpha-cyclodextrin, 3-hydroxypropyl-alpha-cyclodextrin etc., can be wherein one or more, and its consumption is 0.1-20g; But can not add when principal agent concentration is low in medicinal liquid.
Suspending agent comprises polyacrylic acid, polyvinylpyrrolidone, cellulose and derivant, natural gum etc.; Wherein polyacrylic acid comprises the card pool nurse of multiple model etc., and cellulose and derivant thereof comprise methylcellulose, Carboxymethyl cellulose sodium, sodium carboxymethyl cellulose, hydroxyethyl-cellulose etc.; Natural gum comprises like gelatin, arabic gum, sodium alginate etc., can be wherein one or more.
The fragrance correctives comprises sweeting agent and aromatic, and sweeting agent comprises aspartame, stevioside, glucide etc., be wherein one or more, aromatic comprises natural and synthetic perfume, can be wherein one or more.
Osmotic pressure regulator comprises sodium chloride, glucose, mannitol, sodium lactate etc., can be wherein one or more.
Antibiotic antiseptic comprises geramine, bromo geramine, phenethanol, phenyl methylcarbamate, chlorocresol, sodium benzoate, sorbic acid, sodium sorbate etc., be wherein one or more, its consumption is 0.01-10g.
Product of the present invention prepares as stated above, and its detailed component is provided by the following example, but protection scope of the present invention is not limited to this.
The specific embodiment
Specify the present invention with embodiment below, these embodiment should not be construed as going up in all senses the present invention are constituted restriction.
The nasal spray prescription of embodiment 1 solution-type
Form the 1000ml medicinal liquid.
Method for preparing: above principal agent and adjuvant add water to 1000ml, and mixing stirs, and leaves standstill, and filter promptly to get.
Embodiment 2 gel-type nasal sprays prescription
Form the 1000ml medicinal liquid.
Method for preparing: above principal agent and adjuvant add water to 1000ml, and mixing stirs, and adds Fructus Myricae rubrae essence, with adding with stirring, add small amount of acetic acid, and the pH value that is used for regulator solution is 4.0, leaves standstill, and stirs filtration and promptly gets.
Embodiment 3 suspension type nasal sprays prescription
Form the 1000ml medicinal liquid.
Method for preparing: above principal agent and adjuvant add water to 1000ml, mixing, and stirring is left standstill, and adds small amount of acetic acid, and the pH value that is used for regulator solution is 4.5, stirs filtration and promptly gets.
Claims (4)
1. the present invention relates to a kind of nasal formulations of treating epilepsy, main drug component is the m receptor antagonist.
2. said nasal formulations comprise nasal liquid preparation (nasal drop, nasal spray, nasal douche), nose with semi-solid preparation (nasal cavity paste agent) and nose with solid preparation (nose is used powder) etc.
3. the main drug component of said nasal formulations is substituted hydroxyl phenylacetic acid (N-substituted [3,3,1] nonane ester) and substituted leptodactyline (N-substituted [3,3,1] nonane ether).
4. the present invention relates to nasal formulations and can effectively treat and prevent the epilepsy disease.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2011101685712A CN102836432A (en) | 2011-06-22 | 2011-06-22 | Nasal preparation for treating epilepsy |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2011101685712A CN102836432A (en) | 2011-06-22 | 2011-06-22 | Nasal preparation for treating epilepsy |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN102836432A true CN102836432A (en) | 2012-12-26 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN2011101685712A Pending CN102836432A (en) | 2011-06-22 | 2011-06-22 | Nasal preparation for treating epilepsy |
Country Status (1)
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| CN (1) | CN102836432A (en) |
Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1500483A (en) * | 2002-11-12 | 2004-06-02 | 中国人民解放军军事医学科学院毒物药 | Novel use of phencynonate hydrochloride |
| CN1613448A (en) * | 2003-11-07 | 2005-05-11 | 中国人民解放军军事医学科学院毒物药物研究所 | Oral disintegrated and/or oral soluble solid hydrocyclo-benzenenonate |
| WO2005099697A1 (en) * | 2004-04-16 | 2005-10-27 | Institute Of Pharmacology And Toxicology Of The Academy Of Military Medical Sciences | Use of phencynonate hydrochloride for treating or alleviating epilepsy |
| EP2128137A1 (en) * | 2006-12-30 | 2009-12-02 | Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. China | Selective m4 receptor antagonist and its medical use |
| CN102040558A (en) * | 2009-10-09 | 2011-05-04 | 马宏志 | Substituted bicyclo(3,3,1)nonane ether compound and application thereof |
-
2011
- 2011-06-22 CN CN2011101685712A patent/CN102836432A/en active Pending
Patent Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1500483A (en) * | 2002-11-12 | 2004-06-02 | 中国人民解放军军事医学科学院毒物药 | Novel use of phencynonate hydrochloride |
| CN1613448A (en) * | 2003-11-07 | 2005-05-11 | 中国人民解放军军事医学科学院毒物药物研究所 | Oral disintegrated and/or oral soluble solid hydrocyclo-benzenenonate |
| WO2005099697A1 (en) * | 2004-04-16 | 2005-10-27 | Institute Of Pharmacology And Toxicology Of The Academy Of Military Medical Sciences | Use of phencynonate hydrochloride for treating or alleviating epilepsy |
| EP2128137A1 (en) * | 2006-12-30 | 2009-12-02 | Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. China | Selective m4 receptor antagonist and its medical use |
| CN102040558A (en) * | 2009-10-09 | 2011-05-04 | 马宏志 | Substituted bicyclo(3,3,1)nonane ether compound and application thereof |
Non-Patent Citations (2)
| Title |
|---|
| 王晓青: "左旋盐酸苯环壬酯鼻腔喷雾剂的研究", 《中国优秀硕士学位论文全文数据库医药卫生科技辑》, no. 10, 31 October 2009 (2009-10-31), pages 13 - 27 * |
| 高永良，等: "左旋盐酸苯环壬酯鼻腔喷雾剂的评价", 《2008年中国药学会学术年会暨第八届中国药师周论文集》, 31 December 2008 (2008-12-31), pages 2174 - 2186 * |
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| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C02 | Deemed withdrawal of patent application after publication (patent law 2001) | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20121226 |