CN1575795A - Naloxone hydrochloride nasal spray - Google Patents
Naloxone hydrochloride nasal spray Download PDFInfo
- Publication number
- CN1575795A CN1575795A CN 200410049659 CN200410049659A CN1575795A CN 1575795 A CN1575795 A CN 1575795A CN 200410049659 CN200410049659 CN 200410049659 CN 200410049659 A CN200410049659 A CN 200410049659A CN 1575795 A CN1575795 A CN 1575795A
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- nasal mist
- naloxone hydrochloride
- nasal
- mist
- water
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Abstract
The present invention is nasal cavity spray of Naloxine hydrochloride and its preparation process. The preparation of the present invention may be applied in single dosage form or multiple dosage form. The spray of the present invention includes Naloxine hydrochloride, osmotic pressure regulator, preservative, osmotic promoter and water.
Description
Invention field
The present invention relates to naloxone hydrochloride nasal mist and preparation method thereof.The invention still further relates to the nasal mist of naloxone hydrochloride single dose and multiple dose.Nasal mist of the present invention comprises naloxone hydrochloride, osmotic pressure regulator, antiseptic, penetration enhancer and water.
Background technology
Naloxone hydrochloride (Naloxone Hydrochloride) is a morphine antagonist, can be used for the treatment of drug intoxication first aid of morphine class and acute alcoholism etc.This medicine clinical practice has injection and sublingual lozenge, uses but injection will arrive hospital or clinic usually, and all there is the problem of using inconvenience and compliance difference in both; Thereby reducing drug effect and absorption and bioavailability can be affected.
Summary of the invention
The objective of the invention is to overcome the deficiency of present naloxone hydrochloride injection and two kinds of preparations existence of sublingual lozenge, exploitation absorbs fast, and the bioavailability height is easy to use, do not need specified conditions, can use by oneself, a kind of new naloxone hydrochloride single dose and the multiple dose nasal mist of usefulness mutually.
The inventor passes through further investigation, has now found that naloxone hydrochloride, and with the antiseptic of selecting for use, Osmolyte regulator, penetration enhancer and a kind of new nasal spray form of administration of water mixing formation.Said preparation has absorption rapidly, bioavailability high and bland single dose and multiple dose nasal mist.Said preparation is fit to large-scale production and storage.
Therefore, first aspect present invention relates to the spray agent of the via intranasal application administration that contains naloxone, and it comprises naloxone hydrochloride, Osmolyte regulator, antiseptic, penetration enhancer and water.
Further aspect of the present invention relates to the nasal mist that contains the hydrochloric acid naloxone and is alleviating or the purposes of treatment morphine class drug intoxication first aid and acute alcoholism etc.
According to the present invention, the antiseptic that uses in the nasal spray of the present invention is selected from methyl parahydroxybenzoate, ethyl ester, propyl ester, butyl ester, three pears acid, benzoic acid, sodium benzoate, benzyl alcohol, Benzalkonii Chloridum, benzalkonium bromide, chlorobutanol, resorcinol and sodium ethylene diamine tetracetate etc., osmotic pressure regulator is selected from sodium chloride, potassium nitrate, boric acid and glucose.1. penetration enhancer is selected from alcohols, esters, dimethyl sulfoxine and homologue in the organic solvent; 2. fatty acid, aliphatic alcohol and cholic acid salt; 3. month silicon nitrogen ketone and homologue; 4. surfactant such as cationic, anionic, nonionic and lecithin; 5. terpenes; 6. cutin is preserved moisture and softening agent.
The present invention also provides the preparation method of the nasal mist of two kinds of hydrochloric naloxones, it comprises naloxone hydrochloride, antiseptic, osmotic pressure regulator, penetration enhancer mixed with water for injection makes dissolving, regulate pH value to 3.0～4.5, filter, then, the difference fill is in single dose and multiple dose nose sprayer unit.
The present invention is in spray medicinal liquid weight, and the content of naloxone hydrochloride is 0.1～10.0 weight %, and Osmolyte regulator, antiseptic and water content are 94.0～99.9 weight %, and granularity of spray is 5～200 μ m.
Nasal mist of the present invention is with single dose or multiple dose type of service, and each nasal spray dosage is 20～200 μ l.
The following example is used to further specify the present invention, but does not mean that the present invention is had any restriction.
The preparation of the nasal mist of embodiment 1 naloxone hydrochloride.
Take by weighing ethylparaben 0.03g, put in the 100ml measuring bottle, it is an amount of to add the injection water, the tepidarium heating makes dissolving, is cooled to room temperature, adds naloxone hydrochloride dry product 1.0g again, sodium chloride 0.9g, jolting makes dissolving, adds the nearly scale of injection water, shake up, be adjusted to pH value 3.8 ± 0.8 with 0.1mol/L hydrochloric acid, add the injection water again, shake up to scale, clear and bright with 0.25 μ m filtering with microporous membrane to medicinal liquid, promptly get naloxone hydrochloride nasal mist medicinal liquid.Fill packages spare in single dose and multiple dose nose sprayer unit respectively subsequently.
The preparation of the nasal mist of embodiment 2 naloxone hydrochlorides.
Take by weighing ethylparaben 0.03g, put in the 100ml measuring bottle, add propylene glycol 20g, it is an amount of to add the injection water again, and the tepidarium heating makes dissolving, is cooled to room temperature, add naloxone hydrochloride dry product 1.0g again, sodium chloride 0.9g, jolting makes dissolving, add the nearly scale of injection water, shake up, be adjusted to pH value 3.8 ± 0.8 with 0.1mol/L hydrochloric acid, add the injection water again to scale, shake up, clear and bright with 0.25 μ m filtering with microporous membrane to medicinal liquid, promptly get naloxone hydrochloride nasal mist medicinal liquid.Fill packages spare in single dose and multiple dose nose sprayer unit respectively subsequently.
Claims (12)
1. the nasal mist of naloxone hydrochloride comprises naloxone hydrochloride, osmotic pressure regulator, penetration enhancer, antiseptic and water.
2. the nasal mist of claim 1, wherein osmotic pressure regulator is selected from sodium chloride, potassium nitrate, boric acid and glucose.
3. claim 1 or 2 nasal mist, wherein antiseptic is selected from methyl parahydroxybenzoate, ethyl ester, propyl ester, butyl ester, sorbic acid, sodium sorbate, benzoic acid, sodium benzoate, benzyl alcohol, Benzalkonii Chloridum, benzalkonium bromide, chlorobutanol, resorcinol and sodium ethylene diamine tetracetate.
4. 1. the nasal mist that requires of claim 1～3, its penetration enhancer comprise alcohols, esters, dimethyl sulfoxine and homologue in the organic solvent; 2. fatty acid, aliphatic alcohol and cholic acid salt; 3. month silicon nitrogen ketone and homologue; 4. surfactant such as cationic, anionic, nonionic and lecithin; 5. terpenes; 6. cutin is preserved moisture and softening agent.
5. the nasal mist of the arbitrary requirement of claim 1～4, wherein said antiseptic is an ethylparaben.
6. the nasal mist that requires of claim 5, its osmotic pressure regulator is a sodium chloride.
7. the nasal mist of claim 6, its penetration enhancer is a propylene glycol.
8. the nasal mist that requires of claim 7, wherein said water be water for injection or can with the blended alcohols of water such as propylene glycol, glycerol, ethanol and esters.
9. the nasal mist of the arbitrary requirement of claim 1～4, wherein naloxone hydrochloride single-dose dosage is 0.1～10mg.
10. the nasal mist of the arbitrary requirement of claim 1～4, wherein granularity of spray is 5～200 μ m.
11. the nasal mist of the arbitrary requirement of claim 1～4, wherein said spray are the spray of single dose or multiple dose form.
12. the nasal mist of the arbitrary requirement of claim 1～4, wherein the pH of nasal mist is 3.0-4.5.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200410049659 CN1575795A (en) | 2003-06-25 | 2004-06-23 | Naloxone hydrochloride nasal spray |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN03147840.9 | 2003-06-25 | ||
| CN03147840 | 2003-06-25 | ||
| CN 200410049659 CN1575795A (en) | 2003-06-25 | 2004-06-23 | Naloxone hydrochloride nasal spray |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1575795A true CN1575795A (en) | 2005-02-09 |
Family
ID=34593080
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 200410049659 Pending CN1575795A (en) | 2003-06-25 | 2004-06-23 | Naloxone hydrochloride nasal spray |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1575795A (en) |
Cited By (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2012156317A2 (en) | 2011-05-13 | 2012-11-22 | Euro-Celtique S.A. | Intranasal pharmaceutical dosage forms comprising naloxone |
| CN1726915B (en) * | 2004-07-27 | 2013-04-24 | 中国人民解放军军事医学科学院毒物药物研究所 | Nasal cavity drug delivery system and combination of naloxone hydrochloride and preparation method |
| CN104606136A (en) * | 2015-01-06 | 2015-05-13 | 中国人民解放军军事医学科学院毒物药物研究所 | Metoclopramide nasal spray, as well as preparation method and application thereof |
| WO2015095644A1 (en) * | 2013-12-20 | 2015-06-25 | AntiOP, Inc. | Intranasal naloxone compositions and methods of making and using same |
| US9211253B2 (en) | 2014-03-14 | 2015-12-15 | Lightlake Therapeutics Inc. | Nasal drug products and methods of their use |
| US9468747B2 (en) | 2014-03-14 | 2016-10-18 | Opiant Pharmaceuticals, Inc. | Nasal drug products and methods of their use |
| US9561177B2 (en) | 2014-03-14 | 2017-02-07 | Adapt Pharma Limited | Nasal drug products and methods of their use |
| EP3177146A4 (en) * | 2014-07-08 | 2018-01-03 | Insys Pharma, Inc. | Sublingual naloxone spray |
| WO2018034920A1 (en) | 2016-08-17 | 2018-02-22 | Insys Development Company, Inc. | Liquid naloxone spray |
| US10085937B2 (en) | 2014-03-14 | 2018-10-02 | Adapt Pharma Limited | Nasal drug products and methods of their use |
| EP3349756A4 (en) * | 2015-09-17 | 2019-05-15 | Adapt Pharma Limited | Nasal drug products and methods of their use |
| WO2020033402A1 (en) * | 2018-08-06 | 2020-02-13 | Summit Biosciences Inc. | Drug products for nasal administration and uses thereof |
| US11975096B2 (en) | 2014-07-08 | 2024-05-07 | Hikma Pharmaceuticals Usa Inc. | Liquid naloxone spray |
-
2004
- 2004-06-23 CN CN 200410049659 patent/CN1575795A/en active Pending
Cited By (39)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1726915B (en) * | 2004-07-27 | 2013-04-24 | 中国人民解放军军事医学科学院毒物药物研究所 | Nasal cavity drug delivery system and combination of naloxone hydrochloride and preparation method |
| US11020343B2 (en) | 2011-05-13 | 2021-06-01 | Harm Reduction Therapeutics, Inc. | Intranasal pharmaceutical dosage forms comprising naloxone |
| EP3320893A1 (en) * | 2011-05-13 | 2018-05-16 | Euro-Celtique S.A. | Intranasal pharmaceutical dosage forms comprising naloxone |
| CN103764119A (en) * | 2011-05-13 | 2014-04-30 | 欧洲凯尔特公司 | Intranasal pharmaceutical dosage forms comprising naloxone |
| US11806428B2 (en) | 2011-05-13 | 2023-11-07 | Harm Reduction Therapeutics, Inc. | Intranasal pharmaceutical dosage forms comprising naloxone |
| WO2012156317A2 (en) | 2011-05-13 | 2012-11-22 | Euro-Celtique S.A. | Intranasal pharmaceutical dosage forms comprising naloxone |
| CN107260672A (en) * | 2011-05-13 | 2017-10-20 | 欧洲凯尔特公司 | Intranasal pharmaceutical formulation comprising naloxone |
| WO2012156317A3 (en) * | 2011-05-13 | 2013-05-10 | Euro-Celtique S.A. | Intranasal pharmaceutical dosage forms comprising naloxone |
| EP2706982B1 (en) | 2011-05-13 | 2018-01-03 | Euro-Celtique S.A. | Intranasal pharmaceutical dosage forms comprising naloxone |
| TWI486161B (en) * | 2011-05-13 | 2015-06-01 | Euro Celtique Sa | Intranasal pharmaceutical dosage forms comprising naloxone |
| AU2012257785B2 (en) * | 2011-05-13 | 2016-04-14 | Euro-Celtique S.A. | Intranasal pharmaceutical dosage forms comprising naloxone |
| JP2016128453A (en) * | 2011-05-13 | 2016-07-14 | ユーロ−セルティーク エス．エイ． | Intranasal pharmaceutical dosage forms comprising naloxone |
| EP2706982B2 (en) † | 2011-05-13 | 2021-03-10 | Euro-Celtique S.A. | Intranasal pharmaceutical dosage forms comprising naloxone |
| JP2018150336A (en) * | 2011-05-13 | 2018-09-27 | ユーロ−セルティーク エス．エイ． | Intranasal pharmaceutical dosage forms comprising naloxone |
| US9289425B2 (en) | 2013-12-20 | 2016-03-22 | AntiOP, Inc. | Intranasal naloxone compositions and methods of making and using same |
| US9192570B2 (en) | 2013-12-20 | 2015-11-24 | AntiOP, Inc. | Intranasal naloxone compositions and methods of making and using same |
| WO2015095644A1 (en) * | 2013-12-20 | 2015-06-25 | AntiOP, Inc. | Intranasal naloxone compositions and methods of making and using same |
| US9775838B2 (en) | 2014-03-14 | 2017-10-03 | Adapt Pharma Limited | Nasal drug products and methods of their use |
| CN110755372A (en) * | 2014-03-14 | 2020-02-07 | 欧皮安特制药有限公司 | Pharmaceutical product suitable for nasal delivery, pharmaceutical composition for intranasal administration and use thereof |
| US9629965B2 (en) | 2014-03-14 | 2017-04-25 | Opiant Pharmaceuticals, Inc. | Nasal drug products and methods of their use |
| US9561177B2 (en) | 2014-03-14 | 2017-02-07 | Adapt Pharma Limited | Nasal drug products and methods of their use |
| US9211253B2 (en) | 2014-03-14 | 2015-12-15 | Lightlake Therapeutics Inc. | Nasal drug products and methods of their use |
| US9468747B2 (en) | 2014-03-14 | 2016-10-18 | Opiant Pharmaceuticals, Inc. | Nasal drug products and methods of their use |
| CN106163499A (en) * | 2014-03-14 | 2016-11-23 | 欧皮安特制药有限公司 | Nasal medicine product and using method thereof |
| US9480644B2 (en) | 2014-03-14 | 2016-11-01 | Opiant Pharmaceuticals, Inc. | Nasal drug products and methods of their use |
| US10085937B2 (en) | 2014-03-14 | 2018-10-02 | Adapt Pharma Limited | Nasal drug products and methods of their use |
| US9707226B2 (en) | 2014-03-14 | 2017-07-18 | Adapt Pharma Limited | Nasal drug products and methods of their use |
| EP3177146A4 (en) * | 2014-07-08 | 2018-01-03 | Insys Pharma, Inc. | Sublingual naloxone spray |
| US11975096B2 (en) | 2014-07-08 | 2024-05-07 | Hikma Pharmaceuticals Usa Inc. | Liquid naloxone spray |
| CN104606136A (en) * | 2015-01-06 | 2015-05-13 | 中国人民解放军军事医学科学院毒物药物研究所 | Metoclopramide nasal spray, as well as preparation method and application thereof |
| EP3349756A4 (en) * | 2015-09-17 | 2019-05-15 | Adapt Pharma Limited | Nasal drug products and methods of their use |
| JP2019528278A (en) * | 2016-08-17 | 2019-10-10 | インシス・ディベロップメント・カンパニー・インコーポレイテッド | Liquid naloxone spray |
| EP3500261A4 (en) * | 2016-08-17 | 2020-05-06 | Hikma Pharmaceuticals USA Inc. | Liquid naloxone spray |
| WO2018034920A1 (en) | 2016-08-17 | 2018-02-22 | Insys Development Company, Inc. | Liquid naloxone spray |
| JP7114570B2 (en) | 2016-08-17 | 2022-08-08 | ヒクマ・ファーマシューティカルズ・ユー・エス・エイ・インコーポレイテッド | liquid naloxone spray |
| JP2022119843A (en) * | 2016-08-17 | 2022-08-17 | ヒクマ・ファーマシューティカルズ・ユー・エス・エイ・インコーポレイテッド | liquid naloxone spray |
| JP7455157B2 (en) | 2016-08-17 | 2024-03-25 | ヒクマ・ファーマシューティカルズ・ユー・エス・エイ・インコーポレイテッド | liquid naloxone spray |
| WO2020033402A1 (en) * | 2018-08-06 | 2020-02-13 | Summit Biosciences Inc. | Drug products for nasal administration and uses thereof |
| US20210186954A1 (en) * | 2018-08-06 | 2021-06-24 | Summit Biosciences Inc. | Drug products for nasal administration and uses thereof |
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