CN1813739A - Nalmefene hydro chloride lyophilized powder formulation for injection - Google Patents
Nalmefene hydro chloride lyophilized powder formulation for injection Download PDFInfo
- Publication number
- CN1813739A CN1813739A CN 200510022145 CN200510022145A CN1813739A CN 1813739 A CN1813739 A CN 1813739A CN 200510022145 CN200510022145 CN 200510022145 CN 200510022145 A CN200510022145 A CN 200510022145A CN 1813739 A CN1813739 A CN 1813739A
- Authority
- CN
- China
- Prior art keywords
- preparation
- nalmefene
- mannitol
- injection
- nalmefene hydrochloride
- 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
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The present invention relates to a nalmefene hydrochloride freeze-dried powder injection preparation for injection. Said preparation is formed from effective component malmefene hydrochloride and proper medicinal carrier, in which the content range of nalmefene hydrochloride in the preparation is 0.1-4.5 mg generally, the medicinal carrier can be one or several kinds selected from mannitol, glucose, sodium chloride, beta-cyclodextrin, glucosan, fructose and sorbitol. The content range of said medicinal carrier can be 10-100 mg. the pH value of said preparation is 5.0-7.0.
Description
Technical field:
The present invention relates to the Nalmefene hydro chloride lyophilized powder formulation of a kind of pharmaceutical preparation, particularly injection, said preparation contains the nalmefene hydrochloride for the treatment of effective dose and an amount of pharmaceutical carrier.
Background technology:
(chemistry 17-by name encircles third methyl-4 to nalmefene hydrochloride, 5-epoxy-6-methylene morphinan-3, the 14-diol hydrochloride), it is the long-acting opioid antagonist that a kind of injectable is used, this product has advantages such as action intensity is big, longer duration, bioavailability height, few side effects, is usually used in reversing the effect of opioid drug abroad and rescues the excessive patient of opiates.Nalmefene hydrochloride nineteen ninety-five has been obtained the effect that drugs approved by FDA is used to reverse opioid drug, comprises respiration inhibition, lethargy and hypotension.Also can be used for the excessive treatment of known or suspicious opiates at emergency room.Existing animal experiment and clinical trial proof this product are treated the effect of alcohol dependence in addition.
At present domestic also do not have the nalmefene hydrochloride injection to go on the market, and the nalmefene hydrochloride injection that abroad gone on the market is little liquid drugs injection, and its less stable is unfavorable for long term storage.For improving product stability, guarantee product quality, we have developed Nalmefene hydro chloride lyophilized powder formulation for injection, and specification is defined as 0.1108mg, 0.2216mg, 2.216mg, 4.432mg, are respectively by nalmefene: 0.1mg, 0.2mg, 2mg, 4mg.
Summary of the invention:
The object of the invention provides a kind of steady quality, be convenient to transportation and store and can rapid dissolved Nalmefene hydro chloride lyophilized powder formulation, except that containing nalmefene hydrochloride as the effective ingredient, also contains an amount of pharmaceutical carrier in the said preparation.
Nalmefene hydro chloride lyophilized powder formulation of the present invention is made up of nalmefene hydrochloride for the treatment of effective dose and an amount of pharmaceutical carrier basically.
Because lyophilized injectable powder normally is divided in the cillin bottle, with the unit dosage form administration, so Nalmefene hydro chloride lyophilized powder formulation of the present invention, per unit dosage, be that to contain nalmefene hydrochloride in every injection can be 0.1-4.5mg, pharmaceutical carrier for example mannitol or glucose can be 5-100mg.
Nalmefene hydro chloride lyophilized powder formulation of the present invention, the pharmaceutical carrier that is contained is not particularly limited, so long as the carrier that can be used in the injection preparation is just passable.For example can be selected from mannitol, glucose, sodium chloride, beta-schardinger dextrin-, dextran, fructose, the sorbitol etc. one or more, be preferably mannitol and/or glucose; Most preferably be mannitol.The content of pharmaceutical carrier also is not particularly limited, and can at random use pharmaceutical carrier in the scope of harmless effect of the present invention.Nalmefene hydro chloride lyophilized powder formulation of the present invention preferably, contains pharmaceutical carrier for example mannitol or glucose 10-80mg in the preparation of per unit dosage; More preferably, contain pharmaceutical carrier for example mannitol or glucose 20-60mg in the preparation of the present invention; Most preferably, contain for example mannitol 20-40mg of pharmaceutical carrier in the preparation of the present invention;
Nalmefene hydro chloride lyophilized powder formulation of the present invention preferably, contains the 0.1108-4.432mg nalmefene hydrochloride in the preparation of per unit dosage; Most preferably, contain 0.1108mg, 0.2216mg, 2.216mg, 4.432mg nalmefene hydrochloride in the preparation of the present invention.
Nalmefene hydro chloride lyophilized powder formulation of the present invention also contains small amount of moisture sometimes, but small amount of moisture does not influence the performance and the beneficial effect of product of the present invention, moisture is in the scope of the freeze-dried powder permission of routine, and for example moisture is 0～6%.
Nalmefene hydro chloride lyophilized powder formulation of the present invention, pH value are 5.0-7.0.
Nalmefene hydro chloride lyophilized powder formulation of the present invention, its preparation method are that nalmefene hydrochloride is added certain density pharmaceutical carrier for example in the aqueous solution of mannitol or glucose, and stirring and dissolving is filtered the back fill, and lyophilization makes preparation of the present invention.
Its clinical administration method of Nalmefene hydro chloride lyophilized powder formulation of the present invention is: face with before adding sterilized water for injection dissolving back intramuscular or subcutaneous injection or adding 5% glucose, 0.9% sodium chloride injection dissolving posterior vein injection or intravenous drip.
Nalmefene hydro chloride lyophilized powder formulation of the present invention, employed crude drug are nalmefene hydrochloride, and its dissolubility in water is good, so preparation is simple for this product.
Nalmefene hydro chloride lyophilized powder formulation of the present invention does not add pH regulator agent such as hydrochloric acid, the products obtained therefrom pH value is 5.0-7.0, approach neutrality, blood vessel, skin, mucosa and muscle to the patient when carrying out intramuscular injection or intravenous injection in clinical use almost do not stimulate, and have improved patient's toleration greatly.In addition, in Nalmefene hydro chloride lyophilized powder formulation preparation process of the present invention, do not add pH regulator agent such as hydrochloric acid not only reduced in preparation, introduce other impurity may, and simplified technology, reduced production cost.
Nalmefene hydro chloride lyophilized powder formulation reasonable recipe of the present invention, technology is simple, and product is loose porous, and solubility is good, good stability.Factors influencing under high temperature, high humidity, high light condition 10 days and 40 ℃ of accelerated tests 6 months, sample appearance character, pH, active constituent content and related substance etc. have no significant change.
Nalmefene hydrochloride is a known compound, can oneself prepare or commercially available obtaining.
The specific embodiment:
Further specify the present invention by the following examples, but these embodiment do not limit the present invention in any way.
Embodiment 1
Prescription:
Nalmefene hydrochloride 0.1108g
Mannitol 20g
Technology: 1. get 1000ml water for injection and put in the dosing cylinder, add the mannitol of prescription full dose, be stirred to dissolving; 2. add the nalmefene hydrochloride of recipe quantity, be stirred to dissolving; The microporous filter membrane fine straining of reuse 0.22 μ m is to clear and bright; 3. embedding (fill 1ml liquid in the cillin bottle of 2ml volume) in cillin bottle; 4. lyophilization (pre-freeze, make temperature drop to-40 ℃, the heating rate with 0.15 ℃ of per minute after two hours rises to temperature-5 ℃, and sublimation drying is 10 hours under this temperature, heating rate with 0.4 ℃ of per minute rises to 40 ℃ with temperature again, and drying is 7～10 hours under this temperature); 5. gland is labelled, and packing gets product after the assay was approved.
PH value: get 10 of this product, every adds water 1ml dissolving back merging, measures (two appendix VI of Chinese Pharmacopoeia version in 2000 H) in accordance with the law, and pH value is 6.06.
Embodiment 2
Prescription:
Nalmefene hydrochloride 0.1108g
Mannitol 20g
Technology: 1. get 1000ml water for injection and put in the dosing cylinder, add the mannitol of prescription full dose, be stirred to dissolving; 2. add the nalmefene hydrochloride of recipe quantity, be stirred to dissolving; The microporous filter membrane fine straining of reuse 0.22 μ m is to clear and bright; 3. embedding (with embodiment 1) in cillin bottle; 4. lyophilization (pre-freeze, make temperature drop to-40 ℃, the heating rate with 0.15 ℃ of per minute after two hours rises to temperature-5 ℃, and sublimation drying is 10 hours under this temperature, heating rate with 0.4 ℃ of per minute rises to 40 ℃ with temperature again, and drying is 7～10 hours under this temperature); 5. gland is labelled, and packing gets product after the assay was approved.
PH value: assay method is with embodiment 1, and pH value is 6.06.
Embodiment 3
Prescription:
Nalmefene hydrochloride 0.2216g
Mannitol 20g
Technology: 1. get 1000ml water for injection and put in the dosing cylinder, add the mannitol of prescription full dose, be stirred to dissolving; 2. add the nalmefene hydrochloride of recipe quantity, be stirred to dissolving; The microporous filter membrane fine straining of reuse 0.22 μ m is to clear and bright; 3. embedding (with embodiment 1) in cillin bottle; 4. lyophilization (pre-freeze, make temperature drop to-40 ℃, the heating rate with 0.15 ℃ of per minute after two hours rises to temperature-5 ℃, and sublimation drying is 10 hours under this temperature, heating rate with 0.4 ℃ of per minute rises to 40 ℃ with temperature again, and drying is 7～10 hours under this temperature); 5. gland is labelled, and packing gets product after the assay was approved.
PH value: assay method is with embodiment 1, and pH value is 5.85.
Embodiment 4
Prescription:
Nalmefene hydrochloride 0.2216g
Mannitol 40g
Technology: 1. get 1000ml water for injection and put in the dosing cylinder, add the mannitol of prescription full dose, be stirred to dissolving; 2. add the nalmefene hydrochloride of recipe quantity, be stirred to dissolving; The microporous filter membrane fine straining of reuse 0.22 μ m is to clear and bright; 3. embedding (with embodiment 1) in cillin bottle; 4. lyophilization (pre-freeze, make temperature drop to-40 ℃, the heating rate with 0.15 ℃ of per minute after two hours rises to temperature-5 ℃, and sublimation drying is 10 hours under this temperature, heating rate with 0.4 ℃ of per minute rises to 40 ℃ with temperature again, and drying is 7～10 hours under this temperature); 5. gland is labelled, and packing gets product after the assay was approved.
PH value: assay method is with embodiment 1, and pH value is 6.18.
Embodiment 5
Prescription:
Nalmefene hydrochloride 2.216g
Mannitol 20g
Technology: 1. get 1000ml water for injection and put in the dosing cylinder, add the mannitol of prescription full dose, be stirred to dissolving; 2. add the nalmefene hydrochloride of recipe quantity, be stirred to dissolving; The microporous filter membrane fine straining of reuse 0.22 μ m is to clear and bright; 3. embedding (with embodiment 1) in cillin bottle; 4. lyophilization (pre-freeze, make temperature drop to-40 ℃, the heating rate with 0.15 ℃ of per minute after two hours rises to temperature-5 ℃, and sublimation drying is 10 hours under this temperature, heating rate with 0.4 ℃ of per minute rises to 40 ℃ with temperature again, and drying is 7～10 hours under this temperature); 5. gland is labelled, and packing gets product after the assay was approved.
PH value: assay method is with embodiment 1, and pH value is 6.25.
Embodiment 6
Prescription:
Nalmefene hydrochloride 2.216g
Mannitol 40g
Technology: 1. get 1000ml water for injection and put in the dosing cylinder, add the mannitol of prescription full dose, be stirred to dissolving; 2. add the nalmefene hydrochloride of recipe quantity, be stirred to dissolving; The microporous filter membrane fine straining of reuse 0.22 μ m is to clear and bright; 3. embedding (with embodiment 1) in cillin bottle; 4. lyophilization (pre-freeze, make temperature drop to-40 ℃, the heating rate with 0.15 ℃ of per minute after two hours rises to temperature-5 ℃, and sublimation drying is 10 hours under this temperature, heating rate with 0.4 ℃ of per minute rises to 40 ℃ with temperature again, and drying is 7～10 hours under this temperature); 5. gland is labelled, and packing gets product after the assay was approved.
PH value: assay method is with embodiment 1, and pH value is 6.10.
Embodiment 7
Prescription:
Nalmefene hydrochloride 4.432g
Mannitol 20g
Technology: 1. get 1000ml water for injection and put in the dosing cylinder, add the mannitol of prescription full dose, be stirred to dissolving; 2. add the nalmefene hydrochloride of recipe quantity, be stirred to dissolving; The microporous filter membrane fine straining of reuse 0.22 μ m is to clear and bright; 3. embedding (with embodiment 1) in cillin bottle; 4. lyophilization (pre-freeze, make temperature drop to-40 ℃, the heating rate with 0.15 ℃ of per minute after two hours rises to temperature-5 ℃, and sublimation drying is 10 hours under this temperature, heating rate with 0.4 ℃ of per minute rises to 40 ℃ with temperature again, and drying is 7～10 hours under this temperature); 5. gland is labelled, and packing gets product after the assay was approved.
PH value: assay method is with embodiment 1, and pH value is 6.30.
Embodiment 6
Prescription:
Nalmefene hydrochloride 4.432g
Mannitol 40g
Technology: 1. get 1000ml water for injection and put in the dosing cylinder, add the mannitol of prescription full dose, be stirred to dissolving; 2. add the nalmefene hydrochloride of recipe quantity, be stirred to dissolving; The microporous filter membrane fine straining of reuse 0.22 μ m is to clear and bright; 3. embedding (with embodiment 1) in cillin bottle; 4. lyophilization (pre-freeze, make temperature drop to-40 ℃, the heating rate with 0.15 ℃ of per minute after two hours rises to temperature-5 ℃, and sublimation drying is 10 hours under this temperature, heating rate with 0.4 ℃ of per minute rises to 40 ℃ with temperature again, and drying is 7～10 hours under this temperature); 5. gland is labelled, and packing gets product after the assay was approved.
PH value: assay method is with embodiment 1, and pH value is 6.20.
Claims (9)
1, a kind of Nalmefene hydro chloride lyophilized powder formulation for injection is characterized in that containing nalmefene hydrochloride and pharmaceutical carrier.
2, according to the preparation of claim 1, wherein pharmaceutical carrier is selected from one or more in mannitol, glucose, sodium chloride, beta-schardinger dextrin-, dextran, fructose, the sorbitol.
3, according to the preparation of claim 2, wherein pharmaceutical carrier is selected from mannitol and/or glucose.
4, according to the preparation of claim 3, wherein pharmaceutical carrier is a mannitol.
5, according to the preparation of one of claim 1-4, wherein contain nalmefene hydrochloride 0.1-4.5mg in the preparation of per unit dosage, pharmaceutical carrier 5-100mg.
6, according to the preparation of claim 5, wherein contain nalmefene hydrochloride 0.1108mg in the per unit preparation, 0.2216mg, 2.216mg, 4.432mg.
7, according to the preparation of claim 5, wherein contain mannitol 20mg or 40mg in the per unit preparation.
8, one of any preparation of claim 1-7, wherein the pH value of preparation is 5.0-7.0.
9, the preparation method of one of any preparation of claim 1-8 is characterized in that this method comprises nalmefene hydrochloride is added in the aqueous solution of certain density pharmaceutical carrier, and stirring and dissolving is filtered the back fill, lyophilization.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200510022145 CN1813739A (en) | 2005-11-25 | 2005-11-25 | Nalmefene hydro chloride lyophilized powder formulation for injection |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200510022145 CN1813739A (en) | 2005-11-25 | 2005-11-25 | Nalmefene hydro chloride lyophilized powder formulation for injection |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1813739A true CN1813739A (en) | 2006-08-09 |
Family
ID=36906173
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 200510022145 Pending CN1813739A (en) | 2005-11-25 | 2005-11-25 | Nalmefene hydro chloride lyophilized powder formulation for injection |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1813739A (en) |
Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8455471B2 (en) | 2006-10-20 | 2013-06-04 | Icos Corporation | Compositions of CHK1 inhibitors and cyclodextrin |
| CN103202806A (en) * | 2013-04-10 | 2013-07-17 | 安徽恒星制药有限公司 | Method for preparing nalmefene hydrochloride injection and prepared nalmefene hydrochloride injection |
| US10653690B1 (en) | 2019-07-09 | 2020-05-19 | Orexo Ab | Pharmaceutical composition for nasal delivery |
| US10729687B1 (en) | 2019-07-09 | 2020-08-04 | Orexo Ab | Pharmaceutical composition for nasal delivery |
| US11737980B2 (en) | 2020-05-18 | 2023-08-29 | Orexo Ab | Pharmaceutical composition for drug delivery |
| US11957647B2 (en) | 2021-11-25 | 2024-04-16 | Orexo Ab | Pharmaceutical composition comprising adrenaline |
-
2005
- 2005-11-25 CN CN 200510022145 patent/CN1813739A/en active Pending
Cited By (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8455471B2 (en) | 2006-10-20 | 2013-06-04 | Icos Corporation | Compositions of CHK1 inhibitors and cyclodextrin |
| CN103202806A (en) * | 2013-04-10 | 2013-07-17 | 安徽恒星制药有限公司 | Method for preparing nalmefene hydrochloride injection and prepared nalmefene hydrochloride injection |
| US10653690B1 (en) | 2019-07-09 | 2020-05-19 | Orexo Ab | Pharmaceutical composition for nasal delivery |
| US10729687B1 (en) | 2019-07-09 | 2020-08-04 | Orexo Ab | Pharmaceutical composition for nasal delivery |
| US10898480B1 (en) | 2019-07-09 | 2021-01-26 | Orexo Ab | Pharmaceutical composition for nasal delivery |
| US11883392B2 (en) | 2019-07-09 | 2024-01-30 | Orexo Ab | Pharmaceutical composition for nasal delivery |
| US11737980B2 (en) | 2020-05-18 | 2023-08-29 | Orexo Ab | Pharmaceutical composition for drug delivery |
| US11957647B2 (en) | 2021-11-25 | 2024-04-16 | Orexo Ab | Pharmaceutical composition comprising adrenaline |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CN1813739A (en) | Nalmefene hydro chloride lyophilized powder formulation for injection | |
| CN1686116A (en) | Levo ornidazole vein administration agent and its preparation method | |
| CN1203855C (en) | Pharmaceutical solutions for levosimendan | |
| CN1568999A (en) | Stable freeze dried formulation of spheroidine for medical use | |
| CN1650883A (en) | Jixitabing hydrochloride solution type injection agent | |
| CN1706386A (en) | Enrofloxacin suspension and its prepn process | |
| CN1739505A (en) | L-ornidazole injection prepn | |
| CN1897940A (en) | Pharmaceutical composition of vinflunine which is intended for parenteral administration preparation method thereof and use of same | |
| CN1830440A (en) | Metronidazule injection and its preparation method and use | |
| CN1615867A (en) | Naloxone hydrchloride freeze-dried powder preparation for injection | |
| CN1931874A (en) | Prepn process, medicine prepn and medicinal use of ginseng glycopeptide | |
| CN1572296A (en) | Freeze dried vinpocetine powder injection and its preparation process | |
| CN1429558A (en) | Mannosan peptide injection and its preparation and use method | |
| CN1857729A (en) | Medicine composition containing neohouttuynin sodium and solutol HS15 | |
| CN1543976A (en) | Astragaloside injection preparation and its preparing process | |
| CN1626081A (en) | Ropivacaine freeze-dried powder and injection preparation in use for injection and preparation method | |
| CN1186094C (en) | Piracetam medicine composition with function of promoting thinking and memory and its prepn | |
| CN1843334A (en) | Method for promoting liposome encapsulation and its formulation | |
| CN1175811C (en) | Slow-releasing Anixitan tablet | |
| CN1053185A (en) | injectable solution and preparation method thereof | |
| CN1839842A (en) | Pharmaceutical composition containing levosimendan or its pharmaceutically acceptable salt as active ingredient | |
| CN1830426A (en) | New houttuynine sodium bisulfite injection and its preparation method and use | |
| CN1208059C (en) | Medication comprising lornoxicam and niacinamide | |
| CN1565446A (en) | Freeze-drying fluconazole injection and its preparation method | |
| CN1555788A (en) | Thio pronine transfursion liquid and its preparation method |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C02 | Deemed withdrawal of patent application after publication (patent law 2001) | ||
| WD01 | Invention patent application deemed withdrawn after publication |