CN101007005A - Preparation of sublingual administered nalmefene hydrochloride - Google Patents
Preparation of sublingual administered nalmefene hydrochloride Download PDFInfo
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- CN101007005A CN101007005A CN 200610065016 CN200610065016A CN101007005A CN 101007005 A CN101007005 A CN 101007005A CN 200610065016 CN200610065016 CN 200610065016 CN 200610065016 A CN200610065016 A CN 200610065016A CN 101007005 A CN101007005 A CN 101007005A
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- preparation
- sublingual
- nalmefene
- nalmefene hydrochloride
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Abstract
The invention disclosed a kind of hydrochloric acid nalmefene sublingually consumed preparation which includes active ingredients and medical accessories at a ratio of 1:1-10000 (by weight), the active ingredients include hydrochloric acid nalmefene, nalmefene liberated alkali or other medically acceptable nalmefene salts. The active ingredients in the invention can enter the vivo circulation through the capillary under patients' mucous membrane of mouth so as to fasten the effects and increase the bioavailability. The invention can be used in any occasions, so it's convenient to use with low taking dosage and less side effects.
Description
Technical field
The invention belongs to field of medicaments, particularly relate to a kind of preparation of sublingual administered nalmefene hydrochloride.
Background technology
Nalmefene hydrochloride be a kind of after naloxone hydrochloride and Naltrexone Hydrochloride synthetic novel opiate receptor antagonist, it is the derivant of water solublity hydrochloric acid naltrexone, have and opiate receptor μ, κ, δ all can in conjunction with, and with characteristics such as the effect of μ receptors bind is the strongest.Compare with Naltrexone Hydrochloride, its pharmacological action time is long, and action intensity is big and toxic and side effects is lower, is mainly used in treatment operation back clinically because of taking respiration inhibition and the symptoms such as heart failure, shock, alcoholism and addiction that narcosis analgesic causes.At present the nalmefene hydrochloride preparation that uses clinically is the injection through subcutaneous, muscle or intravenous injection administration.Because injection must be injected to the patient by the medical personnel through professional training, thereby the occasion of using is subjected to great restriction.
Summary of the invention
In order to address the above problem, the object of the present invention is to provide a kind of taking convenience, absorption and preparation of sublingual administered nalmefene hydrochloride rapid-action and that bioavailability is high.
In order to achieve the above object, preparation of sublingual administered nalmefene hydrochloride provided by the invention is made according to the technology of routine with 1: 1～10000 weight ratio by other pharmaceutical salts and pharmaceutic adjuvant as nalmefene hydrochloride, nalmefene free alkali or the pharmaceutically acceptable nalmefene of active component.
Described pharmaceutic adjuvant is selected from Macrogol 4000, polyethylene glycol 6000, Tween 80, stearic acid, starch, carboxymethyl starch sodium, microcrystalline Cellulose, dextrin, sucrose, lactose, Herba Menthae, citric acid, beta-schardinger dextrin-, gelatin, insect wax, glycerol, sodium carboxymethyl cellulose, polyvidone, hydroxypropyl starch, low-substituted hydroxypropyl cellulose, magnesium stearate, saccharin sodium, azone (the tall and erect ketone of dodecyl nitrogen) and laurocapram (holding together the tall and erect ketone of cattle base nitrogen).
Described sublingual administration preparation comprises drop pill, chewable tablet, buccal tablet, fast disintegrating tablet, dispersible tablet, sublingual lozenge and common oral tablet.
Effective ingredient in the preparation of sublingual administered nalmefene hydrochloride provided by the invention directly enters body-internal-circulation after can absorbing by the capillary tube under patient's oral mucosa, thereby rapid-action and bioavailability is high.Medicine particularly of the present invention is not subjected to the restriction of use occasion, thereby taking convenience, and taking dose and toxic and side effects are little.
The specific embodiment
Describe preparation of sublingual administered nalmefene hydrochloride provided by the invention in detail below in conjunction with specific embodiment.
Embodiment 1: the nalmefene hydrochloride drop pill
Prescription nalmefene hydrochloride 0.1 gram
Citric acid 3 grams
Azone 1 gram
Polyethylene glycol 6000 30 grams
Make 1000 altogether
30 gram polyethylene glycol 6000s are placed rustless steel container, heating makes its whole thawings in 90～100 ℃ of oil baths, add 0.1 gram nalmefene hydrochloride, 1 gram azone and 3 gram citric acid then, be stirred to fusing, move in the reservoir, and insulation is at 80～90 ℃, regulator solution titer valve splashes in 10～15 ℃ the liquid Paraffin, with the drop pill drop that forms to the greatest extent and clean liquid Paraffin, drying can make 1000 nalmefene hydrochloride drop pill provided by the invention.
Embodiment 2: the nalmefene hydrochloride drop pill
Prescription nalmefene hydrochloride 2 grams
Citric acid 10 grams
Laurocapram 2 grams
Macrogol 4000 20 grams
Polyethylene glycol 6000 20 grams
Make 1000 altogether
20 gram Macrogol 4000s and 20 gram polyethylene glycol 6000s are placed rustless steel container, oil bath heating in 90～100 ℃ makes its whole thawings, add 2 gram nalmefene hydrochlorides, 2 gram laurocapram and 10 gram citric acid then, be stirred to fusing, move in the reservoir, and insulation is at 85 ± 2 ℃, regulator solution titer valve splashes in 10～15 ℃ the liquid Paraffin, with the drop pill drop that forms to the greatest extent and clean liquid Paraffin, drying can make 1000 nalmefene hydrochloride drop pill provided by the invention.
Embodiment 3: the nalmefene hydrochloride sublingual lozenge:
Prescription: nalmefene hydrochloride 0.1 gram
Citric acid 3 grams
Azone 1 gram
Sucrose 80 grams
Carboxymethyl starch sodium 10 grams
10% starch slurry, 100 grams
Magnesium stearate 5 grams
Make 1000 altogether
Citric acid, sucrose are pulverized 100 mesh sieves, carboxymethyl starch sodium crossed three's mix homogeneously behind 100 mesh sieves, nalmefene hydrochloride is dissolved in the 10ml water, add 1 gram azone, join in 10% starch slurry mix homogeneously then and make soft material, cross 14 orders and granulate, under 70～80 ℃, carry out drying as binding agent, cross 16 order granulate, add the magnesium stearate mix homogeneously, tabletting can make 1000 nalmefene hydrochloride sublingual lozenges provided by the invention.
Embodiment 4: the nalmefene hydrochloride sublingual lozenge:
Prescription: nalmefene hydrochloride 5 grams
Citric acid 3 grams
Laurocapram 5 grams
Sucrose 180 grams
Carboxymethyl starch sodium 30 grams
10% starch slurry, 300 grams
Herba Menthae 3 grams
Saccharin sodium 10 grams
Magnesium stearate 15 grams
Make 1000 altogether
Citric acid, sucrose are pulverized 100 mesh sieves, carboxymethyl starch sodium crossed three's mix homogeneously behind 100 mesh sieves, nalmefene hydrochloride is dissolved in the 10ml water, add 5 gram laurocapram, join in 10% starch slurry then and add saccharin sodium and the Herba Menthae mix homogeneously after make soft material as binding agent, cross 14 orders and granulate, carry out drying in 70～80 ℃, cross 16 order granulate, add the magnesium stearate mix homogeneously, tabletting can make 1000 nalmefene hydrochloride sublingual lozenges provided by the invention.
Preparation of sublingual administered nalmefene hydrochloride provided by the invention is white in color or the off-white color sheet, and wherein drop pill weighs 30～50mg, and sublingual lozenge weighs 0.1～0.3g.
In order to verify the assimilation effect of preparation of sublingual administered nalmefene hydrochloride provided by the invention, the inventor has carried out medicine human body Sublingual absorption test; By 10 healthy male trial volunteers being carried out buccal absorption test, the experimenter is divided into 2 groups (the first winding is tested by drop pill, and the second winding is tested by tablet), experimenter's fasting after 10 hours in administration in morning next day.Test method is put into the oral cavity for the buffer 20～25ml with known drug concentration, do the motion of 60 times/min tongue, solution spues behind 5min, buffer with equivalent washes the oral cavity then, to spue solution and flushing liquor is merged into collection liquid, measure content, relatively stock solution Chinese medicine concentration and collection liquid Chinese medicine concentration is poor, is drug absorption.Preparation of sublingual administered nalmefene hydrochloride in people's buccal absorption test statistics result is: average absorption rate＞90%, do not find any untoward reaction simultaneously.
Claims (3)
1, a kind of preparation of sublingual administered nalmefene hydrochloride is characterized in that: described preparation of sublingual administered nalmefene hydrochloride is made according to the technology of routine with 1: 1～10000 weight ratio by other pharmaceutical salts and pharmaceutic adjuvant as nalmefene hydrochloride, nalmefene free alkali or the pharmaceutically acceptable nalmefene of active component.
2, preparation of sublingual administered nalmefene hydrochloride according to claim 1 is characterized in that: described pharmaceutic adjuvant is selected from Macrogol 4000, polyethylene glycol 6000, Tween 80, stearic acid, starch, carboxymethyl starch sodium, microcrystalline Cellulose, dextrin, sucrose, lactose, Herba Menthae, citric acid, beta-schardinger dextrin-, gelatin, insect wax, glycerol, sodium carboxymethyl cellulose, polyvidone, hydroxypropyl starch, low-substituted hydroxypropyl cellulose, magnesium stearate, saccharin sodium, azone (the tall and erect ketone of dodecyl nitrogen) and laurocapram (holding together the tall and erect ketone of cattle base nitrogen).
3, preparation of sublingual administered nalmefene hydrochloride according to claim 1 is characterized in that: described sublingual administration preparation comprises drop pill, chewable tablet, buccal tablet, fast disintegrating tablet, dispersible tablet, sublingual lozenge and common oral tablet.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200610065016 CN101007005A (en) | 2006-01-24 | 2006-03-17 | Preparation of sublingual administered nalmefene hydrochloride |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN200610013104 | 2006-01-24 | ||
| CN200610013104.1 | 2006-01-24 | ||
| CN 200610065016 CN101007005A (en) | 2006-01-24 | 2006-03-17 | Preparation of sublingual administered nalmefene hydrochloride |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN101007005A true CN101007005A (en) | 2007-08-01 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 200610065016 Pending CN101007005A (en) | 2006-01-24 | 2006-03-17 | Preparation of sublingual administered nalmefene hydrochloride |
Country Status (1)
| Country | Link |
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| CN (1) | CN101007005A (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2016146981A1 (en) * | 2015-03-17 | 2016-09-22 | King's College London | Novel formulations |
-
2006
- 2006-03-17 CN CN 200610065016 patent/CN101007005A/en active Pending
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2016146981A1 (en) * | 2015-03-17 | 2016-09-22 | King's College London | Novel formulations |
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| C06 | Publication | ||
| PB01 | Publication | ||
| C02 | Deemed withdrawal of patent application after publication (patent law 2001) | ||
| WD01 | Invention patent application deemed withdrawn after publication |