CN101036650A - Naloxone hydrochloride dropping pills - Google Patents
Naloxone hydrochloride dropping pills Download PDFInfo
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- CN101036650A CN101036650A CN 200610013315 CN200610013315A CN101036650A CN 101036650 A CN101036650 A CN 101036650A CN 200610013315 CN200610013315 CN 200610013315 CN 200610013315 A CN200610013315 A CN 200610013315A CN 101036650 A CN101036650 A CN 101036650A
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- Prior art keywords
- naloxone hydrochloride
- dropping pills
- naloxone
- hydrochloride dropping
- allylnoroxymorphone
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Abstract
A naloxone hydrochloride pill is disclosed in the invention, which is formed by naloxone hydrochloride, naloxone free alkali or the other naloxone acceptable in medicine having a ratio by weight of 1:5~10000 with pharmaceutic edjuvant based on general pill preparation process. Active ingredient of the naloxone hydrochloride pill in the invention can directly participate intracorporeal circulation after absorbed by capillary tube under oral mucosa of a patient, thus has advantages of fast absorption and high bioavailability, additionally, suffering of intramuscular injection of the patient is prevented. In particular, the drugs of the invention can be taken with no requirement of use situation, so that it is convenient for taking the medicine which dosage is controllable and has little side effect.
Description
Technical field
The invention belongs to field of medicaments, particularly relate to a kind of naloxone hydrochloride dropping pills.
Background technology
The chemical name of naloxone hydrochloride is 17-pi-allyl-4,5 α-epoxy radicals-3, and 14-dihydroxy morphinan-6 keto hydrochloride does not have hydrate, monohydrate or dihydrate.It is a kind of opiate receptor antagonist, no intrinsic activity own, but each opioid receptor of energy competitive antagonism, the μ receptor had very strong affinity, having comes into force reaches characteristics such as antagonism is strong rapidly, be mainly used in treatment clinically because of taking symptoms such as excessive respiration inhibition that causes of narcosis analgesic and stupor, thereby cause patient's fever, so that its cardiovascular function is hyperfunction.At present the naloxone hydrochloride preparation that uses clinically is injection and tablet through subcutaneous, muscle or intravenous injection administration.Though that the naloxone hydrochloride injection has is rapid-action, bioavailability is high and be easy to dose titration and advantage such as control, but owing to contain phenolic hydroxyl structure in the molecular structure of naloxone hydrochloride, thereby unstable chemcial property, so in the process that it is prepared into hydro-acupuncture preparation, might decompose because of heat sterilization causes medicine.Although powder injection formulation can avoid this medicine rotten because of the decomposition that high-temperature heating causes, and storage period is longer relatively, but its same with hydro-acupuncture preparation all need be by injecting to the patient through the medical personnel of 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 naloxone hydrochloride dropping pills rapid-action and that bioavailability is high.
In order to achieve the above object, naloxone hydrochloride dropping pills provided by the invention is by making with 1: 5～10000 the weight ratio drop pill preparation technology according to routine as other pharmaceutical salts of naloxone hydrochloride, Allylnoroxymorphone free alkali or the pharmaceutically acceptable Allylnoroxymorphone of active component and pharmaceutic adjuvant.
Described pharmaceutic adjuvant comprises substrate, liquid coolant and absorption enhancer; Its mesostroma is selected from Polyethylene Glycol, polyoxyethylene monostearate (S-40), monostearate glyceride, citric acid, sodium stearate, glycerin gelatine, carbamide, Herba Menthae, the husky nurse of pool network, stearic acid, insect wax, hydrogenated vegetable oil, octadecanol and hexadecanol; Liquid coolant is selected from liquid Paraffin, dimethicone and vegetable oil; Absorption enhancer is selected from azone (the tall and erect ketone of dodecyl nitrogen) and laurocapram (holding together the tall and erect ketone of cattle base nitrogen).
Effective ingredient in the naloxone hydrochloride dropping pills 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, and the patient does not have the misery of intramuscular injection when receiving treatment.Medicine particularly of the present invention is not subjected to the restriction of use occasion, thereby taking convenience, and taking dose is controlled and toxic and side effects is little.
The specific embodiment
Describe naloxone hydrochloride dropping pills provided by the invention in detail below in conjunction with specific embodiment.
Embodiment 1: naloxone hydrochloride dropping pills
Prescription naloxone hydrochloride 0.4 gram
Citric acid 3 grams
Azone 0.04 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 0.4 gram naloxone hydrochloride, azone 0.04 gram 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 naloxone hydrochloride dropping pills provided by the invention.
Embodiment 2: naloxone hydrochloride dropping pills
Prescription naloxone hydrochloride 2 grams
Citric acid 6 grams
Azone 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 naloxone hydrochlorides, azone 2 grams and 6 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 naloxone hydrochloride dropping pills provided by the invention.
Embodiment 3: naloxone hydrochloride dropping pills:
Prescription: naloxone hydrochloride 2 grams
Citric acid 3 grams
Herba Menthae 2 grams
Laurocapram 2 grams
Sodium stearate 100 grams
Insect wax 25 grams
Make 1000 altogether
100 gram sodium stearates, 25 gram insect waxes are added in the container successively, be dissolved in the water mix homogeneously, 100 ℃ of backflows make its whole thawings, add 2 gram naloxone hydrochlorides, 2 gram Herba Menthaes, 2 gram laurocapram and 3 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 ℃ 1% sulfuric acid solution, with the drop pill drop that forms to the greatest extent and clean liquid coolant, drying can make 1000 naloxone hydrochloride dropping pills provided by the invention.
Naloxone hydrochloride dropping pills provided by the invention is white in color or off-white color, and every ball weighs 30～50mg.
In order to verify the assimilation effect of naloxone hydrochloride dropping pills provided by the invention, the inventor has carried out medicine human body Sublingual absorption test; By 8 healthy male trial volunteers being carried out buccal absorption test, 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, then, with the buffer flushing oral cavity of equivalent, will spue solution and flushing liquor are merged into collection liquid, measure content, relatively stock solution Chinese medicine concentration and collection liquid Chinese medicine concentration is poor, is drug absorption.Naloxone hydrochloride dropping pills in people's buccal absorption test statistics result is: average absorption rate＞90%, do not find any untoward reaction simultaneously.
Claims (2)
1, a kind of naloxone hydrochloride dropping pills is characterized in that: described naloxone hydrochloride dropping pills is by making with 1: 5～10000 the weight ratio drop pill preparation technology according to routine as other pharmaceutical salts of naloxone hydrochloride, Allylnoroxymorphone free alkali or the pharmaceutically acceptable Allylnoroxymorphone of active component and pharmaceutic adjuvant.
2, naloxone hydrochloride dropping pills according to claim 1 is characterized in that: described adjuvant comprises substrate, liquid coolant and absorption enhancer; Its mesostroma is selected from Polyethylene Glycol, polyoxyethylene monostearate (S-40), monostearate glyceride, citric acid, sodium stearate, glycerin gelatine, carbamide, Herba Menthae, the husky nurse of pool network, stearic acid, insect wax, hydrogenated vegetable oil, octadecanol and hexadecanol; Liquid coolant is selected from liquid Paraffin, dimethicone and vegetable oil; Absorption enhancer is selected from azone (the tall and erect ketone of dodecyl nitrogen) and laurocapram (holding together the tall and erect ketone of cattle base nitrogen).
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200610013315 CN101036650A (en) | 2006-03-16 | 2006-03-16 | Naloxone hydrochloride dropping pills |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200610013315 CN101036650A (en) | 2006-03-16 | 2006-03-16 | Naloxone hydrochloride dropping pills |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN101036650A true CN101036650A (en) | 2007-09-19 |
Family
ID=38887956
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 200610013315 Pending CN101036650A (en) | 2006-03-16 | 2006-03-16 | Naloxone hydrochloride dropping pills |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN101036650A (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102000037A (en) * | 2009-09-03 | 2011-04-06 | 北京双鹭立生医药科技有限公司 | Sublingual naloxone hydrochloride dripping pill |
| CN103695497A (en) * | 2013-12-20 | 2014-04-02 | 奇方(天津)医药科技有限公司 | Enzymatic preparation of naloxone and pharmaceutical composition thereof |
-
2006
- 2006-03-16 CN CN 200610013315 patent/CN101036650A/en active Pending
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102000037A (en) * | 2009-09-03 | 2011-04-06 | 北京双鹭立生医药科技有限公司 | Sublingual naloxone hydrochloride dripping pill |
| CN103695497A (en) * | 2013-12-20 | 2014-04-02 | 奇方(天津)医药科技有限公司 | Enzymatic preparation of naloxone and pharmaceutical composition thereof |
| CN103695497B (en) * | 2013-12-20 | 2014-09-17 | 奇方(天津)医药科技有限公司 | Enzymatic preparation of naloxone and pharmaceutical composition thereof |
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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 |