CN104434881A - Tapentadol hydrochloride sustained release pellets and preparation method thereof - Google Patents
Tapentadol hydrochloride sustained release pellets and preparation method thereof Download PDFInfo
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- CN104434881A CN104434881A CN201410666708.0A CN201410666708A CN104434881A CN 104434881 A CN104434881 A CN 104434881A CN 201410666708 A CN201410666708 A CN 201410666708A CN 104434881 A CN104434881 A CN 104434881A
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Abstract
The invention discloses tapentadol hydrochloride sustained release pellets and a preparation method thereof. The tapentadol hydrochloride sustained release pellets comprise enteric layers, isolation layers and medicine-containing pellets and are characterized in that the isolation layers are coated with the enteric layers; the medicine-containing pellets are coated with the isolation layers; the enteric layers comprise 178mg of enteric premixing coating agents; the isolation layers comprise 16-32mg of hydroxypropyl methylcellulose, 3-20mg of sucrose, 6-22mg of talcum powder and 280-420mg of purified water; the medicine-containing pellets comprise 50mg of tapentadol hydrochloride, 50mg of hollow cores, 103-165mg of filling agents, 5-28mg of lubricating agents and 5-6mg of bonding agents. The invention relates to enteric pellets with tapentadol hydrochloride as an active ingredient. The pellets are prepared by preparing the medicine-containing pellets from the active ingredient tapentadol hydrochloride and proper amount of the hollow cores, filling agents, bonding agents, stabilizing agents and lubricating agents and then coating the medicine-containing pellets with the isolation layers and the enteric layers. The prepared tapentadol hydrochloride enteric sustained release pellets have novel dosage forms, are steady in medicine release, have good controllability, have obvious technological advantages compared with tablets on the market and conduce to improving the bioavailability.
Description
Technical field
the present invention relates to a kind of pharmaceutical preparation, particularly relate to a kind of tapentadol hydrochloride slow-release micro-pill and preparation method thereof.
Background technology
tapentadol hydrochloride (TapentadolHydrochloride) is the new oral analgesic by Johnson & Johnson of U.S. pharmacy (Johnson & Johnson.) and German GruenenthalGmbH company joint research and development, its quick-release tablet goes on the market (trade name: NUCNTA) in November, 2008 through U.S. FDA approval, the fast-release tablet used clinically has 50,75,100mg3 kind specification, for alleviating moderate and severe acute pain.Its slow releasing tablet through U.S. FDA approval listing (trade name: NUCYNTAER), is used for the treatment of the relevant neuropathic pain that maturity-onset diabetes peripheral neuropathy (DPN) causes in August, 2012.By 2 times/day, oral analgesic mode, can play continuously, opium sample analgesic activity can maintain a period of time.Tapentadol hydrochloride belongs to opioid drug, the shock-resistant extruding of said preparation, and (as drugs) can be prevented to abuse.
tapentadol hydrochloride is a kind of central analgesics of novel dual model of action, tapentadol hydrochloride realizes more potent analgesia effectiveness by two kinds of complementary mechanism of action, it is mu opioid receptor excitomotor, again that norepinephrine heavily absorbs depressant, to acute, the several animal models of inflammatory and chronic neuropathic pain model has analgesic activity, its usefulness is between morphine and tramadol, but tapentadol hydrochloride than other opium kind analgesics as morphine, tramadol etc., more not easily produce analgesic tolerance and dependency, untoward reaction is (as felt sick, vomiting etc.) lighter, side effect is little.
at present, it is low to there is drug release stablizing effect in the existing product on market, poor controllability, and bioavailability is low waits deficiency.
Summary of the invention
the object of this invention is to provide one, to have drug release stablizing effect high, and controllability is good, a kind of tapentadol hydrochloride slow-release micro-pill that bioavailability is high.
in order to realize object of the present invention, the present invention is achieved by the following technical solutions: a kind of tapentadol hydrochloride slow-release micro-pill, comprises enteric layer, sealing coat, pastille micropill; It is characterized in that: described enteric layer is wrapped in outside sealing coat, sealing coat is wrapped in outside pastille micropill; Described enteric layer comprises: enteric premix coating materials 178mg; Described sealing coat comprises: hypromellose 16-32mg, sucrose 3-20mg, Pulvis Talci 6-22mg, purified water 280-420mg; Described pastille micropill comprises: tapentadol hydrochloride 50mg, celphere 50mg, filler 103-165mg, lubricant 5-28mg, binding agent 5-6mg.
in described sealing coat, preferred weight proportion is: cellulose 24mg, sucrose 8mg, Pulvis Talci 10mg, purified water 350mg.
in described pastille micropill, preferred weight proportion is: filler 150mg, lubricant 25mg, binding agent 5mg.
described filler is microcrystalline Cellulose; Described lubricant is Pulvis Talci; Described binding agent is hypromellose.
its manufacture method comprises following operation:
1, purified water is used by binding agent to make the binder solution that concentration is 2%;
2, by thiamphenicol raw material, filler, mix lubricant evenly, mixed point is made, for subsequent use;
3, celphere is put into centrifugal pellet processing machine, spray with binding agent and by above-mentioned mixed powder slowly spread as wherein, put into fluid bed after completing and dry, make pastille micropill, for subsequent use;
4, hypromellose, sucrose, Pulvis Talci, purified water are configured to sealing coat coating materials by above-mentioned weight proportion;
5, pastille micropill is put into fluidized bed coating agent, adjustment parameter, adopt the sealing coat coating materials configured to carry out coating, make sealing coat pill, for subsequent use;
6, enteric premix coating materials and purified water are configured to enteric coating agents;
7, sealing coat pill is put into fluidized bed coating agent, adjustment parameter, adopt the enteric coating agents configured to carry out coating;
8, in the pill after coating being incapsulated.
the present invention relates to the enteric coated micropill that tapentadol hydrochloride is effective ingredient, described micropill is take tapentadol hydrochloride as main component, appropriate celphere, filler, binding agent, stabilizing agent, lubricant are made pastille micropill, then wrapped with sealing coat, enteric coat layer.The molten slow-release micro-pill of tapentadol hydrochloride prepared by the present invention, dosage form is novel, and the release of medicine is steady, controllability good, has obvious technical advantage, improve bioavailability compared with the tablet that goes on the market.
tapentadol hydrochloride is first is also a unique medicine being used for the treatment of the neuropathic pain relevant to DPN through FDA approval.Related to this, tapentadol hydrochloride is also approvedly at present be used for the treatment of the chronic pain of adult's moderate to severe, is continuous, to need an a period of time analgesia.At the nearly 2,600 ten thousand people's diabeticss of the U.S., the diabetics of about 60-70% has the neuropathy of certain form.Modal neuropathy is DPN, and this can cause pain and the sensory deprivation of toe, foot, lower limb, hands and arm, also may comprise persistent fever, twinge or a sensation of pricking.According to estimates, nearly eight million peoples are had to affect by DPN in the U.S..The mechanism that DPN occurs is very complicated, comprises maincenter and periphery mechanism, and some patient suffering from DPN needs number of ways in treatment." pain that DPN causes is difficult to control; this makes some patients and medical personnel go to find replacement therapy; " Miami University's medical college, this a. Candiotti of the base of medical anesthesia and internal medicine, doctor of medicine professor says, " tapentadol hydrochloride is compared with current Therapeutic Method, is a diverse ways, may become the new selection that of these patients is important." tapentadol hydrochloride is a synthesis analgesic acting on maincenter.Its definite mechanism of action is not yet known.Although clinical correlation it be unclear that, the research of preclinical shows, tapentadol hydrochloride is receptor and reuptake inhibitor simultaneously.Extract two random three phase controlled clinical trial data, after display tapentadol hydrochloride treats 3 weeks, the pain intensity of patient at least reduces one point, and in these patients, a part continues the tapentadol hydrochloride taking same dosage, and a part changes oral placebo into.After 12 weeks, compared with the patient changing placebo into those, the pain continuing to take tapentadol hydrochloride obviously alleviates (100-250 milligrams, every day twice).Result of study also shows, tapentadol hydrochloride generally has good toleration.
process characteristic of the present invention: 1, select raw material science, production technology is advanced, and its product is conveniently deposited and used; 2, product Chinese medicine composition is easily absorbed by the body; 3, raw material sources are extensive, add process line short, the easy processing and manufacturing of product.
detailed description of the invention:
embodiment 1
a kind of tapentadol hydrochloride slow-release micro-pill, comprises enteric layer, sealing coat, pastille micropill; It is characterized in that: described enteric layer is wrapped in outside sealing coat, sealing coat is wrapped in outside pastille micropill; Described enteric layer comprises: enteric premix coating materials 178mg; Described sealing coat comprises: hypromellose 16-32mg, sucrose 3-20mg, Pulvis Talci 6-22mg, purified water 280-420mg; Described pastille micropill comprises: tapentadol hydrochloride 50mg, celphere 50mg, filler 103-165mg, lubricant 5-28mg, binding agent 5-6mg.
in described sealing coat, preferred weight proportion is: cellulose 24mg, sucrose 8mg, Pulvis Talci 10mg, purified water 350mg.
in described pastille micropill, preferred weight proportion is: filler 150mg, lubricant 25mg, binding agent 5mg.
described filler is microcrystalline Cellulose; Described lubricant is Pulvis Talci; Described binding agent is hypromellose.
embodiment 2
its manufacture method comprises following operation:
1, purified water is used by binding agent to make the binder solution that concentration is 2%;
2, by thiamphenicol raw material, filler, mix lubricant evenly, mixed point is made, for subsequent use;
3, celphere is put into centrifugal pellet processing machine, spray with binding agent and by above-mentioned mixed powder slowly spread as wherein, put into fluid bed after completing and dry, make pastille micropill, for subsequent use;
4, hypromellose, sucrose, Pulvis Talci, purified water are configured to sealing coat coating materials by above-mentioned weight proportion;
5, pastille micropill is put into fluidized bed coating agent, adjustment parameter, adopt the sealing coat coating materials configured to carry out coating, make sealing coat pill, for subsequent use;
6, enteric premix coating materials and purified water are configured to enteric coating agents;
7, sealing coat pill is put into fluidized bed coating agent, adjustment parameter, adopt the enteric coating agents configured to carry out coating;
8, in the pill after coating being incapsulated.
Claims (5)
1. a tapentadol hydrochloride slow-release micro-pill, comprises enteric layer, sealing coat, pastille micropill; It is characterized in that: described enteric layer is wrapped in outside sealing coat, sealing coat is wrapped in outside pastille micropill; Described enteric layer comprises: enteric premix coating materials 178mg; Described sealing coat comprises: hypromellose 16-32mg, sucrose 3-20mg, Pulvis Talci 6-22mg, purified water 280-420mg; Described pastille micropill comprises: tapentadol hydrochloride 50mg, celphere 50mg, filler 103-165mg, lubricant 5-28mg, binding agent 5-6mg.
2. a kind of tapentadol hydrochloride slow-release micro-pill according to claim 1, is characterized in that: in described sealing coat, preferred weight proportion is: cellulose 24mg, sucrose 8mg, Pulvis Talci 10mg, purified water 350mg.
3. a kind of tapentadol hydrochloride slow-release micro-pill according to claim 1, is characterized in that: in described pastille micropill, preferred weight proportion is: filler 150mg, lubricant 25mg, binding agent 5mg.
4. a kind of tapentadol hydrochloride slow-release micro-pill according to claim 1 or 3, is characterized in that: described filler is microcrystalline Cellulose; Described lubricant is Pulvis Talci; Described binding agent is hypromellose.
5. the preparation method of a kind of tapentadol hydrochloride slow-release micro-pill according to claim 1-3, is characterized in that: comprise following operation:
Used by binding agent purified water to make binder solution that concentration is 2%;
By thiamphenicol raw material, filler, mix lubricant evenly, make mixed point, for subsequent use;
Celphere is put into centrifugal pellet processing machine, spray with binding agent and by above-mentioned mixed powder slowly spread as wherein, put into fluid bed after completing and dry, make pastille micropill, for subsequent use;
Hypromellose, sucrose, Pulvis Talci, purified water are configured to sealing coat coating materials by above-mentioned weight proportion;
Pastille micropill is put into fluidized bed coating agent, adjustment parameter, adopt the sealing coat coating materials configured to carry out coating, make sealing coat pill, for subsequent use;
Enteric premix coating materials and purified water are configured to enteric coating agents;
Sealing coat pill is put into fluidized bed coating agent, adjustment parameter, adopt the enteric coating agents configured to carry out coating;
During pill after coating is incapsulated.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410666708.0A CN104434881A (en) | 2014-11-20 | 2014-11-20 | Tapentadol hydrochloride sustained release pellets and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410666708.0A CN104434881A (en) | 2014-11-20 | 2014-11-20 | Tapentadol hydrochloride sustained release pellets and preparation method thereof |
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| CN104434881A true CN104434881A (en) | 2015-03-25 |
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| Application Number | Title | Priority Date | Filing Date |
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| CN201410666708.0A Pending CN104434881A (en) | 2014-11-20 | 2014-11-20 | Tapentadol hydrochloride sustained release pellets and preparation method thereof |
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Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101601659A (en) * | 2009-07-02 | 2009-12-16 | 昆明积大制药有限公司 | A kind of glutathione enteric-coated pellet and preparation method thereof |
| CN102065852A (en) * | 2007-11-23 | 2011-05-18 | 普罗泰克医药公司 | Tapentadol compositions |
| EP2606879A1 (en) * | 2011-12-21 | 2013-06-26 | Hexal AG | Multiple unit pellet tablet formulation comprising an opioid |
-
2014
- 2014-11-20 CN CN201410666708.0A patent/CN104434881A/en active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102065852A (en) * | 2007-11-23 | 2011-05-18 | 普罗泰克医药公司 | Tapentadol compositions |
| CN101601659A (en) * | 2009-07-02 | 2009-12-16 | 昆明积大制药有限公司 | A kind of glutathione enteric-coated pellet and preparation method thereof |
| EP2606879A1 (en) * | 2011-12-21 | 2013-06-26 | Hexal AG | Multiple unit pellet tablet formulation comprising an opioid |
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Application publication date: 20150325 |
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