CN101467977A - Oxycodone controlled release tablets - Google Patents
Oxycodone controlled release tablets Download PDFInfo
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- CN101467977A CN101467977A CNA2007103084526A CN200710308452A CN101467977A CN 101467977 A CN101467977 A CN 101467977A CN A2007103084526 A CNA2007103084526 A CN A2007103084526A CN 200710308452 A CN200710308452 A CN 200710308452A CN 101467977 A CN101467977 A CN 101467977A
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- controlled release
- oxycodone
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- release tablets
- pain
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Abstract
The invention belongs to the technical field of medicament, disclosing an oxycodone controlled release tablet for easing durative moderate to severe pain. The characteristic of the novel formulation is that the invention is controlled release tablet which slowly and constantly or nearly constantly release medicament in water or determined releasing substrate.
Description
Technical field
The invention belongs to technical field of pharmaceuticals, relate to a kind of dosage form of oxycodone, be used to alleviate durative moderate to pharmaceutical preparation of severe pain and preparation method thereof, specifically a kind of preparation method of oxycodone controlled release tablets.
Background technology
Pain investigation of Japan in 2004 shows that chronic pain patient is suffered from by Japan nearly 1,700 ten thousand, and is satisfied although 88% pain patients is represented the doctor, has only 23% patient that the alleviation degree of pain is pleased oneself.In Japan, also generally do not reach " pain is medicable " common recognition, also lack the common recognition of " must treat " among the doctor to pain.The survey result that the Huang Yuguang professor of China carried out before 4 years similarly.Not only in the Asia, all there is identical problem in the whole world in fact, and promptly pain does not obtain fine control.
In recent years, one of progress of pain therapy aspect was that WHO three step analgesia schemes are known by numerous doctors.WHO recommends, if effectively pain relieving of on-steroidal AID (NSAIDs) can add with a kind of weak opioid drug, also can use the compound formulation of NSAIDs and weak opioid drug.But no matter be to strengthen NSAIDs dosage, or low dose of NSAIDs prolonged application, coagulation disorders or gastrointestinal side effect all can take place in the patient.Therefore, the patient of contraindication is arranged, can directly use the opioid drug in second ladder, from low dose, can reach same analgesic effect, and not have the side effect of NSAIDs for using NSAIDs.At second ladder of pain therapy, there are two kinds of opioid drugs can be for selecting for use, wherein tramadol has the effect of binding, and the oxycodone effect that do not bind.
The oxycodone hydrochloride controlled release tablet is a kind of opium analgesics, and this medicine is a kind of pure opioid receptor agonist, combines with the μ receptor and the kappa receptor of opiate receptor.It has had the history in more than 80 year in clinical practice.The oxycodone hydrochloride controlled release tablet is the novel form that base of a fruit group development is sprouted by the U.S., is first oxycodone that can take every 12h in the world.Go on the market at U.S. Register in nineteen ninety-five, go on the market in China in JIUYUE, 2004.
The dosage range of oxycodone controlled release tablets is wider, can handle the pain that the different causes of disease cause, and is also effective to nociception pain and neuropathic pain as cancer pain, non-cancer pain, and has the advantage of psychological aspects.Its pharmacokinetic characteristics is: oral administration biaavailability is higher than morphine, and the half-life is short, and medication can reach steady plasma-drug concentration in 24～36 hours, it is pure opiates agonist, AD does not have the effect of binding, and long-term prescription does not have to be accumulated, and its metabolite does not have obvious activity etc.
Oxycodone controlled release tablets can administration in per 12 hours 1 time, is used for moderate and severe pain.Oxycodone controlled release tablets is except that having the total characteristics of oxycodone, also comprise: quick acting, be easy to titration, medication can make pain control stable in 2 days, owing to do not have the dosage effect that binds, therefore, can increase dosage with the progress of pain, dosage and blood drug level and drug action dependency are good, therefore can predict blood drug level.In addition, its curative effect is subjected to the influence of age, sex, race and morbid state little, its adverse reaction rate zero difference in the young and old people.
The characteristics of other pharmacology aspects also have: food is to the not influence of its bioavailability, and the delirium incidence rate is lower than morphine, and the skin pruritus incidence rate is well below morphine during dose,equivalent.
Up to now, have 180 multinomial clinical researches all over the world oxycodone controlled release tablets has been carried out analysis and evaluation, the pain cause that these researchs relate to comprises cancer pain, rheumatic/osteoarthritis pain, backache, postherpetic neuralgia, diabetic neuropathic pain, peri-operation period and postoperative pain and other pain, comprises that in addition OxyContin is used for special population such as old people, child, hepatic renal dysfunction patient's research.
Cancer pain is the big field that oxycodone controlled release tablets is used.A research of carrying out in Latin America is assessed the curative effect that 120 routine cancer patients use OxyContin.The result shows, treat 1 week, 2 weeks after, pain intensity obviously weakens, sleep quality improves, the number of times that wake up because of pain night reduces, the patient also increases gradually to the acceptance level of pain.
The safety aspect, the patient feels sick, vomiting, constipation, dizzy and calm incidence rate are all lower, surpasses 4%.Therefore researcher is thought, short application use oxycodone controlled release tablets 41mg/ day, prolonged application 48mg/ day be alleviating pain effectively, in the lenitive while, patients ' life quality also can be improved significantly, oral oxycodone controlled release tablets can effectively be treated chronic pain, and patient tolerability is better, but above-mentioned dosage is mean dose, increase as patient's pain degree, then should increase the oxycodone controlled release tablet amounts.Pharmacological action and clinical practice
1. pharmacological action
Oxycodone is the opiate receptor full agonist, and the opiate receptor of brain and spinal cord is had affinity.The similar morphine of the effect of oxycodone.Main pharmacological is analgesia, and other pharmacological action comprises anxiety, cough-relieving and calmness.No maximum dose restriction.
Can think that from several research datas oxycodone is extremely low to the danger that the people produces genotoxicity.
2. pharmacokinetics
The absorption half-life of promptly releasing oxycodone is 0.4h, and it is a kind of single-phase absorption mode.And oxycodone controlled release tablets is because after having adopted Acro Contin controlled-release technology, it has the absorption mode of a two-phase.Fast Absorption section is because 38% oxycodone discharges the absorption half-life with 37min at once; The slow trapping section is because 62% oxycodone slowly discharges and the absorption half-life of 6.2h.Medicine continuous action 12h, oxycodone absorbs good, and oral administration biaavailability is 60%～87%.
The two-phase of oxycodone absorbs and means that after taking medicine, patient's pain can not only be alleviated rapidly at every turn in the oxycodone controlled release tablet, and they still can experience the benefit that this medicine brings from the pain relief that continues, and reduces medicining times.In the research of pain-suffered patient, 1h pain was just controlled after most patients took medicine after surgery.
3. clinical practice
3.1. cancer pain field
Reports such as German Frank in 2002, research is assessed curative effect and safety that oxycodone controlled release tablets is used for chronic cancer pain and non-cancer pain adult patient after the listing that they carry out, and has estimated medication 3～4 alleviation situations all and pain after 6 months respectively.Curative effect assessment to 3667 routine patients shows, with use oxycodone controlled release tablets before compare, medication phase I (the 1st week), second stage (3～4 week) and after 6 months, the overall pain intensity of patient, cancerous pain, neuropathic pain and musculoskeletal pain intensity all are the decline of carrying out property.General curative effect and toleration to the muscle skeleton pain patients are analyzed, Follow-up results showed in 6 months, most patient's curative effects and toleration are evaluated as or are very good, with the treatment before compare, medication phase I and second stage, patient's general health, locomotor activity and sleep quality all have clear improvement.
3.2. non-cancer pain field
In non-cancer pain treatment field, oxycodone controlled release tablets is mainly used in the pain that pain, peri-operation period and postoperative pain that rheumatic/osteoarthritis pain, backache, postherpetic neuralgia, diabetic neuropathy cause and other reasons cause.October calendar year 2001～in JIUYUE, 2002 is added up the back discovery to the recipe quantity of oxycodone controlled release tablets in the U.S., and the recipe quantity that is used for cancer pain accounts for 15.5%, and the recipe quantity that is used for non-cancer pain accounts for 84.5%.An investigation of Germany also shows, from calendar year 2001 to 2003 year oxycodone controlled release tablets ratio that is used for non-cancer pain increase (increasing to 60%) gradually from 30%.Macro or mass analysis being carried out in four researchs find that the dosage that oxycodone controlled release tablets is used for non-cancer pain is (40～45) mg, is to be used for half of cancer pain patient.
In the research of delivering in 2002, Watson etc. are when the curative effect of assessment oxycodone controlled release tablets treatment neuropathic pain, employing need be accepted the case load (NNT) of additional procedures as the therapeutic evaluation index, and this index value is low more, shows that analgesic effect is good more.The result shows, the therapeutic equivalence of oxycodone controlled release tablets and gabapentin even be better than gabapentin.
This product has following characteristics:
Oxycodone controlled release tablets is the opiates oral analgesic, has safe, efficient and per characteristics of taking 1 time in 12 hours.Oxycodone controlled release tablets has the two-phase absorption mode: medicine discharges to impel medicine to absorb (medicine plays a role in 1 hour) in early days rapidly, when occurring one section long absorption afterwards to guarantee the effective blood drug concentration in 12 hours.This oxycodone dosage form has reduced the number of times that the patient takes medicine, and needn't make the patient have good compliance to medicine because of the disrupted sleep of frequently taking medicine, thereby help the control of pain.
Summary of the invention
The object of the invention be to provide a kind of good stability, quality height, evident in efficacy, untoward reaction is little is tablet of making of principal agent and preparation method thereof with the oxycodone, uses oxycodone controlled release tablets that this method makes constant speed or near the release medicine of constant speed lentamente in water or in the release medium of regulation.
A kind of oxycodone controlled release tablets of the present invention is made up of following component:
40 parts of oxycodones
300 parts in dextrin
300 parts of polyethylene
70%pvp ethanol liquid is an amount of
The prescription of coating solution
50 parts of cellulose acetate
Polysorbate-80 is an amount of
Phthalic acid dibutyl ester is an amount of
90% ethanol-acetone solution adds to 1000 parts
A kind of oxycodone controlled release tablets of the present invention is achieved through the following technical solutions:
Get oxycodone, dextrin, the polyethylene mixing is granulated drying, granulate, tabletting with 70%pvp ethanol liquid.Get cellulose acetate, polysorbate-80 is an amount of, and phthalic acid dibutyl ester is an amount of, with the dissolving of 90% ethanol-acetone mixed solvent 1000ml join coating solution.Coating to every coating tablets layer heavily is 8.5～9mg.Product inspection, coating.
A kind of oxycodone controlled release tablets that the present invention obtains has that method is simple, good stability, characteristics that quality is high.
Embodiment 1: 1000 of specifications
Prescription:
Oxycodone 5/10/20/40g
Dextrin 300g
Polyethylene 300g
70%pvp ethanol liquid is an amount of
The prescription of coating solution
Cellulose acetate 50g
Polysorbate-80 is an amount of
Phthalic acid dibutyl ester is an amount of
90% ethanol-acetone solution adds to 1000ml
Method for making:
Get oxycodone, dextrin, the polyethylene mixing is granulated drying, granulate, tabletting with 70%pvp ethanol liquid.Get cellulose acetate, polysorbate-80 is an amount of, and phthalic acid dibutyl ester is an amount of, with the dissolving of 90% ethanol-acetone mixed solvent 1000ml join coating solution.Coating to every coating tablets layer heavily is 8.5～9mg.Product inspection, coating.
Embodiment 2: 10000 of specifications
Prescription:
Oxycodone 400g
Dextrin 3000g
Polyethylene 3000g
70%pvp ethanol liquid is an amount of
The prescription of coating solution
Cellulose acetate 500g
Polysorbate-80 is an amount of
Phthalic acid dibutyl ester is an amount of
90% ethanol-acetone solution adds to 10000ml
Method for making:
Get oxycodone, dextrin, the polyethylene mixing is granulated drying, granulate, tabletting with 70%pvp ethanol liquid.Get cellulose acetate, polysorbate-80 is an amount of, and phthalic acid dibutyl ester is an amount of, with the dissolving of 90% ethanol-acetone mixed solvent 1000ml join coating solution.Coating to every coating tablets layer heavily is 8.5～9mg.Product inspection, coating.
Claims (7)
1. an oxycodone controlled release tablets is characterized in that this controlled release tablet is is the tablet that principal agent is made with the oxycodone, and every contains oxycodone 10mg～100mg.
2. according to the described oxycodone controlled release tablets of claim 1, it is characterized in that this controlled release tablet constant speed or near the release medicine of constant speed lentamente in water or in the release medium of regulation.
3. according to the described oxycodone controlled release tablets of claim 1, it is characterized in that: the preparation of tablet is not limited to adopt direct compression or the back tabletting of granulating, and this controlled release tablet is made up of following component:
40 parts of oxycodones
300 parts in dextrin
300 parts of polyethylene
70%pvp ethanol liquid is an amount of
The prescription of coating solution
50 parts of cellulose acetate
Polysorbate-80 is an amount of
Phthalic acid dibutyl ester is an amount of
90% ethanol-acetone solution adds to 1000 parts.
4. according to the described oxycodone controlled release tablets of claim 3, it is characterized in that described filler is dextrin, starch, microcrystalline Cellulose, lactose etc., plasticizer is polyethylene, phthalic acid dibutyl ester etc., binding agent is a 70%pvp ethanol liquid, solubilizing agent is a cellulose acetate, emulsifying agent is a polysorbate-80, but is not limited to this filler.
5. according to the described oxycodone controlled release tablets of claim 3, it is characterized in that described filler: plasticizer: binding agent: solubilizing agent: emulsifying agent is 1:0.02～0.5:0.3～5:0.01～1.5:0.01～0.5.
6. oxycodone controlled release tablets according to claim 3, one of prescription that it is characterized in that this controlled release tablet is:
Oxycodone 40g
Dextrin 300g
Polyethylene 300g
70%pvp ethanol liquid is an amount of
The prescription of coating solution
Cellulose acetate 50g
Polysorbate-80 is an amount of
Phthalic acid dibutyl ester is an amount of
90% ethanol-acetone solution adds to 1000ml.
7. oxycodone controlled release tablets according to claim 6 is characterized in that may further comprise the steps:
Get oxycodone, dextrin, the polyethylene mixing is granulated drying, granulate, tabletting with 70%pvp ethanol liquid.Get cellulose acetate, polysorbate-80 is an amount of, and phthalic acid dibutyl ester is an amount of, with the dissolving of 90% ethanol-acetone mixed solvent 1000ml join coating solution.Coating to every coating tablets layer heavily is 8.5～9mg.Product inspection, coating.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2007103084526A CN101467977A (en) | 2007-12-29 | 2007-12-29 | Oxycodone controlled release tablets |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2007103084526A CN101467977A (en) | 2007-12-29 | 2007-12-29 | Oxycodone controlled release tablets |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN101467977A true CN101467977A (en) | 2009-07-01 |
Family
ID=40825941
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNA2007103084526A Pending CN101467977A (en) | 2007-12-29 | 2007-12-29 | Oxycodone controlled release tablets |
Country Status (1)
| Country | Link |
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| CN (1) | CN101467977A (en) |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103933003A (en) * | 2014-02-25 | 2014-07-23 | 王丽丽 | Fentanyl controlled release tablet, and preparation method thereof |
| CN103948551A (en) * | 2014-04-22 | 2014-07-30 | 青岛市市立医院 | Domperidone controlled-release tablet and preparation method thereof |
| CN104000795A (en) * | 2014-06-03 | 2014-08-27 | 青岛市市立医院 | Diammonium glycyrrhizinate controlled release tablets and preparation method thereof |
-
2007
- 2007-12-29 CN CNA2007103084526A patent/CN101467977A/en active Pending
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103933003A (en) * | 2014-02-25 | 2014-07-23 | 王丽丽 | Fentanyl controlled release tablet, and preparation method thereof |
| CN103948551A (en) * | 2014-04-22 | 2014-07-30 | 青岛市市立医院 | Domperidone controlled-release tablet and preparation method thereof |
| CN104000795A (en) * | 2014-06-03 | 2014-08-27 | 青岛市市立医院 | Diammonium glycyrrhizinate controlled release tablets and preparation method thereof |
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| Date | Code | Title | Description |
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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 |
Open date: 20090701 |