CN1757390A - Obtundent-Tilidin hydrochloride preparation - Google Patents

Obtundent-Tilidin hydrochloride preparation Download PDF

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Publication number
CN1757390A
CN1757390A CN 200510012547 CN200510012547A CN1757390A CN 1757390 A CN1757390 A CN 1757390A CN 200510012547 CN200510012547 CN 200510012547 CN 200510012547 A CN200510012547 A CN 200510012547A CN 1757390 A CN1757390 A CN 1757390A
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CN
China
Prior art keywords
preparation
tilidine
agent
tilidine hydrochloride
filler
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
Application number
CN 200510012547
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Chinese (zh)
Inventor
徐进
滑千里
王英利
赵学刚
徐强
岳玉敏
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
YUE ZHENJIANG
Original Assignee
YUE ZHENJIANG
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by YUE ZHENJIANG filed Critical YUE ZHENJIANG
Priority to CN 200510012547 priority Critical patent/CN1757390A/en
Publication of CN1757390A publication Critical patent/CN1757390A/en
Pending legal-status Critical Current

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Abstract

An analgesic in the form of tablet or capsule is prepared from tilidine hydrochloride, filler, disintegrant, lubricant and adhesive.

Description

A kind of preparation of obtundent-Tilidin hydrochloride
Technical field
The present invention relates to analgesic formulations, particularly is a kind of preparation of obtundent-Tilidin hydrochloride.
Background technology
Tilidine hydrochloride is a complete synthesis opium analgesic, acts on the central nervous system, can suppress pain sensation maincenter by selectivity, other sensation is not had influence, and keep patient's Consciousness, belong to the narcosis analgesic thing, have dependency, be used for the pain relieving of moderate to severe pain.Tilidine hydrochloride is a kind of prodrug, and itself does not have analgesic effect, almost completely is being converted into μ-receptor stimulating agent Nortilidine through behind the liver first-pass effect.Having spinal cord produces analgesia, suppresses to breathe, make effects such as the people is glad, physical dependence with the upper part.Tilidate has advantages such as dosage is low, and analgesic effect is good, and addiction is little.Its analgesic activity mechanism is a kind of opioid receptor agonist for the catabolite Nortilidine of tilidate, and with the effect of receptors bind simulation endogenous analgesic opioid peptide, the interior anti-pain sensation of kinetoplast system realizes.Have spasmolysis simultaneously, unlike common opioid analgesics (as morphine etc.), can not produce respiration inhibition effect and obstipation, addiction is low.Its analgesic activity intensity is not subjected to the influence of administering mode, onset in 5-20 minute after the administration, and the persistent period is about 5-6 hour, is WHO " three step analgesia guidelines " recommended drug, and its structural formula is as follows:
It is low that tilidate has a dosage, good analgesic effect, the advantage that addiction is little.For further reducing addiction, Germany has developed the compound preparation of tilidate and Na Luoxi paulownia.But tilidate is urgently soluble in water.Have and intensively draw moistly,, can decomposite impurity such as methyl tilidate, nor-tilidate the photo-thermal instability.Affect the treatment and clinical use.
Summary of the invention
For promoting the clinical practice of tilidate, give full play to its curative effect, satisfy the demand of clinical ground analgesic.The invention provides tilidine hydrochloride tablet and hard capsule.Tilidine hydrochloride tablet of the present invention or hard capsule are made by following weight proportion by the host and the adjuvant of following weight proportion;
A, tilidine hydrochloride 4-8
B, filler 4-12
C, disintegrating agent 2-10
D, lubricant 0.04-1
E, wetting agent or binding agent 1-6.
The preferred weight proportioning of raw material is:
A, tilidine hydrochloride 5-7
B, filler 5-11
C, disintegrating agent 4-8
D, lubricant 0.06-0.08
E, wetting agent or binding agent 2-5.
Its filler can be pregelatinized Starch, lactose, Macrogol 4000, polyethylene glycol 6000, mannitol, a kind of or two kinds or the two or more mixture of xylitol.Its disintegrating agent can be that basic Starch Sodium, low-substituted hydroxypropyl cellulose, microcrystalline Cellulose, crosslinked polyethylene are given a tongue-lashing and coughed up one of bright, the crosslinked first of alkane shallow lake carboxymethylstach sodium or two kinds or two or more mixture.Its lubricant can be a magnesium stearate, or Pulvis Talci or micropowder silica gel, or magnesium stearate and talcous mixture.Its wetting agent is ethanol or dehydrated alcohol.Its binding agent is one of starch slurry, polyvidone, cellulose family, or the mixture of two or more material.
Its manufacture method is: filler, disintegrating agent, lubricant are sieved, with the tilidine hydrochloride of recipe quantity and filler, interior disintegrating agent mix homogeneously, add wetting agent again and make soft material, granulation, drying, granulate sieve, add outer disintegrating agent, mix lubricant is even, tabletting or filling after the assay was approved, tablet check back bag film-coat, promptly aluminum-plastic packaged.The present invention selects for use dehydrated alcohol etc. to make wetting agent, and adopts 45 ℃ of-50 ℃ of dryings of low temperature; Select for use do not have draw moist, can improve tablet appearance, release fast, assay is not had influence, flowability, good filler lactose that compressibility is strong etc.; Select for use the hypromellose with good disintegrative, compressibility, the low hyprolose of getting to make interior disintegrating agent (filler), can quicken the medicine stripping; Select for use have good flowability, compressibility, can improve the tablet molding, increase tablet hardness, carboxymethyl starch sodium that disintegrating property is good etc. makes outer disintegrating agent, can promote principal agent disintegrate stripping from preparation; Select for use have good tack and with the granule mixing after be evenly distributed and not easily separated, only with showing on a small quantity well.Lubrication makes the bright and clean magnesium stearate attractive in appearance of tablet face make lubricant.Thereby make tablet of the present invention unilateral complete, bright and clean, color and luster is even, in water rapidly disintegrate stripping and methyl tilidate etc. to decompose the impurity that produces few, draw moist very lowly, biological utilisation is very high, and is easy to use, can guarantee curative effect, addiction is very little.
The specific embodiment
Embodiment 1:
Take by weighing tilidine hydrochloride 40 grams, add pregelatinized Starch 35 grams, microcrystalline Cellulose 15 grams, low hyprolose 20 grams of getting, polyethylene glycol 6000 40 gram mix homogeneously, add 15% starch slurry and make soft material, soft material is granulated 50 ℃ of dryings, dried granule through 14 mesh sieve granulate by 14 mesh sieves, adds crosslinked carboxymethyl fecula 5 grams, magnesium stearate 5 gram mix homogeneously, after the assay was approved tabletting or be filled in the hard capsule.Use LE coating materials bag film-coat after the assay was approved, plastic-aluminum (aluminum inscription) packing, outer package is promptly.
Embodiment 2
Take by weighing tilidine hydrochloride 30 gram, add mannitol 30 grams,, microcrystalline Cellulose 35 grams.Crosslinked polyethylene is given a tongue-lashing pyrrolidone 10 grams, Macrogol 4000 state 15 gram mix homogeneously, add 5% polyvidone ethanol solution 5 and restrain into suitable soft material, soft material is granulated by 14 mesh sieves, 50 ℃ of dryings, dried granule are through 14 mesh sieve granulate, add crosslinked carboxymethylstach sodium 5 gram Pulvis Talci 3 grams, magnesium stearate 2 gram mix homogeneously, tabletting or fillings after the assay was approved, tablet is used LE coating materials bag film-coat after the assay was approved, and plastic-aluminum (aluminum aluminum) packing, outer package are promptly.
Embodiment 3
Take by weighing tilidine hydrochloride 30 grams. Add xylitol 20 grams, carboxymethyl starch sodium 20 grams.Crospolyvinylpyrrolidone 40 grams.Polyethylene glycol 6000 40 gram mix homogeneously, add 3% poly-dimension copper ethanol solution 30 and restrain into suitable soft material, soft material is granulated by 14 mesh sieves, 50 ℃ of dryings, dried granule are through 14 mesh sieve granulate, add carboxymethyl starch sodium 5 grams, Pulvis Talci 3 grams, mix homogeneously, be up to the standards tabletting or filling, tablet is used LE coating film clothing after the assay was approved, plastic-aluminum (aluminum aluminum) packing, outer package promptly.
Embodiment 4
Take by weighing hydrochloric acid for fixed 30 grams of agent, add lactose 40 grams, carboxymethyl starch sodium 21 grams, crosslinked carboxymethylstach sodium 16 grams, Macrogol 4000 30 gram mix homogeneously.Add ethanol 10 and restrain into suitable soft material, soft material adds carboxymethyl starch sodium 5 grams by 14 mesh sieve granulate, magnesium stearate 5 gram mix homogeneously, tabletting or filling after the assay was approved, tablet is after the assay was approved, with LE coating materials bag film-coat, plastic-aluminum (aluminum aluminum) packing, outer package is promptly.
Embodiment 5
Take by weighing tilidine hydrochloride 40 grams, add lactose 40 grams, hypromellose 18 grams, low hyprolose 18 grams, the Macrogol 4000 25 gram mix homogeneously got, add dehydrated alcohol 15 and restrain into suitable soft material, soft material is upright by 14 mesh sieve systems, 45 ℃ of dryings, dried granule are through 14 mesh sieve granulate, add carboxymethyl starch sodium 5 grams, micropowder silica gel 5 gram mix homogeneously, LE coating materials bag film-coat is used in tabletting or filling after the assay was approved, pateat universis per praesentes after the assay was approved, and plastic-aluminum (aluminum aluminum) packing, outer package are promptly.

Claims (7)

1, a kind of preparation of obtundent-Tilidin hydrochloride is characterized in that it being tablet or hard capsule, is made by following materials of weight proportions:
A, tilidine hydrochloride 4-8
B, filler 4-12
C, disintegrating agent 2-10
D, lubricant 0.04-1
E, wetting agent or binding agent 1-6.
2, the preparation of tilidine hydrochloride according to claim 1 is characterized in that wherein the weight ratio of each raw material is:
A, tilidine hydrochloride 5-7
B, filler 5-11
C, disintegrating agent 4-8
D, lubricant 0.06-0.08
E, wetting agent or binding agent 2-5.
3, the preparation of tilidine hydrochloride according to claim 1 and 2 is characterized in that said filler is a kind of of pregelatinized Starch lactose, Macrogol 4000, polyethylene glycol 6000, mannitol or xylitol, or two kinds, or two or more mixture.
4, the preparation of tilidine hydrochloride according to claim 3, it is characterized in that said disintegrating agent is a kind of of carboxymethyl starch sodium, low-substituted hydroxypropyl cellulose, microcrystalline Cellulose, crospolyvinylpyrrolidone, crosslinked carboxymethylstach sodium, or two or more mixture.
5, the preparation of tilidine hydrochloride according to claim 4 is characterized in that said lubricant is magnesium stearate or Pulvis Talci, or micropowder silica gel, or magnesium stearate and talcous mixture.
6, the preparation of tilidine hydrochloride according to claim 5 is characterized in that said wetting agent is ethanol or dehydrated alcohol.
7, according to the preparation of claims 6 described tilidine hydrochlorides, it is characterized in that said binding agent is a starch slurry, or polyvidone, or cellulose family.
CN 200510012547 2005-05-30 2005-05-30 Obtundent-Tilidin hydrochloride preparation Pending CN1757390A (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN 200510012547 CN1757390A (en) 2005-05-30 2005-05-30 Obtundent-Tilidin hydrochloride preparation

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
CN 200510012547 CN1757390A (en) 2005-05-30 2005-05-30 Obtundent-Tilidin hydrochloride preparation

Publications (1)

Publication Number Publication Date
CN1757390A true CN1757390A (en) 2006-04-12

Family

ID=36703058

Family Applications (1)

Application Number Title Priority Date Filing Date
CN 200510012547 Pending CN1757390A (en) 2005-05-30 2005-05-30 Obtundent-Tilidin hydrochloride preparation

Country Status (1)

Country Link
CN (1) CN1757390A (en)

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