CN103948554A - Anastrozole chewable tablet and preparation method for same - Google Patents
Anastrozole chewable tablet and preparation method for same Download PDFInfo
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- CN103948554A CN103948554A CN201410158211.8A CN201410158211A CN103948554A CN 103948554 A CN103948554 A CN 103948554A CN 201410158211 A CN201410158211 A CN 201410158211A CN 103948554 A CN103948554 A CN 103948554A
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Abstract
The invention relates to the technical field of medicine preparations, and in particular relates to an anastrozole-containing chewable tablet and a preparation method for the same. The anastrozole chewable tablet is composed of main medicine anastrozole, filler, a flavouring agent, a flow aid, a deodorant and an adhesive, capable of being used for patients difficult to swallow common tablets, and good in medicine compliance; the anastrozole chewable tablet can be dissolved in saliva after being chewed in mouth, the medicine can be absorbed by mucous membranes in oral cavity or esophagus, and the bioavailability is high; the anastrozole chewable tablet is sweet in flavour and good in taste, eliminates pungent smell, and is fragrant; the anastrozole chewable tablet is convenient to take and carry; and the anastrozole chewable tablet is prepared by a direct compression method, good in medicine stability, simple in production process, and low in cost.
Description
Invention field
The present invention relates to a kind of pharmaceutical composition containing Anastrozole, more particularly, the present invention relates to a kind of Anastrozole chewable tablet.The invention still further relates to the preparation method of described Anastrozole chewable tablet.
Background of invention
Breast carcinoma is one of common malignant tumor of world women.The positive increase year after year of sickness rate, in current elderly population, the age, what suffer from breast cancer accounted for 26% higher than the women of 65 years old, and wherein approximately 1/3 tumor growth needs high estrogen level to maintain, and has the feature of estrogen-dependent.Estrogen-dependent type breast carcinoma is apt to occur in postmenopausal women.Estrogen-dependent type patient with breast cancer commonly uses antiestrogen, and tamoxifen is as first-line treatment medicine, but when tamoxifen is brought into use, effect is better, and life-time service just easily produces drug resistance, causes disease relapse.The another kind of mechanism of action is different from the arimedex of tamoxifen, effective to above-mentioned drug resistance patient.At present the good arimedex of curative effect is Formestane, clinical use at home and abroad, but Formestane can only drug administration by injection, and oral invalid.
The growth of breast cancer cell can be dependent on estrogenic existence, and the estrogen (estrone and estradiol) during women circulated after menopause is mainly transformed the androgen in adrenal gland and ovary (androstenedione and testosterone) by the aromatase in peripheral tissues.By suppressing aromatase, to stop estrogen production be the method for hormonal dependent breast carcinoma after a kind of effective as selective treatment menopause.
Anastrozole (Anastrozole) is efficient, the non-body class arimedex that stays of high selectivity.The main source of postmenopausal women's estradiol is: under the effect of the aromatase complex of androstenedione in peripheral tissues, be converted into estrone, estrone is converted into estradiol subsequently.The estradiol level reducing in circulation proves to be conducive to breast cancer women.Super-sensitive analytical test demonstration, postmenopausal women takes 1mg Anastrozole every day can reduce more than 80% estradiol level.Anastrozole does not have progestogen sample, androgenic and estrogenic activity, be applicable to the treatment of postmenopausal women's advanced breast cancer, to the patient of estrogen receptor negative, if it presents positive clinical response to tamoxifen, can consider to use, be applicable to the auxiliary treatment of the breast carcinoma of early stage of postmenopausal women's estrogen receptor positive.
Anastrozole is only second to letrozole in arimedex hospital administration, similar to letrozole, from 06 year, medication increases considerably, almost each season medication is increasing, supply falls short of demand in visible market, and potential market demand is discharged, and appeals with clinical disease structural change in recent years and media and medical institutions that energetically paying close attention to the activities such as women's health has substantial connection.
The current clinical practice dosage form of Anastrozole is mainly conventional tablet, needs patient's water to swallow, and for the patient of child, old people and the solid chemicals of can not swallowing, has certain inconvenience.Summary of the invention object of the present invention is just to provide a kind of stable in properties, evident in efficacy, is suitable for old people and the Anastrozole chewable tablet of the patient of the solid chemicals of can not swallowing use.
Summary of the invention
Another order of the present invention is to provide the preparation method of above-mentioned Anastrozole chewable tablet, and it adopts modern technology of preparing, can commercial scale, high efficiency production, and it is stable that product quality keeps.The concrete technical scheme that the present invention adopts is as follows:
On the one hand, the present invention relates to a kind of Anastrozole chewable tablet, wherein, described Anastrozole chewable tablet is composed of the following components: weight portion is the Anastrozole of 10～100 parts, weight portion is the filler of 100～1000 parts, and weight portion is the correctives of 5～200 parts, the fluidizer that weight portion is 2～80 parts, weight portion is the flavoring agent of 10～300 parts, and weight portion is the binding agent of 2～100 parts.
Some embodiments therein, Anastrozole chewable tablet of the present invention is composed of the following components:
Anastrozole 1～10g
Lactose 100～1000g
Cyclamate 5～90g
Sweet 5～the 20g of A Siba
Magnesium stearate 2～80g
Powdered flavor 10～300g
Ethanol 2～100g
Food coloring 2～80g
Be pressed into the sheet that 0.2～2.0g is heavy.
Some embodiments therein, Anastrozole chewable tablet of the present invention, wherein, described filler is lactose, sucrose, dextrin, mannitol, xylitol, sorbitol, microcrystalline Cellulose, glucose, erithritol or starch, or above-mentioned any two kinds or any two or more mixture.
Some embodiments therein, Anastrozole chewable tablet of the present invention, wherein, described correctives is, cyclamate, A Siba are sweet, glycyrrhizin, saccharin sodium, thaumati, vitamin C, or above-mentioned any two kinds or two or more mixture arbitrarily.
Some embodiments therein, Anastrozole chewable tablet of the present invention, wherein, described fluidizer is following formula magnesium stearate, micropowder silica gel, Pulvis Talci, Polyethylene Glycol, stearic acid, or above-mentioned any two kinds or any two or more mixture.
Some embodiments therein, Anastrozole chewable tablet of the present invention, wherein, described binding agent is ethanol, 1～10% Polyethylene Glycol ethanol, 1～10% polyethylene pyrroles protective embankment ketone ethanol, 1～10% ethyl cellulose ethanol, or above-mentioned any two kinds or two or more mixture arbitrarily.
Some embodiments therein, Anastrozole chewable tablet of the present invention, wherein, described flavoring agent is the powdered flavor that human body can be accepted taste.
Some embodiments therein, Anastrozole chewable tablet of the present invention, wherein, described imatinib mesylate chewable tablet is made by following prescription:
Anastrozole 1g
Lactose 699g
Cyclamate 90g
The sweet 20g of A Siba
Magnesium stearate 40g
Powdered flavor 100g
Ethanol 40g
Food coloring 10g
Make 1000.
On the other hand, the present invention relates to a kind of preparation method of Anastrozole chewable tablet, wherein, described method is carried out according to following steps order: a. supplementary material is crossed respectively 100 mesh sieves; B. Anastrozole, filler, rectify and hide agent, mix homogeneously, add binding agent to make soft material, cross 20 mesh sieves and granulate, dry under 30～80oC vacuum condition, then cross 20 mesh sieves and carry out granulate; C. add fluidizer and flavoring agent, mix; D. be pressed into the sheet that 0.2～2.0g is heavy.
Some embodiments therein, the method for preparing Anastrozole chewable tablet of the present invention wherein, adds to rectify in hiding agent also to add food coloring in step b.
Some embodiments therein, the method for preparing Anastrozole chewable tablet of the present invention, wherein, and sugar coating again after steps d tabletting, described food coloring adds in the time of coating.
Used in the present inventionly rectify that to hide agent be the mouthfeel sense of taste of improving tablet, being adjusted to as far as possible human body easily accepts, flavoring agent is especially in order to eliminate the penetrating odor that in tablet, Anastrozole produces, and makes this tablet before entrance, is difficult for being refused by the organum olfactorium of human body.Add the outward appearance that food coloring can chewable tablet more beautiful.Described filler, as diluent, can be selected lactose, sucrose, dextrin, mannitol, xylitol, sorbitol, microcrystalline Cellulose, glucose, erithritol, starch, or above-mentioned any two kinds or any two or more mixture.Wherein preferably lactose is filler.Described correctives is used for correcting the poor taste bringing due to Anastrozole or adjuvant, can select that cyclamate, A Siba are sweet, glycyrrhizin, saccharin sodium, thaumati, vitamin C, or above-mentioned any two kinds or two or more mixture arbitrarily.Be used for increasing the fluidizer of drug flow, can select magnesium stearate, micropowder silica gel, Pulvis Talci, Polyethylene Glycol, stearic acid, or above-mentioned any two kinds or any two or more mixture.Wherein preferably magnesium stearate is fluidizer.In order to correct the flavoring agent of medicine penetrating odor, can accept with human body the powdered flavor of taste, as various fruity powdered flavors.
The dosage of film-making of the present invention can be adjusted on demand, owing to being chewable tablet, can make common sheet heavy prescription amount, also can be made into the special-shaped tablets more great than ordinary tablet, as can be made into polygon, capsule shape, circle, annular.
The beneficial effect of Anastrozole chewable tablet of the present invention and preparation method thereof is mainly reflected in: (1) the inconvenient patient of conventional tablet that can be used for swallowing, and drug compliance is good; (2) can be dissolved in saliva after putting into mouth and chewing, medicine can absorb by oral cavity or intraesophageal mucosa, and bioavailability is high; (3) not only the sweet mouthfeel of taste is good, and has corrected penetrating odor, has fragrance; (4) do not need drinking water also can take, taking convenience and being easy to carry; (5) adopt direct compression process preparation, medicine stability is good, and production technology is simple, cost is low.Detailed description of the invention, by specific embodiment given below, can further be well understood to the present invention, but they is not limitation of the invention.
Detailed description of the invention
Following examples have further described and demonstrated embodiment within the scope of the present invention.Embodiment is only used to the object of illustrations and provides, and is not intended to be regarded as limitation of the present invention, and it may exist the multiple variant that does not deviate from spirit and scope of the invention.
Embodiment 1 Anastrozole chewable tablet preparation
1.1 prescription
Anastrozole 1g
Lactose 699g
Cyclamate 90g
The sweet 20g of A Siba
Magnesium stearate 40g
Powdered flavor 100g
Ethanol 40g
Food coloring 10g
Make 1000
The Anastrozole chewable tablet of the above-mentioned prescription of 1.2 preparation, carries out according to following steps:
1.2.1 supplementary material is crossed respectively 100 mesh sieves;
1.2.2 sweet to Anastrozole, lactose, cyclamate, A Siba, grape pigment mix homogeneously, add ethanol to make soft material, cross 20 mesh sieves and granulate, dry under 50oC vacuum condition, then cross 20 orders. sieve carries out granulate.
1.2.3 add magnesium stearate and fresh cream, mix.
1.2.4 tabletting.
Embodiment 2 Anastrozole chewable tablet preparations
2.1 prescription
Anastrozole 5g
Lactose 695g
Cyclamate 90g
The sweet 20g of A Siba
Magnesium stearate 40g
Powdered flavor 100g
Ethanol 40g
Food coloring 10g
Make 1000
The Anastrozole chewable tablet of the above-mentioned prescription of 2.2 preparation, carries out according to following steps:
2.2.1 supplementary material is crossed respectively 100 mesh sieves;
2.2.2 Anastrozole, dextrin, cyclamate, glycyrrhizin, Fructus Gardeniae blue pigment mix homogeneously, add 5% ethyl cellulose ethanol to make soft material, cross 20 mesh sieves and granulate, dry under 40oC vacuum condition, then cross 20 mesh sieves and carry out granulate.
2.2.3 add micropowder silica gel and green apple essence, mix.
2.2.4 tabletting.
Embodiment 3 Anastrozole chewable tablet preparations
3.1 prescription
Anastrozole 10g
Mannitol 640g
Erithritol 50g
Cyclamate 50g
Stearic acid 10g
Orange flavor 100g
5% polyethylene pyrroles protective embankment ketone ethanol 100g
Gardenia yellow pigment 40g
Make altogether 1000
The Anastrozole chewable tablet of the above-mentioned prescription of 3.2 preparation, carries out according to following steps:
3.2.l supplementary material is crossed respectively 100 mesh sieves:
3.2.2 Anastrozole, mannitol, erithritol, cyclamate mix homogeneously, add 5% polyvinylpyrrolidone ethanol to make soft material, cross 20 mesh sieves and granulate, dry under 55oC vacuum condition, then cross 20 mesh sieves and carry out granulate.
3.2.3 add stearic acid and orange flavor, mix.
3.2.4 tabletting, carries out coating, and wrap and add gardenia yellow pigment farming season.
Embodiment 4 Anastrozole chewable tablet preparations
4.1 prescription
Anastrozole 8g
Sucrose 597g
Dextrin 100g
Glucose 200g
Cyclamate 10g
Thaumati 5g
Polyethylene Glycol 20g
Chocolate essence 20g
8% polyvinylpyrrolidone ethanol 10g
Monascorubin 30g
Make altogether 1000
The Anastrozole chewable tablet of the above-mentioned prescription of 4.2 preparation, carries out according to following steps:
4.2.1 supplementary material is crossed respectively 100 mesh sieves;
4.2.2 Anastrozole, sucrose, dextrin, glucose, cyclamate, thaumati mix homogeneously, add 8% polyvidon ethanol to make soft material, cross 20 mesh sieves and granulate, under 60oC vacuum condition, thousand is dry, then crosses 20 mesh sieves and carry out granulate.
4.2.3 add Polyethylene Glycol and chocolate essence, mix.
4.2.4 tabletting, carries out coating, adds monascorubin when coating.
The clinical bioequivalence Journal of Sex Research of test example 1
20 health volunteers are random intersects after Anastrozole ordinary tablet (commercially available) 5mg (5X1mg/ compositions) of 5 days continuous oral embodiment 1 Anastrozole chewable tablet 5mg (5X1mg/ grain) and reference examples, by Anastrozole concentration in HPLC method mensuration blood plasma.Taking the Anastrozole of Nat'l Pharmaceutical & Biological Products Control Institute as standard control, with the relative bioavailability F of area-method estimation embodiment 1 Anastrozole chewing composition be 97.4% ± 6.3%.After the Anastrozole chewable tablet 5X1mg of 5 days continuous oral embodiment 1 of 20 health volunteers, the elimination half-life of Anastrozole is 0.51 ± 0.10, peak time and reach peak concentration and be respectively 0.8 ± 0.2 hour and 17.54 ± 3.42u g/ml.After Anastrozole ordinary tablet (commercially available) 5X1mg of oral reference examples, the elimination half-life of Anastrozole is 0.52 ± 0.08h hour, peak time and reach that peak concentration is respectively 0.8 ± 0.2 hour and 18.17 ± 4.20u g/ml illustrates that the pharmacokinetic parameter of two kinds of Anastrozole preparations is close.
Claims (10)
1. an Anastrozole chewable tablet, wherein, described Anastrozole chewable tablet is composed of the following components:
Weight portion is the Anastrozole of 10～100 parts, and weight portion is the filler of 100～1000 parts, and weight portion is the correctives of 5～200 parts, the fluidizer that weight portion is 2～80 parts, and weight portion is the flavoring agent of 10～300 parts, weight portion is the binding agent of 2～100 parts.
2. Anastrozole chewable tablet as claimed in claim 1, wherein, described Anastrozole chewable tablet by
Following component composition:
Anastrozole 1～10g
Lactose 100～1000g
Cyclamate 5～90g
Sweet 5～the 20g of A Siba
Magnesium stearate 2～80g
Powdered flavor 10～300g
Ethanol 2～100g
Food coloring 2～80g
Be pressed into the sheet that 0.2～2.0g is heavy.
3. Anastrozole chewable tablet as claimed in claim 1, wherein, described filler is lactose, sucrose, dextrin, mannitol, xylitol, sorbitol, microcrystalline Cellulose, glucose, erithritol or starch, or above-mentioned any two kinds or any two or more mixture.
4. Anastrozole chewable tablet as claimed in claim 1, wherein, described correctives is, cyclamate, A Siba are sweet, glycyrrhizin, saccharin sodium, thaumati, vitamin C, or above-mentioned any two kinds or two or more mixture arbitrarily.
5. Anastrozole chewable tablet as claimed in claim 1, wherein, described fluidizer is following formula magnesium stearate, micropowder silica gel, Pulvis Talci, Polyethylene Glycol, stearic acid, or above-mentioned any two kinds or any two or more mixture.
6. Anastrozole chewable tablet as claimed in claim 1, wherein, described binding agent is ethanol, 1～10% Polyethylene Glycol ethanol, 1～10% polyethylene pyrroles protective embankment ketone ethanol, 1～10% ethyl cellulose ethanol, or above-mentioned any two kinds or two or more mixture arbitrarily.
7. Anastrozole chewable tablet as claimed in claim 1, wherein, described flavoring agent is the powdered flavor that human body can be accepted taste.
8. the Anastrozole chewable tablet as described in claim 1-7 any one, wherein, described Anastrozole chewable tablet is made by following prescription:
Anastrozole 1g
Lactose 699g
Cyclamate 90g
The sweet 20g of A Siba
Magnesium stearate 40g
Powdered flavor 100g
Ethanol 40g
Food coloring 10g
Make 1000.
9. a method of preparing the Anastrozole chewable tablet as described in claim 1-8 any one, wherein, described method is carried out according to following steps order: a. supplementary material is crossed respectively 100 mesh sieves; B. Anastrozole, filler, rectify and hide agent, mix homogeneously, add binding agent to make soft material, cross 20 mesh sieves and granulate, dry under 30～80oC vacuum condition, then cross 20 mesh sieves and carry out granulate; C. add fluidizer and flavoring agent, mix; D. be pressed into the sheet that 0.2～2.0g is heavy.
10. prepare as claimed in claim 9 the method for Anastrozole chewable tablet, wherein, in step b, add to rectify in hiding agent also to add food coloring; Or after steps d tabletting sugar coating again, described food coloring adds in the time of coating.
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| Application Number | Priority Date | Filing Date | Title |
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| CN201410158211.8A CN103948554A (en) | 2014-04-18 | 2014-04-18 | Anastrozole chewable tablet and preparation method for same |
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| Application Number | Priority Date | Filing Date | Title |
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| CN201410158211.8A CN103948554A (en) | 2014-04-18 | 2014-04-18 | Anastrozole chewable tablet and preparation method for same |
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Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1490006A (en) * | 2003-08-20 | 2004-04-21 | 杭州容立医药科技有限公司 | Melazocine masticatory and its preparation |
| CN102085191A (en) * | 2009-12-08 | 2011-06-08 | 北京以岭生物工程有限公司 | Anastrozole oral disintegrating tablet and preparation method thereof |
| DE102010033458A1 (en) * | 2010-08-05 | 2012-02-09 | Helvista Ag | Use of lectin composition for e.g. prophylaxis and/or treatment of gonadotropin releasing hormone-analogues-related adverse drug side effects, comprising emulsified lectin, and optionally further auxiliary substances and carrier substances |
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2014
- 2014-04-18 CN CN201410158211.8A patent/CN103948554A/en active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1490006A (en) * | 2003-08-20 | 2004-04-21 | 杭州容立医药科技有限公司 | Melazocine masticatory and its preparation |
| CN102085191A (en) * | 2009-12-08 | 2011-06-08 | 北京以岭生物工程有限公司 | Anastrozole oral disintegrating tablet and preparation method thereof |
| DE102010033458A1 (en) * | 2010-08-05 | 2012-02-09 | Helvista Ag | Use of lectin composition for e.g. prophylaxis and/or treatment of gonadotropin releasing hormone-analogues-related adverse drug side effects, comprising emulsified lectin, and optionally further auxiliary substances and carrier substances |
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