CN103877052A - Aminophylline tablet and preparation method thereof - Google Patents
Aminophylline tablet and preparation method thereof Download PDFInfo
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- CN103877052A CN103877052A CN201410118013.9A CN201410118013A CN103877052A CN 103877052 A CN103877052 A CN 103877052A CN 201410118013 A CN201410118013 A CN 201410118013A CN 103877052 A CN103877052 A CN 103877052A
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Abstract
The invention relates to an aminophyline tablet and a preparation method thereof. The aminophyline is prepared from the following components in parts by weight: 100 parts of aminophyline, 2-100 parts of microcrystalline cellulose, 1-4 parts of hydroxypropyl methylcellulose, 1-5 parts of silicon dioxide and 1-2 parts of magnesium stearate.
Description
Technical field:
The present invention relates to a kind of preparation of pharmaceutical preparation, particularly a kind of aminophylline sheet and preparation thereof.
Background technology:
Aminophylline is theophylline and ethylenediamine double salt, and its pharmacological action is mainly from theophylline, and ethylenediamine strengthens its water solublity.Aminophylline has direct relexation to airway smooth muscle.Its mechanism of action more complicated, thinks in the past by suppressing phosphodiesterase, makes due to the interior cAMP content raising of cell.Recently experiment thinks that the bronchiectatic activity part of theophylline is that in addition, theophylline is purinoceptor blocker due to endogenous epinephrine and the result of norepinephrine release, can resist the contraction to respiratory tract such as adenine.Theophylline can strengthen contraction of diaphragm power, and especially in the time that contraction of diaphragm is unable, effect is more remarkable, is therefore of value to and improves respiratory function.Aminophylline still has faint diastole coronary artery, peripheral blood vessel and the effect of bile duct smooth muscle.There are slight increase contractility and slight diuresis.
Existing Truphylline mainly comprises following dosage form:
1. aminophylline sheet: 1. 0.1g; 2. 0.2g.
2. aminophylline injection: 1. 2ml:0.25g; 2. 2ml:0.5g.
3. aminophylline suppositories: 0.25g.
4. aminophylline slow releasing tablet: 0.1g.
The most frequently used is aminophylline sheet, easy to use because of it, cheap, welcome by patient, but existing aminophylline sheet exists the prominent problem of releasing, someone has investigated the outer stripping curve in real time of aminophylline lamellar body that different manufacturers is produced, relatively between Liao Ge producer and and Japanese orange paper in difference between aminophylline sheet stripping curve, found that, the stripping quantity of the aminophylline sheet of 31 enterprises in the time of 5min is all greater than 40%, all produces prominent releasing; The in real time stripping behavior in 4 kinds of dissolution mediums of the aminophylline sheet of part producer differs greatly, and inherent quality exists larger difference, and the aminophylline sheet produced of part producing enterprise to criticize interior homogeneity poor, technique is unstable, product quality heterogeneity.
For solving the prominent problem of releasing of aminophylline sheet, the invention provides a kind of Truphylline and preparation method thereof.This Amoline is made up of the supplementary material of following weight portion: the aminophylline of 100 parts, the microcrystalline Cellulose of 2～100 parts, hypromellose, 1～5 silicon dioxide of 1～4 part, the magnesium stearate of 1～2 part are made.Aminophylline flake products of the present invention is stable and controllable for quality, and finished tablet content is even, stripping property good, has prevented from not existing dashing forward releasing problem, and the rate that manufactures a finished product is greatly high, cost is low.
Summary of the invention:
The invention provides a kind of aminophylline sheet, its formula is as follows:
The above part is weight portion, and its unit can be milligram, gram, kilogram, ton etc.
More than formula, if in grams, can prepare 1000 of aminophylline sheets.
The preferred aminophylline sheet of the present invention, its formula is as follows:
Particularly preferred aminophylline sheet, its formula is as follows:
Most preferred aminophylline sheet, its formula is as follows:
The preparation method of aminophylline sheet of the present invention is carried out according to the following steps:
(1) get after aminophylline is pulverized and cross 65 mesh sieves.
(2) get after microcrystalline Cellulose, hypromellose, silicon dioxide are crossed 65 mesh sieves with aminophylline powder and mix homogeneously.
(3) add magnesium stearate mix homogeneously.
(4) will mix rear mixed powder compressed tablets on tablet machine, tablet detects qualified rear packed products.
The present invention's formula obtains through screening, and screening technique is as follows:
Through screening, determine that formula components is aminophylline, microcrystalline Cellulose, hypromellose, silicon dioxide, magnesium stearate.
For obtaining satisfied result of extraction, the present invention has carried out following experiment:
The use amount screening of microcrystalline Cellulose is as follows:
| Component | Formula 1 | Formula 2 | Formula 3 | Formula 4 | Formula 5 | Formula 6 |
| Aminophylline | 100 grams | 100 grams | 100 grams | 100 grams | 100 grams | 100 grams |
| Microcrystalline Cellulose | 1 gram | 25 grams | 50 grams | 75 grams | 100 grams | 125 grams |
| Hypromellose | 2 grams | 2 grams | 2 grams | 2 grams | 2 grams | 2 grams |
| Silicon dioxide | 2 grams | 2 grams | 2 grams | 2 grams | 2 grams | 2 grams |
| Magnesium stearate | 1 gram | 1 gram | 1 gram | 1 gram | 1 gram | 1 gram |
The use amount screening of hypromellose is as follows:
| Component | Formula 7 | Formula 8 | Formula 9 | Formula 10 | Formula 11 | Formula 12 |
| Aminophylline | 100 grams | 100 grams | 100 grams | 100 grams | 100 grams | 100 grams |
| Microcrystalline Cellulose | 50 grams | 50 grams | 50 grams | 50 grams | 50 grams | 50 grams |
| Hypromellose | 0.5 gram | 1 gram | 2 grams | 3 grams | 4 grams | 5 grams |
| Silicon dioxide | 2 grams | 2 grams | 2 grams | 2 grams | 2 grams | 2 grams |
| Magnesium stearate | 1 gram | 1 gram | 1 gram | 1 gram | 1 gram | 1 gram |
Dissolution Rate Testing
Formula 1-12 aminophylline sheet is according to dissolution method (2010 editions two annex XC the second methods of Chinese Pharmacopoeia), taking water as dissolution medium, Revolution Per Minute 50 turns, 5 minutes and sampling in 30 minutes, after dilution, measure trap at the wavelength place of 271nm, obtain as calculated dissolution, limit must not be respectively labelled amount 40% and must not be less than 85% of labelled amount, test data sees the following form.
Table 1, the 5 minutes stripping results of respectively filling a prescription:
| ? | For the first time | For the second time | For the third time | The 4th time | The 5th time | The 6th time |
| Formula 1 | 29.72 | 29.34 | 28.75 | 29.82 | 29.34 | 30.54 |
| Formula 2 | 30.14 | 30.52 | 30.47 | 29.52 | 29.62 | 31.74 |
| Formula 3 | 28.86 | 29.34 | 28.45 | 27.88 | 29.57 | 29.82 |
| Formula 4 | 35.87 | 35.86 | 36.12 | 35.63 | 35.98 | 36.02 |
| Formula 5 | 37.75 | 37.56 | 36.58 | 37.78 | 38.56 | 37.54 |
| Formula 6 | 41.25 | 42.42 | 42.54 | 44.24 | 40.95 | 41.64 |
| Formula 7 | 43.75 | 46.52 | 44.75 | 43.78 | 45.52 | 43.87 |
| Formula 8 | 34.42 | 33.56 | 34.12 | 34.53 | 33.91 | 34.79 |
| Formula 9 | 28.86 | 29.34 | 28.45 | 27.88 | 29.57 | 29.82 |
| Formula 10 | 22.72 | 21.34 | 20.75 | 19.82 | 29.34 | 30.54 |
| Formula 11 | 15.72 | 14.56 | 16.85 | 14.85 | 17.14 | 16.85 |
| Formula 12 | 11.72 | 10.75 | 10.96 | 12.79 | 12.92 | 11.85 |
Table 2, the 30 minutes stripping results of respectively filling a prescription:
| ? | For the first time | For the second time | For the third time | The 4th time | The 5th time | The 6th time |
| Formula 1 | 85.35 | 86.12 | 85.65 | 84.24 | 86.21 | 84.36 |
| Formula 2 | 92.65 | 91.54 | 89.93 | 90.28 | 89.57 | 91.83 |
| Formula 3 | 97.45 | 98.77 | 96.25 | 95.56 | 97.24 | 98.45 |
0039?
| Formula 4 | 99.45 | 99.21 | 101.25 | 99.89 | 100.68 | 99.51 |
| Formula 5 | 99.89 | 99.70 | 101.56 | 99.82 | 100.01 | 99.75 |
| Formula 6 | 99.85 | 99.38 | 100.25 | 100.89 | 99.51 | 99.07 |
| Formula 7 | 99.08 | 99.93 | 100.05 | 100.96 | 99.89 | 99.87 |
| Formula 8 | 98.56 | 99.76 | 98.89 | 99.46 | 99.98 | 99.24 |
| Formula 9 | 97.45 | 98.77 | 96.25 | 95.56 | 97.24 | 98.45 |
| Formula 10 | 92.78 | 91.86 | 90.72 | 90.89 | 89.52 | 89.83 |
| Formula 11 | 86.85 | 86.94 | 85.68 | 86.56 | 85.98 | 85.45 |
| Formula 12 | 84.45 | 83.77 | 85.25 | 84.56 | 83.24 | 84.45 |
The present invention finds unexpectedly, the increase of hypromellose consumption can effectively suppress the release of 5 minutes aminophylline sheets, the increase of microcrystalline Cellulose consumption can effectively improve the release of 30 minutes aminophylline sheets, for this reason, the present invention has carried out appropriateness adjustment to the consumption of hypromellose and microcrystalline Cellulose, thereby find one can effectively control 5 minutes dissolutions of aminophylline sheet, prevent that it is because of the prominent generation toxicity of releasing, can ensure that again it discharged formula completely at 30 minutes, from the known optimum formula of the present invention of experimental result be: formula 3 or formula 9.
Tablet result of extraction of the present invention is good, aminophylline sheet stripping below 40% in the time of 5 minutes, aminophylline sheet stripping more than 85% in the time of 30 minutes, and constant product quality.
Detailed description of the invention:
Further illustrate by the following examples the present invention.
Embodiment 1
A kind of Amoline, percent meter comprises following component by weight:
A preparation method for Amoline, comprises the following steps (each amounts of components is by described in table 1):
(1) aminophylline of getting described weight proportion is pulverized rear 65 mesh sieves of crossing.
(2) microcrystalline Cellulose, hypromellose, the silicon dioxide of getting described weight proportion are mixed homogeneously after crossing 65 mesh sieves with described aminophylline powder.
(3) add the described magnesium stearate mix homogeneously of described weight proportion.
(4) will mix rear mixed powder compressed tablets on tablet machine, tablet detects qualified rear packed products.
Embodiment 2
A kind of Amoline, percent meter comprises following component by weight:
| Component | Weight |
| Aminophylline | 100 grams |
| Microcrystalline Cellulose | 100 grams |
| Hypromellose | 1 |
| Silicon dioxide | 4 grams |
| Magnesium stearate | 2.04 gram |
A preparation method for Amoline, comprises the following steps (each amounts of components is by described in table 2):
(1) aminophylline of getting described weight proportion is pulverized rear 65 mesh sieves of crossing.
(2) microcrystalline Cellulose, hypromellose, the silicon dioxide of getting described weight proportion are mixed homogeneously after crossing 65 mesh sieves with described aminophylline powder.
(3) add the described magnesium stearate mix homogeneously of described weight proportion.
(4) will mix rear mixed powder compressed tablets on tablet machine, tablet detects qualified rear packed products.
Embodiment 3
A kind of Amoline, percent meter comprises following component by weight:
| Component | Weight |
| Aminophylline | 100 grams |
| Microcrystalline Cellulose | 2 grams |
| Hypromellose | 4 grams |
| Silicon dioxide | 2 grams |
| Magnesium stearate | 1 gram |
A preparation method for Amoline, comprises the following steps:
(1) aminophylline of getting described weight proportion is pulverized rear 65 mesh sieves of crossing.
(2) microcrystalline Cellulose, hypromellose, the silicon dioxide of getting described weight proportion are mixed homogeneously after crossing 65 mesh sieves with described aminophylline powder.
(3) add the described magnesium stearate mix homogeneously of described weight proportion.
(4) will mix rear mixed powder compressed tablets on tablet machine, tablet detects qualified rear packed products.
Embodiment 4
A kind of Amoline, percent meter comprises following component by weight:
| Component | Weight |
0071?
| Aminophylline | 100 grams |
| Microcrystalline Cellulose | 2 grams |
| Hypromellose | 1 gram |
| Silicon dioxide | 4.1 gram |
| Magnesium stearate | 2.09 gram |
A preparation method for Amoline, comprises the following steps:
(1) aminophylline of getting described weight proportion is pulverized rear 65 mesh sieves of crossing.
(2) microcrystalline Cellulose, hypromellose, the silicon dioxide of getting described weight proportion are mixed homogeneously after crossing 65 mesh sieves with described aminophylline powder.
(3) add the described magnesium stearate mix homogeneously of described weight proportion.
(4) will mix rear mixed powder compressed tablets on tablet machine, tablet detects qualified rear packed products.
Embodiment 5
A kind of Amoline, percent meter comprises following component by weight:
| Component | Weight |
| Aminophylline | 100 grams |
| Microcrystalline Cellulose | 75 grams |
| Hypromellose | 1 gram |
| Silicon dioxide | 4.0 gram |
| Magnesium stearate | 2.04 gram |
A preparation method for Amoline, comprises the following steps:
(1) aminophylline of getting described weight proportion is pulverized rear 65 mesh sieves of crossing.
(2) microcrystalline Cellulose, hypromellose, the silicon dioxide of getting described weight proportion are mixed homogeneously after crossing 65 mesh sieves with described aminophylline powder.
(3) add the described magnesium stearate mix homogeneously of described weight proportion.
(4) will mix rear mixed powder compressed tablets on tablet machine, tablet detects qualified rear packed products.
Embodiment 6
A kind of Amoline, percent meter comprises following component by weight:
| Component | Weight |
| Aminophylline | 100 grams |
| Microcrystalline Cellulose | 25 grams |
| Hypromellose | 3 grams |
| Silicon dioxide | 2 grams |
| Magnesium stearate | 1 gram |
A preparation method for Amoline, comprises the following steps:
(1) aminophylline of getting described weight proportion is pulverized rear 65 mesh sieves of crossing.
(2) microcrystalline Cellulose, hypromellose, the silicon dioxide of getting described weight proportion are mixed homogeneously after crossing 65 mesh sieves with described aminophylline powder.
(3) add the described magnesium stearate mix homogeneously of described weight proportion.
(4) will mix rear mixed powder compressed tablets on tablet machine, tablet detects qualified rear packed products.
Embodiment 7
| Component | Weight |
0095?
| Aminophylline | 100 grams |
| Microcrystalline Cellulose | 100 grams |
| Hypromellose | 4 |
| Silicon dioxide | 2 grams |
| Magnesium stearate | 1 gram |
A preparation method for Amoline, comprises the following steps (each amounts of components is by described in table 1):
(1) aminophylline of getting described weight proportion is pulverized rear 65 mesh sieves of crossing.
(2) microcrystalline Cellulose, hypromellose, the silicon dioxide of getting described weight proportion are mixed homogeneously after crossing 65 mesh sieves with described aminophylline powder.
(3) add the described magnesium stearate mix homogeneously of described weight proportion.
(4) will mix rear mixed powder compressed tablets on tablet machine, tablet detects qualified rear packed products.
Claims (5)
1. an aminophylline tablet composition, its formula is as follows:
2. according to the compositions of claim 1, its formula is as follows:
3. according to the compositions of claim 1, its formula is as follows:
4. according to the compositions of claim 1, its formula is as follows:
5. the preparation method of the compositions of claim 1, carry out according to the following steps:
(1) get after aminophylline is pulverized and cross 65 mesh sieves,
(2) get after microcrystalline Cellulose, hypromellose, silicon dioxide are crossed 65 mesh sieves with aminophylline powder and mix homogeneously,
(3) add magnesium stearate mix homogeneously,
(4) will mix rear mixed powder compressed tablets on tablet machine, tablet detects qualified rear packed products.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410118013.9A CN103877052B (en) | 2014-03-27 | 2014-03-27 | A kind of aminophylline tablets and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410118013.9A CN103877052B (en) | 2014-03-27 | 2014-03-27 | A kind of aminophylline tablets and preparation method thereof |
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| Publication Number | Publication Date |
|---|---|
| CN103877052A true CN103877052A (en) | 2014-06-25 |
| CN103877052B CN103877052B (en) | 2016-02-03 |
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| Application Number | Title | Priority Date | Filing Date |
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| CN201410118013.9A Expired - Fee Related CN103877052B (en) | 2014-03-27 | 2014-03-27 | A kind of aminophylline tablets and preparation method thereof |
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| Country | Link |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104523569A (en) * | 2014-12-25 | 2015-04-22 | 海南卫康制药(潜山)有限公司 | Aminophylline composition freeze-dried tablet and preparation method thereof |
| CN106265567A (en) * | 2016-08-30 | 2017-01-04 | 林州中农颖泰生物肽有限公司 | A kind of water solublity aminophylline tablets and preparation method thereof |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1762493A (en) * | 2004-10-19 | 2006-04-26 | 上海中西制药有限公司 | Process for preparing compound aminophylline tablet |
| CN103006605A (en) * | 2012-09-24 | 2013-04-03 | 浙江莎普爱思药业股份有限公司 | Bendazac lysine sustained release preparation as well as preparation method and application of preparation |
-
2014
- 2014-03-27 CN CN201410118013.9A patent/CN103877052B/en not_active Expired - Fee Related
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1762493A (en) * | 2004-10-19 | 2006-04-26 | 上海中西制药有限公司 | Process for preparing compound aminophylline tablet |
| CN103006605A (en) * | 2012-09-24 | 2013-04-03 | 浙江莎普爱思药业股份有限公司 | Bendazac lysine sustained release preparation as well as preparation method and application of preparation |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104523569A (en) * | 2014-12-25 | 2015-04-22 | 海南卫康制药(潜山)有限公司 | Aminophylline composition freeze-dried tablet and preparation method thereof |
| CN106265567A (en) * | 2016-08-30 | 2017-01-04 | 林州中农颖泰生物肽有限公司 | A kind of water solublity aminophylline tablets and preparation method thereof |
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| Publication number | Publication date |
|---|---|
| CN103877052B (en) | 2016-02-03 |
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