CN109172539A - A kind of Biomox and its production method and application - Google Patents
A kind of Biomox and its production method and application Download PDFInfo
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- CN109172539A CN109172539A CN201811255007.2A CN201811255007A CN109172539A CN 109172539 A CN109172539 A CN 109172539A CN 201811255007 A CN201811255007 A CN 201811255007A CN 109172539 A CN109172539 A CN 109172539A
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
- A61K31/429—Thiazoles condensed with heterocyclic ring systems
- A61K31/43—Compounds containing 4-thia-1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula, e.g. penicillins, penems
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/485—Inorganic compounds
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/4858—Organic compounds
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
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Abstract
The present invention provides a kind of Biomox and its production method and applications.Raw material granularity range is controlled using dry granulation, in the case where not using disintegrating agent, improves the dissolution rate of capsule by adjusting the dosage of magnesium stearate, reaches product purpose similar to the former dissolved corrosion of triturate.Under the premise of meeting drug quality requirement, the present invention is simpler compared with prior art, and the volume of capsule is reduced, and the compliance of clinical use is improved.
Description
Technical field
The invention belongs to pharmaceutical technology field, it is related to a kind of Biomox and its production method and application.
Background technique
Utimox is semi-synthetic penicillins wide spectrum beta-lactam antibiotic, its chemical name is
(2S, 5R, 6R) -3,3- dimethyl -6- [(R)-(-) -2- amino -2- (4- hydroxy phenyl) acetylamino] -7- oxo -4- sulphur
Miscellaneous -1- azabicyclo [3.2.0] heptane -2- formic acid trihydrate, molecular formula C16H19N3O5S·3H2O, molecular weight are
419.46.Utimox character is off-white color or white crystals sprills, and mildly bitter flavor does not dissolve in ethyl alcohol, is slightly soluble in
Water, specific rotation is within the scope of+290 °~+315 °, chemical structural formula are as follows:
Amoxicillin oral absorption is rapid, and about 75%~90% is absorbed by gastrointestinal tract, and is not influenced by food.It can press down
The synthesis of bacteria cell wall processed makes bacterium quickly become spherical and broken dissolution.Clinically it is used for respiratory tract infection, alimentary canal sense
Dye, urethral infection and Skin and soft tissue infection etc., are the anti-infective medications in basis being most widely used, and country has been arranged
Enter medical insurance catalogue Class A drug.
There are many oral Wymoxes, such as a variety of doses of capsule, tablet, dispersible tablet, granule, dry suspensoid agent
Type, wherein amoxil capsule accounts for 70% or more share.In current amoxil capsule production technology, have through Ah not
It refills after the granulation of XiLin calomel mercurous chloride, also has using micronization technology and to prepare.
Granulation mode includes wet granulation and dry granulation.Although wet granulation can also obtain preferable as a result, still wet
Legal system grain is needed using solvent, and to pass through high-temperature drying step, and Amoxicillin is unstable to high temperature and humidity, easily generation molecule
Between polymerization form the macromolecule impurity of high sensitization, which is unfavorable for improving the stability of preparation.Though dry granulation avoids
High temperature and humidity step, technique simplifies, but there is a problem of that dissolution rate is low, uses disintegrating agent to promote dissolution, and can make more
Plastic capsule volume is excessive, while the addition of disintegrating agent also results in individual difference phenomenon when capsule is disintegrated, Control of Impurities aspect
Also it is not improved.
In addition to process above, the relevant report of micronization technology is also related to.The technique is not avoided that using filler, collapses
Solve agent and wet granulation step.In addition, obtaining fine powder if passing through and being micronized, then piece is obtained by dry granulation with remaining auxiliary material
Shape drug, finally by the broken sieving of concussion to obtain filling particle, although high temperature and humidity step is avoided that, to dissolution rate
Improve, but not improve preparation stability, instead due to micronization make surface area increase and increase with outside
The probability of boundary's contact with moisture keeps impurity more easily generated.
Therefore, the prior art is still to be improved and improves.
Summary of the invention
Therefore, the purpose of the present invention is to overcome the defects in the prior art, provide a kind of Biomox and its
Production method.
To achieve the above object, the first aspect of the present invention provides a kind of Biomox, the Amoxicillin
Capsule is free of disintegrating agent, is only made of Amoxicillin raw medicine and lubricant of dry granulation, wherein the Amoxicillin is former
The mass fraction of medicine and lubricant proportion is 100:0.1~5, preferably 100:0.3~3.5, more preferably 100:0.8~1.
The Biomox according to a first aspect of the present invention, wherein the lubricant is selected from following one kind
It is or a variety of: magnesium stearate, silica and talcum powder；Preferably, the lubricant is magnesium stearate.
The second aspect of the present invention provides the preparation method of Biomox described in first aspect, the preparation side
Method may comprise steps of:
(1) dry press is added in Amoxicillin to pelletize after pneumatic conveying drying, is sieved through pelletizing machine whole grain, spin vibration sieve,
Obtain Amoxicillin weight powder particles；
(2) lubricant is sieved for subsequent use；
(3) Amoxicillin weight powder particles and lubricant are weighed respectively by the proportion, mixing in mixing machine is added；
(4) step (3) mixed medicinal powder is packed into capsule shells with capsule filling machine；With
(5) plastic-aluminum.
Preparation method according to a second aspect of the present invention, wherein in the step (1), the dry press platen pressure is 6
~10Mpa, preferably 8~10MPa；The dry press revolving speed is 8~13 revs/min, preferably 8~10 revs/min；It is described whole
Grain machine revolving speed is 100~150 revs/min, preferably 120 revs/min；The spin vibration sieve is 10~30 meshes, preferably 20 mesh
Sieve.
In the step (1), the particle diameter distribution of the Amoxicillin weight powder particles are as follows: 20~30 mesh: 5%~30%, 20
~80 mesh: 60%~80%, less than 80 mesh: 20%~40%, less than 120 mesh: 5%~20%.
In the step (2), the lubricant crosses 60~100 meshes, preferably 80 meshes.
In the step (3), the incorporation time is 10~15 minutes, preferably 15 minutes；The mixing machine rotary frequency
Rate is 8~10 beats/min, preferably 10 beats/min.
The third aspect of the present invention provides a kind of oral amoxicillin preparation, and the Wymox includes according to
Biomox described in one side or the Biomox prepared according to second aspect the method.
The fourth aspect of the present invention provides the Biomox according to first aspect or according to second aspect
The Biomox of method preparation is preparing the application in the drug for treating infectious diseases.
Preferably, the infectious diseases is selected from one or more of: respiratory tract infection, alimentary canal infection, the urinary tract
Infection and Skin and soft tissue infection.
In view of the deficiencies in the prior art, the present invention provides a kind of Biomox and its production methods.The present invention
People controls raw material granularity range using dry granulation, without using disintegrating agents such as carboxyrnethyl starch sodium and crospovidone
In the case of, the dissolution rate of capsule is improved by adjusting the dosage of magnesium stearate, reaches the dissolved corrosion of product and former triturate
Similar purpose.Under the premise of meeting drug quality requirement, the present invention is simpler compared with prior art, and the volume of capsule is subtracted
It is small, improve the compliance of clinical use.
Biomox of the invention can have but be not limited to it is following the utility model has the advantages that
Under the premise of meeting drug quality requirement, the present invention is simpler compared with prior art, and the volume of capsule is subtracted
It is small, improve the compliance of clinical use.
Detailed description of the invention
Hereinafter, carrying out the embodiment that the present invention will be described in detail in conjunction with attached drawing, in which:
Fig. 1 shows the dissolution curve in 1 amoxil capsule pH4.0 acetate buffer of test example.
Fig. 2 shows the dissolution curves in 1 amoxil capsule pH6.8 phosphate buffer of test example.
Fig. 3 shows the dissolution curve in 1 amoxil capsule water of test example.
Specific embodiment
Present invention will be further explained by specific examples below, it should be understood, however, that, these embodiments are only
It is used, is but should not be understood as present invention is limited in any form for specifically describing in more detail.
This part carries out general description to the material and test method that arrive used in present invention test.Although being
It realizes many materials used in the object of the invention and operating method is it is known in the art that still the present invention still uses up herein
It may detailed description.It will be apparent to those skilled in the art that within a context, if not specified, material therefor of the present invention and behaviour
It is well known in the art as method.
Reagent and instrument used in the following embodiment are as follows:
1 main production equipments list of table
2 main agents sample list of table
| Title | Producer |
| Utimox | Federal pharmacy (Inner Mongol) Co., Ltd |
| Magnesium stearate | Anhui Shanhe Medicinal Subsidiary Material Co., Ltd. |
| Silica | Distributions in Liaocheng of Shandong Province A Hua Pharmacy stock Co., Ltd |
| Talcum powder | Guilin Gui Guang talcum development corporation, Ltd. |
| 1# hungry area softgel shell | Xinchang, Zhejiang Province Kangping capsule Co., Ltd |
| Amoxil capsule original triturate | GlaxoSmithKline PLC |
Embodiment 1
The present invention is achieved by the following technical solutions:
The prescription of amoxil capsule is in parts by mass are as follows:
The prescription of 3 amoxil capsule of table
Above-mentioned amoxil capsule production method is as follows:
(1) dry press is added in Utimox to pelletize after pneumatic conveying drying, is shaken through pelletizing machine whole grain, rotation
Sieve screening obtains Amoxicillin weight powder particles.The platen pressure of dry press is 8MPa, and pressure roller revolving speed is 10 revs/min, and pelletizing machine turns
Speed is 120 revs/min, and spin vibration sieve is 20 meshes.The particle diameter distribution of gained Amoxicillin weight powder particles are as follows: greater than 20 mesh: 0%,
20~30 mesh: 12%, 20~80 mesh: 70%, less than 80 mesh: 30%, less than 120 mesh: 10%.
(2) magnesium stearate is crossed into 80 meshes, it is spare.
(3) Amoxicillin weight powder particles and magnesium stearate are added in V-Mixer and are mixed 10~15 minutes, mixing machine rotation
Turn 10 beats/min of frequency.
(4) it fills: mixed particle is packed into hungry area softgel shell with capsule filling machine to obtain the final product.
(5) plastic-aluminum.
Embodiment 2
The prescription of amoxil capsule is in parts by mass are as follows:
The ingredient and content of 4 amoxil capsule of table
Follow the steps below production:
(1) dry press is added in Utimox to pelletize after pneumatic conveying drying, is shaken through pelletizing machine whole grain, rotation
Sieve screening obtains Amoxicillin weight powder particles.The platen pressure of dry press is 10MPa, and pressure roller revolving speed is 10 revs/min, pelletizing machine
Revolving speed is 120 revs/min, and spin vibration sieve is 20 meshes.The particle diameter distribution of gained Amoxicillin weight powder particles are as follows: be greater than 20 mesh:
0%, 20~30 mesh: 20%, 20~80 mesh: 78%, less than 80 mesh: 22%, less than 120 mesh: 5%.
(2) magnesium stearate is crossed into 80 meshes, it is spare.
(3) Amoxicillin weight powder particles and magnesium stearate are weighed by recipe quantity, mixing 15 minutes in V-Mixer are added,
Revolving speed is 10 revs/min.
(4) it fills: mixed particle is packed into 1 with capsule filling machine#Hungry area softgel shell to obtain the final product.
(5) plastic-aluminum.
Embodiment 3
The prescription of amoxil capsule is in parts by mass are as follows:
The ingredient and content of 5 amoxil capsule of table
Follow the steps below production:
(1) dry press is added in Utimox to pelletize after pneumatic conveying drying, is shaken through pelletizing machine whole grain, rotation
Sieve screening obtains Amoxicillin weight powder particles.The platen pressure of dry press is 8MPa, and pressure roller revolving speed is 10 revs/min, and pelletizing machine turns
Speed is 120 revs/min, and spin vibration sieve is 20 meshes.The particle diameter distribution of gained Amoxicillin weight powder particles are as follows: greater than 20 mesh: 0%,
20~30 mesh: 12%, 20~80 mesh: 70%, less than 80 mesh: 30%, less than 120 mesh: 10%.
(2) magnesium stearate is crossed into 80 meshes, it is spare.
(3) Amoxicillin weight powder particles and magnesium stearate are weighed by recipe quantity, mixing 15 minutes in V-Mixer are added,
Revolving speed is 10 revs/min.
(4) it fills: mixed particle is packed into 1 with capsule filling machine#Hungry area softgel shell to obtain the final product.
(5) plastic-aluminum.
Embodiment 4
The prescription of amoxil capsule is in parts by mass are as follows:
The ingredient and content of 6 amoxil capsule of table
Follow the steps below production:
(1) dry press is added in Utimox to pelletize after pneumatic conveying drying, is shaken through pelletizing machine whole grain, rotation
Sieve screening obtains Amoxicillin weight powder particles.The platen pressure of dry press is 12MPa, and pressure roller revolving speed is 8 revs/min, and pelletizing machine turns
Speed is 120 revs/min, and spin vibration sieve is 20 meshes.The particle diameter distribution of gained Amoxicillin weight powder particles are as follows: greater than 20 mesh: 0%,
20~30 mesh: 35%, 20~80 mesh: 85%, less than 80 mesh: 15%, less than 120 mesh: 3%.
(2) magnesium stearate is crossed into 80 meshes, it is spare.
(3) Amoxicillin weight powder particles and magnesium stearate are weighed by recipe quantity, mixing 15 minutes in V-Mixer are added,
Revolving speed is 10 revs/min.
(4) it fills: mixed particle is packed into 1 with capsule filling machine#Hungry area softgel shell to obtain the final product.
(5) plastic-aluminum.
Embodiment 5
The prescription of amoxil capsule is in parts by mass are as follows:
The ingredient and content of 7 amoxil capsule of table
Follow the steps below production:
(1) dry press is added in Utimox to pelletize after pneumatic conveying drying, is shaken through pelletizing machine whole grain, rotation
Sieve screening obtains Amoxicillin weight powder particles.The platen pressure of dry press is 8MPa, and pressure roller revolving speed is 10 revs/min, and pelletizing machine turns
Speed is 120 revs/min, and spin vibration sieve is 20 meshes.The particle diameter distribution of gained Amoxicillin weight powder particles are as follows: greater than 20 mesh: 0%,
20~30 mesh: 20%, 20~80 mesh: 70%, less than 80 mesh: 30%, less than 120 mesh: 10%.
(2) magnesium stearate is crossed into 80 meshes, it is spare.
(3) Amoxicillin weight powder particles and magnesium stearate are weighed by recipe quantity, mixing 15 minutes in V-Mixer are added,
Revolving speed is 10 revs/min.
(4) it fills: mixed particle is packed into 1 with capsule filling machine#Hungry area softgel shell to obtain the final product.
(5) plastic-aluminum.
Embodiment 6
The prescription of amoxil capsule is in parts by mass are as follows:
The ingredient and content of 8 amoxil capsule of table
Follow the steps below production:
(1) dry press is added in Utimox to pelletize after pneumatic conveying drying, is shaken through pelletizing machine whole grain, rotation
Sieve screening obtains Amoxicillin weight powder particles.The platen pressure of dry press is 9MPa, and pressure roller revolving speed is 9 revs/min, and pelletizing machine turns
Speed is 100 revs/min, and spin vibration sieve is 20 meshes.The particle diameter distribution of gained Amoxicillin weight powder particles are as follows: greater than 20 mesh: 0%,
20~30 mesh: 20%, 20~80 mesh: 78%, less than 80 mesh: 22%, less than 120 mesh: 5%.
(2) magnesium stearate is crossed into 80 meshes, it is spare.
(3) Amoxicillin weight powder particles and magnesium stearate are weighed by recipe quantity, mixing 15 minutes in V-Mixer are added,
Revolving speed is 10 revs/min.
(4) it fills: mixed particle is packed into 1 with capsule filling machine#Hungry area softgel shell to obtain the final product.
(5) plastic-aluminum.
Embodiment 7
The prescription of amoxil capsule is in parts by mass are as follows:
The ingredient and content of 9 amoxil capsule of table
Follow the steps below production:
(1) dry press is added in Utimox to pelletize after pneumatic conveying drying, is shaken through pelletizing machine whole grain, rotation
Sieve screening obtains Amoxicillin weight powder particles.The platen pressure of dry press is 10MPa, and pressure roller revolving speed is 8 revs/min, and pelletizing machine turns
Speed is 110 revs/min, and spin vibration sieve is 20 meshes.The particle diameter distribution of gained Amoxicillin weight powder particles are as follows: greater than 20 mesh: 0%,
20~30 mesh: 20%, 20~80 mesh: 78%, less than 80 mesh: 22%, less than 120 mesh: 5%.
(2) magnesium stearate is crossed into 80 meshes, it is spare.
(3) Amoxicillin weight powder particles and magnesium stearate are weighed by recipe quantity, mixing 15 minutes in V-Mixer are added,
Revolving speed is 10 revs/min.
(4) it fills: mixed particle is packed into 1 with capsule filling machine#Hungry area softgel shell to obtain the final product.
(5) plastic-aluminum.
Test example 1
Illustrate beneficial effects of the present invention below by experiment.For investigation gained amoxil capsule having clinically
Effect property, the present inventor carry out dissolution curve measurement according to Chinese Pharmacopoeia four 0,931 first methods of version in 2015 to Examples 1 to 7,
And pass through f with the data of former triturate2Value calculating compares.
Dissolution curve data in 10 amoxil capsule pH4.0 acetate buffer of table
Dissolution curve data in 11 amoxil capsule pH6.8 phosphate buffer of table
Dissolution curve data in 12 amoxil capsule water of table
As a result by embodiment 1-2 it is found that can be fitted in vitro with former triturate by amoxil capsule produced by the present invention,
Advantageous data are provided for interior curative effect Conformance Assessment.Comparative example 1, embodiment 2 and embodiment 4, it is known that A Moxi
The particle diameter distribution of woods weight powder particles has apparent influence to dissolution rate, also further affects the fitness with former triturate.It is right
Than embodiment 1, embodiment 3 and embodiment 5, it can be seen that the magnesium stearate of different proportion also has shadow to dissolution curve in prescription
It rings.Comparative example 2, embodiment 6 and embodiment 7, it can be seen that different types of lubricant also has dissolution curve in prescription
It influences.
The present inventor also carries out quality testing to Examples 1 to 2, in 40 ± 2 DEG C of high temperature, 75 ± 5% condition of relative humidity
Lower progress accelerated test 6 months detects the variation of every quality index, the results are shown in Table 9.
40 ± 2 DEG C of 13 high temperature of table, 75 ± 5% condition of relative humidity, 6 months test datas of accelerated test
By above data result it is recognised that amoxil capsule obtained, after accelerated test 6 months, although
Dissolution rate is declined, and moisture and impurity are increased slightly, but every quality index is met the quality standard, and illustrates the present invention
Obtained sample quality is fine.
Comparative example 1
The prescription of amoxil capsule is in parts by mass are as follows:
The ingredient and content of 14 amoxil capsule of table
Follow the steps below production:
(1) magnesium stearate is crossed into 80 meshes, it is spare.
(2) Utimox and magnesium stearate are weighed by recipe quantity, mixing 15 minutes in V-Mixer are added,
Revolving speed is 10 revs/min.
(3) mixed particle is added to dry press to pelletize after pneumatic conveying drying, is sieved through pelletizing machine whole grain, spin vibration sieve
Point, obtain Amoxicillin weight powder particles.The platen pressure of dry press is 8MPa, and pressure roller revolving speed is 10 revs/min, and pelletizing machine revolving speed is
120 revs/min, spin vibration sieve is 20 meshes.The particle diameter distribution of gained Amoxicillin weight powder particles are as follows: greater than 20 mesh: 0%, 20~
30 mesh: 15%, 20~80 mesh: 68%, less than 80 mesh: 32%, less than 120 mesh: 10%.
(4) it fills: the particle after granulation is packed into 1 with capsule filling machine#Hungry area softgel shell to obtain the final product.
(5) plastic-aluminum.
Comparative example 2
The prescription of amoxil capsule is in parts by mass are as follows:
The ingredient and content of 15 amoxil capsule of table
Follow the steps below production:
(1) magnesium stearate is crossed into 80 meshes, it is spare.
(2) Utimox and magnesium stearate are weighed by recipe quantity, mixing 15 minutes in V-Mixer are added,
Revolving speed is 10 revs/min.
(3) mixed particle is added to dry press to pelletize after pneumatic conveying drying, is sieved through pelletizing machine whole grain, spin vibration sieve
Point, obtain Amoxicillin weight powder particles.The platen pressure of dry press is 8MPa, and pressure roller revolving speed is 10 revs/min, and pelletizing machine revolving speed is
120 revs/min, spin vibration sieve is 30 meshes.The particle diameter distribution of gained Amoxicillin weight powder particles are as follows: greater than 20 mesh: 0%, 20~
30 mesh: 0%, 20~80 mesh: 62%, less than 80 mesh: 38%, less than 120 mesh: 18%.
(4) it fills: the particle after granulation is packed into 1 with capsule filling machine#Hungry area softgel shell to obtain the final product.
(5) plastic-aluminum.
Comparative example 3
The prescription of amoxil capsule is in parts by mass are as follows:
The ingredient and content of 16 amoxil capsule of table
Follow the steps below production:
(1) magnesium stearate is crossed into 80 meshes, it is spare.
(2) Utimox and magnesium stearate are weighed by recipe quantity, mixing 15 minutes in V-Mixer are added,
Revolving speed is 10 revs/min.
(3) mixed particle is added to dry press to pelletize after pneumatic conveying drying, is sieved through pelletizing machine whole grain, spin vibration sieve
Point, obtain Amoxicillin weight powder particles.The platen pressure of dry press is 14MPa, and pressure roller revolving speed is 8 revs/min, and pelletizing machine revolving speed is
90 revs/min, spin vibration sieve is 30 meshes.The particle diameter distribution of gained Amoxicillin weight powder particles are as follows: greater than 20 mesh: 0%, 20~30
Mesh: 0%, 30~80 mesh: 89%, less than 80 mesh: 11%, less than 120 mesh: 1.7%.
(4) it fills: the particle after granulation is packed into 1 with capsule filling machine#Hungry area softgel shell to obtain the final product.
(5) plastic-aluminum.
The comparison of 17 amoxil capsule embodiment and comparative example formulation and technology of table
18 amoxil capsule quality versus's result of table
| Performance assessment criteria | Embodiment 1 | Embodiment 3 | Comparative example 1 | Comparative example 2 | Comparative example 3 |
| Character | White particle | White particle | White particle | White particle | Yellowish coloured particles |
| Moisture (%) | 12.7 | 13.0 | 12.3 | 12.6 | 12.5 |
| Related substance (%) | 0.27 | 0.25 | 0.31 | 0.28 | 0.73 |
| Polymer (%) | 0.03 | 0.03 | 0.03 | 0.03 | 0.05 |
| Content (%) | 98.6 | 97.2 | 99.7 | 100.1 | 97.9 |
| Dissolution rate (%) | 95 | 85 | 89 | 98 | 82 |
Dissolution curve data in 19 amoxil capsule pH4.0 acetate buffer of table
Dissolution curve data in 20 amoxil capsule pH6.8 phosphate buffer of table
Dissolution curve data in 21 amoxil capsule water of table
By embodiment 3 and comparative example 1 it is found that influence of the interior application process of magnesium stearate to quality is little.To quality shadow
Ringing biggish is grain made parameter, by embodiment 3, comparative example 1 and comparative example 2 it is found that after spin vibration sieve sieve is replaced with 30 mesh,
The particle diameter distribution of gained particle is partially thin, although sample survey do not have from the indexs such as related substance, polymer, content, moisture it is bright
Significant difference is other, but dissolution rate is accelerated, thus causes to decline in dissolution curve with the similarity of reference preparation.Meanwhile replacement is more
After thin spin vibration sieve sieve, so that the loss of batch increases, the coarse granule in 30 meshes of processing is required consideration for how.In order into one
Step embodies particle diameter distribution to the importance of dissolved corrosion, and the present inventor's control is small less than 120 targeted fine powder accountings in comparative example 3
In 2.0%, its impacted dissolution rate obviously slows down, and is even more dissmilarity with reference preparation.Moreover, because granulation conditions are violent,
So that increased significantly in comparative example 3 in relation to substance and polymer, it is unfavorable for the stability of preparation.
Although present invention has been a degree of descriptions, it will be apparent that, do not departing from the spirit and scope of the present invention
Under the conditions of, the appropriate variation of each condition can be carried out.It is appreciated that the present invention is not limited to the embodiments, and it is attributed to right
It is required that range comprising the equivalent replacement of each factor.
Claims (10)
1. a kind of Biomox, which is characterized in that the Biomox is free of disintegrating agent, only by Amoxicillin
Raw medicine and lubricant are made of dry granulation, wherein the mass fraction of the Amoxicillin raw medicine and lubricant proportion is 100:
0.1~5, preferably 100:0.3~3.5, more preferably 100:0.8~1.
2. Biomox according to claim 1, which is characterized in that the lubricant is selected from following a kind of or more
Kind: magnesium stearate, silica and talcum powder；Preferably, the lubricant is magnesium stearate.
3. the preparation method of Biomox according to claim 1 or 2, which is characterized in that the preparation method
The following steps are included:
(1) dry press is added in Amoxicillin to pelletize after pneumatic conveying drying, is sieved through pelletizing machine whole grain, spin vibration sieve, obtains Ah
Amdinocillin weight powder particles；
(2) lubricant is sieved for subsequent use；
(3) Amoxicillin weight powder particles and lubricant are weighed respectively by the proportion, mixing in mixing machine is added；
(4) step (3) mixed medicinal powder is packed into capsule shells with capsule filling machine；
(5) plastic-aluminum.
4. according to the method described in claim 3, it is characterized in that, the dry press platen pressure is 6 in the step (1)
~10Mpa, preferably 8~10MPa；The dry press revolving speed is 8~13 revs/min, preferably 8~10 revs/min；It is described whole
Grain machine revolving speed is 100~150 revs/min, preferably 120 revs/min；The spin vibration sieve is 10~30 meshes, preferably 20 mesh
Sieve.
5. the method according to claim 3 or 4, which is characterized in that in the step (1), the Amoxicillin weight powder
The particle diameter distribution of grain are as follows: 20~30 mesh: 5%~30%, 20~80 mesh: 60%~80%, less than 80 mesh: 20%~40%, it is small
In 120 mesh: 5%~20%.
6. method according to any one of claim 3 to 5, which is characterized in that in the step (2), the lubricant
Cross 60~100 meshes, preferably 80 meshes.
7. method according to any one of claim 3 to 6, which is characterized in that in the step (3), when the mixing
Between be 10~15 minutes, preferably 15 minutes；The mixing machine speed is 8~10 beats/min, preferably 10 beats/min.
8. a kind of oral amoxicillin preparation, which is characterized in that the Wymox includes according to claim 1 or 2 institutes
The Biomox stated or the Biomox prepared according to any one of claim 3 to 7 method.
9. Biomox according to claim 1 or 2 is prepared according to any one of claim 3 to 7 method
Biomox preparing the application in drug for treating infectious diseases.
10. application according to claim 9, which is characterized in that the infectious diseases is selected from one or more of: exhaling
Inhale road infection, alimentary canal infection, urethral infection and Skin and soft tissue infection.
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