CN101708166B - Cefpodoxime proxetil submicron emulsion solid preparation and novel application thereof - Google Patents
Cefpodoxime proxetil submicron emulsion solid preparation and novel application thereof Download PDFInfo
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Abstract
The invention discloses a cefpodoxime proxetil submicron emulsion solid preparation and a novel application thereof, particularly a cefpodoxime proxetil solid preparation which is subjected to micro-emulsification and a novel application thereof. In the invention, the micro-emulsification technology is applied to process cefpodoxime proxetil raw materials so as to obtain a cefpodoxime proxetil submicron emulsion with excellent performance, the stability of the cefpodoxime proxetil is improved and the dissolution rate of the cefpodoxime proxetil preparation is obviously improved, so that the cefpodoxime proxetil submicron emulsion solid preparation has better bioavailability and can be used for preparing a medicament for treating osteomyelitis of jaws.
Description
Technical field
The present invention relates to a kind of Cefpodoxime proxetil submicron emulsion solid preparation and new application the thereof, be specifically related to the solid preparation and new application the thereof of the Cefpodoxime Proxetil of a kind of process microemulsified processing, belong to medical technical field.
Background technology
Osteomyelitis of jaws is a kind of disease that causes because of jawbone is infected, and the accumulative total scope often comprises periosteum, cortical bone and myeloid tissue, and common clinically have pyogenic osteomyelitis of jaws, infant osteomyelitis and a radiation osteomyelitis.That osteomyelitis of jaws can be divided into is suppurative, specificity, radioactivity are several.See so that suppurative osteomyelitis more clinically.The infection genesis of osteomyelitis of jaws mainly contains three kinds of approach, i.e. tooth source property, damaging and haematogenous.The haematogenous osteomyelitis of jaws is more rare, mainly betides children's.Odontogenic osteomyelitis of jaw is seen at most, accounts for 90% of osteomyelitis of jaws.It mainly is because the inflammation of jaws pathological changes that bacterial infection causes.Its pathology also should comprise the inflammation of whole osseous tissues such as the interior blood vessel of periosteum, compact bone and medullary cavity, nerve except that the inflammation of bone marrow, deal with improperly often to cause jawbone necrosis, face deformity and dysfunction.China is owing to the improvement of medical condition, and sickness rate greatly descends, but in the particularly economic under-developed area relatively of basic unit, osteomyelitis of jaws is still one of commonly encountered diseases.
Cefpodoxime Proxetil, its chemical name is: (6R, 7R)-7-[2-(2-amino-4-thiazolyl)-(Z)-2-(methoxyimino)-acetylamino]-the different third oxygen carbonyl oxygen ethyl ester of 3-methoxyl methyl-8-oxo-5-thia-1-azabicyclo-[4.2.0] oct-2-ene-2-carboxylic acid, molecular formula: C
21H
27N
5O
9S
2, molecular weight: 557.61, structural formula is:
Cefpodoxime Proxetil is the prodrug of cefpodoxime, and oral back is produced the cefpodoxime of tool antibacterial activity by intestinal absorption through the intestinal wall esterase hydrolyzed.The antibacterial action of cefpodoxime is by suppressing the film circle transpeptidase of bacterial cell wall system; the turntable effect that forms cross-join can not be carried out, and bacteria cell wall mucopeptide biosynthesis block causes cell wall defective; bacterial cell is to protect barrier, makes the cellular swelling, is out of shape, breaks and death.Cefpodoxime has good stable to beta-lactamase, thereby all effective to the bacterial strain of many anti-ampicillin or anti-amoxicillin.Extracorporeal bacteria inhibitor test shows, cefpodoxime is effective to gram negative bacteria aerobe, gram positive bacteria aerobe, anaerobe, can be used for treating the respiratory system infection due to the sensitive organism, and the urethra system infects and skin soft-tissue infection etc.
In fact, the therapeutic effect of any medicine depends on the design to its pharmaceutical preparation to a great extent.But important target provides the form of cephalosporin compound of the pro ore medicine of high bioavailability, reaches maximization so that this antibiotic enters the absorption of blood, and the antibiotic amount in the intestines and stomach of being retained in reaches and minimizes.Because Cefpodoxime Proxetil is highly hydrophobic medicine, it has the trend that forms gel in water-bearing media, thereby causes slow dissolution and therefore cause poor bioavailability.Thereby therefore need the compounding pharmaceutical compositions to form the defective improvement dissolution of gel to prevent the molecule bridging.At present, the listing preparation of Cefpodoxime Proxetil has tablet, capsule, granule, dispersible tablet, dry suspension, slow releasing tablet and slow releasing capsule, its poor stability, and the problem that dissolution is low can not get effective solution always.
Patent documentation CN1981765A discloses pharmaceutical composition of a kind of Cefpodoxime Proxetil and cyclodextrin and preparation method thereof, patent documentation CN101264087A discloses equally and has contained cefpodoxime proxetil cyclodextrin inclusion compound and preparation method thereof, all be Cefpodoxime Proxetil to be carried out enclose by cyclodextrin and derivant thereof, make various dosage forms again, can solve the problem of Cefpodoxime Proxetil poor solubility, but clathrate process more complicated, and inclusion rate is lower, have only about 50%, cause supplementary product consumption excessive, increased production cost.
Patent documentation CN101278914A discloses a kind of Cefpodoxime proxetil suspension composition and preparation method thereof, comprise the Cefpodoxime Proxetil of 100 weight portions, glycerol Yu acid esters and other excipient of 25-500 weight portion, this patent exists long-term shelf-stability poor, the problem that dissolution is low, the prescription that can not satisfy the prescriptive period.
Patent documentation CN1505515A discloses a kind of stabilizing pharmaceutical composition that relates to the Cefpodoxime Proxetil of pro ore medicine, but its release characteristics depends on specific technology and obtains the Cefpodoxime Proxetil of particular state, its technological requirement is higher, repeatability is not good, and those skilled in the art are difficult to implement its technical scheme.
Therefore, still existing further needs, to provide stripping property better oral cefpodoxime ester formulation.The inventor is through long-term conscientious research, beat all discovery, using micro-emulsion technology handles the Cefpodoxime Proxetil raw material, can improve the stability of Cefpodoxime Proxetil greatly, but also significantly improved the dissolution of preparation, and can be used for preparation treatment osteomyelitis of jaws medicine, finished the present invention thus.
Summary of the invention
The object of the present invention is to provide a kind of Cefpodoxime proxetil submicron emulsion solid preparation and new application the thereof, more specifically, the solid preparation and new application the thereof of the Cefpodoxime Proxetil of handling through microemulsified are provided, the Cefpodoxime Proxetil solid preparation poor stability of present listing, the problem that dissolution is low have been solved well, and provide and can be used for preparation treatment osteomyelitis of jaws medicine, obtained gratifying technique effect.
Bound by theory not, the inventor is through a large amount of formulation optimization designs, after various supplementary materials are screened, found unexpectedly Cefpodoxime Proxetil and cholesterol, Tween 80 and three kinds of materials of sodium deoxycholate are made up, have beyond thought effect, thereby obtained the Cefpodoxime Proxetil submicron emulsion granule of function admirable.Its possible mechanism is physical chemistry attribute and the biopharmacology characteristic that has changed cefpodoxime, has therefore improved dissolution rate, thereby has had bioavailability preferably.
The technical scheme that the present invention solves is as follows:
The invention provides a kind of Cefpodoxime Proxetil submicron emulsion granule, it is made up of by following parts by weight Cefpodoxime Proxetil, cholesterol, Tween 80 and sodium deoxycholate:
1 part of Cefpodoxime Proxetil
Cholesterol 1.8-12 part
Tween 80 0.5-10 part
Sodium deoxycholate 0.2-8 part.
As preferably, the parts by weight of each component of Cefpodoxime Proxetil submicron emulsion granule of the present invention are:
1 part of Cefpodoxime Proxetil
Cholesterol 3.5-8 part
Tween 80 1.2-6 part
Sodium deoxycholate 0.5-4 part.
As preferably, the parts by weight of each component of Cefpodoxime Proxetil submicron emulsion granule of the present invention are:
1 part of Cefpodoxime Proxetil
5.2 parts in cholesterol
3.8 parts of Tween 80s
2.5 parts of sodium deoxycholates.
The present invention also provides a kind of preparation Cefpodoxime Proxetil submicron emulsion particulate method, comprise the steps: cholesterol, Tween 80 and sodium deoxycholate are added in the water for injection, add the Cefpodoxime Proxetil mix homogeneously again, 70-90 ℃ of heating in water bath is stirred to molten condition, adopts tissue mincer's shear agitation, gets colostric fluid, again through high pressure dispersing emulsification machine circulating emulsion, emulsion, lyophilization or spray drying then obtain the submicron emulsion granule of Cefpodoxime Proxetil.
Cefpodoxime Proxetil submicron emulsion granule has galenic pharmacy character preferably, and good stability can not form gel, help drug release, it can be further used for making various dosage forms as the abortion product, for clinical use, so the technical scheme that the present invention solves also comprises:
A kind of Cefpodoxime proxetil submicron emulsion solid preparation, be made up of above-mentioned described Cefpodoxime Proxetil submicron emulsion granule and pharmaceutically acceptable other adjuvants, preferred described Cefpodoxime proxetil submicron emulsion solid preparation is granule, tablet, capsule, dispersible tablet or dry suspension.
Above-mentioned described solid preparation, wherein said adjuvant is not particularly limited, can be the pharmaceutical necessities of solid preparation commonly used in the pharmaceutics, specifically make: 1 part of Cefpodoxime Proxetil submicron emulsion granule, diluent 0.5-3 part by following component by weight, disintegrating agent 0.1-2 part, binding agent 0-0.6 part, correctives 0-20 part, aromatic 0-0.4 part, lubricant 0-0.5 part.
As preferably, wherein said diluent is selected from one or more in microcrystalline Cellulose, lactose, starch, pregelatinized Starch, sorbitol, mannitol, dextrin, calcium sulfate, the calcium hydrogen phosphate; Described disintegrating agent is selected from one or more in carboxymethylstach sodium, low-substituted hydroxypropyl cellulose, polyvinylpolypyrrolidone, cross-linking sodium carboxymethyl cellulose, the dried starch; Described binding agent is selected from one or more in 30 POVIDONE K 30 BP/USP 30, hypromellose, starch slurry, sodium carboxymethyl cellulose, the syrup; Described correctives is selected from one or more in sucrose, Aspartane, saccharin sodium, the steviosin; Described aromatic is selected from one or more in Fructus Citri tangerinae XIANGFEN, Fructus Fragariae Ananssae XIANGFEN, chocolate XIANGFEN, Herba Menthae XIANGFEN, the milk XIANGFEN; Described lubricant is selected from one or more in magnesium stearate, Pulvis Talci, colloidality silicon dioxide, PEG6000, the sodium lauryl sulphate etc.
Further, the present invention also provides the preparation method of above-mentioned described Cefpodoxime proxetil submicron emulsion solid preparation, and it comprises the steps: (1) with the pulverizing of Cefpodoxime Proxetil submicron emulsion granule, and 80 mesh sieves are standby excessively; (2) diluent, disintegrating agent, correctives are pulverized, crossed 80 mesh sieves, mix, standby; (3) with above-mentioned supplementary material mix homogeneously, add binding agent, aromatic system soft material, the granulation of sieving, oven dry, the adding mix lubricant is even, granulate; (4) dried granules is carried out packing or tabletting, make Cefpodoxime proxetil submicron emulsion solid preparation.
The present invention also provides Cefpodoxime proxetil submicron emulsion solid preparation to be used for the treatment of application in the osteomyelitis of jaws in preparation.
The present invention makes Cefpodoxime Proxetil submicron emulsion granule by specific adjuvant and supplementary material proportioning thereof, Cefpodoxime Proxetil submicron emulsion granule provided by the invention and Cefpodoxime Proxetil solid preparation, and compared with prior art, major advantage is as follows:
(1) active component Cefpodoxime Proxetil application micro-emulsion technology is handled, and has improved stability, has increased dissolubility, has solved the low problem of dissolution;
(2) used emulsifying agent, co-emulsifier degradation in vivo, avirulence and the non-immunogenicity of micro-emulsion technology, and can improve the Drug therapy index, reduce drug toxicity and reduce drug side effect;
(3) production technology is simple, and cost is low, can industrial-scale production.
Description of drawings
Fig. 1 is the sample of embodiment of the invention 4-7 preparation and the stripping curve figure of the sample for preparing according to patent documentation CN101278914A, wherein serial 1-4 has represented the dissolution curve of embodiment 4-7 sample respectively, and series 5 has been represented the stripping curve according to the sample of CN101278914A preparation.
The specific embodiment
Further specify the present invention by the following examples, but should not be construed as limitation of the present invention.
The particulate preparation of embodiment 1 Cefpodoxime Proxetil submicron emulsion
260g cholesterol, 190g Tween 80 and 125g sodium deoxycholate are added in the 4000ml water for injection, add 50g Cefpodoxime Proxetil mix homogeneously again, 86 ℃ of heating in water bath are stirred to molten condition, adopt the shear agitation 10min of tissue mincer, rotating speed 14000r/min, get colostric fluid, again through high pressure dispersing emulsification machine circulating emulsion 4 times, emulsion, spray drying then, obtain the submicron emulsion granule 574g of Cefpodoxime Proxetil, yield 91.8%.
The particulate preparation of embodiment 2 Cefpodoxime Proxetil submicron emulsion
350g cholesterol, 120g Tween 80 and 50g sodium deoxycholate are added in the 3000ml water for injection, add 100g Cefpodoxime Proxetil mix homogeneously again, 90 ℃ of heating in water bath are stirred to molten condition, adopt the shear agitation 20min of tissue mincer, rotating speed 12000r/min, colostric fluid, again through high pressure dispersing emulsification machine circulating emulsion 5 times, emulsion, deep bid lyophilization then, pulverize, obtain the submicron emulsion granule 582g of Cefpodoxime Proxetil, yield 93.8%.
The particulate preparation of embodiment 3 Cefpodoxime Proxetil submicron emulsion
800g cholesterol, 600g Tween 80 and 400g sodium deoxycholate are added in the 1500ml water for injection, add 100g Cefpodoxime Proxetil mix homogeneously again, 75 ℃ of heating in water bath are stirred to molten condition, adopt the shear agitation 20min of tissue mincer, rotating speed 13000r/min, get colostric fluid, again through high pressure dispersing emulsification machine circulating emulsion 5 times, emulsion, spray drying then, obtain the submicron emulsion granule 1752g of Cefpodoxime Proxetil, yield 92.2%.
The preparation of embodiment 4 Cefpodoxime Proxetil sheets
63.8g Cefpodoxime Proxetil submicron emulsion granule, 44g starch, 30g lactose and 38g microcrystalline Cellulose, the 10g low-substituted hydroxypropyl cellulose of embodiment 2 preparations are crossed 80 mesh sieves respectively, and mix homogeneously adds 5% 30 POVIDONE K 30 BP/USP then
3070% alcoholic solution 50ml makes soft material, and 20 mesh sieves are granulated, 55 ℃ of oven dry, and 20 mesh sieve granulate add 1.5g magnesium stearate and 2g Pulvis Talci mix homogeneously again, and tabletting makes the Cefpodoxime Proxetil sheet.
The capsular preparation of embodiment 5 Cefpodoxime Proxetils
62.4g Cefpodoxime Proxetil submicron emulsion granule, 48g microcrystalline Cellulose and the 8g carboxymethylstach sodium of embodiment 1 preparation are crossed 80 mesh sieves respectively, and mix homogeneously adds 5% 30 POVIDONE K 30 BP/USP then
3080% alcoholic solution 30ml makes soft material, and 20 mesh sieves are granulated, 60 ℃ of oven dry, and 20 mesh sieve granulate add 0.5g Pulvis Talci and 1g colloidality silicon dioxide mix homogeneously again, and filled capsules makes the Cefpodoxime Proxetil capsule.
The preparation of embodiment 6 Cefpodoxime Proxetil dispersible tablets
64.1g Cefpodoxime Proxetil submicron emulsion granule, 55g pregelatinized Starch, 5g saccharin sodium, 30g microcrystalline Cellulose and the 11g polyvinylpolypyrrolidone of embodiment 2 preparations are crossed 80 mesh sieves respectively, mix homogeneously then, add 1% hypromellose, 60% alcoholic solution 30ml system soft material, 20 mesh sieves are granulated, 60 ℃ of oven dry, 20 mesh sieve granulate add 1.5g magnesium stearate mix homogeneously again, tabletting makes the Cefpodoxime Proxetil dispersible tablet.
The particulate preparation of embodiment 7 Cefpodoxime Proxetils
65.5g Cefpodoxime Proxetil submicron emulsion granule, 1200g sucrose, 120g lactose, 80g carboxymethylstach sodium, 25g chocolate XIANGFEN and the 30g Aspartane of embodiment 2 preparations are crossed 80 mesh sieves respectively, and mix homogeneously adds 10% 30 POVIDONE K 30 BP/USP then
3060% alcoholic solution 300ml makes soft material, and 20 mesh sieves are granulated, 60 ℃ of oven dry, and 20 mesh sieve granulate, packing makes the Cefpodoxime Proxetil granule.
The preparation of embodiment 8 Cefpodoxime proxetil suspensions
191g Cefpodoxime Proxetil submicron emulsion granule, 1100g sucrose, 250g sorbitol, 52g Fructus Fragariae Ananssae XIANGFEN, the 30g Pulvis Talci of embodiment 3 preparation are crossed 80 mesh sieves respectively, mix homogeneously then, packing makes Cefpodoxime proxetil suspension.
Test example 1 dissolution detects
Sample with preparing among the sample of embodiment of the invention 4-7 preparation and the patent documentation CN101278914A carries out the dissolution detection, result such as table 1.
Table 1 dissolution testing result
Draw stripping curve Fig. 1 according to above data, wherein serial 1-4 has represented the dissolution curve of embodiment 4-7 sample respectively, and series 5 has been represented the stripping curve of the sample for preparing among the CN101278914A.
Can be found out that by The above results the sample of embodiment preparation compares among the embodiment sample of the present invention's preparation and the patent documentation CN101278914A, dissolution is significantly improved, and has proved absolutely the superiority of the present invention aspect the raising dissolution.
Test example 2 study on the stability
With the sample of embodiment of the invention 4-8 and patent documentation CN101278914A preparation under 40 ℃ of high temperature, relative humidity 75% ± 5% condition 6 months, carry out accelerated test and investigate, the results are shown in Table 2;
Table 2 accelerated test result
By the above sample character of patent documentation CN101278914A embodiment preparation when quickening March, June that found that bigger variation takes place, related substance raises, and content and dissolution obviously reduce; And the every detection index of sample of embodiment of the invention 4-8 preparation does not all have obvious variation.Illustrated that the present invention is at the superiority that improves aspect stable.
Prepare before 3 clinical trials of test example
1, case selection
Patient's 158 examples, male's 89 examples, women's 69 examples.57 examples of being grown up, child's 101 examples, 14 months～54 years old age, be positioned at the person of mandibular ramus portion 6 examples, person's 56 examples that are positioned in the angle of mandible merely, angle of mandible+lower jaw member person 46 examples is positioned at mandibular bone body person 50 examples merely.Outpatient's 95 examples wherein, inpatient's 63 examples.The patient is odontogenic infection, pericoronitis of the wisdom tooth 96 examples, periapical periodontitis 62 examples.
2, Clinical symptoms and X line performance
Acute stage, is similar to all fascial space infections of jaw, and normal being difficult for differentiated, easily enter chronic phase as malpractice.Chronic phase, is based on topical manifestations.Swollen 90 examples in parotid gland masseteric muscle district, local inflammation lump 19 examples take place in this group.The facial pus fistula of jaw 71 examples.The X line: acute stage, do not have bone destruction more, sparse 55 examples of visible cortical bone of chronic phase, cortical bone 62 examples that make a variation.Local cortical bone thickens, increase in density 23 examples.Sequestrum forms 18 examples.
3, Therapeutic Method
The patient is divided into treatment group, matched group and listing sample group.58 examples are organized in treatment, matched group 49 examples, and listing sample group 51 examples, three groups of patient's sexes, age, course of disease differences do not have significance.The treatment group gives the Cefpodoxime Proxetil sheet 200mg (2) of the embodiment of the invention 4 preparations, 2 times on the one; Matched group gives cefoperazone for inj sulbactam sodium 3.0g, intravenous drip, 2 times/d; Listing sample group gives Cefpodoxime Proxetil sheet (Zhejiang Anglikang Pharmaceutical Co., Ltd.) 200mg (2), 2 times on the one.More than each the group be a course of treatment all with 10d.
4, efficacy assessment standard
Curative effect determinate standard is divided into recovery from illness, improvement, invalid 3 grades.Recovery from illness: whole body and local transference cure, the sinus tract healing, X-ray film confirms the sclerotin reparation, union of fracture, function of joint is replied; Take a turn for the better: whole body and local transference cure, sinus tract heals in the recent period, and X-ray film shows the reparation of disease bone parts; Invalid: only general doing well,improving, but sinus tract and X-ray film do not have obvious improvement.
Test example 4 clinical test results
General curative effect saw Table 3 when 1, three groups of treatments of therapeutic evaluation finished.
Three groups of clinical efficacies are through check, and treatment group and matched group comparison total effective rate are respectively 96.6% and 69.4%, and difference has significance (P＜0.05); The treatment group compares with listing sample group, and total effective rate is respectively 96.6% and 90.2%, and difference has significance.
Three groups of general curative effects of table 3 relatively
Annotate: compare with matched group:
★P＜0.05; Compare with the listing sample:
△P＜0.05.
2, untoward reaction
1 routine patient is organized in treatment had slight diarrhoea on the 2nd day in medication, and all the other have no adverse reaction; Listing sample group 2 routine patients have nauseating, and the epigastric discomfort sensation disappears after the drug withdrawal.
To sum up: Cefpodoxime proxetil submicron emulsion solid preparation of the present invention is at treatment osteomyelitis of jaws determined curative effect, and untoward reaction is few.Simultaneously the osteomyelitis of jaws early diagnosis, in time to remove focus significant to jawbone marginality osteomyelitis (co).
Claims (9)
1. Cefpodoxime proxetil submicron emulsion solid preparation is characterized in that forming Cefpodoxime Proxetil submicron emulsion granule by Cefpodoxime Proxetil, cholesterol, Tween 80 and sodium deoxycholate by following parts by weight:
1 part of Cefpodoxime Proxetil
Cholesterol 1.8-12 part
Tween 80 0 0.5-10 part
Sodium deoxycholate 0.2-8 part;
The preparation method of wherein said Cefpodoxime proxetil submicron emulsion solid preparation comprises the steps: cholesterol, Tween 80 and sodium deoxycholate are added in the water for injection, add the Cefpodoxime Proxetil mix homogeneously again, 70-90 ℃ of heating in water bath is stirred to molten condition, adopt tissue mincer's shear agitation, get colostric fluid,, get emulsion again through high pressure dispersing emulsification machine circulating emulsion, lyophilization or spray drying then obtain the submicron emulsion granule of Cefpodoxime Proxetil.
2. Cefpodoxime proxetil submicron emulsion solid preparation according to claim 1 is characterized in that each composition weight umber is:
1 part of Cefpodoxime Proxetil
Cholesterol 3.5-8 part
Tween 80 1.2-6 part
Sodium deoxycholate 0.5-4 part.
3. Cefpodoxime proxetil submicron emulsion solid preparation according to claim 1 is characterized in that each composition weight umber is:
1 part of Cefpodoxime Proxetil
5.2 parts in cholesterol
3.8 parts of Tween 80s
2.5 parts of sodium deoxycholates.
4. Cefpodoxime proxetil submicron emulsion solid preparation, it is characterized in that being made up of each described Cefpodoxime Proxetil submicron emulsion granule of claim 1-3 and pharmaceutically acceptable other adjuvants, described Cefpodoxime proxetil submicron emulsion solid preparation is granule, tablet, capsule or dry suspension.
5. Cefpodoxime proxetil submicron emulsion solid preparation according to claim 4, described Cefpodoxime proxetil submicron emulsion solid preparation are dispersible tablet.
6. according to each described Cefpodoxime proxetil submicron emulsion solid preparation of claim 4-5, it is characterized in that described solid preparation is to be made by following component by weight: 1 part of Cefpodoxime Proxetil submicron emulsion granule, diluent 0.5-3 part, disintegrating agent 0.1-2 part, binding agent 0-0.6 part, correctives 0-20 part, aromatic 0-0.4 part, lubricant 0-0.5 part.
7. Cefpodoxime proxetil submicron emulsion solid preparation according to claim 6 is characterized in that wherein said diluent is selected from one or more in microcrystalline Cellulose, lactose, starch, pregelatinized Starch, sorbitol, mannitol, dextrin, calcium sulfate, the calcium hydrogen phosphate; Described disintegrating agent is selected from one or more in carboxymethylstach sodium, low-substituted hydroxypropyl cellulose, polyvinylpolypyrrolidone, cross-linking sodium carboxymethyl cellulose, the dried starch; Described binding agent is selected from one or more in 30 POVIDONE K 30 BP/USP 30, hypromellose, starch slurry, sodium carboxymethyl cellulose, the syrup; Described correctives is selected from one or more in sucrose, Aspartane, saccharin sodium, the steviosin; Described aromatic is selected from one or more in Fructus Citri tangerinae XIANGFEN, Fructus Fragariae Ananssae XIANGFEN, chocolate XIANGFEN, Herba Menthae XIANGFEN, the milk XIANGFEN; And/or described lubricant is selected from magnesium stearate, Pulvis Talci, colloidality silicon dioxide, PEG6000, the sodium lauryl sulphate etc. one or more.
8. method for preparing each described Cefpodoxime proxetil submicron emulsion solid preparation of claim 4-7, it comprises the steps: that (1) pulverize Cefpodoxime Proxetil submicron emulsion granule, crosses 80 mesh sieves, and is standby; (2) diluent, disintegrating agent, correctives are pulverized, crossed 80 mesh sieves, mix, standby; (3) with above-mentioned supplementary material mix homogeneously, add binding agent, aromatic system soft material, the granulation of sieving, oven dry, the adding mix lubricant is even, granulate; (4) dried granules is carried out packing or tabletting, make Cefpodoxime proxetil submicron emulsion solid preparation.
9. be used for the treatment of application in the medicine of osteomyelitis of jaws according to each described Cefpodoxime proxetil submicron emulsion solid preparation of claim 4-7 in preparation.
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| CN102327217B (en) * | 2011-07-14 | 2012-11-21 | 海南美大制药有限公司 | Solid cefpodoxime proxetil liposome preparation |
| CN103479589B (en) * | 2013-09-22 | 2016-04-13 | 海南葫芦娃制药有限公司 | cefpodoxime proxetil dispersible tablet and preparation method thereof |
| CN103655486B (en) * | 2013-12-12 | 2015-08-12 | 人福医药集团股份公司 | Sirolimus microemulsion particles and its preparation method and application |
| CN107281261B (en) * | 2017-06-25 | 2021-05-07 | 上海耀大生物科技有限公司 | Easy-to-absorb oral ulcer patch and preparation method thereof |
| CN115813868B (en) * | 2022-12-06 | 2024-06-28 | 江西省保灵动物保健品有限公司 | High-dissolution cefpodoxime proxetil tablet and preparation method thereof |
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Non-Patent Citations (1)
| Title |
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| 赵丽珊,等.亚微乳作为静脉给药载体的研究进展.《医药导报》.2008,第27卷(第5期),560-561. * |
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