CN102327229A - Pidotimod dry suspension - Google Patents
Pidotimod dry suspension Download PDFInfo
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- CN102327229A CN102327229A CN201110290215A CN201110290215A CN102327229A CN 102327229 A CN102327229 A CN 102327229A CN 201110290215 A CN201110290215 A CN 201110290215A CN 201110290215 A CN201110290215 A CN 201110290215A CN 102327229 A CN102327229 A CN 102327229A
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- pidotimod
- dry suspension
- aspartame
- trisodium citrate
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Abstract
The invention provides a Pidotimod dry suspension which is composed of Pidotimod and an adjuvant, wherein the adjuvant comprises a filling agent, a suspending aid and a flavoring agent. The dry suspension is characterized in that the flavoring agent is a mixture of strawberry essence, trisodium citrate, sodium chloride and aspartame. The dry suspension has the advantages that the specific flavoring agent is adopted, thus well solving the taste problem of the Pidotimod dry suspension, and unexpectedly promoting the effect taking speed and facilitating the stability of the Pidotimod dry suspension.
Description
Technical field
The present invention provides a kind of pidotimod preparation, specifically, relates to a kind of pidotimod dry suspension.Belong to field of pharmaceutical preparations.
Background technology
Pidotimod (pidotimod) is a kind of brand-new chemosynthesis immunopotentiating agent, and its similar is in dipeptides.Be applicable to the low disease of cellular immune function, can significantly improve immunity such as human respiratory.Pidotimod works through stimulating and regulating cell-mediated immunoreation, adaptable across cellular immune function low respiratory tract infection, ear, nose, larynx infection and urinary system infection, the gynecological infection of outbreak repeatedly.Can reduce the number of times of acute attack, shorten the course of disease, alleviate the degree of outbreak, antibiotic auxiliary treatment when also can be used as actute infection.
Oral and intramuscular injection has good bioavailability, can promote nonspecific immune reaction, can promote specific immune response again.Pidotimod can promote the activate the phagocytic capacity of macrophage and neutrophilic granulocyte, improves its chemotaxis; Activate natural killer cell; The former lymphopoiesis that causes of mitosis promoting, the helper T lymphocyte (CD that reduces when making immunologic hypofunction
4 +) and suppressor T lymphocyte (CD
8 +) ratio raise or recover normal; Through stimulating interleukin-2 and gamma interferon to promote cell immune response.
Animal experiment and clinical trial all show; Although pidotimod does not have directly antibiotic and antiviral activity, through can bring into play the curative effect that significant treatment antibacterial (Diplococcus pneumoniae, escherichia coli, bacillus pyocyaneus, Bacillus proteus etc.) and virus (influenza virus, herpes simplex virus, murine encephalomyocarditis virus and Mengo virus etc.) infect to the promotion of body's immunity.Pidotimod is heterogeneous wide spectrum immunopotentiating agent, and too many levels enhancing body anti-infectious immunity reacts effectively, significantly improves each item immune indexes of the low patient of immune level; Not only can be used for treating bacterial infection, also can be used to treat viral infection; Not only be used for prevention infection, also can be used for the control of actute infection outbreak, the more important thing is that the intractable repeated infection of treatment is evident in efficacy; Topmost immunodeficiency-the T cell subsets is unbalance and functions of neutrophils reduces can also effectively to correct infant, recovers and strengthen the ability of its removing virus and pathogenic bacterium, reduces the number of times of infection and recurrence; The pidotimod safety is good, and is easy to use, rapid-action, is a kind of immunomodulating promoter that good prospect is arranged.
Summary of the invention
For overcoming the single defective that is unfavorable for clinical practice of pidotimod preparation in the prior art, the present invention's design also provides a kind of pidotimod dry suspension.
Dry suspension mainly is to need suspended particles that suitable dispersion is arranged, and should be uniformly dispersed as far as possible, to reduce the sedimentation velocity of microgranule, makes suspensoid be in steady statue.Secondly also need product that mouthfeel is preferably arranged.And the mouthfeel of pidotimod is relatively poor, and solving its oral compliance also is technical barrier.
The present invention finds, through selecting specific correctives for use, not only can solve the sensory issues of pidotimod dry suspension well, and finds unexpectedly, also has rapid-actionly, helps the effect of the stability of pidotimod dry suspension.
Technical scheme of the present invention is following:
The present invention provides a kind of pidotimod dry suspension, is made up of pidotimod and adjuvant, and described adjuvant is filler, suspending agent and correctives, it is characterized in that described correctives is the mixture of strawberry essence, trisodium citrate, sodium chloride and aspartame.
Wherein, above-mentioned described pidotimod dry suspension is characterized in that in the described correctives, the weight ratio of trisodium citrate and sodium chloride is 1: 1～20: 1, is preferably 10: 1.
Wherein, above-mentioned described pidotimod dry suspension is characterized in that in the described correctives, the weight ratio of aspartame and strawberry essence is 1: 1～20: 1, is preferably 10: 1.
Wherein, above-mentioned described pidotimod dry suspension is characterized in that in the described correctives, the weight ratio of trisodium citrate and aspartame is 5: 1～50: 1, is preferably 25: 1.
Preferably, the above-mentioned described pidotimod dry suspension of the present invention, it is characterized in that in the described correctives trisodium citrate: sodium chloride: aspartame: the weight ratio of strawberry essence is preferably 250: 25: 10: 1.
Wherein, Above-mentioned described pidotimod dry suspension; It is characterized in that wherein said filler is selected from sucrose, lactose, mannitol, starch, xylitol, maltose alcohol, the starch milk saccharide complex one or more, is preferably the mixture of sucrose and mannitol.
Wherein, above-mentioned described pidotimod dry suspension is characterized in that wherein said suspending agent is selected from carbomer, tragakanta, sodium carboxymethyl cellulose, the sodium alginate one or more, is preferably carbomer.
As the embodiment of the invention, a kind of pidotimod dry suspension is provided, it processes 1000 bags by following component:
Wherein, above-mentioned described pidotimod dry suspension is characterized in that it being to process through following method: pidotimod, sucrose, mannitol, trisodium citrate, sodium chloride are crossed 80 mesh sieves respectively, take by weighing by recipe quantity; Mix homogeneously adds 50% ethanol system soft material, and 25 mesh sieves are granulated; 60 ℃ of dryings (moisture＜1.0%), 30 mesh sieve granulate add carbomer, strawberry essence, aspartame; Mix homogeneously, intermediate packing after each item quality inspection is qualified promptly gets.
Uncomfortable because of the pidotimod mouthfeel, for making things convenient for patient's medication, improve compliance thereby need add correctives these article are rectified flavor.Through multiple correctivess such as aspartame, cyclamate, strawberry essence, apple essence, trisodium citrate, sodium chloride are screened; The result finds; Mixed-powder with aspartame, strawberry essence, trisodium citrate and sodium chloride is better as correctives; The pidotimod dry suspension that not only makes has good taste, but also helps stability of formulation.
In the pidotimod dry suspension of the present invention, the not special restriction of diluent can be multiple adjuvant test such as sucrose, lactose, mannitol, starch, wherein, more preferably with sucrose and mannitol as diluent, also can make these article possess mouthfeel preferably.
In the pidotimod dry suspension of the present invention, suspending agent can be selected carbomer, tragakanta, sodium carboxymethyl cellulose, sodium alginate etc. for use, but more preferably uses the suspending agent of carbomer as the pidotimod dry suspension.According to embodiment 1 prescription and preparation technology, different suspending agents, the suspending effect of prepared pidotimod dry suspension all can reach the requirement of dry suspension, but carbomer is than other suspending agent suspending better effects if (seeing table 1).
Table 1 suspending agent result of the test (settling volume ratio)
Description of drawings
Average blood drug level-time graph the comparison diagram of pidotimod behind Fig. 1 20 experimenter's oral tests preparation and the reference preparation
The specific embodiment
Embodiment 1: the pidotimod dry suspension
One. prescription
Two. preparation technology
Pidotimod, sucrose, mannitol, trisodium citrate, sodium chloride are crossed 80 mesh sieves respectively, take by weighing mix homogeneously by recipe quantity; Add 50% ethanol system soft material, 25 mesh sieves are granulated, 60 ℃ of dryings (moisture＜1.0%); 30 mesh sieve granulate add carbomer, strawberry essence, aspartame, mix homogeneously; Intermediate packing after each item quality inspection is qualified promptly gets.
Comparative Examples 1:
(1) form and technology according to embodiment 1 prescription, inventory is 50 bags, respectively strawberry essence is replaced with apple essence (Comparative Examples 1A), flavoring banana essence (Comparative Examples 1B), flavoring orange essence (Comparative Examples 1C), and milk flavour (1D), all the other components are identical with consumption in the prescription.
(2) form and technology according to embodiment 1 prescription, inventory is 50 bags, does not wherein contain strawberry essence (Comparative Examples 1E), and all the other components are identical with consumption in the prescription.
(3) form and technology according to embodiment 1 prescription, wherein inventory is 50 bags, sodium chloride-containing (Comparative Examples 1F) not wherein, and all the other components are identical with consumption in the prescription.
(4) form and technology according to embodiment 1 prescription, wherein inventory is 50 bags, does not wherein contain aspartame (Comparative Examples 1G), and all the other components are identical with consumption in the prescription.
(5) form and technology according to embodiment 1 prescription, wherein inventory is 50 bags, does not wherein contain carbomer (Comparative Examples 1H), and all the other components are identical with consumption in the prescription.
(6) form and technology according to embodiment 1 prescription, inventory is 50 bags, and trisodium citrate is replaced sodium bicarbonate (Comparative Examples 1I), and all the other components are identical with consumption in the prescription.
(7) form and technology according to embodiment 1 prescription, inventory is 50 bags, and it is identical with consumption that aspartame is replaced with in cyclamate (Comparative Examples 1J) prescription all the other components.
Above comparative test result such as following table 2.
Table 2 comparative test result
| The prescription numbering | Mobile | The settling volume ratio | Face shaping | Mouthfeel | Dissolution % | Related substance % |
| Embodiment 1 | Good | 0.99 | White particle | Sour-sweet, mouthfeel is good | 99.3 | 0.45 |
| Comparative Examples 1A | Good | 0.98 | White particle | Sour-sweet, mouthfeel is general | 98.6 | 0.87 |
| Comparative Examples 1B | Good | 0.98 | White particle | Sour-sweet, mouthfeel is general | 96.8 | 0.92 |
| Comparative Examples 1C | Good | 0.97 | White particle | Sour-sweet, mouthfeel is general | 100.2 | 0.68 |
| Comparative Examples 1D | Good | 0.99 | White particle | Sour-sweet, mouthfeel is general | 97.7 | 1.23 |
| Comparative Examples 1E | Good | 0.99 | White particle | Sour-sweet, mouthfeel is poor | 98.4 | 0.52 |
| Comparative Examples 1F | Generally | 0.92 | White particle | Sour-sweet, mouthfeel is general | 98.9 | 0.66 |
| Comparative Examples 1G | Good | 0.98 | White particle | Acid, mouthfeel is very poor | 97.5 | 0.70 |
| Comparative Examples 1H | Generally | 0.86 | White particle | Sour-sweet, mouthfeel is relatively poor | 98.2 | 0.69 |
| Comparative Examples 1I | Generally | 0.78 | The off-white color granule | Sour-sweet, puckery | 95.3 | 0.83 |
| Comparative Examples 1J | Good | 0.98 | White particle | Sour-sweet, mouthfeel is general | 98.0 | 0.73 |
Pidotimod dry suspension of the present invention; Through selecting specific adjuvant and proportioning for use; Prepared pidotimod dry suspension not only has good settling volume ratio, flowability, dispersibility, reaches mouthfeel and dissolution, and prepared pidotimod dry suspension also has good stable property.And technology is simple, and cost of supplementary product is cheap to be easy to get, and is easy to suitability for industrialized production.
Influence factor test and result thereof: get the pidotimod dry suspension sample that embodiment 1 makes and carry out the factors influencing test; High temperature (60 ℃), high humidity (RH92.5%), high light (4500Lx) condition held 10 days, respectively at 5,10 days last sampling and measuring.
The result sees the following form 3.
Table 3 influence factor tests the investigation result
Result of the test shows that the prepared pidotimod dry suspension of the present invention is all stable to high temperature, high humidity, high light, and each item index does not have obvious change.
Accelerated stability test and result thereof: get pidotimod dry suspension sample that embodiment 1 makes and carry out accelerated stability and investigate test, in 40 ℃, the container of RH75%, place, measure respectively at 1,2,3,6 sampling at the end of month.
The result sees table 4.
Table 4 accelerated test result
Long-term stable experiment and result thereof: get pidotimod dry suspension sample that embodiment 1 makes and carry out long-time stability and investigate test, under 25 ℃, RH60% condition, measure respectively at 3,6,9,12,18,24 samplings at the end of month.
The result sees table 5.
Table 5 long-term test results
Accelerated test and long-term stable experiment result show that the prepared pidotimod dry suspension of the present invention each item index does not have obvious change, and preparation of the present invention meets good stability.
The test of pesticide effectiveness that the present invention produces
The test of human-body biological equivalence:
Experimenter's basic condition: 20 healthy male trial volunteers are divided into 2 groups at random, 10 every group.Do not obey any medicine in test the last fortnight.Unified light diet during being tried.
Trial drug:
Receive test preparation (T): the pidotimod dry suspension, specification: the 400mg/ bag prepares according to embodiment 1.
Reference preparation (R): the pidotimod sheet (trade name: Wan Shining), specification: the 400mg/ sheet, lot number: 080203, Taiyangshi (Tangshan) Pharm Ind Co., Ltd. produces.
Method of testing: adopt the method for designing of random packet, the test of binary cycle dual crossing, experimenter's overnight fasting is after at least 10 hours, with 2 bags of (400mg/ bag) pidotimod dry suspension with the 250ml warm water delivery service.(medicine accumulated dose 800mg) takes medicine and can drink water in back 2 hours, advances unified light diet in 4 hours.Before the administration and 0.13,0.25,0.50,0.75,1.0,1.5,2.0,2.5,3.0,4.0,6.0,9.0,12.0 hour 5ml (lucifuge) that respectively takes a blood sample after the administration; With anticoagulant heparin; Centrifugal 15 minutes of 3500rmp, separated plasma also is stored in-40 ℃ of refrigerators to be measured.Take medicine and take a blood sample by above-mentioned same program intersection after one week.
The result sees Fig. 1.
Result of the test: obviously visible from Fig. 1, pidotimod dry suspension of the present invention (T) was being taken medicine back 0.5 hour in, and the blood drug level of human body is more higher than pidotimod sheet (R), explains that chewable tablet of the present invention absorbs easily, has rapid-action characteristics.
Claims (9)
1. a pidotimod dry suspension is made up of pidotimod and adjuvant, and described adjuvant is filler, suspending agent and correctives, it is characterized in that described correctives is the mixture of strawberry essence, trisodium citrate, sodium chloride and aspartame.
2. pidotimod dry suspension according to claim 1 is characterized in that in the described correctives, the weight ratio of trisodium citrate and sodium chloride is 1: 1～20: 1, is preferably 10: 1.
3. according to the described pidotimod dry suspension of claim 1-2, it is characterized in that in the described correctives, the weight ratio of aspartame and strawberry essence is 1: 1～20: 1, is preferably 10: 1.
4. according to the described pidotimod dry suspension of claim 1-3, it is characterized in that in the described correctives, the weight ratio of trisodium citrate and aspartame is 5: 1～50: 1, is preferably 25: 1.
5. according to the described pidotimod dry suspension of claim 1-4, it is characterized in that in the described correctives trisodium citrate: sodium chloride: aspartame: the weight ratio of strawberry essence is preferably 250: 25: 10: 1.
6. according to the described pidotimod dry suspension of claim 1-5; It is characterized in that wherein said filler is selected from sucrose, lactose, mannitol, starch, xylitol, maltose alcohol, the starch milk saccharide complex one or more, is preferably the mixture of sucrose and mannitol.
7. according to the described pidotimod dry suspension of claim 1-6, it is characterized in that wherein said suspending agent is selected from carbomer, tragakanta, sodium carboxymethyl cellulose, the sodium alginate one or more, is preferably carbomer.
8. pidotimod dry suspension, it processes 1000 bags by following component:
9. pidotimod dry suspension according to claim 8 is characterized in that it being to process through following method: pidotimod, sucrose, mannitol, trisodium citrate, sodium chloride are crossed 80 mesh sieves respectively, take by weighing by recipe quantity; Mix homogeneously adds 50% ethanol system soft material, and 25 mesh sieves are granulated; 60 ℃ of dryings (moisture＜1.0%), 30 mesh sieve granulate add carbomer, strawberry essence, aspartame; Mix homogeneously, intermediate packing after each item quality inspection is qualified promptly gets.
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| CN201110290215.8A CN102327229B (en) | 2011-09-28 | 2011-09-28 | A kind of Pidotimod dry suspension |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN108653207A (en) * | 2018-06-25 | 2018-10-16 | 长沙市如虹医药科技股份有限公司 | A kind of Pidotimod dry suspension and preparation method thereof |
| CN109106687A (en) * | 2018-09-14 | 2019-01-01 | 广州大光制药有限公司 | A kind of Pidotimod dry suspension and preparation method thereof |
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| CN1526390A (en) * | 2003-03-03 | 2004-09-08 | 浙江仙琚制药股份有限公司 | Piduomode granule and its prepn |
| CN1813685A (en) * | 2005-12-09 | 2006-08-09 | 韩志强 | Couted particle for reinforcing pidotimod acid-base stability, and its production method and use |
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2011
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Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
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| CN1526390A (en) * | 2003-03-03 | 2004-09-08 | 浙江仙琚制药股份有限公司 | Piduomode granule and its prepn |
| CN1813685A (en) * | 2005-12-09 | 2006-08-09 | 韩志强 | Couted particle for reinforcing pidotimod acid-base stability, and its production method and use |
Non-Patent Citations (2)
| Title |
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| 董海军: "匹多莫德干混悬剂人体药动学及生物等效性研究", 《中国药房》, vol. 19, no. 35, 31 December 2008 (2008-12-31), pages 2750 - 2752 * |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN108653207A (en) * | 2018-06-25 | 2018-10-16 | 长沙市如虹医药科技股份有限公司 | A kind of Pidotimod dry suspension and preparation method thereof |
| CN109106687A (en) * | 2018-09-14 | 2019-01-01 | 广州大光制药有限公司 | A kind of Pidotimod dry suspension and preparation method thereof |
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| CN102327229B (en) | 2016-06-22 |
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