CN1813754A - Diprophylline dropping pill and its preparing method - Google Patents
Diprophylline dropping pill and its preparing method Download PDFInfo
- Publication number
- CN1813754A CN1813754A CN 200510061658 CN200510061658A CN1813754A CN 1813754 A CN1813754 A CN 1813754A CN 200510061658 CN200510061658 CN 200510061658 CN 200510061658 A CN200510061658 A CN 200510061658A CN 1813754 A CN1813754 A CN 1813754A
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- CN
- China
- Prior art keywords
- diprophylline
- drop pill
- pill
- substrate
- dropping pill
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- 229960002819 diprophylline Drugs 0.000 title claims abstract description 31
- KSCFJBIXMNOVSH-UHFFFAOYSA-N dyphylline Chemical compound O=C1N(C)C(=O)N(C)C2=C1N(CC(O)CO)C=N2 KSCFJBIXMNOVSH-UHFFFAOYSA-N 0.000 title claims abstract description 31
- 239000006187 pill Substances 0.000 title claims abstract description 30
- 238000000034 method Methods 0.000 title description 2
- 238000002360 preparation method Methods 0.000 claims abstract description 9
- 239000000758 substrate Substances 0.000 claims description 12
- 239000000203 mixture Substances 0.000 claims description 6
- 239000002826 coolant Substances 0.000 claims description 5
- 238000010438 heat treatment Methods 0.000 claims description 3
- 238000002844 melting Methods 0.000 claims description 3
- 230000008018 melting Effects 0.000 claims description 3
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 claims description 2
- RVGRUAULSDPKGF-UHFFFAOYSA-N Poloxamer Chemical compound C1CO1.CC1CO1 RVGRUAULSDPKGF-UHFFFAOYSA-N 0.000 claims description 2
- 229920002472 Starch Polymers 0.000 claims description 2
- 229940008099 dimethicone Drugs 0.000 claims description 2
- 239000004205 dimethyl polysiloxane Substances 0.000 claims description 2
- 235000013870 dimethyl polysiloxane Nutrition 0.000 claims description 2
- 238000001035 drying Methods 0.000 claims description 2
- 229960000502 poloxamer Drugs 0.000 claims description 2
- 229920001983 poloxamer Polymers 0.000 claims description 2
- 229920000435 poly(dimethylsiloxane) Polymers 0.000 claims description 2
- 239000011734 sodium Substances 0.000 claims description 2
- 229910052708 sodium Inorganic materials 0.000 claims description 2
- 239000008107 starch Substances 0.000 claims description 2
- 235000019698 starch Nutrition 0.000 claims description 2
- 238000003756 stirring Methods 0.000 claims description 2
- 235000021355 Stearic acid Nutrition 0.000 claims 1
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 claims 1
- 239000001768 carboxy methyl cellulose Substances 0.000 claims 1
- 125000002057 carboxymethyl group Chemical group [H]OC(=O)C([H])([H])[*] 0.000 claims 1
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 claims 1
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 claims 1
- 229920001223 polyethylene glycol Polymers 0.000 claims 1
- -1 polyoxyethylene monostearate Polymers 0.000 claims 1
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 claims 1
- 229920001027 sodium carboxymethylcellulose Polymers 0.000 claims 1
- RYYKJJJTJZKILX-UHFFFAOYSA-M sodium octadecanoate Chemical compound [Na+].CCCCCCCCCCCCCCCCCC([O-])=O RYYKJJJTJZKILX-UHFFFAOYSA-M 0.000 claims 1
- 239000008117 stearic acid Substances 0.000 claims 1
- 239000003814 drug Substances 0.000 abstract description 14
- 208000006673 asthma Diseases 0.000 abstract description 13
- 239000011159 matrix material Substances 0.000 abstract 1
- ZFXYFBGIUFBOJW-UHFFFAOYSA-N theophylline Chemical compound O=C1N(C)C(=O)N(C)C2=C1NC=N2 ZFXYFBGIUFBOJW-UHFFFAOYSA-N 0.000 description 10
- 238000004519 manufacturing process Methods 0.000 description 6
- 229960000278 theophylline Drugs 0.000 description 5
- 229940079593 drug Drugs 0.000 description 4
- 230000000694 effects Effects 0.000 description 4
- 238000004090 dissolution Methods 0.000 description 3
- 238000009472 formulation Methods 0.000 description 3
- 230000001088 anti-asthma Effects 0.000 description 2
- 201000010099 disease Diseases 0.000 description 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 2
- 239000000428 dust Substances 0.000 description 2
- 239000007788 liquid Substances 0.000 description 2
- SFLSHLFXELFNJZ-QMMMGPOBSA-N (-)-norepinephrine Chemical compound NC[C@H](O)C1=CC=C(O)C(O)=C1 SFLSHLFXELFNJZ-QMMMGPOBSA-N 0.000 description 1
- UCTWMZQNUQWSLP-VIFPVBQESA-N (R)-adrenaline Chemical compound CNC[C@H](O)C1=CC=C(O)C(O)=C1 UCTWMZQNUQWSLP-VIFPVBQESA-N 0.000 description 1
- 229930182837 (R)-adrenaline Natural products 0.000 description 1
- RZVAJINKPMORJF-UHFFFAOYSA-N Acetaminophen Chemical compound CC(=O)NC1=CC=C(O)C=C1 RZVAJINKPMORJF-UHFFFAOYSA-N 0.000 description 1
- GFFGJBXGBJISGV-UHFFFAOYSA-N Adenine Chemical compound NC1=NC=NC2=C1N=CN2 GFFGJBXGBJISGV-UHFFFAOYSA-N 0.000 description 1
- 229930024421 Adenine Natural products 0.000 description 1
- 206010011224 Cough Diseases 0.000 description 1
- 206010014561 Emphysema Diseases 0.000 description 1
- 102000004861 Phosphoric Diester Hydrolases Human genes 0.000 description 1
- 108090001050 Phosphoric Diester Hydrolases Proteins 0.000 description 1
- 206010037423 Pulmonary oedema Diseases 0.000 description 1
- 102000000033 Purinergic Receptors Human genes 0.000 description 1
- 108010080192 Purinergic Receptors Proteins 0.000 description 1
- 208000037656 Respiratory Sounds Diseases 0.000 description 1
- 208000018569 Respiratory Tract disease Diseases 0.000 description 1
- 206010047924 Wheezing Diseases 0.000 description 1
- 238000010521 absorption reaction Methods 0.000 description 1
- 229960000643 adenine Drugs 0.000 description 1
- 210000005091 airway smooth muscle Anatomy 0.000 description 1
- 229960003556 aminophylline Drugs 0.000 description 1
- PECIYKGSSMCNHN-UHFFFAOYSA-N aminophylline Chemical compound NCCN.O=C1N(C)C(=O)N(C)C2=NC=N[C]21.O=C1N(C)C(=O)N(C)C2=NC=N[C]21 PECIYKGSSMCNHN-UHFFFAOYSA-N 0.000 description 1
- 206010006451 bronchitis Diseases 0.000 description 1
- 230000001914 calming effect Effects 0.000 description 1
- 230000000747 cardiac effect Effects 0.000 description 1
- 230000008576 chronic process Effects 0.000 description 1
- 239000000084 colloidal system Substances 0.000 description 1
- 230000008602 contraction Effects 0.000 description 1
- 230000001934 delay Effects 0.000 description 1
- 230000000857 drug effect Effects 0.000 description 1
- 230000007613 environmental effect Effects 0.000 description 1
- 229960005139 epinephrine Drugs 0.000 description 1
- 230000005284 excitation Effects 0.000 description 1
- 238000002474 experimental method Methods 0.000 description 1
- 230000004927 fusion Effects 0.000 description 1
- 230000007062 hydrolysis Effects 0.000 description 1
- 238000006460 hydrolysis reaction Methods 0.000 description 1
- 208000030603 inherited susceptibility to asthma Diseases 0.000 description 1
- 238000011835 investigation Methods 0.000 description 1
- 239000000463 material Substances 0.000 description 1
- 230000004630 mental health Effects 0.000 description 1
- 239000004531 microgranule Substances 0.000 description 1
- 238000002156 mixing Methods 0.000 description 1
- 230000001537 neural effect Effects 0.000 description 1
- 229960002748 norepinephrine Drugs 0.000 description 1
- SFLSHLFXELFNJZ-UHFFFAOYSA-N norepinephrine Natural products NCC(O)C1=CC=C(O)C(O)=C1 SFLSHLFXELFNJZ-UHFFFAOYSA-N 0.000 description 1
- 230000000414 obstructive effect Effects 0.000 description 1
- 230000003647 oxidation Effects 0.000 description 1
- 238000007254 oxidation reaction Methods 0.000 description 1
- 229940093429 polyethylene glycol 6000 Drugs 0.000 description 1
- 208000005333 pulmonary edema Diseases 0.000 description 1
- 238000010791 quenching Methods 0.000 description 1
- 230000000171 quenching effect Effects 0.000 description 1
- 150000003254 radicals Chemical class 0.000 description 1
- 230000004202 respiratory function Effects 0.000 description 1
- 230000029058 respiratory gaseous exchange Effects 0.000 description 1
- 210000002345 respiratory system Anatomy 0.000 description 1
- 239000007962 solid dispersion Substances 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- 230000000213 tachycardiac effect Effects 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1
- 230000003442 weekly effect Effects 0.000 description 1
Landscapes
- Medicinal Preparation (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
The present invention discloses a diprophylline dripping pill preparation with the function of relieving asthma and its preparation process. It is made up by using diprophylline and dripping pill matrix through a certain preparation process. Its bioavailability is high and its medicine stability is good.
Description
Technical field
The invention belongs to the pharmaceutical technology field, particularly a kind of by diprophylline (Diprophylline) and the formulated diprophylline dropping pill of drop pill substrate.
Background technology
Asthma is a kind of common respiratory tract disease, also is frequently-occurring disease.There is the asthma patient more than 100,000,000 in the whole world, and China's asthma prevalence is near 1%, and number of patients is more than 10,000,000, and wherein half was fallen ill before 12 years old.Asthma is serious harm people physical and mental healths, weakens work capacity, reduces a kind of disease of quality of life, and is difficult to obtain radical cure.Show as uncomfortable in chest, the irritable cough and difficult of unexpected generation based on the breathing system with wheezing sound of expiration.Duration of seizure is changeable, can continue several weeks when serious, or is the chronic process of outbreak repeatedly.A investigation report shows that the situation of asthmatic patient is unsatisfactory, and the asthmatic patient up to 27% is once influence sleep at least weekly, and therefore the adult patients in 2003 22% delays work, and has 49% child patient to delay study.There is 33% patient to accept emergency treatment in hospital last year, wherein 15% patient so hospitalization.This has all brought worry for their life study, and it is very urgent therefore to treat asthma.
Diprophylline is a suppressing panting calming medicine, calls to be diprophylline, dihydroxypropyltheo-pylline.Chemistry is called 1,3-dimethyl-7-(2, the 3-dihydroxypropyl)-3,7-dihydro-1H-purine-2,6-diketone.Diprophylline has direct relaxation effect to airway smooth muscle, thinks in the past by suppressing phosphodiesterase, makes due to the interior cAMP content raising of cell.In recent years experiment thinks that the bronchiectatic activity of theophylline partly is because the result that endogenous epinephrine and norepinephrine discharge.In addition, theophylline is the purinoceptor blocker, can resist the contraction to respiratory tract such as adenine.Theophylline can strengthen the diaphram contractility, especially shrinks when unable more significantly at diaphram, therefore helps to improve respiratory function.The diprophylline antiasthmatic effect than theophylline slightly a little less than, the heart excitation only is 1/20～1/10 of an aminophylline, and is less to heart and neural influence, be applicable to especially companion tachycardic asthmatic patient.Be used for alleviations such as bronchial asthma, asthmatic bronchitis, the obstructive emphysema symptom of panting clinically, also be used for the asthma that cardiac pulmonary edema causes.Especially be applicable to the asthmatic patient that can not tolerate theophylline.
The diprophylline oral formulations is mainly tablet in the market.Because the conventional tablet fabricating technology has, and makes that this class oral formulations disintegration time is long, onset is slow, and bioavailability is lower, thereby influences giving full play to of drug effect.Diprophylline dropping pill bioavailability height of the present invention, disintegrate is molten looses soon, the dissolution height, steady quality, release fast, produce effects is easy to carry and use fast.Preparation process of the present invention is simple, and workshop does not have dust, uses supplementary product kind few, and production process is short, and cost is low.
Summary of the invention
The object of the invention provides a kind of diprophylline dropping pill and preparation technology thereof with antiasthmatic effect.
The invention is characterized in by diprophylline and drop pill substrate formulated.
The weight ratio of each composition is:
Diprophylline: drop pill substrate=1: 1～1: 10
The present invention can be achieved through the following technical solutions:
Get diprophylline, pulverize, sieve.Diprophylline mixes by weight 1: 1～1: 10 with drop pill substrate, and heating and melting stirs, and splashes in dimethicone or other drop pill coolant, separates drop pill, absorbs coolant, drying, promptly.
Utilize the drop pill of method preparation of the present invention, its main feature is:
1. the quick stripping of medicine, the dissolution height, rapid-action, the bioavailability height, side effect is little.Diprophylline dropping pill is to adopt solid dispersion technology, with mixing after medicine and the fusion of drop pill substrate, solidifies by system of dripping and quenching, makes medicine be molecule, colloid or microcrystalline state and is scattered in the substrate.Because the gross area of medicine increases, medicine disengages with crystallite or unformed microgranule, so medicine dissolution and absorption quickening, and bioavailability improves.
2. medicine stability is good.Dropping pill formulation by medicine and substrate heating and melting after, splash in the immiscible liquid coolant and make, reduce with the air contact area, be difficult for oxidation, substrate is non-water thing, is difficult for causing drug hydrolysis, stability of drug is increased, thereby guaranteed drug quality.
3. drop pill production technology, production equipment are simple, with short production cycle, the production efficiency height, and cost is low.
4. in the main production process of drop pill, used material all is to carry out under liquid state, has reduced dust pollution, helps labor protection and environmental protection, helps the GMP management.
The diprophylline dropping pill crude drug is a diprophylline.Chemistry is called 1,3-dimethyl-7-(2, the 3-dihydroxypropyl)-3,7-dihydro-1H-purine-2,6-diketone.
Molecular formula: C
10H
14N
4O
4
Molecular weight: 254.25
The specific embodiment
Further the present invention can be described by the following examples, but not limited by embodiment.
Embodiment: per 1000 diprophylline dropping pill supplementary material proportionings
| The embodiment sequence number | Diprophylline | Polyethylene glycol 6000 | Macrogol 4000 | Carboxymethyl starch sodium | Poloxamer |
| 1 | 5g | 25g | 2g | 5g | |
| 2 | 5g | 50g | |||
| 3 | 10g | 20g | 5g | ||
| 4 | 10g | 25 | 5g | ||
| 5 | 10g | 25g | 2g | 2g | |
| 6 | 10g | 20g | 2g |
Claims (3)
1. diprophylline dropping pill and preparation technology thereof is characterized in that by diprophylline (Diprophylline) and drop pill substrate formulated.The weight ratio of each composition is:
Diprophylline: drop pill substrate=1: 1～1: 10
2. diprophylline dropping pill according to claim 1, it is characterized in that described drop pill substrate is a kind of or several compatibilities in polyethylene glycols, carboxymethyl starch sodium, poloxamer, sodium carboxymethyl cellulose, stearic acid, sodium stearate, the polyoxyethylene monostearate, the content of each compatibility composition all is not equal to zero.
3. according to claim 1 described diprophylline dropping pill, it is characterized in that preparation method is as follows: get diprophylline, pulverize, sieve.Diprophylline mixes by weight 1: 1～1: 10 with drop pill substrate, and heating and melting stirs, and splashes in dimethicone or other drop pill coolant, separates drop pill, absorbs coolant, drying, promptly.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200510061658 CN1813754A (en) | 2005-11-22 | 2005-11-22 | Diprophylline dropping pill and its preparing method |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200510061658 CN1813754A (en) | 2005-11-22 | 2005-11-22 | Diprophylline dropping pill and its preparing method |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1813754A true CN1813754A (en) | 2006-08-09 |
Family
ID=36906186
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 200510061658 Pending CN1813754A (en) | 2005-11-22 | 2005-11-22 | Diprophylline dropping pill and its preparing method |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1813754A (en) |
-
2005
- 2005-11-22 CN CN 200510061658 patent/CN1813754A/en active Pending
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| DD01 | Delivery of document by public notice |
Addressee: Chen Qian Document name: Notification that Application Deemed to be Withdrawn |
|
| C02 | Deemed withdrawal of patent application after publication (patent law 2001) | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Open date: 20060809 |