CN1759827A - Recipe of drop pills of diisopropylamine dichloroacetate, and preparation method - Google Patents
Recipe of drop pills of diisopropylamine dichloroacetate, and preparation method Download PDFInfo
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- CN1759827A CN1759827A CN 200410155350 CN200410155350A CN1759827A CN 1759827 A CN1759827 A CN 1759827A CN 200410155350 CN200410155350 CN 200410155350 CN 200410155350 A CN200410155350 A CN 200410155350A CN 1759827 A CN1759827 A CN 1759827A
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- diisopropylamine dichloroacetate
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- drop pills
- medicine
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- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
A dripping pill 'Ganle' is prepared from diisopropylamine bichlorate and proper matrix. Its advantages are high curative effect and liver protecting effect, quickly taking its effect and low cost.
Description
Technical field
The present invention relates to a kind of prescription and manufacture method of hepatinica, specifically with " diisopropylamine dichloroacetate " be the dropping pill formulation and the technology manufacture method thereof of main component.
Background technology
Diisopropylamine dichloroacetate Diiopropylammonium Dichloroace-tas, another name: DADA, chemical name: diisopropylamine dichloroacetate, molecular formula and molecular weight: C
8H
17Cl
2NO
2=230.00, be used for the liver malfunction that acute and chronic hepatitis, fatty liver, early stage liver cirrhosis and other disease cause.Curative effect is conclusive aspect hepatoprotective, drop pills of diisopropylamine dichloroacetate is a kind of pill that utilizes the solid dispersion technology system of dripping to form, utilize water-solubility carrier to improve the dissolubility and the dissolution rate of medicine, improve the infiltration rate and the absorbtivity of medicine, thereby raising bioavailability, improve the curative effect of medicine, significant advantage is arranged than other dosage form.
Summary of the invention
The object of the present invention is to provide a kind of taking convenience, newtype drug evident in efficacy.
Solution of the present invention is: adopt solid dispersion technology, produce little, quick-acting, the pharmaceutical dosage form efficiently of dosage.
Drop pill is the product of solid dispersion technology, is characterized in: adopt fusion method to make medicine be scattered in the physiology inertia with molecularity and in the carrier soluble in water, form disperse system.(3～4um) is also little, thereby improved surface area greatly, and its bioavailability is much higher than the medicine of general dosage form than micronized particles for drug particle (0.001-0.1um).After entering the intestines and stomach, water-solubility carrier dissolves rapidly, because particle is little, the solid dispersion dissolution velocity is fast, can be absorbed by cell rapidly to enter blood circulation, thereby reach efficient and quick-acting effects.
Medicine of the present invention is formed (consumption is a weight portion) by following component:
5～50 parts of diisopropylamine dichloroacetate
20～100 parts of substrate
The ratio range of the component preferred weight of medicine of the present invention is:
15～40 parts of diisopropylamine dichloroacetate
30～60 parts of substrate
The optimum weight proportioning of medicine of the present invention is:
10 parts of diisopropylamine dichloroacetate
40 parts of substrate
The method of said components being made medicine of the present invention is:
Choose raw material by national standard;
Choose substrate by national standard.
Medicine and molten matrix are uniformly dispersed, are no more than 1um, join then in the molten matrix, wait to stir, join in the fluid reservoir then through high speed shear ultra micro emulsifying to particle diameter.
The cooling column height is not less than 50cm, and its temperature is about 10 ℃; With the water dropper valve open of fluid reservoir, and suitably regulate vacuum equipment.Water dropper apart from the coolant fluid identity distance from being not more than 50cm.Adjust the size of vacuum and valve, drop is splashed in the coolant by preset frequency, medicine drips slowly and sinks, and relies on the tension force of self to be shrunk to ball gradually.After becoming ball, clean surperficial silicone oil or liquid paraffin, drying at room temperature and finished product.
Illustrate:
(1) important feature of the present invention is that medicine and carrier are uniformly dispersed, and makes drug absorption quick, and drug effect is multiplied.
(2) another important feature of the present invention is the high speed shear ultra micro emulsification technology by uniqueness, makes the abundant fusion of effective ingredient.
Medicine of the present invention is taked the recipe quantity of 6 kinds of different proportions, and through dissolve scattered time limit test, its result shows: dissolve scattered time limit has by a relatively large margin raising, bioavailability of medicament the best of the present invention as can be known in view of the above than other dosage form.
Dissolve scattered time limit: check according to inspection technique disintegration (two appendix XA of Chinese Pharmacopoeia version in 2000):
| Numbering | Dissolve scattered time limit (min) |
| Example 1 | 10 |
| Example 2 | 7 |
| Example 3 | 8 |
| Example 4 | 8 |
| Example 5 | 10 |
| Example 6 | 9 |
The specific embodiment
Embodiment (1000, every 50mg)
Diisopropylamine dichloroacetate: 10 parts
Polyethylene Glycol: 40 parts
Make 1000 altogether, every heavy 50mg
Preparation method: join in the molten matrix system of dripping in 85 ℃ of heat-preservation cylinders by medicine.With coolant cools to the 10 ℃ system of dripping, water dropper to the distance of coolant liquid level is 10cm, and medicinal liquid is splashed in the coolant according to certain frequency in cooling column, and messenger drug drips slowly and sinks, and relies on self tension force to be shrunk to ball gradually.After becoming ball, clean the coolant on surface, drying at room temperature or blowing and finished product.
Claims (8)
1. the prescription of drop pills of diisopropylamine dichloroacetate is characterized in that its effective ingredient is made up of following components in weight percentage:
5～50 parts of diisopropylamine dichloroacetate
20～100 parts of substrate
Wherein said diisopropylamine dichloroacetate Diiopropylammonium Dichloroace-tas, another name: DADA, chemistry diisopropylamine dichloroacetate by name, its molecular formula: C8H17Cl2NO2.
2. drop pills of diisopropylamine dichloroacetate prescription according to claim 1 is characterized in that wherein the weight proportion of each component is:
15～40 parts of diisopropylamine dichloroacetate
30～60 parts of substrate
3. the prescription of drop pills of diisopropylamine dichloroacetate according to claim 1 is characterized in that wherein the weight proportion of each component is:
10 parts of diisopropylamine dichloroacetate
40 parts of substrate
4. according to claim 1,2 or 3 described drop pills of diisopropylamine dichloroacetate, it is characterized in that described medicament is a drop pill.
5. method of making the described drop pills of diisopropylamine dichloroacetate of claim 4 is characterized in that:
Choose raw material by standard;
Choose substrate by national standard;
Any one describedly is heated to 85 ℃ of fusings with substrate by claim 1-3 with said medicine, then medicine is joined substrate high speed emulsification pretreatment.Fluid reservoir insulation is injected then and is dripped the system tube at 85 ℃, adjusts pressure and vacuum equipment, splashes at regular time and quantity in 5～15 ℃ the coolant, under capillary effect, is shrunk to ball naturally, clean dry after promptly.
6. the manufacture method of drop pills of diisopropylamine dichloroacetate according to claim 5 is characterized in that:
Medicine added in 85 ℃ of molten matrix of temperature stir.
7. substrate according to claim 5 includes but not limited to Polyethylene Glycol 12000, polyethylene glycol 6000, Macrogol 4000, polyethylene glycol 1500, cetomacrogol 1000, Macrogol 600, PEG400 etc.
8. coolant according to claim 5 includes but not limited to dimethicone, liquid paraffin plant wet goods.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200410155350 CN1759827A (en) | 2004-10-15 | 2004-10-15 | Recipe of drop pills of diisopropylamine dichloroacetate, and preparation method |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200410155350 CN1759827A (en) | 2004-10-15 | 2004-10-15 | Recipe of drop pills of diisopropylamine dichloroacetate, and preparation method |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1759827A true CN1759827A (en) | 2006-04-19 |
Family
ID=36706135
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 200410155350 Pending CN1759827A (en) | 2004-10-15 | 2004-10-15 | Recipe of drop pills of diisopropylamine dichloroacetate, and preparation method |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1759827A (en) |
-
2004
- 2004-10-15 CN CN 200410155350 patent/CN1759827A/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 | ||
| C02 | Deemed withdrawal of patent application after publication (patent law 2001) | ||
| WD01 | Invention patent application deemed withdrawn after publication |