CN104352556A - Radix sophorae flavescentis total alkaloids dropping pill - Google Patents
Radix sophorae flavescentis total alkaloids dropping pill Download PDFInfo
- Publication number
- CN104352556A CN104352556A CN201410652950.2A CN201410652950A CN104352556A CN 104352556 A CN104352556 A CN 104352556A CN 201410652950 A CN201410652950 A CN 201410652950A CN 104352556 A CN104352556 A CN 104352556A
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- Prior art keywords
- radix sophorae
- sophorae flavescentis
- total alkaloids
- flavescentis total
- clathrate
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
- A61K36/18—Magnoliophyta (angiosperms)
- A61K36/185—Magnoliopsida (dicotyledons)
- A61K36/48—Fabaceae or Leguminosae (Pea or Legume family); Caesalpiniaceae; Mimosaceae; Papilionaceae
- A61K36/489—Sophora, e.g. necklacepod or mamani
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/69—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit
- A61K47/6949—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit inclusion complexes, e.g. clathrates, cavitates or fullerenes
- A61K47/6951—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit inclusion complexes, e.g. clathrates, cavitates or fullerenes using cyclodextrin
-
- 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
- A61K9/0002—Galenical forms characterised by the drug release technique; Application systems commanded by energy
-
- 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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/2027—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
-
- 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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
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- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Chemical & Material Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Natural Medicines & Medicinal Plants (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Alternative & Traditional Medicine (AREA)
- Biotechnology (AREA)
- Botany (AREA)
- Medical Informatics (AREA)
- Microbiology (AREA)
- Mycology (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines Containing Plant Substances (AREA)
Abstract
The invention discloses a dropping pill, and particularly relates to a radix sophorae flavescentis total alkaloids dropping pill. The prescription of the dropping pill comprises the following raw materials by weight: 12g of radix sophorae flavescentis total alkaloids clathrate compound, 18g of a mixture of glycerin monostearate, PVP and stearic acid, and 0.2g of disodium hydrogen phosphate and sodium dihydrogen phosphate, wherein the weight ratio of the glycerin monostearate to the PVP and to the stearic acid is 1 to 1 to 1.5; the condensate is liquid paraffin; and the weight ratio of the radix sophorae flavescentis total alkaloids to the inclusion material beta-cyclodextrin in the radix sophorae flavescentis total alkaloids clathrate compound is 1 to 2.
Description
Technical field
The present invention relates to a kind of animal drop pill, particularly comprise the preparation method of Radix Sophorae Flavescentis total alkaloids drop pill.
Background technology
Radix Sophorae Flavescentis total alkaloids, matrine is made up through organic solvent extraction such as ethanol of the dry root of leguminous plant Radix Sophorae Flavescentis, plant, fruit, is alkaloid.Be generally Radix Sophorae Flavescentis total alkaloids, its main component has the multiple alkaloids such as matrine, sophocarpine, N-oxysophocarpine, sophoridine, the highest with matrine, oxymatrine concentration.Other sources are Radix Sophorae Tonkinensis and Radix Sophorae Tonkinensis aerial parts sterling outward appearance is white powder.There are the effects such as heat clearing away, diuresis, parasite killing, damp eliminating, also there is the multiple oxidation kurarinone alkali such as antiviral, anti-tumor be irritated simultaneously in vitro and show in animal model and have strong antiviral activity to HBV, in human body, have Anti-HBV activity effect equally, existing many reports are used for the treatment of chronic viral hepatitis.
Drop pill has the following feature: 1, equipment simple, easy to operate, be beneficial to labor protection, process cycle is short, productivity ratio is high; 2, process conditions are easy to control, steady quality, and dosage is accurate, and heated time is short, after the volatile medicine of oxidizable and tool is dissolved in substrate, can increase its stability; 3, substrate holds liquid drug amount greatly, therefore liquid drug can be made to solidify; 4, have the advantages that absorption is rapid, bioavailability is high with drop pill prepared by solid dispersion technology.
Clathrate has the following advantages: cover bad stink, reduces zest; Increase drug dissolution and bioavailability; Improve medicine stability.
Summary of the invention
The invention provides a kind of Radix Sophorae Flavescentis total alkaloids drop pill, have good inhibitory action to gram negative bacteria, substantially increase oral administration biaavailability, good stability, not drug resistance, overcome the deficiencies in the prior art part.
Radix Sophorae Flavescentis total alkaloids is first prepared into clathrate by the application, and then is prepared into sustained-release dropping pill, is one, plays three aspects a little by enclose, slow release and drop pill technology and three.
Drop pill comprises Radix Sophorae Flavescentis total alkaloids clathrate, substrate, stabilizing agent.
Radix Sophorae Flavescentis total alkaloids clathrate comprises active component and enclose material, active component Radix Sophorae Flavescentis total alkaloids, and enclose material is beta-schardinger dextrin-, hydroxyl beta-schardinger dextrin-, one or more of hydroxypropylβ-cyclodextrin.The part by weight of active component and enclose material is 4:1-1:4.
As preferably, PVP is PVP40K or 60K or is its mixture.
The preparation method of Radix Sophorae Flavescentis total alkaloids clathrate comprises:
(1) in water or aquiferous ethanol medium, by a certain percentage, by Radix Sophorae Flavescentis total alkaloids and alpha-cyclodextrin, beta-schardinger dextrin-, hydroxyl beta-schardinger dextrin-, one or more reactions of hydroxypropylβ-cyclodextrin, by gained solution through filtering with microporous membrane extremely clarification, from mixture, isolate clathrate; Or
(2) in solid form, by Radix Sophorae Flavescentis total alkaloids and alpha-cyclodextrin, beta-schardinger dextrin-, hydroxyl beta-schardinger dextrin-, one or more reactions of hydroxypropylβ-cyclodextrin; Or
(3) Radix Sophorae Flavescentis total alkaloids and alpha-cyclodextrin, beta-schardinger dextrin-, hydroxyl beta-schardinger dextrin-, high energy milling is carried out in one or more reactions of hydroxypropylβ-cyclodextrin.
The substrate of sustained-release dropping pill is the key realizing slow release effect, through many-side research, select glyceryl monostearate, PVP40K and stearic mixture as substrate, and the part by weight of three is 1:1:1.5, can prepare the dropping pill formulation that slow release effect is splendid, and obtained drop pill becomes ball, roundness best.
The above-mentioned Radix Sophorae Flavescentis total alkaloids clathrate prepared is crossed 100-200 mesh sieve, and be mixed into solid dispersion system with substrate and stabilizing agent, instill the condensed fluid of 0-20 DEG C at 65 ± 5 DEG C, adsorption condensing liquid, drop pill drying, to obtain final product.
The stabilizing agent of indication of the present invention comprise phosphatic PH cushion right, as sodium hydrogen phosphate and sodium dihydrogen phosphate.
The condensed fluid of indication of the present invention comprises condensed fluid dimethicone, liquid paraffin, Oleum Camelliae, vegetable oil etc.
Metering of the present invention is weight.
Detailed description of the invention
Embodiment 1
The prescription of drop pill is (by weight):
Radix Sophorae Flavescentis total alkaloids clathrate (Radix Sophorae Flavescentis total alkaloids: hydroxypropylβ-cyclodextrin is 1:2) 4.2g, glyceryl monostearate, PVP60K and stearic mixture (part by weight of three is 1:1:1.5) 18g, sodium hydrogen phosphate and sodium dihydrogen phosphate 0.2g, condensed fluid is liquid paraffin.
Preparation method:
1. prepare Radix Sophorae Flavescentis total alkaloids clathrate by the following method:
(1) in water or aquiferous ethanol medium, in proportion, Radix Sophorae Flavescentis total alkaloids and hydroxypropylβ-cyclodextrin are reacted, by gained solution through filtering with microporous membrane extremely clarification, from mixture, isolate clathrate; Or
(2) in solid form, Radix Sophorae Flavescentis total alkaloids and hydroxypropylβ-cyclodextrin are reacted; Or
(3) Radix Sophorae Flavescentis total alkaloids and hydroxypropylβ-cyclodextrin react and carry out high energy milling.
2. Radix Sophorae Flavescentis total alkaloids clathrate was pulverized 100-200 mesh sieve; Glyceryl monostearate, PVP60K, stearic acid, sodium hydrogen phosphate and sodium dihydrogen phosphate ground and mixed is even, heating and melting on water-soluble, and mix; Radix Sophorae Flavescentis total alkaloids clathrate is added in the fused mass of glyceryl monostearate, polyethylene glycol 6000, stearic acid, sodium hydrogen phosphate and sodium dihydrogen phosphate, mixing, in impouring material fluid bath, keep temperature 65-70 DEG C 10 minutes, drop pill is formed by the liquid paraffin of above-mentioned medicinal liquid instillation 0-20 DEG C, absorb condensed fluid, dry drop pill, packaging.
Matched group 1
The prescription of drop pill is (by weight):
Radix Sophorae Flavescentis total alkaloids clathrate (Radix Sophorae Flavescentis total alkaloids: hydroxypropylβ-cyclodextrin is 1:2) 8.8g
Polyethylene glycol 6000 18g
Sodium hydrogen phosphate and sodium dihydrogen phosphate 0.2g
Condensed fluid is dimethicone.
Preparation method is the same.
Matched group 2
The prescription of drop pill is (by weight):
Radix Sophorae Flavescentis total alkaloids clathrate (Radix Sophorae Flavescentis total alkaloids: hydroxypropylβ-cyclodextrin is 1:2) 4.2g
Glyceryl monostearate 18g
Sodium hydrogen phosphate and sodium dihydrogen phosphate 0.2g
Condensed fluid is liquid paraffin.
Preparation method is the same.
Matched group 3
The prescription of drop pill is (by weight):
Radix Sophorae Flavescentis total alkaloids clathrate (Radix Sophorae Flavescentis total alkaloids: hydroxypropylβ-cyclodextrin is 1:2) 7.2g
Stearic acid 18g
Sodium hydrogen phosphate and sodium dihydrogen phosphate 0.2g
Condensed fluid is liquid paraffin.
Preparation method is the same.
Radix Sophorae Flavescentis total alkaloids clathrate drop pill experimental result presses the smooth rounding rate of the method detection drop pill of Chinese Pharmacopoeia (2000 editions), the results are shown in Table 1.
Table 1
| Group | Smooth rounding rate (%) |
| Embodiment 1 | 97.4 |
| Contrast 1 | 81.2 |
| Contrast 2 | 72.1 |
| Contrast 3 | 57.3 |
Result shows, Radix Sophorae Flavescentis total alkaloids clathrate drop pill provided by the invention meets the regulation of Chinese Pharmacopoeia (2000 editions) about drop pill.
Claims (2)
1. a Radix Sophorae Flavescentis total alkaloids sustained-release dropping pill, is characterized in that: wherein the prescription of drop pill is by weight:
Radix Sophorae Flavescentis total alkaloids clathrate 12g;
Part by weight is glyceryl monostearate, the PVP and stearic mixture 18g of 1:1:1.5;
Sodium hydrogen phosphate and sodium dihydrogen phosphate 0.2g; Condensed fluid is liquid paraffin;
Wherein said Radix Sophorae Flavescentis total alkaloids clathrate, Radix Sophorae Flavescentis total alkaloids: the part by weight of enclose material beta-schardinger dextrin-is 1:2.
2. prepare the method for sustained-release dropping pill according to claim 1, it is characterized in that: as claimed in claim 1, PVP is PVP40K or 60K or is its mixture.
1). prepare Radix Sophorae Flavescentis total alkaloids clathrate by the following method:
(1) in water or aquiferous ethanol medium, in proportion, Radix Sophorae Flavescentis total alkaloids and beta-schardinger dextrin-are reacted, by gained solution through filtering with microporous membrane extremely clarification, from mixture, isolate clathrate; Or
(2) in solid form, Radix Sophorae Flavescentis total alkaloids and beta-schardinger dextrin-are reacted; Or
(3) Radix Sophorae Flavescentis total alkaloids and beta-schardinger dextrin-react and carry out high energy milling;
2). Radix Sophorae Flavescentis total alkaloids clathrate was pulverized 100-200 mesh sieve; Glyceryl monostearate, PVP, stearic acid, sodium hydrogen phosphate and sodium dihydrogen phosphate ground and mixed is even, heating and melting in water-bath, and mix; Radix Sophorae Flavescentis total alkaloids clathrate is added in the fused mass of glyceryl monostearate, polyethylene glycol 6000, stearic acid, sodium hydrogen phosphate and sodium dihydrogen phosphate, mixing, in impouring material fluid bath, keep temperature 65-70 DEG C 10 minutes, drop pill is formed by the liquid paraffin of above-mentioned medicinal liquid instillation 0-20 DEG C, absorb condensed fluid, dry drop pill, packaging.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410652950.2A CN104352556A (en) | 2014-11-13 | 2014-11-13 | Radix sophorae flavescentis total alkaloids dropping pill |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410652950.2A CN104352556A (en) | 2014-11-13 | 2014-11-13 | Radix sophorae flavescentis total alkaloids dropping pill |
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| Publication Number | Publication Date |
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| CN104352556A true CN104352556A (en) | 2015-02-18 |
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| CN201410652950.2A Pending CN104352556A (en) | 2014-11-13 | 2014-11-13 | Radix sophorae flavescentis total alkaloids dropping pill |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104784252A (en) * | 2015-05-07 | 2015-07-22 | 黑龙江省兽医科学研究所 | Preparation method and application of sophora flavescens total alkaloid extractive |
| CN107157943A (en) * | 2017-05-18 | 2017-09-15 | 青岛正大海尔制药有限公司 | A kind of Topiroxostat preparation and preparation method thereof |
-
2014
- 2014-11-13 CN CN201410652950.2A patent/CN104352556A/en active Pending
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104784252A (en) * | 2015-05-07 | 2015-07-22 | 黑龙江省兽医科学研究所 | Preparation method and application of sophora flavescens total alkaloid extractive |
| CN104784252B (en) * | 2015-05-07 | 2018-10-19 | 黑龙江省兽医科学研究所 | The preparation method and applications of total alkaloid from sophora flavescens ait extract |
| CN107157943A (en) * | 2017-05-18 | 2017-09-15 | 青岛正大海尔制药有限公司 | A kind of Topiroxostat preparation and preparation method thereof |
| CN107157943B (en) * | 2017-05-18 | 2021-02-19 | 正大制药（青岛）有限公司 | Topiroxostat preparation and preparation method thereof |
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| PB01 | Publication | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20150218 |
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| WD01 | Invention patent application deemed withdrawn after publication |