CN103623019B - A kind of wettability Herba Andrographis solid dispersal powder and preparation method thereof - Google Patents

A kind of wettability Herba Andrographis solid dispersal powder and preparation method thereof Download PDF

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Publication number
CN103623019B
CN103623019B CN201310682233.XA CN201310682233A CN103623019B CN 103623019 B CN103623019 B CN 103623019B CN 201310682233 A CN201310682233 A CN 201310682233A CN 103623019 B CN103623019 B CN 103623019B
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herba andrographis
wettability
solid dispersal
dispersal powder
solid
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CN103623019A (en
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丁晓刚
房春林
李犹平
杨海涵
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SHANGHAI SIMENON BIOTECH Co Ltd
Chengdu Qiankun Veterinary Pharmaceutical Co Ltd
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SHANGHAI SIMENON BIOTECH Co Ltd
Chengdu Qiankun Veterinary Pharmaceutical Co Ltd
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Abstract

The present invention relates to technical field of animal remedy preparation, particularly a kind of wettability Herba Andrographis solid dispersal powder and preparation method thereof.Wettability Herba Andrographis solid dispersal powder provided by the invention with the addition of cyclodextrin, carrier, suspending agent, Pulvis Talci on the basis of the effective medicinal ingredient of Herba Andrographis, by rational drug ratio and advanced solid dispersion technology, provide a kind of bioavailability high, be easy to dispersed in water, be beneficial to the wettability Herba Andrographis solid dispersal powder of drinking water administration.Wettability Herba Andrographis solid dispersal powder provided by the invention is easy to use, bioavailability is high, is significantly better than (P < 0.05) tilmicosin pre-mixing agent and commercially available Herba Andrographis end to the therapeutic effect of disease; Present invention also offers a kind of preparation method of wettability Herba Andrographis solid dispersal powder, the method technique is simple, low production cost, is applicable to industrialized great production.

Description

A kind of wettability Herba Andrographis solid dispersal powder and preparation method thereof
Technical field
The present invention relates to technical field of animal remedy preparation, particularly a kind of wettability Herba Andrographis solid dispersal powder and preparation method thereof.
Background technology
Herba Andrographis AndrographisPaniculata(Burm.f.) and Nees ] be Acanthaceae Herba Andrographis platymiscium, another name Lan Helian, Herba Andrographitis, India's grass, Andrographis paniculata(Burm.f.)Nees, Herba vallisneriae Spiralis, Rabdosia stracheyi(Benth.ex Hook.f.)Hara[Plectranthus stracheyi Benth.ex Hook.f., circular cone palpus medicinal herbs etc., its bitter in the mouth, cold in nature, return lung, stomach, large intestine, small intestine meridian, originate in India, all there is cultivation on the ground such as China south China, southwest, East China.Herba Andrographis has heat-clearing and toxic substances removing, removing heat from blood detumescence function, joins Herba Menthae, Flos Chrysanthemi, Radix Platycodonis uses, can pharynx-clearing throat-benefiting; Join Gypsum Fibrosum, the Rhizoma Anemarrhenae, Flos Lonicerae, Fructus Forsythiae use, can lung heat clearing eliminating fire and detoxication; Join the Radix Rehmanniae, Cortex Moutan, Folium Isatidis use, can removing pathogenic heat from blood and toxic substance from the body detumescence.Herba Andrographis cures mainly acute bacillary dysentery, gastroenteritis, flu, epidemic encephalitis, tracheitis, pneumonia, pertussis, pulmonary tuberculosis, lung abscess, cholecystitis, hypertension, epistaxis, oropharynx swell and ache, furuncle carbuncle, burn due to hot liquid or fire and venom.
Modern study shows, the chemical composition of Herba Andrographis is mainly lactone and flavone compound.Lactone compound is mainly present in Folium Andrographis, mainly contain following kind: desoxyandrographolide (also known as dexyandrographolide), andrographolide (also known as andrographolide), neoandrographolide (also known as Neoandrographolide), dehydrorographolide (also known as 14-Deoxy-11,12-didehydro-andrographolide), dexyandrographolide glycoside, desoxyandrographolide-19-β-D glycoside, 14-deoxidation-12-methoxyl group andrographolide, 14-deoxidation-11-be oxidized andrographolide and Herba Andrographis peaceful etc., the lactone content of Herba Andrographis herb is at about 2%-5%; Flavone compound is mainly present in andrographis root, is mainly polymethoxyflavone.In addition, Herba Andrographis is also containing the number of chemical composition such as the nutrient substance such as protein, multivitamin and andnrographan, Herba Andrographis wax, phosterin, potassium chloride, sodium chloride, alkaloid (0.6%).Modern pharmacological research is thought, Herba Andrographis has antibacterial, antiviral, antipyretic, antiinflammatory, hepatic cholagogic, immunomodulating, anticancer, antiplatelet aggregation, contraception, adrenal cortex reinforcing function, venom and muscarinic action, anti-alcoholism and suppresses the multiple pharmacologically actives such as acute promyelocytic leukemia cell growth.Research finds, Herba Andrographis resists myocardial ischemia with ischemia resisting reperfusion injury, protection vascular endothelial cell in addition, adjusts fat, blood pressure lowering, atherosclerosis and the postoperative restenosis of prevention vascularization and improve the effects such as hemorheological property.
Clinically be used for the treatment of the infectious disease such as trauma infection contamination, furuncle, carbuncle, erysipelas, upper respiratory tract infection, acute and chronic tonsillitis, acute and chronic pharyngitis, acute/chronic bronchitis, acute bacillary dysentery, acute gastroenteritis, urinary tract infection, endometritis, pelvic inflammatory disease, otitis media, periodontitis.On veterinary clinic, Herba Andrographis single preparations of ephedrine is mainly used in the diseases such as control poultry pneumonia, enteritis, diarrhoea, and strengthen immunity in addition, improve the aspect application such as raise benefit, therefore, Herba Andrographis has larger using value on veterinary clinic.At present, Herba Andrographis has the dosage forms such as injection, tablet, powder, oral capsule or granule, wherein injection, powder and tablet are the common formulations on veterinary clinic, but all there is limitation when using, the breaking method that in the existing dosage form manufacturing process of Herba Andrographis, many employings are general, the powder of obtained thick dispersity, often bioavailability is very low.In addition, existing dosage form uses inconvenient, and when tablet uses, dispensing is inconvenient, is not suitable for a fairly large number of group support animal; Powder needs by feedstuff administration when using, feedstuff medication requirements medicine and feedstuff mix homogeneously, and during practical operation, mix homogeneously is more difficult, easily causes animal to take the photograph dose too much poisoning or take the photograph the situation of the very few inefficacy of dose; And feedstuff administration malleable feedstuff local flavor, cause animal reload stress, thus cause animal feed intake decline and do not reach therapeutic effect; Injection dosage form therapeutic effect is good, but wastes time and energy, and is not suitable for large-scale farming.
In order to allow Herba Andrographis better be applied in livestock-raising and raising pets, the novel form developing a kind of bioavailability Herba Andrographis high, easy to use has great importance.
Summary of the invention
In view of this, the invention provides a kind of wettability Herba Andrographis solid dispersal powder, the basis of the effective medicinal ingredient of Herba Andrographis with the addition of cyclodextrin, carrier, suspending agent, Pulvis Talci, by rational drug ratio and advanced solid dispersion technology, provide a kind of bioavailability high, be easy to dispersed in water, be beneficial to the wettability Herba Andrographis solid dispersal powder of drinking water administration, wettability Herba Andrographis solid dispersal powder provided by the invention is easy to use, bioavailability is high, tilmicosin pre-mixing agent and commercially available Herba Andrographis end are better than to the therapeutic effect remarkable (P < 0.05) of disease, present invention also offers a kind of preparation method of wettability Herba Andrographis solid dispersal powder, the method technique is simple, low production cost, is applicable to industrialized great production.
The invention provides a kind of wettability Herba Andrographis solid dispersal powder, comprise the raw material of following weight portion:
As preferably, wettability Herba Andrographis solid dispersal powder comprises the raw material of following weight portion:
Preferred, wettability Herba Andrographis solid dispersal powder comprises the raw material of following weight portion:
As preferably, Herba Andrographis also can be creat extract, and total drug effect of creat extract is identical with total drug effect of Herba Andrographis.
As preferably, cyclodextrin is DM-β-CD.
As preferably, carrier is a kind of or both the above mixture in sucrose, anhydrous glucose, sodium dihydrogen phosphate.
As preferably, suspending agent is xanthan gum.
As preferably, the raw material of wettability Herba Andrographis solid dispersal powder also comprises correctives.
As preferably, correctives is 0.6 ~ 1.8 weight portion.
In some embodiments of the invention, wettability Herba Andrographis solid dispersal powder comprises the raw material of following weight portion:
In other embodiments of the present invention, wettability Herba Andrographis solid dispersal powder comprises the raw material of following weight portion:
In other embodiments of the present invention, wettability Herba Andrographis solid dispersal powder comprises the raw material of following weight portion:
As preferably, correctives is a kind of or both the above mixture in sweeting agent, bitterness screening agent, bitter inhibitor; Preferred, correctives is the mixture of sweeting agent, bitterness screening agent, bitter inhibitor.
As preferably, wettability Herba Andrographis solid dispersal powder comprises the raw material of following weight portion:
In other embodiments of the present invention, wettability Herba Andrographis solid dispersal powder comprises the raw material of following weight portion:
In other embodiments of the present invention, wettability Herba Andrographis solid dispersal powder comprises the raw material of following weight portion:
As preferably, sweeting agent is a kind of or both the above mixture in aspartame, sucralose, neotame, glucide.
As preferably, bitterness screening agent is tannic acid.
As preferably, bitter inhibitor is phosphatidic acid.
As preferably, the raw material of wettability Herba Andrographis solid dispersal powder also comprises antioxidant.
As preferably, antioxidant comprises 2,6-di-tert-butyl-4-methy phenol.
As preferably, antioxidant is 0.0016 ~ 0.004 weight portion.
In some embodiments of the invention, wettability Herba Andrographis solid dispersal powder comprises the raw material of following weight portion:
In other embodiments of the present invention, wettability Herba Andrographis solid dispersal powder comprises the raw material of following weight portion:
In other embodiments of the present invention, wettability Herba Andrographis solid dispersal powder comprises the raw material of following weight portion:
As preferably, wettability Herba Andrographis solid dispersal powder comprises the raw material of following weight portion:
In other embodiments of the present invention, wettability Herba Andrographis solid dispersal powder comprises the raw material of following weight portion:
In other embodiments of the present invention, wettability Herba Andrographis solid dispersal powder comprises the raw material of following weight portion:
In wettability Herba Andrographis solid dispersal powder, the effect of each raw material is as follows:
Herba Andrographis: having antibacterial, antiviral, antipyretic, antiinflammatory, hepatic cholagogic, immunomodulating, anticancer, antiplatelet aggregation, contraception, adrenal cortex reinforcing function, venom and muscarinic action, anti-alcoholism, suppress the multiple pharmacologically actives such as acute promyelocytic leukemia cell growth, is the main active of medicine.
Cyclodextrin: cyclodextrin can increase the dissolubility of the bad medicine of some water solublity in water and dissolution velocity effectively, it can also improve stability and the bioavailability of medicine, reduce bad smell or the bitterness of Herba Andrographis, and stimulation and the toxic and side effects of medicine can be reduced, slow release and the dosage form improving medicine.
Carrier: medicine high uniformity can be made to be dispersed in carrier mass and form drug-carrier solid dispersion, thus increase the dissolubility of insoluble drug and dissolution rate, and the bad of medicine can be covered smell taste and zest, improve bioavailability.
Pulvis Talci: effect when amount of talc is few with dispersant and processing aid, when solid material is pulverized, is conducive to granule and pulverizes and can keep the stable of dispersion, and can ensure that the medicine course of processing is carried out smoothly; Amount of talc has the effect of quality improver and synergist after increasing.
Suspending agent: the suspending agents such as sodium carboxymethyl cellulose can increase the viscosity of disperse medium, thus reduce the sedimentation velocity of microgranule or increase the hydrophilic of microgranule.
Correctives: comprise sweeting agent, bitterness screening agent and bitter inhibitor; Add sweeting agent in feedstuff and can improve children domestic animal in age, the especially feed intake of pig, can also improve feed conversion rate; The bitterness screening agents such as tannic acid can generate indissoluble salt with Herba Andrographis effective ingredient and be wrapped in outside drug particles, thus play the effect of good elimination bitterness; The bitter inhibitor alternatives such as phosphatidic acid are combined with bitterness receptors, stop the contact of medicine and taste bud, thus play good debitter effect.
Antioxidant: in Herba Andrographis, primary medicinal component andrographolide compounds is diterpenes diterpenoids lactones, character extremely unstable, oxidizable, 2, the antioxidants such as 6-di-tert-butyl-4-methy phenol can stop the oxidation of medicine, the stability of medicine can be improved, Drug safety and effectiveness can be kept, and be beneficial to preparation and long-term preservation.
Present invention also offers a kind of preparation method of wettability Herba Andrographis solid dispersal powder, comprise the following steps:
A) raw material of following weight portion is taken respectively:
B) get Herba Andrographis solvent extraction, obtain extracting solution;
C) get extracting solution to concentrate, mix with cyclodextrin, dehydrated alcohol, carrier, 35 DEG C ~ 65 DEG C dryings, then mix with Pulvis Talci, suspending agent, pulverize, to obtain final product.
In some embodiments of the invention, the preparation method of wettability Herba Andrographis solid dispersal powder comprises the following steps:
A) raw material of following weight portion is taken respectively:
B) get Herba Andrographis solvent extraction, obtain extracting solution;
C) get extracting solution to concentrate, mix with cyclodextrin, dehydrated alcohol, carrier, 35 DEG C ~ 65 DEG C dryings, then mix with Pulvis Talci, suspending agent, pulverize, to obtain final product.
In other embodiments of the present invention, the preparation method of wettability Herba Andrographis solid dispersal powder comprises the following steps:
A) raw material of following weight portion is taken respectively:
B) get Herba Andrographis solvent extraction, obtain extracting solution;
C) get extracting solution to concentrate, mix with cyclodextrin, dehydrated alcohol, carrier, 35 DEG C ~ 65 DEG C dryings, then mix with Pulvis Talci, suspending agent, pulverize, to obtain final product.
As preferably, the preparation method of wettability Herba Andrographis solid dispersal powder comprises the following steps:
A) raw material of following weight portion is taken respectively:
B) get Herba Andrographis solvent extraction, obtain extracting solution;
C) get extracting solution to concentrate, mix with cyclodextrin, bitterness screening agent, carrier, 35 DEG C ~ 65 DEG C dryings, then mix with sweeting agent, bitter inhibitor, Pulvis Talci, suspending agent, pulverize, to obtain final product.
As preferably, solvent is water or organic solvent.
Preferred, organic solvent is ethanol.
As preferably, bitterness screening agent is fat-soluble, water solublity or double dissolubility; Double dissolubility refers to bitterness screening agent both water solubles, dissolves in organic solvent again.
In some embodiments of the invention, bitterness screening agent is water solublity, and the preparation method of wettability Herba Andrographis solid dispersal powder comprises the following steps:
A) raw material of following weight portion is taken respectively:
B) get Herba Andrographis water extraction, obtain extracting solution;
C) get extracting solution to concentrate, mix with cyclodextrin, bitterness screening agent, carrier, 35 DEG C ~ 65 DEG C dryings, then mix with sweeting agent, bitter inhibitor, Pulvis Talci, suspending agent, pulverize, to obtain final product.
In some embodiments of the invention, bitterness screening agent can be water solublity, and the preparation method of wettability Herba Andrographis solid dispersal powder comprises the following steps:
A) raw material of following weight portion is taken respectively:
B) get Herba Andrographis water extraction, obtain extracting solution;
C) get extracting solution to concentrate, mix with cyclodextrin, bitterness screening agent, carrier, 35 DEG C ~ 65 DEG C dryings, then mix with sweeting agent, bitter inhibitor, Pulvis Talci, suspending agent, pulverize, to obtain final product.
In other embodiments of the present invention, bitterness screening agent is water solublity, and the preparation method of wettability Herba Andrographis solid dispersal powder comprises the following steps:
A) raw material of following weight portion is taken respectively:
B) get Herba Andrographis water extraction, obtain extracting solution;
C) get extracting solution to concentrate, mix with cyclodextrin, bitterness screening agent, carrier, 35 DEG C ~ 65 DEG C dryings, then mix with sweeting agent, bitter inhibitor, Pulvis Talci, suspending agent, pulverize, to obtain final product.
As preferably, when bitterness screening agent is water solublity, the preparation method of wettability Herba Andrographis solid dispersal powder comprises the following steps:
A) raw material of following weight portion is taken respectively:
B) get Herba Andrographis organic solvent extraction, obtain extracting solution;
C) get extracting solution to concentrate, mix with cyclodextrin, bitterness screening agent, water, carrier, 35 DEG C ~ 65 DEG C dryings, then mix with sweeting agent, bitter inhibitor, Pulvis Talci, suspending agent, pulverize, to obtain final product.
In some embodiments of the invention, bitterness screening agent can be water solublity, and the preparation method of wettability Herba Andrographis solid dispersal powder comprises the following steps:
A) raw material of following weight portion is taken respectively:
B) get Herba Andrographis organic solvent extraction, obtain extracting solution;
C) get extracting solution to concentrate, mix with cyclodextrin, bitterness screening agent, water, carrier, 35 DEG C ~ 65 DEG C dryings, then mix with sweeting agent, bitter inhibitor, Pulvis Talci, suspending agent, pulverize, to obtain final product.
In other embodiments of the present invention, bitterness screening agent is water solublity, and the preparation method of wettability Herba Andrographis solid dispersal powder comprises the following steps:
A) raw material of following weight portion is taken respectively:
B) get Herba Andrographis organic solvent extraction, obtain extracting solution;
C) get extracting solution to concentrate, mix with cyclodextrin, bitterness screening agent, water, carrier, 35 DEG C ~ 65 DEG C dryings, then mix with sweeting agent, bitter inhibitor, Pulvis Talci, suspending agent, pulverize, to obtain final product.
As preferably, when bitterness screening agent is fat-soluble, the preparation method of wettability Herba Andrographis solid dispersal powder comprises the following steps:
A) raw material of following weight portion is taken respectively:
B) get Herba Andrographis water extraction, obtain extracting solution;
C) get extracting solution to concentrate, mix with cyclodextrin, bitterness screening agent, organic solvent, carrier, 35 DEG C ~ 65 DEG C dryings, then mix with sweeting agent, bitter inhibitor, Pulvis Talci, suspending agent, pulverize, to obtain final product.
In some embodiments of the invention, bitterness screening agent is fat-soluble, and the preparation method of wettability Herba Andrographis solid dispersal powder comprises the following steps:
A) raw material of following weight portion is taken respectively:
B) get Herba Andrographis water extraction, obtain extracting solution;
C) get extracting solution to concentrate, mix with cyclodextrin, bitterness screening agent, organic solvent, carrier, 35 DEG C ~ 65 DEG C dryings, then mix with sweeting agent, bitter inhibitor, Pulvis Talci, suspending agent, pulverize, to obtain final product.
In other embodiments of the present invention, bitterness screening agent is fat-soluble, and the preparation method of wettability Herba Andrographis solid dispersal powder comprises the following steps:
A) raw material of following weight portion is taken respectively:
B) get Herba Andrographis water extraction, obtain extracting solution;
C) get extracting solution to concentrate, mix with cyclodextrin, bitterness screening agent, organic solvent, carrier, 35 DEG C ~ 65 DEG C dryings, then mix with sweeting agent, bitter inhibitor, Pulvis Talci, suspending agent, pulverize, to obtain final product.
As preferably, when bitterness screening agent is fat-soluble, the preparation method of wettability Herba Andrographis solid dispersal powder comprises the following steps:
A) raw material of following weight portion is taken respectively:
B) get Herba Andrographis organic solvent extraction, obtain extracting solution;
C) get extracting solution to concentrate, mix with cyclodextrin, bitterness screening agent, carrier, 35 DEG C ~ 65 DEG C dryings, then mix with sweeting agent, bitter inhibitor, Pulvis Talci, suspending agent, pulverize, to obtain final product.
In some embodiments of the invention, bitterness screening agent is fat-soluble, and the preparation method of wettability Herba Andrographis solid dispersal powder comprises the following steps:
A) raw material of following weight portion is taken respectively:
B) get Herba Andrographis organic solvent extraction, obtain extracting solution;
C) get extracting solution to concentrate, mix with cyclodextrin, bitterness screening agent, carrier, 35 DEG C ~ 65 DEG C dryings, then mix with sweeting agent, bitter inhibitor, Pulvis Talci, suspending agent, pulverize, to obtain final product.
In other embodiments of the present invention, bitterness screening agent is fat-soluble, and the preparation method of wettability Herba Andrographis solid dispersal powder comprises the following steps:
A) raw material of following weight portion is taken respectively:
B) get Herba Andrographis organic solvent extraction, obtain extracting solution;
C) get extracting solution to concentrate, mix with cyclodextrin, bitterness screening agent, carrier, 35 DEG C ~ 65 DEG C dryings, then mix with sweeting agent, bitter inhibitor, Pulvis Talci, suspending agent, pulverize, to obtain final product.
In other embodiments of the present invention, bitterness screening agent is dissolubility of holding concurrently, and the preparation method of wettability Herba Andrographis solid dispersal powder comprises the following steps:
A) raw material of following weight portion is taken respectively:
B) get Herba Andrographis water extraction, obtain extracting solution;
C) get extracting solution to concentrate, mix with cyclodextrin, bitterness screening agent, carrier, 35 DEG C ~ 65 DEG C dryings, then mix with sweeting agent, bitter inhibitor, Pulvis Talci, suspending agent, pulverize, to obtain final product.
In other embodiments of the present invention, bitterness screening agent is dissolubility of holding concurrently, and the preparation method of wettability Herba Andrographis solid dispersal powder comprises the following steps:
A) raw material of following weight portion is taken respectively:
B) get Herba Andrographis organic solvent extraction, obtain extracting solution;
C) get extracting solution to concentrate, mix with cyclodextrin, bitterness screening agent, carrier, 35 DEG C ~ 65 DEG C dryings, then mix with sweeting agent, bitter inhibitor, Pulvis Talci, suspending agent, pulverize, to obtain final product.
As preferably, the preparation method of wettability Herba Andrographis solid dispersal powder comprises the following steps:
A) raw material of following weight portion is taken respectively:
B) get Herba Andrographis solvent extraction, obtain extracting solution;
C) get extracting solution to concentrate, add cyclodextrin, obtain mixture;
D) get antioxidant, dehydrated alcohol mixing, then mix with mixture, bitterness screening agent, carrier, 35 DEG C ~ 65 DEG C dryings, then mix with sweeting agent, bitter inhibitor, Pulvis Talci, suspending agent, pulverize, to obtain final product.
In some embodiments of the invention, the preparation method of wettability Herba Andrographis solid dispersal powder comprises the following steps:
A) raw material of following weight portion is taken respectively:
B) get Herba Andrographis solvent extraction, obtain extracting solution;
C) get extracting solution to concentrate, add cyclodextrin, obtain mixture;
D) get antioxidant, dehydrated alcohol mixing, then mix with mixture, bitterness screening agent, carrier, 35 DEG C ~ 65 DEG C dryings, then mix with sweeting agent, bitter inhibitor, Pulvis Talci, suspending agent, pulverize, to obtain final product.
In other embodiments of the present invention, the preparation method of wettability Herba Andrographis solid dispersal powder comprises the following steps:
A) raw material of following weight portion is taken respectively:
B) get Herba Andrographis solvent extraction, obtain extracting solution;
C) get extracting solution to concentrate, add cyclodextrin, obtain mixture;
D) get antioxidant, dehydrated alcohol mixing, then mix with mixture, bitterness screening agent, carrier, 35 DEG C ~ 65 DEG C dryings, then mix with sweeting agent, bitter inhibitor, Pulvis Talci, suspending agent, pulverize, to obtain final product.
In step b), extracting solution also can be passed through drying and makes creat extract.
As preferably, wettability Herba Andrographis solid dispersal powder, preparation method thereof is as follows:
A) raw material of following weight portion is taken respectively:
B) get Herba Andrographis solvent extraction, obtain extracting solution;
C) get extracting solution to concentrate, dry, obtain creat extract;
D) get cyclodextrin, creat extract, dehydrated alcohol, carrier mixing, 35 DEG C ~ 65 DEG C dryings, then mix with Pulvis Talci, suspending agent, pulverize, to obtain final product.
In certain embodiments, wettability Herba Andrographis solid dispersal powder, preparation method thereof is as follows:
A) raw material of following weight portion is taken respectively:
B) get Herba Andrographis solvent extraction, obtain extracting solution;
C) get extracting solution to concentrate, dry, obtain creat extract;
D) get cyclodextrin, bitterness screening agent, creat extract, dehydrated alcohol, carrier mixing, 35 DEG C ~ 65 DEG C dryings, then mix with sweeting agent, bitter inhibitor, Pulvis Talci, suspending agent, pulverize, to obtain final product.
As preferably, the preparation method of wettability Herba Andrographis solid dispersal powder comprises the following steps:
A) raw material of following weight portion is taken respectively:
B) get Herba Andrographis solvent extraction, obtain extracting solution;
C) get extracting solution to concentrate, dry, obtain creat extract;
D) get antioxidant, dehydrated alcohol mixing, then mix with cyclodextrin, bitterness screening agent, creat extract, carrier, 35 DEG C ~ 65 DEG C dryings, then mix with sweeting agent, bitter inhibitor, Pulvis Talci, suspending agent, pulverize, to obtain final product.
As preferably, in the preparation method of wettability Herba Andrographis solid dispersal powder, in step b), solvent is the mixture of any one or both in water or ethanol.
As preferably, raw material also directly can adopt creat extract, total drug effect of creat extract is identical with total drug effect of Herba Andrographis, when in raw material, Herba Andrographis is replaced by the creat extract of identical effective ingredient, be equivalent to the creat extract of 5g Herba Andrographis for 1g, wettability Herba Andrographis solid dispersal powder, preparation method thereof is as follows:
A) raw material of following weight portion is taken respectively:
B) get creat extract, cyclodextrin, 60% ethanol mixing, obtain creat extract diluent;
C) get creat extract diluent, dehydrated alcohol, carrier mixing, 35 DEG C ~ 65 DEG C dryings, then mix with Pulvis Talci, suspending agent, pulverize, to obtain final product.
In some embodiments of the invention, wettability Herba Andrographis solid dispersal powder, preparation method thereof is as follows:
A) raw material of following weight portion is taken respectively:
B) get creat extract, cyclodextrin, bitter inhibitor, 60% ethanol mixing, obtain creat extract diluent;
C) get antioxidant, dehydrated alcohol mixing, add creat extract diluent, carrier, mixing, 35 DEG C ~ 65 DEG C dryings, then mix with bitterness screening agent, sweeting agent, Pulvis Talci, suspending agent, pulverize, to obtain final product.
In other embodiments of the present invention, wettability Herba Andrographis solid dispersal powder, preparation method thereof is as follows:
A) raw material of following weight portion is taken respectively:
B) get creat extract, cyclodextrin, 60% ethanol mixing, obtain creat extract diluent;
C) get antioxidant, dehydrated alcohol mixing, then mix with creat extract diluent, bitterness screening agent, carrier, 35 DEG C ~ 65 DEG C dryings, then mix with bitter inhibitor, sweeting agent, Pulvis Talci, suspending agent, pulverize, to obtain final product.
Wettability Herba Andrographis solid dispersal powder provided by the invention significantly improves the dispersibility of the total effective ingredient of Herba Andrographis in water, make it be evenly distributed on for a long time in water, during Clinical practice, add water suspensoid, by the mode administration of drinking-water, be applicable to large-scale farming.Wettability Herba Andrographis solid dispersal powder can also by be sprayed on feedstuff, the form administration of directly spice or drug administration by injection.
The invention provides a kind of wettability Herba Andrographis solid dispersal powder, comprise the raw material of following weight portion: Herba Andrographis 200 ~ 400 weight portion; Cyclodextrin 0.4 ~ 32 weight portion; Carrier 13.1 ~ 57.8 weight portion; Suspending agent 0.4 ~ 1.2 weight portion; Pulvis Talci 0.2 weight portion; Preferably, correctives is 0.6 ~ 1.8 weight portion; Preferred, correctives comprises a kind of in sweeting agent, bitterness screening agent, bitter inhibitor or both above mixture, and as preferably, wettability Herba Andrographis solid dispersal powder provided by the invention also comprises antioxidant, preferred, antioxidant is 0.0016 ~ 0.004 weight portion.Add suspending agent in formula of the present invention, significantly improve the dispersibility of the total effective ingredient of Herba Andrographis in water, make it be evenly distributed on for a long time in water, convenient clinically by drinking water administration; Add cyclodextrin, carrier, Pulvis Talci in wettability Herba Andrographis solid dispersal powder formula, and adopt solid dispersion technology to carry out the preparation of medicine, be beneficial to the dispersed of the total effective ingredient of Herba Andrographis, improve the bioavailability of medicine.In certain embodiments, correctives is added in formula, substantially improve the palatability of medicine, wherein bitterness screening agent and bitter inhibitor effectively can hide the bitterness of Herba Andrographis, sweeting agent can increase the palatability of medicine further, expand the scope of application of wettability Herba Andrographis solid dispersal powder, for the faunichron that pig etc. has a sharp sense of taste, have luring function.
Formulation screening test shows, wettability Herba Andrographis solid dispersal powder provided by the invention can be dispersed in water, sedimentation velocity slow, is beneficial to clinical drinking water administration; In certain embodiments, wettability Herba Andrographis solid dispersal powder good palatability, has luring function to pig; In addition, wettability Herba Andrographis solid dispersal powder drug loading is large, improves the bioavailability of medicine, reduces side effects of pharmaceutical drugs.
To the display of hyopneumoniae clinical tests result, wettability Herba Andrographis solid dispersal powder provided by the invention has good therapeutic effect to hyopneumoniae, and therapeutic effect is significantly better than tilmicosin pre-mixing agent; And it is easy to use; In certain embodiments, wettability Herba Andrographis solid dispersal powder good palatability, applied widely; In further embodiments, owing to adding antioxidant, medicine stability improves a lot; Because preparation process adopts solid dispersion technology, in wettability Herba Andrographis solid dispersal powder, effective ingredient is uniformly dispersed, and bioavailability is high.
To the display of broiler Hakuri clinical tests result, wettability Herba Andrographis solid dispersal powder provided by the invention has good therapeutic effect to broiler Hakuri, and compared with commercially available Herba Andrographis end, therapeutic effect is significantly increased, and easy to use; In further embodiments, owing to adding antioxidant, medicine stability improves a lot; In addition, because preparation process adopts solid dispersion technology, in wettability Herba Andrographis solid dispersal powder, effective ingredient is uniformly dispersed, and bioavailability is high.
Therefore, the invention provides one and be easy to dispersed in water, be beneficial to drinking water administration and the high wettability Herba Andrographis solid dispersal powder of bioavailability, compare with commercially available Herba Andrographis end with tilmicosin pre-mixing agent, wettability Herba Andrographis solid dispersal treated powder is effective, easy to use, in certain embodiments, owing to adding correctives in formula, effective bitterness hiding Herba Andrographis, improves palatability of drugs, expands the scope of application of medicine; In further embodiments, owing to adding antioxidant in formula, medicine stability improves a lot; In addition, because preparation process adopts solid dispersion technology, in wettability Herba Andrographis solid dispersal powder, effective ingredient is uniformly dispersed, and bioavailability is high.Present invention also offers a kind of preparation method of wettability Herba Andrographis solid dispersal powder, the method technique is simple, low production cost, is applicable to industrialized great production.
Detailed description of the invention
The invention provides a kind of wettability Herba Andrographis solid dispersal powder and preparation method thereof, those skilled in the art can use for reference present disclosure, and suitable improving technique parameter realizes.Special needs to be pointed out is, all similar replacements and change apparent to those skilled in the art, they are all deemed to be included in the present invention.Method of the present invention and application are described by preferred embodiment, related personnel obviously can change methods and applications herein or suitably changes and combination not departing from content of the present invention, spirit and scope, realizes and applies the technology of the present invention.
For pharmaceutical composition, supplementary product kind, consumption and auxiliary material combination etc. are the key factors of preparation, they be directly connected to can obtain said preparation and obtain the quality of the quality of the pharmaceutical preparations.For wettable powder of the present invention, main inspection target is dispersion and sedimentation velocity.Dispersion detects and can drop in water by medicine, observes or stirs and observe its deployment conditions, and then judging that whether dispersion is qualified.Sedimentation velocity detects can by " solution for oral administration, suspensoid for oral administration, Emulsion for oral administration " sedimentation volume ratio inspection technique requirement in " People's Republic of China's veterinary drug allusion quotation (version in 2010) " annex, the formula sedimentation volume ratio of the wettability Herba Andrographis solid dispersal powder in embodiment is measured, and then judges that whether product is qualified.
During drinking water for animals administration, the veterinary drug of some palatability differences badly smells taste owing to having, and the animal amount of drinking of the sense of taste sensitivities such as pig can be caused to reduce and even do not drink, thus not easily reach the therapeutic effect of expection.Therefore, the palatability of veterinary drug has larger impact for the curative effect of veterinary drug.The method that palatability detects: veterinary drug is converted drinking water by quantity, drinks for healthy swinery, observe the drinking-water situation of swinery, whether the palatability evaluating medicine with this is good.
Drug loading is evaluated: by the dosage and the ratio of the wettability Herba Andrographis solid dispersal powder total amount made that calculate Herba Andrographis goods, calculate the drug loading of wettability Herba Andrographis solid dispersal powder of the present invention.
In the present invention, the test of animal clinical tests adopts wettability Herba Andrographis solid dispersal powder to the test of hyopneumoniae clinical tests and tests the clinical tests of broiler Hakuri.The stimulation that hyopneumoniae is subject to pathogenic microorganism or foreign body by the lung tissue of pig causes.Clinical main manifestations is: heating, lack of appetite, and cough, diminished breath sound, nasal cavity stream mucus, expired gas has corrupt abnormal smells from the patient.Herba Andrographis has effect of antibacterial, antiviral, antipyretic, antiinflammatory, has good therapeutic effect to hyopneumoniae.Respectively wettability Herba Andrographis solid dispersal powder provided by the invention and tilmicosin pre-mixing agent are applied to the treatment of hyopneumoniae in clinical trial of the present invention, by the contrast of the two curative effect, show outstanding advantage of the present invention.In the clinical tests test of wettability Herba Andrographis foot couple hyopneumoniae, it is as follows that drug level arranges standard: positive controls " spice concentration " specifies the Dosage calculation gained of tilmicosin pre-mixing agent to pig according to " veterinary drug allusion quotation "; It is specify the Dosage calculation at Herba Andrographis end according to the amount of drinking water weight ratio of pig with " veterinary drug allusion quotation " and obtain that test group " converts potable water concentration ".
White diarrhea disease be by S. pullonum cause in all generable a kind of infectious disease of various age.Sick chicken clinical manifestation is: lethargy, bows and closes order, and disorderly, two wings are sagging for feather pine, and loss of appetite or absolutely useless, faint, diarrhoea, arranges white, yellow, green or brown loose stool.Herba Andrographis can suppress the growth of S. pullonum, therefore, has good therapeutic effect to the Hakuri of broiler.The present invention, to the treatment respectively wettability Herba Andrographis solid dispersal powder provided by the invention and commercially available Herba Andrographis end being applied to broiler Hakuri in broiler Hakuri clinical trial, by the contrast of the two curative effect, shows outstanding advantage of the present invention.
Formulation screening test shows, wettability Herba Andrographis solid dispersal powder provided by the invention can be dispersed in water, sedimentation velocity slow, is beneficial to clinical drinking water administration; In certain embodiments, wettability Herba Andrographis solid dispersal powder good palatability, has luring function to pig.In addition, wettability Herba Andrographis solid dispersal powder drug loading is large, improves the bioavailability of medicine, reduces side effects of pharmaceutical drugs.
Show the clinical tests result of hyopneumoniae, wettability Herba Andrographis solid dispersal powder provided by the invention has good therapeutic effect to hyopneumoniae; Therapeutic effect is significantly higher than tilmicosin pre-mixing agent, and easy to use, applied widely.Show the clinical tests result of broiler Hakuri, wettability Herba Andrographis solid dispersal powder provided by the invention has good therapeutic effect to broiler Hakuri, and compared with commercially available Herba Andrographis end, therapeutic effect is significantly increased, and easy to use.Therefore, the invention provides one and be easy to dispersed in water, be beneficial to the wettability Herba Andrographis solid dispersal powder of drinking water administration; In certain embodiments, owing to adding correctives in formula, improve palatability of drugs, expand the scope of application of medicine; In further embodiments, owing to adding antioxidant in formula, make the effective ingredient in Herba Andrographis more stable; In addition, owing to adopting solid dispersion technology, in wettability Herba Andrographis solid dispersal powder, effective ingredient is uniformly dispersed, and bioavailability is high.
Present invention also offers a kind of preparation method of wettability Herba Andrographis solid dispersal powder, the method technique is simple, low production cost, is applicable to industrialized great production.
Wettability Herba Andrographis solid dispersal powder preparation test provided by the invention, wettability Herba Andrographis solid dispersal powder are in hyopneumoniae and broiler Hakuri clinical trial, and raw materials used source is as follows:
Creat extract: manufacturer is Sichuan Guanghan City Wei Kang plant company limited, and 100g Herba Andrographis crude drug is equivalent to creat extract 20g.
Tilmicosin pre-mixing agent: manufacturer is Chengdu Qiankun Animal Drug Industry Co., Ltd., containing tilmicosin 20g in 100g tilmicosin pre-mixing agent.
Herba Andrographis end: manufacturer is Chengdu Qiankun Animal Drug Industry Co., Ltd., containing Herba Andrographis primary crude drug 100g in 100g Herba Andrographis end.
Experimental animal: the sick pig of the hyopneumoniae of Chengdu suburbs and counties under the jurisdiction of a large city first pig farm natural occurrence; The sick chicken of the broiler Hakuri of Leshan chicken house natural occurrence.
Below in conjunction with embodiment, set forth the present invention further:
The recipe determination of embodiment 1 wettability Herba Andrographis solid dispersal powder
Screening formula is as shown in formula 1 ~ formula 6 in table 1:
The preferred version of table 1 wettability Herba Andrographis solid dispersal powder formula
Take the raw material of each weight portion in formula 1 ~ formula 6 in table 1 respectively, get creat extract, DM-β-CD, phosphatidic acid, add 60% ethanol and melt, make creat extract diluent;
Get 2,6-di-tert-butyl-4-methy phenol, mix after adding 100mL ~ 200mL anhydrous alcohol solution with for creat extract diluent, add sodium dihydrogen phosphate by ormal weight under corresponding formula item, moistening soft material is made in mixing, 50 DEG C of oven dry of ventilating, add tannic acid, aspartame, Pulvis Talci, xanthan gum, mixing, pulverizes, prepares wettability Herba Andrographis solid dispersal powder of the present invention.
Wettability Herba Andrographis solid dispersal powder obtained for formula 1 ~ formula 6 is carried out dispersion quality evaluation, sedimentation volume ratio quality evaluation, palatability quality evaluation and drug loading quality evaluation.
Dispersion quality evaluation: get each 1g of wettability Herba Andrographis solid dispersal powder prepared by formula 1 ~ formula 6 in table 1, drop into respectively in 1000mL drinking water, observe or stir and observe its deployment conditions, dispersion evaluation criterion is as shown in table 2:
Table 2 dispersion evaluation criterion
Sedimentation volume ratio quality evaluation: get each 0.25g of wettability Herba Andrographis solid dispersal powder prepared by formula 1 ~ formula 6, be placed in 50mL tool plug graduated cylinder respectively, add water to 50mL, fill in close, firmly jolting 1min, record suspended matter height, calculated settlement volume ratio respectively.
Computing formula:
Sedimentation volume ratio=H/H0
Wherein, H0 is suspended matter elemental height; H is the height of standing 3 hours suspended matters.
Criterion of acceptability: sedimentation volume ratio >=0.90.
Palatability quality evaluation: the wettability Herba Andrographis solid dispersal powder prepared by formula 1 ~ formula 6 in table 1 is converted drinking water by the concentration of 0.25% respectively, drink for healthy swinery, observe and record swinery and drink situation, choose palatability grade, evaluation criterion is as shown in table 3.
Table 3 Palatability evaluation standard
opinion rating evaluation criterion
excellent when providing the drinking-water of dosing, swinery is induced by abnormal smells from the patient, initiatively fights for and drinks.
good when providing the drinking-water of dosing, swinery is drunk by daily drinking habit.
difference when providing the drinking-water of dosing, swinery refusal is drunk or the amount of drinking declines relatively usually.
Drug loading quality evaluation: according to creat extract dosage and the wettability Herba Andrographis solid dispersal powder total drug loading made, computing formula is as follows:
Result of the test is as shown in table 4:
Table 4 wettability Herba Andrographis solid dispersal powder quality evaluation result
Evaluation index listed by his-and-hers watches 4 is carried out comprehensive analysis and can be obtained: by the wettability Herba Andrographis solid dispersal dressing sieve choosing obtained to formula 1 ~ formula 6, obtain be uniformly dispersed, sedimentation velocity is slow, good palatability, drug loading are large wettability Herba Andrographis solid dispersal powder, the wettability Herba Andrographis solid dispersal powder that wherein formula 1 ~ formula 5 is obtained all reaches qualified level, be optimum again with formula 4.
As can be seen here, wettability Herba Andrographis solid dispersal powder provided by the invention is uniformly dispersed in water, stable, and the mode administration that drinking-water can be adopted to add, greatly reduces the working strength of administration; And wettability Herba Andrographis solid dispersal powder good palatability, not only may be used for chicken etc. and to have a bad nose quick animal, also can be applicable to the sharp-nosed animals such as pig, applied widely; Wettability Herba Andrographis solid dispersal powder has the effect of food calling when being applied to the sharp-nosed animals such as pig; In addition wettability Herba Andrographis solid dispersal powder drug loading is large,
Improve the bioavailability of medicine, reduce side effects of pharmaceutical drugs.
The preparation of embodiment 2 wettability Herba Andrographis solid dispersal powder
Formula:
Get Herba Andrographis, extract 2 times, 3h/ time with 60% ethanol, 40 DEG C ~ 45 DEG C heat-insulation soakings, for the first time 10 times amount, second time 8 times amount.Merge extractive liquid, filter, reduction vaporization is concentrated into the concentrated solution that every gram is equivalent to 3g crude drug; Add DM-β-CD while hot, be stirred to dissolve, with sucrose, moistening soft material is made in mixing, and 35 DEG C of oven dry of ventilating, add Pulvis Talci, xanthan gum, mixing, pulverize, obtain wettability Herba Andrographis solid dispersal powder of the present invention.
The preparation of embodiment 3 wettability Herba Andrographis solid dispersal powder
Formula:
Get Herba Andrographis, adjust the aqueous alkali of pH=8 with sodium carbonate, keep slight boiling condition to decoct extraction 3 times, 30min/ time, merge extractive liquid, reduction vaporization is concentrated into the concentrated solution that every gram is equivalent to 3g crude drug, add DM-β-CD while hot, be stirred to dissolve, with tannic acid, anhydrous glucose, moistening soft material is made in mixing, 40 DEG C of oven dry of ventilating, add neotame, glucide, phosphatidic acid, Pulvis Talci, xanthan gum, mixing, pulverize, obtain wettability Herba Andrographis solid dispersal powder of the present invention.
The preparation of embodiment 4 wettability Herba Andrographis solid dispersal powder
Formula:
Get Herba Andrographis, extract 2 times, 3h/ time with 60% ethanol, 40 DEG C ~ 45 DEG C heat-insulation soakings, for the first time 10 times amount, second time 8 times amount.Merge extractive liquid, filter, reduction vaporization is concentrated into the concentrated solution that every gram is equivalent to 3g crude drug, adds DM-β-CD while hot, be stirred to dissolve, add sodium dihydrogen phosphate, moistening soft material is made in mixing, 45 DEG C of oven dry of ventilating, add sucralose, neotame, aspartame, Pulvis Talci, xanthan gum, mixing, pulverizes, obtains wettability Herba Andrographis solid dispersal powder of the present invention.
The preparation of embodiment 5 wettability Herba Andrographis solid dispersal powder
Formula:
Get Herba Andrographis, adjust the aqueous alkali of pH=8 with sodium carbonate, keep slight boiling condition to decoct extraction 3 times, 30min/ time, merge extractive liquid, reduction vaporization is concentrated into the concentrated solution that every gram is equivalent to 3g crude drug, adds DM-β-CD while hot, is stirred to dissolve; Get 2,6-di-tert-butyl-4-methy phenol, be added in extracting solution after dissolving with dehydrated alcohol 2000mL, mixing, with sucrose, moistening soft material is made in mixing, and 50 DEG C of oven dry of ventilating, add Pulvis Talci, xanthan gum, mixing, pulverizes, obtains wettability Herba Andrographis solid dispersal powder of the present invention.
The preparation of embodiment 6 wettability Herba Andrographis solid dispersal powder
Formula:
Get Herba Andrographis, the aqueous alkali of pH=8 is adjusted with sodium carbonate, slight boiling condition is kept to decoct extraction 3 times, 30min/ time, merge extractive liquid, reduction vaporization is concentrated into the concentrated solution that every gram is equivalent to 3g crude drug, add DM-β-CD while hot, be stirred to dissolve, get 2, 6-di-tert-butyl-4-methy phenol, be added in extracting solution after dissolving with dehydrated alcohol 2000mL, mixing, add tannic acid, anhydrous glucose, moistening soft material is made in mixing, 55 DEG C of oven dry of ventilating, add sucralose, Pulvis Talci, xanthan gum, mixing, pulverize, obtain wettability Herba Andrographis solid dispersal powder of the present invention.
The preparation of embodiment 7 wettability Herba Andrographis solid dispersal powder
Formula:
Get Herba Andrographis, extract 2 times, 3h/ time with 60% ethanol, 40 DEG C ~ 45 DEG C heat-insulation soakings, for the first time 10 times amount, second time 8 times amount.Merge extractive liquid, filter, reduction vaporization is concentrated into the concentrated solution that every gram is equivalent to 3g crude drug, adds DM-β-CD while hot, is stirred to dissolve; Get 2,6-di-tert-butyl-4-methy phenol, be added in extracting solution after dissolving with dehydrated alcohol 2000mL, mixing, adds tannic acid, sodium dihydrogen phosphate, moistening soft material is made in mixing, 60 DEG C of oven dry of ventilating, add phosphatidic acid, Pulvis Talci, xanthan gum, mixing, pulverize, obtain wettability Herba Andrographis solid dispersal powder of the present invention.
The preparation of embodiment 8 wettability Herba Andrographis solid dispersal powder
Formula:
Get Herba Andrographis, adjust the aqueous alkali of pH=8 with sodium carbonate, keep slight boiling condition to decoct extraction 3 times, 30min/ time, merge extractive liquid, reduction vaporization is concentrated into the concentrated solution that every gram is equivalent to 3g crude drug, adds DM-β-CD while hot, is stirred to dissolve; Get tannic acid, sucrose, anhydrous glucose, moistening soft material is made in mixing, and 65 DEG C of oven dry of ventilating, add Pulvis Talci, xanthan gum, mixing, pulverize, obtain wettability Herba Andrographis solid dispersal powder of the present invention.
The preparation of embodiment 9 wettability Herba Andrographis solid dispersal powder
Formula:
Get Herba Andrographis, extract 2 times, 3h/ time with 60% ethanol, 40 DEG C ~ 45 DEG C heat-insulation soakings, for the first time 10 times amount, second time 8 times amount.Merge extractive liquid, filter, reduction vaporization is concentrated into the concentrated solution that every gram is equivalent to 3g crude drug, add DM-β-CD while hot, be stirred to dissolve, get 2,6-di-tert-butyl-4-methy phenol, is added in extracting solution after dissolving, mixing with dehydrated alcohol 2000mL, add tannic acid, anhydrous glucose, potassium dihydrogen phosphate, moistening soft material is made in mixing, 50 DEG C of oven dry of ventilating, add aspartame, phosphatidic acid, Pulvis Talci, xanthan gum, mixing, pulverizes, obtains wettability Herba Andrographis solid dispersal powder of the present invention.
The preparation of embodiment 10 wettability Herba Andrographis solid dispersal powder
Formula:
Get Herba Andrographis, the aqueous alkali of pH=8 is adjusted with sodium carbonate, slight boiling condition is kept to decoct extraction 3 times, 30min/ time, merge extractive liquid, reduction vaporization is concentrated into the concentrated solution that every gram is equivalent to 3g crude drug, add DM-β-CD while hot, be stirred to dissolve, get 2, 6-di-tert-butyl-4-methy phenol dehydrated alcohol 2000mL is added in extracting solution after dissolving, mixing, add tannic acid, sucrose, anhydrous glucose, potassium dihydrogen phosphate, moistening soft material is made in mixing, 45 DEG C of oven dry of ventilating, add glucide, phosphatidic acid, Pulvis Talci, xanthan gum, mixing, pulverize, obtain wettability Herba Andrographis solid dispersal powder of the present invention.
The preparation of embodiment 11 wettability Herba Andrographis solid dispersal powder
Formula:
Get Herba Andrographis, the aqueous alkali of pH=8 is adjusted with sodium carbonate, slight boiling condition is kept to decoct extraction 3 times, 30min/ time, merge extractive liquid, reduction vaporization is concentrated into the concentrated solution that every gram is equivalent to 3g crude drug, add DM-β-CD while hot, be stirred to dissolve, get 2, 6-di-tert-butyl-4-methy phenol dehydrated alcohol 2000mL is added in extracting solution after dissolving, mixing, add tannic acid, sucrose, moistening soft material is made in mixing, 40 DEG C of oven dry of ventilating, add neotame, phosphatidic acid, Pulvis Talci, xanthan gum, mixing, pulverize, obtain wettability Herba Andrographis solid dispersal powder of the present invention.
The preparation of embodiment 12 wettability Herba Andrographis solid dispersal powder
Formula:
Get Herba Andrographis, extract 2 times, 3h/ time with 60% ethanol, 40 DEG C ~ 45 DEG C heat-insulation soakings, for the first time 10 times amount, second time 8 times amount.Merge extractive liquid, filter, reduction vaporization is concentrated into the concentrated solution that every gram is equivalent to 3g crude drug, add DM-β-CD while hot, be stirred to dissolve, get 2,6-di-tert-butyl-4-methy phenol, is added in extracting solution after dissolving, mixing with dehydrated alcohol 2000mL, add tannic acid, anhydrous glucose, moistening soft material is made in mixing, 35 DEG C of oven dry of ventilating, add sucralose, phosphatidic acid, Pulvis Talci, xanthan gum, mixing, pulverizes, obtains wettability Herba Andrographis solid dispersal powder of the present invention.
The preparation of embodiment 13 wettability Herba Andrographis solid dispersal powder
Formula:
Get Herba Andrographis, adjust the aqueous alkali of pH=8 with sodium carbonate, keep slight boiling condition to decoct extraction 3 times, 30min/ time, merge extractive liquid, reduction vaporization is concentrated into the concentrated solution that every gram is equivalent to 3g crude drug, transfers 50 DEG C of aeration-dryings to, obtains creat extract; Get 2,6-di-tert-butyl-4-methy phenol, dehydrated alcohol 200L mixes, add DM-β-CD, tannic acid mixing, be stirred to dissolve, add creat extract, potassium dihydrogen phosphate, mixing, makes moistening soft material, 50 DEG C of oven dry of ventilating, add aspartame, phosphatidic acid, Pulvis Talci, xanthan gum, mixing, pulverizes, obtains wettability Herba Andrographis solid dispersal powder of the present invention.
The preparation of embodiment 14 wettability Herba Andrographis solid dispersal powder
Formula:
Get Herba Andrographis, the aqueous alkali of pH=8 is adjusted with sodium carbonate, slight boiling condition is kept to decoct extraction 3 times, 30min/ time, merge extractive liquid, reduction vaporization is concentrated into the concentrated solution that every gram is equivalent to 3g crude drug, add DM-β-CD while hot, be stirred to dissolve, get 2, 6-di-tert-butyl-4-methy phenol dehydrated alcohol 2000mL is added in extracting solution after dissolving, mixing, add tannic acid, sucrose, moistening soft material is made in mixing, 50 DEG C of oven dry of ventilating, add aspartame, phosphatidic acid, Pulvis Talci, xanthan gum, mixing, pulverize, obtain wettability Herba Andrographis solid dispersal powder of the present invention.
The preparation of embodiment 15 wettability Herba Andrographis solid dispersal powder
Formula:
Get Herba Andrographis, extract 2 times, 3h/ time with 60% ethanol, 40 DEG C ~ 45 DEG C heat-insulation soakings, for the first time 10 times amount, second time 8 times amount.Merge extractive liquid, filter, reduction vaporization is concentrated into the concentrated solution that every gram is equivalent to 3g crude drug, add DM-β-CD while hot, be stirred to dissolve, get 2,6-di-tert-butyl-4-methy phenol dehydrated alcohol 2000mL is added in extracting solution after dissolving, and mixing, adds tannic acid, anhydrous glucose, moistening soft material is made in mixing, 50 DEG C of oven dry of ventilating, add aspartame, phosphatidic acid, Pulvis Talci, xanthan gum, mixing, pulverize, obtain wettability Herba Andrographis solid dispersal powder of the present invention.
The preparation of embodiment 16 wettability Herba Andrographis solid dispersal powder
Formula:
Get creat extract (being equivalent to crude drug 100kg), DM-β-CD, melt as creat extract diluent with 60% ethanol 10L; Get 2,6-di-tert-butyl-4-methy phenol, add in creat extract diluent after dissolving with dehydrated alcohol 2000mL, mixing, adds tannic acid, sodium dihydrogen phosphate, moistening soft material is made in mixing, 50 DEG C of oven dry of ventilating, add aspartame, phosphatidic acid, Pulvis Talci, xanthan gum, mixing, pulverize, obtain wettability Herba Andrographis solid dispersal powder of the present invention.
The preparation of embodiment 17 wettability Herba Andrographis solid dispersal powder
Formula:
Get Herba Andrographis, extract 2 times, 3h/ time with 60% ethanol, 40 DEG C ~ 45 DEG C heat-insulation soakings, for the first time 10 times amount, second time 8 times amount.Merge extractive liquid, filter, reduction vaporization is concentrated into the concentrated solution that every gram is equivalent to 3g crude drug, adds DM-β-CD while hot, be stirred to dissolve, get tannic acid, anhydrous glucose, potassium dihydrogen phosphate, moistening soft material is made in mixing, 50 DEG C of oven dry of ventilating, add aspartame, phosphatidic acid, Pulvis Talci, xanthan gum, mixing, pulverizes, obtains wettability Herba Andrographis solid dispersal powder of the present invention.
The preparation of embodiment 18 wettability Herba Andrographis solid dispersal powder
Formula:
Get Herba Andrographis, adjust the aqueous alkali of pH=8 with sodium carbonate, keep slight boiling condition to decoct extraction 3 times, 30min/ time, merge extractive liquid, reduction vaporization is concentrated into the concentrated solution that every gram is equivalent to 3g crude drug, add DM-β-CD while hot, be stirred to dissolve, get tannic acid, sucrose, anhydrous glucose, potassium dihydrogen phosphate, moistening soft material is made in mixing, 45 DEG C of oven dry of ventilating, add glucide, phosphatidic acid, Pulvis Talci, xanthan gum, mixing, pulverize, obtain wettability Herba Andrographis solid dispersal powder of the present invention.
Embodiment 19 wettability Herba Andrographis solid dispersal powder is to the clinical tests of hyopneumoniae
Select the growing and fattening pigs suffering from pneumonia that body weight is substantially suitable, in same pig house, be divided into following 3 groups under identical rearing conditions at random:
Blank group: establish disease pig 15, by daily feeding manner feedwater feed, not administration, is used in conjunction 7 days.
Positive controls: establish disease pig 16, with tilmicosin pre-mixing agent by 0.01% concentration spice, feeding for sick pig, be used in conjunction 7 days.
Test group: establish disease pig 16, converts drinking water with wettability Herba Andrographis solid dispersal powder prepared by embodiment 16 by 0.13% concentration, drinks, be used in conjunction 7 days for sick pig.
After 7 days, observe disease pig spirit appetite behavior and make statistics, calculate cure rate, obvious effective rate, effective percentage and inefficiency, curative effect determinate standard is as shown in table 5.
Table 5 curative effect determinate standard
therapeutic effect judging index
recovery from illness medication is after 7 days, and spiritual appetite recovers normal.
effective medication is after 7 days, and spiritual appetite takes a turn for the better.
invalid medication is after 7 days, and symptom is not improved.
Computing formula:
Cure rate=recovery from illness case quantity/total cases × 100%
Obvious effective rate=effective case quantity/total cases × 100%
Effective percentage=cure rate+obvious effective rate
Inefficiency=Ineffective Cases quantity/total cases × 100%
Result of the test is as shown in table 6.
Table 6 wettability Herba Andrographis solid dispersal powder is to the clinical tests result of hyopneumoniae
From the result of the test shown in table 6, medication is after 7 days, and blank group effective percentage is 0, and positive controls and test group effective percentage are 100%, shows that tilmicosin pre-mixing agent and wettability Herba Andrographis solid dispersal powder all have good curative effect to hyopneumoniae; And test group cure rate (100%) is significantly higher than the cure rate (81%) of positive controls; Repeatedly repeated trials shows, test repeatability is good.As can be seen here, wettability Herba Andrographis solid dispersal treated powder Be very effective provided by the invention is better than (P < 0.05) tilmicosin pre-mixing agent; In sum, wettability Herba Andrographis solid dispersal powder has good curative effect to hyopneumoniae, and therapeutic effect is significantly better than tilmicosin pre-mixing agent.
Find in process of the test, compared with tilmicosin pre-mixing agent, wettability Herba Andrographis solid dispersal powder provided by the invention is easy to use, add water suspensoid, greatly reduce the working strength of administration; Owing to taking the mode administration added of drinking water, wettability Herba Andrographis solid dispersal powder of the present invention does not in use affect the feed intake of disease pig.
In addition, owing to the addition of bitterness screening agent and bitter inhibitor in wettability Herba Andrographis solid dispersal powder formula, effectively can hide the bitterness of Herba Andrographis, sweeting agent can increase the palatability of medicine further, expand the scope of application of medicine, have food calling effect to sharp-nosed animals such as pigs.
Also add antioxidant in wettability Herba Andrographis solid dispersal powder, effectively can prevent the oxidation of Herba Andrographis effective ingredient andrographolide, improve the stability of medicine, ensure that Drug safety and effectiveness, and be beneficial to preparation and longer-term storage.
Because medicine preparation process adopts solid dispersion technology, in gained wettability Herba Andrographis solid dispersal powder, effective ingredient is uniformly dispersed, and bioavailability is high; And wettability Herba Andrographis solid dispersal powder drug loading is large, improves the bioavailability of medicine, reduces side effects of pharmaceutical drugs.
The wettability Herba Andrographis solid dispersal powder embodiment of the present invention 1 ~ 15 and embodiment 17 ~ 18 provided respectively is applied in the clinical tests test of hyopneumoniae, test method is with embodiment 19, obtained experimental result is similar to embodiment 19 result of the test, and the wettability Herba Andrographis solid dispersal treated powder effect namely provided in other embodiments of the invention is all significantly better than (P < 0.05) tilmicosin pre-mixing agent.
Comprehensive above-mentioned result of the test: the invention provides one and be easy to dispersed in water, be beneficial to the wettability Herba Andrographis solid dispersal powder of drinking water administration, compared with tilmicosin pre-mixing agent, wettability Herba Andrographis solid dispersal treated powder is effective, easy to use; In certain embodiments, owing to adding correctives in formula, improve palatability of drugs, expand the scope of application of medicine; In further embodiments, owing to adding antioxidant in formula, improve the stability of medicine; In addition, because medicine preparation process adopts solid dispersion technology, in gained wettability Herba Andrographis solid dispersal powder, effective ingredient is uniformly dispersed, and bioavailability is high.Wettability Herba Andrographis solid dispersal powder provided by the invention is applicable to the more animal of kind and is applicable to the cultivation of different scales.
Embodiment 20 wettability Herba Andrographis solid dispersal powder is to the clinical tests of broiler Hakuri
Select the sick chicken suffering from broiler Hakuri of 20 ages in days, in same hen house, be divided into following 3 groups under identical rearing conditions at random:
Blank group: negative control group is raised by daily feeding manner, not administration.
Positive controls: to feed commercially available Herba Andrographis end (every 1 gram is equivalent to crude drug in whole 1g) by 2g/ plumage dosage spice, every day 2 times, be used in conjunction 3 days;
Test group: supply drink by 1g/ plumage dosage after the wettability Herba Andrographis solid dispersal powder that (every 1 gram is equivalent to crude drug in whole 2g) is prepared by test group embodiment 16 is watered, every day 2 times, be used in conjunction 3 days;
Efficacy determination method: medication is after 3 days, and observe disease chicken spirit appetite behavior and make statistics, calculate cure rate, obvious effective rate, effective percentage and inefficiency, curative effect determinate standard is as shown in table 7.
Table 7 curative effect determinate standard
therapeutic effect judging index
recovery from illness after 3 days, spiritual appetite recovers normal, clinical symptom disappearance.
effective after 3 days, spiritual appetite takes a turn for the better, clinical symptom disappearance or alleviate.
invalid after 3 days, symptom is not improved.
Computing formula:
Cure rate=recovery from illness case quantity/total cases × 100%
Obvious effective rate=effective case quantity/total cases × 100%
Effective percentage=cure rate+obvious effective rate
Inefficiency=Ineffective Cases quantity/total cases × 100%
Result of the test is as shown in table 8.
Table 8 wettability Herba Andrographis solid dispersal powder is to the clinical tests result of broiler Hakuri
From the result of the test shown in table 8, medication is after 3 days, and blank group effective percentage is 0, and positive controls and test group effective percentage are 100%, shows that commercially available Herba Andrographis end and wettability Herba Andrographis solid dispersal powder all have good curative effect to broiler Hakuri; And test group cure rate (89%) is significantly higher than the cure rate (60%) of positive controls; Repeatedly repeated trials shows, test repeatability is good.As can be seen here, wettability Herba Andrographis solid dispersal treated powder Be very effective provided by the invention is better than (P < 0.05) commercially available Herba Andrographis end; In sum, wettability Herba Andrographis solid dispersal powder has good curative effect to broiler Hakuri, and therapeutic effect is significantly better than commercially available Herba Andrographis end.
Find in process of the test, relatively commercially available Herba Andrographis end spice administering mode, wettability Herba Andrographis solid dispersal powder provided by the invention, by drinking-water dispensing, saves spice process, greatly reduces dispensing labor intensity.
In addition, owing to the addition of bitterness screening agent and bitter inhibitor in wettability Herba Andrographis solid dispersal powder formula, effectively can hide the bitterness of Herba Andrographis, sweeting agent can increase the palatability of medicine further, expands the scope of application of medicine.
Also add antioxidant in wettability Herba Andrographis solid dispersal powder, effectively can prevent the oxidation of Herba Andrographis effective ingredient andrographolide, improve the stability of medicine, ensure that Drug safety and effectiveness, and be beneficial to preparation and longer-term storage.
Because medicine preparation process adopts solid dispersion technology, in gained wettability Herba Andrographis solid dispersal powder, effective ingredient is uniformly dispersed, and bioavailability is high.And wettability Herba Andrographis solid dispersal powder drug loading is large, improves the bioavailability of medicine, reduces side effects of pharmaceutical drugs.
The wettability Herba Andrographis solid dispersal powder embodiment of the present invention 1 ~ 15 and embodiment 17 ~ 18 provided respectively is applied in the clinical tests test of broiler Hakuri, test method is with embodiment 20, obtained experimental result is similar to embodiment 20 result of the test, and the wettability Herba Andrographis solid dispersal treated powder effect namely provided in other embodiments of the invention is all significantly better than (P < 0.05) commercially available Herba Andrographis end.
Comprehensive above-mentioned result of the test: the invention provides one and be easy to dispersed in water, be beneficial to the wettability Herba Andrographis solid dispersal powder of drinking water administration, compared with commercially available Herba Andrographis end, wettability Herba Andrographis solid dispersal treated powder is effective, easy to use, in certain embodiments, owing to adding correctives in formula, improve palatability of drugs, expand the scope of application of medicine, in certain embodiments, owing to adding antioxidant in formula, improve the stability of medicine; In addition, because medicine preparation process adopts solid dispersion technology, in gained wettability Herba Andrographis solid dispersal powder, effective ingredient is uniformly dispersed, and bioavailability is high.Wettability Herba Andrographis solid dispersal powder provided by the invention is applicable to a greater variety of animal and is applicable to the cultivation of different scales.
Below be only the preferred embodiment of the present invention; it should be pointed out that for those skilled in the art, under the premise without departing from the principles of the invention; can also make some improvements and modifications, these improvements and modifications also should be considered as protection scope of the present invention.

Claims (10)

1. a wettability Herba Andrographis solid dispersal powder, is characterized in that, it comprises the raw material of following weight portion:
Described cyclodextrin is DM-β-CD; Described carrier is sodium dihydrogen phosphate; Described suspending agent is xanthan gum.
2. wettability Herba Andrographis solid dispersal powder according to claim 1, it is characterized in that, described raw material also comprises correctives.
3. wettability Herba Andrographis solid dispersal powder according to claim 2, is characterized in that, described correctives is a kind of or both the above mixture in sweeting agent, bitterness screening agent, bitter inhibitor.
4. wettability Herba Andrographis solid dispersal powder according to claim 3, it is characterized in that, it comprises the raw material of following weight portion:
5. the wettability Herba Andrographis solid dispersal powder according to any one of Claims 1 to 4, it is characterized in that, described raw material also comprises antioxidant.
6. wettability Herba Andrographis solid dispersal powder according to claim 5, it is characterized in that, it comprises the raw material of following weight portion:
7. a preparation method for wettability Herba Andrographis solid dispersal powder as claimed in claim 1, is characterized in that, comprise the following steps:
A) raw material of following weight portion is taken respectively:
B) get described Herba Andrographis solvent extraction, obtain extracting solution;
C) get described extracting solution to concentrate, mix with described cyclodextrin, dehydrated alcohol, described carrier, 35 DEG C ~ 65 DEG C dryings, then mix with described Pulvis Talci, described suspending agent, pulverize, to obtain final product.
8. a preparation method for wettability Herba Andrographis solid dispersal powder as claimed in claim 4, is characterized in that, comprise the following steps:
A) raw material of following weight portion is taken respectively:
B) get described Herba Andrographis solvent extraction, obtain extracting solution;
C) get described extracting solution to concentrate, mix with described cyclodextrin, described bitterness screening agent, described carrier, 35 DEG C ~ 65 DEG C dryings, then mix with described sweeting agent, described bitter inhibitor, described Pulvis Talci, described suspending agent, pulverize, to obtain final product.
9. a preparation method for wettability Herba Andrographis solid dispersal powder as claimed in claim 6, is characterized in that, comprise the following steps:
A) raw material of following weight portion is taken respectively:
B) get described Herba Andrographis solvent extraction, obtain extracting solution;
C) get described extracting solution to concentrate, add described cyclodextrin, obtain mixture;
D) described antioxidant, dehydrated alcohol mixing is got, mix with described mixture, described bitterness screening agent, described carrier again, 35 DEG C ~ 65 DEG C dryings, then mix with described sweeting agent, described bitter inhibitor, described Pulvis Talci, described suspending agent, pulverize, to obtain final product.
10. the preparation method of wettability Herba Andrographis solid dispersal powder according to claim 1, is characterized in that, comprise the following steps:
A) raw material of following weight portion is taken respectively:
B) get described Herba Andrographis solvent extraction, obtain extracting solution;
C) get described extracting solution to concentrate, dry, obtain creat extract;
D) get described cyclodextrin, described creat extract, dehydrated alcohol, the mixing of described carrier, 35 DEG C ~ 65 DEG C dryings, then mix with described Pulvis Talci, described suspending agent, pulverize, to obtain final product.
CN201310682233.XA 2013-12-12 2013-12-12 A kind of wettability Herba Andrographis solid dispersal powder and preparation method thereof Expired - Fee Related CN103623019B (en)

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Publication number Priority date Publication date Assignee Title
CN1989960A (en) * 2005-12-29 2007-07-04 江西本草天工科技有限责任公司 Andrographolide dispersed tablet
CN101693113A (en) * 2009-10-21 2010-04-14 严洁 Divalproex sodium medicine composition with improved oral absorptivity

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1989960A (en) * 2005-12-29 2007-07-04 江西本草天工科技有限责任公司 Andrographolide dispersed tablet
CN101693113A (en) * 2009-10-21 2010-04-14 严洁 Divalproex sodium medicine composition with improved oral absorptivity

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