Chinese juniper beach wormwood Bulbus Allii Macrostemonis Rhizoma Pinelliae oral formulations and preparation method thereof
Technical field
The invention belongs to medical technical field, be specifically related to a kind of unable to tie down due to obstruction of QI in the chest that cures mainly, oral formulations of chest pain radiating to the back and preparation method thereof, particularly the extract with Chinese juniper beach wormwood Bulbus Allii Macrostemonis Rhizoma Pinelliae Chinese medicine prescription is the oral formulations of active constituents of medicine.
Background technology
" Chinese juniper beach wormwood Bulbus Allii Macrostemonis Rhizoma Pinelliae soup " is initiative in " Medical Treasures of the Golden Chamber " of Han dynasty Zhang Zhongjing book, the representative prescription that the treatment obstruction of qi in the chest and cardialgia must not crouch, formed by Chinese juniper beach wormwood, Bulbus Allii Macrostemonis, the Rhizoma Pinelliae, Chinese liquor, has the migratory arthralgia of activating yang, by the effect of drink sending down the abnormal ascending QI, cure mainly sun and let out turbid, eliminating phlegm relieving accumulation of pathogens card, the original text cloud: " unable to tie down due to obstruction of QI in the chest; chest pain radiating to the back person, Chinese juniper beach wormwood Bulbus Allii Macrostemonis Rhizoma Pinelliae master it." hypofunction of YANG QI in chest, diseases caused by retention of fluid knot is poly-, the turbid heap soil or fertilizer over and around the roots resistance of expectorant, mechanism of qi is obstructed, and causes chest pain radiating to the back, in addition can not put down for sleeping in, so control with the Chinese juniper beach wormwood Bulbus Allii Macrostemonis Rhizoma Pinelliae.This prescription has been widely used in various cardiovascular disease, as: arrhythmia, pulmonary heart disease, diastole rhythm of the heart failure, heart neurosis, cardiomyopathy, coronary heart disease etc. have all been received good curative effect, and all get at aspects such as theory, experiment, pharmacology and clinical practices gratifying achievement, its purposes is " Medical Treasures of the Golden Chamber " scope of being put down in writing head and shoulders above.
The source of the Chinese crude drug of " Chinese juniper beach wormwood Bulbus Allii Macrostemonis Rhizoma Pinelliae soup " is as follows:
The Chinese juniper beach wormwood: the mature peel of Cucurbitaceae liana Chinese juniper beach wormwood or bilateral Chinese juniper beach wormwood, have coronary artery dilating, antithrombotic resists myocardial ischemia, microcirculation improvement, pharmacological functions such as slow down aging,
Bulbus Allii Macrostemonis: the dry bulb for the liliaceous plant Allium macrostemon, activating YANG and eliminating stagnation is arranged, the effect of circulation of qi promoting intestinal stasis relieving,
The Rhizoma Pinelliae: the tuber for the aroid Rhizoma Pinelliae, drying dampness to eliminate phlegm is arranged, stopping nausea and vomiting by lowering the adverse flow of QI, the effect of dissolving lump and resolving mass,
The Chinese juniper beach wormwood is used for the chest stuffiness relieving eliminating phlegm in the side, the hot temperature of Bulbus Allii Macrostemonis, and with a surname's numbness of activating yang, promptly " the Zhang Shi doctor is logical " is said: " Chinese juniper beach wormwood profit is in order to wash the greasy expectorant of dirt; Bulbus Allii Macrostemonis is smelly dirty, and in order to logical foul gas, People of the same tastes and habits like to be together also." the hot temperature of the Rhizoma Pinelliae, give birth to wet in order to dry spleen.Capable the stagnating of the smooth blood of Chinese liquor in the side.All medicines are harmonious, and playing altogether activates yang lets out effect turbid, the eliminating phlegm relieving accumulation of pathogens.
" the Chinese juniper beach wormwood Bulbus Allii Macrostemonis Rhizoma Pinelliae soup " in ancient times has only decoction, decoct behind the needs purchase decoction pieces and take, carry take all very inconvenient, we quantitatively control by index components and make the modern Chinese medicine oral formulations through studying, and product dosage is accurate, steady quality, conveniently take, be applicable to the big production of commercialization, overcome that the Chinese medicine decoction consumption is big, consumption is inaccurate, carry take inconvenience, can't commercialization etc. shortcoming, the needs that make things convenient for clinical treatment and family to use.
Summary of the invention
The objective of the invention is to preparation method according to modern Chinese medicine, quantitatively control by index components and to make the modern Chinese medicine oral formulations, with the Chinese juniper beach wormwood Bulbus Allii Macrostemonis Rhizoma Pinelliae be developed to product dosage accurately, steady quality, conveniently take, be applicable to the Chinese patent medicine of the big production of commercialization, make things convenient for clinical treatment and family to use.
The medicine of oral formulations involved in the present invention is by the Chinese juniper beach wormwood, Bulbus Allii Macrostemonis, the Rhizoma Pinelliae, the mixed extract of Chinese liquor (extractum or dry powder) is a raw material, with as the pharmaceutically acceptable carrier of substrate or excipient routinely prepared form, owing to record " the Chinese juniper beach wormwood Bulbus Allii Macrostemonis Rhizoma Pinelliae " recipe quantity in the different medical books be: real one piece of Chinese juniper beach wormwood, three liang of Bulbus Allii Macrostemonis, half jin of the Rhizoma Pinelliae, Chinese liquor are a pipeful of, and each flavour of a drug is converted to weight fraction (unit is g or kg) and is:
Chinese juniper beach wormwood 5-15, Bulbus Allii Macrostemonis 10-15 part, Rhizoma Pinelliae 25-50 part, Chinese liquor 150-200 part
Substrate: the common medicinal supplementary material in the medicament book in preparation oral administration solid and the liquid preparation;
Proportioning: extract (extractum or dry powder): substrate=9: 1~1: 9.
The extraction process of the present invention's " Chinese juniper beach wormwood Bulbus Allii Macrostemonis Rhizoma Pinelliae " mixed extract is as follows:
(1) each flavor medical material is cleaned, take by weighing each medical material and added 6~20 times of amount soaking in Chinese liquor 2-12 hour by best deal, heating extraction 2-3 time, extracting solution merges;
(2) Chinese liquor extraction liquid left standstill 12-48 hour, crossed the leaching supernatant, and concentrating under reduced pressure gets extractum or spray drying, and to get dry powder be the Chinese liquor extraction thing;
(3) " the Chinese juniper beach wormwood Bulbus Allii Macrostemonis Rhizoma Pinelliae " extract and pharmaceutically acceptable carrier or excipient composition routinely technology make various oral administration solids or liquid preparation, wherein said carrier or excipient pharmaceutically selected according to different dosage forms, and these used carriers or excipient can determine for the those of ordinary skill of pharmaceutical field.
The extracting method of the present invention's " Chinese juniper beach wormwood Bulbus Allii Macrostemonis Rhizoma Pinelliae " extract is a lot, has only provided a kind of method here, but has been not limited to this kind method.
Medicine of the present invention, wherein dosage form comprises oral solid formulation and oral liquid, wherein oral solid formulation comprises: tablet, hard capsule, liquid type capsule, granule, soft capsule, drop pill, pill, pellet, slow releasing preparation; Oral liquid comprises: oral liquid, syrup, medicated wine; Granule wherein, oral liquid, hard capsule and additive of tablet are selected from starch, sodium bicarbonate, Icing Sugar, lactose, amylum pregelatinisatum, microcrystalline Cellulose, inorganic salts mainly is some inorganic calcium salts, as calcium sulfate, citric acid, calcium hydrogen phosphate and medicinal calcium carbonate, mannitol, starch slurry, sodium carboxymethyl cellulose, hydroxypropyl cellulose, methylcellulose and ethyl cellulose, hydroxypropyl emthylcellulose, hypromellose, other binding agent, dried starch, carboxymethyl starch sodium, low-substituted hydroxypropyl cellulose, polyethylene compares pyrrolidone, cross-linking sodium carboxymethyl cellulose, magnesium stearate, micropowder silica gel, Pulvis Talci, hydrogenated vegetable oil, in polyethylene glycols (Macrogol 2000-6000) and month pure magnesium sulfate of extension and the xylitol one or more; Wherein the adjuvant of soft capsule, liquid type capsule and drop pill is selected from Polyethylene Glycol (Macrogol 200-6000), propylene glycol, Cera Flava, Lac, polyoxyethylene monostearate, glycerol, ethanol, (polysorbas20,40,60,65,80), spans (span 20,40,60,65,80), soybean oil, Oleum Camelliae, safflower oil, Radix Oenotherae erythrosepalae oil, olive oil, C
5-C
14Triglyceride, in the ethyl oleate one or more, can also dose antioxidant, be selected from alpha-tocopherol, ascorbyl palmitate, Butylated hydroxyanisole (BHA), the dibenzylatiooluene (BHT) one or more.
Pharmaceutical preparation of the present invention, wherein tablet specifically refers to common compressed tablet, coated tablet, coated tablet, Film coated tablets, enteric coated tablet, effervescent tablet, chewable tablet, multilayer tablet, dispersible tablet, Sublingual tablet, buccal tablet.
Pharmaceutical preparation of the present invention wherein can also contain aromatic and antiseptic, and wherein aromatic comprises one or more in Fructus Citri tangerinae essence, flavoring banana essence, strawberry essence, the cream flavour, and antiseptic comprises one or more in parabens, the benzoic acids.
" the Chinese juniper beach wormwood Bulbus Allii Macrostemonis Rhizoma Pinelliae " method for preparing extractive is as follows:
Prescription: Chinese juniper beach wormwood 10-30 part, Bulbus Allii Macrostemonis 5-15 part, Rhizoma Pinelliae 2-15 part
Method for making: the medical material of respectively distinguishing the flavor of of will writing out a prescription cleans, and takes by weighing each medical material of recipe quantity and adds 6~20 times of amount soaking in Chinese liquor 2-12 hour, heating extraction 2-3 time, extracting solution merging; Chinese liquor extraction liquid left standstill 12-48 hour, crossed the leaching supernatant, and concentrating under reduced pressure gets extractum or spray drying is that dry powder is that the Chinese liquor extraction thing is standby.
Preparation " the Chinese juniper beach wormwood Bulbus Allii Macrostemonis Rhizoma Pinelliae " oral liquid and mixture
" the Chinese juniper beach wormwood Bulbus Allii Macrostemonis Rhizoma Pinelliae " extract and correctives, antiseptic and water are made oral liquid, and wherein correctives is selected from one or more in sucrose, saccharin sodium, sodium cyclamate, stevioside, aspartoyl aminotoluene acid methyl ester, the Oleum menthae (alcohol); Antiseptic is selected from sorbic acid methyl ester, benzoic acids, you moor in golden class etc. one or more.
The preparation method of oral liquid and mixture is as follows: extract adds water and Chinese liquor is adjusted to preparation amount " the Chinese juniper beach wormwood Bulbus Allii Macrostemonis Rhizoma Pinelliae ", add correctives, antiseptic mix homogeneously, through technologies such as sterilization, fill, check, packings, promptly get Chinese juniper beach wormwood Bulbus Allii Macrostemonis Rhizoma Pinelliae oral liquid and mixture.
Wherein the weight percent content of Jia Ruing is: " the Chinese juniper beach wormwood Bulbus Allii Macrostemonis Rhizoma Pinelliae " extract 5-80%, correctives 0, and 05-5%, antiseptic 0,001-2%, water 10-90%,
Preparation " the Chinese juniper beach wormwood Bulbus Allii Macrostemonis Rhizoma Pinelliae " granule, pill, pellet, capsule, tablet
Granule, pill, pellet, capsule, and tablet are made the used adjuvant of concentrated granule or pill or tablet and are comprised diluent, binding agent, lubricant; Diluent is selected from one or more of starch, lactose, dextrin, microcrystalline Cellulose kind; Binding agent comprise water, macromolecular material and alcoholic acid one or more; Lubricant comprises one or more in magnesium stearate, Pulvis Talci, the stearic acid.
Granule, pill, pellet, capsule, and the preparation method of tablet as follows:
With " the Chinese juniper beach wormwood Bulbus Allii Macrostemonis Rhizoma Pinelliae " extract and an amount of pharmaceutic adjuvant mixing, adding binding agent etc. is made soft material, makes granule with granulator; dry, granulate promptly gets granule; or the general pill of making, or make capsule through capsule filling machine, or make tablet through tabletting.
Granule, pill, pellet, capsule, and tablet, wherein every gram granule is equivalent to contain 0, the crude drug amount of 1-10 gram.
Preparation " the Chinese juniper beach wormwood Bulbus Allii Macrostemonis Rhizoma Pinelliae " soft capsule
With " the Chinese juniper beach wormwood Bulbus Allii Macrostemonis Rhizoma Pinelliae " extract and adjuvant diluent, antioxidant, antiseptic, suspending agent, wherein diluent is selected from one or more in Polyethylene Glycol, propylene glycol, vegetable oil, the mineral oil; Antioxidant is selected from that glycine, vitamin E and derivant thereof, ascorbic acid, pyrosulfurous acid are received, in the potassium metabisulfite one or more; Antiseptic comprises sorbic acid methyl ester, benzoic acids, you moor in golden class etc. one or more; Suspending agent is selected from one or more in chitin, cellulose family, agar, the Cera Flava.
Preparation method is as follows: " the Chinese juniper beach wormwood Bulbus Allii Macrostemonis Rhizoma Pinelliae " extract 5-50%, add an amount of diluent, antioxidant, antiseptic, suspending agent mix homogeneously, prepared forms routinely, and wherein every gram soft capsule is equivalent to contain 0, the crude drug amount of 1-10 gram.
Specific embodiment
Embodiment one: " the Chinese juniper beach wormwood Bulbus Allii Macrostemonis Rhizoma Pinelliae " extract 1 (extractum) preparation method
Prescription: Chinese juniper beach wormwood 30g, Bulbus Allii Macrostemonis 6g, Rhizoma Pinelliae 10g
Method for making: the medical material of respectively distinguishing the flavor of of will writing out a prescription cleans, and takes by weighing each medical material by recipe quantity, adds 6~15 times of amount soaking in Chinese liquor 2-10 hour, heat little boiling and extracts 2-3 time, the extracting solution merging; Extracting solution left standstill 12-48 hour, crossed the leaching supernatant, and concentrating under reduced pressure gets extractum and is the about 7.2g of Chinese liquor extraction thing.
Embodiment two: " the Chinese juniper beach wormwood Bulbus Allii Macrostemonis Rhizoma Pinelliae " extract 2 (dry powder) preparation method
Prescription: Chinese juniper beach wormwood 30g, Bulbus Allii Macrostemonis 15g, Rhizoma Pinelliae 10g
Method for making: the medical material of respectively distinguishing the flavor of of will writing out a prescription cleans, and takes by weighing each medical material by recipe quantity, adds 8~10 times of amount soaking in Chinese liquor 2-8 hour, and being heated to boils extracts 2-3 time, the extracting solution merging; Extracting solution left standstill 12-48 hour, crossed the leaching supernatant, concentrating under reduced pressure, and spray drying gets dry powder and is the about 12.0g of Chinese liquor extraction thing.
Embodiment three: " the Chinese juniper beach wormwood Bulbus Allii Macrostemonis Rhizoma Pinelliae " oral solid formulation preparation method
(1) preparation " the Chinese juniper beach wormwood Bulbus Allii Macrostemonis Rhizoma Pinelliae " granule
Prescription:
" the Chinese juniper beach wormwood Bulbus Allii Macrostemonis Rhizoma Pinelliae " extract 1 10-90%
Starch 5.0-70%
Dextrin 2.0-20%
Xylitol 5.0-20%
Sorbic acid methyl ester 0.001-2,0%
Optimizing prescriptions:
" the Chinese juniper beach wormwood Bulbus Allii Macrostemonis Rhizoma Pinelliae " extract 1 7.2g
Starch 3.0g
Dextrin 3.0g
Xylitol 2.0g
Sorbic acid methyl ester 0.002g
Method for making: press method preparation " the Chinese juniper beach wormwood Bulbus Allii Macrostemonis Rhizoma Pinelliae " extract among the embodiment one, add the recipe quantity adjuvant and make granule according to a conventional method, an amount of dissolve with ethanol of volatile oil evenly is sprayed on the granule, cold drying, and packing is made.
(2) preparation " the Chinese juniper beach wormwood Bulbus Allii Macrostemonis Rhizoma Pinelliae " tablet:
(1) ordinary tablet prescription:
" the Chinese juniper beach wormwood Bulbus Allii Macrostemonis Rhizoma Pinelliae " extract 2 5.0-90%
Starch 5.0-50%
Dextrin 2.0-20%
Microcrystalline Cellulose 5.0-20%
Pulvis Talci 0.5-5.0%
Magnesium stearate 0.1-5.0%
Optimizing prescriptions:
" the Chinese juniper beach wormwood Bulbus Allii Macrostemonis Rhizoma Pinelliae " extract 2 12g
Starch 4g
Dextrin 3g
Microcrystalline Cellulose 2g
Pulvis Talci 0.2g
Magnesium stearate 0.1g
Method for making: press method preparation " the Chinese juniper beach wormwood Bulbus Allii Macrostemonis Rhizoma Pinelliae " extract among the embodiment two, add the recipe quantity adjuvant and make granule according to a conventional method, an amount of dissolve with ethanol of volatile oil evenly is sprayed on the granule, cold drying, and tabletting is promptly.
(2) effervescent tablet is write out a prescription and is prepared as follows:
Prescription: " the Chinese juniper beach wormwood Bulbus Allii Macrostemonis Rhizoma Pinelliae " extract 2 12g
Starch 2g
Dextrin 2g
Microcrystalline Cellulose 1g
Pulvis Talci 0.1g
Magnesium stearate 0.5g
Anhydrous citric acid 1.0g
Sodium bicarbonate 1.0g
Lactose 0.5g
Water is an amount of
Method for making: press method preparation " the Chinese juniper beach wormwood Bulbus Allii Macrostemonis Rhizoma Pinelliae " extract among the embodiment two, add the recipe quantity adjuvant and make granule according to a conventional method, an amount of dissolve with ethanol of volatile oil evenly is sprayed on the granule, cold drying, and tabletting is promptly.
(3) buccal tablet is write out a prescription and is prepared as follows:
Prescription: " the Chinese juniper beach wormwood Bulbus Allii Macrostemonis Rhizoma Pinelliae " extract 2 12g
Starch 2g
Dextrin 3g
Microcrystalline Cellulose 1g
Pulvis Talci 0.1g
Magnesium stearate 0.1g
Citric acid 0.1g
Aspartame 0.02g
Water is an amount of
Method for making: press method preparation " the Chinese juniper beach wormwood Bulbus Allii Macrostemonis Rhizoma Pinelliae " extract among the embodiment two, add the recipe quantity adjuvant and make granule according to a conventional method, an amount of dissolve with ethanol of volatile oil evenly is sprayed on the granule, cold drying, and tabletting is promptly.
(4) coated tablet is write out a prescription and is prepared as follows:
Prescription: " the Chinese juniper beach wormwood Bulbus Allii Macrostemonis Rhizoma Pinelliae " extract 2 12g
Starch 3g
Dextrin 2g
Microcrystalline Cellulose 2g
Pulvis Talci 0.1g
Magnesium stearate 0.1g
Method for making: press method preparation " the Chinese juniper beach wormwood Bulbus Allii Macrostemonis Rhizoma Pinelliae " extract among the embodiment two, add the recipe quantity adjuvant and make granule according to a conventional method, the an amount of dissolve with ethanol of volatile oil, evenly be sprayed on the granule, cold drying, tabletting is made coating material according to conventional method, with coating machine coating promptly, the difference according to coating material can be bundled into sugar-coat and film-coat.
(3) preparation " the Chinese juniper beach wormwood Bulbus Allii Macrostemonis Rhizoma Pinelliae " pill
Prescription:
" the Chinese juniper beach wormwood Bulbus Allii Macrostemonis Rhizoma Pinelliae " extract 2 12g
Starch 3g
Magnesium stearate 0.1g
Dextrin 3g
Water is an amount of
Method for making: press method preparation " the Chinese juniper beach wormwood Bulbus Allii Macrostemonis Rhizoma Pinelliae " extract among the embodiment two, add the recipe quantity adjuvant and make granule according to a conventional method, an amount of dissolve with ethanol of volatile oil evenly is sprayed on the granule, cold drying, and pelleting is promptly.
(4) preparation " the Chinese juniper beach wormwood Bulbus Allii Macrostemonis Rhizoma Pinelliae " soft capsule
The content prescription:
" the Chinese juniper beach wormwood Bulbus Allii Macrostemonis Rhizoma Pinelliae " extract 2 12g
Vegetable oil 10g
Ethylparaben 0.01g
Cera Flava 2g
Method for making: press method preparation " the Chinese juniper beach wormwood Bulbus Allii Macrostemonis Rhizoma Pinelliae " extract among the embodiment two, add vegetable oil, the Cera Flava of optimizing prescriptions percentage amounts, ethylparaben prepared routinely forms.
(5) preparation " the Chinese juniper beach wormwood Bulbus Allii Macrostemonis Rhizoma Pinelliae " capsule
Prescription:
" the Chinese juniper beach wormwood Bulbus Allii Macrostemonis Rhizoma Pinelliae " extract 2 10-95%
Starch 5-55%
Magnesium stearate 0.1-5%
Optimizing prescriptions:
" the Chinese juniper beach wormwood Bulbus Allii Macrostemonis Rhizoma Pinelliae " extract 2 12g
Starch 5g
Magnesium stearate 0.5g
Method for making: press method preparation " the Chinese juniper beach wormwood Bulbus Allii Macrostemonis Rhizoma Pinelliae " extract among the embodiment two, add the recipe quantity adjuvant and make granule according to a conventional method, an amount of dissolve with ethanol of volatile oil evenly is sprayed on the granule, and cold drying, fill are promptly.
Embodiment four: " the Chinese juniper beach wormwood Bulbus Allii Macrostemonis Rhizoma Pinelliae " oral liquid preparation method
Prescription: " the Chinese juniper beach wormwood Bulbus Allii Macrostemonis Rhizoma Pinelliae " extract 2 5-80%
Chinese liquor 5.0-50%
Distilled water 10-90%,
Optimizing prescriptions:
" the Chinese juniper beach wormwood Bulbus Allii Macrostemonis Rhizoma Pinelliae " extract 12g
Chinese liquor 30ml
Distilled water is settled to 60ml
Method for making: press method preparation " the Chinese juniper beach wormwood Bulbus Allii Macrostemonis Rhizoma Pinelliae " extract among the embodiment one, add each adjuvant of prescription and distilled water, again through the ultrafilter ultrafiltration, the ultrafiltrate fill, sterilization, promptly.