CN107213125A - One kind treats silicosis, rheumatalgia, arthralgia and neuralgic medicine and preparation method thereof - Google Patents
One kind treats silicosis, rheumatalgia, arthralgia and neuralgic medicine and preparation method thereof Download PDFInfo
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- A61K9/0056—Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals
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- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
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Abstract
Silicosis, rheumatalgia, arthralgia and neuralgic medicine and preparation method thereof are treated the invention discloses one kind.The treatment silicosis, rheumatalgia, arthralgia and neuralgic medicine include the component of following parts by weight：100 parts of hanfangchin A, 600 800 parts of beta cyclodextrin, 200 250 parts of PVP, 50 150 parts of carboxyrnethyl starch sodium, 25 50 parts of lauryl sodium sulfate, 350 500 parts of hydroxypropyl methyl cellulose, 13 18 parts of superfine silica gel powder.Main ingredient composition hanfangchin A is prepared into inclusion compound by preparation method of the present invention using beta cyclodextrin inclusion technique, then further by main ingredient inclusion compound prepared composition discrete piece.The dissolubility increase of product hanfangchin A of the present invention, dissolution rate are higher, and disintegration time limited shortens, and bioavilability is improved, and its preparation method technique is simple, and production cost is low, consume energy low, easily realize industrialized production.
Description
Technical field
The invention belongs to medicine field, it is related to a kind of medicine and preparation method thereof, it is more particularly to a kind of to be used to treat list
The pure phase of property silicosis I, II, III, each phase quartz lung and rheumatalgia, arthralgia and neuralgic medicine and preparation method thereof.
Background technology
Hanfangchin A (also known as Tet), molecular formula C38H42N2O6, be Fourstamen Stephania Root medicinal material it is extracted, separation, it is pure
The chemicals of the high-purity of gained after change.Modern pharmacological research shows that hanfangchin A element is a kind of cerebrocrast, main
Act on calcium channel, the transmembrane transport and distribution in the cell for influenceing calcium ion are utilized, and it has：(1) resist swollen
Knurl is acted on, and can suppress growth of cancer cells, promotes it dead, and mechanism of action may be relevant with regulation BC1-2 and Bax expression；(2) resist
Bacterium acts on, and can suppress the growth of methicillin-resistant staphylococcus aureus, and can influence the synthesis of Candida albicans and suppress white
The generation of the link intermediate product such as glycolysis, energetic supersession of color candida albicans, reaches the synergistic effect of collaboration Fluconazole；(3) have
Effect slows down cardiac muscle cell's hypertrophy trend as caused by AB, can also reduce fibrosis and the inflammatory reaction of heart；(4) the anti-rhythm of the heart
It is not normal, by influenceing Na+ reset to reach antiarrhythmic effect；(5) suppress osteoporosis, can effectively suppress model mice
Osteoporosis；(6) diaphragmatocele of careless ether induction can effectively be reduced.
Because having above-mentioned good drug effect, hanfangchin A is made into bulk drug, tablet and parenteral solution, wherein Stephania tetrandra first
Plain piece is the chemical drugs preparation being made using hanfangchin A as raw material, and hanfangchin A piece is recorded in state food drug surveilance pipe
The reason office national drug standards, standard code is WS-10001 (HD-0700) -2002, and specification is 20mg/ pieces, for treating rheumatism
Bitterly, arthralgia, neuralgia, merge for lung cancer with low dose radiation；Also it is used for the phase of simple silicosis I, II, III and each phase coal silicon
Lung.Although oral tablet, injection that hanfangchin A is made are had on the market, due to originals such as its property and technologies of preparing
Cause, hanfangchin A piece poorly water-soluble, have that limit for length when being leached after taking, dissolution rate be low, absorption is poor and bioavilability compared with
Low problem, directly affects the effect for the treatment of, and changes the purpose that formulation is unable to reach increase dissolution merely.In addition, rheumatalgia,
Arthralgia, neuralgia, simple silicosis, quartz lung Disease need long-term treatment, injection are such as used for a long time, not only very
Inconvenience, manufacture and medical treatment cost are also high, making patients' financial burden.Therefore, it is necessary to prepare that disintegration rate is very fast, dissolution compared with
Good, decentralization is high, be easy to the treatment silicosis, rheumatalgia, arthralgia and the neuralgia that absorb, bioavilability is higher, convenient to take
Medicine, to meet a variety of demands that clinical treatment and family use.
Dispersible tablet (Dispersible tablets) is also known as water dispersion tablet (Water dispersible tablets), is
The tablet to form homogeneous viscous suspension can be disintegrated rapidly by referring to chance water.For conventional tablet, dispersible tablet absorbs fast, biological
Availability is high, and adverse reaction is small, can reduce excitant of the medicine to intestines and stomach.Dispersible tablet is convenient to take, can swallow, chew,
Containing sucking, it can also put and individually be taken after disperseing in water or with fruit juice, milk with taking, be especially suitable for old, children and to swallow solid difficult
Patient.Therefore, hanfangchin A is done composition for main ingredient for treating silicosis, rheumatalgia, arthralgia and neuralgic medicine
Discrete piece, overcomes the shortcoming of hanfangchin A piece presence, meets a variety of demands that clinical treatment and family use.
The content of the invention
The present invention is directed to existing hanfangchin A piece poorly water-soluble, and limit for length when being leached after taking, dissolution rate are low, absorption is poor
It is relatively low with bioavilability, the effect for the treatment of is directly affected, and change formulation merely and be unable to reach purpose etc. of increase dissolution and ask
Inscribe there is provided a kind of disintegration rate is fast, dissolution is good, decentralization is high, be easy to the treatment silicon that absorbs, bioavilability is high, convenient to take
Lung, rheumatalgia, arthralgia and neuralgic medicine and preparation method thereof, the hanfangchin A piece solved at present on the market are present
Above mentioned problem.Present invention treatment silicosis, rheumatalgia, arthralgia and neuralgic medicine, improve disintegration rate and biology profit
Expenditure, so as to improve curative effect, the present invention treats the preparation method of silicosis, rheumatalgia, arthralgia and neuralgic medicine, technique
Simply, production cost is low, consumes energy low, easily realizes industrialized production.
In order to solve the above technical problems, the present invention is achieved by the following technical solutions：
One kind treats silicosis, rheumatalgia, arthralgia and neuralgic medicine, by the component of following parts by weight：Stephania tetrandra first
100 parts of element, 600-800 parts of beta-schardinger dextrin, 200-250 parts of PVP, 50-150 parts of carboxyrnethyl starch sodium, lauryl sodium sulfate
25-50 parts, 350-500 parts of hydroxypropyl methyl cellulose, 13-18 parts of superfine silica gel powder.
Treatment silicosis described above, rheumatalgia, arthralgia and neuralgic medicine, most preferably preferably by the group of following parts by weight
Point：100 parts of hanfangchin A, 700 parts of beta-schardinger dextrin, 230 parts of PVP, 100 parts of carboxyrnethyl starch sodium, lauryl sodium sulfate 40
Part, 420 parts of hydroxypropyl methyl cellulose, 15 parts of superfine silica gel powder.
Silicosis, rheumatalgia, arthralgia and the neuralgic medicine preparation described above for the treatment of is into dispersible tablet.
More than one described silicosis, rheumatalgia, arthralgia and neuralgic medicine preparations for the treatment of are into the preparation side of dispersible tablet
Method, comprises the following steps：
T1：Following components is weighed by weight：100 parts of hanfangchin A, 600-800 parts of beta-schardinger dextrin, PVP 200-
250 parts, 50-150 parts of carboxyrnethyl starch sodium, 25-50 parts of lauryl sodium sulfate, 350-500 parts of hydroxypropyl methyl cellulose, micro mist
13-18 parts of silica gel, crosses 100 mesh sieves, standby；
T2：Prepare hanfangchin A inclusion compound；
T3：Take PVP to be dissolved in the ethanol of 800-1000 parts 65% and PVP Diluted Alcohol solution is made；
T4：It is another to take carboxyrnethyl starch sodium, lauryl sodium sulfate, hydroxypropyl methyl cellulose and the lower preparation gained of step T2
Hanfangchin A inclusion compound is added in mixer, is stirring evenly and then adding into PVP Diluted Alcohol solution, and stirring is made for 10-15 minutes
Softwood；
T5：Take the softwood being made to put in oscillating granulator, cross 20 mesh sieve wet granulations, wet granular is put in drying box and dried,
Take out, put and 50 mesh sieves progress whole grain is crossed in pelletizing machine, obtain dry particl after whole grain；
T6：Dry particl after grain is rounded to put in high efficient mixer, plus superfine silica gel powder, mix 30 minutes, be made and treat that the tabletting Chinese is prevented
Own A prime mixed powder；
T7：Take hanfangchin A mixed powder to put in tablet press machine, be pressed into plain piece, produce.
The preparation method of hanfangchin A inclusion compounds is under step T2 described above：
S1：Hanfangchin A is dissolved in 300-500 parts of absolute ethyl alcohols hanfangchin A ethanol solution is made；
S2：Beta-schardinger dextrin is placed in material-compound tank, 600-800 parts of water are added, heating dissolves it at 35 DEG C -45 DEG C,
Obtain beta-schardinger dextrin solution；
S3：Hanfangchin A ethanol solution is slowly added into beta-schardinger dextrin solution, stirring while adding, temperature is kept
3h-4h is stirred at 35 DEG C -45 DEG C, puts and places 6h-8h to rearmounted 4 DEG C -6 DEG C of room temperature, filters, discards mother liquor, filter residue
Dry, take out, cross 80 mesh sieves, obtain hanfangchin A inclusion compound.
Further, the mixing speed is 50rpm-100rpm under step S3, and filter residue and drying temperature is 50 DEG C -60
DEG C, drying time is 5h-8h, gained hanfangchin A inclusion compound control moisture≤5%.
The drying temperature of step T5 described above lower drying steps is 50 DEG C -60 DEG C, and drying time is 8h-10h, gained
Dry particle controls moisture≤5%.
The beneficial effects of the invention are as follows：
1. the present invention overcomes the poorly water-soluble that existing hanfangchin A piece is present, limit for length when being leached after taking, dissolution rate be low,
Absorb poor and bioavilability relatively low, directly affect therapeutic effect, and change the mesh that formulation is unable to reach increase dissolution merely
The problems such as, significantly improve product disintegration rate, absorb very fast, can quick acting, be conducive to improving curative effect.
2. product drug dissolution of the present invention reaches more than 90%, more former formulation (sugar coated tablet) significantly improves, and greatly improves
The bioavilability of medicine, reduces adverse reaction.
3. the present invention with beta-schardinger dextrin, carboxyrnethyl starch sodium, lauryl sodium sulfate, hydroxypropyl methyl cellulose, PVP,
Superfine silica gel powder gelatin, without sugared part, is conducive to the long-term taking of hyperglycemic patients as auxiliary material, overcomes former formulation (sugar coated tablet)
The shortcomings of being unfavorable for hyperglycemic patients long-term taking.
4. preparation method technique of the present invention is simple, production equipment is operated without particular/special requirement, easily, consume energy it is low, time saving, raw
Produce cost low, easily realize industrialized production.
Embodiment
Although this specification is drawn a conclusion by particularly pointing out and claims of the present invention being clearly claimed, should
This believes that following explanation is better understood with the present invention.
As used herein, word " preferably " and variant refer to that this hair of specific beneficial effect can be provided in certain circumstances
Bright embodiment.However, other embodiments can also be preferred under identical or other environment.In addition, one
Or it is useless that the detailed description of multiple preferred embodiments, which is not offered as other embodiments, and it is not intended to from scope of the invention
Exclude other embodiments.
First, formulation conditions are screened
1. the selection of disintegrant
The species and consumption of disintegrant are most important to the disintegration of dispersible tablet, result of extraction, are the factors for first having to consider.
The disintegrant commonly used in dispersible tablet has sodium carboxymethyl starch, low-substituted hydroxypropyl cellulose, PVPP, cross-linked carboxymethyl fine
Plain sodium of dimension etc..Using PVP as adhesive, superfine silica gel powder is glidant, respectively to 5% sodium carboxymethyl starch, 5% low substitution hydroxyl
Propyl cellulose, 5% PVPP, 5% Ac-Di-Sol, 4 kinds of disintegrants carry out Selection experiment, with outward appearance, collapse
It is that evaluation index carries out overall merit to solve time limit and dispersing uniformity, to determine disintegrant species optimal in dispersible tablet.As a result
It is shown in Table 1.
The optimization test result table of the disintegrant of table 1
It was found from the result of the test in table 1：It is smooth using sodium carboxymethyl starch tablet surface made from disintegrant, and disintegration
Time limit and dispersing uniformity are preferable, therefore present invention selection sodium carboxymethyl starch is disintegrant.The present invention continues to optimize carboxymethyl
The consumption of sodium starch, result of the test is shown in Table 2.
The sodium carboxymethyl starch consumption of table 2 investigates result table
It was found from the result of the test in table 2：The present invention is tablet made from disintegrant using 3%-8% sodium carboxymethyl starches
Surface is smooth, and disintegration time limited and dispersing uniformity are preferable, thus the present invention selection sodium carboxymethyl starch as disintegrant when use
Measure to account for the 3%-8% of recipe quantity.
2. adhesive is selected
The present invention compared for the tabletting again of compressing dry granulation, wet granulation, and compressing dry granulation is bad using conventional tablet machines effect, right
Equipment requirement is high, therefore the present invention uses wet granulation tabletting again.Dispersible tablet uses the particle that hydrophilic adhesive is made, surface tool
Moisture is easily moistened after hydrophily, tabletting, is penetrated into, beneficial to disintegration of tablet.Investigated in experiment water, 65% ethanol solution, 25% gather
65% ethanol solution, 65% ethanol solution of 35% PVP of dimension ketone make adhesive, with the situation of pelletizing, tablet appearance, disintegration
Time limit and dispersing uniformity are that evaluation index carries out overall merit, the results are shown in Table 3.
The adhesive of table 3 investigates result table
It was found from the result of the test in table 3：The present invention uses the 65% ethanol solution granulation situation of 25% PVP, tablet
Outward appearance, disintegration time limited and dispersing uniformity effect are best, therefore invention adhesives select 65% ethanol solution of 25% PVP.
The present invention continues to optimize the consumption of PVP, and result of the test is shown in Table 4.
The binder dosage of table 4 investigates result table
It was found from the result of the test in table 4：The present invention, which is used, accounts for recipe quantity 13%-15% PVPs as adhesive when system
Grain situation, tablet appearance, disintegration time limited and dispersing uniformity effect are preferable, therefore present invention selection accounts for recipe quantity 13%-15%
PVP is used as adhesive.
3. it is swelled the selection of auxiliary material
Dispersible tablet is mainly medicine with least one disintegrant and being swelled supplementary product compatibility and forming.What is used at present is swelled auxiliary material
There are guar gum, XANTHAN GUM, alginates, glucan, amylum pregelatinisatum, HPMC, polysaccharide and calcium carboxymethylcellulose, hydroxypropyl fine
Tie up the hydrophilic high molecular polymers such as element.XANTHAN GUM, sodium alginate, glucan, HPMC and hydroxy propyl cellulose are compared in experiment
Element is swelled auxiliary material, using disintegration time as inspection target, the results are shown in Table 5.
Table 5 is swelled auxiliary material and investigates result table
It was found from the result of the test in table 5：Using HPMC as when being swelled auxiliary material, the disintegration effect of dispersible tablet is best, therefore this hair
Bright selection HPMC is to be swelled auxiliary material.Compare through experiment investigation, HPMC is to account for recipe quantity as being swelled auxiliary material to be best suitable for consumption
26%.
4. the selection of surfactant
Surfactant has wetting and the effect of solubilising in pharmaceutical preparation, and surface is added in the prescription of dispersible tablet and is lived
Property agent is greatly improved the dissolution rate of dispersible tablet.Lauryl sodium sulfate, dodecyl sodium sulfate, Luo Bo are compared in experiment
Husky nurse and the dissolution experiment for not adding dispersible tablet in the case of three kinds of surfactant, the results are shown in Table 6.
The surfactant of table 6 investigates result table
Result of the test in table 6：In the dissolution results of three kinds of dispersible tablets, with lauryl sodium sulfate as
Result of extraction is best during surfactant, therefore present invention selection lauryl sodium sulfate is surfactant.Through experiment investigation pair
Than its consumption be recipe quantity 2% when tablet result of extraction it is best.
5. the selection of glidant
Powder flowbility is a critical nature in solid pharmaceutical preparation technique.Superfine silica gel powder, magnesium stearate are conventional
Glidant, can effectively improve the mobility of particle or powder in pelletizing press sheet or direct powder compression.Contrasted in experiment
1% superfine silica gel powder, 1% magnesium stearate, 1% magnesium stearate-superfine silica gel powder (0.5: 0.5) are as glidant, with disintegration time
It is inspection target with hardness, carries out overall merit.It the results are shown in Table 7.
The glidant of table 7 investigates result table
Result of the test in table 7：1% superfine silica gel powder is best as glidant effect, therefore the present invention is micro- from 1%
Powder silica gel is as glidant.
2nd, the preparation method for the treatment of silicosis, rheumatalgia, arthralgia and neuralgic medicine preparation into dispersible tablet
Embodiment 1
A kind of silicosis, rheumatalgia, arthralgia and neuralgic medicine preparation for the treatment of is into the preparation method of dispersible tablet, including such as
Lower step：
T1：Following components is weighed by weight：Hanfangchin A 2000g, beta-schardinger dextrin 12000g, PVP 4000g, carboxylic
First sodium starch 1000g, lauryl sodium sulfate 500g, hydroxypropyl methyl cellulose 7000g, superfine silica gel powder 260g, cross 100 mesh
Sieve, it is standby；
T2：Prepare hanfangchin A inclusion compound：Take hanfangchin A to be dissolved in 6000g absolute ethyl alcohols and Stephania tetrandra first is made
Plain ethanol solution；Take load weighted beta-schardinger dextrin to be placed in material-compound tank, add 12000g water, heating makes its molten at 35 DEG C
Solution, obtains beta-schardinger dextrin solution；Hanfangchin A ethanol solution is slowly added into beta-schardinger dextrin solution, it is stirring while adding,
Mixing speed is 50rpm, and temperature is maintained at 35 DEG C and stirs 4h, puts and places 8h to rearmounted 4 DEG C of room temperature, filters, discards
Mother liquor, the dry 8h of 50 DEG C of filter residue takes out, and crosses 80 mesh sieves, obtains hanfangchin A inclusion compound, and it is 4.8% to determine its moisture；
T3：PVP is dissolved in the ethanol of 16000g 65% PVP Diluted Alcohol solution is made；
T4：It is another to take carboxyrnethyl starch sodium, lauryl sodium sulfate, hydroxypropyl methyl cellulose and the lower preparation gained of step T2
Hanfangchin A inclusion compound is added in mixer, is stirring evenly and then adding into PVP Diluted Alcohol solution, and stirring is made soft for 10 minutes
Material；
T5：Take the softwood being made to put in oscillating granulator, cross 20 mesh sieve wet granulations, wet granular is put in drying box 50 DEG C and done
Dry 10h, takes out, and puts and 50 mesh sieves progress whole grain is crossed in pelletizing machine, obtain dry particl after whole grain, it is 4.7% to determine its moisture；
T6：Dry particl after grain is rounded to put in high efficient mixer, plus superfine silica gel powder, mix 30 minutes, be made and treat that the tabletting Chinese is prevented
Own A prime mixed powder；
T7：Take hanfangchin A mixed powder to put in tablet press machine, be pressed into plain piece, produce.
Embodiment 2
A kind of silicosis, rheumatalgia, arthralgia and neuralgic medicine preparation for the treatment of is into the preparation method of dispersible tablet, including such as
Lower step：
T1：Following components is weighed by weight：Hanfangchin A 2000g, beta-schardinger dextrin 16000g, PVP 5000g, carboxylic
First sodium starch 3000g, lauryl sodium sulfate 1000g, hydroxypropyl methyl cellulose 10000g, superfine silica gel powder 360g, cross 100 mesh
Sieve, it is standby；
T2：Prepare hanfangchin A inclusion compound：Take hanfangchin A to be dissolved in 10000g absolute ethyl alcohols and Stephania tetrandra is made
A prime ethanol solution；Take load weighted beta-schardinger dextrin to be placed in material-compound tank, add 16000g water, heating makes it at 45 DEG C
Dissolving, obtains beta-schardinger dextrin solution；Hanfangchin A ethanol solution is slowly added into beta-schardinger dextrin solution, side edged is stirred
Mix, mixing speed is 100rpm, temperature is maintained at 45 DEG C and stirs 3h, put and place 6h to rearmounted 6 DEG C of room temperature, filter,
Mother liquor is discarded, the dry 5h of 60 DEG C of filter residue takes out, crosses 80 mesh sieves, obtain hanfangchin A inclusion compound, determining its moisture is
2.5%；
T3：PVP is dissolved in the ethanol of 20000g 65% PVP Diluted Alcohol solution is made；
T4：It is another to take carboxyrnethyl starch sodium, lauryl sodium sulfate, hydroxypropyl methyl cellulose and the lower preparation gained of step T2
Hanfangchin A inclusion compound is added in mixer, is stirring evenly and then adding into PVP Diluted Alcohol solution, and stirring is made soft for 15 minutes
Material；
T5：Take the softwood being made to put in oscillating granulator, cross 20 mesh sieve wet granulations, wet granular is put in drying box 60 DEG C and done
Dry 8h, takes out, and puts and 50 mesh sieves progress whole grain is crossed in pelletizing machine, obtain dry particl after whole grain, it is 2.6% to determine its moisture；
T6：Dry particl after grain is rounded to put in high efficient mixer, plus superfine silica gel powder, mix 30 minutes, be made and treat that the tabletting Chinese is prevented
Own A prime mixed powder；
T7：Take hanfangchin A mixed powder to put in tablet press machine, be pressed into plain piece, produce.
Embodiment 3
A kind of silicosis, rheumatalgia, arthralgia and neuralgic medicine preparation for the treatment of is into the preparation method of dispersible tablet, including such as
Lower step：
T1：Following components is weighed by weight：Hanfangchin A 2000g, beta-schardinger dextrin 14000g, PVP 4600g, carboxylic
First sodium starch 2000g, lauryl sodium sulfate 800g, hydroxypropyl methyl cellulose 8400g, superfine silica gel powder 300g, cross 100 mesh
Sieve, it is standby；
T2：Prepare hanfangchin A inclusion compound：Take hanfangchin A to be dissolved in 8000g absolute ethyl alcohols and Stephania tetrandra first is made
Plain ethanol solution；Take load weighted beta-schardinger dextrin to be placed in material-compound tank, add 14000g water, heating makes its molten at 40 DEG C
Solution, obtains beta-schardinger dextrin solution；Hanfangchin A ethanol solution is slowly added into beta-schardinger dextrin solution, it is stirring while adding,
Mixing speed is 80rpm, and temperature is maintained at 40 DEG C and stirs 3.5h, puts and places 7h to rearmounted 5 DEG C of room temperature, filters, abandons
Mother liquor is removed, the dry 6.5h of 55 DEG C of filter residue takes out, crosses 80 mesh sieves, obtain hanfangchin A inclusion compound, determining its moisture is
3.2%；
T3：PVP is dissolved in the ethanol of 18000g 65% PVP Diluted Alcohol solution is made；
T4：It is another to take carboxyrnethyl starch sodium, lauryl sodium sulfate, hydroxypropyl methyl cellulose and the lower preparation gained of step T2
Hanfangchin A inclusion compound is added in mixer, is stirring evenly and then adding into PVP Diluted Alcohol solution, and stirring is made soft for 13 minutes
Material；
T5：Take the softwood being made to put in oscillating granulator, cross 20 mesh sieve wet granulations, wet granular is put in drying box 55 DEG C and done
Dry 9h, takes out, and puts and 50 mesh sieves progress whole grain is crossed in pelletizing machine, obtain dry particl after whole grain, it is 3.3% to determine its moisture；
T6：Dry particl after grain is rounded to put in high efficient mixer, plus superfine silica gel powder, mix 30 minutes, be made and treat that the tabletting Chinese is prevented
Own A prime mixed powder；
T7：Take hanfangchin A mixed powder to put in tablet press machine, be pressed into plain piece, produce.
3rd, the quality evaluation for the treatment of silicosis, rheumatalgia, arthralgia and neuralgic medicine
1. determine disintegration time limited
Using Chinese Pharmacopoeia version " disintegration time limited inspection technique " (general rule 0921) in 2015, the above-mentioned embodiment 1- prepared is taken
3 samples and commercially available hanfangchin A piece are detected, disintegration time limited is recorded respectively, 8 are the results are shown in Table.
The disintegration time mensuration situation of table 8
As can be seen from Table 8：The dispersible tablet of medicine preparation of the present invention is disintegrated than the commercially available sugar coated tablet that common preparation method is made
Time in time limit shortens, and shows that it absorbs very fast, and energy quick acting is conducive to improving curative effect.
2. determine dissolution rate
Using Chinese Pharmacopoeia version " dissolution rate and drug release determination method " first method (general rule 0931) in 2015, above-mentioned preparation is taken
Good embodiment 1-3 samples and commercially available hanfangchin A piece is detected that sample size is determined using using ultraviolet spectrometry light
Degree method, using hanfangchin A as reference substance, absorbance is determined at 280nm, dissolution rate is then calculated, the results are shown in Table 9.
The dissolution determination situation of table 9
As can be seen from Table 9：The dispersible tablet of medicine preparation of the present invention is than commercially available sugar coated tablet dissolution that common preparation method is made
Degree is significantly improved, and shows that its bioavilability is higher.
Claims (10)
1. one kind treats silicosis, rheumatalgia, arthralgia and neuralgic medicine, it is characterised in that include the group of following parts by weight
Point：100 parts of hanfangchin A, 600-800 parts of beta-schardinger dextrin, 200-250 parts of PVP, 50-150 parts of carboxyrnethyl starch sodium, 12
25-50 parts of sodium alkyl sulfate, 350-500 parts of hydroxypropyl methyl cellulose, 13-18 parts of superfine silica gel powder.
2. treatment silicosis, rheumatalgia, arthralgia and neuralgic medicine as claimed in claim 1, it is characterised in that including with
The component of lower parts by weight：100 parts of hanfangchin A, 700 parts of beta-schardinger dextrin, 230 parts of PVP, 100 parts of carboxyrnethyl starch sodium, 12
40 parts of sodium alkyl sulfate, 420 parts of hydroxypropyl methyl cellulose, 15 parts of superfine silica gel powder.
3. silicosis, rheumatalgia, arthralgia and neuralgic medicine are treated as claimed in claim 1 or 2, it is characterised in that institute
Medicine preparation is stated into dispersible tablet.
4. a kind of silicosis, rheumatalgia, arthralgia and neuralgic medicine preparation as claimed in claim 3 for the treatment of is into dispersible tablet
Preparation method, comprises the following steps：
T1：Following components is weighed by weight：100 parts of hanfangchin A, 600-800 parts of beta-schardinger dextrin, PVP 200-250
Part, 50-150 parts of carboxyrnethyl starch sodium, 25-50 parts of lauryl sodium sulfate, 350-500 parts of hydroxypropyl methyl cellulose, micro mist silicon
13-18 parts of glue, crosses 100 mesh sieves, standby；
T2：Prepare hanfangchin A inclusion compound；
T3：Take PVP to be dissolved in the ethanol of 800-1000 parts 65% and PVP Diluted Alcohol solution is made；
T4：It is another to take carboxyrnethyl starch sodium, lauryl sodium sulfate, hydroxypropyl methyl cellulose and the lower gained Chinese for preparing of step T2 to prevent
Own A prime inclusion compound is added in mixer, is stirring evenly and then adding into PVP Diluted Alcohol solution, and stirring is made soft for 10-15 minutes
Material；
T5：Take the softwood being made to put in oscillating granulator, cross 20 mesh sieve wet granulations, wet granular is put in drying box and dried, and takes out,
Put and 50 mesh sieves progress whole grain is crossed in pelletizing machine, obtain dry particl after whole grain；
T6：Dry particl after grain is rounded to put in high efficient mixer, plus superfine silica gel powder, mix 30 minutes, be made and treat tabletting Stephania tetrandra first
Plain mixed powder；
T7：Take hanfangchin A mixed powder to put in tablet press machine, be pressed into plain piece, produce.
5. the preparation for the treatment of silicosis, rheumatalgia, arthralgia and neuralgic medicine preparation into dispersible tablet as claimed in claim 4
Method, it is characterised in that the preparation method of hanfangchin A inclusion compounds is under described step T2：
S1：Hanfangchin A is dissolved in 300-500 parts of absolute ethyl alcohols hanfangchin A ethanol solution is made；
S2：Beta-schardinger dextrin is placed in material-compound tank, add 600-800 part water, at 35 DEG C -45 DEG C heat dissolve it, obtain β -
Cyclodextrin solution；
S3：Hanfangchin A ethanol solution is slowly added into beta-schardinger dextrin solution, stirring while adding, temperature is maintained at 35
3h-4h is stirred at DEG C -45 DEG C, puts and places 6h-8h to rearmounted 4 DEG C -6 DEG C of room temperature, filter, mother liquor is discarded, filter residue and drying,
Take out, cross 80 mesh sieves, obtain hanfangchin A inclusion compound.
6. the preparation for the treatment of silicosis, rheumatalgia, arthralgia and neuralgic medicine preparation into dispersible tablet as claimed in claim 5
Method, it is characterised in that the mixing speed is 50rpm-100rpm under described step S3.
7. the preparation for the treatment of silicosis, rheumatalgia, arthralgia and neuralgic medicine preparation into dispersible tablet as claimed in claim 5
Method, it is characterised in that the filter residue and drying temperature is 50 DEG C -60 DEG C under described step S3, and drying time is 5h-8h.
8. the preparation for the treatment of silicosis, rheumatalgia, arthralgia and neuralgic medicine preparation into dispersible tablet as claimed in claim 5
Method, it is characterised in that described step S3 lower gained hanfangchin A inclusion compound control moisture≤5%.
9. the preparation for the treatment of silicosis, rheumatalgia, arthralgia and neuralgic medicine preparation into dispersible tablet as claimed in claim 4
Method, it is characterised in that the drying temperature of the drying steps is 50 DEG C -60 DEG C under step T5, and drying time is 8h-10h.
10. silicosis, rheumatalgia, arthralgia and neuralgic medicine preparation are treated as claimed in claim 4 into the system of dispersible tablet
Preparation Method, it is characterised in that dry particl control moisture≤5% under step T5.
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Application publication date: 20170929 |