CN105832751A - Pharmaceutical composition for improving osteoarticular diseases, disintegrating tablet and preparation method thereof - Google Patents
Pharmaceutical composition for improving osteoarticular diseases, disintegrating tablet and preparation method thereof Download PDFInfo
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- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7008—Compounds having an amino group directly attached to a carbon atom of the saccharide radical, e.g. D-galactosamine, ranimustine
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- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
- 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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- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
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Abstract
The invention provides a pharmaceutical composition for improving osteoarticular diseases, a disintegrating tablet and a preparation method thereof. The pharmaceutical composition comprises main materials and auxiliary materials. The main materials are composed of, by weight, 90-120 parts of glucosamine and 0.001-0.05 part of vitamin K. The glucosamine can stimulate chondrocytes to synthesize protein polysaccharide and collagen fiber so as to generate cartilage matrix and repair articular cartilage. Vitamin K controls bone and calcium metabolism such that effective mineral deposition and retention of calcium intake on bones are guaranteed, bone quality and bone mineral density are enhanced and repairing function of articular cartilage is effectively raised. By using glucosamine and vitamin K as the main material and controlling ratio of the two components within the above range, the two active components have a synergistic interaction so as to raise mechanical strength of bone tissues of a patent, effectively inhibit decline in bone mineral density of middle-aged and old people, completely improve symptoms of osteoarthritis and mitigate arthralgia. Therefore, bone health problems such as bone aging of middle-aged and old people are alleviated.
Description
Technical field
The present invention relates to medicines and health protection field, in particular to a kind of improve the pharmaceutical composition of joint disease, disintegrating tablet and
Its preparation method.
Background technology
Osteoarthritis is modal joint disease, and it is impaired that Americanism damp disease association is defined as articular cartilage integrity, cartilage
That lower hone lamella and joint margins osseous lesion cause, based on a kind of different substantiality disease of joint symptoms and sign, i.e. articular cartilage
Regression and a kind of chronic joint disease of Secondary cases hyperosteogeny.Its cardinal symptom is the pain that causes of articular cartilage degeneration and function funeral
Lose.After people steps into the middle age, joint tissue starts the most aging, knee joint, joint of vertebral column that degeneration particularly bears a heavy burden occurs
The most easily damaged.In 50～the crowd of 60 years old, suffer from osteoarthritis person and exceed half.Because after people in middle age, movable minimizing,
Metabolism is not normal, and the important substance in cartilage matrix starts to run off, and causes cartilage water retention property to reduce, and articular cavity synovial fluid is formed and reduces,
Cartilaginous tissue loses protection, rub, inflammation, hypertrophy, swelling, pain etc., even there is joint deformity, even lose
Function.
And the medicine of existing treatment joint disease can not meet market to diversified demands such as relevant medicine or health product,
Thus, it is still necessary to provide the medicine of a kind of new treatment joint disease or health product to provide more choosing for joint disease patient
Select.
Summary of the invention
Offer is provided and a kind of improves the pharmaceutical composition of joint disease, disintegrating tablet and preparation method thereof,
Market can not be met to diversified demands such as relevant medicine or health product solving prior art is treated the medicine of joint disease
Problem.
To achieve these goals, according to an aspect of the invention, it is provided a kind of pharmaceutical composition improving joint disease,
Pharmaceutical composition includes major ingredient and adjuvant, and in parts by weight, major ingredient is raw by 90～120 parts of glucosamine and 0.001～0.05 part of dimension
Element K composition.
Further, in parts by weight, major ingredient is by 96 parts～110 parts of glucosamine and 0.003 part～0.04 part of vitamin K group
Become.
Further, in parts by weight, adjuvant includes 10 parts～30 parts of cartilage reinforcing agents；Preferably 15 parts～25 parts of cartilage reinforcing agents.
Further, in parts by weight, adjuvant also includes 10 parts～25 portions of disintegrating agents；Preferably 15 parts～20 portions of disintegrating agents.
Further, in parts by weight, adjuvant also includes: 15 parts～35 parts of filleies, 10 parts～23 parts of correctivess, 2 parts～10
Part binding agent, 5 parts～15 parts of lubricants；Preferably 20 parts～30 parts of filleies, 13 parts～20 parts of correctivess, 4 parts～8 parts of binding agents,
7.5 parts～13.5 parts of lubricants.
Further, glucosamine is selected from Glucosamine sulfate potassium chloride, Glucosamine sulfate sodium chloride, glucosamine salt
Any one or more in acid potassium salt, glucosamine salt acid sodium-salt and glucosamine sulphate acid potassium salt；Vitamin K
One or both in vitamin K1, Menaquinone K6, vitamin K3 and methylnaphthohydroquinone.
Further, cartilage reinforcing agent is selected from chondroitin sulfate, Rhizoma Drynariae, skeletal calcium, Cervus elaphus Linnaeas bone, calcium lactate, Radix Puerariae, Portugal
Grape Calciofon, shark cartilage, Rhizoma Dioscoreae, crisp Calciofon, Radix Panacis Quinquefolii, calcium glycine, soybean isoflavone, calcium pantothenate, Fructus Lycii,
One or more in calcium citrate and calcium cirate malate；Preferably, disintegrating agent is selected from polyvinylpolypyrrolidone, crosslinking carboxylic first
Base sodium cellulosate, the hydroxypropyl cellulose of hydroxypropyl content≤20wt%, crospolyvinylpyrrolidone, sodium starch glycollate with
And one or both in carboxymethyl starch sodium；Preferably, filler is selected from microcrystalline Cellulose, mannitol, sorbitol, dextrin
And any one or more of modified starch；Preferably, correctives selected from xylitol, stevioside, neotame, aspartame,
Saccharin sodium, high fructose, alitame, cyclamate, Radix Glycyrrhizae, Fructus Citri Limoniae essence, cream flavour, sucrose, acesulfame potassium and glucose
In any one or more；Preferably, binding agent selected from hydroxypropyl methyl cellulose, sodium carboxymethyl cellulose, polyvidone,
Any one or more in methylcellulose, hydroxypropyl cellulose, ethyl cellulose, gelatin, carbomer and starch slurry；
Preferably, lubricant is selected from Pulvis Talci, micropowder silica gel, magnesium stearate, silicon dioxide, PEG6000, fumaric acid sodium, lauryl alcohol
One or more in magnesium sulfate and sodium laurylsulfate.
To achieve these goals, according to an aspect of the invention, it is provided a kind of disintegrating tablet improving joint disease, collapse
Solve sheet and contain any of the above-described kind of pharmaceutical composition.
Further, disintegrating tablet is orally disintegrating tablet, and the content of the major ingredient in preferably every disintegrating tablet Chinese medicine compositions is
0.5g～1.6g.
According to a further aspect in the invention, it is provided that the preparation method of a kind of disintegrating tablet improving joint disease, preparation method bag
Include the major ingredient in pharmaceutical composition and adjuvant sieved successively, weigh, mixing granulation and the step of tabletting, pharmaceutical composition
For any of the above-described kind of pharmaceutical composition.
Application technical scheme, glucosamine can stimulate chondrocyte synthetic proteins polysaccharide and collagen fiber, generate soft
Bone matrix, repairing articular cartilage.Vitamin K controls bone and calcium metabolism, it is ensured that the calcium of absorption on skeleton effective mineralising deposition and
Keep, increase bone mass and bone density, be effectively improved the repair function of articular cartilage.Pharmaceutical composition of the present invention is by by amino
Glucose and vitamin K are as effective ingredient (i.e. major ingredient), and control the proportioning between two components within the above range so that two
Planting the mutual synergism of effective ingredient, improve the osseous tissue mechanical strength of patient, the effectively bone density of suppression middle-aged and elderly people declines,
Improve osteoarthritis symptom comprehensively, alleviate arthralgia, thus slow down the bone health problems such as middle-aged and elderly people skeleton aging.
Detailed description of the invention
It should be noted that in the case of not conflicting, the embodiment in the application and the feature in embodiment can be mutually combined.
The present invention is described in detail below in conjunction with embodiment.
In the application, major ingredient refers to that effective ingredient, adjuvant refer to drug effect auxiliary element, including assisting to strengthen the ingredient of drug effect
Or it is prepared as food ingredient required during medicine.In parts by weight, in major ingredient and adjuvant, each mean with identical weight
Calculate as 1 weight portion.
As background section is previously mentioned, the medicine improving treatment joint disease of the prior art or health product can not meet
, for increase patient to this quasi drugs or the diversified demand of health product, the most easily there is osteoporosis in the demand of market diversification
And often with the demand of the middle-older patient that osteoarthritis occurs, in a kind of typical embodiment of the present invention, it is provided that one
Planting the pharmaceutical composition improving joint disease, this pharmaceutical composition includes major ingredient and adjuvant, and in parts by weight, major ingredient is by 90～120
Part glucosamine and 0.001～0.05 part of vitamin K composition.
In aforementioned pharmaceutical compositions, glucosamine can stimulate chondrocyte synthetic proteins polysaccharide and collagen fiber, generates cartilage base
Matter, repairing articular cartilage.Vitamin K controls bone and calcium metabolism, it is ensured that the calcium of absorption is effective mineralising deposition and holding on skeleton,
Increase bone mass and bone density, be effectively improved the repair function of articular cartilage.Pharmaceutical composition of the present invention is by by glucosamine
With vitamin K as effective ingredient (i.e. major ingredient), and control the proportioning between above-mentioned two components within the above range so that two kinds
The mutual synergism of effective ingredient, improves the osseous tissue mechanical strength of patient, and the effectively bone density of suppression middle-aged and elderly people declines, entirely
Face is improved osteoarthritis symptom, is alleviated arthralgia, thus slows down the bone health problems such as middle-aged and elderly people skeleton aging.
In aforementioned pharmaceutical compositions, the proportioning of major ingredient glucosamine and vitamin K can carry out the most excellent within the above range
Changing and adjust, with the component proportion more optimized, but the ratio range after optimizing and revising is the most within the scope of the present invention.
In one preferred embodiment of the present invention, in aforementioned pharmaceutical compositions, in parts by weight, major ingredient is by 96 parts～110 parts of amino Portugals
Grape sugar and 0.003 part～0.04 part of vitamin K composition.
In aforementioned pharmaceutical compositions, the major ingredient being made up of glucosamine and vitamin K is the drug effect improving osteoarthrosis relevant disease
Composition, and the composition of required interpolation when adjuvant is that this active ingredient is prepared as suitable medicine, be to play auxiliary to major ingredient composition
Help, protect or the composition of potentiation.The concrete composition of adjuvant is relevant with the dosage form to be prepared as, can be according to different dosage form institute
Rationally need to select from conventional adjuvant.In one preferred embodiment of the present invention, in aforementioned pharmaceutical compositions
Adjuvant, in parts by weight, including 10 parts～30 parts of cartilage reinforcing agents；More preferably 15 parts～25 parts of cartilage reinforcing agents.With amino Portugal
Grape sugar salt and vitamin K are major ingredient, and cartilage reinforcing agent is used in combination, and are possible not only to be effectively improved the osteoarthritis disease of old people
Disease, and bone metabolism can be strengthened, thus reduce the morbidity risk rate of old people's joint disease.
In another kind preferred embodiment of the present invention, the adjuvant of aforementioned pharmaceutical compositions, in parts by weight, also include 10 parts～25
Part disintegrating agent；Preferably 15 parts～20 portions of disintegrating agents.Contribute to being prepared as being suitable to disintegrate by this pharmaceutical composition by adding disintegrating agent
Medicament forms, and it is short to select the disintegrating agent of above-mentioned deal to be conducive to being prepared as disintegration time, and is suitable to Orally disintegrating, can improve
The compliance of Drug therapy, is especially suitable for older, the old people that swallow declines.
Aforementioned pharmaceutical compositions adds disintegrating agent and contributes to being prepared as disintegrating tablet, is beneficial to improve drug compliance, in order to carry further
The compliance of high medicine and the performance such as storage, drug effect, in another preferred embodiment of the present invention, aforementioned pharmaceutical compositions
Adjuvant, in parts by weight, also includes: 15 parts～35 parts of filleies, 10 parts～23 parts of correctivess, 2 parts～10 parts of binding agents, 5
Part～15 parts of lubricants；Preferably 20 parts～30 parts of filleies, 13 parts～20 parts of correctivess, 4 parts～8 parts of binding agents, 7.5 parts～13.5
Part lubricant.Select above-mentioned multiple auxiliary materials and carry out proportioning with above-mentioned each weight portion, it is possible to above-mentioned major ingredient is prepared as disintegration time
The oral cavity disintegration tablet that short, hardness is suitable, should not crush, only need to be placed in lingual surface, it is not necessary to chew, and meets saliva within several seconds quickly
Dissolving, borrow and swallow power, medicine can enter stomach onset.It is particularly suitable for old age, is unable to leave the bed and the patient of hydropenia environment.
The glucosamine of the major ingredient in combining for said medicine, main selection chemical property is relatively stable, be difficult to oxidized ammonia
Base glucose salt, includes but are not limited to Glucosamine sulfate potassium chloride, Glucosamine sulfate sodium chloride, glucosamine salt
In acid potassium salt, glucosamine salt acid sodium-salt and glucosamine sulphate acid potassium salt any one or more.
Vitamin K in aforementioned pharmaceutical compositions is relevant with the synthesis of alanine (Gla), thus participates in bone metabolism, including but
Be not limited only in vitamin K1, Menaquinone K6, vitamin K3 and methylnaphthohydroquinone one or both.Vitamin K can
Regulation bone metabolism, the carboxylation of promotion Bone Gla protein, it is ensured that the calcium of absorption is effective mineralising deposition and holding on skeleton, by increasing capacitance it is possible to increase bone
Matter loosen patient bone density, reduce fracture incidence rate.
The adjuvants such as cartilage reinforcing agent, disintegrating agent, filler, correctives, binding agent and lubricant in above-mentioned composition are
Conventional adjuvant, selects the most concrete kind according to actual production demand.Specifically, cartilage reinforcing agent include but not only
Be limited to chondroitin sulfate, Rhizoma Drynariae, skeletal calcium, Cervus elaphus Linnaeas bone, calcium lactate, Radix Puerariae, calcium gluconate, shark cartilage, Rhizoma Dioscoreae,
Crisp Calciofon, Radix Panacis Quinquefolii, calcium glycine, soybean isoflavone, calcium pantothenate, Fructus Lycii, calcium citrate and citrate malate acid
One or more in calcium.
Similarly, disintegrating agent rationally can also select according to the difference of actual production demand, specifically can be poly-selected from crosslinking
Dimension ketone, cross-linking sodium carboxymethyl cellulose, the hydroxypropyl cellulose (i.e. low-substituted hydroxypropyl cellulose) of hydroxypropyl content≤20wt%,
One or both in crospolyvinylpyrrolidone, sodium starch glycollate and carboxymethyl starch sodium.Filler can be selected from
Any one or more of microcrystalline Cellulose, mannitol, sorbitol, dextrin and modified starch.Correctives can be selected from xylitol,
Stevioside, neotame, aspartame, saccharin sodium, high fructose, alitame, cyclamate, Radix Glycyrrhizae, Fructus Citri Limoniae essence, creamy
Any one or more in essence, sucrose, acesulfame potassium and glucose.Binding agent is selected from hydroxypropyl methyl cellulose, carboxymethyl
In sodium cellulosate, polyvidone, methylcellulose, hydroxypropyl cellulose, ethyl cellulose, gelatin, carbomer and starch slurry
Any one or more.Lubricant is selected from Pulvis Talci, micropowder silica gel, magnesium stearate, silicon dioxide, PEG6000, fumaric acid
One or more in sodium, magnesium laurylsulfate and sodium laurylsulfate.
In the another kind of typical embodiment of the present invention, it is provided that a kind of disintegrating tablet improving joint disease, this disintegrating tablet contains
There is any of the above-described kind of pharmaceutical composition.Older due to old man, swallow declines, and the old man that there are about 50% swallows tablet
Time have any problem, have impact on the compliance of Drug therapy.The preferred above-mentioned disintegrating tablet of the present invention is oral cavity disintegration tablet (i.e. oral type), can
Improve the compliance of Drug therapy.Oral cavity disintegration tablet is without chewing, and tablet is placed in lingual surface, meets saliva rapid solution within several seconds,
Borrowing and swallow power, medicine can enter stomach onset.
Most oral cavity disintegration tablet hardness is relatively low, long-term storage, and tablet is likely damaged before taking medicine, and extends disintegration, shadow
Ring drug absorption.And the disintegrating tablet containing aforementioned pharmaceutical compositions has the advantage that disintegration time is short, hardness suitable, should not crush,
It is particularly suitable for old age, is unable to leave the bed and the patient of hydropenia environment.The content of the most every disintegrating tablet Chinese medicine compositions
For 0.5g～1.6g, content is the most not only beneficial to patient and carries, takes medicine conveniently, and medicine can be utilized by the most effective.
In the another kind of typical embodiment of the present invention, it is provided that the preparation method of a kind of disintegrating tablet improving joint disease,
This preparation method includes sieving the major ingredient in pharmaceutical composition and adjuvant successively, weighs, mixing granulation and the step of tabletting,
Wherein, pharmaceutical composition is any of the above-described kind of pharmaceutical composition of the present invention.Use the composition in aforementioned pharmaceutical compositions and proportioning
The disintegrating tablet being prepared from has the advantage that disintegration time is short, hardness suitable, should not crush.
In the actual preparation of above-mentioned disintegrating tablet produces, kind and proportioning according to selected concrete adjuvant can be prepared as multiple
Different disintegrating tablets.Specifically, when containing only disintegrating agent in pharmaceutical composition, its preparation method is: (1) is by quality control
Standard inspection improves major ingredient and the adjuvant of joint disease pharmaceutical composition, by glucosamine, vitamin K, cartilage reinforcing agent,
Disintegrating agent sieves, preferably 80 mesh sieves.(2) according to the above-mentioned weight proportion of the present invention, each raw material that accurate weighing sieves, mixed
Closing in granulator and the disintegrating agent of glucosamine, vitamin K, cartilage reinforcing agent and interior part is pulverized, mixed, stirring is all
Soft material is made after even.(3) soft material is prepared granule by screen cloth extruding.In order to make granule evenly, fine powder amount is less, also may be used
With by granule again by screen cloth.(4) granule made is put in exsiccator, dry run prevents particle adhesion, caking,
The size being made granule by granulate is the most suitable.(5) in granule, add the disintegrating agent of residue external, always mix.By various
After former material mix homogeneously, measure content tabletting.Disintegrating agent prepared by the method has the advantage that disintegration time is short, be prone to absorption.
When in pharmaceutical composition possibly together with other cartilage reinforcing agents, filler, correctives, binding agent and lubricant, it is prepared
Method is: (1) is improved major ingredient and the adjuvant of the pharmaceutical composition of joint disease by quality control standard inspection, by aminoglucose
Sugar, vitamin K, cartilage reinforcing agent, disintegrating agent, filler, correctives, binding agent and lubricant sieve, preferably 80 mesh sieves.
(2) according to the above-mentioned weight proportion of the present invention, each raw material that accurate weighing sieves.(3) by aminoglucose in mixer-granulator
Sugar, vitamin K, cartilage reinforcing agent, filler, correctives and partial disintegration agent carry out pulverizing, mixing, and add the rule weighed up
Determine the binding agent of consumption, after stirring, make soft material.(4) soft material is prepared granule by screen cloth extruding.In order to make granule more
Uniformly, fine powder amount is less, it is also possible to by granule again by screen cloth.(5) granule made is put in exsiccator, dried
Preventing particle adhesion, caking in journey, the size being made granule by granulate is the most suitable.(6) in granule, add the lubrication of respective amount
Agent and remaining disintegrating agent, always mix.(7) by after various former material mix homogeneously, content tabletting is measured.
Further illustrate beneficial effects of the present invention below in conjunction with specific embodiments.Inventor is according to 9 kinds shown in table 1
The formula of embodiment, every kind of formula is prepared 1000 samples, and has been carried out repeating test, the formula of each embodiment such as table 1-1
Shown in table 1-2.
Table 1-1:
Table 1-2:
One, preparation technology
By Glucosamine sulfate potassium chloride, vitamin K1 (or Menaquinone K6), chondroitin sulfate, polyvinylpolypyrrolidone, crystallite fibre
Dimension element, xylitol, hydroxypropyl methyl cellulose, Pulvis Talci, micropowder silica gel and magnesium stearate cross 80 mesh sieves.
The each raw material of accurate weighing, and by soft to the Glucosamine sulfate potassium chloride sieved, vitamin K1 (or Menaquinone K6), sulphuric acid
Ossein, microcrystalline Cellulose, xylitol and partial cross-linked polyvidone are pulverized in mixer-granulator, are mixed, and add specified volume
Binding agent, makes soft material after stirring.
Soft material is prepared granule by screen cloth extruding, the granule made is put in exsiccator and be dried, dry run prevents granule
Adhesion, caking, the size being made granule by granulate is the most suitable.
In granule, add Pulvis Talci, micropowder silica gel, magnesium stearate and remaining polyvinylpolypyrrolidone, always mix.Mix homogeneously
After, measuring content tabletting, the content making every flake products is 1.45g ± 5%.
Then inventor again by major ingredient and the consumption of adjuvant and concrete kind respectively according to condition listed in table 2 and table 3, according to
The step that embodiment 1-9 is identical has been prepared the medicament of embodiment 10-14 and reference examples 1-2.
Table 2:
Table 3:
Two, result test
1. drug quality detection
Disintegration detection method: according to " 2010 editions second annex Ⅹ A inspection technique disintegration of Chinese Pharmacopoeia " measure sample
Disintegration.Use lift disintegration tester, hanging basket is hung on metal rack by the stainless steel shaft of upper end, immerse 1000ml
In beaker, and regulate screen cloth when hanging basket position makes it decline in beaker bottom 25mm, beaker, fill the water that temperature is 37 ± 1 DEG C,
When regulating liquid surface height makes hanging basket rise, screen cloth is under liquid level at 15mm.Take test sample 6, put the glass of above-mentioned hanging basket respectively
Guan Zhong, often manages and adds 1, starts disintegration tester immediately and checks.Each all should whole disintegrates in 5 minutes, record disintegrate
Time limit.If any 1 can not disintegrate completely, should separately take 6 retrials, regulation all should be met.Except recording the initial burst of sample
In the time limit, also needing to record sample is 25 DEG C in temperature, humidity be 50% environment in place the disintegration after one month.
Friability detection method: measure sample according to " 2010 editions second annex Ⅹ G tablet friability inspection technique of Chinese Pharmacopoeia "
Friability.Measure the friability of disintegrating tablet with tablet friability somascope, take 10 and be measured.Blow away de-with hair-dryer
The powder fallen, precise weighing, put in cylinder, rotate 100 times.Take out, remove powder, precise weighing, less loss weight with method
1% must not be crossed, and fracture, the sheet chapping and pulverizing must not be detected.This test is normally only made 1 time, if less loss weight is more than 1%
Time, can recheck 2 times, the average less loss weight of 3 times must not cross 1%, and must not detect fracture, the sheet chapping and pulverizing.
Hardness detection method: measure the hardness of disintegrating tablet with tablet hardness meter.Hardness analyzer is placed on stable work
In station, switch on power, open switch, make system enter test mode.Rotating circular disk handle, moves right probe counterclockwise
Move to appropriate location, tested tablet is put between probe and testboard.Rotating circular disk handle, makes probe slowly move counterclockwise,
Applying extruding force to tested tablet, window display force value is gradually increased.When tested tablet is extruded broken, window display pressure
Force value is maximum and is locked, and is the hardness number of this tablet.Carrying out test next time subsequently, every batch sample tests 10 tablets, note
Record the hardness number of each test of this batch sample, and calculate hardness meansigma methods.Before measurement by clean for the defragmentation of tablet surface.
In order to investigate the sample stability to environment, need record tablet initial hardness and be 25 DEG C in temperature, humidity is 50%
Environment in place the tablet hardness after month.
14 embodiments and 2 reference examples samples to the present invention carry out disintegration, friability and hardness and enter according to the method described above
Row detection, and detect initial sample and place disintegration and the hardness of sample after month, and friability only records initial sample
Detection data, testing result is as shown in table 4.
The testing result of the disintegrating tablet of each embodiment of table 4 and reference examples
Knowable to the data of table 4, the formula of embodiments of the invention 1-14 the sample disintegration time prepared is short, respectively less than 46s.
Wherein, sample disintegration time prepared by the formula of embodiment 1-9 is shorter, respectively less than 40s, even up to tens seconds.Embodiment 10-14
Initial disintegration time be 38-46s.The disintegration time of reference examples 1-2 is more than 60s.Being 25 DEG C by sample in temperature, humidity is 50%
Environment in place after one month, disintegration has extended, but the prolongation time is 1-2s, during the disintegrate of reference examples 1 and 2
Between extend 3-4s.Considering, the disintegrating property of embodiment 1-14 sample is more excellent.
The friability of embodiment of the present invention 1-9 sample is respectively less than 0.4%, and the friability of embodiment 10 is 0.33%.Embodiment 11-14
Friability be 0.45%-0.51%.The friability of reference examples 1-2 sample is respectively 0.6% and 0.63%.The enforcement of the application is described
Example sample is compared reference examples sample and is had good impact resistance, and impact resistance at least improves 15%.
The initial hardness of the sample of embodiment 1-9 is more than 30N less than 40N, and hardness is suitable, is 25 DEG C in temperature, and humidity is 50%
Environment in place the sample hardness after one month and be declined slightly, decline numerical value less than 1N.The initial hardness of embodiment 10 is
45.2N, the hardness after one month is 44.7N.The initial hardness of embodiment 11-14 is 30N-35N, and the hardness after one month is
30N-35N。
Visible, the sample hardness of above-described embodiment 1-14 in one month before and after difference between 0.3～0.6N.And reference examples 1-2
The initial hardness of sample is respectively 27.4N and 25.8N, and the hardness after one month is respectively 26.7N and 24.9N, and its hardness is one
Before and after in individual month, difference is between 0.7～0.9N.It follows that the sample of reference examples not only relatively embodiment in terms of initial hardness
Low, and in one month, the stability of hardness is the most poor.
Disintegration, friability and hardness data in summary analysis 4, it is known that embodiments of the invention 1-9 sample combination property is excellent
Good, good stability.The disintegration time of embodiment 10-14 sample is slightly longer, and performance is taken second place.The performance of reference examples 1-2 sample is worst,
Disintegration time is the longest, and friability is big, and hardness is low.
2. Composition analyzed
Zoopery detection method: 144 pure lines male mices are randomly divided into normal group, model group, treatment 1-14 by body weight
Group, comparison 1-2 group, often 8 mices of group.
8 mices of normal group are left intact, to the bacterial origin of remaining 136 mice right Injection in knuckle articular cavity 1mg/kg
Property collagenase induced arthritis, prepares arthritis animal model.
After model is successfully prepared 1 week, respectively to treatment 1-14 group, the mice right Injection in knuckle articular cavity embodiment of comparison 1-2 group
The sample solution (in each sample solution, the mass concentration of disintegrating tablet medicine is 10%) of 1-14 and reference examples 1-2, injects every day
1 time, each dosage is 5ml/kg, continuously injection 2 weeks.
Model group gives the normal saline of equivalent.
Arthritis and the inflammatory cytokine of macrophages secrete, interleukin-1 beta (IL-1 β), tumor necrosis factor α (TNF-α)
Relevant.IL-1 β and TNF-α can promote the activity of the propagation of osteoclast, differentiation and mature osteoclast, inducing osteoblast
Apoptosis, thus suppress bone formation and bone resorption, ultimately result in osteoporosis.In osteoarthritis or sufferers of osteoporosis face knuckle synovia
IL-1 β and TNF-α content abnormal the highest.It is administered second day after terminating by each group of sacrifice, takes blood, centrifugal, use enzyme
Interleukin-1 beta (IL-1 β) in connection immunoabsorption (ELISA) detection serum and tumor necrosis factor α (TNF-α)
Content.
By mouse animal experiment, measure the interleukin-1 beta (IL-1 β) in mice serum and tumor necrosis factor α (TNF-α)
Content, comparing embodiment 1-14 and the drug effect of reference examples 1-2, testing result is shown in Table 5:
Table 5: the impact that IL-1 β in arthritic mice blood and TNF-α are expressed by each embodiment and reference examples
Note: a represents and compares with normal group, and P < 0.05, b represents and compares with model group, P < 0.05.
As can be known from Table 5, embodiments of the invention are by with glucosamine salt and vitamin K as principal agent, being used in combination cartilage
Said medicine is also prepared as oral type disintegrating tablet by the adjuvants such as reinforcing agent and other suitable excipient, compares prepared by reference examples 1-2
Disintegrating tablet, have significantly improve at the treatment aspect such as osteoarthritis, osteoporosis.Visible, such medicine non-active ingredients
Kind and content are The more the better, but the coordinated optimization being between effective ingredient in drug action.
As can be seen from the above description, the above embodiments of the present invention achieve following technique effect: the present invention selects energy
Enough increase bone density, improve skeleton and the glucosamine salt of function of joint and vitamin K is principal agent, cartilage is used in combination and strengthens
Said medicine is also prepared as oral type disintegrating tablet by the adjuvants such as agent and other suitable excipient, to improve the Orally disintegrating speed of medicine
Degree and hardness, be possible not only to be effectively improved the osteoarthritis disorders of old people, and can strengthen bone metabolism, reduces from root
Easily there is osteoporosis and often with the sickness rate that the joint disease such as osteoarthritis occur in elderly population.
The foregoing is only the preferred embodiments of the present invention, be not limited to the present invention, for those skilled in the art
For, the present invention can have various modifications and variations.All within the spirit and principles in the present invention, any amendment of being made, etc.
With replacement, improvement etc., should be included within the scope of the present invention.
Claims (13)
1. improving a pharmaceutical composition for joint disease, described pharmaceutical composition includes major ingredient and adjuvant, it is characterised in that with weight
Amount part meter, described major ingredient is made up of 90～120 parts of glucosamine and 0.001～0.05 part of vitamin K.
Pharmaceutical composition the most according to claim 1, it is characterised in that in parts by weight, described major ingredient is by 96 parts～110 parts
Glucosamine and 0.003 part～0.04 part of vitamin K composition.
Pharmaceutical composition the most according to claim 1, it is characterised in that in parts by weight, described adjuvant includes 10 parts～30
Part cartilage reinforcing agent；Preferably 15 parts～25 parts of cartilage reinforcing agents.
Pharmaceutical composition the most according to claim 3, it is characterised in that in parts by weight, described adjuvant also includes 10 parts～25
Part disintegrating agent；Preferably 15 parts～20 portions of disintegrating agents.
Pharmaceutical composition the most according to claim 4, it is characterised in that in parts by weight, described adjuvant also includes: 15 parts
～35 parts of filleies, 10 parts～23 parts of correctivess, 2 parts～10 parts of binding agents, 5 parts～15 parts of lubricants；Preferably 20 parts～30
Part filler, 13 parts～20 parts of correctivess, 4 parts～8 parts of binding agents, 7.5 parts～13.5 parts of lubricants.
6. according to pharmaceutical composition according to any one of claim 1 to 5, it is characterised in that described glucosamine is selected from amino Portugal
Grape sugar potassium sulfate salt, Glucosamine sulfate sodium chloride, glucosamine salt acid potassium salt, glucosamine salt acid sodium-salt and ammonia
Any one or more in base glucosamine sulphate salt acid potassium salt.
7. according to pharmaceutical composition according to any one of claim 1 to 5, it is characterised in that described vitamin K is selected from vitamin
One or both in K1, Menaquinone K6, vitamin K3 and methylnaphthohydroquinone.
8. according to the pharmaceutical composition according to any one of claim 3 to 5, it is characterised in that described cartilage reinforcing agent is selected from sulphuric acid
Chrondroitin, Rhizoma Drynariae, skeletal calcium, Cervus elaphus Linnaeas bone, calcium lactate, Radix Puerariae, calcium gluconate, shark cartilage, Rhizoma Dioscoreae, brittleness
Acid calcium, Radix Panacis Quinquefolii, calcium glycine, soybean isoflavone, calcium pantothenate, Fructus Lycii, calcium citrate and calcium cirate malate
In one or more.
Pharmaceutical composition the most according to claim 4, it is characterised in that described disintegrating agent is selected from polyvinylpolypyrrolidone, crosslinking carboxylic first
Base sodium cellulosate, the hydroxypropyl cellulose of hydroxypropyl content≤20wt%, crospolyvinylpyrrolidone, starch glycolate NF
One or both in sodium and carboxymethyl starch sodium.
Pharmaceutical composition the most according to claim 5, it is characterised in that described filler selected from microcrystalline Cellulose, mannitol,
Any one or more of sorbitol, dextrin and modified starch；
Preferably, described correctives selected from xylitol, stevioside, neotame, aspartame, saccharin sodium, high fructose, Ah
Power is sweet, cyclamate, Radix Glycyrrhizae, Fructus Citri Limoniae essence, cream flavour, sucrose, in acesulfame potassium and glucose any one or many
Kind；
Preferably, described binding agent selected from hydroxypropyl methyl cellulose, sodium carboxymethyl cellulose, polyvidone, methylcellulose,
Any one or more in hydroxypropyl cellulose, ethyl cellulose, gelatin, carbomer and starch slurry；
Preferably, described lubricant is selected from Pulvis Talci, micropowder silica gel, magnesium stearate, silicon dioxide, PEG6000, rich horse
One or more in acid sodium, magnesium laurylsulfate and sodium laurylsulfate.
11. 1 kinds of disintegrating tablets improving joint disease, it is characterised in that described disintegrating tablet contains any one of claim 1 to 10
Described pharmaceutical composition.
12. disintegrating tablets according to claim 11, it is characterised in that described disintegrating tablet is orally disintegrating tablet, preferably described in every
The content of the major ingredient in pharmaceutical composition described in disintegrating tablet is 0.5g～1.6g.
The preparation method of 13. 1 kinds of disintegrating tablets improving joint disease, described preparation method includes the major ingredient in pharmaceutical composition and auxiliary
Material carries out successively sieving, weighs, mixing granulation and the step of tabletting, it is characterised in that described pharmaceutical composition is that right is wanted
Seek the pharmaceutical composition according to any one of 1 to 10.
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Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN108451915A (en) * | 2018-05-04 | 2018-08-28 | 杨晓艳 | A kind of calcium glycine tablet composition and preparation method thereof |
| CN112535706A (en) * | 2020-12-16 | 2021-03-23 | 解中胜 | Medicine and food dual-purpose powder for repairing joints and preparation method and application thereof |
| CN113398241A (en) * | 2020-12-31 | 2021-09-17 | 江中药业股份有限公司 | Bone peptide composition, bone peptide tablet, preparation method and evaluation method |
| CN114259042A (en) * | 2020-09-16 | 2022-04-01 | 山东荆卫生物科技有限公司 | Health food for increasing bone density and preventing and treating osteoarthritis and preparation method and application thereof |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101537170A (en) * | 2008-03-17 | 2009-09-23 | 哈药集团制药六厂 | Compound for preventing osteoporosis and osteoarthrosis |
-
2016
- 2016-03-23 CN CN201610170273.XA patent/CN105832751A/en active Pending
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101537170A (en) * | 2008-03-17 | 2009-09-23 | 哈药集团制药六厂 | Compound for preventing osteoporosis and osteoarthrosis |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN108451915A (en) * | 2018-05-04 | 2018-08-28 | 杨晓艳 | A kind of calcium glycine tablet composition and preparation method thereof |
| CN114259042A (en) * | 2020-09-16 | 2022-04-01 | 山东荆卫生物科技有限公司 | Health food for increasing bone density and preventing and treating osteoarthritis and preparation method and application thereof |
| CN112535706A (en) * | 2020-12-16 | 2021-03-23 | 解中胜 | Medicine and food dual-purpose powder for repairing joints and preparation method and application thereof |
| CN113398241A (en) * | 2020-12-31 | 2021-09-17 | 江中药业股份有限公司 | Bone peptide composition, bone peptide tablet, preparation method and evaluation method |
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Effective date of registration: 20170410 Address after: 100078 Beijing city Fengtai District park is a District 17 building 15 layer A-1805 Applicant after: Beijing 3 Biological Technology Co. Ltd. Address before: 100078 Beijing city Fengtai District Fangzhuang park is a District 17 building the world building block A room 1606 Applicant before: BEIJING HEALTHGEM BIOTECHNOLOGY CO., LTD. |
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Application publication date: 20160810 |