CN109172545A - The NADH nanosphere and its preparation process of cladding konjak glucomannan and application - Google Patents
The NADH nanosphere and its preparation process of cladding konjak glucomannan and application Download PDFInfo
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Abstract
The present invention relates to pharmaceutical technology field, a kind of NADH nanosphere for coating konjak glucomannan and its preparation process and application are provided.A kind of preparation process for the NADH nanosphere coating konjak glucomannan, pre-composition is obtained including dispersing NADH nanosphere in pharmaceutical adjunct, the pharmaceutical adjunct includes konjak glucomannan nanosphere, polyvinylpyrrolidone, microcrystalline cellulose, calcium polyphosphate, xanthan gum, sodium alginate, magnesia and magnesium stearate；Wetting agent and adhesive are added into the pre-composition, the NADH nanosphere of required cladding konjak glucomannan can be obtained after evenly mixing.The present invention also provides a kind of NADH nanospheres for coating konjak glucomannan, are prepared using the preparation process of the NADH nanosphere of above-mentioned cladding konjak glucomannan.The present invention also provides a kind of applications of NADH nanosphere for coating konjak glucomannan.
Description
Technical field
The present invention relates to pharmaceutical technology field more particularly to it is a kind of coat konjak glucomannan NADH nanosphere and
Its preparation process and application.
Background technique
With the growth at people's age, the aging of body, many health problems generate therewith, seriously affect people's lives
Quality.Such as dysfunction of blood vessel, locomitivity, the decline of big brain cognitive function, or even the illnesss such as Parkinson occur.
The drug for being intended to improve Health and Living quality has gradually obtained extensive research in recent years, such as niacinamide monokaryon glycosides
Sour (NADH) should have been celebrated university day in 2016 and the joint study group of Washington, DC university is applied to clinical trial,
NADH is proved that it has the effect of reversing the parts tracheal tissue agings such as nerve in animal experiments.University of Washington professor is modern
The research team that well Shinichiro is led has published its newest research results on " Cell Metabolism ": experimental mouse being allowed to take
After nicotinamide mononucleotide, the function at the positions such as energetic supersession, muscle, eyes of experimental mouse is obviously improved.
NADH is existed in human body, is played an important role in human body cell energy generating process, is participated in intracellular
The synthesis of nicotinamide adenine dinucleotide (NAD, the important coenzyme of cellular energy conversion), studies have shown that parenteral administration NADH
There are positive effect, NADH or various hydrogen transportases (dehydrogenase, oxidoreducing enzyme) for treatment Parkinson and major depressive disorder
Coenzyme, support brain, heart, blood vessel and muscle cell regeneration.This biological substance, which is considered to have, promotes physical fitness
Effect and without side-effects, but it can be reduced in the intracorporal content of people with the growth at age, be contained so as to cause NAD in human body
Amount is reduced, these variations are easy to cause the diseases such as metabolism decline and diabetes.
Supplement NADH is of great advantage to human body in due course, but NADH unstable chemcial property, and when infusion needs Fresh,
It is difficult to be widely applied, and since it is very sensitive to light and oxygen, this hypersensitivity and unstable biological nature, so that NADH
It is difficult to be prepared into oral preparation or long-time storage, directly takes rear effective component and be decomposed, it is difficult to it is absorbed by the body, pole
NADH is limited in the application and popularization in body-care field greatly.
Summary of the invention
It is an object of the invention to overcoming the above-mentioned prior art, a kind of cladding konjak glucomannan is provided
NADH nanosphere and its preparation process and application.
In order to solve the above technical problems, invention uses technical solution as described below.A kind of cladding konjak glucomannan
NADH nanosphere preparation process, including disperse NADH nanosphere in pharmaceutical adjunct and obtain pre-composition, the system
Agent auxiliary material includes konjak glucomannan nanosphere, polyvinylpyrrolidone, microcrystalline cellulose, calcium polyphosphate, xanthan gum, seaweed
Sour sodium, magnesia and magnesium stearate；
Wetting agent and adhesive are added into the pre-composition, required cladding Amorphophallus rivieri glucomannan can be obtained after evenly mixing
Reveal the NADH nanosphere of glycan；
The NADH nanosphere, konjak glucomannan nanosphere, polyvinylpyrrolidone, microcrystalline cellulose, poly- phosphorus
Mass ratio between sour calcium, xanthan gum, sodium alginate, magnesia, magnesium stearate, wetting agent and adhesive is 1-20:20-80:
1-10:1-30:1-10:1-30:1-30:1-20:1-10:1-15:1-15.
Preferably, the konjak glucomannan nanosphere is by konjak glucomannan, quaternized konjaku glucomannan, carboxylic
At least one of methyl konjaku glucomannan, deacetylated konjaku glucomannan are made.
Preferably, the konjak glucomannan nanosphere is modified konjaku glucomannans nanosphere, the cladding
The preparation process of the NADH nanosphere of konjak glucomannan further comprises the system of modified konjaku glucomannans nanosphere
It is standby: will be in konjaku glucomannan, quaternized konjaku glucomannan, Carboxymethyl Konjac Glucomannan or deacetylated konjaku glucomannan
It is one or more of carry out chemical degradations, obtain the modified konjaku glucomannans that molecular weight is 8000-20000Da, then will
The particle that the modified konjaku glucomannans and sodium alginate co-ground obtain 200-1000nm is required modified evil spirit
The preparation of taro glucomannans nanosphere.
Preferably, the chemical degradation are as follows: konjak glucomannan and hydrochloric acid or sodium hydroxide are sufficiently mixed 2-10h,
Obtain modified konjaku glucomannans.
Preferably, the mass ratio of the modified konjaku glucomannans and sodium alginate is 1:0.5-5.
Preferably, the wetting agent includes the ethyl alcohol and/or water of mass concentration 70%.
Preferably, described adhesive includes the hydroxypropyl of the pregelatinized starch of 10wt%, the starch slurry of 10wt% or 10wt%
One or more of methylcellulose.
A kind of NADH nanosphere coating konjak glucomannan, using above-mentioned cladding konjak glucomannan
The preparation process of NADH nanosphere is prepared, and the NADH nanosphere of the cladding konjak glucomannan includes that NADH receives
Rice ball, is coated with konjak glucomannan nanosphere outside the NADH nanosphere.
Preferably, the partial size of the NADH nanosphere is 500-1000nm, the grain of the konjak glucomannan nanosphere
Diameter is 200-1000nm.
A kind of application for the NADH nanosphere coating konjak glucomannan, by above-mentioned cladding konjak glucomannan
NADH nanosphere be used to prepare oral class medicine object.
Preferably, the oral class medicine object is particle, tablet or soft capsule.
The beneficial effects of the present invention are:
(1) by outside the unstable NADH of property coat konjak glucomannan (KGM) nano particle, KGM nanometers
NADH material protection inside it, is solved the problems, such as unstable, labile after NADH meets light or oxygen by particle, and what is obtained is compound
Object can save for a long time, which can be used for producing oral preparation, and NADH is made to be suitable for being used as medicine component.Meanwhile it will
After NADH and KGM is prepared as coated composites, NADH can be sustained within a certain period of time, avoid NADH component at once by gastric acid point
Solution, the composite nano-microsphere can be used for producing oral preparation, to anticancer.By from different supplementary product compatibilities, be also Parkinson
The improvement of the diseases such as disease, Alzheimer's disease, depression provides ideal drug.
NADH helps human body to anticancer from the following aspect, and the first step that cancer occurs first is that DNA is attacked by carcinogen
It hits, cause damage, and NADH has the function of that DNA repair enzyme is activated to help DNA plerosis, secondly NADH is a kind of strong oxidizer
It can help to remove interior free yl, cancer is prevented further to develop, third, the increasing that NADH can provide energy, prevent cancer cell
It growing, last NADH can activate NO synthase, promote the synthesis of NO, and NO can dissolve cancer cell, prevent its transfer.
(2) preparation process of the NADH nanosphere of cladding konjak glucomannan of the present invention, by NADH, KGM
Nanosphere is mixed with various auxiliary materials, obtains the composite material for being coated with konjak glucomannan nanosphere.It uses
In auxiliary material, xanthan gum have good adhesive effect, sodium alginate have concentrate solution, formed gel ability, with KGM,
Xanthan gum together, can form protective layer on the surface NADH, and NADH can be made to be sustained out.Microcrystalline cellulose, hydroxypropyl cellulose
So that composite material obtained is easy to compressing tablet process, it is more suitable for preparing medicinal preparation for oral administration, the step of preparation process is simple, condition temperature
With high production efficiency is suitable for industrialized mass production.
Detailed description of the invention
Fig. 1 is that tablet made from embodiment 1 is impregnated to 2h under conditions of simulation hydrochloric acid solution S GF pH=2 then in mould
8h is impregnated under conditions of quasi- colon solution S CF pH=6.8, tests the 2nd respectively, 4,6,8, gained after the release rate of 10h NADH
Test result figure.
Tablet made from embodiment 1 is impregnated 8h under conditions of simulating colon solution S CF pH=6.8 by Fig. 2, is surveyed respectively
Try the 2nd, 4,6, resulting test result figure after the release rate of 8hNADH.
Specific embodiment
To make those skilled in the art that the purposes, technical schemes and advantages of invention be more clearly understood, below
Invention is further elaborated in conjunction with the accompanying drawings and embodiments.
Embodiment one
A kind of preparation process for the NADH nanosphere coating konjak glucomannan, including NADH nanosphere is dispersed
Obtain pre-composition in pharmaceutical adjunct, the pharmaceutical adjunct includes konjak glucomannan nanosphere, polyvinylpyrrolidone, micro-
Crystalline cellulose, calcium polyphosphate, xanthan gum, sodium alginate, magnesia and magnesium stearate；
Wetting agent and adhesive are added into the pre-composition, required cladding Amorphophallus rivieri glucomannan can be obtained after evenly mixing
Reveal the NADH nanosphere of glycan；
The NADH nanosphere, konjak glucomannan nanosphere, polyvinylpyrrolidone, microcrystalline cellulose, poly- phosphorus
Mass ratio between sour calcium, xanthan gum, sodium alginate, magnesia, magnesium stearate, wetting agent and adhesive is 1-20:20-80:
1-10:1-30:1-10:1-30:1-30:1-20:1-10:1-15:1-15.
Preferably, the wetting agent includes the ethyl alcohol and/or water of mass concentration 70%.Described adhesive includes 10wt%'s
One or more of pregelatinized starch, the starch slurry of 10wt% or hydroxypropyl methylcellulose of 10wt%.
Preferably, the konjak glucomannan nanosphere is by konjak glucomannan, quaternized konjaku glucomannan, carboxylic
At least one of methyl konjaku glucomannan, deacetylated konjaku glucomannan are made.It is described in some preferred embodiments
Konjak glucomannan nanosphere is modified konjaku glucomannans nanosphere, the NADH of the cladding konjak glucomannan
The preparation process of nanosphere further comprises the preparation of modified konjaku glucomannans nanosphere: by konjaku glucomannan, season
Ammonium konjaku glucomannan, Carboxymethyl Konjac Glucomannan or the one or more of of deacetylated konjaku glucomannan carry out chemical drop
Solution obtains the modified konjaku glucomannans that molecular weight is 8000-20000Da, then by the modified konjaku glucomannans
It is the system of required modified konjaku glucomannans nanosphere with the particle that sodium alginate co-ground obtains 200-1000nm
It is standby.Further, the chemical degradation are as follows: konjak glucomannan and hydrochloric acid or sodium hydroxide are sufficiently mixed 2-10h, i.e.,
Obtain modified konjaku glucomannans.Preferably, the mass ratio of the modified konjaku glucomannans and sodium alginate is 1:
0.5-5。
The beneficial effect of the preparation process of the NADH nanosphere of cladding konjak glucomannan provided by the present invention exists
In:
(1) by outside the unstable NADH of property coat konjak glucomannan (KGM) nano particle, KGM nanometers
NADH material protection inside it, is solved the problems, such as unstable, labile after NADH meets light or oxygen by particle, and what is obtained is compound
Object can save for a long time, which can be used for producing oral preparation, and NADH is made to be suitable for being used as medicine component.Meanwhile it will
After NADH and KGM is prepared as coated composites, NADH can be sustained within a certain period of time, avoid NADH component at once by gastric acid point
Solution, the composite nano-microsphere can be used for producing oral preparation, to anticancer.By from different supplementary product compatibilities, be also Parkinson
The improvement of the diseases such as disease, Alzheimer's disease, depression provides ideal drug.
NADH helps human body to anticancer from the following aspect, and the first step that cancer occurs first is that DNA is attacked by carcinogen
It hits, cause damage, and NADH has the function of that DNA repair enzyme is activated to help DNA plerosis, secondly NADH is a kind of strong oxidizer
It can help to remove interior free yl, cancer is prevented further to develop, third, the increasing that NADH can provide energy, prevent cancer cell
It growing, last NADH can activate NO synthase, promote the synthesis of NO, and NO can dissolve cancer cell, prevent its transfer.
(2) preparation process of the NADH nanosphere of cladding konjak glucomannan of the present invention, by NADH, KGM
Nanosphere is mixed with various auxiliary materials, obtains the composite material for being coated with konjak glucomannan nanosphere.It uses
In auxiliary material, xanthan gum have good adhesive effect, sodium alginate have concentrate solution, formed gel ability, with KGM,
Xanthan gum together, can form protective layer on the surface NADH, and NADH can be made to be sustained out.Microcrystalline cellulose, hydroxypropyl cellulose
So that composite material obtained is easy to compressing tablet process, it is more suitable for preparing medicinal preparation for oral administration, the step of preparation process is simple, condition temperature
With high production efficiency is suitable for industrialized mass production.
Embodiment two
A kind of NADH nanosphere coating konjak glucomannan, using cladding konjaku Portugal provided in embodiment one
The preparation process of the NADH nanosphere of mannosan is prepared.The NADH nanosphere of the cladding konjak glucomannan
Including NADH nanosphere, konjak glucomannan nanosphere is coated with outside the NADH nanosphere.Preferably, the NADH receives
The partial size of rice ball is 500-1000nm, and the partial size of the konjak glucomannan nanosphere is 200-1000nm.
Embodiment three
A kind of application for the NADH nanosphere coating konjak glucomannan, by the cladding Amorphophallus rivieri glucomannan in embodiment two
The NADH nanosphere of dew glycan is used to prepare oral class medicine object.Preferably, the oral class medicine object is particle, tablet or flexible glue
Capsule.
1, particle
The NADH nanosphere for coating konjak glucomannan can be prepared by particle using wet granulation technology, specifically
Be to be placed in the material for having weighed weight on a set of sieve that screen size is successively decreased from inside to outside, material is according to granular size point
Each layer compass screen surface is not stayed in, and wet feed obtained by then sieving is dried, and drying course is to be dried in vacuo 2h at 40 DEG C.The particle
The drug that can be used for producing pet treat can also be used for production anticancer drug, anticancer health-care product etc., and particle obtained can be in 8h
Sustained release NADH.
2, tablet
After particle is made in the NADH nanosphere for coating konjak glucomannan using wet granulation technology, by particle
Tablet can be prepared by tabletting, obtained tablet can also in 8h sustained release NADH effective component, the tablet can
For as anticancer drug, health medicine or pet drug.
3, soft capsule
The preparation process of soft capsule is as follows:
1) it prepares content: dried raw material being crossed into 60 meshes respectively first, raw material keeps drying, then will screen
Raw material carry out proportion weighing, while relevant auxiliary materials are added, and uniformly.The raw material is to coat konjak glucomannan
NADH nanosphere.
2) prepared by soft capsule body: first glycerol and water being added in glue pot, is then separately added into gelatin and relevant auxiliary materials, stirs
It mixes, vacuum outgas, flexible glue utricule is made.
3) prepare capsule: by above-mentioned prepared content and flexible glue utricule by pelleting, sizing is dry, wash ball, the ball that dries in the air,
Ball and packaging and other steps are picked up, soft capsule is made.
Some specific embodiments are provided below
Embodiment 1
The present embodiment provides a kind of preparation processes of soft capsule, and steps are as follows:
1) it prepares content: dried raw material being crossed into 60 meshes respectively first, raw material keeps drying, then will screen
Raw material carry out proportion weighing, while relevant auxiliary materials are added, and uniformly.
2) prepared by soft capsule body: now glycerol and water being added in glue pot, is then separately added into gelatin and relevant auxiliary materials, stirs
It mixes, vacuum outgas, flexible glue utricule is made.
3) prepare capsule: by above-mentioned prepared content and flexible glue utricule by pelleting, sizing is dry, wash ball, the ball that dries in the air,
Ball and packaging and other steps are picked up, soft capsule is made.
The NADH nanosphere of cladding konjak glucomannan (KGM) comprising NADH nanosphere, the NADH
KGM nanosphere is coated with outside nanosphere, wherein the partial size of the NADH nanosphere is 700nm, KGM nanometers described
The partial size of microballoon is 600nm, further includes other pharmaceutical adjuncts, and in the present embodiment, the KGM nanosphere is gathered by konjac mannan
Sugar is made.
This implementation also provides a kind of technique of NADH nanosphere for preparing cladding konjak glucomannan comprising as follows
Step:
S1, it disperses 10 parts by weight NADH nanospheres in pharmaceutical adjunct, obtains pre-composition, wherein the auxiliary material is with weight
Measure part meter, including 60 parts of konjak glucomannan nanospheres, 6 parts of polyvinylpyrrolidones, 14 parts of microcrystalline celluloses, 5 parts of poly- phosphorus
Sour calcium, 10 parts of xanthan gum, 10 parts of sodium alginates, 9 parts of magnesia, 5 parts of magnesium stearates.
In above-mentioned auxiliary material, xanthan gum has good adhesive effect, and sodium alginate has the ability for forming gel and film forming,
Layer protecting film is collectively formed in KGM nanosphere and sodium alginate and xanthan gum, plays the role of protecting NADH and is sustained NADH.It is poly-
Vinylpyrrolidone is a kind of aqueous high-molecular compound of synthesis, has a colloid protective effect, good film forming, caking property,
Hygroscopicity etc. also has excellent physiological compatibility.
S2,6 parts by weight wetting agents and 5 parts by weight of binder are added into the pre-composition, stir evenly, obtain cladding evil spirit
The NADH nanosphere of taro glucomannans nanosphere.Wherein, the wetting agent use concentration for 70% ethyl alcohol, the bonding
Agent is the pregelatinized starch of 10wt%.The pregelatinized starch has good disintegration, adhesive effect, can improve the hard of mixture
Degree, disintegration and surface brightness, also can be improved dissolution rate, the mixture added with pregelatinized starch is easily pelletized, particle granulating
Property and compressibility are good.
The KGM nanosphere is prepared using following technique:
A, by konjaku glucomannan chemical degradation, the konjaku glucomannan is total at normal temperature with the HCl of 0.5mol/L
With 6h is stirred to react, the modified konjaku glucomannans that viscosity average molecular weigh is 8000-20000Da is obtained.
B, the modified konjaku glucomannans and sodium alginate co-ground are obtained into the particle that partial size is 600nm, institute
The mass ratio for stating modified konjaku glucomannans and sodium alginate is 1:1.
It further, further include by composite nano-microsphere after the NADH nanosphere of preparation cladding konjak glucomannan
It is pelletized, i.e., is placed in the material for having weighed weight on a set of sieve that screen size is successively decreased from inside to outside with medium size steel wet sieving diameter,
Material stays in each layer compass screen surface according to granular size respectively, and wet feed obtained by then sieving is dried, and drying course is at 40 DEG C
It is dried in vacuo 2h.
The drug that the particle can be used for producing pet treat can also be used for production anticancer drug, anticancer health-care product etc., system
Particle can in 8h sustained release NADH.
Tablet further also is made by tabletting in particle in the present embodiment, obtained tablet can also persistently be released in 8h
NADH effective component is put, the tablet is used as anticancer drug, health medicine or pet drug.
Embodiment 2
The present embodiment provides a kind of NADH nanospheres for coating konjak glucomannan (KGM) comprising NADH nanometers
Microballoon is coated with KGM nanosphere outside the NADH nanosphere, wherein the partial size of the NADH nanosphere is
500nm, the partial size of the KGM nanosphere are 200nm, further include other pharmaceutical adjuncts, KGM nanometers described in the present embodiment
Microballoon is the mixture of quaternized konjaku glucomannan (QKGM), Carboxymethyl Konjac Glucomannan (CKMG).
This implementation also provides a kind of technique of NADH nanosphere for preparing cladding konjak glucomannan comprising as follows
Step:
S1, it disperses 1 parts by weight NADH nanosphere in pharmaceutical adjunct, obtains pre-composition, wherein the auxiliary material is with weight
Measure part meter, including 80 parts of konjak glucomannan nanospheres, 1 part of polyvinylpyrrolidone, 30 parts of microcrystalline celluloses, 1 part of poly- phosphorus
Sour calcium, 30 parts of xanthan gum, 1 part of sodium alginate, 20 parts of magnesia, 1 part of magnesium stearate.
In above-mentioned auxiliary material, xanthan gum has good adhesive effect, and sodium alginate has the ability for forming gel and film forming,
Layer protecting film is collectively formed in KGM nanosphere and sodium alginate and xanthan gum, plays the role of protecting NADH and is sustained NADH.It is poly-
Vinylpyrrolidone is a kind of aqueous high-molecular compound of synthesis, has a colloid protective effect, good film forming, caking property,
Hygroscopicity etc. also has excellent physiological compatibility.
S2,1 parts by weight wetting agent and 15 parts by weight of binder are added into the pre-composition, stir evenly, is coated
The NADH nanosphere of konjak glucomannan nanosphere.Wherein, the wetting agent use concentration for 70% second alcohol and water
The volume ratio of mixture, the ethyl alcohol and water is 3:1.Described adhesive be 10wt% starch slurry and 10% hypromellose
The mixture of element, the volume ratio of the two are 1:1.The hydroxypropyl methylcellulose has the function of improving disintegration, improves dissolution rate.
The KGM nanosphere is prepared using following technique:
A, by konjaku glucomannan chemical degradation, quaternized konjaku glucomannan (QKGM), carboxy methyl konjaku Portugal is sweet poly-
Sugared (CKMG) is stirred together for reaction 10h with the HCl of 0.1mol/L at normal temperature, and obtaining viscosity average molecular weigh is 8000-20000Da's
Modified konjaku glucomannans.
B, the modified konjaku glucomannans and sodium alginate co-ground are obtained into the particle that partial size is 200nm, institute
The mass ratio for stating modified konjaku glucomannans and sodium alginate is 1:3.
It further, further include by composite nano-microsphere after the NADH nanosphere of preparation cladding konjak glucomannan
It is pelletized, i.e., is placed in the material for having weighed weight on a set of sieve that screen size is successively decreased from inside to outside with medium size steel wet sieving diameter,
Material stays in each layer compass screen surface according to granular size respectively, and wet feed obtained by then sieving is dried, and drying course is at 40 DEG C
It is dried in vacuo 3h.
Particle obtained can in 8h sustained release NADH, can be used as anticancer drug, anticancer health-care product or pet drug.
Embodiment 3
The present embodiment provides a kind of NADH nanospheres for coating konjak glucomannan (KGM) comprising NADH nanometers
Microballoon is coated with KGM nanosphere outside the NADH nanosphere, wherein the partial size of the NADH nanosphere is
1000nm, the partial size of the KGM nanosphere are 1000nm, further include other pharmaceutical adjuncts, and in the present embodiment, the KGM is received
Meter Wei Qiu is deacetylated konjaku glucomannan (da-KGM).
This implementation also provides a kind of technique of NADH nanosphere for preparing cladding konjak glucomannan comprising as follows
Step:
S1, it disperses 20 parts by weight NADH nanospheres in pharmaceutical adjunct, obtains pre-composition, wherein the auxiliary material is with weight
Measure part meter, including 20 parts of konjak glucomannan nanospheres, 10 parts of polyvinylpyrrolidones, 1 part of microcrystalline cellulose, 10 parts of poly- phosphorus
Sour calcium, 1 part of xanthan gum, 30 parts of sodium alginates, 1 part of magnesia, 10 parts of magnesium stearates.
In above-mentioned auxiliary material, xanthan gum has good adhesive effect, and sodium alginate has the ability for forming gel and film forming,
Layer protecting film is collectively formed in KGM nanosphere and sodium alginate and xanthan gum, plays the role of protecting NADH and is sustained NADH.It is poly-
Vinylpyrrolidone is a kind of aqueous high-molecular compound of synthesis, has a colloid protective effect, good film forming, caking property,
Hygroscopicity etc. also has excellent physiological compatibility.
S2,15 parts by weight wetting agents and 1 parts by weight of binder are added into the pre-composition, stir evenly, is coated
The NADH nanosphere of konjak glucomannan nanosphere.Wherein, the wetting agent use concentration for 70% second alcohol and water
The volume ratio of mixture, the ethyl alcohol and water is 4:1.Described adhesive is the hydroxypropyl methylcellulose of 10wt%.The hydroxypropyl first
Cellulose has the function of improving disintegration, improves dissolution rate.
The KGM nanosphere is prepared using following technique:
A, by konjaku glucomannan chemical degradation, the konjaku glucomannan is common at normal temperature with the HCl of 1mol/L
It is stirred to react 2h, obtains the modified konjaku glucomannans that viscosity average molecular weigh is 8000-20000Da.
B, the modified konjaku glucomannans and sodium alginate co-ground are obtained into the particle that partial size is 1000nm, institute
The mass ratio for stating modified konjaku glucomannans and sodium alginate is 1:1.5.
It further, further include by composite nano-microsphere after the NADH nanosphere of preparation cladding konjak glucomannan
It is pelletized, i.e., is placed in the material for having weighed weight on a set of sieve that screen size is successively decreased from inside to outside with medium size steel wet sieving diameter,
Material stays in each layer compass screen surface according to granular size respectively, and wet feed obtained by then sieving is dried, and drying course is at 40 DEG C
It is dried in vacuo 2h.
It further, further include by the obtained particle of granulation with tablet press machine pressure is tablet, the tablet is easy to oral, and
Can in 8h sustained release NADH, can be used as anticancer drug, anticancer health-care product or pet drug.
Experimental example
1, tablet made from embodiment 1 is impregnated to 2h under conditions of simulation hydrochloric acid solution S GF pH=2 and then is being simulated
8h is impregnated under conditions of colon solution S CF pH=6.8, tests the release rate of the 2nd, 4,6,8,10h NADH, test result respectively
As shown in table 1 and Fig. 1.
Table 1
| Time h | Release rate % |
| 0 | 0 |
| 2 | 0.94 |
| 4 | 13.59 |
| 6 | 27.41 |
| 8 | 61.26 |
| 10 | 69.95 |
| Surplus | 8.08 |
2, tablet made from embodiment 1 is impregnated into 8h under conditions of simulating colon solution S CF pH=6.8, tested respectively
The release rate of 2nd, 4,6,8hNADH, test result is as shown in table 2 and figure 2.
Table 2
| Time h | Release rate % |
| 0 | 0 |
| 2 | 39.34 |
| 4 | 64.23 |
| 6 | 81.54 |
| 8 | 83.55 |
| Surplus | 1.38 |
Above-mentioned test result shows in the case where simulation hydrochloric acid solution and simulation colon solution impregnate, effective in tablet obtained
Ingredient NADH can be sustained into solution, be a kind of long-acting medicament.
Obviously, the above embodiments are merely examples for clarifying the description, and does not limit the embodiments.It is right
For those of ordinary skill in the art, can also make on the basis of the above description it is other it is various forms of variation or
It changes.There is no necessity and possibility to exhaust all the enbodiments.And it is extended from this it is obvious variation or
It changes still within the protection scope of the invention.
Claims (10)
1. a kind of preparation process for the NADH nanosphere for coating konjak glucomannan, it is characterised in that: including receiving NADH
Meter Wei Qiu, which is scattered in pharmaceutical adjunct, obtains pre-composition, and the pharmaceutical adjunct includes konjak glucomannan nanosphere, polyethylene
Pyrrolidones, microcrystalline cellulose, calcium polyphosphate, xanthan gum, sodium alginate, magnesia and magnesium stearate；
Wetting agent and adhesive are added into the pre-composition, it is poly- that required cladding konjac mannan can be obtained after evenly mixing
The NADH nanosphere of sugar；
The NADH nanosphere, konjak glucomannan nanosphere, polyvinylpyrrolidone, microcrystalline cellulose, calcium polyphosphate,
Mass ratio between xanthan gum, sodium alginate, magnesia, magnesium stearate, wetting agent and adhesive is 1-20:20-80:1-10:
1-30:1-10:1-30:1-30:1-20:1-10:1-15:1-15.
2. the preparation process of the NADH nanosphere of cladding konjak glucomannan as described in claim 1, it is characterised in that:
The konjak glucomannan nanosphere is sweet poly- by konjak glucomannan, quaternized konjaku glucomannan, carboxy methyl konjaku Portugal
At least one of sugared, deacetylated konjaku glucomannan is made.
3. the preparation process of the NADH nanosphere of cladding konjak glucomannan as claimed in claim 2, it is characterised in that:
The konjak glucomannan nanosphere is modified konjaku glucomannans nanosphere, the cladding konjak glucomannan
The preparation process of NADH nanosphere further comprises the preparation of modified konjaku glucomannans nanosphere: by konjak portuguese gansu polyose
Sugared, quaternized konjaku glucomannan, Carboxymethyl Konjac Glucomannan or the one or more of of deacetylated konjaku glucomannan carry out
Chemical degradation obtains the modified konjaku glucomannans that molecular weight is 8000-20000Da, then that the modified konjaku Portugal is sweet
It is required modified konjaku glucomannans nanometer that dew glycan and sodium alginate co-ground, which obtain the particle of 200-1000nm,
The preparation of ball.
4. the preparation process of the NADH nanosphere of cladding konjak glucomannan as claimed in claim 3, it is characterised in that:
The chemical degradation are as follows: konjak glucomannan and hydrochloric acid or sodium hydroxide are sufficiently mixed 2-10h to get modified konjaku Portugal is arrived
Mannosan.
5. the preparation process of the NADH nanosphere of cladding konjak glucomannan as claimed in claim 3, it is characterised in that:
The mass ratio of the modified konjaku glucomannans and sodium alginate is 1:0.5-5.
6. the preparation process of the NADH nanosphere of konjak glucomannan is coated as described in claim any one of 1-5,
It is characterized by: the wetting agent includes the ethyl alcohol and/or water of mass concentration 70%.
7. the preparation process of the NADH nanosphere of konjak glucomannan is coated as described in claim any one of 1-5,
It is characterized by: described adhesive includes the hydroxypropyl first fibre of the pregelatinized starch of 10wt%, the starch slurry of 10wt% or 10wt%
Tie up one or more of element.
8. a kind of NADH nanosphere for coating konjak glucomannan, it is characterised in that: using packet as described in claim 1
The preparation process for covering the NADH nanosphere of konjak glucomannan is prepared, the NADH of the cladding konjak glucomannan
Nanosphere includes NADH nanosphere, is coated with konjak glucomannan nanosphere outside the NADH nanosphere.
9. the NADH nanosphere of cladding konjak glucomannan as claimed in claim 8, it is characterised in that: the NADH receives
The partial size of rice ball is 500-1000nm, and the partial size of the konjak glucomannan nanosphere is 200-1000nm.
10. a kind of application for the NADH nanosphere for coating konjak glucomannan, it is characterised in that: will be such as claim 8 institute
The NADH nanosphere for the cladding konjak glucomannan stated is used to prepare oral class medicine object.
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| CN109908089A (en) * | 2019-03-27 | 2019-06-21 | 泓博元生命科技（深圳）有限公司 | Nanosphere and the preparation method and application thereof containing NADH or NADPH |
| CN110339179A (en) * | 2019-05-29 | 2019-10-18 | 泓博元生命科技（深圳）有限公司 | Soft capsule and its preparation method and application containing NADH or NADPH |
| WO2020113812A1 (en) * | 2018-12-03 | 2020-06-11 | 泓博元生命科技（深圳）有限公司 | Nadh-containing biological high-molecular-weight nanosphere, preparation method for same, and applications thereof |
| CN112807280A (en) * | 2021-01-07 | 2021-05-18 | 钇澜杉生物科技(北京)有限公司 | Preparation process and application of polysaccharide biopolymer coated NMN and NADH |
| WO2023000736A1 (en) * | 2021-07-20 | 2023-01-26 | 泓博元生命科技（深圳）有限公司 | Microcapsule powder stable in gastric acid, preparation method therefor and application thereof |
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| CN109350607A (en) * | 2018-07-03 | 2019-02-19 | 泓博元生命科技（深圳）有限公司 | The NADH nanosphere and its preparation process of cladding konjak glucomannan and application |
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| CN109350607A (en) * | 2018-07-03 | 2019-02-19 | 泓博元生命科技（深圳）有限公司 | The NADH nanosphere and its preparation process of cladding konjak glucomannan and application |
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| WO2020113812A1 (en) * | 2018-12-03 | 2020-06-11 | 泓博元生命科技（深圳）有限公司 | Nadh-containing biological high-molecular-weight nanosphere, preparation method for same, and applications thereof |
| CN109908089A (en) * | 2019-03-27 | 2019-06-21 | 泓博元生命科技（深圳）有限公司 | Nanosphere and the preparation method and application thereof containing NADH or NADPH |
| WO2020192557A1 (en) * | 2019-03-27 | 2020-10-01 | 泓博元生命科技（深圳）有限公司 | Nadh or nadph-containing nano-microsphere and preparation method therefor and application thereof |
| CN110339179A (en) * | 2019-05-29 | 2019-10-18 | 泓博元生命科技（深圳）有限公司 | Soft capsule and its preparation method and application containing NADH or NADPH |
| CN112807280A (en) * | 2021-01-07 | 2021-05-18 | 钇澜杉生物科技(北京)有限公司 | Preparation process and application of polysaccharide biopolymer coated NMN and NADH |
| CN112807280B (en) * | 2021-01-07 | 2023-02-03 | 钇澜杉合成生物技术(北京)有限公司 | Preparation process and application of polysaccharide biopolymer coated NMN and NADH |
| WO2023000736A1 (en) * | 2021-07-20 | 2023-01-26 | 泓博元生命科技（深圳）有限公司 | Microcapsule powder stable in gastric acid, preparation method therefor and application thereof |
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