CN107095852A - Resveratrol oral disnitegration tablet - Google Patents
Resveratrol oral disnitegration tablet Download PDFInfo
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- CN107095852A CN107095852A CN201710160074.5A CN201710160074A CN107095852A CN 107095852 A CN107095852 A CN 107095852A CN 201710160074 A CN201710160074 A CN 201710160074A CN 107095852 A CN107095852 A CN 107095852A
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- China
- Prior art keywords
- resveratrol
- pvpp
- disnitegration tablet
- oral
- oral disnitegration
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Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/045—Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
- A61K31/05—Phenols
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/2027—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
Abstract
A kind of resveratrol oral disnitegration tablet, microcrystalline cellulose, PVPP, low-substituted hydroxypropyl cellulose are have selected for major auxiliary burden by single factor experiment and orthogonal test of multiple factors result.It the experiment proved that, oral disnitegration tablet resveratrol dissolution rate of the invention is accelerated, and resveratrol can at utmost improve the bioavilability of resveratrol by the mucosa absorption in oral cavity or esophagus.
Description
Technical field：
It is more particularly to a kind of to improve the white black false hellebore of bioavailability of resveratrol the present invention relates to a kind of pharmaceutical preparation
Alcohol oral disnitegration tablet.
Background technology：
Resveratrol (resveratrol, Res), is a kind of aldehydes matter of non-flavonoids, is colorless needle crystals, difficult
Be dissolved in water, be soluble in ether, chloroform, methanol, ethanol and propyl alcohol, with the sharp liver of liver protection, anti-inflammatory, antiallergy, resisting pathogenic microbes,
The anti-multiple beneficial such as cardiovascular, antitumor is in the biological action of human body.
The difficult soluble substance of resveratrol, into internal rear rapid metabolization, internal blood concentration is far below experiment in vitro
Valid density, thus be not enough to play corresponding bioactivity, therefore, how to improve bioavailability of resveratrol turns into mesh
Preceding exploitation resveratrol product urgent problem to be solved.
The content of the invention
The oral resveratrol preparation of bioavailability of resveratrol can be improved it is an object of the invention to provide a kind of.
In order to improve the bioavilability of resveratrol, the present invention is with microcrystalline cellulose, PVPP, low-substituted hydroxypropyl
Base cellulose and citric acid etc. are that auxiliary material develops a kind of resveratrol oral disnitegration tablet.Resveratrol can pass through oral cavity or esophagus
Interior mucosa absorption, at utmost improves the bioavilability of resveratrol.
The present invention determines the type and consumption of auxiliary material by experiment of single factor, be disintegrated according to oral disnitegration tablet, decentralization it is special
It is different to require, filler, disintegrant and adhesive in prescription are screened.Collapsed by the preferred resveratrol oral cavity of orthogonal experiment
The optimal preparation technology of piece is solved, and has formulated its quality standard.
The proportioning (weight part ratio) for the resveratrol oral disnitegration tablet that the present invention is provided is as follows：
Resveratrol 100, microcrystalline cellulose (MCC) 45-55, PVPP (PVPP) 42-52, low substituted hydroxy-propyl is fine
Tie up element (L-HPC) 10-15.
The preferred proportion of mentioned component is：Resveratrol 100, microcrystalline cellulose 52, PVPP 50, low-substituted hydroxypropyl
Base cellulose 13.
Those skilled in the art can add the tablets such as flavouring, lubricant and often use assistant agent according to actual needs.
In an example of the invention, it is formulated as follows：
Resveratrol 100g, microcrystalline cellulose 52g, PVPP 50g, low-substituted hydroxypropyl cellulose 13g, citric acid
4g, stevioside 2g, fruit essence 2g, magnesium stearate 1g
The advantageous effects of the present invention are：It is prepared into resveratrol dissolution rate after oral disnitegration tablet to accelerate, favorably
The advantages of bioavilability is improved.By testing the quality and dissolution rate of detection resveratrol oral disnitegration tablet, as a result show,
The dissolution rate that resveratrol is substantially increased after oral disnitegration tablet is prepared into, bioavilability is improved.
Brief description of the drawings
Fig. 1 is the comparison of oral disnitegration tablet and conventional tablet agent dissolution rate.
It can be seen that oral disnitegration tablet resveratrol dissolution rate is substantially better than ordinary tablet.
Embodiment
Experiment instrument and reagent are as follows below：
Instrument：
ZRD6-A types medicine intelligence dissolution rate instrument (Shanghai Huanghai Sea medicine inspection instrument plant)；
CS22B friabilators (Tianjin Chuan Xing electronic equipment manufacturings Co., Ltd)；
UlitMate3000 high performance liquid chromatographs；
TDP type single-punch tablet presses；
CQX25-06 types ultrasonic cleaner (Shanghai must can believe ultrasonic Co., Ltd),
TA2004 type analysis balance (Shanghai instrument manufacturing factory).
Reagent：
Resveratrol (the prosperous bio tech ltd's lot number in Hubei Province three：20160910),
Microcrystalline cellulose (MCC, Shanghai thick really Fine Chemical Works, lot number：20160511),
Low-substituted hydroxypropyl cellulose (L-HPC, lot number：20160407),
PVPP (Pvpp, lot number：20160302),
Sodium carboxymethyl starch (CMC-Na, lot number：20160507),
Tween 80 (Dalian reagent Co., Ltd).
Water is purified water, and remaining reagent is that analysis is pure.
The resveratrol oral disnitegration tablet of embodiment 1
Formula：
Resveratrol 100g, microcrystalline cellulose 52g, PVPP 50g, low-substituted hydroxypropyl cellulose 13g, citric acid
4g, stevioside 2g, fruit essence 2g, magnesium stearate 1g
Preparation method：
The main ingredient and auxiliary material of recipe quantity are weighed, 80 mesh sieves are crossed respectively, first by resveratrol and PVPP equal increments
Method is well mixed, then by microcrystalline cellulose, low-substituted hydroxypropyl cellulose is mixed with method, and binder is made with 85% ethanol, wet
Method is pelletized, and stevioside and fruit essence are added after whole grain, magnesium stearate is added, and is mixed, is pressed into 1000.
The resveratrol oral disnitegration tablet of embodiment 2
Formula：
Resveratrol 100g, microcrystalline cellulose 50g, PVPP 42g, low-substituted hydroxypropyl cellulose 15g, citric acid
4g, stevioside 2g, fruit essence 2g, magnesium stearate 1g
Preparation method such as embodiment 1.
The resveratrol oral disnitegration tablet of embodiment 3
Formula：
Resveratrol 100g, microcrystalline cellulose 55g, PVPP 52g, low-substituted hydroxypropyl cellulose 12g, citric acid
4g, stevioside 2g, fruit essence 2g, magnesium stearate 1g
Preparation method such as embodiment 1.
Filler, disintegrant and adhesive screening test
Be disintegrated according to oral disnitegration tablet, decentralization particular/special requirement, following sieve has been carried out to filler, disintegrant and adhesive
Choosing：
First, experiment of single factor
Test the selection of 1 filler
Experimental method：
The species and consumption of filler in fixed prescription, fixed tableting pressure, with disintegration time limited and 30min accumulation dissolution
Spend for evaluation index, the influence to tablet quality when starch, lactose, microcrystalline cellulose make filler is investigated respectively；
Experimental result：
It is shown in Table 1.
The filler of table 1 is selected
Experiment conclusion：
When making filler from microcrystalline cellulose, tablet forming, surface aesthetic, disintegration and dissolution rate are conformed to
Ask, therefore selection microcrystalline cellulose is filler.
Test the selection of 2 disintegrants
Experimental method：
Using disintegration time limited and accumulation dissolution rate as evaluation index, the consumption of microcrystalline cellulose is fixed in prescription, is investigated respectively
Influence of the species, consumption of disintegrant to tablet.
Experimental result：
As a result the use in conjunction of disintegrant is shown, disintegration time limited is substantially better than independent disintegrant.
Sodium carboxymethylcellulose (CMC-Na) and PVPP (PVPP), PVPP (PVPP) and low-substituted hydroxypropyl
Base cellulose (L-HPC), low-substituted hydroxypropyl cellulose (L-HPC) are disintegrated with sodium carboxymethylcellulose (CMC-Na) use in conjunction
Effect with dissolution is preferable, wherein being disintegrated with PVPP (PVPP) with low-substituted hydroxypropyl cellulose (L-HPC) and molten
Go out effect best.
The disintegrant of table 2 is selected
Experiment conclusion：As a result (being shown in Table 2) is shown, with PVPP (PVPP) and low-substituted hydroxypropyl cellulose (L-
HPC it is) preferable for disintegrant.
Test the selection of 3 disintegrant feed postitions
Experiment purpose：
The different Adding Way of disintegrant has a certain impact to disintegration time limited, is that interior addition has been investigated in this this experiment respectively
Influence with the inside and outside method for respectively Jia 50% to disintegration time limited.
Experimental result：
As a result interior addition disintegration time limited 50s, the inside and outside disintegration time limited 40s for respectively Jia 50% shows respectively to add using inside and outside
50% method tabletting, disintegration time is substantially better than interior add.
Experiment conclusion：
Disintegrant is using inside and outside addition.
Test the selection of 4 adhesive concentration of alcohol
Experimental method：
In the case where main ingredient, filler and disintegrant etc. are constant, 75%, 85% and 95% ethanol conduct has been investigated respectively
The slice, thin piece hardness of adhesive and disintegration time limited,.
Experimental result and conclusion：
It is good as the slice, thin piece hardness of adhesive using 75%, 85% and 95% ethanol.75% ethanol is used for bonding
Agent disintegration time limited is 53s, and 85% ethanol makees adhesive for 39s, and 95% ethanol makees adhesive for 45s, as a result shows with 85% second
It is ideal that alcohol makees adhesive.
Test the selection of 5 lubricants
Experimental method：
Lubricant can improve the mobility and fillibility of particle before tabletting.The cunning for comparing different additions is investigated respectively
Stone flour and magnesium stearate help fluidity, particle angle of repose, flow velocity and tablet weight variation.
Experimental result and conclusion：
By comparing, select using 0.4% (W/W) magnesium stearate as lubricant.
2nd, orthogonal test of multiple factors
Experimental method：
The principal element of pre- test result display influence Orally disintegrating tablet quality has：Filler MCC consumption (A), disintegrant
L-HPC (B) and PVPP consumption (C) and the consumption (D) of 85% ethanol.
L is pressed using orthogonal design9(34) orthogonal trial experiment, with accumulation dissolution percentage in the water of 60min resveratrols
Rate is that index is evaluated, and determines best prescription.
Variance analysis：
As a result extreme difference R shows that four factor influence sizes of this experiment are A>C>B>D, it follows that MCC consumption is influence
The principal element of Orally disintegrating tablet quality, and variance analysis shows that MCC has significant difference (P ＜ 0.05), PVPPH and L-
HPC is secondary cause, and each factor level influence size is：A:1>2>3；B:1>3>2；C:3>2>1；D:1>3>2, it is thus determined that most
Good prescription is A1B1C3D1, i.e. embodiment 1 formula.Refer to table 3,4,5.
The orthogonal experiment factor level table of table 3
The orthogonal experiment of table 4 and result
The variance analysis of table 5
F0.05(2 2)=19
Checking test
By preferred A1B1C3D1Technique carries out 3 batches of experiments.The average dissolution rate of result oral disnitegration tablet is 78%, is disperseed
Uniformity and weight differential meet regulation.
Experiment conclusion：
The formulation efficacy of embodiment 1 is optimal.
3rd, with resveratrol conventional tablet agent Comparative Study on Dissolution
Sample：Sample (lot number is prepared according to formula and preparation method under example 1：20161011)
Experimental method：
The resveratrol oral disnitegration tablet of Example 16,
According to《Chinese Pharmacopoeia》Two methods of annex XC Dissolution Rate Testings the 3rd of version in 2010, with 900ml hydrochloric acid (9 → 1000)
Solution is dissolution medium, bath temperature (37 ± 0.5 DEG C), and rotating speed is 50rmin-1, respectively at 3,5,10,20,30,60,
90min samples 5mL, while adding the blank dissolution medium 5mL of equitemperature, with 0.45um filtering with microporous membrane, takes subsequent filtrate,
Its concentration is determined, stripping curve is drawn.
Conventional tablet separately is taken, is sampled by above-mentioned condition respectively at 3,5,10,20,30,60,90min, is determined its concentration, paint
Stripping curve processed.
Experimental result：
See Fig. 1.It can be seen that the resveratrol oral disnitegration tablet dissolution rate of inventive formulation is substantially better than white black false hellebore
Alcohol ordinary tablet.
Claims (5)
1. a kind of oral resveratrol preparation, it is characterized in that, the preparation is oral disnitegration tablet, prepares the raw material of the preparation
Weight is as follows：
Resveratrol 100, microcrystalline cellulose 45-55, PVPP 42-52, low-substituted hydroxypropyl cellulose 10-15.
2. the oral formulations described in claim 1, the weight for preparing the raw material of the preparation is as follows：
Resveratrol 100, microcrystalline cellulose 52, PVPP 50, low-substituted hydroxypropyl cellulose 13.
3. the oral formulations described in claim 1, also containing one kind in filler, disintegrant, disintegrant, lubricant or several
Kind.
4. oral formulations described in claim 3, the filler is microcrystalline cellulose, the disintegrant is that low substituted hydroxy-propyl is fine
Dimension element and PVPP, described adhesive are 85% ethanol, and the lubricant is magnesium stearate.
5. a kind of resveratrol oral disnitegration tablet, the weight for preparing the raw material of the oral disnitegration tablet is as follows：
Resveratrol 100g, microcrystalline cellulose 52g, PVPP 50g, low-substituted hydroxypropyl cellulose 13g, citric acid 4g,
Stevioside 2g, fruit essence 2g, magnesium stearate 1g.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201710160074.5A CN107095852A (en) | 2017-03-17 | 2017-03-17 | Resveratrol oral disnitegration tablet |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201710160074.5A CN107095852A (en) | 2017-03-17 | 2017-03-17 | Resveratrol oral disnitegration tablet |
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| Publication Number | Publication Date |
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| CN107095852A true CN107095852A (en) | 2017-08-29 |
Family
ID=59675074
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201710160074.5A Pending CN107095852A (en) | 2017-03-17 | 2017-03-17 | Resveratrol oral disnitegration tablet |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN108968051A (en) * | 2018-08-06 | 2018-12-11 | 大连医诺生物股份有限公司 | Resveratrol sustained release preparation and preparation method thereof |
Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101199540A (en) * | 2007-12-18 | 2008-06-18 | 深圳海王药业有限公司 | Polygonin sheet dose and preparing method thereof |
| US20140057839A1 (en) * | 2012-08-27 | 2014-02-27 | Red Mountain Med Spa, LLC | Formulations and methods for weight loss and body contouring |
| CN103622925A (en) * | 2012-08-30 | 2014-03-12 | 山东博奥克生物科技有限公司 | Resveratrol tablet and preparation method therefor |
| CN104706607A (en) * | 2015-03-31 | 2015-06-17 | 临沂大学 | Preparation method of resveratrol dispersible tablet |
| US20160346308A1 (en) * | 2014-02-07 | 2016-12-01 | Shaker A. Mousa | Composition and method of use for combinations of anti-viral protease, polymerase inhibitors and natural bioactive compounds in the treatment of hepatitis c infection |
-
2017
- 2017-03-17 CN CN201710160074.5A patent/CN107095852A/en active Pending
Patent Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101199540A (en) * | 2007-12-18 | 2008-06-18 | 深圳海王药业有限公司 | Polygonin sheet dose and preparing method thereof |
| US20140057839A1 (en) * | 2012-08-27 | 2014-02-27 | Red Mountain Med Spa, LLC | Formulations and methods for weight loss and body contouring |
| CN103622925A (en) * | 2012-08-30 | 2014-03-12 | 山东博奥克生物科技有限公司 | Resveratrol tablet and preparation method therefor |
| US20160346308A1 (en) * | 2014-02-07 | 2016-12-01 | Shaker A. Mousa | Composition and method of use for combinations of anti-viral protease, polymerase inhibitors and natural bioactive compounds in the treatment of hepatitis c infection |
| CN104706607A (en) * | 2015-03-31 | 2015-06-17 | 临沂大学 | Preparation method of resveratrol dispersible tablet |
Non-Patent Citations (2)
| Title |
|---|
| 中国执业药师协会组织编写: "《2008年度全国执业药师继续教育教材》", 30 April 2008, 中国中医药出版社 * |
| 喻樊等: "白藜芦醇口崩片制备工艺及质量评价研究", 《中草药》 * |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN108968051A (en) * | 2018-08-06 | 2018-12-11 | 大连医诺生物股份有限公司 | Resveratrol sustained release preparation and preparation method thereof |
| CN108968051B (en) * | 2018-08-06 | 2022-07-12 | 大连医诺生物股份有限公司 | Resveratrol sustained-release preparation and preparation method thereof |
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Application publication date: 20170829 |