CN101543298B - Rutin chewing agent and method for preparing same - Google Patents

Abstract

The invention relates to an oral rutin chewing agent and a method for preparing the same. The rutin chewing agent comprises 1 to 50 percent of rutin, 20 to 96 percent of thinner, 2 to 50 percent of vitamin C and 0 to 10 percent of additive. The invention also provides a method for preparing rutin chewing powder, a rutin chewing particle and a rutin chewing tablet. The method for preparing the rutin chewing agent comprises the following steps that: hydrophilic auxiliary materials are used as a main thinner; and by adopting the advanced preparation technology, the rutin is highly dispersed in the materials, so that the solubility of the rutin in water is increased, the dissolution rate is quick, and the biological utilization rate is improved. Compared with the conventional rutin oral solid dosage form, the rutin chewing agent has the advantages of high oral biological utilization rate and good taste, and easy acceptance by a patient, improving the compliance of the patient on taking the drug and facilitating the absorption. Moreover, the chewing agent is firstly chewed into fine powder in the mouth, thereby increasing the dissolving and dispersing rates of the active ingredients. Therefore, the chewing agent is suitable to be used by the patient suffering the dysphagia.

Description

Rutin chewing agent and preparation method thereof

Technical field

The present invention relates to a kind of oral rutin chewing agent and preparation method thereof.

Background technology

Rutin has another name called rutin sophorin, is a kind of active ingredient of natural plant with extensive physiologically active.Rutin can be strengthened ascorbic effect, promotes vitamin C to put aside in vivo, and the human body lipid cholesterol is reduced; Rutin is kept the normal resistance of capillary, reduces permeability, reduces the effect of its fragility, can prevent and treat hypertension.Rutin can also suppress hematoblastic gathering, prevents thrombosis, can resist simultaneously the injury of blood vessel that 5 one hydroxytryptamines, bradykinin cause, can prevent the oedema that vasopermeability raises and causes.In addition, rutin Anhydroalkannin, diuresis, antiallergy have significantly antitumor, anti-oxidant and influence effect such as various enzymatic activitys, are the important component in the Chinese herbal medicine for preventing prescription.

Rutin is present in the plant of multiple integration of drinking and medicinal herbs, like buckwheat, the sophora bud, asparagus, red date etc., for the development and use of rutin provide wide natural resources.The rutin side effect is little, in the disease treatment process, is bringing into play the complex treatment effect and the overall efficiency of multipath, many target spots, has the incomparable advantage of Western medicine, can be used as health food or medicine and uses.Clinically, rutin is used to treat cardiovascular and cerebrovascular diseases such as hypertension, cerebral hemorrhage, also can prevent and treat diabetes and reducing blood lipid simultaneously.

At present, having multiple on the market is the health products and the medicine sale of functional component with the rutin, like buckwheat tea in bag, rutin parenteral solution, rutin tablets and rutin sustained release preparation etc.Health-related food preparation technology is comparatively coarse, and active constituent content wherein is low, a little less than the health care and therapeutic action relatively to disease; Injection is inconvenient because of method of administration, be used for the emergency and severe disease patient more, limited its suffer from chronic disease, application among the crowd that need take medicine for a long time; Oral solid formulation such as tablet, granule, sustained release tablets etc. can reach the purpose of slowly-releasing or quick-release through the auxiliary material of packaging technique or use different performance because medication conveniently, is easy to carry about with one and transports, and medicine stability is high, become application formulation the most widely.Rutin is mainly used in chronic diseases such as treatment cardiovascular and cerebrovascular disease, diabetes, and oral solid formulation is its suitable formulation, but because of the rutin poorly water-soluble, oral administration biaavailability is low, makes the clinical therapeutic efficacy of this type preparation unsatisfactory.

Summary of the invention

The object of the present invention is to provide a kind of mouthfeel good, the rutin bioavilability is high, is beneficial to rutin chewing agent of absorption and preparation method thereof.

A kind of rutin chewing agent is characterized in that: comprise rutin 1%-50% in the said masticatory, diluent 20%-96%, vitamin C 2%-50% and additive 0%-10%.

Scheme further is: described additive is one or more in flavouring, lubricant, wetting agent and the adhesive.

Scheme further is: described flavouring is one or more in peppermint oil, orange oil, caryophyllus oil, oil of ginger, flavoring orange essence, lemon extract, strawberry essence, cherry essence, flavoring banana essence, syrup, sucrose, honey, xylitol, maltose, stevioside, the aspartame; Said lubricant is one or more in stearic acid, dolomol, calcium stearate, talcum powder, hydrogenated vegetable oil, polyethylene glycol, lauryl sodium sulfate, Stepanol MG, the superfine silica gel powder; Said wetting agent is water and the fused solution of ethanol; Said adhesive is to comprise a kind of in PVP, cellulose family adhesive, starch slurry, syrup, the rubber cement.

Scheme further is: comprise rutin 2%-30% in the said masticatory, diluent 40%-90%, vitamin C 4%-30% and additive 0.1%-8%.

Scheme further is: said diluent is one or more in sweet mellow wine, lactose, glucose, sorbierite, sucrose, microcrystalline cellulose, starch, dextrin and the pregelatinized starch.

Scheme further is: described rutin chewing agent is that rutin chews powder.

A kind ofly prepare the method that above-mentioned rutin chews powder, it is characterized in that passing through successively step 1 to step 3:

Step 1 is got 1%-50% rutin and 2%-50% vitamin C, pulverizes, and crosses 100 mesh sieves;

Step 2 adds 20%-93% diluent, 1%-5% flavouring and 0.1%-3% lubricant, mixes;

Step 3 sub-dose packaging.

Scheme further is: described rutin chewing agent is that rutin chews granule.

A kind ofly prepare the method that rutin chews granule, it is characterized in that passing through successively step 4 to step 10:

Step 4 is got 1%-50% rutin, 2%-50% vitamin C, 20%-93% diluent, 1%-5% flavouring, pulverizes, and crosses 80 mesh sieves;

Step 5 mixes rutin and vitamin C, diluent and flavouring, makes its high degree of dispersion in material;

Step 6 adds an amount of wetting agent or adhesive, processes softwood;

Step 7 softwood is crossed 14 mesh sieves, makes wet granular;

Step 8 is at 50-70 ℃ of following dry wet particle 0.5-2h;

Step 9 is got dried particle, sieve whole grain, classification;

Step 10 adds the 0.1%-3% lubricant, sub-dose packaging behind the mixing.

Scheme further is: described rutin chewing agent is the rutin chewable tablets.

A kind of method for preparing the rutin chewable tablets is characterized in that passing through successively step 11 to step 15:

Step 11 is got 1%-50% rutin, 2%-50% vitamin C, 20%-93% diluent, pulverizes, and crosses 80 mesh sieves;

Step 12 is even with rutin, vitamin C, mixing diluents, and rutin is dispersed in the material;

Step 13 is got the 0.1%-3% lubricant, pulverizes, and cross 100 mesh sieves and add in the mixture, and abundant mixing;

Step 14 adds 0.5%-2% aromatic, mixing, airtight 2-4 hour;

Step 15 compressing tablet;

A kind of method for preparing the rutin chewable tablets is characterized in that passing through successively step 16 to step 23:

Step 16 is got 1%-50% rutin, 2%-50% vitamin C, 20%-93% diluent, 1%-5% flavouring, pulverizes, and crosses 80 mesh sieves;

Step 17 is with the abundant mixing of rutin, vitamin C, diluent and flavouring;

Step 18 adds an amount of wetting agent or adhesive, the preparation softwood;

Step 19 softwood is crossed 14 mesh sieves, makes wet granular;

Step 20 is at 50-70 ℃ of following dry wet particle 0.5-2h, and the control moisture is at 1%-3%;

The dried particle of step 21 is crossed the whole grain of 16 mesh sieves;

Step 22 is got the 0.1%-3% lubricant, crosses 100 mesh sieves and adds in the dried particle mixing;

Step 23 compressing tablet.

Said rutin comprises that purity is greater than 70% rutin raw material, the active component that comprises rutin and the rutin derivatives that from plant, extract.

Said rutin derivatives refers to the rutin to be salt, ester, rutin of the rutin of main active and compound or complex compound, structure of modification product and the analyte that other compound forms.

The salt of said rutin comprises sodium salt, sylvite, calcium salt, zinc salt, selenium salt of rutin etc.

Said rutin ester comprises rutin acetic acid esters, formic acid esters, malate, propionic ester, citrate etc.

Said rutin also comprises the combination of rutin and other drug.

Rutin chewing agent of the present invention, with hydrophilicity condiment as main diluent; Adopt advanced preparation technique to make the rutin high degree of dispersion in material, thereby increase the solubility of rutin in water, dissolution rate is accelerated, and bioavilability improves.

Compare with traditional rutin oral dosage form, rutin chewing agent of the present invention is except that oral administration biaavailability is higher relatively, and other has following advantage: 1) mouthfeel is good, is prone to accepted by the patient, has increased the compliance of patient's medication; 2) be beneficial to absorption.Masticatory at first need be chewed into fine powder in the oral cavity, increased the speed of active ingredient dissolving and diffusion; 3) be suitable for having the patient of aphetite disorder to use.

The practical implementation method

Through the practical implementation instance, can further understand the present invention, but following instance is not a limitation of the present invention.

Embodiment 1

Rutin chews the preparation of particle (1)

Rutin 100g, sweet mellow wine 450g, lactose 450g, flavoring orange essence 1g.Get rutin, sweet mellow wine, lactose, flavoring orange essence, pulverize, cross 80 mesh sieves, put and grind 10min in the beveller and make fully and mix; With 3%PVP ethanolic solution system softwood, cross 14 mesh sieves, get wet granular, wet granular is tiled on the porcelain dish; Thickness is no more than 3mm, and dry 30min under 60 ℃ crosses No. 1 sieve and No. 5 sieves respectively and carries out whole grain and classification; Add 1% talcum powder, mixing, sub-dose packaging in the particle.

Embodiment 2

Rutin chews the preparation of particle (2)

Rutin 100g, sweet mellow wine 300g, xylitol 100g, vitamin C 100g, lactose 350g, glucose 50g.Get rutin, sweet mellow wine, xylitol, vitamin C, lactose, glucose, pulverize, cross 80 mesh sieves, put and grind 10min in the beveller and make fully and mix; With 20% ethanolic solution system softwood, cross 14 mesh sieves, get wet granular, wet granular is tiled on the porcelain dish; Thickness is no more than 3mm, and dry 1h under 60 ℃ crosses No. 1 sieve and No. 5 sieves respectively and carries out whole grain and classification; Add 1% talcum powder, mixing, sub-dose packaging in the particle.

Embodiment 3

Rutin chews the preparation of powder

Rutin 100g, xylitol 100g, vitamin C 100g, lactose 700g.Get rutin and vitamin C, pulverize, cross 100 mesh sieves, add xylitol, by equivalent progressively increase method and lactose mixing, sub-dose packaging.

Embodiment 4

The preparation of rutin chewable tablets

Rutin 100g, sweet mellow wine 300g, xylitol 100g, vitamin C 100g, lactose 400g, flavoring orange essence 1g.Get rutin, sweet mellow wine, xylitol, vitamin C, lactose, flavoring orange essence, pulverize, cross 80 mesh sieves, put and grind 10min in the beveller and make fully and mix; With 20% ethanolic solution system softwood, cross 14 mesh sieves, get wet granular, wet granular is tiled on the porcelain dish; Thickness is no more than 3mm, and dry 1h under 60 ℃ is with the whole grain of 16 mesh sieves; Add 1% talcum powder, mixing, compressing tablet.

Adopt that " 2005 editions two appendix XC dissolution methods of Chinese pharmacopoeia, one method has been measured the dissolution rate of rutin chewable tablets, and rotating speed is 100rmin ^-1, the result sees table 1.

The dissolution rate of table 1 rutin chewable tablets

Can be found out that by table 1 rutin in the chewable tablets is in 1h stripping basically, assimilation effect is better.

Claims (2)

1. preparation method that rutin chews particle is characterized in that passing through successively step 4 to step 10:

Step 4 is got 1%-50% rutin, 2%-50% vitamin C, 20%-93% diluent, 1%-5% flavouring, pulverizes, and crosses 80 mesh sieves;

Step 5 mixes rutin and vitamin C, diluent and flavouring, makes its high degree of dispersion in material;

Step 6 adds an amount of wetting agent or adhesive, processes softwood;

Step 7 softwood is crossed 14 mesh sieves, makes wet granular;

Step 8 is at 50-70 ℃ of following dry wet particle 0.5-2h;

Step 9 is got dried particle, sieve whole grain, classification;

Step 10 adds the 0.1%-3% lubricant, sub-dose packaging behind the mixing;

Described flavouring is one or more in peppermint oil, orange oil, caryophyllus oil, oil of ginger, flavoring orange essence, lemon extract, strawberry essence, cherry essence, flavoring banana essence, syrup, sucrose, honey, xylitol, maltose, stevioside, the aspartame; Said wetting agent is water and the fused solution of ethanol;

Said lubricant is one or more in talcum powder, hydrogenated vegetable oil, polyethylene glycol, lauryl sodium sulfate, Stepanol MG, the superfine silica gel powder;

Said adhesive is to comprise a kind of in PVP, syrup, the rubber cement;

Said diluent is one or more in sweet mellow wine, lactose, glucose, sorbierite, sucrose, microcrystalline cellulose, the dextrin.

2. the preparation method of a rutin chewable tablets is characterized in that passing through successively step 16 to step 23:

Step 16 is got 1%-50% rutin, 2%-50% vitamin C, 20%-93% diluent, 1%-5% flavouring, pulverizes, and crosses 80 mesh sieves;

Step 17 is with the abundant mixing of rutin, vitamin C, diluent and flavouring;

Step 18 adds an amount of wetting agent or adhesive, the preparation softwood;

Step 19 softwood is crossed 14 mesh sieves, makes wet granular;

Step 20 is at 50-70 ℃ of following dry wet particle 0.5-2h, and the control moisture is at 1%-3%;

The dried particle of step 21 is crossed the whole grain of 16 mesh sieves;

Step 22 is got the 0.1%-3% lubricant, crosses 100 mesh sieves and adds in the dried particle mixing;

Step 23 compressing tablet;

Described flavouring is one or more in peppermint oil, orange oil, caryophyllus oil, oil of ginger, flavoring orange essence, lemon extract, strawberry essence, cherry essence, flavoring banana essence, syrup, sucrose, honey, xylitol, maltose, stevioside, the aspartame; Said lubricant is one or more in talcum powder, hydrogenated vegetable oil, polyethylene glycol, lauryl sodium sulfate, Stepanol MG, the superfine silica gel powder;

Said wetting agent is water and the fused solution of ethanol;

Said adhesive is to comprise a kind of in PVP, syrup, the rubber cement;

Said diluent is one or more in sweet mellow wine, lactose, glucose, sorbierite, sucrose, microcrystalline cellulose, the dextrin.