Solid dosage form of ifosfamide

 

(57) Abstract:

Solid legform for oral application made in the form of capsules containing mainly ifosfamide as active ingredient and microcrystalline cellulose, or made in the form of tablets containing per wt.h. the ifosfamide of 0.1 to 1.0 wt.h tricalcium phosphate and 0.04 to 0.4 wt.h. polyethylene glycol, and (based on the weight of the tablet) 5 to 60 wt. filler and regulating the flow of the additive 1 to 10 wt. carrier, 0.1 to 10 wt. supplements providing protivoukachiwauschee action, and 0.1 to 80 wt. the binder and the way his receipts.

The invention relates to solid dosage forms for oral administration containing as active substance ifosfamide: 3-(2-chloroethyl)-2-(chloroethylamino)-tetrahydro-2H-1,3,2-oxazaphosphorin-2-oxide. Ifosfamide is a drug type oksazafosforina with cytostatic activity.

Ifosfamide is a white crystalline powder highly hygroscopic substance with a melting point 48-51aboutC. At temperatures below the melting temperature ifosfamide begins to specalise, so it should be stored at lower temperatures. It is in the water. However, aqueous solutions can be stored for a limited time.

Still the use of ifosfamide was allowed only in the form of preparations for parenteral administration. Ifosfamide is available in the form of sterile kristalliset in ampoules for injection in packaging 200-2000 mg Before using this sterile crystallised must be dissolved in water intended for injection. The concentration of such solution should not exceed 4% of the Prepared solution can be used for intravenous injection. For short-term intravenous infusion of a solution of ifosfamide dissolved in 500 ml of ringer's solution or other similar liquids for injection. The duration of infusion is usually around 30 minutes But it can last 1-2 hours In a 24-hour infusion of a solution of ifosfamide is dissolved, for example, in 3 l of 5% dextrose and salt.

Upon receipt and processing of ifosfamide, there are several problems.

When receiving sterile crystalline ifosfamide formed product physical characteristics which may be different. Different flowability of the obtained product, in particular, dramatically affects the accuracy and low melting point. During long-term storage sterile crystallized is sintered, the resulting decrease the rate of dissolution. With the beginning of sintering decreases pH and transparency of the resulting solution and at the same time he painted in yellow color. Usually this drug is already unsuitable for therapeutic applications.

Main disadvantages associated with its use. Parenteral administration can be carried out only by qualified medical personnel. For this purpose the patient should be placed in a hospital or daily to report for treatment. This is due to time-consuming for both staff and patients.

Obtain a sterile solution for injection of dry matter because of the hazard makes it necessary to take costly measures to protect personnel. For patients parenteral administration of the drug is an unpleasant procedure, as it requires to make a painful injection and infusion to connect their equipment.

The result of all these shortcomings is the resulting need for preparations for oral administration, does not have these disadvantages. In oral introduction probably am the rata for oral administration failed due to physico-chemical properties of ifosfamide. Medicines in the form of soft gelatin capsules could not be obtained. Apparently, the active ingredient reacts with the shell of the capsule becomes hard, and the result is already capsule does not dissolve in the gastric juice. Similarly, numerous unsuccessful attempts to obtain tablets. Substance stuck to the stamps tabledelete machine, the resulting tablets were too soft, liquefied active substance when the compression was partially released from the matrix.

The ifosfamide in a mixture with microcrystalline cellulose can be filled capsules of hard gelatin. In this case there is no undesirable interaction of ifosfamide with shell capsules. Although the shell of the capsule contains 12-15 wt. water and ifosfamide is hygroscopic and moisture sensitive material containing capsule of hard gelatin can be stored for many years and even after such long storage capsule shell dissolves in the gastric juice for a few minutes.

Ifosfamide capsules in accordance with the invention contain, for example 100-800, preferably 200-500 mg ifosfamide.

The contents of the capsule consists mainly of ifosfamide and mikicic regulating the fluidity and preventing the bonding additives. These control the fluidity and articleimage additives can be used both in relativity and in mixture. The total content of these additives per 1 wt. hours of ifosfamide is, for example, about 0.001 to 0.1, preferably 0.01 to 0.04 wt. 'clock as such regulating the fluidity and providing protivoukachiwauschee effect of additives can be used known additives.

In particular, as these components can be used stearate and other stearates, highly dispersed silicon dioxide, stearic acid, talc and polyglycols (e.g., with a molecular weight of 4000-6000).

The preferred content of regulating the flow of the additive is 0,002-0,02, most preferably 0.005 to 0,008 and additives that provide protivoukachiwauschee act of 0.004 to 0.08, and most preferably 0,016-to 0.032 wt. including 1 wt. hours of ifosfamide.

In addition, the contents of the capsule may include a filler, such as starch, cellulose, lactose, fructose, sucrose, mannitol, sorbitol, calcium phosphate; binder, such as gelatin, cellulose, pectin, alginate, polyvinylpyrrolidone; media, such as alginate, carboxymethylcellulose, polyvinylpyrrolidone, ultramylonite.

As is, is Aerosil), and magnesium stearate.

The content of microcrystalline cellulose capsules is usually 0.2 to 4, preferably 0.25 to 1, most preferably from 0.3 to 0.35 wt. including 1 wt. hours of ifosfamide. Used microcrystalline cellulose should have a degree of crystallinity, characterized by a crystallinity index (under the crystallinity index refers to the ratio of the crystalline fraction to the total content of the crystalline and amorphous fractions. For crystalline cellulose with a particle size of about 50 μm, the value of this index is, for example, 0,71.) 0.5 and 0.9, for example, of 0.7. The degree of polymerization of microcrystalline cellulose should be in the range of 200-300. In addition, used microcrystalline cellulose must have an average grain size, for example about 50, preferably less than 50 μm. It is desirable that he was less than 40, in particular of the order of 20 microns. Preferably as microcrystalline cellulose to utilize cellulose, avicelfor example, avicelwith the distribution of particle size less than 38 microns (avicelPH 105) (this means that the average size of at least 90% of microcrystalline particles is etoc on the basis of ifosfamide as the active substance, moreover, the most appropriate was a combination of tricalcium phosphate and polyethylene glycol. Thanks to this method the first time it was possible to get such tablets by pressing on a conventional tablet press.

Physico-chemical properties of ifosfamide not allow you to receive from him the tablet by pressing on normal tablemodellistener machines. All attempts of pressing of this active substance, using known auxiliary additives, such as, for example, microcrystalline cellulose, lactose, starch, talc, highly dispersed silicon dioxide, calcium phosphate, failed. And with granulation carried out in the usual way or in the fluidized bed, also failed to get the mass from which it would be easy to extrude tablets. In all cases, in the process of pressing was the adherence of the mass to the stamp or to the matrix.

Tablets in accordance with the present invention per 1 wt. hours of ifosfamide contains: 0.1 to 1.0 wt. including tricalcium phosphate and 0.04 to 0.4 wt. hours of polyethylene glycol (for example, with a molecular weight of 4000-6000) and in addition (calculated on the weight of the tablet), 5-60 wt. filler and additives regulating fluidity, 1-10 wt. N. the art of ifosfamide in accordance with the invention is used, for example, 0.1 to 10 wt. hours, preferably 0.2 to 0.5, most preferably from 0.25 to 0.30 wt. including tricalcium phosphate. Based on the weight of the tablet, the amount of tricalcium phosphate is, for example, 35, preferably 7-17,8, most preferably 9-1 wt.

The content of polyethylene glycol is, for example, from 0.04 to 0.4, preferably 0.1 to 0.2, most preferably of 0.13 to 0.15 wt. including 1 wt. hours of ifosfamide. It is preferable to use a polyethylene glycol with a molecular weight of 4000-6000, most preferably with a molecular weight of 6000. Based on the weight of the tablet content of polyethylene glycol is, for example, 1-14,0, preferably of 3.5 and 7.5, most preferably 4.5 to 7, in particular 4.5 to 6 wt. The weight ratio of tricalcium phosphate and polyethylene glycol is, for example, 1:0.5 in.

In addition to these ingredients tablets contain: filler and regulating the flow additive in the amount of 5-60 wt. based on the weight of the tablet. As filler can be used, for example, starches, cellulose, lactose, sucrose, fructose, sorbitol, mannitol, calcium phosphate, calcium carbonate, calcium sulfate, carbonate or magnesium oxide. These compounds are used in an amount of 5-60 wt. based on the weight of the tablets.

ctsu, polyglycols, starches, cellulose, talc, siliconized talc, Arahant or calcium stearate, cetyl alcohol, stearyl alcohol, ministerului alcohol, stearic acid, lauric acid. In that case, if the regulatory fluidity additive does not play simultaneously the role of filler, it is used in amount of 0.5-10 wt. based on the weight of the tablets.

Media: for example alginates, starches (e.g. corn starch), pectin, carboxymethylcellulose, polyvinylpyrrolidone, ultramylonite, bentonite. Its content is 1-10 wt. based on the weight of the tablets.

Supplement providing protivoukachiwauschee action, such as glycols, talc, siliconized talc, staringat talc, calcium stearate, aluminum stearate, stearic acid. Its content is 0.1-10 wt. based on the weight of the tablets.

Binder, such as gelatin, a cellulose ether, amylose, pectin, cellulose, dextrose, polyglycol, tragant. Its content is 0.1-80 wt. based on the weight of the tablets.

Preferably tablets, addition of ifosfamide, tricalcium phosphate and polyethylene glycol, contain the following materials: microcrystalline cellulose in an amount of 0.1 to 1.2, preferably of 0.4 to 1.0, naibolee on the weight of the tablet; lactose in the amount of 0.15 to 1.0, preferably of 0.24 and 0.68, most preferably between 0.30 and 0.40 wt. hours per weight part of ifosfamide or 5.0-36, preferably of 8.5-25 wt. based on the weight of the tablet; corn starch in the amount of 0.02-0.24 wt. hours, preferably from 0.05 to 0.20, most preferably 0.1 to 0.15 wt. hours per wt. hours of ifosfamide or 0.7 to 8.5, preferably from 2.0 to 6.5 wt. based on the weight of the tablet; talc in amounts of 0.02-0,30, preferably 0,06-0,20, most preferably 0.07 to 0.09 wt. hours per wt. hours of ifosfamide or 0.70 to 10, preferably 2 to 6,5 wt. based on the weight of the tablet; magnesium stearate in an amount of 0.004 to 0.2, preferably 0.02 to 0.12 and most preferably a 0.035 to 0.05 wt. hours per wt. hours of ifosfamide or 0.1 to 7.2, preferably 0.7 to 4.5 wt. based on the weight of the tablets.

And on tablets, and capsules can be applied in a known manner the floor. It can be water-soluble, swellable, water-soluble or resistant to gastric juice coating of an aqueous dispersion or aqueous solution or dispersion in an organic solvent, such as, for example, ethanol, isopropanol, acetone, ether, dichloromethane, methanol.

Capsules and tablets are temperature, eg is GNA to exceed 40%

The examples illustrate how a specific implementation of the invention.

To obtain the offer in accordance with the invention, the solid dosage forms on the basis of ifosfamide for oral administration of 1 wt. hours of ifosfamide mixed with 15-30aboutWith from 0.1 to 4, preferably 0.2 to 4, most preferably 0.25 to 1 wt. including microcrystalline cellulose and, optionally, small quantities of regulating the fluidity and providing protivoukachiwauschee effect of additives to education gomogennoi mixture and this mixture is filled capsules or mix 1 wt. hours of ifosfamide with 0.1 to 1.0 wt. including tricalcium phosphate, 0.04 to 0.4 wt. hours of polyethylene glycol and 0.15 to 2, preferably 0.5 to 1.5, most preferably 1-1,3 wt. including filler and regulating the flow of the additive, of 0.03 to 0.5, preferably from 0.05 to 0.4 most preferably 0.08 to 0.2 wt. H. carrier, of 0.003 to 0.5, preferably from 0.01 to 0.4 most preferably 0.05 to 0.2 wt. including supplements, providing protivoukachiwauschee action, and 0.003 to 3, preferably from 0.01 to 2, most preferably 0.1 to 1 wt. including a binder prior to the formation of a homogeneous mixture. Then pressed from this mixture tablets and optionally applied on the obtained capsules or tablets regular floor.

P R I m e R 1. Containing ifosfamide weight is the following.

To obtain 12000 capsules containing the active ingredient 250 mg sift, for example, 3.0 kg of ifosfamide, 1,002 kg microcrystalline cellulose and 0,018 kg of highly disperse silicon dioxide through a sieve with a mesh size of 0.8 mm and stirred the mixture for 4 minutes in the mixer. Then to the mixture is added 0.06 kg of magnesium stearate (screened through a sieve with mesh size 0.8 mm) and stirred the mixture for another minute. The mixture is Packed in a machine for making capsules with the aspect nozzles No. 1 hard gelatin capsules of size N 1 so that each capsule contained approximately 340 mg mass.

To get 20,000 capsules containing the active ingredient 500 mg sift through a sieve with a mesh size of 0.8 mm, for example, 10,0 kg ifosfamide, 3,34 kg microcrystalline cellulose and 0.06 kg of highly disperse silicon dioxide and stirred the mixture for 4 minutes in the mixer. Then to this mixture, add 0.2 kg of magnesium stearate (screened through a sieve with mesh size 0.8 mm) and stirred the mixture for one minute. Ready weight Packed on a machine for the manufacture of capsules with the aspect nozzles N 00 hard gelatin capsules size 00 so that ka is avicel PH 105, having a certain range of the distribution of particle size and representing a filler having good fluidity, which can successfully play the role of a binder.

To obtain capsules resistant to gastric juice, for example at 2500 capsules of size 1 with a content of active substance (ifosfamide) 250 mg are coated with 3000 g of a suspension in an organic solvent (isopropanol). 3000 g of a suspension containing 1440 g of anionic polymerizate methacrylic acid and its esters with an average molecular weight of, for example, 150000, with the addition of the usual plasticizers, 18 g of 1,2-propane diol, 36 g of magnesium stearate and 1506 isopropanol.

As copolymerizate methacrylic acid and methyl methacrylate can be used, for example, Eudragit Lin particular in the form of a 12.5% solution in isopropanol (12,5% Eudragit). Such copolymerizate soluble in the environment of neutral to slightly alkaline due to the formation of salts of alkali metals.

P R I m m e R 2. Getting ifosfamide tablets.

Tablets containing the active substance 250 mg can have, for example, the following composition:

One tablet weighing 700 mg contains mg: Ifosfamide 250 Melodiers LK 20 Stearate 10

To prepare the masses to get 1500 tablets 375 g of ifosfamide, 105 g of fine tricalcium phosphate, 300 g of microcrystalline cellulose, of 127.5 g of lactose, 52,5 g polyglycol 6000, 45 g of corn starch 80 g of talc pass through a sieve with a mesh size of 0.8 mm and stirred the mixture for 15 minutes in a suitable mixer. Then to the mixture is added 15 g of sifted in the same way of stearate and mix for another 2 minutes Of the cooked mass is pressed tablets on a suitable tablet press.

To obtain tablets, gastro-resistant juice, 1050 g of the tablets are coated with, for example, 500 g of the aqueous dispersion of the following composition.

100 g of aqueous dispersions contain, g: Polyglycol 6000 1,600 titanium Dioxide 1,100 Yellow iron oxide 0,156 Talc 4,000 Dimethylpolysiloxane 0,100 Eudragit L 30D 55,000 Water 38,044

_______< / BR>
100,000

Eudragit Lis an aqueous dispersion of copolymerizate anionic character based on methacrylic acid and ethyl acrylate. The ratio of free carboxyl groups and ester groups is approximately 1:1, and the average molecular weight of about 250,000.

Spraying plenkoobrazuyushchie the solvent and the dispersant is continuously removed by drying.

SOLID DOSAGE FORM of IFOSFAMIDE, characterized in that the powder comprises, by weight. including the active ingredient and microcrystalline cellulose 1 - 0,2 4 for filling hard gelatin capsules and tablets contain, by weight. h

Ifosfamide 1,0

Tricalcium phosphate 0,1 1,0

The glycol 0,04 0,4

and auxiliary substances in the calculation of the mass of tablets, wt.

Moving 5 60

Loosening 1 10

Lubricating 0.1 to 10

The binder is 0.1 to 80

 

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