Radiopharmaceutical composition for the diagnosis of diseases of the gastrointestinal tract

 

(57) Abstract:

The invention relates to the field of medicine and relates to a radiopharmaceutical composition for the diagnosis of diseases of the gastrointestinal tract. The invention lies in the fact that the radiopharmaceutical (RN) contains an aqueous solution of urea labeled with a radionuclide carbon - 14, anhydrous sodium pyro phosphate, enclosed in hard gelatin capsule is used as a diagnostic tool ulcerative diseases of the gastrointestinal tract. The invention provides a more accurate distribution of active urea solution and inert carrier and quick shipping capsules with the drug layer of the gastric mucosa. 3 C.p. f-crystals.

The invention relates to medicine, namely to radiopharmaceutical drugs, and can be used as a diagnostic tool for diseases of the gastrointestinal tract for the analysis of exhaled air. The drug is designed for oral administration.

The essence of this diagnostic test breathing is the following. A capsule containing urea labeled with a radionuclide carbon-14, eaten by the patient. In the stomach of the patient in the presence of ulcers is B>2and ammonia, NH3that are absorbed into the blood and appear in the exhaled air of the patient.

After 10 min after swallowing the capsules, a portion of the exhaled air is collected in a tank, is passed through a special liquid for absorption of labeled CO2. The solution with the absorbed CO2investigated in liquid scintillation counter.

The quantitative test to determine the presence of Hp in the stomach of a patient in various diseases of the stomach and duodenum. Excess levels 14With over a control value indicates the presence of a pathological process.

Urea labeled with a radionuclide14With that not disintegrate under the action of (Hp), gets into the urine with a half-life of 12 hours, About 10% of the radionuclide14With remains in the body and gradually decreases with the biological half-life of about 40 hours

Radionuclide14With is a beta emitter with a half-life of T1/2= 5730 years with the energy of the beta particles Emax- 157 Kev, Ecf=49 Kev.

As the prototype used a radiopharmaceutical composition (RN) containing urea labeled with a radionuclide carbon - in [1].

[1] Application WO 98/53808. Publication date 03.12.1998, (priority 28.05.97).

The radiopharmaceutical composition described in [1], is the following:

Carbon-14 is - 1 µci, 37 kBq

Sugar is 200 mg

The gelatin capsule is the Size of the room 3

The method of obtaining this radiopharmaceutical composition is as follows: powdered or granulated sugar is placed in one of the known rotating devices, such as rotary dryer, start the dryer and one of the known methods to the surface of inert carrier (sugar) is dispersed in alcohol solution of urea labeled with a radionuclide carbon-14 in a predetermined ratio: volume of the urea solution, the weight of sugar. As the drum rotates, the alcohol evaporates, and urea labeled with a radionuclide carbon-14, is dispersed on the surface of the inert carrier is a sugar. Then urea, dispersed on an inert carrier (sugar), one of the known methods is loaded into hard gelatin capsule No. 3, which contains 200 mg of sugar with an activity of 1 µci (37 kBq).

Defects in the structure of the prototype are:

1. Based on the activity of the urea solution (alcohol solution), most uneven distribution of the active urea solution on poverhnosti carbon-14 in each capsule of the nominal value (20%).

3. The complexity of the technology for this part of RFP requiring recovery and return to duty cycle the evaporated ethanol; the danger of entrainment of radioactive urea ethanol.

4. The use of capsules, number 3, not very convenient for swallowing her patient.

The objectives of the claimed invention are:

1. Simplification of technology for the composition of the RN, using inert media.

2. Reducing bias values activity of carbon-14 in each capsule of the nominal value.

3. More accurate distribution of active urea solution and an inert carrier.

4. The use of heavier inert carrier, providing quick delivery capsules with the drug layer of the gastric mucosa.

5. The use of smaller capsules number 4 for ease of swallowing her patient.

Objectives of the invention are achieved by the fact that as the inert carrier radiopharmaceuticals containing urea labeled with a radionuclide carbon-14 in a hard gelatin capsule, used anhydrous sodium pyro phosphate (196-204 mg), phosphorus in the form of anhydrous sodium pyro phosphate 42-52 mg used water rest what about the inert carrier, is 0,0334 to 0.2 µci/µl, inert carrier with a dispersed solution of urea is contained within a gelatin capsule, size 4, total activity of one capsule is 1 µci (37 kBq). Anhydrous inert Carrier is dispersed from 5 to 30 μl of an aqueous solution of urea labeled with a radionuclide carbon-14.

The method of obtaining the composition of RN containing labeled urea with radionuclide Plenum-14, is as follows.

In cell nests one of the devices, one known method loads the specified number of hard gelatin capsules of size 4. Capsules are oriented in this device covers up. One of the known methods with buildings capsules take off the lid closed on the transport "castle", opening access inside capsules, using one of the known devices, one of the known methods is loaded into the body of each capsule in the cell nests, the specified number of anhydrous sodium pyro phosphate. On the surface of anhydrous sodium pyro phosphate one of the known methods is dispersed aqueous urea solution of a given concentration, labeled with a radionuclide carbon-14. Sodium pyrophosphate anhydrous ispolzuem prevent the destruction of the gelatin capsules. One of the known methods is closed housing gelatin capsules caps and lock them in a "castle". Prepared RFP Packed in bottles for medicines or blister packing.

Limit values of concentrations of the components installed on the basis of experimental data obtained by analyzing a number of samples of the drug, is presented below.

Examples of the implementation of the proposed method

Example 1

In one known device, containing 10 nests under the capsule, one of the known methods load 10 empty gelatin capsules size 4 and removed from the body of the capsule lid closed on transport "castle". Electronic scales weigh 200 mg 2% inert carrier anhydrous sodium pyro phosphate and one of the known methods load it into each hard gelatin capsule. One of the known methods using an automatic pipette, dispense (dispersed) on the surface of inert carrier each capsule 5 µl of an aqueous solution of urea to carbon-14 concentration of 0.2 µci/µl. One of the known methods close corps capsules caps lock to "lock". Using a scintillation counter to determine the activity of the SC is Olney capsule of the nominal value does not exceed 15%. Capsules with radiopharmaceuticals sent for packaging in blisters.

The patient K., aged 80 years, took one capsule RN "Breakups,14With" activity 1 µci. Breath test on a scintillation counter showed 1428 location. /min, indicating the presence of the patient To the Islands of the gastro-intestinal tract. Peptic 12 SC ulcer confirmed by gastroscopy.

Example 2

In one of the known devices containing 20 nests under the capsule, one of the known methods load 20 empty gelatin capsules size 4 and removed from the body of the capsule lid closed on transport "castle". Electronic scales weigh 200 mg 2% inert carrier anhydrous sodium pyro phosphate and one of the known methods load it into each hard gelatin capsule. One of the known methods using an automatic pipette, dispense (dispersed) on the surface of inert carrier each capsule 10 μl of an aqueous solution of urea to carbon-14 concentration of 0.1 µci/µl. One of the known methods close corps capsules caps lock to "lock". Using a scintillation counter to determine the activity of the capsules, which should be not less than 1 µci (37 kBq).

The patient-Ko, aged 47 years, took 1 capsule RN "Breakups,14With" activity 1 µci. Breath test on a scintillation counter showed 1882 location. /min, indicating the presence of the patient To to diseases of the gastrointestinal tract. Stomach cancer is confirmed by gastroscopy and histologically.

Example 3

In one known device, containing 50 nests under the capsule, one of the known methods download 50 empty gelatin capsules size 4 and removed from the body of the capsule lid closed on transport "castle". Electronic scales weigh 200 mg 2% inert carrier anhydrous sodium pyro phosphate and one of the known methods load it into each hard gelatin capsule. One of the known methods using an automatic pipette, dispense (dispersed) on the surface of inert carrier each capsule 20 µl of aqueous solution of urea to carbon-14 concentration of 0.05 µci/µl. One of the known methods close corps capsules caps lock to "lock". Using a scintillation counter to determine the activity of the capsules, which should be not less than 1 µci (37 kBq).

The deviation of the activity of carbon-14 in Konig funds. Patient M., aged 65 years, took 1 capsule RN "Breakups, 14With" activity 1 µci. Breath test on a scintillation counter showed 714 location./min, indicating the presence of the patient M. gastro-intestinal tract. Peptic 12 SC ulcer confirmed by gastroscopy.

Example 4

In one of the known devices containing 100 nests under the capsule, one of the known methods load 100 empty gelatin capsules size 4 and removed from the body of the capsule lid closed on transport "castle". Electronic scales weigh 200 mg 2% inert carrier anhydrous sodium pyro phosphate and one of the known methods load it in hard gelatin capsule. One of the known methods using an automatic pipette, dispense (dispersed) on the surface of the inert carrier of each capsule in 30 μl of an aqueous solution of urea to carbon-14 concentration 0,0333 µci/µl. One of the known methods close corps capsules caps lock to "lock". Using a scintillation counter to determine the activity of the capsules, which should be not less than 1 µci (37 kBq). The deviation of the activity of carbon-14 in the control capsule from nominiert With-Ko, at the age of 63, took 1 capsule RN "Breakups,14With" activity 1 µci. Breath test on a scintillation counter showed 67 pacn. /min, which suggests that he had no gastro-intestinal tract.

Example 5

In one known device, containing 25 nests under the capsule, one of the known methods load 25 empty gelatin capsules size 4 and removed from the body of the capsule lid closed on transport "castle". Electronic scales weigh 200 mg 2% inert carrier anhydrous sodium pyro phosphate and one of the known methods load it into each hard gelatin capsule. One of the known methods using an automatic pipette, dispense (dispersed) on the surface of inert carrier each capsule 50 ál of an aqueous solution of urea with carbon-14 at a concentration of 0.02 µci/µl. It was established experimentally that when dosing an aqueous solution of urea labeled with a radionuclide carbon-14 on a solid inert carrier (sodium pyro phosphate) at a ratio of 0.25 µl of 1 mg, aqueous urea solution does not have time to absorb with an inert carrier, is the deformation of the capsule.

When the dispersion of 50 m is psula softened, not locked on "castle", the capsule is deformed and shall be rejected.

Laboratory (preclinical) studies of the drug were conducted in the Cardiology research and production complex. It was tested 8 parties RN with urea labeled with a radionuclide carbon-14 capsules on an inert carrier (sodium pyrophosphate) "Breakups,14With".

Laboratory tests showed the safety and functionality RN "Breakups,14With".

The solubility of the capsule at 37oWith in distilled water for no more than 20 minutes

This method of obtaining RN on the proposed composition was tested in a laboratory setup, the accumulated sample RFP for laboratory and clinical trials developed by the laboratory regulations.

The composition of the radiopharmaceutical (RN), for the diagnosis of diseases of the gastrointestinal tract, including urea labeled with a radionuclide carbon - 14, a solid inert carrier, enclosed in hard gelatin capsule, characterized in that it contains an aqueous solution of urea labeled with a radionuclide carbon - 14, as a solid inert carrier used anhydrous sodium pyro phosphate, enclosed in hard gelatin ka the logo Piro.

2. Composition under item 1, characterized in that it contains an aqueous solution of urea labeled with a radionuclide carbon - 14, with a concentration 0,0333-0,20 µci/µl.

3. Composition under item 1, characterized in that the solid inert carrier of each capsule is dispersed from 5 to 30 μl of an aqueous solution of urea labeled with a radionuclide carbon - 14 set concentration.

4. Composition under item 1, characterized in that it includes urea labeled with a radionuclide carbon - 14, with activity 0,85-1,15 µci.

 

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