JP2003183155A - Pharmaceutical composition for washing intestinal tract - Google Patents

Abstract

<P>PROBLEM TO BE SOLVED: To provide a novel pharmaceutical preparation which furnishes convenience to a composition for washing the intestinal tracts which contains magnesium citrate and is orally administered after being dissolved into a predetermined amount of water. <P>SOLUTION: The pharmaceutical preparation has a composition for preparing a washing liquid agent for washing the intestinal tracts, when the composition is dissolved in a suitable amount of water to make 180 ml of its solution, and the solution contains from 6.4 to 7.2 g of magnesium citrate, and also contains suitable amounts of sodium chloride, potassium hydroxide and saccharides so as to adjust the osmotic pressure of the solution from 290 to 310 mOsm/L, and the preparation is characterized by press tableting each a quantity of the composition which contains an equivalently divided amount of the composition into a tablet form. <P>COPYRIGHT: (C)2003,JPO

Description

Detailed Description of the Invention

[0001]

TECHNICAL FIELD The present invention relates to a composition preparation for intestinal lavage used to completely excrete and cleanse contents of the large intestine before enema X-ray examination or colonoscopy.

[0002]

2. Description of the Related Art In recent years, the number of patients with large intestine containing a malignant tumor has been increasing due to westernization of diet, aging, and the like. Intestinal lavage is an indispensable pretreatment for diagnosis of colorectal diseases by enema X-ray examination and colonoscopy.

The prevailing pretreatment for intestinal lavage currently in use is taking an oral intestinal lavage solution (hereinafter referred to as "PEG solution") containing polyethylene glycol and an electrolyte as main components. PE
Although the cleaning effect of the G solution is high, taking a large amount (about 2 L or more) of the cleaning solution within a limited time is not only painful for the patient, but also has a difficulty in taste. Some patients may also have nausea.

For this reason, recently, instead of the PEG solution, a solution prepared by dissolving an intestinal tract cleaning composition containing an electrolyte and a saccharide in magnesium citrate in water so as to be isotonic with the body fluid has been used. It has been confirmed that the cleaning effect is equivalent to or higher than that of the liquid. PE in terms of taste
It is much easier to drink than G liquid.

Applicant's Patent No. 3047143 contains magnesium citrate, sodium chloride, potassium hydroxide and sugars and when dissolved in water 290-310.
An intestinal tract cleaning composition and a cleaning solution that provide an osmolarity of mOsm / L are proposed.

This composition is a powder and must be dissolved in an appropriate amount of water to prepare an isotonic solution before use. Therefore, for example, 1.
In order to prepare 8 L of isotonic washing liquid, it is necessary to prepare a large container having a volume of 2 L or more, put a predetermined amount of powder and water therein, and stir well. Otherwise the powder will clump and not evenly disperse in the water. For this reason, considerable effort is required such as shaking the container up and down, which is difficult for women and elderly people to carry out.

In order to avoid such difficulty, for example, 18
It is possible to prepare a cleaning liquid with a small amount of powder by preparing a 0 mL capacity cup and repeat this. However, such an operation causes a change in the composition of the cleaning liquid each time, and also increases the chance of accidentally scattering the powder out of the container.

Therefore, it is desired to develop a new dosage form of a magnesium citrate-containing intestinal lavage composition, which enables simple and accurate preparation of an isotonic intestinal lavage solution using a small volume container such as a cup. .

[0009]

The present invention solves the above problems by providing the intestinal cleansing composition in powder form in the form of a compressed tablet.

According to the present invention, it is dissolved in an appropriate amount of water to give 18
When the solution was made into 0 mL, it contained 6.4 to 7.2 g of magnesium citrate, and the osmolarity of the solution was 290.
A composition for preparing an intestinal lavage solution containing sodium chloride, potassium hydroxide and a saccharide in an amount of about 310 mOsm / L, wherein an equal aliquot of this powdery composition is in the form of tablets. There is provided a composition preparation for intestinal lavage, which is characterized by being compressed and compressed.

The tablet of the present invention is intended to form an intestinal tract cleaning liquid that is isotonic with body fluid when the determined number is dissolved in an appropriate amount of water to make a 180 mL solution. This brings many conveniences to the preparation of the cleaning solution at the time of use. Further, if desired, the hypertonic washing solution can be prepared using the same number of tablets, or the tablets can be taken as they are with water to achieve the washing effect.

[0012]

[Preferred embodiment] The citric acid Maguneshiune used in the present invention means a citrate monosodium magnesium hydrogen pentahydrate _{(MgHC 6 H 5 O 7 ·} 5H 2 O). Since the administration of an isotonic solution of magnesium citrate may disturb the electrolyte balance in the body, sodium chloride, potassium hydroxide and saccharides are further added in the above-cited applicant's patent to make an isotonic solution.

In the present invention, since 180 mL is intended as a unit of the washing liquid, 290 to 31
180 mL of the solution having an osmolarity of 0 mOsm / L contained 6.4 to 7.2 g of magnesium citrate, 0.9 to 1.1 mmol of sodium chloride, and 1.7 to 1.
It must contain 9 mmol, 2.2-0.4 g of sugar. The sugars used here are sugars having sweetness such as sucrose, maltose, glucose, fructose and invert. White sugar is preferred.

The powder composition containing the above components in the above proportions is prepared by, for example, dispersing magnesium carbonate in water, adding citric acid thereto and dissolving it, and adding a predetermined amount of an aqueous solution of sodium chloride and potassium hydroxide to the solution. Then, for example, the solution can be obtained by spray-drying the solution to give a powder, and finally adding and mixing the sugar to the obtained powder.

In the present invention, an amount of this powder corresponding to 6.4 to 7.2 g of magnesium citrate is tabletted into a predetermined number of tablets. Since tableting requires auxiliary components such as excipients, binders, disintegrants, lubricants, etc., magnesium citrate 6.4 as a whole component including these auxiliary components.
The powder composition content per tablet is determined so that an amount equivalent to ˜7.2 g is contained in the entire tablet of the determined number.
For example, when 5 tablets are to be used for preparing 180 mL of washing solution, tablets each containing 1.28 g to 1.44 g of the powder composition as magnesium citrate may be tabletted.

As mentioned above, tableting requires various auxiliary ingredients for tableting. Crystalline cellulose among these,
Disintegrants such as sodium carboxymethyl starch are needed to increase the water solubility of the tablets. If the mixture is to be granulated and then tabletted, a binder such as carmellose sodium, low substituted hydroxypropylcellulose is also required. Lubricating agents such as magnesium stearate are also required. Excipients such as lactose are usually not needed. If necessary, water-insoluble excipients that do not substantially affect osmotic pressure, such as starch, should be used or should be limited to amounts that do not substantially affect osmotic pressure. Since tablet manufacturing methods are well known in the pharmaceutical industry, no further detailed explanation is necessary.

The size (weight) of each tablet is 18
Depends on the number of tablets to make 0 mL. For example, a tablet containing 6.4 to 7.2 g of magnesium citrate in one tablet is too large and requires a long time to dissolve. Therefore, for example, the dissolution time can be shortened by dividing this into 5 equal parts and preparing 180 mL of the washing liquid with 5 tablets.
However, the number of divided doses of magnesium citrate can be appropriately determined depending on the solubility of the tablet, whether it is intended to be taken directly, and the like.

The compressed tablets can be packaged in the required amount of water and packaged in the required number to prepare 180 mL of isotonic solution. In use, for example, 180 mL of a washing solution is prepared and taken in a cup according to the instruction, and this is repeated as many times as a complete intestinal washing.

[0019]

The invention will now be illustrated by the following non-limiting examples.

Example 1 Magnesium carbonate (JP) 86.5 in 480 L of purified water
After dispersing kg, citric acid (JPC product) 184.0 kg
Is gradually added and heated until a nearly transparent liquid is obtained. After cooling, add purified water to make 640 L. Citric acid 2 in this solution
Add 1.0 kg to dissolve and further potassium hydroxide 4.
A solution prepared by previously dissolving 0 kg and 2.4 kg of sodium chloride in water is added and mixed with stirring. The mixed solution is dried and pulverized to obtain 290 kg of dry powder.

Example 2 1000 g of the powder obtained in Example 1, 350 g of sucrose and 98 g of crystalline cellulose are uniformly mixed, 2 g of magnesium stearate is mixed with this mixture, and each tablet is tableted to 2.9 g.

Five tablets were dissolved in water to make a total amount of 180
The total volume of 180 mL contains about 6.8 g of magnesium citrate in 180 mL, and the osmolarity is about 300 mOs.
A m / L washing solution is obtained. This solution is prepared 10 times and taken.

   ─────────────────────────────────────────────────── ─── Continued front page    F term (reference) 4C076 AA29 AA36 BB01 CC16 DD23                       DD30 DD41 DD43 DD67 EE31                       FF14                 4C086 AA01 AA02 HA04 HA16 HA20                       MA03 MA05 MA35 MA52 NA06                       NA09 ZA72

Claims (2)

[Claims] 1. When dissolved in an appropriate amount of water to form a 180 mL solution, the solution contains 6.4 to 7.2 g of magnesium citrate, and the osmolarity of the solution is 290 to 310 mO.
A composition for preparing an intestinal tract cleaning solution containing an amount of sm / L of sodium chloride, potassium hydroxide and a saccharide, wherein an equal amount of this powdery composition is compressed into tablets. A composition preparation for intestinal tract washing, which is characterized by being tableted. 2. The powdery composition has a sodium chloride content of 0.04 g per 6.4 to 7.2 g of magnesium citrate.
The formulation of claim 1 which contains 9 to 1.1 mmol, 1.7 to 1.9 mmol of potassium hydroxide, and 2.2 to 0.4 g of sugar.