JPH107561A - Easily swallowable jelly-like preparation containing donperidone - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain the subject new preparation containing donperidone and a gelling agent, easily swallowable even by a patients having a dysphagia, etc., for administering a dose capable of obtaining a sufficient medicinal effect. SOLUTION: This easily swallowable jelly-like preparation containing donperidone contains (A) donperidone and (B) a gelling agent. Further, the preparation contains 0.05-5wt.% component (A) and 0.1-25wt.% polysaccharide or peptide as the component (B), and it is preferable to use e.g. 5- chloro-1- 1-[3-(2-oxo-1-benzimidazolinyl)-propyl]-4-piperizyl}-2-benzimidazolinone of the formula as the component (A) and sodium alginate, etc., as the component (B).

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

TECHNICAL FIELD The present invention relates to an oral pharmaceutical preparation of domperidone, and more particularly, to a swallowable jelly-like preparation having a novel oral administration form and containing domperidone as an active ingredient.

[0002]

BACKGROUND OF THE INVENTION Domperidone (5-chloro-1- {1- [3- (2-oxo-1-benzimidazolinyl) -propyl] -4-piperidyl} -2-benzimidazo represented by the following formula: Linone) is conventionally used in the form of tablets, fine granules, suppositories and dry syrup as a gastrointestinal motility improving agent having an antiemetic effect.

[0003]

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However, dysfunction of food intake due to deterioration of various functions and senile dementia due to aging (dysphagia etc.)
Therefore, when a drug is administered in the form of tablets, fine granules, or the like, it may remain in the oral cavity and cannot be swallowed, and a sufficient drug effect may not be obtained.

In the case of administration as a syrup, it is much easier to swallow than tablets and fine granules, but the taste is too sweet to make it easy to take, and after taking it, Dehydration of the oral cavity may require water instead.

[0006] In particular, many patients who are bedridden after surgery require the drug, and it is difficult to take tablets, fine granules, syrups and the like in such bedridden state.

[0007] Furthermore, at present, considerable care is required for taking care of a caregiver who cares for a bedridden patient, which is cited as a problem.

[0008]

DISCLOSURE OF THE INVENTION The present inventors have found that when oral administration of domperidone to patients with dysphagia, bedridden patients after surgery, etc., the above-mentioned problems have been raised, It can be swallowed easily, can take a certain amount of medicine enough to obtain a sufficient drug effect, and take water to reduce the dehydration effect in the oral cavity as seen when taking syrups It is an object of the present invention to provide a swallowable domperidone-containing jelly-form preparation improved so as to reduce the labor of a caregiver when taking a drug in a patient requiring further care.

[0009]

Means for Solving the Problems In order to solve these problems, the present inventors have studied various efficacious domperidone-containing preparations which are more effective as oral dosage forms. Was. As a result, these problems could be solved by preparing a gel-like preparation using a gelling agent.

That is, by adding a gelling agent and making the dosage form jelly-like, a swallowable domperidone-containing jelly-like preparation could be prepared.

In the present invention, domperidone is 0.05
The gelling agent preferably contains 0.1 to 25% by weight.

As the gelling agent used in the preparation of the present invention, polysaccharides or peptides can be used. In particular, alginic acid or a salt thereof (eg, sodium salt), carrageenan, curdlan, gelatin, agar, starch, etc. Can be used. One or more of these can be used in combination. Among them, sodium alginate, carrageenan and curdlan are preferred.

The jelly preparation of the present invention may further contain appropriate amounts of sweet components and flavoring agents in addition to the above-mentioned components. As the flavoring agent, those usually used for foods can be used.

Further, the stability of the preparation can be improved by adding an antibacterial agent. As antibacterial agents,
Sodium benzoate, potassium sorbate, methyl p-hydroxybenzoate and propyl p-hydroxybenzoate can be used.

The jelly-form preparation of the present invention can be made into a heat-resistant domperidone-containing jelly-form preparation by using curdlan as a gelling agent. Since this preparation is heat-resistant, it is heated at 115 ° C., 30 ° C. in an autoclave.
Minutes of sterilization can be performed.

By preparing an easy-to-swallow domperidone-containing jelly-form preparation using these gelling agents, patients having dysphagia, bedridden patients after surgery, etc. are extremely easy to take and have a sufficient drug effect. It is possible to reliably take only a certain amount as much as possible, and to considerably reduce the care of the caregiver when taking the medicine in patients requiring care.

[0017]

DESCRIPTION OF THE PREFERRED EMBODIMENTS Hereinafter, the present invention will be described in detail with reference to embodiments. The jelly-like preparation containing domperidone, which is easy to swallow, of the present invention is not limited to the formulation examples described in Examples.

[0018]

EXAMPLES A swallowable jelly-like preparation (Formulation Example 1 ') prepared so that physical properties are equivalent to those obtained by adding domperidone as a preparation except that domperidone is excluded from Preparation Examples 1 and 2 shown below. 2 ′) was taken by 5 subjects (subjects A to E) who complained of swallowing difficulty, and the difficulty of taking was determined. The results are shown in Table 1 below. In addition, about 5 caregivers (subjects F to J) engaged in nursing care for the elderly, those in bedridden state were given an easy-to-swallow jelly-like preparation (Formulation Examples 1 ′ and 2 ′).
Was taken, and the difficulty was determined. The results are shown in Table 2 below.

(Formulation Example 1) (1) Formulation Component Blending amount (% by weight) Group A Domperidone 5.0 Sodium alginate 2.5 Purified water qs Group B Carrageenan 0.89 Sucrose 10.0 qs Purified water

(2) Preparation Method A swallowable domperidone-containing jelly-like preparation was prepared using the above components and amounts. That is, Group A was prepared by dissolving sodium alginate as a gelling agent in an appropriate amount of purified water, further adding domperidone, stirring and dispersing. Separately, add carrageenan to an appropriate amount of purified water and add
The mixture was dissolved by heating to 0 ° C., and sucrose and other additives were added thereto, followed by stirring and dissolving to prepare Group B. The mixture of Group A and Group B was mixed at a ratio of 1: 9 and cooled to obtain a preparation of the present invention.

Formulation Example 2 (1) Formulation Component Blended amount (% by weight) Domperidone 0.5 Curdlan 1.0 Sucrose 10.0 Appropriate amount of purified water

(2) Preparation Method A swallowable domperidone-containing jelly-form preparation was prepared using the above components and amounts. That is, 10 sucrose is added to purified water.
%, Add curdlan, and add about 5000 rp
Heat while stirring at m / min to prepare a gel. Domperidone is added thereto and further stirred to prepare a uniform dispersion. If necessary, degas under reduced pressure, fill a container, gel in a boiling water bath, and autoclave for 115 minutes.
It sterilized at 30 degreeC and 30 minutes, and obtained the formulation of this invention.

[0023]

[Stability test] In order to examine the stability of the jelly-form preparation of the present invention, Formulation Examples 1 and 2 were prepared and filled in a sealed container.
Stored at 0 ° C. for 3 months. As a result, it was confirmed that there was no change in the appearance of the jelly-like appearance, and there was almost no change in the content of domperidone.

[0024]

[Table 1]

[0025]

[Table 2]

[0026]

As described above, in the case of oral administration of domperidone to a patient having dysphagia, a bedridden patient after surgery, etc., the oral preparation of domperidone is converted into a jelly-like preparation using a gelling agent. In order to be able to swallow easily, to be able to take a certain amount of medicine enough to obtain a sufficient drug effect, and to reduce the dehydration effect in the oral cavity as seen when taking syrups Improvements have been made to reduce the caregiver's hassle in taking the drug in patients who do not need to take water and who need further care.

──────────────────────────────────────────────────続 き Continuation of the front page (51) Int.Cl. ⁶ Identification code Agency reference number FI Technical display location // (C07D 401/14 211: 58 235: 26) (72) Inventor Hiroshi Yamaga Musashi, Tokyo 2-11-9 Honcho, Murayama-shi Limited company NAC Corporation

Claims (3)

[Claims] 1. A swallowable domperidone-containing jelly-like preparation comprising domperidone and a gelling agent. 2. The swallowable domperidone-containing jelly-form preparation according to claim 1, which contains 0.05 to 5% by weight of domperidone. 3. The swallowable domperidone-containing jelly-form preparation according to claim 1, which comprises 0.1 to 25% by weight of a polysaccharide or a peptide as a gelling agent.