JPH07126188A - Granular solid preparation - Google Patents
Granular solid preparationInfo
- Publication number
- JPH07126188A JPH07126188A JP29247693A JP29247693A JPH07126188A JP H07126188 A JPH07126188 A JP H07126188A JP 29247693 A JP29247693 A JP 29247693A JP 29247693 A JP29247693 A JP 29247693A JP H07126188 A JPH07126188 A JP H07126188A
- Authority
- JP
- Japan
- Prior art keywords
- granular solid
- solid preparation
- silicic acid
- calcium lactate
- drug
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
Abstract
Description
【０００１】[0001]
【産業上の利用分野】本発明は、粒状固形製剤及び粒状
固形製剤の製造方法に関する。FIELD OF THE INVENTION The present invention relates to a granular solid preparation and a method for producing the granular solid preparation.
【０００２】[0002]
【従来の技術】不快な味を有する薬剤において、不快な
味をマスキングする方法は種々知られている。その中で
も調剤の容易さや服用性の良さから、顆粒剤あるいは細
粒剤などの粒状固形製剤にマスキングを施した製剤が増
えてきた。一般に、良く用いられるマスキング方法とし
ては、ワックスや水不溶性高分子物質などの口中で溶解
しにくい物質を粒状製剤にコーティングする方法があ
る。一方、特開昭６３−２４３０３５号には、ケイ酸カ
ルシウム等のケイ酸類に薬物を吸着させ苦味を軽減する
方法が開示されている。2. Description of the Related Art There are various known methods for masking an unpleasant taste in a drug having an unpleasant taste. Among them, formulations in which granular solid formulations such as granules or fine granules are masked have been increasing due to ease of preparation and easy administration. In general, a masking method that is often used is a method of coating a granular preparation with a substance that is difficult to dissolve in the mouth, such as wax or a water-insoluble polymer substance. On the other hand, Japanese Patent Laid-Open No. 63-243035 discloses a method of adsorbing a drug to silicic acid such as calcium silicate to reduce bitterness.
【０００３】[0003]
【本発明が解決しようとする問題点】しかし、従来の方
法によりマスキングを施した製剤は、服用した時に口中
でザラつき感があり、特に高齢者では、歯間に粒状物が
つまり不快感がある等の問題があった。また、有機溶媒
を使用することが多いため、その残留の危険性や、作業
者の健康を害するなどの可能性がある。However, the preparation masked by the conventional method has a gritty feeling in the mouth when it is taken, and especially in the elderly, there is a granular substance between the teeth, which causes discomfort. There were some problems. In addition, since an organic solvent is often used, there is a possibility that it may remain and the worker's health may be impaired.
【０００４】[0004]
【課題を解決するための手段】本発明者らは、上記問題
点を解決すべく鋭意検討した結果、以下に示す構成によ
り問題を解決できることを見いだし本発明を完成した。
即ち、本発明は、薬物、ケイ酸類及び乳酸カルシウムを
含有する粒状固形製剤である。また、本発明は、薬物と
ケイ酸類を混合し、次に乳酸カルシウムを添加する粒状
固形製剤の製造方法である。Means for Solving the Problems As a result of intensive studies to solve the above-mentioned problems, the present inventors have found that the problems can be solved by the following constitution, and completed the present invention.
That is, the present invention is a granular solid preparation containing a drug, silicic acid and calcium lactate. Further, the present invention is a method for producing a granular solid preparation, which comprises mixing a drug and silicic acid and then adding calcium lactate.
【０００５】本発明によると、苦味等の不快な味を有す
る薬物をマスキングし、服用しやすくなるが、この服用
性の改善が本発明の目的である。本発明にかかる薬物
は、不快な味、特に苦味や刺激を有する薬物であれば特
に限定されない。例えば、苦味を有する薬物としては、
臭化プロパンテリン、塩酸アゼラスチン、アテノロー
ル、カフェイン等を挙げることができる。本発明におけ
るケイ酸類は、特に限定されないが、ケイ酸カルシウ
ム、無水ケイ酸水加物または無水ケイ酸等をその例とし
て挙げることができる。本発明における乳酸カルシウム
は、結晶形、水和物等にかかわらず、いずれも用いるこ
とができ、例えば、無水乳酸カルシウム、乳酸カルシウ
ム５水和物等を挙げることができる。本発明において
は、ケイ酸類に代えてセルロース類もしくは、ケイ酸類
とセルロース類の混合物を用いることもできる。According to the present invention, a drug having an unpleasant taste such as a bitterness is masked to make it easier to take, but the object of the present invention is to improve this taking property. The drug according to the present invention is not particularly limited as long as it has an unpleasant taste, particularly bitterness and irritation. For example, as a drug having a bitter taste,
Propanthelin bromide, azelastine hydrochloride, atenolol, caffeine and the like can be mentioned. The silicic acid in the present invention is not particularly limited, but examples thereof include calcium silicate, anhydrous silicic acid hydrate, and silicic acid anhydride. The calcium lactate in the present invention can be used regardless of the crystal form, hydrate and the like, and examples thereof include anhydrous calcium lactate and calcium lactate pentahydrate. In the present invention, instead of silicic acid, cellulose or a mixture of silicic acid and cellulose can be used.
【０００６】本発明にかかる粒状固形製剤は、薬物とケ
イ酸類を混合し、次に乳酸カルシウムを添加して製造す
ることができる。薬物とケイ酸類の混合は、単に混合す
るだけで良く、特開昭６３−２４３０３５号に開示され
るような吸着操作は必要ない。混合に際しては、乳糖等
の通常使用される賦形剤を添加することができる。The granular solid preparation of the present invention can be produced by mixing a drug and silicic acid and then adding calcium lactate. The drug and the silicic acid can be mixed simply by mixing, and the adsorption operation as disclosed in JP-A-63-243035 is not necessary. Upon mixing, a commonly used excipient such as lactose can be added.
【０００７】乳酸カルシウムの添加は、通常は水に溶解
して行うが、必要により、水溶性有機溶媒を加えてもよ
く、溶解時に加温してもよい。添加は、通常は薬物とケ
イ酸類の混合物を攪拌しながら徐々に行う。[0007] Calcium lactate is usually dissolved in water, but if necessary, a water-soluble organic solvent may be added or the solution may be heated at the time of dissolution. The addition is usually carried out gradually while stirring the mixture of drug and silicic acid.
【０００８】本発明において、薬物と乳酸カルシウムの
割合は、通常は、乳酸カルシウム１重量部に対し、薬物
が８重量部以下であり、好ましくは、３重量部以下であ
る。薬物とケイ酸類との割合は特に限定されないが、通
常は、ケイ酸類１重量部に対し薬物が３重量部以下であ
り、好ましくは１重量部以下である。また、乳酸カルシ
ウムの添加に際しては、通常乳酸カルシウム１重量部に
対し、水を１〜７重量部、好ましくは３〜５重量部使用
し、５０℃以上に加温することが好ましい。In the present invention, the ratio of drug to calcium lactate is usually 8 parts by weight or less, preferably 3 parts by weight or less, with respect to 1 part by weight of calcium lactate. The ratio of the drug to the silicic acid is not particularly limited, but is usually 3 parts by weight or less, and preferably 1 part by weight or less with respect to 1 part by weight of the silicic acid. When adding calcium lactate, it is preferable to use 1 to 7 parts by weight, preferably 3 to 5 parts by weight, of water per 1 part by weight of calcium lactate, and to heat to 50 ° C. or higher.
【０００９】本発明における、粒状固形製剤の剤形は特
に限定されず、散剤、顆粒剤、細粒剤等とすることがで
きる。製剤化に際しては、必要に応じて更に白糖等の甘
味剤と造粒し、整粒することもできる。また、本発明に
より得られた粒状固形製剤を錠剤、カプセル剤等とする
こともできる。The dosage form of the granular solid preparation in the present invention is not particularly limited, and may be powder, granules, fine granules and the like. Upon formulation, the granules may be granulated with a sweetening agent such as sucrose, if necessary. Further, the granular solid preparation obtained by the present invention can be used as tablets, capsules and the like.
【００１０】[0010]
【効果】本発明にかかる粒状固形製剤は、苦味、刺激等
の薬物の不快な味が効果的にマスキングされているた
め、子供や、老人にも服用しやすくなるという効果を奏
する。また、服用した時に口中でのザラつき感が少ない
ため、歯間に詰まりにくく、特に入れ歯を使用している
老人に有用である。更に、有機溶媒を使用する必要がな
いため、安全性に優れるだけでなく、ワックスや水不溶
性高分子などを使用する方法に比べて設備の洗浄も容易
である。[Effect] The granular solid preparation of the present invention effectively masks the unpleasant taste of a drug such as bitterness and irritation, and thus has the effect of being easy to take even for children and the elderly. Further, since it does not cause a rough feeling in the mouth when taken, it is less likely to cause clogging between teeth, which is particularly useful for an elderly person who uses dentures. Furthermore, since it is not necessary to use an organic solvent, not only is the safety excellent, but the equipment can be easily cleaned as compared with the method using a wax or a water-insoluble polymer.
【００１１】[0011]
【実施例】次に実施例を挙げて本発明を更に詳細に説明
するが、本発明はこれら実施例に限定されるものではな
い。The present invention will be described in more detail with reference to examples, but the present invention is not limited to these examples.
【００１２】［実施例１］混合練合機（スーパーミキサ
ーSMV-20型）にアテノロール２５０ｇとケイ酸カルシウ
ム（徳山曹達株式会社製、商品名フローライトＲ）２５
０ｇを入れ混合する。日本薬局方乳酸カルシウム（昭和
化工株式会社製）２５０ｇを精製水９００ｇに入れ、加
温溶解する。乳酸カルシウム溶液を５５℃に冷却後、ア
テノロールとケイ酸カルシウムの混合物に添加し、造粒
した後乾燥して粒状固形製剤を得た[Example 1] 250 g of atenolol and calcium silicate (trade name: Florite R, manufactured by Tokuyama Soda Co., Ltd.) 25 in a mixing and kneading machine (Super Mixer SMV-20 type)
Add 0 g and mix. 250 g of calcium lactate (manufactured by Showa Kako Co., Ltd.) of the Japanese Pharmacopoeia is put in 900 g of purified water and dissolved by heating. The calcium lactate solution was cooled to 55 ° C., added to a mixture of atenolol and calcium silicate, granulated and dried to obtain a granular solid preparation.
【００１３】［試験例１］実施例１で得られた粉末、及
び以下に示す比較例１または２で得られた粉末を用い
て、被験者５名により官能試験を行った。試験方法は、
粉末１５０ｍｇを口中に含み表１の基準にしたがって評
価を行った。Test Example 1 Using the powder obtained in Example 1 and the powder obtained in Comparative Example 1 or 2 shown below, a sensory test was conducted by 5 test subjects. The test method is
The powder was contained in the mouth in an amount of 150 mg and evaluated according to the criteria shown in Table 1.
【００１４】比較例１ 混合練合機にアテノロール２５
０ｇと乳糖２５０ｇを入れ混合する。日本薬局方乳酸カ
ルシウム２５０ｇを精製水２５０ｇに入れ、加温溶解す
る。乳酸カルシウム溶液を５５℃に冷却後、アテノロー
ルと乳酸の混合物に添加し、造粒した後、乾燥して粒状
固形製剤を得た。Comparative Example 1 Atenolol 25 was added to a mixing and kneading machine.
Add 0 g and lactose 250 g and mix. 250 g of Japanese Pharmacopoeia calcium lactate is added to 250 g of purified water and dissolved by heating. The calcium lactate solution was cooled to 55 ° C., added to a mixture of atenolol and lactic acid, granulated, and then dried to obtain a granular solid preparation.
【００１５】比較例２ 混合練合機にアテノロール２５
０ｇとケイ酸カルシウム２５０ｇを入れ混合する。乳糖
２５０ｇを精製水９００ｇに入れ、加温溶解する。乳糖
溶液を５５℃に冷却後、アテノロールとケイ酸カルシウ
ムの混合物に添加し、造粒した後、乾燥して粒状固形製
剤を得た。結果を表２に示した。Comparative Example 2 Atenolol 25 was added to a mixing and kneading machine.
Add 0 g and 250 g of calcium silicate and mix. Lactose (250 g) is added to purified water (900 g) and dissolved by heating. The lactose solution was cooled to 55 ° C., added to a mixture of atenolol and calcium silicate, granulated, and dried to obtain a granular solid preparation. The results are shown in Table 2.
【００１６】[0016]
【表１】 [Table 1]
【００１７】[0017]
【表２】 [Table 2]
【００１８】表２より本発明にかかる粒状固形製剤が優
れた苦みマスキング効果を示すことが明らかである。It is clear from Table 2 that the granular solid preparation according to the present invention has an excellent bitterness masking effect.
───────────────────────────────────────────────────── フロントページの続き (51)Int.Cl.6 識別記号 庁内整理番号 ＦＩ 技術表示箇所 Ａ６１Ｋ 47/02 Ｌ 47/12 Ｂ Ｌ ─────────────────────────────────────────────────── ─── Continuation of the front page (51) Int.Cl. 6 Identification code Internal reference number FI technical display area A61K 47/02 L 47/12 BL
Claims (4)
する粒状固形製剤。1. A granular solid preparation containing a drug, silicic acid and calcium lactate.
ウムを添加する粒状固形製剤の製造方法。2. A method for producing a granular solid preparation, which comprises mixing a drug and silicic acid and then adding calcium lactate.
水加物または無水ケイ酸である請求項１記載の粒状固形
製剤。3. The granular solid preparation according to claim 1, wherein the silicic acid is calcium silicate, anhydrous silicic acid hydrate or anhydrous silicic acid.
水加物または無水ケイ酸である請求項２記載の粒状固形
製剤の製造方法。4. The method for producing a granular solid preparation according to claim 2, wherein the silicic acid is calcium silicate, anhydrous silicic acid hydrate or anhydrous silicic acid.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP29247693A JP3731904B2 (en) | 1993-10-29 | 1993-10-29 | Granular solid formulation |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP29247693A JP3731904B2 (en) | 1993-10-29 | 1993-10-29 | Granular solid formulation |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JPH07126188A true JPH07126188A (en) | 1995-05-16 |
| JP3731904B2 JP3731904B2 (en) | 2006-01-05 |
Family
ID=17782311
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP29247693A Expired - Fee Related JP3731904B2 (en) | 1993-10-29 | 1993-10-29 | Granular solid formulation |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JP3731904B2 (en) |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2006052169A (en) * | 2004-08-12 | 2006-02-23 | Wakoudou Kk | Sol-like or gel-like administration assistant food |
| JP2008094837A (en) * | 2006-09-13 | 2008-04-24 | Kyoto Pharmaceutical Industries Ltd | Masking for bitter taste |
| WO2013058496A1 (en) * | 2011-10-21 | 2013-04-25 | Daewoong Pharmaceutical Co., Ltd. | Taste-masked pharmaceutical composition for oral administration and a process for the preparation thereof |
| KR20210053887A (en) | 2018-08-31 | 2021-05-12 | 하우스 웰니스 푸드 코퍼레이션 | Composition for oral intake that is chewed in the oral cavity and/or dissolved in the oral cavity, comprising a component derived from turmeric |
-
1993
- 1993-10-29 JP JP29247693A patent/JP3731904B2/en not_active Expired - Fee Related
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2006052169A (en) * | 2004-08-12 | 2006-02-23 | Wakoudou Kk | Sol-like or gel-like administration assistant food |
| JP2008094837A (en) * | 2006-09-13 | 2008-04-24 | Kyoto Pharmaceutical Industries Ltd | Masking for bitter taste |
| WO2013058496A1 (en) * | 2011-10-21 | 2013-04-25 | Daewoong Pharmaceutical Co., Ltd. | Taste-masked pharmaceutical composition for oral administration and a process for the preparation thereof |
| KR20210053887A (en) | 2018-08-31 | 2021-05-12 | 하우스 웰니스 푸드 코퍼레이션 | Composition for oral intake that is chewed in the oral cavity and/or dissolved in the oral cavity, comprising a component derived from turmeric |
Also Published As
| Publication number | Publication date |
|---|---|
| JP3731904B2 (en) | 2006-01-05 |
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