クロスカルメルロースナトリウム 化学特性,用途語,生産方法
外観
本品は白色～帯黄白色の粉末である．
本品はエタノール(99.5)又はジエチルエーテルにほとんど
溶けない．
本品は水を加えるとき，膨潤し，懸濁液となる．
本品は吸湿性である．
確認試験
(１) 本品1gにメチレンブルー溶液(1→250000)100mLを加
え，よくかき混ぜて放置するとき，青色綿状の沈殿を生じる．
(２) 本品1gに水50mLを加えてよくかき混ぜ，懸濁液とす
る．この液1mLに水1mL及び用時製した1－ナフトールのメ
タノール溶液(1→25)5滴を加え，硫酸2mLを管壁に沿って
静かに加え層積するとき，液の境界面は赤紫色を呈する．
(３) (2)の懸濁液は，ナトリウム塩の定性反応(1)を
呈する．
ｐＨ 本品1.0gに水100mLを加えて5分間かき混ぜると
き，上澄液のpHは5.0～7.0である．
貯法
容器 気密容器．
乾燥減量
10.0％以下(1g，105℃，6時間).
強熱残分
14.0～28.0％(1g，乾燥物質換算)．
化学的特性
Croscarmellose sodium occurs as an odorless, white or grayishwhite powder.
使用
Croscarmellose Sodiumis a super disintegrant used in pharmaceuticals in the synthesis of tablets for oral administration.
調製方法
Alkali cellulose is prepared by steeping cellulose, obtained from wood pulp or cotton fibers, in sodium hydroxide solution. The alkali cellulose is then reacted with sodium monochloroacetate to obtain carboxymethylcellulose sodium. After the substitution reaction is completed and all of the sodium hydroxide has been used, the excess sodium monochloroacetate slowly hydrolyzes to glycolic acid. The glycolic acid changes a few of the sodium carboxymethyl groups to the free acid and catalyzes the formation ofcrosslinkstoproducecroscarmellosesodium.Thecroscarmellose sodium is then extracted with aqueous alcohol and any remaining sodium chloride or sodium glycolate is removed. After purification, croscarmellose sodium of purity greater than 99.5% is obtained. The croscarmellose sodium may be milled to break the polymer fibers into shorter lengths and hence improve its flow properties.
応用例（製薬）
Croscarmellose sodium is used in oral pharmaceutical formulations as a disintegrant for capsules,tablets, and granules.
In tablet formulations, croscarmellose sodium may be used in bothdirect-compressionandwet-granulationprocesses.Whenused in wet granulations, the croscarmellose sodium should be added in both the wet and dry stages of the process (intra- and extragranularly) so that the wicking and swelling ability of the disintegrant is best utilized. Croscarmellose sodium at concentrations up to 5% w/w may be used as a tablet disintegrant, although normally 2% w/w is used in tablets prepared by direct compression and 3% w/w in tablets prepared by a wet-granulation process.
安全性
Croscarmellose sodium is mainly used as a disintegrant in oral pharmaceutical formulations and is generally regarded as an essentially nontoxic and nonirritant material. However, oral consumption of large amounts of croscarmellose sodium may have a laxative effect, although the quantities used in solid dosage formulations are unlikely to cause such problems.
In the UK, croscarmellose sodium is accepted for use in dietary supplements.
The WHO has not specified an acceptable daily intake for the related substance carboxymethylcellulose sodium, used as a food additive, since the levels necessary to achieve a desired effect were not considered sufficient to be a hazard to health.
貯蔵
Croscarmellose sodium is a stable though hygroscopic material.
A model tablet formulation prepared by direct compression, withcroscarmellosesodiumasadisintegrant,showednosignificant differenceindrugdissolutionafterstorageat30°Cfor14months.
Croscarmellose sodium should be stored in a well-closed container in a cool, dry place.
不和合性
The efficacy of disintegrants, such as croscarmellose sodium, may be slightly reduced in tablet formulations prepared by either the wet-granulation or direct-compression process that contain hygroscopic excipients such as sorbitol.
Croscarmellose sodium is not compatible with strong acids or with soluble salts of iron and some other metals such as aluminum, mercury, and zinc.
規制状況(Regulatory Status)
Included in the FDA Inactive Ingredients Database (oral capsules, granules, sublingual tablets, and tablets). Included in nonparenteral medicines licensed in the UK. Included in the Canadian List of Acceptable Non-medicinal Ingredients.
クロスカルメルロースナトリウム 上流と下流の製品情報
原材料
準備製品