| Size | Price | |
|---|---|---|
| Other Sizes |
| Targets |
Croscarmellose sodium is a pharmaceutical excipient that does not have specific biological receptors as its primary targets. Its mechanism of action is physical rather than pharmacological: it rapidly absorbs water and swells, assisting in the disintegration and dissolution of tablet formulations when they come into contact with moisture in the gastrointestinal tract. The cross-linking prevents the polymer from dissolving in water, allowing it to swell and create channels for water penetration. Its primary applications are as a superdisintegrant in oral solid dosage forms.
|
|---|---|
| ln Vitro |
In vitro, croscarmellose sodium is used as a pharmaceutical excipient and superdisintegrant in tablet formulations. It is often used in conjunction with or in place of microcrystalline cellulose as an excipient for active pharmaceutical ingredients and nutritional tablets. The compound's ability to rapidly absorb water and swell makes it effective for enhancing the dissolution and disintegration of tablets, thereby improving drug absorption and bioavailability. It is also used to increase the viscosity of water-based drilling muds.
|
| ln Vivo |
Croscarmellose sodium is a pharmaceutical excipient that is not intended to have systemic pharmacological activity. When administered orally as part of a tablet formulation, it acts locally in the gastrointestinal tract to facilitate tablet disintegration. It is not absorbed systemically and is excreted unchanged in the feces. The compound is classified as a pharmaceutical excipient and is generally recognized as safe for use in pharmaceutical formulations.
|
| Enzyme Assay |
In vitro assays for croscarmellose sodium typically evaluate its disintegration and swelling properties. A standard protocol involves compressing the excipient into tablets with a model active ingredient. Tablet disintegration time is measured using a disintegration apparatus in simulated gastric or intestinal fluid at 37°C. Swelling volume is assessed by measuring the volume increase of the polymer upon hydration. Water uptake is measured by gravimetric analysis. The compound's effectiveness as a superdisintegrant is evaluated by comparing disintegration times and dissolution rates of tablets with and without the excipient.
|
| Cell Assay |
Cellular assays for croscarmellose sodium are not standard, as it is a pharmaceutical excipient that is not intended to interact with cells. The compound is used as an inert ingredient in tablet formulations and is not expected to have direct cellular effects. Any cellular studies would focus on evaluating the bioavailability of the active pharmaceutical ingredient in formulations containing croscarmellose sodium. The compound's primary value lies in its physical properties as a disintegrant rather than any biological activity.
|
| Animal Protocol |
In vivo animal studies for croscarmellose sodium are typically conducted to evaluate its safety as a pharmaceutical excipient. A common protocol involves administering the compound to rodents via oral gavage at doses far exceeding those used in pharmaceutical formulations. Body weight, clinical signs, and organ histopathology are monitored. The compound's lack of systemic absorption and low toxicity profile are confirmed through these studies. The compound is generally recognized as safe for use in pharmaceutical formulations.
|
| ADME/Pharmacokinetics |
Pharmacokinetic data for croscarmellose sodium indicates that it is not absorbed systemically when administered orally. The compound has a molecular weight of approximately 263.20 g/mol. It is a free-flowing, odorless, white powder with a bulk density of 0.48 g/cc and a pH of 5.0-7.0. It is hydrophilic but insoluble in water. As a cross-linked polymer, it remains in the gastrointestinal tract and is excreted unchanged in the feces. Specific ADME data is available from the published literature.
|
| Toxicity/Toxicokinetics |
Croscarmellose sodium is generally recognized as safe for use as a pharmaceutical excipient. The compound is classified as a pharmaceutical excipient and is not intended for therapeutic use. Standard safety precautions include handling with appropriate personal protective equipment (gloves, lab coat, safety goggles) in a well-ventilated area. The compound should be stored in a dry, cool place away from incompatible materials. No significant toxicity is expected at normal usage levels. No specific LD₅₀ values are available in the public domain.
|
| References | |
| Additional Infomation |
cellulose derivative belonging to the β-(1,4)-D-glucopyranose polymer family. It can be used as a bulk-forming laxative, an emulsifier and thickener in cosmetics and pharmaceuticals, and a stabilizer for reagents.
See also: Sodium carboxymethyl cellulose (note moved to); Cross-linked sodium carboxymethyl cellulose (note moved to)... See more... Croscarmellose sodium (CAS 74811-65-7) is a pharmaceutical excipient and superdisintegrant with the molecular formula of a cross-linked sodium carboxymethyl cellulose polymer. It is widely used in oral tablet formulations to enhance disintegration and dissolution, improving drug absorption and bioavailability. It is classified as a pharmaceutical excipient and is generally recognized as safe. It is available from multiple commercial suppliers in various pack sizes. No clinical trials or approved drug status exist for this compound as it is not a therapeutic agent. |
| Exact Mass |
263.074
|
|---|---|
| CAS # |
74811-65-7
|
| PubChem CID |
6328154
|
| Appearance |
White to off-white solid powder
|
| Melting Point |
>205C
|
| Hydrogen Bond Donor Count |
6
|
| Hydrogen Bond Acceptor Count |
8
|
| Rotatable Bond Count |
5
|
| Heavy Atom Count |
17
|
| Complexity |
169
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
DPXJVFZANSGRMM-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C6H12O6.C2H4O2.Na/c7-1-3(9)5(11)6(12)4(10)2-8;1-2(3)4;/h1,3-6,8-12H,2H2;1H3,(H,3,4);
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
