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| Carbocistein Basic information |
| |
| Carbocistein Chemical Properties |
| Melting point |
208-213 °C (dec.) |
| alpha |
-31 º (c=1, 10% NaH2CO3) |
| Boiling point |
417.3±45.0 °C(Predicted) |
| density |
1.315 (estimate) |
| refractive index |
1.5216 (estimate) |
| storage temp. |
2-8°C |
| solubility |
Aqueous Acid, Aqueous Base (Sparingly, Sonicated) |
| pka |
2.06±0.10(Predicted) |
| form |
Amorphous Powder |
| color |
White to slightly off-white |
| Water Solubility |
SOLUBLE IN COLD WATER |
| Merck |
14,1802 |
| BRN |
1725012 |
| CAS DataBase Reference |
638-23-3(CAS DataBase Reference) |
| EPA Substance Registry System |
L-Cysteine, S-(carboxymethyl)- (638-23-3) |
| Hazard Codes |
Xi |
| Risk Statements |
36/37/38 |
| Safety Statements |
24/25-36-26 |
| WGK Germany |
2 |
| RTECS |
AY4342000 |
| TSCA |
Yes |
| HS Code |
29309090 |
| Toxicity |
LD50 oral in rat: > 15gm/kg |
| Provider |
Language |
| 3-Carboxymethylthio-L-alanine |
English |
| SigmaAldrich |
English |
| ACROS |
English |
| ALFA |
English |
| |
| Carbocistein Usage And Synthesis |
| Chemical Properties |
white to slightly off-white amorphous powder |
| Originator |
Rhinathiol,Kramer,Switz. |
| Uses |
carbocysteine is an amino acid. It can be used to help control sebum production. |
| Uses |
Carbocisteine is a mucolytic agent used in the treatment of respiratory disorders ranging from the influenza virus infection to chronic obstructive pulmonary disease (COPD). |
| Uses |
Labeled Carbocisteine, intended for use as an internal standard for the quantification of Carbocisteine by GC- or LC-mass spectrometry. |
| Manufacturing Process |
There were placed 120g of L-cysteine (0.5 mol) in a 2 liter three-necked flask equipped with a stirrer thermometer and methanol/dry ice cooling and 1.5 liters of liquid ammonia were allowed to enter at -40°C. Then there were added under continuous cooling 50 g (2.17 mols) of sodium metal in portions of 1 to 2 g during the course of one hour. The end of the reaction was recognized by the continuation of the blue color. After the end of the reaction the excess sodium was destroyed by the addition of ammonium chloride and the ammonia vaporized at normal pressure. The residue was taken up in 500 ml of water and concentrated in a vacuum to 200 ml in order to remove residual ammonia, and again treated with 300 ml of water. The entire operations were carried out under a nitrogen atmosphere.
The aqueous solution of the disodium salt of L-cysteine obtained is then reacted at 20°C to 30°C under a nitrogen atmosphere in the course of 30 minutes with stirring with a solution of 104 g of chloroacetic acid (1.1 mols) and 4 g of sodium pyrosulfite in 200 ml of water. It is also allowed to post react for 15 minutes at 20°C, the solution clarified over activated carbon and the filtrate treated with 90 ml of concentrated hydrochloric acid to a pH of 2.5.
Thereby the S-carboxymethyl-L-cysteine precipitates out in crystalline form. The product is filtered off with suction, well stirred in 500 ml of water, again filtered with suction and dried in a vacuum at 70°C. The yield is 92% based on L-cysteine. |
| Brand name |
Loviscol (Wyeth-Ayerst); Mucofan (Wyeth-Ayerst). |
| Therapeutic Function |
Mucolytic, Expectorant, Nasal antiinfective |
| Biochem/physiol Actions |
S-Carboxymethyl-L-cysteine is studied as a small molecule mucoactive drug in vivo. These studies include analyzing the oxidative metabolism of S-carboxymethyl-L-cysteine by enzymes such as phenylalanine monooxygenase(s). |
| Safety Profile |
contact. A riot control agent. When heated |
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| Carbocistein Preparation Products And Raw materials |
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| L-Cysteine hydrochloride anhydrous Chemical Properties |
| Melting point |
180°C |
| alpha |
5.5 º (c=8, 6 N HCL) |
| storage temp. |
Inert atmosphere,Room Temperature |
| solubility |
H2O: 1 M at 20 °C, clear, colorless |
| form |
Solid |
| color |
White to light brown |
| optical activity |
[α]20/D +6.4±0.3°, c = 5% in 5 M HCl |
| Water Solubility |
SOLUBLE |
| Sensitive |
Hygroscopic |
| Merck |
14,2781 |
| BRN |
3560277 |
| Stability: |
Stable, but light, moisture and air sensitive. Incompatible with strong oxidizing agents, some metals. |
| InChIKey |
IFQSXNOEEPCSLW-DKWTVANSSA-N |
| CAS DataBase Reference |
52-89-1(CAS DataBase Reference) |
| NIST Chemistry Reference |
L-cysteine hydrochloride(52-89-1) |
| EPA Substance Registry System |
L-Cysteine hydrochloride (52-89-1) |
| Hazard Codes |
Xi |
| Risk Statements |
36/37/38 |
| Safety Statements |
26-36 |
| WGK Germany |
2 |
| RTECS |
HA2275000 |
| F |
3-10-23 |
| TSCA |
Yes |
| HS Code |
29309013 |
| Toxicity |
LD50 intraperitoneal in mouse: 1250mg/kg |
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| L-Cysteine hydrochloride anhydrous Usage And Synthesis |
| Chemical Properties |
solid |
| Uses |
As dough conditioner. |
| Uses |
L-Cysteine hydrochloride, anhydrous is widely used as additive in food production. It is used as an antioxidant to promote fermentation and keep the flavor. It is also used in cosmetics and animal feed. |
| Definition |
ChEBI: A hydrochloride obtained by combining L-cysteine with one molar equivalent of hydrogen chloride. |
| General Description |
L-cysteine is a sulfur-containing amino acid.
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| Biochem/physiol Actions |
NMDA glutamatergic receptor agonist that is also an agonist at AMPA glutamatergic receptors at high concentrations. |
| Safety Profile |
: Moderately toxic by intraperitoneal, intravenous, and possibly other routes. Mutation data reported. When heated to decomposition it emits very toxic fumes of NOx, SOx, and Cl-. |
| Purification Methods |
Likely impurities are cystine and tyrosine. Crystallise the salt from MeOH by adding diethyl ether, or from hot 20% HCl. Dry it under vacuum over P2O5. Hygroscopic. [Beilstein 4 III 1580, 1600.] |
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| L-Cysteine hydrochloride anhydrous Preparation Products And Raw materials |
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| Product Name: |
L-TYROSINE DISODIUM SALT |
| Synonyms: |
DISODIUM TYROSINE;L-3-[4-HYDROXYPHENYL]ALANINE DISODIUM SALT;L-TYROSINE DISODIUM SALT;L-TYROSINE DISODIUM SALT, DIHYDRATE;(S)-2-AMINO-3-(4-HYDROXYPHENYL)PROPIONIC ACID, DISODIUM SALT;L-TYROSINE DISODIUM SALT 95+%;CultureSure L-Tyrosine Disodium Salt Dihydrate, Animal-derived-free;disodium,(2S)-2-amino-3-(4-oxidophenyl)propanoate,dihydrate |
| CAS: |
122666-87-9 |
| MF: |
C9H9NNa2O3 |
| MW: |
225.15 |
| EINECS: |
|
| Product Categories: |
|
| Mol File: |
122666-87-9.mol |
 |
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| L-TYROSINE DISODIUM SALT Chemical Properties |
| storage temp. |
2-8°C |
| form |
powder |
| color |
off-white to tan |
| Water Solubility |
Soluble in water. |
| Sensitive |
Hygroscopic |
| Hazard Codes |
Xi |
| Risk Statements |
36/37/38 |
| Safety Statements |
26-36 |
| WGK Germany |
3 |
| Provider |
Language |
| SigmaAldrich |
English |
| |
| L-TYROSINE DISODIUM SALT Usage And Synthesis |
| Uses |
Tyrosine is a polar, naturally occurring, non-essential amino acid. It is used as a cell culture media component for the commercial biomanufacture of therapeutic recombinant proteins and monoclonal antibodies. |
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| L-TYROSINE DISODIUM SALT Preparation Products And Raw materials |
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| Product Name: |
CALCIUM BUTYRATE |
| Synonyms: |
Butanoicacid,calciumsalt;calciumdibutyrate;BUTYRIC ACID CALCIUM SALT;CALCIUM BUTYRATE;Calcium Butyrate (~90%);Bisbutanoic acid calcium salt;Dibutyric acid calcium salt;Calcium dibutanoate |
| CAS: |
5743-36-2 |
| MF: |
C8H14CaO4 |
| MW: |
214.27 |
| EINECS: |
227-265-7 |
| Product Categories: |
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| Mol File: |
5743-36-2.mol |
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| CALCIUM BUTYRATE Chemical Properties |
| Melting point |
>300°C |
| density |
1.30 g/cm3 |
| storage temp. |
Room Temperature, under inert atmosphere |
| solubility |
DMSO (Soluble), Methanol (Slightly) |
| form |
Solid |
| color |
White to Off-White |
| CAS DataBase Reference |
5743-36-2(CAS DataBase Reference) |
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| CALCIUM BUTYRATE Usage And Synthesis |
| Uses |
Calcium Butyrate was used in the biological study in small intestine of pigs where Butyrate improved digestive and absorptive capacities. |
| Purification Methods |
Recrystallise it from water (5mL/g) by partial evaporation in a desiccator and dry it in a vacuum to constant weight. [Pathak & Bhide J Indian Chem Soc 30 47, 48 1953.] Its dissociation constant at 25o is 0.29 [Colman-Porter & Monk J Chem Soc 4363 1952, Beilstein 2 IV 785]. |
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| CALCIUM BUTYRATE Preparation Products And Raw materials |
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| BETA-CYCLODEXTRIN Chemical Properties |
| Melting point |
290-300 °C (dec.) (lit.) |
| alpha |
[α]D25 +159～+165° (c=1, H2O) (After Drying) |
| Boiling point |
844.96°C (rough estimate) |
| density |
1.2296 (rough estimate) |
| FEMA |
4028 | BETA-CYCLODEXTRIN |
| refractive index |
1.7500 (estimate) |
| storage temp. |
room temp |
| solubility |
1 M NaOH: 50 mg/mL |
| pka |
11.73±0.70(Predicted) |
| form |
powder |
| color |
white |
| PH |
5.0-8.0 (1% in solution, Ph Eur) |
| optical activity |
[α]20/D +162±3°, c = 1.5% in H2O |
| Water Solubility |
Soluble in water and ammonium hydroxide. |
| Merck |
14,2718 |
| BRN |
78623 |
| Stability: |
Stable. Incompatible with strong oxidizing agents. |
| EPA Substance Registry System |
.beta.-Cyclodextrin (7585-39-9) |
| Hazard Codes |
Xi |
| Risk Statements |
36/37/38-20 |
| Safety Statements |
26-36-24/25 |
| WGK Germany |
2 |
| RTECS |
GU2293000 |
| TSCA |
Yes |
| HS Code |
29400000 |
| Provider |
Language |
| SigmaAldrich |
English |
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| BETA-CYCLODEXTRIN Usage And Synthesis |
| Description |
Cyclodextrins refer to a family of compounds consisting of sugar molecules bound together in ring (cyclic oligosaccharides). It is produced from starch through enzymatic conversion. Beta-cyclodextrin is the 7-membered sugar ring molecular form of cyclodextrin. Cyclodextrin has various applications. In the pharmaceutical industry, it can be used as complexing agents for increasing the solubility of poorly soluble drug as well as increasing their bioavailability and stability. It can also alleviate the gastrointestinal drug irritation, and prevent drug-drug and drug-excipient interactions. It can also be used in food, pharmaceutical, drug delivery, and chemical industries, as well as agriculture and environmental engineering. |
| References |
#
# |
| Chemical Properties |
white powder |
| Chemical Properties |
Cyclodextrins occur as white, practically odorless, fine crystalline powders, having a slightly sweet taste. Some cyclodextrin derivatives occur as amorphous powders. |
| Chemical Properties |
A biennial herbaceous plant very common in Europe, Asia, Africa and the United States, it has a tapering fleshy root, furrowed stem, finely cut feathery leaves, umbels of small flower heads in midsummer, and capsules containing two curved narrow seeds. The plant grows to about 60 cm and it blooms from May to July. The part used is the fruit, containing approximately 15% of fixed oils and 3 to 7% of essential oil. Caraway has a warm, biting flavor with a strong, fatty, harsh undernote. |
| Chemical Properties |
beta Cyclodextrin is a virtually odorless, slightly sweet-tasting, white or almost white crystalline solid or fine powder. |
| Occurrence |
A derivative of naturally occurring starch. |
| Uses |
Use to solubilize non-polar compounds such as fatty acids, lipids and cholesterol. Reported useful for the selective precipitation of enantiomeric, positional or structural isomersβ-Cyclodextrin is used with dansyl chloride to form water-soluble complexes for fluorescent labeling of proteins. It is an active ingredient of household odor eliminator. It is also used in personal care products like toothpastes, skin creams and dusting powders. It finds applications in the cosmetic industry for products like detergents and perfumes for the controlled release of fragrances. Further, it is used to produce HPLC columns allowing chiral enantiomers separation. In addition to this, it is used to decrease the level of cholesterol in milk fat. |
| Uses |
β-Cyclodextrin is a cyclic oligosaccharide produced from starch via enzymatic conversion. β-Cyclodextrin is commonly used to produce HPLC columns allowing chiral enantiomers separation. |
| Production Methods |
Cyclodextrins are manufactured by the enzymatic degradation of starch using specialized bacteria. For example, β-cyclodextrin is produced by the action of the enzyme cyclodextrin glucosyltransferase upon starch or a starch hydrolysate. An organic solvent is used to direct the reaction that produces β-cyclodextrin, and to prevent the growth of microorganisms during the enzymatic reaction. The insoluble complex of β-cyclodextrin and organic solvent is separated from the noncyclic starch, and the organic solvent is removed in vacuo so that less than 1 ppm of solvent remains in the β-cyclodextrin. The β-cyclodextrin is then carbon treated and crystallized from water, dried, and collected. |
| Preparation |
Usually produced commercially from Bacillus macerans or B. circulans fermentation of starch or starch hydrolysate. |
| Essential oil composition |
In addition to carvone, the oil contains d-limonene, carveol, diacetyl furfural, methyl alcohol, acetic aldehyde and other substances. Caraway oil consists of 3.5 to 7% volatile and fatty oils; resin, sugar, tannin, mucilage. |
| Taste threshold values |
Reported to have a taste threshold value lower than that of sucrose with a detection level of 3.9 to 27 ppm and a recognition level of 11 to 52 ppm |
| General Description |
Beta-Cyclodextrin is the most abundant and cheap cyclic oligosaccharide that forms inclusion complexes with several drug molecules. Its main application is in tablet and capsule formulations.
Pharmaceutical secondary standards for application in quality control, provide pharma laboratories and manufacturers with a convenient and cost-effective alternative to the preparation of in-house working standards.
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| Pharmaceutical Applications |
Cyclodextrins are ‘bucketlike’ or ‘conelike’ toroid molecules, with a rigid structure and a central cavity, the size of which varies according to the cyclodextrin type. The internal surface of the cavity is hydrophobic and the outside of the torus is hydrophilic; this is due to the arrangement of hydroxyl groups within the molecule. This arrangement permits the cyclodextrin to accommodate a guest molecule within the cavity, forming an inclusion complex.
Cyclodextrins may be used to form inclusion complexes with a variety of drug molecules, resulting primarily in improvements to dissolution and bioavailability owing to enhanced solubility and improved chemical and physical stability.
Cyclodextrin inclusion complexes have also been used to mask the unpleasant taste of active materials and to convert a liquid substance into a solid material.
b-Cyclodextrin is the most commonly used cyclodextrin, although it is the least soluble. It is the least expensive cyclodextrin; is commercially available from a number of sources; and is able to form inclusion complexes with a number of molecules of pharmaceutical interest. However, b-cyclodextrin is nephrotoxic and should not be used in parenteral formulations. b-Cyclodextrin is primarily used in tablet and capsule formulations.
In oral tablet formulations, b-cyclodextrin may be used in both wet-granulation and direct-compression processes. The physical properties of b-cyclodextrin vary depending on the manufacturer. However, b-cyclodextrin tends to possess poor flow properties and requiresalubricant,such as 0.1% w/w magnesium stearate,when it is directly compressed.
In parenteral formulations, cyclodextrins have been used to produce stable and soluble preparations of drugs that would otherwise have been formulated using a nonaqueous solvent.
In eye drop formulations, cyclodextrins form water-soluble complexes with lipophilic drugs such as corticosteroids. They have been shown to increase the water solubility of the drug; to enhance drug absorption into the eye; to improve aqueous stability; and to reduce local irritation.
Cyclodextrins have also been used in the formulation of solutions,suppositories, and cosmetics. |
| Biochem/physiol Actions |
β-Cyclodextrin is the cyclic α heptamer of glucose. It acts as a host to form inclusion compounds with the guests including derivatives of benzene, cyclohexane, adamantane, other alicyclic guests, and also inorganic molecules or ions. It is generally used to solubilize non-polar compounds such a fatty acids, lipids and cholesterol. |
| Safety |
Cyclodextrins are starch derivatives and are mainly used in oral and parenteral pharmaceutical formulations. They are also used in topical and ophthalmic formulations.
Cyclodextrins are also used in cosmetics and food products, and are generally regarded as essentially nontoxic and nonirritant materials. However, when administered parenterally, β-cyclodextrin is not metabolized but accumulates in the kidneys as insoluble cholesterol complexes, resulting in severe nephrotoxicity.
Cyclodextrin administered orally is metabolized by microflora in the colon, forming the metabolites maltodextrin, maltose, and glucose; these are themselves further metabolized before being finally excreted as carbon dioxide and water. Although a study published in 1957 suggested that orally administered cyclodextrins were highly toxic, more recent animal toxicity studies in rats and dogs have shown this not to be the case, and cyclodextrins are now approved for use in food products and orally administered pharmaceuticals in a number of countries.
Cyclodextrins are not irritant to the skin and eyes, or upon inhalation. There is also no evidence to suggest that cyclodextrins are mutagenic or teratogenic.
β-Cyclodextrin
LD50 (mouse, IP): 0.33 g/kg(16)
LD50 (mouse, SC): 0.41 g/kg
LD50 (rat, IP): 0.36 g/kg
LD50 (rat, IV): 1.0 g/kg
LD50 (rat, oral): 18.8 g/kg
LD50 (rat, SC): 3.7 g/kg |
| storage |
Cyclodextrins should be stored in a tightly sealed container, in a cool, dry place.Cyclodextrins are stable in the solid state if protected from high humidity. |
| Purification Methods |
Recrystallise β-cyclodextrin from water and dry it for 12hours in a vacuum at 110o, or 24hours in a vacuum at 70o. The purity is assessed by TLC on cellulose containing a fluorescent indicator. [Taguchi, J Am Chem Soc 108 2705 1986, Tabushi et al. J Am Chem Soc 108 4514 1986, Orstam & Ross J Phys Chem 91 2739 1987.] [Beilstein 19 IV 6287, 19/12 V 801.] |
| Regulatory Status |
Included in the FDA Inactive Ingredients Database: α-cyclodextrin (injection preparations); β-cyclodextrin (oral tablets, topical gels); γ-cyclodextrin (IV injections).
Included in the Canadian List of Acceptable Non-medicinal Ingredients (stabilizing agent; solubilizing agent ); and in oral and rectal pharmaceutical formulations licensed in Europe, Japan, and the USA. |
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| BETA-CYCLODEXTRIN Preparation Products And Raw materials |
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| Product Name: |
Cystamine dihydrochloride |
| Synonyms: |
2,2’-dithiobis-ethanamindihydrochloride;2,2’-dithiobis-ethylamindihydrochloride;2-aminoethyldisulfidedihydrochloride;aed;Cystamine dihydrochloride, 98+%;bis-B-aminoethyldisulphide dihydrochloride;2,2μ-Diaminodiethyl disulfide dihydrochloride, 2,2μ-Dithiobis(ethylamine) dihydrochloride, Decarboxycystine dihydrochloride;Ethylamine, 2,2'-dithiobis-, dihydrochloride |
| CAS: |
56-17-7 |
| MF: |
C4H14Cl2N2S2 |
| MW: |
225.2 |
| EINECS: |
200-260-7 |
| Product Categories: |
Pyridines;Building Blocks;Chemical Synthesis;Organic Building Blocks;Sulfides/Disulfides;Sulfur Compounds;Pharmaceutical Intermediates |
| Mol File: |
56-17-7.mol |
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| Cystamine dihydrochloride Chemical Properties |
| Melting point |
217-220 °C (dec.)(lit.) |
| storage temp. |
Store below +30°C. |
| solubility |
H2O: soluble1.0g/10 mL, clear to almost clear, colorless to almost colorless (<5.5 NTU) |
| form |
Crystalline Powder, Crystals or Chunks |
| color |
White to yellow |
| Water Solubility |
soluble |
| Sensitive |
Hygroscopic |
| Merck |
14,2776 |
| BRN |
3616850 |
| Stability: |
Stable. Incompatible with strong oxidizing agents. |
| CAS DataBase Reference |
56-17-7(CAS DataBase Reference) |
| EPA Substance Registry System |
Ethanamine, 2,2'-dithiobis-, dihydrochloride (56-17-7) |
| Hazard Codes |
Xn |
| Risk Statements |
22-36/37/38 |
| Safety Statements |
37/39-26-36/37/39 |
| WGK Germany |
3 |
| RTECS |
KR7260000 |
| TSCA |
Yes |
| HazardClass |
IRRITANT |
| HS Code |
29309070 |
| |
| Cystamine dihydrochloride Usage And Synthesis |
| Chemical Properties |
white powder |
| Uses |
hepatoprotectant, t-glutaminase inhibitor, heat shock protein promoter, caspase inhibitor |
| Uses |
sulfhydryl modifying reagent and heparin antagonist |
| Uses |
Cystamine dihydrochloride acts as an anti-infective agent, which is used in the treatment of urinary tract infections. It is also used as a radiation-protective agent that interferes with sulfhydryl enzymes. Further, it serves as a heparin antagonist and sulfhydryl modifying reagent. In addition to this, it is used as an inhibitor of TGase. |
| Safety Profile |
A poison by subcutaneous and intraperitoneal routes. Experimental reproductive effects. When heated to decomposition it emits very toxic fumes of HCl, SOx, and NOx. See also SULFIDES. |
| Purification Methods |
Recrystallise the salt by dissolving in EtOH containing a few drops of dry EtOH/HCl, filtering and adding dry Et2O. The solid is dried in a vacuum and stored in a dry and dark atmosphere. It has been recrystallised from EtOH (solubility: 1g in 60mL of boiling EtOH) or MeOH (plates). The free base has b 90-Purification of Biochemicals — Amino Acids and Peptides 100o/0.001mm, 106-108o/5mm and 135-136o/760mm, d 4 1.1559, n D 1.5720. [Verly & Koch Biochem J 58 663 1954, Gonick et al. J Am Chem Soc 76 4671 1954, Jackson & Block J Biol Chem 113 137 1936.] The dihydrobromide has m 238-239o (from EtOH/Et2O) [Viscontini Helv Chim Acta 36 835 1953]. [Beilstein 4 H 287, 4 IV 1578.] |
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| Cystamine dihydrochloride Preparation Products And Raw materials |
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| Product Name: |
Sodium carboxyl methylstarch |
| Synonyms: |
sodium carboxyl methylstarch;SODIUM STARCH GLYCOLATE;SODIUM STARCH GLYCOLLATE;PRIMOJEL(R);CARBOXYMETHYL STARCH SODIUM;CARBOXYMETHYL STARCH SODIUM SALT;SodiumStarchGlycolateExtraPure;Primojel |
| CAS: |
9063-38-1 |
| MF: |
C2H4O3·xNa·x |
| MW: |
0 |
| EINECS: |
618-597-7 |
| Product Categories: |
9063-38-1 |
| Mol File: |
Mol File |
 |
| |
| Sodium carboxyl methylstarch Chemical Properties |
| Melting point |
>210°C (dec.) |
| storage temp. |
Inert atmosphere,Room Temperature |
| solubility |
Practically insoluble in methylene chloride. It gives a translucent suspension in water. |
| form |
neat |
| color |
White to Off-White |
| CAS DataBase Reference |
9063-38-1 |
| EPA Substance Registry System |
Starch, carboxymethyl ether, sodium salt (9063-38-1) |
| WGK Germany |
1 |
| HS Code |
3505100092 |
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| Sodium carboxyl methylstarch Usage And Synthesis |
| Chemical Properties |
White or almost white, fine, free-flowing powder, very hygroscopic. |
| Chemical Properties |
Sodium starch glycolate is a white or almost white free-flowing very hygroscopic powder. The PhEur 6.0 states that when examined under a microscope it is seen to consist of: granules, irregularly shaped, ovoid or pear-shaped, 30–100 mm in size, or rounded, 10–35 mm in size; compound granules consisting of 2–4 components occur occasionally; the granules have an eccentric hilum and clearly visible concentric striations. Between crossed nicol prisms, the granules show a distinct black cross intersecting at the hilum; small crystals are visible at the surface of the granules. The granules show considerable swelling in contact with water. |
| Uses |
Sodium starch glycolate is widely used in oral pharmaceuticals as a disintegrant in capsule and tablet formulations. It is recommended to use in tablets prepared by either directcompression or wet-granulation processes. |
| Uses |
Sodium Starch Glycolate is a starch of potato origin with α1-4 short linear linkages and branched α1-6 linkages between glucose units. Used in the synthesis of capsules for delivery of drugs or medicaments. |
| Production Methods |
Sodium starch glycolate is a substituted derivative of potato starch. Typically, commercial products are also crosslinked using either sodium trimetaphosphate (Types A and B) or dehydration (Type C).
Starch is carboxymethylated by reacting it with sodium chloroacetate in an alkaline, nonaqueous medium, typically denatured ethanol or methanol, followed by neutralization with citric acid, acetic acid, or some other acid. Vivastar P is manufactured in methanolic medium, and Explotab in ethanolic medium. |
| Pharmaceutical Applications |
Sodium starch glycolate is widely used in oral pharmaceuticals as a disintegrant in capsule and tablet formulations. It is commonly used in tablets prepared by either direct-compression or wet-granulation processes. The usual concentration employed in a formulation is between 2% and 8%, with the optimum concentration about 4%, although in many cases 2% is sufficient. Disintegration occurs by rapid uptake of water followed by rapid and enormous swelling.
Although the effectiveness of many disintegrants is affected by the presence of hydrophobic excipients such as lubricants, the disintegrant efficiency of sodium starch glycolate is unimpaired. Increasing the tablet compression pressure also appears to have no effect on disintegration time.
Sodium starch glycolate has also been investigated for use as a suspending vehicle. |
| Safety |
Sodium starch glycolate is widely used in oral pharmaceutical formulations and is generally regarded as a nontoxic and nonirritant material. However, oral ingestion of large quantities may be harmful. |
| storage |
Tablets prepared with sodium starch glycolate have good storage properties. Sodium starch glycolate is stable although very hygroscopic, and should be stored in a well-closed container in order to protect it from wide variations of humidity and temperature, which may cause caking.
The physical properties of sodium starch glycolate remain unchanged for up to 3 years if it is stored at moderate temperatures and humidity. |
| Incompatibilities |
Sodium starch glycolate is incompatible with ascorbic acid. |
| Regulatory Status |
Included in the FDA Inactive Ingredients Database (oral capsules and tablets). Included in nonparenteral medicines licensed in the UK. Included in the Canadian List of Acceptable Non-medicinal Ingredients. |
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| Sodium carboxyl methylstarch Preparation Products And Raw materials |
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