Docusate Sodium is the Sodium salt of Dioctyl Sulfosuccinate, a waxy solid. It is commercially available as a white or off-white, waxy or plastic solid with an odor somewhat reminiscent of Octanol. It is highly hygroscopic and soluble in water and is widely used in pharmaceutical formulations and cosmetics. It is primarily a synthetic anionic surfactant and wetting agent.
It is commercially sold in different physical forms: as pure waxy material, free flowing powder or as liquid. There are several available product forms: Docusate Sodium as a 100% waxy material or 85% powder (Docusate Granular) for tablets, as Docusate Sodium 50% in Polyethylene glycol (PEG 400) and as Docusate Sodium 37% in PEG 400, as well as a compounded Docusate Sodium (85%) and sodium benzoate (15%) powder.
WHAT ARE THE BENEFITS OF DOCUSATE SODIUM?
- Docusate Sodium meets the compendial standards of quality, strength, purity, and potency recognized worldwide.
- Docusate Sodium in medications causes the least possible disturbance of normal body physiology; it is not addictive.
- Its use provides the ability to optimize pharmaceutical formulations and enhance performance results.
- Multiple available Docusate Sodium product types provide flexibility in application, handling and ease of use.
WHAT IS DOCUSATE SODIUM USED FOR?
Docusate is used in the pharmaceutical industry both as an active pharmaceutical ingredient at high concentrations for laxative products and as an excipient where it provides exceptional wetting properties to formulate hydrophobic active ingredients.
Docusate belongs to the class of drugs known as laxatives. Docusate is specifically a stool softener and is mostly used to treat constipation. It works by softening stool. It also helps the muscles in your intestines to move stool.
Docusate is thought to work by lowering the surface tension of hard, dry, stools, allowing water and fats to penetrate which makes the bowel motion softer and easier to pass. This also reduces straining.
Docusate is furthermore a highly effective solubilizing agent in the formulation of poorly soluble active pharmaceutical ingredients (APIs). It can be used in many manufacturing processes such as wet granulation, hot-melt extrusion, extrusion and milling of various high permeability but low solubility compounds that otherwise do not easily dissolve in water.
Docusate is employed as anionic surfactant and wetting agent in many creams and gels. It can also be used (at concentrations of 0.1%-1.0%) to enhance API solubility and in coating formulations (typical 20%). It can act (at 0.1%-1.0%) as a solubilizing agent for dyes, chlorophyll and bile acids. It also finds use as an emulsifying agent for oil and water mixtures and as dispersing agent for hard-to-wet materials.
As API
Docusate Sodium is particularly effective as an active pharmaceutical ingredient in:
- Laxatives and stool softeners for the prevention and treatment of various types of constipation. As a laxative, Docusate is extremely gentle. Unlike other irritant and stimulant laxatives, Docusate is a stool softener laxative without the typical side effects of cramping. It increases the amount of moisture in stools, making them softer and easier to pass, and provides a comfortable bowel movement.
- Prenatal and geriatric vitamin preparations to overcome constipation induced by iron salts
- Colon cleansing aids that find use in the preparation of patients for X-ray examination or surgery
- Ear wax removal aids where it acts as a wetting agent to soften compacted wax
One of the special features of Docusate Sodium is that it is virtually free from adverse reactions when used in recommended dosages. It is effective alone or in combination with peristaltic stimulants and bulking agents. Peristaltic stimulants promote peristalsis, which is a series of contractions that move food through the digestive tract. They can be used to treat constipation, gastric motor failure, and reflux esophagitis.
As Excipient
Docusate Sodium is used in the symptomatic treatment of constipation, and in painful anorectal conditions, such as hemorrhoids and anal fissures for people avoiding straining during bowel movements. Together with Senna it is often the first method for preventing and treating constipation. Docusate often finds use when straining with bowel movements should be avoided (such as after a heart attack or surgery). Docusate is also a stool softener. It works by dissolving water and fats in stool to soften it. This makes it easier to pass, especially when you need to avoid pushing or straining. Docusate sodium and Senna are two different types of laxatives often combined in one formula. One is a stool softener the other is a bowel stimulant. Together, they can produce a bowel movement in six to twelve hours.
Docusate Sodium works by increasing the amount of water the stool absorbs in the gut, making the stool softer and easier to pass. Relief is usually seen in 1 to 3 days with this medication.
As an excipient, Docusate Sodium is one of the best wetting agents in the pharmaceutical industry. It allows in particular to wet very hydrophobic active ingredients, to stabilize micro or nano dispersions and disperse formulations in wet granulation and direct compression.
Docusate Sodium is a pharmaceutical grade surfactant. It is a very efficient wetting, emulsifier, dispersing and solubilizing agent, which has proven effective in more than 50 unique formulations. It is also found as a dispersing agent in tablet manufacture, for liquid or gel suspensions and as emulsifier for creams and gels. In the production of tablets, it can act as a lubricant and as an emulsifier in suspensions. In addition to excellent solubilizing, wetting, dispersing and emulsifying properties, Docusate Sodium gives a low order level of toxicity and is stable and compatible with a wide range of pharmacologically active drugs.
Docusate sodium is known as a powerful solubilizing agent, aiding in the formulation of poorly soluble active pharmaceutical ingredients (APIs). Many new APIs (reported to be 40-70%) have poor aqueous solubility and hence reduced bioavailability. Reduced bioavailability has efficacy and financial consequences, as patients are not receiving the benefits of the medication and companies are often unable to take full advantage of expensive APIs. There is also an unforeseen impact on the environment as trace quantities of these APIs might find their way into the water table. Docusate Sodium can be used to overcome this bioavailability issue by improving solubility using a variety of manufacturing techniques, such as wet granulating, nano milling and hot melt extrusion.
Docusate sodium can be essential as a wetting agent (0.025%-0.25%) in the manufacture of tablets, capsules, creams and gels, for enhancing API solubility (0.1%-1.0%), in coating formulations (20% typical), as solubilizing agent for dyes, chlorophyll, bile acids (0.1%-1.0%), as an emulsifying agent for oil and water mixtures and as dispersing agent for hard-to-wet materials.
REGULATORY STATUS OF DOCUSATE SODIUM
Docusate Sodium is a Food and Drug Administration (FDA) approved excipient. Docusate is listed by the FDA as ‘Generally Regarded As Safe’ (GRAS) product. It is also listed in the European (Ph.Eur) and USP-NF Monographs and is included in the FDA IIG Database (Injections, oral tablets, capsules, suspensions and topical formulations). Docusate sodium has extensive applications as an active pharmaceutical ingredient (API) in stool softener formulations, where it affords consistent and gentle relief. It is an effective and versatile anionic surfactant in a variety of combination laxative/stool softener formulations.
WHAT ARE THE SIDE EFFECTS OF DOCUSATE SODIUM?
What products may interact with Docusate Sodium? Mineral oil is incompatible.
Docusate should also not be used for longer than one week, unless directed by a physician or when abdominal pain, nausea, or vomiting are observed. Give your health care provider therefore a list of all the medicines, herbs, non-prescription drugs, or dietary supplements you use.
Possible side effects of Docusate Sodium use include: allergic reactions that may include skin rash, itching, hives, swelling of the face, lips, tongue, or throat. Side effects that usually do not require medical attention are nausea, stomach pain and vomiting. Other problems can include intestinal obstruction, symptoms of appendicitis, acute abdominal pain, and fecal impaction, especially in children.
CARBOMER, INC.’S DOCUSATE SODIUM PRODUCTS
CarboMer, Inc. offers Docusate Sodium as a pharmaceutical grade that is manufactured under cGMP; it is EP and USP monograph compliant. CarboMer, Inc. also offers Docusate Sodium compounded with Sodium Benzoate as a pharmaceutical grade. These products are all manufactured under cGMP conditions, with USP/EP monographs compliance,
CarboMer, Inc. adheres to strict guidelines set by the Food and Drug Administration (FDA), ensuring the safety and consistent quality of its Docusate products. Additionally, compliance with USP standards and those of other international regulatory bodies reflects CarboMer, Inc.’s commitment to providing the highest-quality Docusate products. Adherence to these regulatory standards guarantees that clients always receive reliable Docusate products of excellent quality.
CarboMer Inc. offers Docusate sodium as: Docusate Sodium: waxy material 100% active Docusate Granular: and as powder 85% active combined with NF grade sodium benzoate 15%.
SUMMARY
Features and Benefits of Docusate Sodium:
It is a very versatile compendial excipient. It is also a highly effective solubilizing agent for use in the formulation of poorly soluble APIs. It can be used in wet granulation, hot-melt extrusion, spheronization-extrusion and milling of poorly soluble compounds and as anionic surfactant and wetting agent in creams and gels.