Disintegrants – Pharmaceutical Excipients

Disintegrants and superdisintegrant excipients are essential components used in the pharmaceutical industry to enhance the dissolution and bioavailability of active pharmaceutical ingredients (APIs). These excipients facilitate the disintegration and rapid breakup of tablets or capsules, which ultimately increases their rate of absorption in the body.

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Definition of Disintegrants and Superdisintegrants

According to the United States Pharmacopeia (USP/NF), disintegrants are defined as “agents added to tablet or capsule formulations to facilitate the breakup or disintegration of the tablet or capsule into smaller particles that dissolve more rapidly in the gastrointestinal fluids” (USP 41-NF 36 General Chapter <701> Disintegration). On the other hand, superdisintegrants are defined as “highly effective disintegrants that, when used at low levels, provide rapid disintegration and dissolution of the tablet or capsule dosage form” (USP 41-NF 36 General Chapter <2040> Superdisintegrants).

The European Pharmacopoeia (Pharm Eur) defines disintegrants and superdisintegrants in a similar manner, but also includes that these agents should be non-toxic, non-irritant, and compatible with other components of the dosage form.

Definition of disintegrants by Peter C. Schmidt in “Pharmazeutische Hilfsstoffe” (1) Disintegrants are substances that are intended to promote the rapid disintegration of a tablet. The mechanism of disintegration can be described as follows: during disintegration, the tablet absorbs water capillary in the disintegration medium. The penetrating water reaches the particles of the disintegrating agent embedded between the granules – or the fillers and binders in the case of direct tableting – in the tablet matrix, which spontaneously absorb water under swelling without dissolving. This results in the so-called swelling pressure, which is the driving force of tablet disintegration (List and Muazzam1979a and 1979b). The amount of swelling pressure depends on the material of the disintegrant and also on its particle size. The particles must be large enough to completely fill the space between the granules or the fillers and binders in order to generate a high swelling pressure. Micronized disintegration aids generally do not promote disintegration.

Schmidt (1) makes the following differentiation of disintegrants by origin. Many have other functions such as binder and fillers.

• Natural Disintegrants

  • Alginic acid
  • Bentonit
  • Microcrystalline Cellulose
  • Powdered Cellulose
  • Guargalactomannan

• Semi-Synthetic Disintegrants

  • Carboxymethylcellulose Calcium
  • Carmellose Sodium
  • Croscarmellose Sodium
  • Sodium Starch Glycolate Type A, B
  • Low-Substituted Carboxymethylcellulose Sodium
  • Low-Substituted Hydroxypropyl Cellulose

• Synthetic Disintegrants

  • Crospovidon

NEWS ON PHARMAEXCIPIENTS “DISINTEGRANT / SUPERDISINTEGRANT”

 

 

Excipients Used as Disintegrants and Superdisintegrants

There are several excipients used as disintegrants and superdisintegrants in the pharmaceutical industry, including:

1. Starches: This is the most commonly used disintegrant in the industry. It includes corn starch, potato starch, and modified starches such as pregelatinized starch, sodium starch glycolate, and starch 1500.
2. Cellulose-based excipients: These include microcrystalline cellulose, croscarmellose sodium, sodium carboxymethyl cellulose, and hydroxypropyl methylcellulose.
3. Natural gums: These include guar gum, xanthan gum, and locust bean gum.
4. Ion exchange resins: These include polacrilin potassium and Amberlite IRP69.
5. Calcium silicates: These include dicalcium phosphate and tricalcium phosphate.
6. Others: These include sodium alginate, cross-linked polyvinylpyrrolidone, and chitosan.

Chemical Background of Disintegrants and Superdisintegrants

The chemical structure of disintegrants and superdisintegrants varies widely depending on the excipient used. Starches, for example, are polysaccharides made up of glucose molecules linked together by alpha 1-4 glycosidic bonds. Modified starches have been chemically modified to improve their functionality. Sodium starch glycolate, for instance, is a cross-linked sodium carboxymethyl ether of starch, while starch 1500 is a pre-gelatinized maize starch that has been modified with sodium sulfate.

Cellulose-based excipients are also polysaccharides, but they are made up of glucose molecules linked together by beta 1-4 glycosidic bonds. Microcrystalline cellulose, for example, is a partially depolymerized cellulose that has been mechanically processed to produce small, crystalline particles. Croscarmellose sodium, on the other hand, is a cross-linked sodium carboxymethyl cellulose.

Natural gums, such as guar gum, xanthan gum, and locust bean gum, are polysaccharides that are obtained from plant sources. They are long chains of sugar molecules linked together by glycosidic bonds. These gums have the ability to absorb water and swell, which helps to facilitate the breakup of the tablet or capsule.

Ion exchange resins, such as polacrilin potassium and Amberlite IRP69, are synthetic polymers that contain functional groups that can exchange ions. They work by absorbing water and swelling, which disrupts the tablet or capsule structure and promotes rapid disintegration.

Calcium silicates, such as dicalcium phosphate and tricalcium phosphate, are inorganic compounds that are commonly used as excipients in the pharmaceutical industry. They have the ability to absorb water and swell, which helps to facilitate disintegration.

Sodium alginate is a natural polysaccharide obtained from brown algae that has been modified with sodium ions. Cross-linked polyvinylpyrrolidone is a synthetic polymer that has been cross-linked to increase its functionality, while chitosan is a natural polymer derived from chitin.

In conclusion, disintegrants and superdisintegrant excipients are essential components used in the pharmaceutical industry to enhance the dissolution and bioavailability of APIs. There are several excipients used as disintegrants and superdisintegrants, including starches, cellulose-based excipients, natural gums, ion exchange resins, calcium silicates, and others. These excipients have different chemical structures and mechanisms of action, but they all work to facilitate the rapid disintegration of tablets or capsules. The use of disintegrants and superdisintegrants in pharmaceutical formulations is an important factor in improving the effectiveness of drugs and ensuring patient safety.

Disintegrant Excipients on pharmaexcipients.com – in alphabetical order

Product	Composition	Manufacturer
AC-DI-SOL® SD-711	Croscarmellose Sodium	DuPont
CORN STARCH 400L-NF	Native Starches	Roquette
DiCom® PL009 P60	Maize starch, Microcrystalline Cellulose	Gangwal Healthcare
EMCOSOY®	Soy Polysaccharides	JRS Pharma
EXPLOTAB®	Sodium Starch Glycolate	JRS Pharma
GLYCOLYS®	Sodium starch glycolate	Roquette
GLYCOLYS® LOW PH	Sodium starch glycolate	Roquette
GLYCOLYS® Low Solvent	Sodium starch glycolate	Roquette
GLYCOLYS® LV	Sodium starch glycolate	Roquette
GLYCOLYS® MAIZE	Sodium starch glycolate	Roquette
Kollidon® CL	Crospovidone	BASF
Kollidon® CL-SF	Crospovidone	BASF
Ludiflash®	Crospovidone, Mannitol, Polyvinyl acetate	BASF
Ludipress® LCE	Kollidon® 30, Lactose Monohydrate, Povidone	BASF
LYCATAB® C	Pregelatinised Starch	Roquette
LYCATAB® C LM	Pregelatinised Starch	Roquette
LYCATAB® CT	Pregelatinised Starch	Roquette
MAIZE STARCH 5%	Maize starch	Roquette
MAIZE STARCH AMYLO N-400	Maize starch	Roquette
MAIZE STARCH B	Maize starch	Roquette
MAIZE STARCH EXTRA WHITE	Maize starch	Roquette
MAIZE WAXY STARCH N-200	Maize starch	Roquette
MICROCEL™ 101 SD	Microcrystalline Cellulose	Roquette
MICROCEL™ 102 SD	Microcrystalline Cellulose	Roquette
MICROCEL™ 112 SD	Microcrystalline Cellulose	Roquette
MICROCEL™ 200 SD	Microcrystalline Cellulose	Roquette
MICROCEL™ 301 SD	Microcrystalline Cellulose	Roquette
MICROCEL™ 302 SD	Microcrystalline Cellulose	Roquette
MICROCEL™ MC-101	Microcrystalline Cellulose	Roquette
MICROCEL™ MC-102	Microcrystalline Cellulose	Roquette
MICROCEL™ MC-112	Microcrystalline Cellulose	Roquette
MICROCEL™ MC-12	Microcrystalline Cellulose	Roquette
MICROCEL™ MC-200	Microcrystalline Cellulose	Roquette
MICROCEL™ MC-302	Microcrystalline Cellulose	Roquette
Omyanutra® 300 Flash	Calcium Carbonate, Tribasic Calcium Phosphate	Omya
Parteck® CCS Croscarmellose Sodium	Croscarmellose Sodium	Merck KGaA
PEA STARCH N-735	Native Starches	Roquette
PEARLITOL® FLASH	Mannitol & Maize Starch	Roquette
Plasdone K-12	Crospovidone	Ashland
Polyplasdone Crospovidone	Crospovidone	Ashland
Polyplasdone INF-10 (Type B)	Crospovidone	Ashland
Polyplasdone Ultra (Type A)	Crospovidone	Ashland
Polyplasdone Ultra-10 (Type B)	Crospovidone	Ashland
Polyplasdone XL-10 (Type B)	Crospovidone	Ashland
POTATO STARCH 6%	Potato Starch	Roquette
POTATO STARCH 8%	Potato Starch	Roquette
POTATO STARCH SUPRA NP	Potato Starch	Roquette
Powdered GP-USP	Native Starches	Roquette
POWDERED NF CORN STARCH	Corn Starch	Roquette
Primojel®	Sodium starch glycolate	DFE PHARMA
PVP-P SANAQ®	Crospovidone	Pharmatrans SANAQ
SOLUTAB® A	Croscarmellose Sodium	Roquette
SOLUTAB® A-IP	Croscarmellose Sodium	Roquette
SOLUTAB® EDP	Croscarmellose Sodium	Roquette
Solvostar	Sodium starch glycolate	Gangwal Healthcare Private Limited
SSG SANAQ®	Sodium starch glycolate	Pharmatrans SANAQ
StarLac®	Co-processed lactose starch	Roquette
STARLOSE®	Lactose Monohydrate, Maize starch	Gangwal Healthcare
VIVAPHARM® PVPP XL	Crospovidone	JRS Pharma
VIVAPHARM® PVPP XL-10	Crospovidone	JRS Pharma
VIVASOL ®	Croscarmellose Sodium	JRS Pharma
VIVASOL® GF	Croscarmellose Sodium	JRS Pharma
VIVASOL® GF LM	Croscarmellose Sodium	JRS Pharma
VIVASTAR® P	Sodium Starch Glycolate	JRS Pharma
VIVASTAR® P 1000 SF	Sodium Starch Glycolate	JRS Pharma
VIVASTAR® P 3500	Sodium Starch Glycolate	JRS Pharma
VIVASTAR® P 5000	Sodium Starch Glycolate	JRS Pharma
WHEAT STARCH TB	Wheat Starch	Roquette

 

References
(1) „Pharmazeutische Hilfsstoffe“ Peter C. Schmidt · Siegfried Lang