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СATALOGUE / PHARMACEUTICAL PRODUCTION TECHNOLOGIES / FILM-COATING OF TABLETS / Film coatings for modified-release applications

Film coatings for modified-release applications

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СATALOGUE / PHARMACEUTICAL PRODUCTION TECHNOLOGIES / FILM-COATING OF TABLETS / Film coatings for modified-release applications

Film coatings for modified-release applications

Modified-release film coatings can be applied to pharmaceutical products to achieve a modified, controlled release of the drug substance. All coatings can be divided into the following four types based on the kinetics of drug release: Coatings that provide intermittent release of the drug substance (intermittent release). This type includes coatings that are resistant to gastric juice – enteric soluble coatings. Coatings that provide immediate release of the drug. Coatings that provide sustained (continuous) release of drugs. Coatings that provide delayed (delayed) release of the drug. Let us consider each type of coatings in more detail. Coatings providing periodic release of the drug substance. This type of coatings provides prolonged action of the dosage form, when administered into the body, the drug is released in portions, which resembles the plasma concentrations created by normal administration during every 4 hours. Such coatings provide repeated action of the drug product.
In dosage forms with this type of coating, one dose is separated from the other by a barrier layer, which may be film, pressed or draped. Depending on the composition of the layer, the dose of the drug substance can be released either after a predetermined time regardless of the localization of the drug in the gastrointestinal tract, or at a certain time in the required part of the digestive tract. Intestine-soluble coatings belong to this type of coatings. They are usually insoluble in the stomach, but dissolve easily when they enter the small intestine.

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  • Information updated : 09 / 11 / 2024
  • In stock
  • Manufacturer : 1 year for Film coatings for modified-release applications

Model: Film coatings

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Delivery of the active substance to any part of the GI tract is achieved by using as a coating exactly those types of Eudragit polymers that dissolve at certain acidity (pH) values of the environment peculiar to this or that part of the GI tract. It is also possible to use combinations of separate types of polymers when it is necessary to deliver drugs to a strictly defined part of the GI tract. The described feature of Eudragit films is crucial for more effective treatment of a number of diseases, including ulcerative colitis, Crohn’s disease and even some cancers. The intestinal soluble coating (water-based) is Kollicoat MAE 30DP (methacrylic acid + ethyl acrylate 1+1) polymer as a 30% water-soluble dispersion and Kollicoat MAE 100P polymer as a 100% water-dispersible powder. Kollicoat is the patented name for all BASF coatings. Kollicoat MAE 1 OOP is a powder consisting mainly of methacrylic acid-ethyl acrylate copolymer (1:1). It has an average molecular weight of approximately 250,000 kDa. It is prepared from Kollicoat MAE*30DP by neutralizing up to about 6 mol% of the copolymer with sodium hydroxide. Additionally, this powder includes two stabilizers to prevent sedimentation and degradation of the copolymer. These polymers form non-hygroscopic films, which require a plasticizer to give the product the necessary elasticity, as the film is quite brittle. Kollicoat MAE films are completely insoluble in acidic media (e.g. 0.1 M HC1 or gastric juice). However, at pH values >5.5 they dissolve at an increasing rate. Therefore, these films are optimally suited for enteric-coated tablets that dissolve after passing through the stomach.

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Technical specifications

Intestine-soluble coatings are used for dosage forms that, when administered, are expected to delay the release of drugs, may be destroyed in the stomach (e.g., pancreatin, erythromycin), may cause nausea or bleeding, or may cause irritation of the gastric mucosa (e.g., aspirin, steroids). Such coatings can be used to re-release drugs in different parts of the GI tract. The action of intestine-soluble coating is due to the difference in properties of gastric and intestinal media due to different acidity and enzyme composition. Although some time ago there were attempts to create coatings that degrade under the action of intestinal enzymes, these developments were not popular, because enzymatic degradation of the film is a rather long process. Thus, most of the widely used intestine-soluble coatings are weak acids that do not dissociate at low pH values, but are easily ionized when the pH of the medium is increased to 5. The most effective enteric soluble polymers are polyacids. Enzyme-degradable coatings are currently used as protective coatings for delivery of polypeptide drug substances into the colon. One of the first synthetic polymers used for intestine-degradable coatings is phthalate cellulose acetate (PCA). However, pH>6 is required for dissolution of the coating, which significantly delays drug release. This polymer is relatively permeable to moisture and gastric juice compared to most enteric soluble polymers. In addition, it is highly susceptible to hydrolytic degradation, in which phthalic acid separates from acetic acid, leading to changes in the properties of the polymer and hence the action of the enteric coating.

Additional information

Other useful polymers used in enteric coating formulations include: Polyvinyl acetate phthalate (PVAP), which is less permeable to moisture and gastric juice, more resistant to hydrolysis, and able to ionize at low pH values; hydroxypropyl methylcellulose phthalate (HPMCP), which has properties similar to those of PVAP; acrylic polymers such as methacrylic acid or methacrylic acid ester copolymer (some of which have a high dissociation constant); cellulose acetate trimellitate (ATC), which has properties similar to those of AFC; carboxymethyl ethyl cellulose (CMEC); hydroxypropyl methylcellulose acetate succinate (HPMCS).
In recent years, acrylic copolymers have been considered most suitable for the development of enteric coatings. A new type of film coatings has emerged, based on poly-methyl methacrylates (PMMA), polymers derived from acrylic acid, called Eudragit, which have the following properties: Excellent moisture-, heat- and light-protective properties, hence increasing the shelf life of drugs (far exceeding the corresponding properties of cellulose); complete neutralization of unpleasant taste and odor, which are often possessed by the active ingredients in the tablet; ease of swallowing large-sized tablets due to the sliding properties of the films; uniformly colored tablets of any shade when combined with pigments; delivery of the active ingredient to any part of the GI tract; use of Eudragit as a matrix for dosage forms with retarded

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