Tablet formulations enteric-coated

Aspirin is commercially available in numerous formulations (Table 7-1). It is compounded as a tablet, an enteric-coated tablet, a controlled-release tablet, and as a suppository. Enteric-coated aspirin, which decreases GI tract irritation, is recommended for chronic use but is rarely required for the treatment of acute ocular pain, which usually resolves over several days. Likewise, controlled-release aspirin, because of its relatively long onset of action, is not recommended for treatment of acute ocular pain. 

Aabakken L, Bjornbeth BA, Hofstad B, Olaussen B, Larsen S, Osnes M. Comparison of the gastrointestinal side effects of naproxen formulated as plain tablets, enteric-coated tablets, or enteric-coated granules in capsules. Scand J Gastroenterol Suppl 1989 163 65-73. 

Uses. Aspirin has analgesic, antiinflammatory, and antipyretic activity. It is used for the reHef of less severe types of pain, such as headache, neuritis, acute and chronic rheumatoid arthritis, and toothache. Aspirin can be purchased in a variety of OTC and prescription dosage forms made and formulated by many companies. Tablets, ie, buffered, plain, or enteric-coated, are the most familiar in the United States, but other forms such as powder and effervescent formulations are of considerable importance in other parts of the world. 

Comparable daily doses of PPIs are omeprazole 20 mg = esomeprazole 20 mg = lansoprazole 30 mg = rabeprazole 20 mg = pantoprazole 40 mg. The PPIs degrade in acidic environments and are therefore formulated in delayed-release capsules or tablets.16 Lansoprazole, esomeprazole, and omeprazole contain enteric-coated (pH-sensitive) granules in a capsule form. For patients unable to swallow the capsule or in pediatric patients, the contents of the capsule can be mixed in applesauce or placed in orange juice. If a patient has a nasogastric tube, the contents of an omeprazole capsule can be... 

RH Blythe, GM Grass, DR MacDonnell. The formulation and evaluation of enteric coated aspirin tablets. Am J Pharm 131 206-216, 1959. 

Designed experimentation, involving mostly some type or modification of factorial design, has been used to study many different types of formulation problems. These include a pharmaceutical suspension [21], a controlled-release tablet formulation [22], and a tabletcoating operation [23]. In the latter case, Dincer and Ozdurmus studied an enteric film coating and utilized the steepest descent graphic method to select the optimum. 

By administering both sizes of formulation simultaneously, a better discrimination of relative transit of the two phases can be made. In a cohort of 22 healthy young volunteers, an enteric-coated capsule was administered which contained tablets ("mTc-labeled 5 mm or 8.4 mm diameter) together with pellets (mIn-labeled 0.2 mm ion-exchange resin particles). The unit delivered the radiopharmaceuticals simultaneously to the ileocecal junction [44]. Under control conditions, no difference was observed between the rate of transit through the ascending colon of 0.2-mm particles versus 5-mm tablets, or 0.2-mm particles versus 8.4-mm tablets. The mean period of residence of 50% of the administered 0.2-mm particles in the ascending colon was 11.0 + 4.0 h. 

Duloxetine hydrochloride, a novel anti-depressive, is known to be acid labile and, consequently, it has been formulated as an enteric-coated tablet. Interestingly, Jansen et al. [97] subsequently found that the drug was destabilised by degradation products within these enteric polymers. The authors found that succinyl and phthalyl residues from the hydroxypropyl methylcellulose acetate succinate (HPMCAS) and hydroxypropyl methylcellulose phthalate (HPMCP) formed... 

Sugar-coated products have been marketed that contain KCl in a wax matrix (Slow-K and Kaon-Ct) and are purportedly slow- and controlled-release preparations. Available evidence indicates that these slow-release forms of KCl are occasionally capable of causing local tissue damage and therefore prol5ably should be used with caution for K+ supplementation. Solutions of potassium gluconate, like the tablets, also have been associated with intestinal ulceration. Microencapsulated KCl preparations Micro-K, K-Dur) that are neither enteric coated nor contained within a wax matrix appear to be superior to the wax matrix formulation. 

Sustained release preparations of potassium chloride have been widely used to overcome the gastrointestinal side effects following medication with enteric coated tablets. Such formulation techniques delay the rate of absorption and produce a slow release of potassium chloride during the passage through the gastrointestinal tract [1,2]. 

Pancrelipase is available in both non-enteric-coated and enteric-coated preparations. Pancrelipase enzymes are rapidly and permanently inactivated by gastric acids. Therefore, non-enteric-coated preparations (eg, Viokase tablets or powder) should be given concomitantly with acid suppression therapy (proton pump inhibitor or H2 antagonist) to reduce acid-mediated destruction within the stomach. Encapsulated formulations contain acid-resistant microspheres (Creon) or microtablets (Pancrease, Ultrase). Enteric-coated formulations are more commonly used because they do not require concomitant acid suppression therapy. 

The original formulation, a buffered powder, has been replaced by chewable and dispersible buffered tablets with greater bioavailability (30-40%) a new enteric-coated formulation further improves patient convenience and tolerability. Since the chewable tablets contain both phenylalanine (36.5 mg) and sodium (1380 mg), caution should be exercised in patients with phenylketonuria and those taking sodium-restricted diets. Didanosine should be taken on an empty stomach and, because of the buffered formulation, should be administered at least 2 hours after administration of drugs requiring acidity for optimal absorption (eg, ketoconazole, itraconazole, dapsone). 

As previously discussed, food effects are an important parameter for enteric-coated systems, especially for drugs, that are sensitive to food. Pancreatic enzyme-containing products fail when they come in contact too early with lipids, proteins, and carbohydrates present in food. The clinical efficacy of pancreatic enzymes formulated as enteric-coated tablets was investigated in man and dog [44], The enteric materials examined were hydroxypropyl methylcellulose phthal-ate (HPMCP), cellulose acetate phthalate (CAP), and the methacrylic acid copolymer USP/NF Type C. In vivo behavior monitored by x-ray scintigraphy showed clear differences between the three coating formulations. HPMCP-coated products adhered to the gastric mucosa, whereas CAP and methacrylate copolymer... 

The pharmaceutical and biological availability of eight commercial furose-mide preparations was compared including two products with modified release properties [67], an enteric-coated tablet and a sustained-release preparation, in the form of a capsule containing diffusion pellets [28], A correlation between the rate of dissolution of different techniques and the area under the plasma concentration time curve was documented. The sustained-release preparation and the enteric-coated formulation clearly showed different pharmacokinetic behavior compared with conventional tablets. Although the literature mentions the maximal absorption at pH 5.5, the modified release formulations only showed a relative bioavailability of 80%. 

Pantoprazole is sensitive to degradation in the acidic medium of the stomach, so the drug is formulated in enteric-coated formulations. Pantoprazole is rapidly absorbed after oral administration, with peak plasma concentrations (Cmax) of 1.1 to 3.1 (mean 2.1 mg/L) occurring at 2 to 4 (mean 2.7) hours (tmax) after ingestion of an enteric coated 40 mg tablet. 

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