Immediate release capsule formulations

Apart from immediate release tablet formulations, neural networks have also been applied to modeling immediate release capsule formulations and rapidly disintegrating or dissolving tablets. In the latter, Sunada and Bi from Japan used both statistics and neural networks to optimize both the formulation and processing conditions for rapidly disintegrating tablets developed using both direct compression and wet granulation techniques. 

Maanen R, Bentley D. Bioequivalence of zonisamide orally dispersible tablet and immediate-release capsule formulations results from two open-label, randomized-sequence, single-dose, two-period, two-treatment crossover studies in healthy male volunteers. Clin Ther 2009 31(6) 1244-55. 

To investigate the pharmacokinetics (PK) of an XYZ1234 formulation (200 mg) following topical release in the proximal small bowel, distal small bowel and colon via the Enterion capsule in healthy subjects and to compare to the PKof an XYZ1234 immediate release reference formulation (200 mg). 

The bioavailability from immediate-release capsules ranges from 50% to 95%. Sustained-release formulations are designed to deliver release of procainamide over 12 h. In overdose, absorption... 

Formulations in the United States inclnde lithinm citrate syrnp, lithium immediate-release capsules and tablets, and two snstained-release products. 

Zegerid is a combination product containing omeprazole 20 or 40 mg with sodium bicarbonate in immediate-release oral capsules and powder for oral suspension. It should be taken on an empty stomach at least 1 hour before a meal. Zegerid offers an alternative to the delayed-release capsules or the IV formulation in adult patients with nasogastric tubes. 

Apparatus. The nature of the dosage form will determine the type of dissolution apparatus that will be used for method development and validation. The following questions must be asked when selecting the dissolution apparatus. Is it a capsule Will a sinker be required How stable is the drug substance after dissolution in the medium Is the formulation an immediate release or an extended release formulation Is this a transdermal patch ... 

We include certain excipients in a formulation specifically because they interact with the physiological fluids and the bodily functions in a certain way. For example, as discussed above, we include disintegrants in immediate release tablet and capsule formulations, because we know that when they encounter the aqueous environment of the stomach, they will cause the tablet or capsule to disintegrate and thereby aid dissolution of the API. Another example is the general case of hydrophilic colloid matrices used as prolonged release drug delivery systems. We know that when these materials contact the aqueous environment of the GIT they swell and create a diffusion barrier that slows the rate of dissolution of the dissolved drug. 

Bioavailability studies quantify rate and extent of absorption. They compare the efficiency of the disposition of several drug formulations, e.g. immediate-release vs. extended-release or capsule vs. tablet or tablet A vs. tablet B etc., or they compare the disposition of different routes of administration, e.g. oral vs. subcutaneous or oral vs. intravenous. According to the definition, a comparison to the intravenous bolus injection yields the absolute bioavailability. 

Laminar flow conditions are typically used for tablets, hard gelatin capsules, powders, and granules. Suppositories and soft gelatin capsules are placed in the cell without beads for turbulent flow. Nicolaides, Hempenstall, and Reppas have reported differences in the dissolution rate of a poorly soluble drug, tiaglitazone, from an immediate-release (IR) tablet formulation based on the presence or absence of a tablet holder and/or beads in the flow-through cell. 

Acetyltributyl citrate is used to plasticize polymers in formulated pharmaceutical coatings, including capsules, tablets, beads, and granules for taste masking, immediate release, sustained-release and enteric formulations. 

Oral dosage forms include solutions as well as immediate-release and slow-release tablets and capsules. Since theophylline is cleared from the body relatively rapidly, particularly in children, slow-release formulations have been developed that minimize fluctuations in steady-state serum concentrations during an 8- to 12-h... 

One capsule formulation, Avinza, contains both immediate-release and extended-release beads of morphine for once-daily oral administration. Upon ingestion, 10% of the beads release their morphine content immediately while the residual beads gradually release their morphine content over the next 24 hours. Another capsule formulation is Kadian, which is indicated for every 12 hours or 24 hours dosing. Unlike Avinza it does not contain immediate-release morphine. 

While primarily employed as an analgesic, hydromor-phone is an excellent cough suppressant and is associated with less histamine release and pruritus than codeine. Hydrocodone is only available for oral administration, as either a tablet, capsule, or syrup formulation, and is usually combined with acetaminophen or ibuprofen. Standard immediate-release tablets provide 4-6 h of analgesia for patients with... 

Drug formulations In a 3-month, randomized, blinded study in patients with type I or type II bipolar affective disorder, who were already taking carbamazepine or who were starting to take it, immediate-release or extended-release carbamazepine capsules were substituted. Autonomic and gastrointestinal adverse events were significantly less common in those who took the extended-release formulation [99 ]. 

Drug formulations The bioequivalence of oral dispersible tablets of zonisamide 100 and 300 mg and immediate-release reference capsules has been assessed in two open, randomized-sequence, single-dose, two-period, two-treatment, crossover studies the test formulation met regulatory criteria for bioequivalence [448 ]. 

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