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Oral controlled release

Oral controlled release

Oral controlled release forms offer many advantages, such as nearly constant drug level at the site of action, prevention of peak-trough fluctuations, reduction in dose of drug, reduced dosage frequency, avoidance of side effects, and improved patient compliance. Taste masking, enteric protection, colon targeting, sustained ph-independent release, pulsatile release or combinations thereof: drugs can be delivered at a predetermined rate, locally or systemically and for a specified period of time.

AmatsiSEPS is highly experienced in the development of both single unit (eg, tablet or capsule) or multiple unit (eg, pellets) systems with a customized release pattern. By means of hydrophilic or lipophilic matrix tablet technology and/or coating technologies, several factors as pH, osmotic pressure, swelling, diffusion and erosion are exploited to design a customized release pattern.

Colon targeting delivery system

Colon specific drug delivery has gained increased importance not just for the delivery of drugs for the local treatment of diseases associated with the colon but also as potential site for the systemic delivery of therapeutic peptide and proteins. To achieve successful colon targeted drug delivery, a drug needs to be protected from degradation, release and/or absorption in the upper portion of the GI tract and then ensure abrupt or controlled release in the proximal colon.

AmatsiSEPS uses several approaches for site-specific drug delivery. One is the use of pH sensitive polymers. These polymers are insoluble at low pH levels but become increasingly soluble as pH rises. Time controlled release system such as sustained or delayed release dosage forms are also very promising. However, due to potentially large variations of gastric emptying time, colon arrival time cannot be accurately predicted, resulting in poor colonical availability. Appropriate integration of pH sensitive and time release functions into a single dosage form may improve the site specificity of drug delivery to the colon.


Pulsatile drug delivery system

Much emphasis has lately been laid on the potential of delayed release for meeting chronotherapeutical needs that are being recognised for a number of widespread chronic pathologies, particularly in the case of pathologies which exhibit circadian manifestations. In addition, the pharmacokinetics of some drugs show circardian rhythm and both the pharmacological and toxicological effects of such drugs are dependent on the time of day when the drug is administered. Furthermore, delayed release performances are also exploited to target proximal as well as distal colonic regions via the oral route. When multiple-dosing daily regimens are dealt with, repeated pulsatile delivery patterns could help to enhance the treatment compliance in case the active ingredient is not eligible for prolonged release formulations, for example because of a strong first-pass effect or tolerance development.

Pulsatile systems are basically time-controlled drug delivery systems in which the system controls the lag time independent of environmental factors like pH, enzymes, gastro-intestinal motility, etc.

AmatsiSEPS develops single unit (eg, tablet or capsule) or multiple unit (eg, pellets) pulsatile delivery systems based on the use of erodible barrier coatings or rupturable coatings, that release the drug by pressure build up caused by effervescent excipients, swelling agents, or osmotic pressure.