Ignoring the physical aspects of a formulation can be disastrous because a variety of solid-state reactions can compromise the stability of a drug entity in its tablet matrix. This situation has changed dramatically over the past decade, with an ever-increasing degree of attention being given to the physical properties of the solids that can compromise a dosage form. Until recently, the priority of regulatory bodies had always been to focus on concerns of safety and efficacy, which led to the required emphasis on aspects of chemical purity ( Chapter 3 ). The most commonly used method of administration for the majority of pharmaceutically active agents is as solid dosage forms, and these units are ordinarily produced by the formulation and processing of powdered solids.
Ahuja, in Separation Science and Technology, 2001 B. Rapid disintegration time was obtained for tablets produced from lactose/chitin, lactose/chitosan, lactose/MCC, potato starch/chitosan, and potato starch/MCC below a certain concentration level of excipient (chitin, chitosan, and MCC) as shown in Fig. Results suggest that chitin and chitosan can be used as direct compression diluents. This study also shows that the hardness of chitin tablets is greater than that of chitosan due to the structural rigidity of chitin, attributed to the acetylamino groups. The hardness of the tablets containing chitin, chitosan, and MCC is increased by increasing the compression force ( Fig. Comparing the hardness of starch/MCC tablets with that of starch/chitin, there was no statistical difference at 10% and 30% (w/w) addition. Using lactose/chitin, lactose/chitosan, and lactose/MCC, tablet hardness increases with the addition of chitin, chitosan, and MCC as shown in Fig. In conclusion, PAMgA polymer allows controlling the release of highly lipophilic drugs as budesonide, being an useful excipient for the development of sustained release matrix tablets.A study was undertaken of directly compressed tablet matrices containing chitin or chitosan in addition to lactose, MCC, or starch formulation. When the dissolution medium was changed sequentially throughout the trial, 75% of the budesonide dose was released in a sustained manner between 4 and 20 h of testing from PAMgA tablets, showing a more controlled budesonide release than Entocort® and Budenofalk® (commercially available sustained release formulations of budesonide).
Budesonide was released slowly from PAMgA tablets, both in gastric and intestinal environment, following Super case II transport kinetics (relaxation-controlled delivery), with a lag time of around 1–2 h. Swelling and erosion of PAMgA tablets was influenced by the reticulation grade of the polymer and the biorelevant media assayed, being water uptake higher for PAMgA 40 tablets in intestinal fluid, whereas PAMgA 5 showed more intense erosion in this biorelevant medium. All the studies were carried out using biorelevant media (FaSSGF and FaSSIF). Tablets with two reticulation grades of PAMgA (PAMgA 5 and 40) and with 9 mg of budesonide were developed and characterized. For this purpose, budesonide, a highly lipophilic compound, was used as model drug. The objective of this work was to evaluate the potential use of a new polymer (PAMgA) in the development sustained release matrix tablets for the treatment of bowel inflammatory diseases.
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