Molecular scale drug entrapment as a precise method of controlled drug release III: In vitro and In vivo studies of drug release

✍ Scribed by C. T. Rhodes; K. Wai; G. S. Banker

• Publisher: John Wiley and Sons
• Year: 1970
• Tongue: English
• Weight: 467 KB
• Volume: 59
• Category: Article
• ISSN: 0022-3549
• DOI: 10.1002/jps.2600591108

✦ Synopsis

acrylic copolymer entrapment product containing 25 % drug, is quite different. The diffraction pattern indicates that crystalline drug is absent. The absence of crystalline drug in this sample demonstrates that the drug in the entrapment product is uniformly dispersed at a molecular level.

The mechanism by which the carboxylic acid anion facilitator increases the amount of drug bound by the polymer is of considerable theoretical interest and is the subject of a further study. Several modes of action appear possible. The formation of complex ions between the polymer carboxyl group, drug, and acid anions has been suggested, the resultant electrostatic forces binding the drug to the polymer. Presumably, inclusion-type complex formation may also be involved to some extent.

SUMMARY

A new method for the preparation of sustained-action pharmaceuticals by stoichiometric entrapment of drugs in polymer flocculates is described.

The advantages of the use of a suitable entrapment facilitator, an organic acid, to enhance the binding of drugs by polymers is demonstrated.

In vitro tests indicate that the products obtained by this technique could be used in either solid or liquid dosage forms.