Somatostatin is a peptide hormone that regulates the endocrine system and affects neurotransmission and cell proliferation via interaction with G-protein-coupled somatostatin receptors and inhibition of the release of numerous secondary hormones.Somatostatin has two active forms produced by alternative cleavage of a single preproprotein: one of 14 amino acids, the other of 28 amino acids.
Somatostatin, which is a therapeutic peptide drug, is entrapped within polymeric microspheres made from high molecular weight poly or low molecular weight poly by various modifications of the O/W-solvent evaporation method. Somatostatin is either dispersed as solid, dissolved with the aid of a co-solvent or emulsified as an aqueous solution in the organic polymer solution prior to emulsification into an external aqueous phase. In addition, a non-aqueous O/O-method was evaluated for the formation of the microspheres. Acceptable encapsulation efficiencies are obtained with all methods, regardless of the physical state of drug and the polymer type. The total volume of organic solvent and the co-solvent content were found to be important preparation factors of the O/W-co-solvent method. A more lipophilic solvent system appeared to favor efficient drug encapsulation. Replace the widely used but toxic methylene chloride, ethyl acetate, leading to significantly reduce the drug load. The preparation method substantially affected the morphology of the microspheres and the drug release.
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