Anonymous ID: 1df312 Feb. 28, 2025, 7:01 p.m. No.22678223   🗄️.is 🔗kun   >>8257

>>22678176

 

Septocaine (Articaine) with 1:100,000/1:200,000 Epinephrine: Pregnancy Category C Concentration/carpule: 68mg in 1.7mL single use carpule Lasts: 45–75 minutes Recommended dose: 3.2mg/lb Healthy adult: Max. 6 carpules Has 1.5 times Lidocaine potency. Action occurs within 1–3 minutes. Avoid use in all conditions listed under Citanest Forte.

 

Septocaine (Articaine) is unique among amide-type local anesthetics in the way that it is metabolized. Septocaine is actually a hybrid of both an amide and an ester class anesthetic because of the presence of both an amide and an ester intermediate chain in its chemical composition. Biotransformation of 90–95% of septocaine begins immediately upon the drug entering the blood stream where the plasma carboxyesterase enzymes initiate the metabolic breakdown process via hydrolysis of the ester chain to its primary metabolite, articainic acid, which is inactive. The remainder of septocaine (5–10%) is metabolized in the liver by the hepatic microsomal enzymes. Amides have a high rate of first pass metabolism as the local anesthetic (LA) passes through the liver. Slow absorption from tissue is less likely to result in toxicity. If toxicity occurs, it often results from accidental parenteral injection or due to LA overdose.

Anonymous ID: 1df312 Feb. 28, 2025, 7:13 p.m. No.22678299   🗄️.is 🔗kun   >>8342 >>8379

>>22678257

 

Drug can be slow released in:

 

DepoFoam™ technology: a vehicle for controlled delivery of protein and peptide drugs

 

Qiang Ye

,

John Asherman

,

Mark Stevenson

,

Elizabeth Brownson

,

Nandini V Katre

 

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https://doi.org/10.1016/S0168-3659(99)00146-7

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Abstract

 

A major challenge in the development of sustained-release formulations for protein and peptide drugs is to achieve high drug loading sufficient for prolonged therapeutic effect coupled with a high recovery of the protein/peptide. This challenge has been successfully met in the formulation of several peptide and protein drugs using the DepoFoam™, multivesicular lipid-based drug delivery system. DepoFoam technology consists of novel multivesicular liposomes characterized by their unique structure of multiple non-concentric aqueous chambers surrounded by a network of lipid membranes. The objective of this paper is to demonstrate that DepoFoam technology can be used to develop sustained-release formulations of therapeutic proteins and peptides with high loading. DepoFoam formulations of a protein such as insulin, and peptides such as leuprolide, enkephalin and octreotide have been developed and characterized. The data show that these formulations have high drug loading, high encapsulation efficiency, low content of free drug in the suspension, little chemical change in the drug caused by the formulation process, narrow particle size distribution, and spherical particle morphology. Drug release assays conducted in vitro in biological suspending media such as human plasma indicate that these formulations provide sustained release of encapsulated drug over a period from a few days to several weeks, and that the rate of release can be modulated. In vivo pharmacodynamic studies in rats also show a sustained therapeutic effect over a prolonged period. These results demonstrate that the DepoFoam system is capable of efficiently encapsulating therapeutic proteins and peptides and effectively providing controlled delivery of these biologically active macromolecules.