Locally acting orally administered drugs

Trospium is a QTA in which the tropine N-atom is part of two alkyl ring structures (Fig. 1). This drug acts as an antimuscarinic agent that is clinically used as orally administered first-line urinary antispasmodic to treat overactive bladder (OAB) [34], Due to the absence of significant biotransformation, trospium is excreted mainly unchanged into urine allowing to exhibit primarily local activity [84],... 

The occnrrence of a mucus layer that present at the surface of various organs has been exploited to develop mucoadhesive dosage forms. These layers act as administration site to prolong time, and increase the local and/or systemic bioavailability of the administered drug [58]. The appearance of micro and nanotechnologies simultaneously with the execution of non-invasive and painless administration routes has transforms the pharmaceutical market and the management of disease. Intending to minimize the chief limitations of the oral route and... 

Animal and human studies have demonstrated that rifaximin has very poor intestinal absorption after oral administration, so that blood and urine concentrations of rifaximin are practically undetectable [6], Rifaximin excretion is essentially exclusively by the fecal route [5]. Therefore, when rifaximin is administered by the oral route, it acts locally at the intestinal level and eliminates the bacterial organisms that are causing the infection. The important antibacterial activity of rifaximin appears to be directly related to the high intestinal concentration of the drug and inhibition of bacterial growth. The drug has... 

The emetines include emetine and dehydroemetine. These drugs act only against trophozoites. Their mechanism of action is based on eukaryote protein synthesis. They are parenterally administered because oral preparations are absorbed erratically and may induce severe vomiting. They are widely distributed and accumulate in liver, lungs and other tissues. The emetines are slowly elimination via the kidneys. Local side-effects in the area of the intramuscular injection are pain, tenderness and muscle weakness. Serious toxicity is common if the drugs are given for more than 10 days. Side effects include nausea, vomiting, diarrhoea but also cardiotoxicity. 

These can be sprayed orally onto the buccal or the sublingual membrane to achieve a local or a systemic effect. One such spray called insulin buccal spray (IBS) was developed with soybean lecithin and propanediol [94], Soybean lecithin has high affinity for biomembranes but does not enhance the transport of drugs due to low solubility. Propanediol can improve the solubility of soybean lecithin, and act as an enhancer. IBS was administered to diabetic... 

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