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The Science to Support Rectal Suppositories

The following are the words of scientists and researchers around the world

who explore this field of science and medicine.  We believe it helps the patient

population understand the validity and therapeutic potential of this mode of

delivery.


Suppositories are useful drug delivery systems

in many situations where the patient cannot receive medicine orally,

intravenously, or by injection (such as when a patient is vomiting,

experiencing seizures, or has an obstruction of the upper gastrointestinal

tract) or where the medicine is not orally effective and an alternate route of

administration is necessary (such as when medicine exhibits first-pass

metabolism).”


Rectal drug administration has many advantages over other routes of

drug administration such as oral administration and parenteral administration. For example, many drug substances that are given orally undergo inactivation in the stomach

because of the acidic, enzymatic content of the stomach or the drug may be

subject to digestive attack in the gut and/or to microbial degradation in the

lower gut. Oral administration of drugs also directs all of the absorbed

substances through the liver where they can be inactivated or reduced in

effectiveness.

Rectal administration overcomes wholly, or in part, these known

disadvantages of oral drug administration. Rectal drug administration also has advantages over parenteral administration. For example, rectal drug administration does not require highly trained personnel required for parenteral administration and also represents significantly less hazard to the patient.


In view of the known disadvantages of oral and parenteral drug

administration, drug administration by rectal delivery enables many drugs to

be absorbed from the anorectal area, and yet retain their therapeutic value.

The lower hemorrhoidal vein, surrounding the colon and rectum, enters the

inferior vena cava and thereby bypasses the liver. Therefore, drugs are

absorbed directly into the general circulation when rectally administered.”



Promoting better therapeutic efficacy

Dr. Bindu Boddupalli’s October-December 2010 article, “Mucoadhesive drug

delivery system: An Overview”, published out of the Department of

Pharmaceutics, Nalanda College of Pharmacy, Nalgonda,India  in the Journal

of Advanced Pharmaceutical Technology & Research  stated that

“the rectal lumen have also been explored for the delivery of active agents

both systemically and locally. The active agents meant for the systemic

delivery by this route of administration bypass the hepatic first-pass

metabolism, increase plasma concentrations and thereby promote better

therapeutic efficacy.”


Reference:  http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3255397/?report=pri

ntable


“Mucoadhesive (adhesion of compounds to a mucous layer such as the

rectum, gut or nose) drug delivery systems prolong the residence time of the

dosage at the site of application for absorption.”

Reference:  http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3255397/

This delivery method has the chance for tremendous success


Dr.Rahamatullah Shaikh, affiliated with the Drug Delivery Group, School of

Pharmacy, Queen’s University Belfast, Medical Biology Centre, Belfast,

UK discusses how this delivery method has the chance for tremendous

success in his January-March 2011 article “Mucoadhesive (medicine that

adheres to a mucous membrane) drug delivery systems” in The Journal of

Pharmacy and BioAllied Sciences.  Dr. Shaikh firmly states that

“application of dosage forms to mucosal surfaces (rectal mucosal wall) are of

benefit to drug molecules not amenable to the oral route, such as those that

undergo acid degradation or extensive first-pass metabolism.  Drugs that are

liable to extensive first-pass metabolism can benefit greatly if delivered to the

rectal area.”


Reference:  http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3053525/?report=pri

ntable


Exhibiting a significant anti-tumor effect with a reduced toxicity profile

The College of Pharmacy at Yeungnam University in Gyongsan, South

Korea’s researcher Dr. Seo, published a March 2013 article titled “Docetaxel-

loaded Thermosensitive and Bioadhesive Nanomicells as a Rectal Drug

Delivery System for enhanced Chemotherapeutic Effect” in Pharmaceutical

Research.  Dr. Seo shows that “rectally administered Docetaxel (currently used chemotherapy for refractory breast, lung and prostate cancer)-loaded nanomicelles exhibited a significant

anti-tumor effect with a reduced toxicity profile when compared to orally

administered Docetaxel.”


Reference:  http://www.ncbi.nlm.nih.gov/pubmed/23549753


Cyclodextrins in delivery systems

Dr. Tiwari co-authored the 2010 article “Cyclodextrins in delivery systems:

Applications” which was published in the Journal of Pharmaceutical and

Bioallied Sciences. 

“Recent studies have shown that rectal mucosa can be used as a potential

site for delivering drugs which have a high first-pass metabolism and degrade

in the gastrointestinal pH.  A number of excipients have been used, and

amongst them CDs(cyclodextrins) have been found to be quite useful.”


Reference:  http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3147107/

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