The mentioning of rectal suppositories often results in a brief silence followed by a surprised nervous laugh. However, when the rationale of how rectal suppositories could be effective and make the difference between health and sickness, opinions quickly change from surprise to appreciation.
There is a growing acknowledgement of the need to provide safer, more cost-effective treatments that can either reduce the need for pharmaceuticals (ie: drugs) and/or to reduce their side effects. Currently, there exists ample research to demonstrate nutrients, herbals and nutraceuticals can do just that, if only they could be absorbed in such a manner as to allow greater therapeutic effect. Rectal suppositories clearly offer a safer and demonstrably more effective option.
In the U.S. there always has been a perceived patient compliance issue with the marketing of rectal suppositories. It has been assumed that although the rest of the world (especially the Japanese and Europeans) are comfortable with the use of suppositories, Americans would resist such a mode of delivery. However, in the ten years of selling the products, they have found the adage “some will and some won’t” to be true. Also, there is the American public’s predisposition to do or take whatever it takes, if it is effective.
How do Rectal Suppositories Work?
All drugs, or compounds that act like drugs, when administered orally, are absorbed from the gastrointestinal tract into the portal venous circulation and pass through the liver (first pass metabolism) where the process of drug metabolism begins. Suppositories, like intravenous (IV), intramuscular (IM), and transdermal methods of administration, bypass this “first pass” effect and are absorbed into the lower and middle hemorroidal veins without encountering liver metabolism. In addition, the rectum is filled with blood vessels that offer direct access into the body’s bloodstream via the inferior vena cava. This allows for rapid access to systemic circulation.
When nutrients are put into an active delivery system, called a suppository base, and then placed in the rectum, a “transfer” of water from the rectum to the fat-based suppository must occur for the separation of the active ingredients from the base into the rectal mucosa. Zetpil™’s proprietary base is formulated with key ingredients that not only protect the active ingredients but also facilitate the movement of the active compounds from the base to the rectum. This technology facilitates solubility, and allows a compound that is usually insoluble in water (hydrophobic) to dissolve, and thus be absorbed. This is crucial for poorly absorbed compounds.
Zetpil™ suppositories are comfortable, non-irritating, rapid-melting, fully absorbed in 15-20 minutes, and imperceptible after insertion.
Why Suppositories Make Sense
- Rectal suppositories deliver nutrients directly into the bloodstream, resulting in superior nutrition.
- The rectum is ideal for nutrient absorption because it is not buffered and has a neutral pH. Unlike the stomach and intestines, there is no acid or enzymatic activity that causes degradation of the nutrients.
- The anorectal physiology provides a large surface area for nutrient absorption.
- The rectal mucosa is capable of tolerating a much higher level of irritation than gastric mucosa.
- Suppository formulations are extremely efficient in delivering medications because they do not occupy much volume. Therefore, suppositories can deliver a higher concentration of vitamins, minerals, amino acids and nutraceuticals when compared to foods or oral supplements required to maintain health.
- Suppositories eliminate food interactions and competitive absorption chemistry which occurs with oral supplementation. This further increases nutrient bioavailability and thus, bioactivity.
- Deliver nutrients and/or nutraceuticals directly into the bloodstream;
- Achieve therapeutic dosages of key nutrients which are unachievable with oral delivery;
- Reduce the need for pharmaceuticals and/or minimize their side effects;
- Provide a delivery system for those unable to take oral nutrients, and thus struggle
The Zetpil “NOW” Solution
Comfortable, easy to use and cost effective.
Zetpil™ has developed a suppository that is comfortable, cost effective and easy to take. They have developed an entire line of herbal, nutrient and nutraceutical rectal suppositories which demonstrate high levels of safety, tolerance, and efficacy that cannot be matched by most of the current nutrient formulations on the world’s market. Zetpil™ is not only nutrition you can feel but represents the most honest nutritional product on the market today- period.
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.
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).”
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.”
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.”
“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.”
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.”
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.”
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.”