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Insulin Is Not Administered Through Oral Route Because

Development And Evaluation Of Insulin Incorporated Nanoparticles For Oral Administration

Development And Evaluation Of Insulin Incorporated Nanoparticles For Oral Administration

Copyright © 2013 Amiya kumar Prusty and Susanta Kumar Sahu. This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. Abstract The current study was designed to prepare and characterize insulin incorporated nanoparticles by complex coacervation process followed by antidiabetic study of orally administered insulin incorporated nanoparticles in diabetic rats. The nanoparticles were characterized for particle size, loading and entrapment efficiency as well as in vitro release of incorporated insulin. The prepared nanoparticles were found to have an average particle size of 551.67 nm . The highest entrapment efficiency and loading capacity values were found to be of and , respectively. Oral administration of 10 IU/Kg of insulin loaded nanoparticles to diabetic rats showed a maximum blood glucose change of at 5-hours time period. The results obtained indicate the potential of prepared nanoparticulate system as a carrier for oral delivery of insulin. 1. Introduction Oral route is considered to be more convenient, safe, and most the acceptable route of administration of drugs for chronic therapy. In the treatment of insulin dependent diabetes mellitus or type-1 diabetes, insulin is generally administered parenterally via subcutaneous route. But this clinical therapy suffers from many disadvantages, for example, local discomfort, inconvenience of multiple administration, and occasional hyperinsulinemia due to overdose [1]. However insulin administered by oral route is not as effective as by subcutaneous route because of poor absorption in gastrointestinal tract because of it’s large size and hydrophilic nature. Insulin d Continue reading >>

How To Give Insulin To A Dog

How To Give Insulin To A Dog

Dogs with diabetes aren't able to make enough insulin, a hormone that allows the body to store energy from food and move glucose into cells. Because this condition has serious and potentially fatal consequences, diabetic dogs are typically treated with insulin injections one or two times each day. Because insulin is not a sturdy substance, it is important to handle it gently and avoid exposing it to extreme temperatures or excessive motion. Store unopened bottles of insulin in your refrigerator. After they have been opened, it is still advisable to keep insulin in the fridge. It can tolerate short periods of time at room temperature in an area where it’s out of direct sunlight. Before attempting to give your dog insulin, it is wise to practice loading the syringe with the appropriate amount of sterile water or saline. You can even use an apple or orange to practice giving insulin injections until you feel you are ready to try it on your dog. Because there are many different kinds of dog insulin syringes, make sure you buy the size and type recommended by your veterinarian. Always use a new syringe and needle every time you give your dog an insulin injection. This will guarantee that your supplies are sterile and minimize risk of infection. Unwrap the syringe and needle, but leave the needle itself capped until you are prepared to load the syringe with insulin. Carefully roll the bottle of insulin in your hands to make sure the hormone is well mixed. Do not shake it. Remove the needle cap. Then, use the pointer finger and thumb of one hand to hold the insulin syringe while drawing back on the plunger with the other hand. Continue to pull back, filling the plunger with air, until you reach the correct marker for the amount of insulin your dog will need. Hold the bottle Continue reading >>

Oral Insulin (swallowed) And Rectal Insulin Suppository For Diabetics:

Oral Insulin (swallowed) And Rectal Insulin Suppository For Diabetics:

In Part I of this article, we discussed diabetes treatments and the dangers of alternative inhalation insulin delivery systems when used as a replacement for insulin shots.1,2 In recent times, we have seen the research we discussed supported. Pfizer Pharmaceuticals has reported six lung cancer cases resulting from the use of their FDA-approved Exubera, an inhalation insulin product. Pfizer consequently withdrew the drug from the market, taking a 2.5 billion-dollar loss.3,4 The FDA still has not withdrawn their approval. Pharmaceutical giants Amlyin and Eli Lilly have reported six deaths and 30 cases of pancreatitis resulting from the use of the anti-hypoglycemic agent Byetta (Exenatide: oral and injectable forms). These are good examples of the deadly adverse effects of newly introduced, FDA-approved anti-diabetic drugs. Fear of needles and a resistance to the inconvenience of administering insulin injections have created a burgeoning demand for alternative methods of treating diabetes. An apparent breakthrough arrived with the development of insulin inhalation preparations. While the FDA deemed this novel insulin preparation safe and effective, Pfizer, as mentioned, withdrew their inhalation insulin product after publication of our article detailing its dangers.1 Oral and nasal spray insulin preparations are not much different than inhalation insulin, which increases the incidence of cancers and other diseases, hence none of these preparations should be approved for public use. Given the inhalation insulin debacle, many research centers and pharmaceutical companies are now scrambling to find other alternative methods of delivery to replace painful subcutaneous insulin injections and help make diabetics more compliant. One out of every ten health care dollars spent in t Continue reading >>

K Gowthamarajan And Giriraj T Kulkarni

K Gowthamarajan And Giriraj T Kulkarni

GENERAL I ARTICLE Oral Insulin - Fact or Fiction? Possibilities of Achieving Oral Delivery for Insulin K Gowthamarajan is on the faculty of the Department of Pharmaceutics in JSS College of Pharmacy, Ootacamund. His research interests are in the area of designing drug delivery systems for peptides and proteins. He is currently involved in research on pharmaceutical applications of plant polysaccharides. Giriraj T Kulkarni is on the faculty of the Department of Pharmaceutics in JSS College of Pharmacy, Ootacamund. Currently, he is involved in research on pharmaceutical and biotechnological applica- tions of plant polysaccha- rides. He has authored a book 'Biotechnology and its Applications in Pharmacy' for undergraduate and post- graduate students of pharmacy. Key words Oral insulin, penetration en- hancers, protease inhibitors, microspheres, nanoparticles, bioodhesive delivery. Insulin is a major protein hormone secreted by the p-cells of the pancreas and is important for the control of diabetes. Insulin is usually administered to diabetic patients through subcutaneous injection. This mode of therapy has certain inherent disadvantages such as local pain, itching and insulin lipodystrophy around the injection site. Hence, pharmaceutical scientists have been trying to design an oral delivery system for insulin. Many challenges are asso- ciated with the oral delivery of insulin, relating to the physical and chemical stability of the hormone, and its absorption and metabolism in the human body. Here we discuss various strategies for the oral delivery of insulin that are being tried out, as well as methods used to improve the absorption of orally consumed insulin and to reduce its degradation by digestive enzymes. Before the discovery of insulin (Box 1) by Banting and Best i Continue reading >>

Are Injections More Effective Than Tablets?

Are Injections More Effective Than Tablets?

Legionella Testing Lab - High Quality Lab Results CDC ELITE & NYSDOH ELAP Certified - Fast Results North America Lab Locations legionellatesting.com There is a common belief among many people that injections are more effective than tablets. In fact, some patients will claim that they have not been treated if they are not given injections. These patients probably think that since injections are more painful then it means that they are more effective. However, the pain experienced by injections such as quinine is as a result of their high acidity or alkalinity and not due to their effectiveness. In order to understand best whether injections are more effective than tablets, it is paramount to address the reasons why certain medications are in form of injections while others are in tablet form. There are certain drugs which if given as tablets would be completely ineffective since they would be destroyed by the enzymes that digest food in the stomach. A good example is the insulin injection used in the treatment of diabetes. Insulin is a protein and therefore if given as tablet it would be digested by the same enzymes that digest meat (a protein) in the stomach. For this reason you will never come across insulin tablets. Similarly, certain drugs are also ineffective if given in an injection form except when given as tablets. This is because some drugs are only effective when in a solid form. Once formulated into an injectable liquid, they easily break down and lose their medicinal properties. To understand this better, let’s use an illustration of powdered milk. Powdered milk in solid form can last years, even without refrigeration while liquid milk may not last for three days in the open. To address this instability issue, some injections come as powders which have to b Continue reading >>

Oral Insulin And Buccal Insulin: A Critical Reappraisal

Oral Insulin And Buccal Insulin: A Critical Reappraisal

Go to: Abstract Despite the availability of modern insulin injection devices with needles that are so sharp and thin that practically no injection pain takes place, it is still the dream of patients with diabetes to, for example, swallow a tablet with insulin. This is not associated with any pain and would allow more discretion. Therefore, availability of oral insulin would not only ease insulin therapy, it would certainly increase compliance. However, despite numerous attempts to develop such a “tablet” in the past 85 years, still no oral insulin is commercially available. Buccal insulin is currently in the last stages of clinical development by one company and might become available in the United States and Europe in the coming years (it is already on the market in some other countries). The aim of this review is to critically describe the different approaches that are currently under development. Optimal coverage of prandial insulin requirements is the aim with both routes of insulin administration (at least with most approaches). The speed of onset of metabolic effect seen with some oral insulin approaches is rapid, but absorption appears to be lower when the tablet is taken immediately prior to a meal. With all approaches, considerable amounts of insulin have to be applied in order to induce therapeutically relevant increases in the metabolic effect because of the low relative biopotency of buccal insulin. Unfortunately, the number of publications about clinical–experimental and clinical studies is surprisingly low. In addition, there is no study published in which the variability of the metabolic effect induced (with and without a meal) was studied adequately. In summary, after the failure of inhaled insulin, oral insulin and buccal insulin are hot candidate Continue reading >>

How Is Chemotherapy Given?

How Is Chemotherapy Given?

Chemotherapy drugs can be given in a variety of different ways. The method of administration of chemo treatments along with the dose is determined by rigorous testing called clinical trials, which are done prior to the specific chemo drug being available for commercial use with patients. During this testing process, scientists and doctors determine how specific chemo drugs are absorbed in the body and how they work. Sometimes stomach juices can destroy different chemicals, making some medications impossible to give as a pill. Other substances are found to have better anti-cancer action if given intravenously (needle in the vein). Some medications can be given as an injection into the muscle and still others are absorbed when given directly into the bladder or the abdominal cavity. Oral Chemotherapy Medications (Taken by Mouth) Oral chemotherapy medications - those that can be swallowed - come in a variety of oral forms (pills, tablets, capsules, liquid), all of which can be absorbed by the stomach or under the tongue. Oral chemo medications that are swallowed are encased in a protective coating that is broken down by the digestive juices in the stomach. The stomach acids dissolve the coating releasing the medication, which is then absorbed through the lining of the stomach. Some therapy medications can be encased in different protective coatings which are released at different times in the system allowing for a time delay, called an extended release. This method allows longer periods of time between doses. Sub-lingual chemo medications are adsorbed under the tongue are referred to as sub-lingual. These medications are placed under the tongue where they dissolve and quickly absorb into the circulation of the body. This is a rapid way to have medication introduced into th Continue reading >>

Oral Arginine Does Not Stimulate An Increase In Insulin Concentration But Delays Glucose Disposal1,2,3

Oral Arginine Does Not Stimulate An Increase In Insulin Concentration But Delays Glucose Disposal1,2,3

Abstract Background: Ingested protein increases circulating insulin concentrations. Several years ago it was also determined that an intravenously administered mixture of 10 essential amino acids stimulated insulin secretion. Of these, arginine was the most potent. The effect was synergistic with administered glucose. Objective: Because the amounts of amino acid administered intravenously were very large and because ingested arginine is partially metabolized in the intestinal mucosa, we were interested in determining whether orally administered arginine stimulates a rise in circulating insulin concentration and whether arginine affects the glucose-induced rise in insulin concentration. Design: Nine healthy subjects (4 women and 5 men aged 21–52 y) ingested 1 mmol arginine/kg lean body mass, 1 mmol arginine/kg lean body mass + 25 g glucose, 25 g glucose alone, and water only, in random order on separate occasions, at 0800. Blood samples were obtained at baseline and at 10-min intervals over the next 2 h and were assayed for glucose, insulin, glucagon, and amino acid concentrations. The half-time for gastric emptying was determined by scintigraphy. Results: Unlike with intravenous administration, ingested arginine did not stimulate a rise in insulin concentration. The glucagon concentration was increased. Arginine attenuated and prolonged the glucose rise when it was ingested with glucose. Gastric emptying time was similar after ingestion of glucose alone or arginine plus glucose. Conclusion: Arginine, in an amount likely to be ingested in a high-protein meal, does not stimulate insulin secretion but attenuates the increase in glucose when given with glucose. INTRODUCTION It has been known for many years that ingestion of protein stimulates insulin secretion. In healthy Continue reading >>

Bioavailability Of Drugs

Bioavailability Of Drugs

Fraction of the dose of a drug contained in any dosage form that reaches the systemic circulation in unchanged or active form administered through any route is known as bioavailability. Drugs injected using intravenous route of administration have 100% bioavailability, while others have much less bioavailability, because: All of the drug may not be adsorbed Metabolism of the drug might occur before reaching the site of action Bioavailability = AUC (oral)/ AUC (I/V) x 100 Where AUC is the area under the curve X-axis represents time, while y-axis represents the plasma concentration. Bioavailability is the ratio of the area calculated for oral route of administration to the intravenous route of administration. It is determined by comparing the plasma levels of a drug after administration with plasma drug level achieved by I/V injection. Factors Affecting Bioavailability: 1. Route of administration Drugs given by intravenous route have 100% bioavailability. Exception includes prostaglandins, which are inactivated/metabolized in the lungs, therefore, their bioavailability may be zero after I/V injection. Those given by intramuscular route have bioavailability less than I/V route but more than subcutaneous route, while subcutaneous route has bioavailability more than the oral route. Only 10% of the dose of digoxin reaches systemic circulation after oral administration because of lack of absorption and bacterial metabolism within intestines. Even some of the drugs given by oral route may have 100% bioavailability but this is rare. By rectal route, half of the drug undergoes first pass metabolism. Chloramphenicol, an antibiotic, administered by intravenous route has bioavailability less than oral route because it is present in pro form and has to be activated in the intestines. Continue reading >>

Pharmacology: Why Some Drugs Could Not Be Taken Orally, Only As Muscular Or Venous Injections?

Pharmacology: Why Some Drugs Could Not Be Taken Orally, Only As Muscular Or Venous Injections?

Besides from the first pass metabolism mentioned by Arindam Chattopadhyay, for which we mostly can compensate by adjusting the dose taken by mouth, there are some other reasons: -some drugs will be destroyed in the stomach by the acid secreted, or digested, so can't be taken by mouth, e.g. insulin although some companies are developing ways to make this possible. The same is true for a lot of so called biologicals that inhibit Tumor necrosis factors used to modulate your immune system in e.g. rheumatoid arthritis, inflammatory bowel disease etc. -some drugs won't be absorbed from the bowels, so have to be injected. There's something known as first pass metabolism that happens when drugs are given orally. This occurs due to the liver. Some drugs when given orally will go extensive metabolism in the liver and hence cannot reach the Systemic circulation in adequate quantities. Thus, it's bioavailability decreases. Hence, it's action decreases due to decrease in its concentration. In order for the drug to reach Systemic circulation without any loss from first pass metabolism, they're given orally. Also, it takes time for drugs to be digested orally. Hence, they cannot be used in emergency. Hence the intramuscular and intravenous routes are preferred. Intravenous route of drug administration has 100% bioavailability. Since the medicine can only reach your blood stream through the injection route. If taken orally, the medicine maybe destroyed or not absorbed. There are some drugs that can be given both orally and through injection and is given through injection if needed to act fast or if the patient is not able to take orally Continue reading >>

Drug Administration

Drug Administration

Drugs are introduced into the body by several routes. They may be Given by injection into a vein (intravenously), into a muscle (intramuscularly), into the space around the spinal cord (intrathecally), or beneath the skin (subcutaneously) Placed under the tongue (sublingually) or between the gums and cheek (buccally) Placed in the eye (by the ocular route) or the ear (by the otic route) Sprayed into the nose and absorbed through the nasal membranes (nasally) Breathed into the lungs, usually through the mouth (by inhalation) or mouth and nose (by nebulization) Applied to the skin (cutaneously) for a local (topical) or bodywide (systemic) effect Delivered through the skin by a patch (transdermally) for a systemic effect Each route has specific purposes, advantages, and disadvantages. Oral route Many drugs can be administered orally as liquids, capsules, tablets, or chewable tablets. Because the oral route is the most convenient and usually the safest and least expensive, it is the one most often used. However, it has limitations because of the way a drug typically moves through the digestive tract. For drugs administered orally, absorption may begin in the mouth and stomach. However, most drugs are usually absorbed from the small intestine. The drug passes through the intestinal wall and travels to the liver before being transported via the bloodstream to its target site. The intestinal wall and liver chemically alter (metabolize) many drugs, decreasing the amount of drug reaching the bloodstream. Consequently, these drugs are often given in smaller doses when injected intravenously to produce the same effect. When a drug is taken orally, food and other drugs in the digestive tract may affect how much of and how fast the drug is absorbed. Thus, some drugs should be taken Continue reading >>

Insulin Administration

Insulin Administration

Insulin is a protein formed by two cross-linked peptide chains. Insulin is secreted in pulses by the pancreas and reaches the liver via the portal circulation. Some 80% of the insulin reaching the liver is cleared from the circulation, which means that insulin attains much higher concentrations in the liver than in the peripheral circulation. Insulin has a short plasma half-life (3-4 minutes), and choice of the route and timing of insulin administration is a major determinant of metabolic control. Conventional insulin injections are given into the thigh, abdomen or outer side of the buttock. Standard needles range from 0.8 - 1.6 cm in length, are used with a syringe or pen device and deliver insulin into the subcutaneous fat. Too long a needle or poor injection technique can result in injection into a muscle, which is painful and results in more rapid absorption of insulin. Many alternative routes of administration have been tested, but none can match direct injection or infusion. Subcutaneous insulin injection or infusion share the disadvantages of delivery into the systemic rather than portal circulation, and rates of appearance in the blood stream which are delayed and rendered somewhat erratic by the process of absorption from subcutaneous tissues. Characteristics of an ideal insulin administration system Nature has placed the pancreatic beta cell inside a digestive gland and astride an arterial supply that continuously samples the rate of nutrient absorption from the gut. It responds instantaneously to these blood-borne signals by releasing insulin in synchronised pulses, a pattern of secretion that maximises its effect on liver cells. Furthermore, it matches this insulin secretion with reciprocal suppression or release of its partner hormone pancreatic glucagon, t Continue reading >>

*half-life (plasma Half-life) (tâ½):

*half-life (plasma Half-life) (tâ½):

-The time required for the amount of drug to fall to 50% of an earlier measurement. -In 1st-order kinetic, (t½) is constant regardless of concentration. -(t½) is increased when the drug has high Vd, slow clearance and when there is high plasma –protein binding. -(t½) is not indicative of duration of action and dosing schedule in the fallowing cases: a-in drug which zero-order kinetic e.g. phenytoin b-in drug with active metabolites e.g. diazepam. c-hit and run drugs e.g. reserpine, organophospharous poisoning d-presence of renal or hepatic dysfunction. -(t½) is determined by volume of distribution(Vd) and clearance(CL) 0.693× Vd -(t½) = ------------------ (unit = time) CL -(t½) may be used to predict the manner in which plasma conc. alters in response to starting, altering or ceasing drug administ. *Steady-state concentration: - The condition in which the rate of drug elimination equals the rate of administration. -When a drug is given at a constant rate(continuous or intermittent) the time to reach the steady-state depends only on the (t½) and, for all practical purposes, after 5 (t½) the amount of drug in the body will be constant and the plasma concentration will be at a plateau. -Time to reach steady state for dobutamine((t½)=2 min) will be 10 min while for digoxin ((t½)= 36 hrs ) it will be more than 7.5 days. *Volume of distribution(apparent) (Vd): The ratio of the amount of drug in the body to the drug concentration in the plasma or blood. Amount of drug in the body Vd = ------------------------------------------ (unit=volume) Plasma drug concentration The calculated parameter for the Vd has no direct physical equivalent, therefore it is called apparent Vd. -Drugs with low Vd (e.g. insulin=15, gentamicin=18) are mainly ret Continue reading >>

About Insulin

About Insulin

What is this stuff I have to take? Is it a drug? Will it make me better, so I don't have to take it anymore? What does it do? Why can't I just drink it, or take a big shot once a month? And why are there so many different types? Will there ever be something better? Insulin is a hormone, normally produced in sufficient amounts by the healthy human pancreas. Its role is to facilitate the final digestion of glucose by the human body. When insulin is lacking (diabetes), glucose remains undigested in the blood. The body isn't being fed, and the high blood sugar can cause damage, the ramifications of diabetes. The two major types of diabetes (type 1 and type 2, IDDM and NIDDM) are separated by presence of insulin. The pancreas of the type 1 diabetic has ceased producing insulin, and insulin must be injected. This injected insulin is a replacement, and, barring the transplantation of a healthy pancreas, will need to be continued for life. The type 2 (NIDDM) diabetic has an impaired insulin supply. He or she doesn't have enough, or has some difficulty assimilating it (insulin resistance), or both. Lifestyle and diet changes, and oral medications, some of which stimulate the failing pancreas to produce more insulin, are used in treatment. Many veteran type 2 diabetics find their insulin supply, already impaired, has lessened to the point where they need to inject insulin. Insulin cannot be taken by mouth because it is digestible. Oral insulin would be obliterated in the stomach, long before it reached the bloodstream where it is needed. Once injected, it starts to work and is used up in a matter of hours. Depending on a number of factors, individuals vary insulin volume, type, and frequency, to optimize blood glucose management. That there are so many different formulations of i Continue reading >>

Diabetes Medication Misconceptions

Diabetes Medication Misconceptions

If you or a loved one has recently been diagnosed with type 1 or type 2 diabetes, you may have some questions about how the diseases are treated. There are many misconceptions about diabetes medications, mainly because the treatment for type 1 and type 2 diabetes can be very different. One of the most pervasive myths about diabetes--both forms of it--is that the disease can be treated by simply refining your diet or exercising more. While this is certainly an option for some people with type 2 diabetes, it is absolutely untrue for people with type 1. Type 1 diabetes is an auto-immune disease that occurs when the body’s disease fighting system, the immune system, destroys all your body's insulin-producing cells. Insulin is a vital agent that your body needs to convert food into energy. If your body is not producing insulin, you must take it by injection or a pump to live. Insulin currently cannot be taken by mouth because the digestive juices in your stomach and intestine will break down the insulin before it has a chance to get into your bloodstream to do its job. If you have type 2 diabetes, you may or may not have to take insulin injections, depending on a variety of factors. Contrary to popular belief, insulin injections are not for people with diabetes who have been "bad"—instead, taking insulin is a reflection of insulin production by the pancreas. People diagnosed with type 2 diabetes in general are still producing some insulin, although the amount they produce is not enough for their needs. Their cells may also be resistant to the effects of insulin, which makes them require more insulin than a person who does not have diabetes. Frequently when type 2 diabetes is diagnosed, weight loss, exercise, and changes in how much you eat can bring blood glucose levels Continue reading >>

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