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Chondroprotectors:

Chondroprotectors:

WHAT ARE THESE?

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Glucosamine

Glucosamine is an amino-nosaccharide. Glucosamine is a universal precursor and building block of all necessary joint lubricants and tissue dampers, which are known as glucosaminoglycans, including hyaluronic acid and chondroitin sulfate, and the proteoglycans that are formed from them. In the body, glucosamine is used by chondrocytes as the starting material for the synthesis of proteoglycans, glycosaminoglycans and hyaluronic acid - components of the cartilage tissue of the joint. About 30% of the administered glucosamine are in the connective tissue for a long time. By the way, healthy connective tissue is not only the health of the joints, but also of the blood vessels, skin and internal organs, the “skeletons” of which are also built from connective tissue.

Sources of production and types of glucosamine

Glucosamine hydrochloride (HCL) of plant origin. This form of glucosamine is made from corn husks. The raw materials are ground and fermented. As a result of this process, glucosamine hydrochloride is obtained in very high purity. It does not contain animal protein, which can cause allergies. This form of glucosamine is currently the best, but has a higher cost.

Glucosamine hydrochloride (HCL) of animal origin. It is made from chitin (shell) of crustacean mollusks (crabs, shrimps, lobsters, crayfish, lobsters) by chemical reaction. This form of glucosamine is the most available. Its disadvantage is that this glucosamine can cause allergic reactions in people who are allergic to seafood.

Glucosamine sulfate (stabilized 2KCl). Glucosamine sulfate is not as stable when produced, therefore it is required to stabilize it with other auxiliary substances. It is also made from crustacean chitin and stabilized by potassium chloride. This form is well tolerated and has good bioavailability.

Glucosamine sulfate (stabilized with NaCl). This form of glucosamine is stabilized by sodium chloride, the common table salt. This form also has good bioavailability and is well absorbed by the body. But the use of glucosamine sulfate, stabilized with sodium chloride, has its own important features. When taking 1500 mg per day of glucosamine sulfate, stabilized with sodium chloride, a person receives up to 400 mg (25% by weight) of salt. However, the daily intake of salt is just 400 mg. But the man still gets salt with food. It turns out its excess. This is unacceptable in the treatment of hypertensive patients. For people leading a healthy lifestyle, working on weight loss or exercising heavily, excess salt is also harmful: salt causes water retention in the body. Thus, the use of glucosamine sulfate, stabilized with sodium chloride, is undesirable - especially during long courses of treatment. Better preparations of glucosamine sulfate stabilized with potassium chloride (2KCL) or glucosamine hydrochloride in general. In addition, glucosamine hydrochloride is cheaper than glucosamine sulfate.

N-acetyl-glucosamine or N-acetyl-D-glucosamine (NAG). Glucosamine taken from the outside is converted into N-acetyl-glucosamine by special cells in the intestine. N-acetyl-glucosamine is a structural unit of glycosaminoglycans, components of the intercellular matrix. In production, it is obtained from the same sources - crustaceans. N-acetyl-glucosamine (NAG) is an amino sugar, a natural structural component of hyaluronic acid, which is present in all tissues of our body. In the course of complex reactions, N-acetyl-glucosamine is obtained by combining glucosamine and acetic acid. That is, taking glucosamine together with N-acetyl-glucosamine, we stimulate not only the regeneration of cartilage tissue and get anti-inflammatory and analgesic effect, but also stimulate the production of one of the main components of the joint fluid - hyaluronic acid.

This is a very difficult level of reactions occurring in our body. Scientists on this issue is not all clear. In some cases, this form of glucosamine manifests itself, in others it does not. There are studies, and manufacturers themselves say this: this form of glucosamine has worse digestibility, but better tolerability.

The N-acetyl-glucosamine form contains 81% pure glucosamine. This gives the false impression that this form is better than glucosamine sulfate, but N-acetyl-glucosamine is metabolized differently than other forms of glucosamine. Instead of being absorbed relatively intact, intestinal bacteria quickly digest N-acetyl-glucosamine, and other tissues of the gastrointestinal tract absorb a large part of it before it reaches cartilage. There are studies showing positive effects of N-acetyl-glucosamine. He is involved in the production of hyaluronic acid and helps with intestinal inflammation. But, in general, the need to take this form of glucosamine, especially if it affects the price of the acquired dietary supplement, remains a point of contention.

Poly N-acetyl-glucosamine (Poly NAG). The most expensive and least effective form of glucosamine.

Which glucosamine is better?

In principle, chloride or sulphate is attached to glucosamine - does not matter. Glucosamine remains glucosamine. A number of studies were conducted with various forms of glucosamine, and it was found that with an equal number of different forms of glucosamine in dietary supplements, their effect on the effectiveness is the same. But the subtleties of use are still there, and they depend precisely on the substances “attached” to glucosamine.

Glucosamine sulfate and glucosamine hydrochloride of animal origin are obtained from chinite of marine crustaceans (shrimps, crabs and lobsters). The main world supplier of raw materials today are the farms of the South China Sea. And it is no secret to anyone that for faster growth of crustaceans, hormonal feed additives are used. For example, the United Kingdom a few years ago banned the import of crustacean products from China due to the large amount of hormones in them.

Today, it is technically impossible to remove all ballast substances from the raw materials. But the chemical purity of glucosamine may still differ depending on the manufacturer, the technology used by it, its decency and other factors. Therefore, it is not glucosamine itself, but excipients and seafood components remaining during production that can cause allergic reactions. It must be said that the research also did not confirm, but did not disprove the possibility of allergic reactions. So if you have a strong allergy to seafood, you must be careful and choose the right dietary supplement for yourself.

Difference between glucosamine sulfate and glucosamine hydrochloride

Glucosamine hydrochloride usually contains about 83-88% pure glucosamine, and glucosamine sulfate contains only 59-65% pure glucosamine; everything else is auxiliary substances.

Research has shown that, when taken orally, glucosamine is well absorbed, but some of it is still lost in our digestive system. The uptake of glucosamine sulfate - up to 80%, glucosamine hydrochloride - up to 95% due to better solubility. That is, the final goal - the joints, reaches a maximum of 83% of glucosamine from the administered glucosamine hydrochloride and 52% of the accepted glucosamine sulfate.

Glucosamine hydrochloride (HCL) is a stable compound. Glucosamine sulfate, requires stabilization with potassium chloride (2KCl) or sodium chloride (NaCl). Both forms have good bioavailability.

Today, manufacturers offer supplements that contain glucosamine hydrochloride and N-acetyl glucosamine (NAG) in its pure form, without containing additional stabilizing impurities in the form of salts. But it was found that in the process of biosynthesis occurring in our body, glucosamine hydrochloride and N-acetyl-D-glucosamine are used differently than other sulfate forms of glucosamine. Glucosamine hydrochloride and N-acetyl-glucosamine are selectively taken up by the cells of the liver and other body tissues, after which glucosamine is used to build new proteins, and only a smaller part gets into the cartilage tissue. At the same time, their use is still justified, since these forms contain more pure glucosamine (up to 88%), and the BAA does not contain sodium salt.

Forms of glucosamine in descending order of utility, digestibility, safety, and efficacy

Glucosamine hydrochloride of plant origin

Glucosamine hydrochloride of animal origin

Glucosamine sulfate, stabilized with potassium chloride (2KCl)

N-acetyl-D-glucosamine (NAG)

Glucosamine sulfate stabilized with sodium chloride (NaCl)

Poly N-acetyl-glucosamine (Poly NAG)

The clinical efficacy of glucosamine in arthrosis

Short-term use of glucosamine - up to 3 months

The clinical efficacy of glucosamine in osteoarthritis can be compared with the use of nonsteroidal anti-inflammatory drugs (NSAIDs). With a short course of treatment during the first 2 weeks, the severity of symptoms of arthrosis decreased faster in the group of patients receiving ibuprofen. At the end of the course, there was no difference in the groups treated with glucosamine and ibuprofen. In other studies, pain reduction with short-term use of glucosamine even exceeded the performance of the ibuprofen group. In all cases, glucosamine was easier tolerated by patients and had fewer side effects than NSAIDs.

A clinical comparison was made of the efficacy of glucosamine and MSM, a popular combination of foreign combined chondroprotectors. MSM is a naturally occurring form of sulfur with some anti-inflammatory and analgesic effects. The combined use of glucosamine with MSM led to a significant reduction in pain syndromes in arthrosis compared with the isolated use of glucosamine. Puffiness decreased equally in all groups.

Long-term use of glucosamine - up to 3 years

With prolonged use in osteoarthritis, glucosamine prevents the progression of manifestations of arthrosis, detected radiologically (the size of the inter-articular interval), reduces the severity of pain, increases the mobility of the affected joint.

The combination of glucosamine sulfate and ibuprofen has a synergistic interaction, with the result that the pain syndrome is stopped at a lower dose of ibuprofen (the analgesic effect provides a 2.4 times lower dose of ibuprofen).

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Chondroitin

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Chondroitin, a structural analogue of human cartilage tissue, is obtained from the cartilage and bone tissue of farm animals, bones and cartilage tissue of fish. Among sharks, the most valuable food is the prickly shark, or the katran, the stingrays. Also, cartilaginous tissue for the isolation of chondroitin sulfates is learned when cutting sturgeon. Chondroitin sulfate isolated from animal cartilage and bone cartilage has a lower biological activity. The antiprotease activity of shark cartilage components, for example, is 100 times higher than that of cattle. Glycosaminoglycans maintain the elasticity of cartilage tissue and contribute to its hydrophobicity.

The mechanism of action of chondroitin

Chondroitin sulfate has anti-inflammatory effect, stimulates the development of cartilage cells - chondrocytes and the synthesis of proteoglycans. Chondroitin sulfate activates the synthesis of hyaluronic acid, prolongs the life of chondrocytes and normalizes the structure of the subchondral bone. The effect of chondroitin sulfate in the intensification of hyaline cartilage repair has also been proven. Chondroitin sulfate contributes to a better penetration of glucosamine into the inflamed joints (therefore, in particular, it is better to use the combined BAA of chondroitin + glucosamine, even better in combination with MSM sulfur, which has anti-inflammatory and anti-edema effects).

Interesting fact. With oral administration of chondroitin sulfate, its bioavailability is 13%, while for external use it increases to 20–40%. This fact makes it relevant to include chondroitin sulfate (ointments, creams, gels) into the complex treatment of external preparations.

Sources of production and types of chondroitin

Chondroitin is naturally found in the skin, tendons, bone marrow, and animal cartilage. Chondroitin is even more abundant and in more bioavailable form in fish (especially salmon, salmon, prickly shark or quatre, stingrays, sturgeon).

Chondroitin has different names:

- Chondroitin sulfate (Chondroitin sulfate) - an international name;

- Chondroitin sodium sulfate is the full chemical name, as the structure is a sodium salt.

- Chondroitin-4-sulfate - is extracted mainly from the tissues of mammals (trachea or bull cartilage).

- Chondroitin-6-sulfate - is extracted mainly from shark cartilage.

Chondroitin is harvested by extracting the active substance from cattle trachea, pigs and shark cartilage or sturgeon. Depending on this, chondroitin sulfate is different and has different molecular weight, bioavailability and purity.

Chondroitin sulfate, isolated from fish cartilage, has a higher biological activity. Studies have shown that the activity of the components of shark cartilage is 100 times higher than that of cattle. Therefore, this type of chondroitin sulfate is preferable.

Clinical efficacy of chondroitin sulfate

With a one year course, chondroitin sulfate in patients significantly improves joint mobility (up to 50%), reduces the severity of pain syndrome and stabilizes radiological indicators (the size of the inter-articular gap and the total thickness of the cartilage plate). A decrease in the severity of pain and an increase in the range of motion occur as early as the third month of treatment and significantly increase in the sixth and twelfth month since the beginning of the course of treatment with chondroitin sulfate.

When comparing the clinical efficacy of NSAIDs (diclofenac) and chondroitin sulfate during a 6-month course of treatment of osteoarthritis, it turned out that pain syndrome in patients treated with diclofenac disappeared faster compared to the group of patients treated with chronitin sulfate. However, after the withdrawal of diclofenac followed by a rapid recurrence of pain. In the group receiving chondroitin sulfate, the clinical effect occurred later, but lasted another three months after discontinuation of the drug. Also, chondroitin sulfate has an antithrombotic heparin-like effect, reduces cholesterol and lipoproteins in the blood, which makes it an important component of the complex of products for overweight patients.

Daily doses of glucosamine and chondroitin

During sports training or at the beginning of arthrosis treatment, in the absence of allergic reactions and other side effects, the dose for the first 1-2 months is set to 2000-2500 mg (only for glucosamine without the content of salt, otherwise it will exceed its allowable daily intake). The maximum safe dose is 3000 mg per day.

Maintenance dose of glucosamine is 1000-1500 mg per day.

When taking glucosamine sulfate stabilized with sodium chloride from the diet is required to exclude table salt.

Chondroitin sulfate is administered in a dose of 200-400 mg twice or three times a day, or 800-1200 mg once a day. Increasing the dose to 2000 mg has the same clinical effect as the dose of 1200 mg.

The duration of admission must be at least 3 months. Long - up to 3 years - therapy with chondroprotectors gives the best results. According to clinical indications, an intermittent treatment regimen may be justified: 3-4 months of admission with a break of 2-2.5 months, that is, glucosamine and chondroitin sulfate are recommended to be taken approximately 150 days a year for 3-5 years.

If you decide to take longer and more of these substances, you should probably consult with an experienced doctor or nutraceutical. It is better not to do without consultation and with overweight, disorders of the kidneys and other diseases

There is a way to calculate the dosage of the drug for yourself more accurately. This method is proposed by Dr. Jason Theodosakis. He conducted trials of drugs and doses in more than six hundred patients and suggested dosage depending on body weight.

1. With a weight of less than 55 kg, a dosage of 1000 mg of glucosamine and 800 mg of chondroitin is sufficient for daily intake.

2. With a weight of 55 to 90 kg, the dosage is 1500 mg of glucosamine and 1200 mg of chondroitin.

3. With a weight of more than 90 kg, 2000 mg of glucosamine and 1600 mg of chondroitin per day are recommended. If you have great physical exertion, this will be the standard norm. If there are no loads, then this option will be considered a therapeutic dose.

The daily dose should be divided by 2-3 times and taken during the day.

Forms of use of chondroprotective supplements in decreasing order of time of their digestibility and convenience of reception

Gel capsules. The best combination of liquid absorption and capsule convenience. They contain active substances in gel-form fast absorbable form. Convenient to use, their soft smooth surface makes it easy to swallow with water. Possess high bioavailability. Easily absorbed by people with sensitive digestive system, do not irritate the gastrointestinal tract, as dissolved in the intestine.

Liquid. Although the liquid form has the best absorption in the stomach, it is inconvenient to transport and store, it is difficult to calculate the dose, it must be stored in the refrigerator.

Capsules This is the most common and most convenient form. Powder is placed in capsules. It is convenient to store, take, calculate the required dose of the substance and transport.

Powder. This form is not very convenient to store and take. But it is absorbed by the body well. Naturally, slightly worse than the liquid form.

Tablets. This dietary supplement from the pressed substance. Tablets are easy to take, transport and store. But they are worst absorbed by the body, because they need more and dissolve.

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Side effects and contraindications of glucosamine and chondroitin

Among the side effects of taking glucosamine may be: allergic reactions, increased flatulence, thinning of the stool, increased insulin tolerance.

When taking large doses of chondroitin sulfate may cause nausea. Chondroitin sulfate can reduce blood clotting. Also possible are headache, stiffness of movements, skin reactions, photophobia, diarrhea and constipation, increased sweating, hair loss and high blood pressure, a theoretical increase in the risk of bleeding (due to the heparin-like effect).

At the same time, glucosamine and chondroitin, in fact, are simple sugars. Both are natural products found in humans and mammals. They are part of the food. The only problem is that dietary supplements contain additional pollutants that are completely technically impossible to get rid of. Their amount in the dietary supplement depends on the manufacturer and the processing technologies and the necessary substances available to it. These substances can cause allergic reactions.

Chondroprotectors are not recommended for pregnant and nursing mothers and children under 15 years of age, due to lack of research.

There are individual characteristics of the organism in terms of sensitivity to any substances, or the presence of chronic diseases in which it is necessary to observe strict nutritional principles (diseases of the kidneys, liver, prostate gland, diabetes mellitus).

Chondroitin can slightly thin the blood. Therefore, if you are taking special blood-thinning drugs, this must be borne in mind in order to avoid bleeding.

Studies have been conducted on the effect of glucosamine on pancreatic cells and, accordingly, an increase in the risk of diabetes. Studies have shown that there is some impact, however, it was tested on animals, and the dose of maximum consumption was increased 6-7 times from the norm. But people with diabetes are advised to carefully monitor their sugar levels when using chondroprotective supplements.

It has been proven that long-term use of glucosamine is 1000–4000 times safer than taking conventional nonsteroidal anti-inflammatory drugs (NSAIDs) prescribed for osteoarthritis, arthrosis, and other diseases. When co-administered with other drugs, glucosamine and chondroitin do not interact.

Individual characteristics of the body can also affect the digestibility of supplements of glucosamine and chondroitin. Without movement, nothing will penetrate the cartilage. Consumption of dietary supplements is justified only if the principles of a healthy lifestyle and nutrition, healthy functioning of all body systems and organs are observed. In order for supplements to work, you need adequate water intake, a varied and nutritious diet, movement.

Features of the combined drugs chondroitin sulfate and glucosamine

The advantages of combined chondroprotectors over monodrugs are confirmed in experimental and clinical studies. For example, glucosamine in the experiment on rabbits increased the production of glucose aminoglycans by 32% compared with the control group, chondroitin - by 32%, and the combination of chondroitin and glucosamine - by 97%. The combination of glucosamine and chondroitin sulfate more effectively slows down the process of degenerative changes in the joints than the action of these substances separately, stops the destruction of cartilage. Treatment is accompanied by a decrease in pain, preservation or improvement of the function of the joints, which allows to reduce the dose of NSAIDs or to refuse to take them.

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