Andriol Testocaps re-examined
If someone asks a question on a bodybuilding discussion forum about Andriol (Testosterone Undecanoate) most of the time members chime in and answer the same stereotype answers that where valid some years ago. About Andriol being a poor choice due to poor absorption rate and therefore has a low bioavalability. It is expensive etc etc.
Testosterone undecanoate has been available on the market for more than 20 years. Andriol capsules are available in more than 80 countries worldwide, but not in the USA. This should actually show that it has much potential. Also for bodybuildersit has a lot of uses like in bridging, cycling, PCT, HRT/TRT, anti-aging etc. More of that later.
Given Testosterone Undecanoate’s “age,” there would be little financial incentive to market the drug in the United States, as any generic manufacturer (foreign or domestic) could introduce a cheaper version, negating any potential for profit. Thus, it is unlikely that Testosterone Undecanoate will enter the United States market in the near future.
This testosterone ester is used worldwide for oral treatment of male hypogonadism. So far, testosterone undecanoate has been dissolved in oleic acid, leading to inconvenient storage conditions. Since the year 2003 it is available in a new formulation with castor oil and propylene glycol laurate instead of oleic acid, thus improving storage conditions markedly (stable at room temperature for approximately 3 years).
Pharmacokinetic and pharmacodynamic studies have demonstrated bioequivalence of the old and the new formulation of testosterone undecanoate. Therefore, the results of studies that were performed with the old formulation can be transferred to the clinical use of the new formulation.
Controlled studies have shown its efficacy in the treatment of symptoms associated with reduced serum testosterone levels. In these cases testosterone undecanoate improves bone mineral density, quality of life, muscle mass, libido and mood. Further studies will help evaluate the efficacy and safety of the new formulation in the treatment of elderly men with late-onset hypogonadism.
Effect of food
A study published in 2003 first reported the need for taking TU with a fatty meal, showing 16 times maximal concentration when taken with a meal that had 23 grams of fat.
A study in 2007 compared meals of varying fat content and demonstrated that near-maximal benefit was achieved with a meal containing 19 grams of fat and that increasing the fat content to 44 grams did not provide sufficient benefit to recommend higher fat intake. So far, the “take-home message” from this study was that the maximal delivery of TU is attained when the drug is taken with a meal containing roughly 20 grams of fat, or more. This effect was first noted in 1987, but sadly follow-up was delayed for more than a decade.
A study in 2012 investigated the effect of dietary fat on the testosterone (T) pharmacokinetics in hypogonadal men following administration of a self-emulsifying capsule formulation of oral T undecanoate (TU). In an open-label, 2-center, 5-way crossover study, a single oral dose of TU containing 300-mg equivalents of T (maximum anticipated human dose per administration) was administered to 16 hypogonadal men with a washout period of at least 5 days between doses. All participants were randomized to receive the TU capsules fasting or 30 minutes after an approximately 800-calorie meal containing 10%, 20%, 30%, or 50% fat. Serial blood samples were collected from 2 hours predose to 25 hours postdose to determine serum T and dihydrotestosterone (DHT) by liquid chromatography tandem mass spectrometry. Administering TU with a meal increased serum T concentrations, with the magnitude of the increase being directly dependent on the amount of fat in the meal. Average and peak serum T concentrations and area under the curve increased as the fat content of the meal was increased. Neither the high-fat meal (50% fat) nor the lower-fat meal (20% fat) showed a significant food effect relative to the normal-fat (Western diet) meal (30% fat). However, administering TU while fasting resulted in 50% or less of the cumulative exposure obtained when administered with 20%- to 50%-fat meals (albeit still substantial). A very-low-fat meal (10% fat) showed a significant food effect relative to the normal meal, but still exceeded the fasting condition by approximately 50%. Serum DHT concentrations showed corresponding increases to the serum T. As expected with the maximum anticipated clinical dose of TU (300 mg T), oral administration of this new formulation with food containing 20% to 50% dietary fat produced T levels at or above the upper range of adult men, and T levels trended higher as dietary fat content increased. Only with a very-low-fat diet (10%) or in a fasted state did a clinically significant food effect occur, but even then sufficient TU was absorbed with the self-emulsifying TU formulation to produce average serum T concentration predicted to be in the normal reference range (10 to 35 nmol/L).
However, there is another nugget in the body of TU research worth noting.
Oral TU does increase testosterone effectively, but a greater relative increase in DHT, the androgenic metabolite of testosterone, is seen. This suggests that men who are prone to prostate enlargement or hair loss may wish to avoid using TU. 5α-reductase inhibitors may be somewhat useful with this drug as well, as much of the conversion appears to take place in the gut or during absorption.
Doping
Victor Conte from Balco Labs said: “The use of designer drugs is significantly lower now because they [Wada] have changed the rules and now, if they find anything related in structure [to another illegal substance], even if they don’t know what it is, they can call it a positive test,” “So now people are doing it with fast-acting testosterone. They can use, for example, testosterone undecanoate; a lot of athletes are doing it in Italy, it’s freely available in Mexico.
You take these pills – typically 40 milligrams each – three or four times a day and you need to duck and dive for only a short time because they clear the system in four days. So you can do very intense weight training for just a couple of weeks and significantly enhance your explosive strength.
This business of “ducking and diving” is where Conte believes the system is beatable. “I don’t consider in-competition testing to even be dope-testing,” he said. “I call that IQ-testing. If you are dumb enough to be caught in a competition, then you are mentally retarded. It’s during the off-season that athletes do their real weight training. That’s where the doping problem has always been.”
Synergism with Tamoxifen Citrate (Nolvadex)
Nolvadex is suitable to restore endogenous (body-own) release of LH and FSH after a cycle. Nolvadex can block receptors in the brain glands normally signaling high circulating estradiol levels. A high estradiol level is a signal to your body to stop endogenous testosterone production. If the receptors for estradiol are blocked, the pituitary gland increases the production of the hormones LH and FSH.
Therefore, Greek endocrinologists discovered, your body does not reduce the production of endogenous testosterone if you combine 3 times 40 milligrams Andriol daily, with 10 mg Nolvadex twice daily. Even after three months, the natural production of testosterone did not decrease.
An empiric treatment for idiopathic oligozoospermia revisited: a 20-year investigative saga
E. Koukkou et all 2012
A series of studies aiming at introducing an effective treatment for idiopathic oligozoospermia was conducted in a step-wise fashion spanning over a 20-year period. The concept was that co-administration of an accessory gland-stimulating androgen, testosterone undecanoate (40 mg t.i.d.) and the FSH raising anti-oestrogen tamoxifen citrate (10 mg b.i.d.) may improve sperm parameters.
A prerequisite for such an effect was the demonstration that testosterone undecanoate had no suppressing action on pituitary-testicular axis. In this context, initial studies demonstrated no change in basal or stimulated gonadotrophin and testosterone secretion in short- or long-term protocols. Two subsequent trials with this combination showed a marked improvement of sperm parameters and pregnancy incidence, with a seasonal variation noted in response to treatment, this being higher during the cold seasons of autumn and winter. Regarding the mechanism of testosterone undecanoate's action, a recent study from our unit showed that its administration resulted in a marked rise of serum DHT levels. Because this steroid is an epididymal function promoter, it appears that its contribution in the combination is mediated mainly through its DHT raising effect. By and large, this empiric approach for the treatment of idiopathic oligozoospermia was satisfactorily documented after a 20-year investigative saga.
Oral testosterone undecanoate supplement therapy improves the quality of life for men with testosterone deficiency
Park et all 2003
In a single-blind, placebo-controlled study, the effects of a 3-month oral administration of 160 mg/day testosterone undecanoate (Andriol®) on the quality of life of men with testosterone deficiency were evaluated. The subjects included ten men with primary hypogonadism and 29 with andropause with sexual dysfunction as the most common problem. The changes in subjective symptoms were evaluated by the PNUH QoL scoring system and the St. Louis University Questionnaire for androgen deficiency in aging males (ADAM). Digital rectal examination (DRE) was performed and serum testosterone, prostate-specific antigen (PSA) and liver profile were monitored. Testosterone undecanoate treatment (n = 33) significantly improved sexual dysfunction and symptom scores of metabolic, cardiopulmonary, musculo-skeletal and gastrointestinal functions compared to baseline and to placebo. ADAM score also significantly improved after 3 months of treatment.
Additional testosterone undecanoate is also supplemented to postmenopausal women and showed to improve female sexual function and overall quality of life.
Dosing
There is much controversy about Andriols potency and usefulness for Bodybuilding , the same controversy is seen about dosing and stacking. It’s used for bridging between cycles, in PCT , anti-aging, TRT/HRT, as doping in baseball (Mexican beans) cycling, sprinters etc. And even a pro like Milos Sarcev said he used them in cycling. I could give you my opinion on Andriols use and dosing, but it is exactly as with all other steroidal compounds, some people like it others don’t, some use 500 mg/week other believe you need at least 3 gram. So I’ll give you some quotes I gathered from the net, like by example here: //forums.steroid.com/anabolic-steroids-questions-answers/247014-andriol.html And anyone’s opinion is as good as mine..
“What can I say, I will never use another type of test in a cutting cycle, only andriol. I never look for big results in cycles, the problem is many people on this board want to gain 25 pounds and over per cycle so andriol is not ideal. So many places sell andriol for our use, you must ask why? Well we have a huge market for this drug ,but usually in Different circles, like the dude today who broke the 100 meter record, many rugby players use it, as it`s the best test to beat drug tests. It`s funny how the people on this board that diss this drug have no Experience with it (parrots) or if they have used it they have used it incorrectly. I`m not saying it`s for everyone, but if you respond well it`s a Magical drug.”
“Friend of mine is on deca and andriol and is getting good results and hasn't seen any sides, except some zits.
You guys are all way off and wrong on the Andriol, it's great stuff, I have extensive experience with it in several cycles..it's a great alternative to eod prop shots. “
“They changed the formulation about 2 years ago, All you guys are still reading about the poorly absorbed Andriol caps. The new ones absorb must better, though MUST BE TAKEN WITH FOOD. I am using 3 a day and feel fucking amazing on them, don't expect them to hit you like Sust or Test E , but to include in a nice cutter summer cycle to keep your sex drive good, they are fucking GREAT, legit human grade Organon. I take mine 3x a day split up into morning, lunch and dinner.”
“Make sure to take it with food, you will be happy with the results. It even says on top of the box that they used to have a poor absorption rate so Organon modified the formula for them. I love them, esp. since my health insurance covers them and I get a box of 120 caps for about $20 “
“Just want to update. I'm on my 4th day of andriol (in week day I take 4caps in morning and 3 evening ; during week end I take only 3 caps in the morning).”
“I feel really good, I went to the gym and I exploded I know it's expensive but as I know it's from pharmacy I don't mind to pay more.”
“Andriol is a great drug if it used correctly, I’ve used it many times and I just love the feeling on this drug I can’t say enough about it how it makes you feel, the dose is an individual thing but normally the dose would be high, there are no side effects only positives ones, it’s very underrated on this board but i feel that is because some don't know how to use it correctly.”
“ I’ve used it to cut and bulk and either way it’s a very good compound to have within a cycle, hardness/strength/size are the results what I receive from Andriol.”
“I would advise any serious BB to try it and see if it works for them because when it does the results are amazing without any sides, There were studies done in England regarding Andriol and it came out on top for test replacement no other test came near it, no sides only benefits, but you must learn how to use it correctly IE dose and other compounds to get the whole benefit from Andriol.”
PCT
“….it boils down to this:
if u were going to do a bridge which compound would be best to do it with between:
anavar 10mg first thing in morning
dianabol 10mg first thing in morning
andriol testocaps 80mg first thing in morning
From my reading I think that dianabol has the advantage of having a 4hr 1/2 life and it’s also very anti catabolic. I know that anavars 1/2 life is 9hrs which means it might not be well suited for this purpose. On the other hand andriol testocaps have the shortest 1/2 life of all but im not sure how anti catabolic they would be. I assume taking two caps a day would be roughly equivalent to what my body should be producing naturally anyway so it shouldn't suppress. “
“…see a lot of people saying Andriol is ineffective and is a waste. I myself have done a cycle with Proviron, (yes i dont like injectables). With the proviron added to my cycle it allowed all test to remain free flowing and it takes aromatazation into Estrogen out of the picture.
“I was able to get nice gains with 240mg. Andriol and 75mg Proviron per day. I gained 18 pounds in a 40 day cycle with 1-1/4" arm growth, bench went up 45 lbs. this is a nice cycle to me. Any thoughts anyone”
“DADAWG, why would you call bull shit, i was 190 when i started the cycle. The proviron keeps all of the andriol as free flowing test and does not let it aromatize at all. This is a great oral as long as you do your research, it has to be taken with meals for max absorption due to the fact that it absorbes through the small intestines. If one does their homework they can make this a great option, obviously you need to keep your diet in check and train tough as with any cycle. This stuff is great as far as I’m concerned!”
Nanostructured lipid carriers (NLC)
Does that mean that after 20 years we finally know how to work with ANDRIOL TESTOCAPS? Nope companies see so much potential in oral TU that they experiment with nanostructured lipid carriers (NLC) and Testosterone was used as a nanocrystal formulation.
“Due to the low solubility of TU in the oil a single dose of 80 mg has to be administered in two capsules. Each Andriol Testocaps® capsule contains a total amount of 335 mg TU solution. Taking two capsules is not very convenient for the patient and reduces compliance. Therefore the aim was to develop a formulation which allows administration in a single oral unit.
The approach taken was to incorporate TU into nanostructured lipid carriers (NLC). NLC are lipid nanoparticles made from a blend of a solid lipid and a liquid lipid (oil) which is solid at body temperature Another promising approach to increase the oral bioavailability of poorly soluble drugs are drug nanocrystals
To avoid administration of a single dose in two oral units and to increase lymphatic absorption to minimise side effects in the liver, TU was incorporated into nanostructured lipid carriers (NLC) and formulated as drug nanocrystals. Testosterone (T) was run as nanocrystal formulation for reasons of comparison. NLC and drug nanocrystals were produced by high pressure homogenisation. The in vivo studies were performed in male Wistar rats. The drug absorbed was quantified as testosterone analysed by EIA assay. The nanocarriers were compared with the commercial product Andriol Testocaps®. The drug nanocrystals reached about half the AUC of Andriol Testocaps® (testosterone) or were just below (testosterone undecanoate). The best NLC formulations possessed a 2 times higher AUC compared to Andriol Testocaps®.”