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Purpose: The objective of this study was to evaluate the thermal behavior of crystalline and amorphous bisoprolol fumarate and its compatibility with amorphous valsartan. This pharmacologically relevant drug combination is a potential candidate for fixed-dose combination formulation. Methods: DSC and TMDSC were used to examine thermal behavior of bisoprolol fumarate. SSNMR and XRPD were applied to probe the solid state forms. The thermal behavior of physical mixtures with different concentrations of bisoprolol and valsartan were examined by DSC and TMDSC, and the observed interactions were investigated by XRPD, solution- and solid-state NMR. Results: The phase transitions from thermal methods and solid-state NMR spectra of crystalline and amorphous bisoprolol fumarate are reported.Bisoprolol
Strong interactions between bisoprolol fumarate and valsartan were observed above 60 C, resulting in the formation of a new amorphous material. Solution- and solid-state NMR provided insight into the molecular nature of the incompatibility. Conclusions: A combined analysis of thermal methods, solution- and solid-state NMR and XRPD experiments allowed the investigation of the conformational and dynamic properties of bisoprolol fumarate. Since bisoprolol fumarate and valsartan react to form a new amorphous product, formulation of a fixed-dose combination would require separate reservoirs for bisoprolol and valsartan to prevent interactions. Similar problems might be expected with other excipients or APIs containing carboxylic groups.
Bisoprolol fumarate has a molecular weight of 766.97. It is a white crystalline powder which is approximately equally hydrophilic and lipophilic, and is readily soluble in water, methanol, ethanol, and chloroform.
Bisoprolol Fumarate Tablets, USP is available as 5 and 10 mg tablets for oral administration.
Inactive ingredients include colloidal silicon dioxide, partially pregelatinized starch, crospovidone, anhydrous dibasic calcium phosphate, hypromellose, magnesium stearate, microcrystalline cellulose, polyethylene glycol, titanium dioxide and talc.
Bisoprolol fumarate is a beta1-selective (cardioselective) adrenoceptor blocking agent without significant membrane stabilizing activity or intrinsic sympathomimetic activity in its therapeutic dosage range. Cardioselectivity is not absolute, however, and at higher doses ( 20 mg) Bisoprolol fumarate also inhibits beta2-adrenoceptors, chiefly located in the bronchial and vascular musculature; to retain selectivity it is therefore important to use the lowest effective dose.
Pharmacokinetics and Metabolism
The absolute bioavailability after a 10 mg oral dose of Bisoprolol fumarate is about 80%. Absorption is not affected by the presence of food. The first pass metabolism of Bisoprolol fumarate is about 20%.
Binding to serum proteins is approximately 30%. Peak plasma concentrations occur within 2 to 4 hours of dosing with 5 to 20 mg, and mean peak values range from 16 ng/mL at 5 mg to 70 ng/mL at 20 mg. Once daily dosing with Bisoprolol fumarate results in less than twofold intersubject variation in peak plasma levels. The plasma elimination half-life is 9 to 12 hours and is slightly longer in elderly patients, in part because of decreased renal function in that population. Steady state is attained within 5 days of once daily dosing. In both young and elderly populations, plasma accumulation is low; the accumulation factor ranges from 1.1 to 1.3, and is what would be expected from the first order kinetics and once daily dosing. Plasma concentrations are proportional to the administered dose in the range of 5 to 20 mg. Pharmacokinetic characteristics of the two enantiomers are similar.
Bisoprolol fumarate is eliminated equally by renal and non-renal pathways with about 50% of the dose appearing unchanged in the urine and the remainder appearing in the form of inactive metabolites. In humans, the known metabolites are labile or have no known pharmacologic activity. Less than 2% of the dose is excreted in the feces. Bisoprolol fumarate is not metabolized by cytochrome P450 II D6 (debrisoquin hydroxylase).
In subjects with creatinine clearance less than 40 mL/min, the plasma half-life is increased approximately threefold compared to healthy subjects. In patients with cirrhosis of the liver, the elimination of Bisoprolol fumarate is more variable in rate and significantly slower than that in healthy subjects, with plasma half-life ranging from 8.3 to 21.7 hours.
How should I give it?
Furosemide and bumetanide come in liquid and tablet form. It is usually given 1 to 3 times a day. Your child should be awake and alert when taking any medicine. Follow the checked instructions below:β-agonist Powder
___ If using the liquid form, draw up the correct amount of medicine in the medicine dropper or a syringe. Give a small squirt of the medicine inside the cheek. To avoid choking, let your child swallow each squirt before giving more.
___ For babies, you may want to mix the medicine with a small amount of formula or breast milk and give it with a bottle nipple before a feeding. Do not add medicine to a whole bottle because if your baby does not finish it, you will not know how much of the medicine was taken.
___ For children who cannot swallow pills:
Crush it between 2 spoons, inside a plastic bag, or in folded paper.
Mix the powder with a very small amount (about 1 teaspoon) of soft food, such as applesauce, chocolate syrup, ice cream, jelly, or yogurt.Furosemide and bumetanide can be given with or without food or milk. These medicines can decrease the potassium level in the blood, so your child may need to have potassium blood tests.
Cas No.: 72956-09-3
Molecular Formula: C24H26N2O4
Molecular Weight: 406.48
Melting point: 113-117ºC
Density:1.25 g/cm3
Boiling Point: 655.2 °C at 760 mmHg
Flash Point: 350.1 °C
Appearance: white or almost white crystalline powder
Assay:98%min
Usage: Carvedilol powder is a non-selective beta blocker/alpha-1 blocker indicated in the treatment of mild to moderate congestive heart failure (CHF).
Carvedilol is a AR (α1 and β-adrenergic receptor) antagonist with antioxidant properties. Studies show that the receptors α1D-AR and α1B-AR have a greater affinity for Carvedilol in comparison to the receptor β1-AR subtype. Carvedilol has been observed to block the oscillatory intracellular calcium changes induced by α1D-AR and α1B-AR, and shown to have a higher oxidative effect than Atenolol (sc-204895). The S(-) enantiomer of Carvedilol acts as a β-blocker, and the R(+) and S (-) enantionmers both block the α1. Carvedilol is an inhibitor of α1B-AR, β1-AR, β2-AR and α1D-AR.
Celiprolol powder General Description Celiprolol powder is a medication in the class of beta blockers, used in the treatment of high blood pressure. It has a unique pharmacology: it is a selective β1 receptor antagonist, but a β2 receptor partial agonist. It is also a weak α2 receptor antagonist. Celiprolol powder is believed to provide clinical benefit for people with vascular Ehlers–Danlos syndrome by promoting normal collagen synthesis in the blood vessels, and by shifting the pressure load away from the vessels most prone to dissection and rupture. In 2019, a new drug application (NDA) for celiprolol was denied by the Food an the U.S. Food and Drug Administration (FDA), instead calling for an “adequate and well-controlled” trial to determine whether celiprolol reduced the risk of clinical events in patients with vEDS. Celiprolol is a vasoactive beta-1 selective adrenoceptor antagonist with partial beta-2 agonist activity. The beta-2 agonist activity is thought to account for its mild vasodilating properties. It lowers blood pressure in hypertensive patients at rest and on exercise. The effects on heart rate and cardiac output are dependent on the pre-existing background level of sympathetic tone. Under conditions of stress such as exercise, celiprolol attenuates chronotropic and inotropic responses to sympathetic stimulation. However, at rest minimal impairment of cardiac function is seen. Before you start the treatment, read the manufacturer’s printed information leaflet from inside the pack. It will give you more information about celiprolol and will provide you with a full list of the side-effects which you may experience from taking it. Take celiprolol exactly as your doctor tells you to. There are two strengths of tablet – 200 mg and 400 mg. It is usual to start by taking one 200 mg tablet daily, although your doctor may later increase this to the 400 mg strength tablet. You should take the tablet first thing in the morning, preferably ‘on an empty stomach’. This means that you should take the tablet at least 30 minutes before you have breakfast, or wait until two hours after you have eaten. Swallow the Celiprolol: A Unique Selective Adrenoceptor Modulator. Celiprolol is a β-blocker with a unique pharmacologic profile: it is a β1-andrenoceptor antagonist with partial β2 agonist activity. Given this combination of effects, celiprolol may be better described as a selective adrenoreceptor modulator. It has antihypertensive and antianginal properties and is indicated for those uses in various countries around the world. In the United States, however, the proposed indication for this drug will be for the treatment of vascular type Ehlers-Danlos syndrome, a rare connective tissue disorder characterized by fragile arterial structure and an increased risk of life-threatening vascular complications. By reducing heart rate and pulsatile pressure, celiprolol may reduce the mechanical stress on collagen fibers within the arterial wall and be of benefit in patients with vascular type Ehlers-Danlos syndrome. The largest investigation of celiprolol in vascular Ehlers-Danlos syndrome was prematurely terminated due to significant benefit with celiprolol in reducing arterial events in patients with this condition. Celiprolol, therefore, represents a β-blocker that is unique from others in its class in both its pharmacology and clinical applications.
The Most Powerful Health Care Product Antiaging Tomato Extract Lycopene Powder Tomatoes are rich in vitamins A and C and fibre , and are cholesterol free. An average size tomato (148 gram, or 5 oz) boasts only 35 calories. Furthermore, new medical research suggests that the consumption of lycopene - the stuff that makes tomatoes red - may prevent cancer. Lycopene is part of the family of pigments called carotenoids, which are natural compounds that create the colours of fruits and vegetables. For example, beta carotene is the orange pigment in carrots.As with essential amino acids, they are not produced by the human body. Lycopene is the most powerful antioxidant in the carotenoid family and, with vitamins C and E, protect us from the free radicals that degrade many parts of the body.Antiaging Powder Lycopene is a bright red carotene and carotenoid pigment and phytochemical found in tomatoes and other red fruits & vegetables, such as,GAC, red carrots, watermelons and papayas (but not strawberries or cherries). Although lycopene is chemically a carotene, it has no vitamin A activity. In plants, algae, and other photosynthetic organisms, lycopene is an important intermediate in the biosynthesis of many carotenoids, including beta carotene, responsible for yellow, orange or red pigmentation, photosynthesis, and photo-protection. Structurally, it is a tetraterpene assembled from eight isoprene units, composed entirely of carbon and hydrogen, and is insoluble in water. Lycopene is not an essential nutrient for humans, but is commonly found in the diet, mainly from dishes prepared with tomato sauce. When absorbed from the stomach, lycopene is transported in the blood by various lipoproteins and accumulates in the liver, adrenal glands, and testes. The related carotenoid antioxidant, beta-carotene, has been shown to increase the number of prostate cancer cases in a subset of patients, although this area of research remains controversial and ongoing. 1) Prevention and suppression of cancer; 2) Protection of the cardiovascular; 3) Anti-ultraviolet radiation; 4) Suppression mutagenesis; 5) Anti-aging and enhancing immunity; 6) Improving skin allergies; 7) Improving a variety of body tissues 8)With a strong hangover effect; 9) With the prevention of osteoporosis, lower blood pressure,reducing the exercise induced asthma, and other physiological functions; 10) Without any side effects, ideal for taking long-term care; 11) Preventing and improving prostatic hyperplasia; prostatitis and other urological diseases; 12) Helping to improve sperm quality, reduce the risk of infertility.
Nootropic Powder J147 Pharmaceutical Intermediate J147 powder was discovered based upon efficacy in multiple cell culture models of age-associated pathologies rather than exclusively amyloid metabolism. It is an exceptionally potent, orally active and broadly neuroprotective compound has the ability to enhance memory in normal animals as well as to prevent memory deficits in Alzheimer's disease (AD) transgenic mice. The neurotrophic and memory-enhancing activities of J147 are associated with an increase in brain derived neurotrophic factor (BDNF) levels and the expression of BDNF responsive proteins, the enhancement of LTP, the preservation of synaptic protein, the reduction of amyloid plaques, etc. These pleiotrophic effects of a single molecule suggest that J147 has potential for the treatment of AD. J 147 is a novel neurotrophic drug for cognitive enhancement and Alzheimer's disease. J 147 is an exceptionally potent, orally active and broadly neuroprotective compound has the ability to enhance memory in normal animals as well as to prevent memory deficits in Alzheimer's disease (AD) transgenic mice. The neurotrophic and memory-enhancing activities of J147 are associated with an increase in brain derived neurotrophic factor (BDNF) levels and the expression of BDNF responsive proteins, the enhancement of LTP, the preservation of synaptic protein, the reduction of amyloid plaques. Function: Enhance mental intelligence; Boost memory and leaning capabilities;Improve brain power to solve problems and protect it from any chemical or physical injury;Enhance motivation level;Enhance the control of cortical/subcortical brain mechanism;Improve sensory perception.
Pharmaceutical Grade Alpha Lipoic Acid Lipoic Acid CAS No.: 1077-28-7 EINECS No.: 200-534-6 Type: Vitamins, Antioxidant, Nutrition Enhancers Appearance: Slightly yellow crystal powder Application: 1.Alpha lipoic acid is a vitamin drugs, limited physical activity in its dextral, basically no physical activity in its Lipoic acid , and no side effects. 2.Alpha lipoic acid always used for acute and chronic hepatitis, liver cirrhosis, hepatic coma, fatty liver, diabetes, Alzheimer's disease ,and applies as an antioxidant health products. Packaging & Delivery Packaging Details: 25kg/carton Delivery Time: within 7 days after payment Product Description Alpha lipoic acid is a vitamin drugs, limited physical activity in its dextral, basically no physical activity in its Lipoic acid, and no side effects. It is always used for acute and chronic hepatitis, liver cirrhosis, hepatic coma, fatty liver, diabetes, Alzheimer's disease ,and applies as an antioxidant health products.Alpha-lipoic Acid powder 1.Alpha lipoic acid is a fatty acid found naturally inside every cell in the body. 2.Alpha lipoic acid is needed by the body to produce the energy for our body's normal functions. 3.Alpha lipoic acid converts glucose(blood sugar) into energy. 4.Alpha lipoic acid is also an antioxidant, a substance that neutralizes potentially harmful chemicals called free radicals. What makes alpha lipoic acid unique is that it functions in water and fat. 5. Alpha lipoic acid appears to be able to recycle antioxidants such as vitamin C and glutathione after they have been used up. Alpha lipoic acid increases the formation of glutathione.
People are drinking collagen powder Do a quick scroll through Instagram, and chances are you’ll see a slew of wellness and fitness personalities touting the benefits of collagen peptide powder and adding it to their smoothies.Antiaging Powder So what exactly is collagen and why are some people clamoring for it?“Collagen is a structural protein made up of amino acids that's found naturally in the connective tissue of our bodies, such as our skin, hair, muscles, bones and even blood vessels,” Keri Gans, registered dietitian nutritionist and author of The Small Change Diet, tells Yahoo Lifestyle. “It is essentially the ‘glue’ that holds our body together, enables us to move and find stability.” Adds Joshua Zeichner, MD, director of cosmetic and clinical research in Mount Sinai Hospital’s department of dermatology, “Collagen is the main protein in our skin that provides structure and support.”And it’s that structure and support that plays a role in keeping skin looking smooth, firm, and wrinkle-free. But collagen production slows down as we age, which is why many people are turning to consuming collagen peptides (also known as hydrolyzed collagen) in the hopes that the supplements will reverse or at least stave off skin aging. “The hope for ingestible collagen is that it helps strengthen our skin to improve the appearance of fine lines and wrinkles, as well as enhance skin texture,” Zeichner tells Yahoo Lifestyle. But does consuming collagen powder actually do anything? Possibly.“The true benefit of ingestible collagen is unclear,” says Zeichner. “Since collagen is a large molecule, it is broken down by our gut into smaller pieces. The smaller pieces and individual amino acids may serve as building blocks for new collagen production. I look at ingestible collagen similar to the way I look at eating a high-protein meal.” Adds Gans: “Many individuals believe the numerous health claims in regards to collagen. There are claims that it can reduce constipation, improve gut health, improve sleep, decrease anxiety, reduce joint pain, eliminate food cravings and has anti-aging properties.” What are the benefits? Although more research is needed, there are some studies that have looked into collagen supplements’ potential benefits — particularly for easing joint pain. “Some preliminary research suggests collagen supplements may help reduce knee pain among people with osteoarthritis, and help reduce joint deterioration in athletes,” says Gans. While it’s no fountain of youth, there is some good news for people who are consuming collagen hoping to improve their skin and hair. “One small study revealed collagen supplements improved skin elasticity, but didn't do any more than a placebo to improve skin moisture and evaporation,” says Gans. A 2019 review of several studies showed that collagen supplements increase skin elasticity and hydration. It may also help with brittle, fragile nails. A small 2017 study in the Journal of Cosmetic Dermatology found that consuming collagen peptides daily for 24 weeks helped prevent nail breakage, increase nail growth, and improved the appearance of brittle nails. How safe is it? Collagen supplements are considered safe for the most part — as Zeichner puts it: “The only harm is to your pocketbook, as many of the collagen powders are pricey.” However, it’s important to read up on the source of the supplement’s main ingredient. The collagen found in supplements is typically sourced from cow (bovine) hides, as well as chicken cartilage, but in some cases they can be made from fish or eggs, which can be dangerous for people with those food allergies. “As with any supplement, one should read the label closely to make sure it doesn’t include any allergens that they are sensitive to,” suggests Gans. “Also, if on any medications a person should discuss with their doctor or a registered dietitian before implementing in their daily diet.” If you’re interested in trying collagen peptides powder, your best bet is to stick with a well-known brand, such as Vital Proteins. As Gans points out: “Like all supplements, collagen is not closely regulated by the Food and Drug Administration — therefore, one should choose nationally-recognized brands or store brands from a retailer they trust. Consumers can also look for a seal from a third-party certifier, such as NSF International, UL or USP.” You may also want to start with unflavored collagen peptide powder, which you can add to smoothies, as well as hot and cold beverages like coffee, without altering the flavor.