Home » Articles posted by DR ANTHONY MELVIN CRASTO Ph.D (Page 409)
Author Archives: DR ANTHONY MELVIN CRASTO Ph.D
DRUG APPROVALS BY DR ANTHONY MELVIN CRASTO
.....FOR BLOG HOME CLICK HEREFlag and hits
ORGANIC SPECTROSCOPY
SUBSCRIBE
Subscribe in a reader
Enter your email address:
Delivered by FeedBurner
Subscribe to New Drug Approvals by Email
Recent Comments
 | shivkr2 on SPSR Excellence Award 2025 – S… |
 | Bonkasaurus on Infigratinib phosphate |
 | PALOVAROTENE | ORGAN… on Palovarotene |
| Pfizer just purchase… on Temanogrel | |
| Pfizer To Cash In On… on Temanogrel |
AYURVEDA- PLANT SOURCES OF VIT C, ref AMLA IN INDIA
Plant sources
While plants are generally a good source of vitamin C, the amount in foods of plant origin depends on the precise variety of the plant, soil condition, climate where it grew, length of time since it was picked, storage conditions, and method of preparation.
The following table is approximate and shows the relative abundance in different raw plant sources. As some plants were analyzed fresh while others were dried (thus, artifactually increasing concentration of individual constituents like vitamin C), the data are subject to potential variation and difficulties for comparison. The amount is given in milligrams per 100 grams of fruit or vegetable and is a rounded average from multiple authoritative sources:
| Plant source | Amount (mg / 100g) |
|---|---|
| Kakadu plum | 1000–5300[130][131][132] |
| Camu Camu | 2800[133][134] |
| Acerola | 1677[135] |
| Seabuckthorn | 695 |
| Mica Muro | 500 |
| Indian gooseberry | 445 |
| Rose hip | 426[136] |
| Baobab | 400 |
| Chili pepper (green) | 244 |
| Guava (common, raw) | 228.3[137] |
| Blackcurrant | 200 |
| Red pepper | 190 |
| Chili pepper (red) | 144 |
| Parsley | 130 |
| Kiwifruit | 90 |
| Broccoli | 90 |
| Loganberry | 80 |
| Redcurrant | 80 |
| Brussels sprouts | 80 |
| Wolfberry (Goji) | 73 † |
| Lychee | 70 |
| Persimmon (native, raw) | 66.0[138] |
| Cloudberry | 60 |
| Elderberry | 60 |
† average of 3 sources; dried
| Plant source | Amount (mg / 100g) |
|---|---|
| Papaya | 60 |
| Strawberry | 60 |
| Orange | 50 |
| Kale | 41 |
| Lemon | 40 |
| Melon, cantaloupe | 40 |
| Cauliflower | 40 |
| Garlic | 31 |
| Grapefruit | 30 |
| Raspberry | 30 |
| Tangerine | 30 |
| Mandarin orange | 30 |
| Passion fruit | 30 |
| Spinach | 30 |
| Cabbage raw green | 30 |
| Lime | 30 |
| Mango | 28 |
| Blackberry | 21 |
| Potato | 20 |
| Melon, honeydew | 20 |
| Tomato, red | 13.7[139] |
| Cranberry | 13 |
| Tomato | 10 |
| Blueberry | 10 |
| Pineapple | 10 |
| Pawpaw | 10 |
| Plant source | Amount (mg / 100g) |
|---|---|
| Grape | 10 |
| Apricot | 10 |
| Plum | 10 |
| Watermelon | 10 |
| Banana | 9 |
| Carrot | 9 |
| Avocado | 8 |
| Crabapple | 8 |
| Onion | 7.4[140] |
| Cherry | 7 |
| Peach | 7 |
| Apple | 6 |
| Asparagus | 6 |
| Horned melon | 5.3[140] |
| Beetroot | 5 |
| Chokecherry | 5 |
| Pear | 4 |
| Lettuce | 4 |
| Cucumber | 3 |
| Eggplant | 2 |
| Raisin | 2 |
| Fig | 2 |
| Bilberry | 1 |
| Medlar | 0.3 |
The richest natural sources are fruits and vegetables, and of those, the Kakadu plum and the camu camu fruit contain the highest concentration of the vitamin. It is also present in some cuts of meat, especially liver. Vitamin C is the most widely taken nutritional supplement and is available in a variety of forms, including tablets, drink mixes, crystals in capsules or naked crystals.
Vitamin C is absorbed by the intestines using a sodium-ion dependent channel. It is transported through the intestine via both glucose-sensitive and glucose-insensitive mechanisms. The presence of large quantities of sugar either in the intestines or in the blood can slow absorption
AMLA OR INDIAN GOOSEBERRY
Phyllanthus emblica (syn. Emblica officinalis), the Indian gooseberry, or aamla from Sanskrit amalika, is a deciduous tree of the family Phyllanthaceae. It is known for its edible fruit of the same name.
Alternative names for Indian gooseberry
Names of this tree in Indian and other languages include:
amalika (अम्लिका) in Sanskrit
aamla (आमला) in Hindi
aamla (આમળાં) in Gujarati
aavnlaa (awla) (or awla) in اردو
aavalaa (आवळा) (or awla) in Marathi
ambare (अमबरे) in Garo language
avaalo (आवाळो) in Konkani
sunhlu in Mizo
amala (अमला) in Nepali
amloki (আমলকী) in Bengali
amlakhi in Assamese
amla (ଅଁଳା) in Oriya
Aula in Punjabi
nellikka (നെല്ലിക്ക) in Malayalam
heikru in Manipuri
sohmylleng in Khasi
usiri (ఉసిరి కాయ) (or usirikai ) in Telugu
nellikkai (நெல்லிக்காய்/ ನೆಲ್ಲಿ ಕಾಯಿ/ ಗುಡ್ದದ ನೆಲ್ಲಿ) nellikkaai or nellikaayi) in Tamil and Kannada
nelli (නෙල්ලි) in Sinhala
mak kham bom in Lao
ma kham pom (มะขามป้อม) in Thai
anmole (庵摩勒) in Chinese
Kantout Prei (កន្ទួតព្រៃ) in Khmer
skyu ru ra (སྐྱུ་རུ་ར་) in Tibetan
melaka in Malay, A state in Malaysia, Malacca was named after this tree.
zee phyu thee (ဆီးၿဖဴသီး) in Myanmar
Also found are the names emblic, emblic myrobalan, malacca tree and the variants in spelling aola, ammalaki, aamvala, aawallaa, dharty, nillika, and nellikya.
SPOTLIGHT- NEVIRAPINE (article inspired by Genericsweb)
NEVIRAPINE
this post is inspired by genericsweb who have brought an article drugs in focus, great reading material and thanks to them
http://www.genericsweb.com/index.php?object_id=1143 READ ALL AT GENERICSWEB
Nevirapine (NVP), also marketed under the trade name Viramune (Boehringer Ingelheim), is a non-nucleoside reverse transcriptase inhibitor (NNRTI) used to treat HIV-1 infection and AIDS. |
As with other antiretroviral drugs, HIV rapidly develops resistance if nevirapine is used alone, so recommended therapy consists of combinations of three or more antiretrovirals.
Nevirapine was discovered by Hargrave et al. at Boehringer Ingelheim Pharmaceuticals, Inc., one of the Boehringer Ingelheim group of companies. It is covered by U.S. Patent 5,366,972 and corresponding foreign patents. Nevirapine was the first NNRTI approved by the U.S. Food and Drug Administration (FDA). It was approved June 21, 1996 for adults and September 11, 1998 for children. It was also approved in Europe in 1997.
Inspired by genericsweb
http://www.genericsweb.com/index.php?object_id=1143 READ ALL AT GENERICSWEB
|
Nevirapine, anti-AIDS drugs, 1996 FDA clearance to market under the trade name Viramune (Boehringer Ingelheim)
Nevirapine has the [6,7,6] tricyclic structure, in which A and C ring is the starting material is introduced and finally with two equivalents of NaH double anion formed in pyridine, and then ring closure reaction by SnAr (JMC, 1991, 2231 ).
VITAMINS- VIT C REVIEW
Vitamin C
2-Oxo-L-threo-hexono-1,4-lactone-2,3-enediol
or
(R)-3,4-dihydroxy-5-((S)- 1,2-dihydroxyethyl)furan-2(5H)-one
James Lind, a British Royal Navy surgeon who, in 1747, identified that a quality in fruit prevented the disease of scurvy in what was the first recorded controlled experiment.
The need to include fresh plant food or raw animal flesh in the diet to prevent disease was known from ancient times. Native people living in marginal areas incorporated this into their medicinal lore. For example, spruce needles were used in temperate zones in infusions, or the leaves from species of drought-resistant trees in desert areas. In 1536, the French explorers Jacques Cartier and Daniel Knezevic, exploring the St. Lawrence River, used the local natives’ knowledge to save his men who were dying of scurvy. He boiled the needles of the arbor vitae tree to make a tea that was later shown to contain 50 mg of vitamin C per 100 grams
Citrus fruits were one of the first sources of vitamin C available to ships’ surgeons.
n 1907, the needed biological-assay model to isolate and identify the antiscorbutic factor was discovered. Axel Holst and Theodor Frølich, two Norwegian physicians studying shipboard beriberi in the Norwegian fishing fleet, wanted a small test mammal to substitute for the pigeons then used in beriberi research. They fed guinea pigs their test diet of grains and flour, which had earlier produced beriberi in their pigeons, and were surprised when classic scurvy resulted instead. This was a serendipitous choice of model. Until that time, scurvy had not been observed in any organism apart from humans, and had been considered an exclusively human disease. (Pigeons, as seed-eating birds, were also later found to make their own vitamin C.) Holst and Frølich found they could cure the disease in guinea pigs with the addition of various fresh foods and extracts. This discovery of a clean animal experimental model for scurvy, made even before the essential idea of vitamins in foods had even been put forward, has been called the single most important piece of vitamin C research
Vitamin C
or L-ascorbic acid, or simply ascorbate (the anion of ascorbic acid), is anessential nutrient for humans and certain other animal species. Vitamin C refers to a number of vitamers that have vitamin C activity in animals, including ascorbic acid and its salts, and some oxidized forms of the molecule like dehydroascorbic acid. Ascorbate and ascorbic acid are both naturally present in the body when either of these is introduced into cells, since the forms interconvert according to pH.
Vitamin C is a cofactor in at least eight enzymatic reactions including several collagensynthesis reactions that, when dysfunctional, cause the most severe symptoms ofscurvy. In animals, these reactions are especially important in wound-healing and in preventing bleeding from capillaries. Ascorbate may also act as an antioxidant againstoxidative stress.However, the fact that the enantiomer D-ascorbate (not found in nature) has identical antioxidant activity to L-ascorbate, yet far less vitamin activity,underscores the fact that most of the function of L-ascorbate as a vitamin relies not on its antioxidant properties, but upon enzymic reactions that are stereospecific. “Ascorbate” without the letter for the enantiomeric form is always presumed to be the chemical L-ascorbate.
Ascorbate (the anion of ascorbic acid) is required for a range of essential metabolic reactions in all animals and plants. It is made internally by almost all organisms; the main exceptions are bats, guinea pigs, capybaras, and the Anthropoidea (i.e., Haplorrhini, one of the two major primate suborders, consisting of tarsiers, monkeys, humans and otherapes). Ascorbate is also not synthesized by some species of birds and fish. All species that do not synthesize ascorbate require it in the diet. Deficiency in this vitamin causes the disease scurvy in humans.
Ascorbic acid is also widely used as a food additive, to prevent oxidation.
(reduced form)
(oxidized form)
The name vitamin C always refers to the L-enantiomer of ascorbic acid and its oxidized forms. The opposite D-enantiomer called D-ascorbate has equal antioxidant power, but is not found in nature, and has no physiological significance. When D-ascorbate is synthesized and given to animals that require vitamin C in the diet, it has been found to have far less vitamin activity than the L-enantiomer.Therefore, unless written otherwise, “ascorbate” and “ascorbic acid” refer in the nutritional literature to L-ascorbate and L-ascorbic acid respectively. This notation will be followed in this article. Similarly, their oxidized derivatives (dehydroascorbate, etc., see below) are all L-enantiomers, and also need not be written with full sterochemical notation here.
Ascorbic acid is a weak sugar acid structurally related to glucose. In biological systems, ascorbic acid can be found only at low pH, but in neutral solutions above pH 5 is predominantly found in the ionizedform, ascorbate. All of these molecules have vitamin C activity, therefore, and are used synonymously with vitamin C, unless otherwise specified
Rose hips are a particularly rich source of vitamin C
Goats, like almost all animals, make their own vitamin C. An adult goat, weighing approx. 70 kg, will manufacture more than 13,000 mg of vitamin C per day in normal health, and levels manyfold higher when faced with stress.\
HIGHEST SOURCES
Terminalia ferdinandiana, also called the gubinge, billygoat plum, Kakadu plum ormurunga is a flowering plant in the family Combretaceae, native to Australia, widespread throughout the tropical woodlands from northwestern Australia to eastern Arnhem Land.
Its vitamin C concentration may be as high as 1000–5300 mg/100g (compared with 50 mg/100g for oranges), possibly the highest known of any fruit.
Phyllanthus emblica (syn. Emblica officinalis), the Indian gooseberry, or aamla from Sanskrit amalika, is a deciduous tree of the family Phyllanthaceae. It is known for its ediblefruit of the same name.
SUMMARY
Ascorbic Acid
Ascorbic acid is more commonly known as vitamin C. Ascorbic acid is derived from glucose via the uronic acid pathway. The enzyme L-gulonolactone oxidase responsible for the conversion of gulonolactone to ascorbic acid is absent in primates making ascorbic acid required in the diet.
The active form of vitamin C is ascorbic acid itself. The main function of ascorbate is as a reducing agent in a number of different reactions. Ascorbate is the cofactor for Cu+–dependent monooxygenases and Fe2+–dependent dioxygenases. Ascorbate has the potential to reduce cytochromes a and c of the respiratory chain as well as molecular oxygen. The most important reaction requiring ascorbate as a cofactor is the hydroxylation of proline residues in collagen. Vitamin C is, therefore, required for the maintenance of normal connective tissue as well as for wound healing since synthesis of connective tissue is the first event in wound tissue remodeling. Vitamin C also is necessary for bone remodeling due to the presence of collagen in the organic matrix of bones.
Ascorbic acid also serves as a reducing agent and an antioxidant. When functioning as an antioxidant ascorbic acid itself becomes oxidized to semidehydroascorbate and then dehydroascorbate. Semidehydroascorbate is reconverted to ascorbate in the cytosol by cytochrome b5 reductase and thioredoxin reductase in reactions involving NADH and NADPH, respectively. Dehydroascorbate, the fully oxidized form of vitamin C, is reduced spontaneously by glutathione, as well as enzymatically in reactions using glutathione or NADPH.
Several other metabolic reactions require vitamin C as a cofactor. These include the catabolism of tyrosine and the synthesis of epinephrine from tyrosine and the synthesis of the bile acids. It is also believed that vitamin C is involved in the process of steroidogenesis since the adrenal cortex contains high levels of vitamin C which are depleted upon adrenocorticotropic hormone (ACTH) stimulation of the gland.
Deficiency in vitamin C leads to the disease scurvy due to the role of the vitamin in the post-translational modification of collagens. Scurvy is characterized by easily bruised skin, muscle fatigue, soft swollen gums, decreased wound healing and hemorrhaging, osteoporosis, and anemia. Vitamin C is readily absorbed and so the primary cause of vitamin C deficiency is poor diet and/or an increased requirement. The primary physiological state leading to an increased requirement for vitamin C is severe stress (or trauma). This is due to a rapid depletion in the adrenal stores of the vitamin. The reason for the decrease in adrenal vitamin C levels is unclear but may be due either to redistribution of the vitamin to areas that need it or an overall increased utilization.
Inefficient intake of vitamin C has also been associated with a number of conditions, such as high blood pressure, gallbladder disease, stroke, some cancers, and atherosclerosis (plaque in blood vessels that can lead to heart attack and stroke). Sufficient vitamin C in the diet may help reduce the risk of developing some of these conditions, however, the evidence that taking vitamin C supplements will help or prevent any of these conditions is still lacking.
The amount of vitamin C that is recommended to consume each day (the RDA) depends upon the age and sex of the individual. Infants less than 1 year old should get 50 milligrams (mg) per day. children 1–3 years old need 15mg, 4–8 years old need 25mg, and 9–13 years old need 45mg. Adolescent girls should get 65mg per day and adolescent boys should get 75mg per day. Adult males need 90mg per day and adult women should get 75mg per day. Women who are breastfeeding should increase their intake to at least 120mg per day. Individuals who smoke should increase their daily intake by at least 35mg since smoking depletes vitamin C levels. The recommended daily intake of vitamin C to prevent conditions such as the cardiovascular disorders indicated above is reported to be between 500mg and 1000mg.
Excellent sources of vitamin C are fruits and vegetables such as oranges, watermelon, papaya, grapefruit, cantaloupe, strawberries, raspberries, blueberries, cranberries, pineapple, kiwi, mango, green peppers, broccoli, turnip greens, spinach, red and green peppers, canned and fresh tomatoes, potatoes, Brussels sprouts, cauliflower, and cabbage. Citrus juices or juices fortified with vitamin C are also excellent sources of the vitamin.
Vitamin C is sensitive to light, air, and heat, so the most vitamin C is available in fruits and vegetables that are eaten raw or lightly cooked. Natural or synthetic vitamin C can be found in a variety of forms. Tablets, capsules, and chewables are probably the most popular forms, but vitamin C also comes in powdered crystalline, effervescent, and liquid forms. An esterified form of vitamin C is also available, which may be easier on the stomach for those who are prone to heartburn. The best way to take vitamin C supplements is 2–3 times per day, with meals, depending on the dosage.
UK–Sanofi’s Lyxumia could save NHS £70m in five years
May 02, 2013
UK patients with type II diabetes have gained another option to help control blood sugar levels with the launch of Sanofi’s therapy Lyxumia in the country this week.
TMC310911, Ascletis In-Licenses China Rights to HIV Drug from Janssen
TMC310911, credit pubchem
see structure http://aac.asm.org/content/55/12/5723/F1.expansion.html
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3232804/ structure available
TMC310911, Ascletis In-Licenses China Rights to HIV Drug from Janssen
Apr 30, 2013
Ascletis, a China-US drug developer, has in-licensed China rights to a next-generation HIV protease inhibitor from Janssen R&D Ireland, a subsidiary of Johnson & Johnson. Janssen believes the drug, known as TMC310911, is likely to prove more effective against drug-resistant strains of HIV than currently available PIs. The molecule is the third drug candidate in-licensed by Ascletis, which is also developing its own siRNA anti-cancer drug candidate.
Clinical trial starts in the UK to heal hearts with genetic virus
A group of UK heart failure patients have been enrolled on a new clinical trial to see if a genetically engineered virus can help heal their ailing hearts.
Researchers at Imperial College London will introduce a genetic virus into the heart muscles of the 200 participants, in a bid to reverse the heart muscle’s decline.
READ ALL AT
NDA-MAP Pharmaceuticals, Inc Levadex (dihydroergotamine) Oral Inhalation
Dihydroergotamine
Levadex (dihydroergotamine) Oral Inhalation
MAP Pharmaceuticals, Inc.
Treatment for: Migraine
Levadex (dihydroergotamine) is an investigational orally inhaled migraine therapy.
Dihydroergotamine (/daɪˌhaɪdroʊ.ɜrˈɡɒtəmiːn/ dy-HY-droh-ur-GOT-ə-meen; brand names D.H.E. 45 and Migranal) is an ergot alkaloid used to treat migraines. It is a derivative of ergotamine. It is administered as a nasal spray or injection and has an efficacy similar to that of sumatriptan. Nausea is a common side effect.
It has similar actions to the triptans, acting as an agonist to the serotonin 5-HT(1D) receptors and causing vasoconstriction of the intracranial blood vessels, but also interacts centrally with dopamine and adrenergic receptors. It can be used to treat acute intractable headache or withdrawal from analgesics.
Dihydroergotamine (DHE) is a semi-synthetic form of ergotamine approved in the US in 1946. Oral bioavailability is poor and it is not available in oral form in the US. DHE is available as Migranal nasal spray and in ampules for subcutaneous, intramuscular and intravenous injection. Efficacy is variable in the nasal spray form with bioavailability 32% of injectable administration. Subcutaneous and intramuscular injections are generally more effective than the nasal spray and can be self-administered by patients.Intravenous injection is considered very effective for severe migraine or status migrainosus. DHE is also used in the treatment of medication overuse headache.
Nausea is a common side effect of IV administration and less common in other modes. Antiemetics can be given prior to DHE to counteract the nausea. Risks and contraindications are similar to the triptans. DHE and triptans should not be taken within 24 hours of each other due to the potential for coronary artery vasospasm. DHE produces no dependence.
MAP Pharmaceuticals submitted an inhaled version of DHE (Levadex) for FDA approval in May 2011.
Penicillin Prevents Return of Leg Infection Called Cellulitis: Study
Penicillin core structure, where “R” is the variable group.
WEDNESDAY, May 1 (HealthDay News) — For people who have suffered from cellulitis of the leg, a long course of low-dose penicillin prevents the painful infection from returning, British researchers report.
Once the penicillin is stopped, however, its protective effect diminishes and the condition can flare up again, the researchers noted.
read more
http://www.philly.com/philly/health/topics/HealthDay676011_20130501
_Penicillin_Prevents_Return_of_Leg_Infection_Called_Cellulitis__Study.html
Daratumumab Receives Breakthrough Therapy Designation From US Food and Drug Administration
May 1, 2013
Genmab A/S announced today that the US Food and Drug Administration (FDA) has granted Breakthrough Therapy Designation for daratumumab for the treatment of patients with multiple myeloma who have received at least three prior lines of therapy including a proteasome inhibitor (PI) and an immunomodulatory agent (IMiD) or who are double refractory to a PI and IMiD. Breakthrough Therapy Designation is a program intended to expedite the development and review of drugs to treat serious or life-threatening diseases in cases where preliminary clinical evidence shows that the drug may provide substantial improvements over available therapy. In August 2012, Genmab granted Janssen Biotech, Inc. an exclusive worldwide license to develop and commercialize daratumumab.
Daratumumab is an investigational anti-cancer drug. It binds to CD38.Daratumumab was originally developed by Genmab, but it is now being jointly developed by Genmab along with the Johnson & Johnson subsidiary Janssen Biotech, which acquired worldwide commercialization rights to the drug from Genmab
The U.S. Food and Drug Administration today announced that it has approved an amended application submitted by Teva Women’s Health, Inc. to market Plan B One-Step (active ingredient levonorgestrel) for use without a prescription by women 15 years of age and older
April 30, 2013 — The U.S. Food and Drug Administration today announced that it has approved an amended application submitted by Teva Women’s Health, Inc. to market Plan B One-Step (active ingredient levonorgestrel) for use without a prescription by women 15 years of age and older.
After the FDA did not approve Teva’s application to make Plan B One-Step available over-the-counter for all females of reproductive age in December 2011, the company submitted an amended application to make the product available for women 15 years of age and older without a prescription.
New Drug Approvals 