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Zhejiang Hisun Pharma inlicenses China rights to liver cancer drug (ThermoDox) from Celsion Corporation
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| (7S,9S)-7-[(2R,4S,5S,6S)-4-amino-5-hydroxy-6-methyloxan-2-yl]oxy-6,9,11-trihydroxy-9-(2-hydroxyacetyl)-4-methoxy-8,10-dihydro-7H-tetracene-5,12-dione |
doxorubicin
Jan. 25, 2013
LINK
Heat–activated liposome encapsulated doxorubicin – NIHR Horizon …Heat–activated liposome encapsulated doxorubicin (ThermoDox) for hepatocellular carcinoma.
Zhejiang Hisun Pharma inlicenses China rights to liver cancer drug (ThermoDox) from Celsion Corporation
About ThermoDox
The study is designed to evaluate the efficacy of ThermoDox® in combination with RFA when compared to patients who receive RFA alone as the control. The primary endpoint for the study is progression-free survival (PFS) with a secondary confirmatory endpoint of overall survival. ThermoDox® has been granted orphan drug designation in both the U.S. and Europe. In addition to meeting the U.S. FDA and European EMA enrollment objectives, the Phase 3 Study has also enrolled a sufficient number of patients to support registration filings in China, South Korea and Taiwan, three of the largest potential markets for ThermoDox® around the world.
Terms of the Deal
Under the terms of the agreement, Hisun will pay $5 million to Celsion immediately, while Celsion will provide Hisun with support for its ThermoDox® manufacturing development program. This payment is non-refundable and comes in advance of Celsion’s expected reporting of results from its pivotal Phase III trial (the HEAT Study) in hepatocellular carcinoma (HCC), also known as primary liver cancer later this month.
In addition, the companies anticipate signing an agreement in which Celsion provides Hisun an exclusive option to license ThermoDox® for the Greater China market, which includesChina, Hong Kong and Macau. This option period will be secured by a second $5 millionpayment that must be received by Celsion from Hisun within 60 days after execution of the Technology Development Agreement. The key provisions of the anticipated license agreement have been negotiated and agreed to by the parties and provide a basis for a definitive contract. These provisions are:
- A credit of $10 million from the two payments ($5 million for the technology development agreement and $5 million for the exclusive option) toward a non-refundable upfront license payment of $25 million due to Celsion at signing of the definitive license agreement.
- An approximate 10 year total value to Celsion of well over several hundred million US dollars, which includes:
- $55 million in upfront milestone and regulatory milestone payments within the next 18 months;
- $45 million in milestone payments for reaching certain sales targets; and
- Escalating double-digit royalties on net sales of ThermoDox® in the Greater China Territory.
- Hisun will serve as both the manufacturer and distributor of the ThermoDox® drug product for the Greater China Territory, and also take responsibility for local regulatory activities including submitting approvals in China to the state Food and Drug Administration (sFDA).
Deal Rationale
“Pursuing this arrangement with Hisun allows us to evaluate the fastest path to the Chinamarket, potentially the largest opportunity in the world for ThermoDox®. A long-term partnership will provide the greatest synergies with respect to sales, marketing, distribution, and manufacturing, which could ensure significant value to the ThermoDox® asset,” saidMichael H. Tardugno, Celsion’s President and Chief Executive Officer. “In addition, this partnership provides Hisun and Celsion with immediate access to an accelerated pathway for sFDA review and approval of ThermoDox®, a business strategy with exceptional potential to serve China’s HCC population, and strong, uncompromised economics for both parties.”
Mr. Hua Bai, CEO and Chairman of Hisun, stated, “We are extremely excited to pursue this arrangement with Celsion. Hisun is well positioned to provide ThermoDox® — potentially one of the most important and innovative drugs to treat HCC to patients in China, the world’s largest market. China is one of the countries with the highest HCC incidence and mortality and, up until now, there has not been any standard of care for treating HCC in China.
This joint effort will most likely facilitate the local manufacturing and commercial launch inChina, thereby providing physicians with more options for better care and prolonging the survival of HCC patients. In the meantime, we are also hopeful that this collaboration will enable Hisun to increase its focus on more innovative drugs. Given the fact that we are a leading Chinese pharmaceutical company with international standards of R&D and manufacturing technology, Hisun will seek to manufacture and supply the global markets, along with distribution exclusivity in Greater China. This venture will help spearhead Hisun’s globalization in manufacturing and commercialization capabilities.”
About Primary Liver Cancer
Primary liver cancer is one of the most deadly forms of cancer and ranks as the fifth most common solid tumor cancer. The incidence of primary liver cancer today is approximately 26,000 cases per year in the United States, approximately 40,000 cases per year in Europeand is rapidly growing worldwide at approximately 750,000 cases per year, 55 percent of which are in China, due to the high prevalence of Hepatitis B and C in developing countries. . The World Health Organization estimates that primary liver cancer may become the number one cancer worldwide, surpassing lung cancer, by 2020.
The standard first-line treatment for liver cancer is surgical resection of the tumor; however, 90% of patients are ineligible for surgery. Radio frequency ablation (RFA) has increasingly become the standard of care for non-resectable liver tumors, but the treatment becomes less effective for larger tumors. There are few non-surgical therapeutic treatment options available as radiation therapy and chemotherapy are largely ineffective in the treatment of primary liver cancer.
Doxorubicin trade name Adriamycin; also known ashydroxydaunorubicin) is a drug used in cancer chemotherapy. It is an anthracyclineantibiotic, closely related to the http://en.wikipedia.org/wiki/Natural_product” rel=”nofollow”>natural product daunomycin, and like all anthracyclines, it works by intercalating DNA, with the most serious adverse effect being life-threatening heart damage. It is commonly used in the treatment of a wide range of cancers, includinghematological malignancies, many types of carcinoma, and soft tissue sarcomas.
The drug is administered intravenously, as the hydrochloride salt. It may be sold under the brand names Adriamycin PFS, Adriamycin RDF, or Rubex.[2] Doxorubicin is photosensitive, and containers are often covered by an aluminum bag and/or brown wax paper to prevent light from affecting it.
Doxorubicin is available in liposome-encapsulated forms as Doxil, Caelyx and Myocet.
Doxorubicin is commonly used to treat some leukemias and Hodgkin’s lymphoma, as well as cancers of the bladder, breast, stomach,lung, ovaries, thyroid, soft tissue sarcoma, multiple myeloma, and others.[2] Commonly used doxorubicin-containing regimens are AC (Adriamycin, cyclophosphamide), TAC (Taxotere, CA), ABVD (Adriamycin, bleomycin, vinblastine, dacarbazine), BEACOPP, CHOP(cyclophosphamide, Adriamycin, vincristine, prednisone) and FAC (5-fluorouracil, Adriamycin, cyclophosphamide).
Doxil (see below) is used primarily for the treatment of ovarian cancer where the disease has progressed or recurred after platinum-based chemotherapy, or for the treatment of AIDS-related Kaposi’s sarcoma.[7]
- Laginha, K.M. “Determination of Doxorubicin Levels in Whole Tumor and Tumor Nuclei in Murine Breast Cancer Tumors.”Clinical Cancer Research. October 1, 2005. Vol. 11 (19). Retrieved on April 19, 2007.
- “Doxorubicin (Systemic).” Mayo Clinic. Last updated on: June 15, 1999. Retrieved on April 19, 2007. Archived April 3, 2007 at the Wayback Machine
- Weiss RB (December 1992). “The anthracyclines: will we ever find a better doxorubicin?”. Seminars in Oncology 19 (6): 670–86. PMID 1462166.
- Tan C, Tasaka H, Yu KP, Murphy ML, Karnofsky DA (March 1967). “Daunomycin, an antitumor antibiotic, in the treatment of neoplastic disease. Clinical evaluation with special reference to childhood leukemia”. Cancer 20 (3): 333–53. doi:10.1002/1097-0142(1967)20:3<333::AID-CNCR2820200302>3.0.CO;2-K.PMID 4290058.
- Arcamone F, Cassinelli G, Fantini G, et al. (1969). “Adriamycin, 14-hydroxydaunomycin, a new antitumor antibiotic from S. peucetius var. caesius“. Biotechnol Bioeng 11 (6): 1101–10. doi:10.1002/bit.260110607. PMID 5365804.
- Di Marco A, Gaetani M, Scarpinato B (February 1969). “Adriamycin (NSC-123,127): a new antibiotic with antitumor activity”. Cancer Chemother Rep 53 (1): 33–7. PMID 5772652.
- “DOXIL Product Information.” Ortho Biotech Products, L.P. Retrieved on April 19, 2007. Archived September 21, 2007 at the Wayback Machine
Bedaquiline
Bedaquiline
Fast-track approval for treatment of tuberculosis
May 3, 2013
Bedaquiline (Sirturo) represents a new class of anti-TB drugs called diarylquinolines that have a novel mechanism of action to stop replication of TB. It has FDA approval for treatment of multi-drug resistant pulmonary TB. The drug has not been evaluated with extra-pulmonary TB affecting the CNS. Standard treatment involves a four-drug regimen with isoniazid, rifampin and pyrazinamide (PZA). A recent meta-analysis showed the percentage of patients dying from TB was 3% in non-HIV patients, 9.2% in HIV-infected patients and 30.9% in HIV-infected patients with multi-drug resistant TB. This drug achieved fast-track approval by the FDA due to risks associated with multi-drug resistant TB.
Recent clinical trials included patients with pulmonary TB and used the same dosing strategy (400 mg orally twice daily for two weeks followed by 200 mg three times per week). The clinical endpoint was the time to…
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Human medicines European Public Assessment Report EPAR : Pantecta Control, pantoprazole, Revision: 3,
Human medicines European Public Assessment Report EPAR : Pantecta Control, pantoprazole, Revision: 3,
pantoprazole
* The original URL is http://www.ema.europa.eu/ema/index.jsp?curl=pages/medicines/human/medicines/001099/human_med_000967.jsp&mid=WC0b01ac058001d124
Pantoprazole (sold under various brand names including Somac, Tecta, Pantoloc, Controloc, Protium, Protonix, Pantecta, Pantoheal, Pantpas, Ppi-40, and Neoppi) is a proton pump inhibitor drug that inhibits gastric acid secretion.
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Country
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Patent Number
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Approved
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Expires (estimated)
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| Canada | 2428870 | 2006-05-23 | 2021-11-17 |
| Canada | 2092694 | 2005-04-05 | 2011-09-06 |
| Canada | 2341031 | 2006-04-04 | 2019-08-12 |
| United States | 7544370 | 2006-12-07 | 2026-12-07 |
| United States | 4758579 | 1993-07-19 | 2010-07-19 |
sNDA- FDA OKs HIV Drug Sustiva
EFAVIRENZ
FDA OKs HIV Drug Sustiva
Bristol-Myers Squibb Receives US FDA sNDA Approval for Use of SUSTIVA® (efavirenz) in HIV-1 Infected Pediatric Patients
Approval offers a once-daily option as part of a regimen for HIV-1 infected infants as young as three months and weighing at least 3.5 kg
“Capsule sprinkle” administration allows dosing in patients who cannot swallow capsules or tablets
“Bristol-Myers Squibb recognizes the importance of offering alternative methods of administration of HIV medicines, including for pediatric patients who cannot swallow tablets or capsules, and their caregivers who help manage their treatment,”
Bristol-Myers Squibb Company first week may 2013, announced that the U.S. Food and Drug Administration (FDA) has approved a supplemental new drug application (sNDA) for SUSTIVA® (efavirenz), including dosing recommendations for HIV-1 infected pediatric patients three months to three years old and weighing at least 3.5 kg. This approval offers a once-daily option as part of a regimen for this population and includes a “capsule sprinkle” administration method for patients who cannot swallow capsules or tablets. Detailed information about the “capsule sprinkle” method is provided in the ‘Instructions for Use’ at the end of the Patient Information section of the Package Insert.
SUSTIVA is a non-nucleoside reverse transcriptase inhibitor (NNRTI) that was originally approved in the U.S. in 1998 to treat HIV-1 infected children three years of age or older and weighing at least 10 kg. SUSTIVA is not to be taken by patients who are allergic to efavirenz, or to any of its ingredients.
“Bristol-Myers Squibb recognizes the importance of offering alternative methods of administration of HIV medicines, including for pediatric patients who cannot swallow tablets or capsules, and their caregivers who help manage their treatment,” said Brian Daniels, M.D., Senior Vice President, Global Development and Medical Affairs. “This approval is one example of our enduring commitment to the HIV patient community.”
This sNDA was based on results from three open-label studies that evaluated the pharmacokinetics, safety, and antiretroviral activity of SUSTIVA in combination with other antiretroviral agents in 182 antiretroviral-naïve and –experienced HIV-1 infected pediatric patients (three months to 21 years of age) for a median of 123 weeks. Virologic and immunologic response was observed across all ages at the end of the studies, as measured by HIV RNA and CD4 cell count.
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.
DR ANTHONY MELVIN CRASTO
ORGANIC SPECTROSCOPY
New Drug Approvals 