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    Chemistry

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    Also known as: 2,6-diisopropylphenol, 2078-54-8, Diprivan, Disoprofol, Disoprivan, Fresofol
    Molecular Formula
    C12H18O
    Molecular Weight
    178.27  g/mol
    InChI Key
    OLBCVFGFOZPWHH-UHFFFAOYSA-N
    FDA UNII
    YI7VU623SF
    Propofol
    An intravenous anesthetic agent which has the advantage of a very rapid onset after infusion or bolus injection plus a very short recovery period of a couple of minutes. (From Smith and Reynard, Textbook of Pharmacology, 1992, 1st ed, p206). Propofol has been used as ANTICONVULSANTS and ANTIEMETICS.
    Propofol is a General Anesthetic. The physiologic effect of propofol is by means of General Anesthesia.
    1 2D Structure

    Propofol

    2 Identification
    2.1 Computed Descriptors
    2.1.1 IUPAC Name
    2,6-di(propan-2-yl)phenol
    2.1.2 InChI
    InChI=1S/C12H18O/c1-8(2)10-6-5-7-11(9(3)4)12(10)13/h5-9,13H,1-4H3
    2.1.3 InChI Key
    OLBCVFGFOZPWHH-UHFFFAOYSA-N
    2.1.4 Canonical SMILES
    CC(C)C1=C(C(=CC=C1)C(C)C)O
    2.2 Other Identifiers
    2.2.1 UNII
    YI7VU623SF
    2.3 Synonyms
    2.3.1 MeSH Synonyms

    1. 2,6 Diisopropylphenol

    2. 2,6-bis(1-methylethyl)phenol

    3. 2,6-diisopropylphenol

    4. Aquafol

    5. Diprivan

    6. Disoprivan

    7. Disoprofol

    8. Fresofol

    9. Ici 35,868

    10. Ici 35868

    11. Ici-35,868

    12. Ici-35868

    13. Ici35,868

    14. Ici35868

    15. Ivofol

    16. Propofol Abbott

    17. Propofol Fresenius

    18. Propofol Mct

    19. Propofol Rovi

    20. Propofol-lipuro

    21. Recofol

    2.3.2 Depositor-Supplied Synonyms

    1. 2,6-diisopropylphenol

    2. 2078-54-8

    3. Diprivan

    4. Disoprofol

    5. Disoprivan

    6. Fresofol

    7. Diisopropylphenol

    8. 2,6-bis(1-methylethyl)phenol

    9. Ampofol

    10. Rapinovet

    11. Phenol, 2,6-bis(1-methylethyl)-

    12. 2,6-di(propan-2-yl)phenol

    13. Propofolum

    14. Recofol

    15. Ivofol

    16. Propofol-lipuro

    17. Pofol

    18. Ici 35868

    19. 2,6-diisopropyl Phenol

    20. Diprifusor

    21. Diprofol

    22. Propovan

    23. Phenol, 2,6-diisopropyl-

    24. Diprivan 10

    25. Ici-35868

    26. Lipuro

    27. Nsc 5105

    28. Ici 35,868

    29. 2,6-bis(propan-2-yl)phenol

    30. 2,6-diisopropyl-phenol

    31. Ici35,868

    32. Mfcd00008885

    33. Chembl526

    34. Yi7vu623sf

    35. Chebi:44915

    36. Nsc5105

    37. 2,6-di-iso-propylphenol-d18

    38. Phenol, 2,6-bis(1-methylethyl)

    39. Nsc-5105

    40. Ici 35-868

    41. Propofolum [latin]

    42. Ncgc00015389-08

    43. Aquafol

    44. Cas-2078-54-8

    45. Dsstox_cid_3523

    46. Dsstox_rid_77063

    47. Dsstox_gsid_23523

    48. Diprivan Injectable Emulsion

    49. 2,6 Diisopropylphenol

    50. Dipravan

    51. Propoven

    52. Aquafo

    53. Propofol Idd-d

    54. Diprivan (tn)

    55. Smr000059151

    56. Ccris 9000

    57. Propofol(2,6-diisopropylphenol)

    58. Hsdb 7123

    59. 2, 6-diisopropylphenol

    60. Sr-01000075468

    61. Einecs 218-206-6

    62. 2,6-bis(isopropyl)phenol

    63. Unii-yi7vu623sf

    64. Brn 1866484

    65. Dds-04f

    66. Ghl.pd_mitscher_leg0.558

    67. Ai3-26295

    68. Propofol Solution

    69. Propofol [usan:usp:inn:ban]

    70. Propofol (diprivan)

    71. Zd-0859

    72. Phenol,6-diisopropyl-

    73. Propofol [hsdb]

    74. Propofol [usan]

    75. Propofol [inn]

    76. Propofol [jan]

    77. Propofol [mi]

    78. Propofol [vandf]

    79. Prestwick0_000931

    80. Prestwick1_000931

    81. Prestwick2_000931

    82. Prestwick3_000931

    83. 2,6-di Isopropyl Phenol

    84. Propofol [mart.]

    85. 2,6-dipropan-2-ylphenol

    86. Biomol-nt_000248

    87. Lopac-d126608

    88. Propofol [usp-rs]

    89. Propofol [who-dd]

    90. Diisopropylphenol (related)

    91. Propofol (jan/usp/inn)

    92. Lopac0_000437

    93. Schembl36245

    94. Bspbio_000862

    95. 4-06-00-03435 (beilstein Handbook Reference)

    96. Mls001066348

    97. Mls001335999

    98. Mls002454360

    99. Bidd:gt0436

    100. Propofol [green Book]

    101. Spectrum1505022

    102. Spbio_003031

    103. 2,6-diisopropylphenol, 97%

    104. Propofol [ep Impurity]

    105. Propofol [orange Book]

    106. Bpbio1_000950

    107. Bpbio1_000969

    108. Gtpl5464

    109. Phenol,6-bis(1-methylethyl)-

    110. Propofol [ep Monograph]

    111. Propofol [usp Impurity]

    112. Dtxsid6023523

    113. Propofol [usp Monograph]

    114. Ketafol Component Propofol

    115. Propofol 1.0 Mg/ml In Methanol

    116. 2,6-diisopropylphenol, >=97%

    117. 3f33

    118. 3p50

    119. Hms1570l04

    120. Hms2089o21

    121. Hms2094e17

    122. Hms2097l04

    123. Hms2231e16

    124. Hms3259e03

    125. Hms3261g16

    126. Hms3369i16

    127. Hms3714l04

    128. Pharmakon1600-01505022

    129. Zinc968303

    130. Albb-036351

    131. Bcp02920

    132. Hy-b0649

    133. Tox21_110134

    134. Tox21_201371

    135. Tox21_303225

    136. Tox21_500437

    137. Ac8633

    138. Bdbm50058046

    139. Nsc758909

    140. Phenol, 2, 6-bis(1-methylethyl)-

    141. Akos009159417

    142. Tox21_110134_1

    143. Ac-2038

    144. Am90311

    145. Ccg-204529

    146. Cs-w020057

    147. Db00818

    148. Lp00437

    149. Nc00449

    150. Nsc-758909

    151. Sdccgmls-0318084.p029

    152. Sdccgsbi-0050422.p002

    153. 2,6-diisopropylphenol; Propofol

    154. Mls-0318084

    155. Ncgc00015389-01

    156. Ncgc00015389-02

    157. Ncgc00015389-03

    158. Ncgc00015389-04

    159. Ncgc00015389-05

    160. Ncgc00015389-06

    161. Ncgc00015389-07

    162. Ncgc00015389-09

    163. Ncgc00015389-10

    164. Ncgc00015389-11

    165. Ncgc00015389-14

    166. Ncgc00015389-17

    167. Ncgc00091538-01

    168. Ncgc00091538-02

    169. Ncgc00091538-03

    170. Ncgc00091538-04

    171. Ncgc00091538-05

    172. Ncgc00091538-06

    173. Ncgc00257228-01

    174. Ncgc00260670-01

    175. Ncgc00261122-01

    176. As-13299

    177. Sy013479

    178. 2,6-diisopropylphenol, Analytical Standard

    179. Bcp0726000298

    180. Mls-0318084.p017

    181. Ab00513968

    182. D0617

    183. Eu-0100437

    184. C07523

    185. D00549

    186. Ab00513968-07

    187. Ab00513968_08

    188. A814898

    189. D126608

    190. Q422740

    191. Q-201631

    192. Sr-01000075468-1

    193. Sr-01000075468-4

    194. Sr-01000075468-6

    195. Brd-k82255054-001-03-5

    196. Brd-k82255054-001-08-4

    197. Propofol, British Pharmacopoeia (bp) Reference Standard

    198. Propofol, European Pharmacopoeia (ep) Reference Standard

    199. Z1245735300

    200. Propofol, United States Pharmacopeia (usp) Reference Standard

    201. Propofol, Pharmaceutical Secondary Standard; Certified Reference Material

    202. Propofol For Peak Identification, European Pharmacopoeia (ep) Reference Standard

    203. Propofol Solution, 1.0 Mg/ml In Methanol, Ampule Of 1 Ml, Certified Reference Material

    204. 113981-41-2

    2.4 Create Date
    2005-03-25
    3 Chemical and Physical Properties
    Molecular Weight 178.27 g/mol
    Molecular Formula C12H18O
    XLogP33.8
    Hydrogen Bond Donor Count1
    Hydrogen Bond Acceptor Count1
    Rotatable Bond Count2
    Exact Mass178.135765193 g/mol
    Monoisotopic Mass178.135765193 g/mol
    Topological Polar Surface Area20.2 Ų
    Heavy Atom Count13
    Formal Charge0
    Complexity135
    Isotope Atom Count0
    Defined Atom Stereocenter Count0
    Undefined Atom Stereocenter Count0
    Defined Bond Stereocenter Count0
    Undefined Bond Stereocenter Count0
    Covalently Bonded Unit Count1
    4 Drug and Medication Information
    4.1 Drug Information
    1 of 4  
    Drug NameDiprivan
    PubMed HealthPropofol (Injection)
    Drug ClassesSedative-Hypnotic
    Drug LabelFor IV Administration OnlyRx OnlyStrict aseptic technique must always be maintained during handling. Diprivan Injectable Emulsion is a single-use parenteral product which contains 0.005% disodium edetate to inhibit the rate of growth of microorgani...
    Active IngredientPropofol
    Dosage FormInjectable
    RouteInjection
    Strength10mg/ml
    Market StatusPrescription
    CompanyFresenius Kabi Usa

    2 of 4  
    Drug NamePropofol
    PubMed HealthPropofol (Injection)
    Drug ClassesSedative-Hypnotic
    Drug LabelPropofol injectable emulsion is a sterile, nonpyrogenic emulsion containing 10 mg/mL of propofol suitable for intravenous administration. Propofol is chemically described as 2,6-diisopropylphenol and has a molecular weight of 178.27. The structural a...
    Active IngredientPropofol
    Dosage FormInjectable
    Routeinjection; Injection
    Strength10mg/ml
    Market StatusTentative Approval; Prescription
    CompanyHospira; Teva Pharms Usa; Gensia Sicor Pharms; Baxter Hlthcare; Esi Lederle

    3 of 4  
    Drug NameDiprivan
    PubMed HealthPropofol (Injection)
    Drug ClassesSedative-Hypnotic
    Drug LabelFor IV Administration OnlyRx OnlyStrict aseptic technique must always be maintained during handling. Diprivan Injectable Emulsion is a single-use parenteral product which contains 0.005% disodium edetate to inhibit the rate of growth of microorgani...
    Active IngredientPropofol
    Dosage FormInjectable
    RouteInjection
    Strength10mg/ml
    Market StatusPrescription
    CompanyFresenius Kabi Usa

    4 of 4  
    Drug NamePropofol
    PubMed HealthPropofol (Injection)
    Drug ClassesSedative-Hypnotic
    Drug LabelPropofol injectable emulsion is a sterile, nonpyrogenic emulsion containing 10 mg/mL of propofol suitable for intravenous administration. Propofol is chemically described as 2,6-diisopropylphenol and has a molecular weight of 178.27. The structural a...
    Active IngredientPropofol
    Dosage FormInjectable
    Routeinjection; Injection
    Strength10mg/ml
    Market StatusTentative Approval; Prescription
    CompanyHospira; Teva Pharms Usa; Gensia Sicor Pharms; Baxter Hlthcare; Esi Lederle

    4.2 Therapeutic Uses

    Propofol is indicated for the induction of general anesthesia. It is also indicated for the maintenance of anesthesia utilizing balanced techniques with other appropriate agents such as opioids and inhalation anesthetics.

    MICROMEDEX Thomson Health Care. USPDI - Drug Information for the Health Care Professional. 22nd ed. Volume 1. MICROMEDEX Thomson Health Care, Greenwood Village, CO. 2002. Content Reviewed and Approved by the U.S. Pharmacopeial Convention, Inc., p. 2466

    Propofol is indicated for the sedation in critically ill patients confined to intensive care units.

    MICROMEDEX Thomson Health Care. USPDI - Drug Information for the Health Care Professional. 22nd ed. Volume 1. MICROMEDEX Thomson Health Care, Greenwood Village, CO. 2002. Content Reviewed and Approved by the U.S. Pharmacopeial Convention, Inc., p. 2466

    Propofol has successfully controlled seizures in status epilepticus.

    Ellenhorn, M.J., S. Schonwald, G. Ordog, J. Wasserberger. Ellenhorn's Medical Toxicology: Diagnosis and Treatment of Human Poisoning. 2nd ed. Baltimore, MD: Williams and Wilkins, 1997., p. 1181

    Propofol appears to have significant antiemetic action and is a good choice for sedation or anesthesia in patients at high risk for nausea and vomiting.

    Hardman, J.G., L.E. Limbird, P.B., A.G. Gilman. Goodman and Gilman's The Pharmacological Basis of Therapeutics. 10th ed. New York, NY: McGraw-Hill, 2001., p. 345

    4.3 Drug Warning

    Compromised cardiovascular function may be aggravated by cardiovascular-depressant and hypotensive effects.

    MICROMEDEX Thomson Health Care. USPDI - Drug Information for the Health Care Professional. 22nd ed. Volume 1. MICROMEDEX Thomson Health Care, Greenwood Village, CO. 2002. Content Reviewed and Approved by the U.S. Pharmacopeial Convention, Inc., p. 2467

    Caution is also recommended in geriatric, debilitated, and/or hypovolemic patients, because they may require lower induction and maintenance doses.

    MICROMEDEX Thomson Health Care. USPDI - Drug Information for the Health Care Professional. 22nd ed. Volume 1. MICROMEDEX Thomson Health Care, Greenwood Village, CO. 2002. Content Reviewed and Approved by the U.S. Pharmacopeial Convention, Inc., p. 2468

    Substantial decreases in mean arterial pressure and cerebral perfusion may occur in patients with existing impaired cerebral circulation or increased intracranial pressure.

    MICROMEDEX Thomson Health Care. USPDI - Drug Information for the Health Care Professional. 22nd ed. Volume 1. MICROMEDEX Thomson Health Care, Greenwood Village, CO. 2002. Content Reviewed and Approved by the U.S. Pharmacopeial Convention, Inc., p. 2468

    Rarely, a clinical syndrome including bronchospasm, erythema, and hypotension has occured shortly after administration of propofol, and sequelae including anoxic brain damage and death have been reported. /SRP: May be from metabisulfite./

    MICROMEDEX Thomson Health Care. USPDI - Drug Information for the Health Care Professional. 22nd ed. Volume 1. MICROMEDEX Thomson Health Care, Greenwood Village, CO. 2002. Content Reviewed and Approved by the U.S. Pharmacopeial Convention, Inc., p. 2468

    For more Drug Warnings (Complete) data for PROPOFOL (17 total), please visit the HSDB record page.

    4.4 Drug Indication

    Used for induction and/or maintenance of anaesthesia and for management of refractory status epilepticus.

    FDA Label

    5 Pharmacology and Biochemistry
    5.1 Pharmacology

    Propofol is a sedative-hypnotic agent for use in the induction and maintenance of anesthesia or sedation. Intravenous injection of a therapeutic dose of propofol produces hypnosis rapidly with minimal excitation, usually within 40 seconds from the start of an injection (the time for one arm-brain circulation).

    5.2 MeSH Pharmacological Classification

    Anesthetics, Intravenous

    Ultrashort-acting anesthetics that are used for induction. Loss of consciousness is rapid and induction is pleasant, but there is no muscle relaxation and reflexes frequently are not reduced adequately. Repeated administration results in accumulation and prolongs the recovery time. Since these agents have little if any analgesic activity, they are seldom used alone except in brief minor procedures. (From AMA Drug Evaluations Annual, 1994, p174) (See all compounds classified as Anesthetics, Intravenous.)

    Hypnotics and Sedatives

    Drugs used to induce drowsiness or sleep or to reduce psychological excitement or anxiety. (See all compounds classified as Hypnotics and Sedatives.)

    5.3 FDA Pharmacological Classification
    5.3.1 Active Moiety
    PROPOFOL
    5.3.2 FDA UNII
    YI7VU623SF
    5.3.3 Pharmacological Classes
    General Anesthetic [EPC]; General Anesthesia [PE]
    5.4 ATC Code

    N01AX10

    S76 | LUXPHARMA | Pharmaceuticals Marketed in Luxembourg | Pharmaceuticals marketed in Luxembourg, as published by d'Gesondheetskeess (CNS, la caisse nationale de sante, www.cns.lu), mapped by name to structures using CompTox by R. Singh et al. (in prep.). List downloaded from https://cns.public.lu/en/legislations/textes-coordonnes/liste-med-comm.html. Dataset DOI:10.5281/zenodo.4587355

    N - Nervous system

    N01 - Anesthetics

    N01A - Anesthetics, general

    N01AX - Other general anesthetics

    N01AX10 - Propofol

    5.5 Absorption, Distribution and Excretion

    Absorption

    Rapid - time to onset of unconsciousness is 15-30 seconds, due to rapid distribution from plasma to the CNS. Distribution is so rapid that peak plasma concentrations cannot be readily measured. Duration of action is 5-10 minutes.

    Route of Elimination

    It is chiefly eliminated by hepatic conjugation to inactive metabolites which are excreted by the kidney.

    Volume of Distribution

    60 L/kg [healthy adults]

    Clearance

    23 - 50 mL/kg/min

    1.6 - 3.4 L/min [70 Kg adults]

    The initial apparent volume of distribution is 13 to 76 L/kg.

    MICROMEDEX Thomson Health Care. USPDI - Drug Information for the Health Care Professional. 22nd ed. Volume 1. MICROMEDEX Thomson Health Care, Greenwood Village, CO. 2002. Content Reviewed and Approved by the U.S. Pharmacopeial Convention, Inc., p. 2467

    Propofol is rapidly and extensively distributed in the body. It crosses the blood-brain barrier quickly, and its short duration of action is due to rapid redistribution from the CNS to other tissues, high metabolic clearance and high lipophilicity.

    MICROMEDEX Thomson Health Care. USPDI - Drug Information for the Health Care Professional. 22nd ed. Volume 1. MICROMEDEX Thomson Health Care, Greenwood Village, CO. 2002. Content Reviewed and Approved by the U.S. Pharmacopeial Convention, Inc., p. 2467

    Approximately 70% of a dose is excreted in the urine within 24 hours after administration, and 90% is excreted within 5 days. Clearance of propofol ranges from 1.6 to 3.4 liters per minute in healthy 70 kg patients. As the age of the patient increases, total clearance of propofol may decrease. Clearance rates of 1.4 to 2.2 liters per minute in patients 18 to 35 years of age have been reported, in contrast to clearance rates of 1.0 to 1.8 liters per minute in patients 65 to 80 years of age.

    MICROMEDEX Thomson Health Care. USPDI - Drug Information for the Health Care Professional. 22nd ed. Volume 1. MICROMEDEX Thomson Health Care, Greenwood Village, CO. 2002. Content Reviewed and Approved by the U.S. Pharmacopeial Convention, Inc., p. 2467

    The pharmacokinetics of propofol were best described by a three-compartment model. Weight was found to be a significant covariate for elimination clearance, the two intercompartmental clearances, and the volumes of the central compartment, the shallow peripheral compartment, and the deep peripheral compartment; power functions with exponents smaller than 1 yielded the best results. The estimates of these parameters for a 70-kg adult were 1.44 l/min, 2.25 l/min, 0.92 l/min, 9.3 l, 44.2 l, and 266 l, respectively. For patients older than 60 yr the elimination clearance decreased linearly. The volume of the central compartment decreased with age. For children, all parameters were increased when normalized to body weight. Venous data showed a decreased elimination clearance; bolus data were characterized by increases in the volumes of the central and shallow peripheral compartments and in the rapid distribution clearance (Cl2) and a decrease in the slow distribution clearance (Cl3). Pharmacokinetics of propofol can be well described by a three-compartment model. Inclusion of age and weight as covariates significantly improved the model. Adjusting pharmacokinetics to the individual patient should improve the precision of target-controlled infusion and may help to broaden the field of application for target-controlled infusion systems.

    PMID:10719952 Schuttler J, Ihmsen H; Anesthesiology 92 (3): 727-38 (2000)

    An iv dose of 14C-propofol (0.47 mg/kg) administered to 6 male volunteers was rapidly eliminated with 88% recovered in the urine in 5 days and <2% in feces. The dose was cleared by metabolism with <0.3% excreted unchanged. The major metabolites were the glucuronic acid conjugate of propofol and the glucuronic acid and sulfate conjugates of its hydroxylated derivative, 2,6-diisopropyl-1,4-quinol. Propofol glucuronide accounted for about 53% of the urinary radioactivity and was the major metabolite in plasma from 30 min post dose. The blood concentration of propofol declined in a biphasic manner from a maximum mean value of 0.44 ug/ml, 2 min after injection. The half-lives of the first and second exponential phases, mean values 5 min and 97 min respectively, varied widely among subjects. A proportion of the dose was cleared slowly, probably due to slow release from less well perfused tissues. Propofol accounted for 94% of the total blood radioactivity at 2 min but only about 6% from 3 to 8 hr post dose. Propofol has a volume of distribution equivalent to about 3 to 4 times body weight, and a mean total body clearance of 2.2 l/min.

    PMID:3261062 Simons P, Cockshott I; Xenobiotica 18 (4): 429-40 (1988)

    5.6 Metabolism/Metabolites

    Hepatically metabolized mainly by glucuronidation at the C1-hydroxyl. Hydroxylation of the benzene ring to 4-hydroxypropofol may also occur via CYP2B6 and 2C9 with subsequent conjugation to sulfuric and/or glucuronic acid. Hydroxypropofol has approximately 1/3 of hypnotic activity of propofol.

    Hepatic; rapidly undergoes glucuronide conjugation to inactive metabolites. An unidentified route of extrahepatic metabolism may also exist, suggested by the fact that propofol clearance exceeds estimated hepatic blood flow.

    MICROMEDEX Thomson Health Care. USPDI - Drug Information for the Health Care Professional. 22nd ed. Volume 1. MICROMEDEX Thomson Health Care, Greenwood Village, CO. 2002. Content Reviewed and Approved by the U.S. Pharmacopeial Convention, Inc., p. 2467

    To determine the cytochrome P450 (CYP) isoforms involved in the oxidation of propofol by human liver microsomes. The rate constant calculated from the disappearance of propofol in an incubation mixture with human liver microsomes and recombinant human CYP isoforms was used as a measure of the rate of metabolism of propofol. The correlation of these rate constants with rates of metabolism of CYP isoform-selective substrates by liver microsomes, the effect of CYP isoform-selective chemical inhibitors and monoclonal antibodies on propofol metabolism by liver microsomes, and its metabolism by recombinant human CYP isoforms were examined. The mean rate constant of propofol metabolism by liver microsomes obtained from 6 individuals was 4.2 (95% confidence intervals 2.7, 5.7) nmol/min/mg protein. The rate constants of propofol by microsomes were significantly correlated with S-mephenytoin N-demethylation, a marker of CYP2B6 (r=0.93, P<0.0001), but not with the metabolic activities of other CYP isoform-selective substrates. Of the chemical inhibitors of CYP isoforms tested, orphenadrine, a CYP2B6 inhibitor, reduced the rate constant of propofol by liver microsomes by 38% (P<0.05), while other CYP isoform-selective inhibitors had no effects. Of the recombinant CYP isoforms screened, CYP2B6 produced the highest rate constant for propofol metabolism (197 nmol/min/nmol P450). An antibody against CYP2B6 inhibited the disappearance of propofol in liver microsomes by 74% /and SRP: reduced in vitro metabolism by blocking CYP 2B6/. Antibodies raised against other CYP isoforms had no effect on the metabolism of propofol. CYP2B6 is predominantly involved in the oxidation of propofol by human liver microsomes.

    Oda Y, Hamaoka N; Br J Clin Pharmacol 51 (3): 281-5 (2001

    Propofol has known human metabolites that include (2S,3S,4S,5R)-6-[2,6-Di(propan-2-yl)phenoxy]-3,4,5-trihydroxyoxane-2-carboxylic acid and 4-hydroxy-propofol.

    S73 | METXBIODB | Metabolite Reaction Database from BioTransformer | DOI:10.5281/zenodo.4056560

    5.7 Biological Half-Life

    Initial distribution phase t1/2α=1.8-9.5 minutes. Second redistirubtion phase t1/2β=21-70 minutes. Terminal elimination phase t1/2γ=1.5-31 hours.

    Terminal elimination half-life is 3 to 12 hours; prolonged administration may result in longer duration.

    MICROMEDEX Thomson Health Care. USPDI - Drug Information for the Health Care Professional. 22nd ed. Volume 1. MICROMEDEX Thomson Health Care, Greenwood Village, CO. 2002. Content Reviewed and Approved by the U.S. Pharmacopeial Convention, Inc., p. 2467

    ...The first-stage elimination half-life (t1/2 beta) of propofol /SRP: administered mixed with lidocaine/ in children was shorter (mean 9.3 +/- 3.8 (s.d.) min) than the values found in adults. This pharmacokinetic alteration may have clinical significance following repeated administration or continuous infusion of propofol.

    PMID:2646847 Valtonen M, et al; Acta Anaesthesiol Scand 33 (2): 152-5 (1989)

    An intravenous dose of 14C-propofol (0.47 mg/kg) /was/ administered to six male volunteers... . ...The half-lives of the first and second exponential phases, mean values 5 min and 97 min respectively, varied widely among subjects.

    PMID:3261062 Simons P, Cockshott I; Xenobiotica 18 (4): 429-40 (1988)

    5.8 Mechanism of Action

    The action of propofol involves a positive modulation of the inhibitory function of the neurotransmitter gama-aminobutyric acid (GABA) through GABA-A receptors.

    API SUPPLIERS

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    Bachem AG

    Switzerland

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    Submission : 1994-11-22

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    Certificate Number : CEP 2005-003 - Rev 05

    Issue Date : 2024-09-04

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    Registration Number : 221MF10007

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    Registrant Name : Daewon Pharmaceutical Co., Ltd.

    Registration Date : 2023-02-15

    Registration Number : 20200806-210-J-463(4)

    Manufacturer Name : Bachem SA

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    Midas Pharma

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    Abbott Laboratories

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    Bachem Sa

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    DMF Review : Complete

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    Neuland Laboratories Ltd

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    Zeneca Pharmaceuticals

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    Zeneca Pharmaceuticals

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    Curia Italy Srl

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    Curia Italy Srl

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    Novadel Pharma Inc

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    Novadel Pharma Inc

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    Si Group

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    Si Group

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    Zeon Pharma Industries India Pvt Lt...

    India
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    CPhI India 2024
    Booth #IP-68
    • fda
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    Virtual BoothZeon Pharma is a manufacturer and supplier of APIs & Intermediates.

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    About the Company : Zeon Pharma Industries India Pvt ltd is an ISO & GMP certified manufacturer of Bulk drugs & Intermediate and also supplies our associate manufacturing plant API / Semi finish form...

    Zeon Pharma Industries India Pvt ltd is an ISO & GMP certified manufacturer of Bulk drugs & Intermediate and also supplies our associate manufacturing plant API / Semi finish formulations/Excipients, Phytochemicals/Enzymes & Intermediate and also has a GMP certified Manufacturing facility for Phytochemicals/Herbal extract and Enzymes through our associates.
    Zeon Pharma Industries India Pvt Ltd

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    09

    Curia

    U.S.A
    The Pharmacy Technology
    Not Confirmed
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    Curia

    U.S.A
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    The Pharmacy Technology
    Not Confirmed
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    Virtual Booth Boost your online visibility by uploading your products, APIs, FDFs, intermediates, excipients, and services for free on PharmaCompass. Rank higher among suppliers and expand your reach across the internet efficiently and cost-effectively.
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    About the Company : Curia is a global contract research, development and manufacturing organization (CDMO), offering products and services across the drug development spectrum to help our partners tur...

    Curia is a global contract research, development and manufacturing organization (CDMO), offering products and services across the drug development spectrum to help our partners turn their ideas into real-world impact. We partner closely with pharmaceutical and biotechnology companies to boost business performance and improve patients’ lives. From early discovery and development through manufacturing and commercialization, our suite of custom solutions allows us to tailor every engagement to your precise needs, whether that’s an independent project or an opportunity that cuts across the drug continuum.
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    10

    Hanways Chempharm

    China
    The Pharmacy Technology
    Not Confirmed
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    Hanways Chempharm

    China
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    The Pharmacy Technology
    Not Confirmed
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    • EDQM
    • WHO-GMP
    Virtual Booth Boost your online visibility by uploading your products, APIs, FDFs, intermediates, excipients, and services for free on PharmaCompass. Rank higher among suppliers and expand your reach across the internet efficiently and cost-effectively.
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    About the Company : Hanways Chempharm Co., Limited, the former one is Hubei Hanways Pharchem CO.,Limited, set up in 2009 in Wuhan, China. We are engaged in supplying APIs, pharmaceutical intermediate...

    Hanways Chempharm Co., Limited, the former one is Hubei Hanways Pharchem CO.,Limited, set up in 2009 in Wuhan, China. We are engaged in supplying APIs, pharmaceutical intermediates, and fine chemicals for worldwide markets. With decades of development, now we grow to a leading and outstanding company. We are not just a trading company, but a comprehensive solutions supplier. With our sound knowledge of pharmaceutical business, our advantage is to integrate resources and adapt to all different demands of markets. We are a young but dynamic and energetic company with high efficient and high flexible decision making system.
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    Only 10 entries up to this point, click to access all click full view read-more
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    22-Jan-2021
    17-Oct-2024
    KGS
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    Drugs in Development

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    Amneal Receives U.S. FDA Approval For Propofol Injectable Emulsion Single Dose Vials

    Details:

    Diprivan-Generic (propofol) is approved in the US, which is an intravenous drug commonly used in hospitals for the induction and maintenance of anesthesia and sedation.


    Lead Product(s): Propofol

    Therapeutic Area: Neurology Brand Name: Diprivan-Generic

    Study Phase: ApprovedProduct Type: Small molecule

    Sponsor: Not Applicable

    Deal Size: Not Applicable Upfront Cash: Not Applicable

    Deal Type: Not Applicable August 20, 2024

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    Amneal Pharmaceuticals

    U.S.A
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    Amneal Pharmaceuticals

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    Lead Product(s) : Propofol

    Therapeutic Area : Neurology

    Highest Development Status : Approved

    Partner/Sponsor/Collaborator : Not Applicable

    Deal Size : Not Applicable

    Deal Type : Not Applicable

    DEALS_DEV arrow-down

    Amneal Receives U.S. FDA Approval For Propofol Injectable Emulsion Single Dose Vials

    Details : Diprivan-Generic (propofol) is approved in the US, which is an intravenous drug commonly used in hospitals for the induction and maintenance of anesthesia and sedation.

    Brand Name : Diprivan-Generic

    Molecule Type : Small molecule

    Upfront Cash : Not Applicable

    August 20, 2024

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    Hospira Issues A Voluntary Nationwide Recall For One Lot of Propofol Injectable Emulsion (containing benzyl alcohol), Due To The Potential Presence of V...

    Details:

    Propofol is an intravenous general anesthetic and sedation drug for use in the induction and maintenance of anesthesia or sedation. Propofol Injectable Emulsion is a terminally sterilized (TS) product.


    Lead Product(s): Propofol

    Therapeutic Area: Neurology Brand Name: Propofol-Generic

    Study Phase: ApprovedProduct Type: Small molecule

    Sponsor: Not Applicable

    Deal Size: Not Applicable Upfront Cash: Not Applicable

    Deal Type: Not Applicable August 22, 2022

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    Hospira, Inc.

    U.S.A
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    Hospira, Inc.

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    Lead Product(s) : Propofol

    Therapeutic Area : Neurology

    Highest Development Status : Approved

    Partner/Sponsor/Collaborator : Not Applicable

    Deal Size : Not Applicable

    Deal Type : Not Applicable

    DEALS_DEV arrow-down

    Hospira Issues A Voluntary Nationwide Recall For One Lot of Propofol Injectable Emulsion (containi...

    Details : Propofol is an intravenous general anesthetic and sedation drug for use in the induction and maintenance of anesthesia or sedation. Propofol Injectable Emulsion is a terminally sterilized (TS) product.

    Brand Name : Propofol-Generic

    Molecule Type : Small molecule

    Upfront Cash : Not Applicable

    August 22, 2022

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    Hospira Issues A Voluntary Nationwide Recall For One Lot of Propofol Injectable Emulsion, USP (Containing Benzyl Alcohol), Due To The Potential Presence...

    Details:

    Propofol is an intravenous general anesthetic and sedation drug for use in the induction and maintenance of anesthesia or sedation. Propofol Injectable Emulsion, USP is a terminally sterilized (TS) product.


    Lead Product(s): Propofol

    Therapeutic Area: Neurology Brand Name: Propofol-Generic

    Study Phase: ApprovedProduct Type: Small molecule

    Sponsor: Not Applicable

    Deal Size: Not Applicable Upfront Cash: Not Applicable

    Deal Type: Not Applicable July 13, 2022

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    03

    Hospira, Inc.

    U.S.A
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    Lead Product(s) : Propofol

    Therapeutic Area : Neurology

    Highest Development Status : Approved

    Partner/Sponsor/Collaborator : Not Applicable

    Deal Size : Not Applicable

    Deal Type : Not Applicable

    DEALS_DEV arrow-down

    Hospira Issues A Voluntary Nationwide Recall For One Lot of Propofol Injectable Emulsion, USP (Con...

    Details : Propofol is an intravenous general anesthetic and sedation drug for use in the induction and maintenance of anesthesia or sedation. Propofol Injectable Emulsion, USP is a terminally sterilized (TS) product.

    Brand Name : Propofol-Generic

    Molecule Type : Small molecule

    Upfront Cash : Not Applicable

    July 13, 2022

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    Avet Pharmaceuticals Announces Approval and Launch of Propofol Injectable Emulsion, USP

    Details:

    Propofol injectable emulsion, an AB-rated generic equivalent of DIPRIVAN® (propofol) Injectable Emulsion USP is an intravenous general anesthetic and sedation drug indicated for initiation and maintenance of Monitored Anesthesia Care (MAC) sedation.


    Lead Product(s): Propofol

    Therapeutic Area: Neurology Brand Name: Propofol-Generic

    Study Phase: ApprovedProduct Type: Small molecule

    Sponsor: Not Applicable

    Deal Size: Not Applicable Upfront Cash: Not Applicable

    Deal Type: Not Applicable April 07, 2022

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    Avet Pharmaceuticals

    U.S.A
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    Lead Product(s) : Propofol

    Therapeutic Area : Neurology

    Highest Development Status : Approved

    Partner/Sponsor/Collaborator : Not Applicable

    Deal Size : Not Applicable

    Deal Type : Not Applicable

    DEALS_DEV arrow-down

    Avet Pharmaceuticals Announces Approval and Launch of Propofol Injectable Emulsion, USP

    Details : Propofol injectable emulsion, an AB-rated generic equivalent of DIPRIVAN® (propofol) Injectable Emulsion USP is an intravenous general anesthetic and sedation drug indicated for initiation and maintenance of Monitored Anesthesia Care (MAC) sedation.

    Brand Name : Propofol-Generic

    Molecule Type : Small molecule

    Upfront Cash : Not Applicable

    April 07, 2022

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    Premier Inc. ProvideGx™ Program Partners with Fresenius Kabi to Secure the Supply of Sedation Drug Essential for COVID-19 Care

    Details:

    Premier through its ProvideGx™ program, has partnered with Fresenius Kabi to supply Diprivan® (propofol) injectable emulsion, USP to healthcare providers, helping to stabilize the long-term supply of a medication vital for COVID-19 patient care.


    Lead Product(s): Propofol

    Therapeutic Area: Neurology Brand Name: Diprivan

    Study Phase: ApprovedProduct Type: Small molecule

    Sponsor: Premier

    Deal Size: Undisclosed Upfront Cash: Undisclosed

    Deal Type: Partnership July 13, 2020

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    05

    Fresenius Kabi AG

    Germany
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    Not Confirmed

    Fresenius Kabi AG

    Germany
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    Lead Product(s) : Propofol

    Therapeutic Area : Neurology

    Highest Development Status : Approved

    Partner/Sponsor/Collaborator : Premier

    Deal Size : Undisclosed

    Deal Type : Partnership

    DEALS_DEV arrow-down

    Premier Inc. ProvideGx™ Program Partners with Fresenius Kabi to Secure the Supply of Sedation Dr...

    Details : Premier through its ProvideGx™ program, has partnered with Fresenius Kabi to supply Diprivan® (propofol) injectable emulsion, USP to healthcare providers, helping to stabilize the long-term supply of a medication vital for COVID-19 patient care.

    Brand Name : Diprivan

    Molecule Type : Small molecule

    Upfront Cash : Undisclosed

    July 13, 2020

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    Nanjing Well Pharmaceutical

    China
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    Virtual BoothNanjing Well is focused on R&D, production & sales of Pharmaceutical Excipients & Synthetic Lubricating base oils.

    Dosage Form : Emulsion, Injectable / Parenteral

    Grade : Parenteral, Oral, Topical

    Category : Emulsifying Agents, Parenteral, Solubilizers, Topical

    Brand Name : Oleic Acid

    Application : Emulsifying Agents, Parenteral, Solubilizers, Topical

    Excipient Details : Oleic acid is used as a co-emulsifier in fat emulsion injections and as an emulsifier and transdermal penetration enhancer in topical formulations.

    Pharmacopoeia Ref : USP/EP

    Technical Specs : NA

    Ingredient(s) : Oleic Acid Excipient

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    Nanjing Well Pharmaceutical

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    Virtual BoothNanjing Well is focused on R&D, production & sales of Pharmaceutical Excipients & Synthetic Lubricating base oils.

    Dosage Form : Emulsion, Injectable / Parenteral

    Grade : Parenteral

    Category : Emulsifying Agents, Parenteral, Solubilizers

    Brand Name : Egg Yolk Lecithin

    Application : Emulsifying Agents, Parenteral, Solubilizers

    Excipient Details : Egg yolk lecithin is used as an emulsifier, solubilizer & liposome membrane material in fat emulsions, lipid microspheres, mixed micelles & liposomes.

    Pharmacopoeia Ref : ChP/USP/EP

    Technical Specs : NA

    Ingredient(s) : Egg Yolk Lecithin

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    Nanjing Well Pharmaceutical

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    Virtual BoothNanjing Well is focused on R&D, production & sales of Pharmaceutical Excipients & Synthetic Lubricating base oils.

    Dosage Form : Cream / Lotion / Ointment, Gel, Injectable / Parenteral, Tablet

    Grade : Parenteral, Oral, Topical

    Category : Parenteral, Solubilizers, Topical

    Brand Name : Benzyl Alcohol

    Application : Parenteral, Solubilizers, Topical

    Excipient Details : Benzyl alcohol is used as a bacteriostatic & preservative in parenteral & ophthalmic products. It is widely used in oral & topical formulations.

    Pharmacopoeia Ref : ChP/USP/EP/JP

    Technical Specs : NA

    Ingredient(s) : Benzyl Alcohol

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    Pluviaendo

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    Dosage Form : Injectable / Parenteral

    Grade : Parenteral

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    Brand Name : Soybean Oil

    Application : Parenteral

    Excipient Details : Soybean oil is used as a solvent for common and complex injections.

    Pharmacopoeia Ref : Chp/USP/EP/JP

    Technical Specs : NA

    Ingredient(s) : Soybean Oil

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    United_States_of_America.png
    Propofol (1 kg - 100 kg) API needed in the U.S.A [ENA20879]
    A CDMO that focuses on development and manufacturing of various APIs and finished formulations is looking for suppliers of Propofol (1 kg - 100 kg) API for commercial purposes. The suppliers must support this enquiry with USDMF, GMP & CoA .
    18 Oct 2024

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    18 Oct 2024

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    18 Oct 2024

    Uzbekistan.png
    Various APIs needed in Uzbekistan [ENA17520]
    A company that focuses on research, development & manufacturing of injectables is looking for suppliers of Various APIs for development purposes. The suppliers must support this enquiry with DMF & CoA. 1. Injectable Grade Propofol (500 g) API 2. Injectable Grade Dexmedetomidine HCl (5.9 g) API
    11 Jul 2023

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    11 Jul 2023

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    Reply Comment (8)

    11 Jul 2023

    turkeypng-1602828403png-1622460951png-1622462103.png
    Propofol API needed in Turkey [ENA17190]
    A company that deals in various pharmaceutical products is looking for suppliers of Propofol API for commercial purposes. The suppliers must support this enquiry with CoA.
    30 May 2023

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    30 May 2023

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    30 May 2023

    india-flag.png
    Various APIs needed in India [ENA16334]
    A company that focuses on the manufacturing of liquid injections, dry powder injections, eye, ear and nasal drops is looking for suppliers of Various APIs for development purposes. The suppliers must support this enquiry with CoA. 1. Phytomenadione API 2. Pilocarpine API 3. Polymyxin B Sulfate API 4. Propofol API 5. Triamcinolone Hexacetonide API
    08 Feb 2023

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    08 Feb 2023

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    Reply Comment (9)

    08 Feb 2023

    india-flag.png
    BP/ USP Grade Propofol (MOQ) API needed in India [ENA16279]
    A company that focuses on the development and manufacturing of tablets, capsules, dry powder syrups/ suspensions, ointments, creams, gels and injectables is looking for suppliers of BP/ USP Grade Propofol (MOQ) API for development purposes. The suppliers must support this enquiry with CoA.
    02 Feb 2023

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    02 Feb 2023

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    Reply Comment (5)

    02 Feb 2023

    india-flag.png
    Various APIs needed in India [ENA12916]
    A company that deals in various pharmaceutical products like injections, syrups & hygiene products is looking for suppliers of Various APIs for commercial purpose. The suppliers must support this enquiry with CoA. 1. Mephentermine Sulfate (25 kg) API 2. Sterile Grade Amiodarone (25 kg) API 3. Terlipressin (10 kg) API 4. Propofol (10 kg) API 5. Diclofenac Sodium (25 kg) API 6. Doxofylline (25 kg) API 7. Lincomycin (50 kg) API 8. Calcium Gluconate (25 kg) API 9. Dicyclomine Hydrochloride (25 kg) API 10. Calcium Lactobionate (25 kg) API
    07 Mar 2022

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    07 Mar 2022

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    07 Mar 2022

    Mexico.png
    Propofol (5 kg) API needed in Mexico [ENA11298]
    A company that deals in research & development, production and marketing of 198 products of more than 300 dosage forms is looking for suppliers of Propofol (5 kg) API for development of injectable formulation. The suppliers must support this enquiry with DMF & cGMP.
    04 Sep 2021

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    04 Sep 2021

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    04 Sep 2021

    Brazil.png
    Various APIs needed in Brazil [ENA10423]
    A company with more than 40 years of experience in the pharmaceutical industry that aims to provide a reliable and efficient source of supply is looking for suppliers of Various APIs for development purposes. The suppliers must support this enquiry with CoA. 1. Duloxetine API 2. Dexlansoprazole API 3. Propofol API 4. Lisdexamfetamine Dimesylate API 5. Levothyroxine Sodium API
    15 May 2021

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    15 May 2021

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    15 May 2021

    india-flag.png
    USP Grade Fluorescein & Injectable Grade Propofol APIs needed in India [ENA10247]
    A company that specializes in the development and manufacturing of APIs and finished dosage pharmaceutical formulations is looking for suppliers of USP Grade Fluorescein & Injectable Grade Propofol APIs for both development and commercial purposes. The final market is the US.
    17 Apr 2021

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    17 Apr 2021

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    17 Apr 2021

    Indonesia.png
    EP Grade Propofol (25 kg) API needed in Indonesia [ENA09504]
    A pharmaceutical manufacturing company that specializes in the production of sterile products (liquid and powder), tablets and capsules is looking for suppliers of EP Grade Propofol (25 kg) API for commercial purposes. The suppliers must support this enquiry with GMP, DMF (closed part) and CoA.
    15 Jan 2021

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    15 Jan 2021

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    15 Jan 2021

    Only 10 entries up to this point, click to access all click full view read-more
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    Patents & EXCLUSIVITIES

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    01

    FRESENIUS KABI USA

    PROPOFOL

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    Compamed
    Not Confirmed

    FRESENIUS KABI USA

    U.S.A
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    Compamed
    Not Confirmed

    Patent Expiration Date : 2025-06-01

    PROPOFOL

    US Patent Number : 8476010*PED

    Drug Substance Claim :

    Drug Product Claim :

    Application Number : 19627

    Patent Use Code :

    Delist Requested :

    Patent Use Description :

    Patent Expiration Date : 2025-06-01

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    FRESENIUS KABI USA

    PROPOFOL

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    FRESENIUS KABI USA

    U.S.A
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    Compamed
    Not Confirmed

    Patent Expiration Date : 2024-12-01

    PROPOFOL

    US Patent Number : 8476010

    Drug Substance Claim : Y

    Drug Product Claim : Y

    Application Number : 19627

    Patent Use Code :

    Delist Requested :

    Patent Use Description :

    Patent Expiration Date : 2024-12-01

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