4. Drug and Excipients Profile: 4.1 Drug Profile:62 4.1.1 Carvedilol phosphate: Synonyms: Carvedilol; Carvedilolum [Latin] Chemical Formula: C24H26N2O4 Chemical Name (IUPAC): (2RS)-1-(9H-Carbazol-4-yloxy)-3-[[2-(2-methoxyphenoxy)ethyl]amino]propan-2-ol phosphate salt (1:1) hemihydrate. CAS Registry Number: 72956-09-3 Structural Formula: Description: Carvedilol phosphate is a nonselective β-adrenergic blocking agent with α1-blocking activity. Carvedilol phosphate is a white to almost-white solid with a molecular weight of 513.5 (406.5 carvedilol free base) and a molecular formula of C24H26N2O4•H3PO4•1/2 H2O. Half life: 6-8 h Melting Range: 148-150 °C Log P: 3.5 pKa: 7.4 BCS Class: Class II drug Bioavailability: 25-35% Solubility: Free soluble …show more content…
Povidones with K-values equal to or lower than 30 are manufactured by spray-drying and occur as spheres. Povidone K-90 and higher K-value povidones are manufactured by drum drying and occur as plates. The USP 28 describes povidone as a synthetic polymer consisting essentially of linear 1-vinyl-2-pyrrolidinone groups, the differing degree of polymerization of which results in polymers of various molecular weights. It is characterized by its viscosity in aqueous solution, relative to that of water, expressed as a K-value, in the range 10–120. The K-value is calculated using Fikentscher’s …show more content…
The ammonium groups are present as salts and give rise to pH-independent permeability of the polymers. Both polymers are water-insoluble, and films prepared from Eudragit RL are freely permeable to water, whereas, films prepared from Eudragit RS are only slightly permeable to water. They are available as 12.5% ready-to-use solutions in propan-2-ol–acetone (60 : 40). Solutions are colorless or slightly yellow in color, and may be clear or slightly turbid; they have an odor characteristic of the solvents. Solvent-free granules (Eudragit RL 100 and Eudragit RS 100) contain ≥97% of the dried weight content of the
6. The solubility of the solids were tested using a micro tray, by placing them in water and oil to observe their polarity,
(Q3:Purification) Product was purified via crystallization and using ice-cold water ensured product remain intact while impurities were washed into the filtrated liquid. The results gathered were measured against already scientifically established melting points of the product, the standard solutions provided, and retention factor (Rf) values to conclude the unknown nucleophile used in the beginning was 4-methoxyphenyl.
Methaqualone, is also referred to as Disco Biscuits, Down And Dirties, Jekyll-and-Hyde, Joe Fridays, Lemmon 714, Lemons, Lennon's, Lovers, Ludes, Mandies, Mandrake, Q, Qua, Quack, Quad, Quaaludes, Soaper, Supper, Vitamin Q, The Love Drug, Wallbangers, Whore Pills, and Sopor. This list of street names for the drug goes on and on.
The light yellow precipitate was collected by suction filtration using a Hirsch funnel. The product was washed with two 1-mL portions of cold methanol followed by two 1-mL portions of diethyl ether. The product was dried in the oven at 110°C. The IR spectrum as a KBr pellet was obtained for the product and inosine for analysis.
4-(2-aminoethyl)morpholine (742 mg, 5.7 mmol) and acetone (10 mL) were mixed together on ice, while a mixture of 4-chlorobenzoyl chloride (0.55 ml, 4.3 mmol) in acetone (2.5 mL) was added drop-wise for 10 minutes. Then, the mixture was mixed on ice for an addition five minutes, then for ten minutes at room temperature. Diethyl ether (10 mL) was added to the mixture and the resultant white precipitate was filtered. The product was recrystallized using ethanol (95%) and filtered. After drying, the crystals were dissolved in a mixture of dichloromethane (10 mL) and ammonia (concentrated, 10 mL). The organic layer was removed and the aqueous layer was washed with dichloromethane (10 mL). The combined organic layer was dried with sodium sulfate (anhydrous) and evaporated, which afforded a white powder (0.68 g, 66%) mp: 130-133°C; 1H NMR (400 MHz, CDCl3) δ (ppm) 7.71 (d, 2H), 7.41 (d, 2H), 6.87 (s, 1H), 3.73 (t, 4H), 3.53 (q, 2H), 2.60 (t, 2H), 2.5 (t, 4H); IR (ATR) υmax (cm-1) 3277, ~2900, 1633, 1595, 1546, 1486, 1469, 1461, 1142, 1116,
As I have mentioned, inhaled nitric oxide, epoprostenol, iloprost, and sildenafil are the common treatment for pulmonary hypertension that I would encounter in the hospital where I am currently employed. Nitric oxide and iloprost are administered through inhalation, epoprostenol by continuous intravenous infusion, and sildenafil is taken orally. The main advantage of inhaled route for the treatment of PH is the direct delivery of drug to the target organ thus, reducing the systemic side effects (Hill, Preston, & Roberts, 2015). It also improves the gas exchange by dilating the vessels supplying the ventilated areas (Hill et al., 2015).
Materials. The following chemicals are purchased and used as received. Cadmium oxide (CdO, 99.99 %), and potassium sulfide (K2S, 95 %) are obtained from Strem Chemicals. 1-octadecene (90 %), 3-mercaptopropionic acid (99 %), and α-terpineol (97 %) are purchased from Acros Organics. Selenium powder (Se, 99.99 %), oleic acid (OLAC, 90 %), oleylamine (OLAM, 70 %) and acetic acid (99.7 %) are purchased from Sigma-Aldrich. Toluene (99.9 %), 2-propanol (99.9 %), ethanol (90 %), acetonitrile (99.9 %), and formamide (FA, 99.6 %) are acquired from Fisher Scientific. P25 TiO2 and ethyl cellulose (5 % in toluene and ethanol) are supplied by Evonik Degussa Corporation and TCI, respectively. OLAC, OLAM, and FA are dried using standard procedures.
Atenolol is relatively beta 1 cardioselective blocker having low lipid solubility but no intrinsic sympathomimetic activity and membrane stabilizing activity. Atenolol is used as a first line drug for the management of hypertension,angina, and cardiac arrhythmia. Atenolol is sold as TENORMIN in the UK and wordwide market. The international union of pure and applied chemistry name is -2-{4-[2-Hydroxy-3-(propan-2-ylamino)propoxy]phenyl}acetamide. The m.w. is 266.336 g/mol, and the melting point stands around
The acidic thermoplastic rosin can be isolated from pine trees, and is known to have many properties that could be applied to the production and administrations of active pharmaceutical ingredients (APIs). Rosin is both bio renewable and biodegradable, and research suggests that rosin can be made into many forms, such as films, beads and fibers. These forms can then be used in the controlled release of APIs.
Methyl paraben and propyl paraben occurs as colorless crystals or a white crystalline powder. They are odorless or almost odorless and have a slight burning taste. The parabens are effective antimicrobials over a wide pH range of 4 to 8 and have a broad spectrum of antimicrobial activity (100). Methylparaben is the least active of the parabens; antimicrobial activity increases with increasing chain length of the alkyl moiety (Propyl paraben) but aqueous solubility decreases; therefore a mixture of parabens is frequently used to provide effective preservation(101). Methyl paraben (1 in 400) is more water soluble than propyl paraben (1 in 2500).
Voriconazole (VRZ), a second-generation synthetic triazole fluconazole derivative is designated chemically as (2R, 3S)-2-(2,4-difluorophenyl)-3-(5-fluoro-4-pyrimidinyl)- 1-(1H-1,2,4-triazol-1-yl)-2-butanol (Fig. 1). It was developed for treatment of serious, invasive fungal infections in immune compromised patients [1]. VRZ is active against all Candida species resistant to fluconazole and more recently used for the treatment of candidiasis and aspergillosis infections in skin, wounds, abdomen, kidney, and bladder walls [2, 3].
BREO ELLIPTA is inhalation powder for oral inhalation belonging to the class of inhaled corticosteroids combined with long-acting [[beta].sub.2] agonists (Breo Ellipta, 2013). Thus, Breo Ellipta represents itself a fixed combination of fluticasone furoate (100 mcg/200mcg, ICS) and vilanterol (25 mcg, LABA) (GlaxoSmithKline, 2013).
Polylactic acid polymers (PLA) appear to be a very promising material for use as a
Platinum, HiSPEC 4000, nominally 40% on carbon black, was acquired from Alfa Aesar. Chitosan (Mn ~ 20k, 85% deacetylation, PDI ~ 4) was from Ta Ming Enterprises Co., Ltd., Thailand. Epichlorohydrin (Acros Organics), acetic acid (Sigma-Aldrich), and sodium hydroxide (MERCK) were used as received. Gas diffusion layers (GDL Sigracet GDL 10BB, 420 µm) were purchased from SGL Carbon Group, whereas the 5 wt.% Nafion solution and NR-212 Nafion membrane were from Aldrich and Ion Power, respectively. All other chemicals of analytical grade were used as supplied.
The contents of the aqueous dispersion used for film formation are: dibutyl sebacate, poloxamer 407, magnesium stearate, water with or without different flavorings include 2-acetylpyridine,