Posted by admin on May 31, 2020 in |
The reaction of 5- (2- chlorophenyl)- 7- nitro- 3H- 1, 4-benzodiazepin-2-thione (I) with glycine (A) by means of Na2CO3 in refluxing ethanol in water gives 2-carboxymethylamino-7-nitro-5-(2-chlorophenyl)-3H-1, 4-benzodiazepine(II), which is cyclized by means of dicyclohexylcarbodiimide in methylene chloride to afford 8-nitro-(2-chlorophenyl)-1,2-dihydro-1H,4H-imidazo[1, 2-a] [1, 4]benzodiazepin-1-one (III). The reaction of (III) with dimethylformamide diethylacetal (B) by means of triethylamine in benzene yields 8-nitro-2-(dimethylaminomethylene)-6-(2-chlorophenyl)-1,2-dihydro-1H, 4H-imidazo[1,2a] [1,4]benzodiazepin-1-one(IV), which is treated with N-methylpiperazine (C) in refluxing toluene result 8-nitro-(2-chlorophenyl)-2-(N-methylpiperazin-1- ylmethylene)- 1, 2- dihydro- 1H, 4H- imidazo[1,2a] [1,4] benzodiazepin-1-one (V). This compound is finally treated with methanesulfonic acid. The condensation of 6-(2-chlorophenyl)-1,2-dihydro-8-nitro-1H, 4H-imidazo [1,2-a] [1,4] benzodiazepin-1one, with 1(dimethoxymethyl)-4-methylpiperazine (II) gives the free base of Loprazolam Mesylate (III), which is then treated with methanesulfonic acid. 5-aryl-1, 3-di-hydro-7-substitued-2H-1,4-benzodiazepine-2-thiones were condensed with glycine in aqueous ethanol to give the previously unreported amino acid. Dicyclohexylcarbodiimide in dry methylenechloride cyclized. These acids to the imidazolobenzodiazepines which were found to oil unstable to hydrolytic...
Read More
Posted by admin on May 31, 2020 in |
Oral route has always been the preferred route of drug administration in many diseases. This route is limited to those drugs molecules that are permeable across the gastric mucosa and are sparingly soluble. Solubility is an important parameter to achieve the desired concentration of drug in systemic circulation for therapeutic response. As a consequence of modern drug discovery techniques, there has been a steady increase in the number of new active lipophilic compounds that are poorly water-soluble. It is a challenge for a scientist to convert those molecules into an orally administered formulation with sufficient bioavailability. Improving oral bioavailability of poorly water-soluble drugs using self micro emulsifying drug delivery systems (SMEDDS) appears most promising. Currently, various technologies are available to deal with insoluble drugs such as micronization, solid dispersions, complex formation, etc. Among the several approaches, SMEDDS has emerged as a distinctive approach used to improve the bioavailability of hydrophobic drugs. SMEDDS is isotropic mixture of drug, surfactants, cosurfactants, and oil which have unique ability to form fine o/w...
Read More
Posted by admin on May 31, 2020 in |
Candesartan cilexetil is a novel, potent, and highly selective non-peptide angiotensin II type 1 receptor blocker. It is a hydrophobic drug that belongs to the BCS Class II drug. For enhancement, the bioavailability and quick systemic action of Candesartan cilexetil a novel formulation of buccal (effervescent) tablet, was designed. Preformulation is an important step in the rational formulation of an active pharmaceutical ingredient (API). Micromeritics properties: Bulk density (du), Tapped density (db), Compressibility Index (% C) and sieve analysis was performed in order to determine the best excipients to be used in the formulation development of Candesartan cilexetil (effervescent) tablets. Results show that Candesartan Cilexetil has a fair flow and compressibility properties (du 0.8 g/mL, db 0.7 g/mL, % C 12.5, and sieve analysis time 4.5 min. HPLC method for estimation of Candesartan cilexetil shows linearity ( R2 = 1) and specific with no interference of excipients. Solubility studies reveal that it soluble at pH 6.8 and 7.5 in phosphate buffer. The ability of a material to absorb water...
Read More
Posted by admin on May 31, 2020 in |
Even though numerous herbal preparations have been recommended in alternative systems of medicine against hepatic disorders, many of them cause severe toxicity upon prolonged use. Volvariella volvacea (Bull.: Fr.) Singer is a highly nutritious mushroom that can be incorporated into the regular diet without the fear of side effects. The protective effect of the aqueous ethanol extract of V. volvacea mycelia was evaluated against acetaminophen (APAP) induced hepatic damage in Wistar rats. A single dose of APAP (3 g/kg, p.o.) was used for inducing hepatic damage. The extract was administrated orally at doses of 250 and 500 mg/kg, once daily for 7 days. Treatment with APAP (3 g/kg) increased the activities of liver function enzymes serum glutamate oxaloacetate transaminase (SGOT), serum glutamate pyruvate transaminase (SGPT) and alkaline phosphatase (ALP). APAP also reduced the activities of superoxide dismutase (SOD), catalase (CAT), and glutathione peroxidase (GPx) and enhanced lipid peroxidation in liver tissue. Administration of V. volvacea extract (500 mg/kg, p.o.) decreased the activities of SGPT, SGOT, and ALP. It also...
Read More
Posted by admin on May 31, 2020 in |
Prostate cancer is one of the most important cancer in men. In most cases, prostate cancer confirmed by histological and transrectal biopsy for the examination of prostatic tissue. Metastatic prostate cancer is second leading cause of death from cancer. Androgen deprivation therapy is common treatment in men with prostate cancer that may cause fatigue, increased body fatness, and loss of lean body tissue. Abiraterone acetate improved overall survival in Metastatic Castration-Resistant Prostate Cancer. Enzalutamide is a novel anti-androgen that is approved for the treatment of Metastatic Castration-Resistance Prostate Cancer after taxane-based chemotherapy. The management options include surveillance, radiotherapy, and radical prostatectomy, but there is no evidence base to evaluate the benefits of each approach. Advanced prostate cancer is managed by hormonal therapy. Active surveillance is a novel and fascinating approach to distinguish between patients who are at higher risk and need active therapy and patients who are at low risk for disease progression. This review provides a short overview of the various approaches of prostate...
Read More
