Posted by admin on May 31, 2020 in |
Substances that loose stools and boost bowel movements are laxatives, purgatives, or aperitives. They are used to treat constipation and to stop it. Constipation relates to infrequent or difficult to transfer bowel movements. Often the stool is hard and dry. Other symptoms may include abdominal pain, bloating, and feeling as if the bowel movement has not been fully passed. Hemorrhoid’s anal fissure or fecal impaction may be complications from constipation. It is a common gastrointestinal functional disorder. IBS is considered to be a complex condition with physiological and psychosocial elements in which stimuli from the central nervous system modulates altered bowel motility or sensation. Medical treatments for constipation include the provision of bulk laxatives, osmotic agents, stimulants, lubricants, and neuromuscular agents. Animal models are important tools in experimental medical science to understand the pathological process of human diseases. Animal models include drug-induced constipation in rat model, canine slow transit constipation model, low-fiber diet-induced constipation in rats, gastrointestinal motility test, castor oil-induced enter pooling. Gastrointestinal motility depicts the muscle contraction...
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Posted by admin on May 31, 2020 in |
Transdermal delivery of therapeutics has been identified by scientific researchers as an alternative choice of drug administration, owing to its unique and tremendous benefit over conventional and oral administrations, but its exploration has been limited because of the “skin barricade” as its major challenge. A special formulation that is capable of meeting up and overcoming its associated challenges is required. Nanotechnology is already established as one of the developing areas of technology, and its application in drug delivery has proven overwhelming success. Nanoemulsions are unique nanotechnological formulations that represent a novel drug delivery system towards resolving pharmaceutical challenges as well as improves dermal and transdermal drug delivery. Since the majority of novel drug candidates, especially those phyto-pharmaceutically discovered, are of less solubility and bioavailability, their pharmaceutical applications have been underexplored. This study aims at presenting nanoemulsion as a novel formulation capable of solving undesirable pharmaceutical challenges such as toxicity, first-pass metabolic effect, drug solubility, and bioavailability. Its potential as an exclusive nanocarrier that mobilizes and promotes transdermal therapeutic delivery...
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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...
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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...
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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...
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