Effect of methyl branching of C8H18 alkanes and water activity on lipase-catalyzed enantioselective esterification of ibuprofen

The purpose of this research was to study the effect of the methyl branching of a high log P alkane solvent and the water activity in the organic medium on the initial rate and the enantioselectivity of ibuprofen esterification catalyzed by Candida rugosa lipase. Resolution of ibuprofen is important because S-(+)-ibuprofen has the desired pharmacological activity, whereas the R-(-)-enantiomer causes much of the side effects. The Candida rugosa lipase-catalyzed reaction in isooctane at 40ºC and 0.73 water activity gave the best results, both in terms of the initial reaction rate and the enantioselectivity of the reaction. An increase in water activity allowed a higher reaction rate and enantiomeric excess in each of the four solvents. An increase in methyl branching did not necessarily increase the initial reaction rate, but it allowed a higher enantioselectivity, evidenced by an increase in the substrate enantiomeric excess.

Influence of acidic beverage (Coca-Cola) on pharmacokinetics of ibuprofen in healthy rabbits.

The study was aimed at determining the effect of Coca-Cola on the pharmacokinetics of ibuprofen in rabbits. In a cross-over study, ibuprofen was given orally in a dose of 56 mg/kg, prepared as 0.5% suspension in carboxymethyl cellulose (CMC) and blood samples (1 ml) were drawn at different time intervals from 0-12 hr. After a washout period of 7 days, Coca-Cola in a dose of (5 ml/kg) was administered along with ibuprofen (56 mg/kg) and blood samples were drawn from 0-12 hr. To these rabbits, 5 ml/kg Coca-Cola was administered once daily for another 7 days. On 8th day, Coca-Cola (5 ml/kg) along with ibuprofen (56 mg/kg), prepared as a suspension was administered and blood samples (1 ml each) were drawn at similar time intervals. Plasma was separated and assayed for ibuprofen by HPLC technique and various pharmacokinetic parameters were calculated. The Cmax and AUC0-alpha of ibuprofen were significantly increased after single and multiple doses of Coca-Cola, thereby indicating increased extent of absorption of ibuprofen. The results warrant the reduction of ibuprofen daily dosage, frequency when administered with Coca-Cola.

Ibuprofen: Adverse Effects

Ibuprofen is the first member of the class propionic acid introduced in 1969. It is better-tolerated analgesic as compared to aspirin. All members belonging to propionic acid group inhibit prostaglandins, easily absorbed on oral administration, enter brain, synovial fluid and cross placenta, largely metabolized in liver by hydroxylation and glucuronic conjugation excreted in urine as well as in bile. It has analgesic, antipyretic and anti-inflammatory effects. It is commonly used in rheumatoid arthritis, osteoarthritis, and other musculoskeletal disorders. It is useful drug but cannot be considered free of adverse effects, the side effects comprise of milder gastric discomfort, nausea and vomiting, headache, dizziness, blurring of vision, tinnitus, depression, rashes, itching and other hypersensitive phenomena. Anaphylactic shock has also been reported, salt retention and hypertension has also been reported in elderly patients. In our study we noticed 10 male and 25 female patients developing gastric discomfort on prolonged use of ibuprofen. Two females patients have been noted developing analgesic headache. 5 male and 2 female observed nausea. 3 males and 2 females reported dizziness. 2 male patients were observed to have fixed drug eruptions

Estudo comparativo da cinética de dissolução de ibuprofeno em comprimidos de liberação imediata comercializados no Brasil / Comparative study of the dissolution kinetics of ibuprofen in immediate-release tablets of the Brazilian market

Avaliaram-se as características físicas e físico-químicas de diferentes lotes de quatro especialidades farmacêuticas contendo ibuprofeno (produtos A, B, C e D), sob a forma de comprimidos de liberação imediata, disponíveis no mercado nacional e comercializados como similares intercambiáveis, enfatizando-se o estudo comparativo da cinética de dissolução do fármaco. Utilizou-se equipamento para dissolução de formas sólidas de acordo com a USP 23, empregando-se tampão fosfato pH 7,2 como meio de dissolução a 37,0 ñ 0,5 ºC e aparato 1 na velocidade de 150 rpm. Os produtos A e B e os produtos C e D, respectivamente, poderiam, teoricamente, ser considerados equivalentes farmacêuticos, segundo a definição da Food and Drug Administration (FDA-USA)...

Revisäo - O ibuprofeno e seu uso na dismenorréia primária / Review - Ibuprofen and its use in primary dysmenorrhea

Os autores apresentam uma revisäo sobre as propriedades farmacológicas do ibuprofeno, droga antiinflamatória-näo-esteroidal (AINE), e seu emprego na dismenorréia primária (DP), enfermidade de importante aspecto sócio-econômico devido a seus sintomas incapacitantes quando na forma severa. Säo abordados aspectos sobre farmacocinética, farmacodinâmica, indicaçöes clínicas, interaçöes medicamentosas e efeitos adversos da droga, revelando-se o ibuprofeno como o AINE que apresenta, na vigência de seu uso, a menor incidência de distúrbios gastrointestinais quando comparado aos demais AINE. Em relaçäo a seu uso na DP, säo analisados estudos onde compara-se a eficácia do ibuprofeno à eficácia de outros AINES em relaçäo ao alívio dos sintomas dismenorreícos. Conclui-se ser o ibuprofeno, devido à sua ótima eficácia no alívio da dor e sua baixíssima incidência efeitos adversos, e a droga de escolha no tratamento da DP, tendo nesta sua grande indicaçäo

Effect of concentration, pH, and preservative on in vitro transcorneal permeation of ibuprofen and flurbiprofen from non-buffered aqueous drops.

Influence of drug concentration, pH of aqueous drops and some commonly used preservatives on in vitro transcorneal permeation of ibuprofen and flurbiprofen were investigated using goat cornea. Increase in drug concentration in the drops made in normal saline resulted in increase in quantity permeated but decrease in cumulative percent permeation of both drugs. Permeation of each drug from 0.5% drops was maximum at acidic pH (6.4) and decreased with increase in pH of the drops. Normal saline, as a vehicle, favoured permeation of each drug, hence retained in the formulation. Benzalkonium chloride and chlorobutanol enhanced cumulative percent permeation of ibuprofen while benzalkonium chloride and phenyl mercuric nitrate increased permeation of flurbiprofen. Benzalkonium chloride being incompatible with 0.5% drops (pH 6.4) of either drug, chlorobutanol appears suitable for ibuprofen drops and phenyl mercuric nitrate for flurbiprofen drops.

Studying the effect of surfactant on eudragit RS100 microspheres prepared by solvent evaporation technique

Solvent evaporation technique was used to prepare Eudragit RS100 microspheres containing ibuprofen as an example for acidic drugs. The aqueous phase was 0.1 N HCl containing different concentrations of either cetrimide or dioctyl sodium sulfosuccinate [DOSS] as an antiaggregating agent. It was found that the percent of drug content was equal to theoretical drug content on using 0.25, 0.5 or 1% cetrimide. This may be due to that, cetrimide acts as a good transport barrier for dichloromethane, but not for the drug. At the same time the percent of drug content was markedly decreased on using 1.5% cetrimide. That is may be due to the cetrimide micelle formation. The effect of different concentrations of DOSS on the percent of drug content was also studied