[Biopharmaceutical study of para-aminosalicyclic acid tablets].
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The effect of particle size on the time elapsing between administration and loss of righting reflex and % of deaths by determining the LD50 has been studied in mice. The drug used was pentobarbituric acid. In one preparation the particle size was less than 44 mum and in the other preparation it was greater than 297 mum and less than 420 mum. For both preparations a 1% sodium carboxymethylcellulose solution was used as suspending medium. It was found that both the curve for loss of righting reflex and the log dose-response curve, and hence the LD50, were significantly shifted to the right. There is a reflex LRR between the suspended pentobarbituric acid and the equivalent amount of sodium pentobarbital, both in 1% sodium carboxymethylcellulose solution. In reporting LD50 data it is essential not only to state the exact composition of the vehicle (viscosity factor) but also to state the exact particle size or particle size range, because by using increasing particle size the LD50 decreases.
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Hydrophilic-lipophilic properties (water solubility, n-octanol/water partition coefficient, transport across membranes) of some mercaptopurines (6-MP, 6-TG, AZA and a new AZA derivative--metazathioprine (MAZA) were determined. MAZA is the most lipophilic compound due to low aqueous solubility and high n-octanol/water partition coefficient. The fluxes from the donor medium into the membrane and from the membrane into the acceptor medium are highest for MAZA as well. The partition coefficients of the other purines decrease in the order: AZA > 6-TG > 6-MP.
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In the present investigation, an attempt was made to study and compare, analgesic and anti-inflammatory activity produced by four marketed topical diclofenac formulations in order to justify their usefulness in the treatment of pain and inflammation. By using a diffusion cell, in vitro percutaneous permeation studies were carried out to correlate in vivo activity. The in vivo analgesic activity study was performed by tail flick method on Wistar albino rats. The anti-inflammatory activity was performed on rats by carrageenan induced inflammation. It was evident from the study that three among tested three gels; diclofenac permeated effectively through the skin and was able to elicit analgesic and anti-inflammatory responses. The study also indicated the presence of therapeutic inequivalence among the marketed topical formulation and the need of bio equivalency and therapeutic equivalency testing of marketed topical applications meant for therapeutic use.
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