A suppository-base-matrix tablet for time-dependent colon-specific delivery system

Our research has focused on the main design features and release performances of time-dependent colon-specific (TDCS) delivery tablets, which relies on the relative constancy that is observed in the small intestinal transit time of dosage forms. But inflammatory bowel disease（IBD）can affect the transit time, and usually results in watery stool. Compared to the TDCS and wax-matrix TDCS tablet, a promising time-dependent colon-specific delivery system was investigated. In our study, a suppository-base-matrix coated tablet was evaluated. Water soluble suppository-base helps the expansion of tablet, facilitates uniform film dissolution and achives high osmotic pressure. Combining the expansion of carboxymethyl starch sodium (CMS-Na) and the moisture absorption of NaCl, the coated TDCS tablet obtained a burst and targeted drug delivery system. A very good correlation between in vitro drug release and in vivo outcome was observed. This TDCS coated tablet provides a promising strategy to control drug release to the desired lower gastrointestinal region.

Nossa pesquisa focou-se nas principais características de planejamento e de desempenho de liberação cólon-específica tempo-dependente (TDCS) de comprimidos, que leva em conta a constância relativa observada no tempo de trânsito intestinal das formas de dosagem. A doença inflamatória do intestino (IBD) pode afetar o tempo de trânsito e, geralmente, resulta em fezes aquosas. Comparando ao TDCS e a comprimidos TDCS com matriz-cerosa, investigou-se sistema promissor de liberação cólon-específica tempo-dependente. Em nosso estudo, avaliou-se comprimido revestido com matriz base de supositório. A base de supositório solúvel em água auxilia a expansão do comprimido, facilita a dissolução uniforme do filme e atinge alta pressão osmótica. Associando a expansão do carboximetil amido sódico (CMS-Na) à absorção de umidade do NaCl, o comprimido revestido TDCS originou sistema de liberação direcionado e de erupção. Observou-se correlação muito boa entre a liberação in vitro e a in vivo do fármaco. Este comprimido revestido TDCS representa estratégia promissora para o controle da liberação do fármaco na região gastrintestinal mais baixa.

Effect of certain adjuvants on the mass transfer of diclofenac sodium from suppositories

In this investigation, suppositories containing 100 mg of diclofenac sodium were prepared by fusion method. The bases tested were Witepsol H15 and carbowax base [mixture of PEG 6000, 1540 and 400 in a ratio of 4: 3: 3]. Drug was incorporated either untreated, as a solid dispersion or a physical mixture with selected carriers. The carriers selected were surfactants viz sodium and magnesium stearates, in addition to stearic acid. The prepared solid dispersions were evaluated by various instrumental methods as IR analysis, X-ray diffraction, thermal analysis, in addition to determination of partition behavior. The formulated suppositories were tested for physicochemical characteristics, such as weight variation, uniformity of content, hardness, softening and melting points, in addition to kinetics of drug release. Certain selected formulations were evaluated in vivo in human volunteers

Effect of deoxycholic acid, polycarbophil or both on the relative hyperglycemia of rectal insulin suppositories containing sodium salicylate in diabetic rabbits

The effect of insulin [50 u] suppositories containing sodium salicylate [50 mg] without and with 50 mg of either polycarbophil, deoxycholic acid or 50 mg of each on plasma glucose levels of hyperglycemic rabbits was studied. The hypoglycemia of these formulations was determined relative to that produced after s.c. injection of insulin suspension and were 45.6%, 46.7%, 48.2% and 39.5% respectively. Insulin suppositories containing sodium salicylate were effective in reducing plasma glucose levels which steadily decreased and reached 66% of the initial values by the 3rd h.the addition of polycarbophil to insulin suppositories containing sodium salicylate induced faster and higher rate of insulin absorption as indicated by the shorter Tmax and higher Cmax. addition of deoxycholic acid increased non significantly the Tmax MRT, AUC0-7 h of that of insulin suppositories containing sodium salicylate. The incorporation of both polycarbophil and deoxycholic acid in insulin suppositories containing sodium salicylate is not recommended as these additives reduced the Cmax and AUC0-7 h. accordingly, insulin suppositories containing sodium salicylate with and without the addition of polycarbophil or deoxycholic acid may be considered as a good alternative to insulin injection

Pharmaceutical and microbiological aspects of nalidixic acid suppositories

Nalidixic acid was formulated in suppository form using Witepsol H15, Witepsol E15, Novata 75, cocoa butter and polyethylene glycol as bases. The prepared suppositories were evaluated using the following tests: Uniformity of weight and content, disintegration time, differential scanning calorimetry and kinetics of release. The effect of type and concentration of the nonionic surfactants, viz. Tween 80, 60 and 20, Myrj 51 and 53, Brij 58 and 35 and 35 on the rate of drug release from Witepsol H15 was studied. It is worthy to note that maximum release rate [mg%/hour] obtained from plain base [Witepsol H15] was 4.5 while, addition of 10% Tween 80 to this base increased the release rate to 19.36 mg%/hour. The microbiological potency of the suggested formula [90% Witepsol H15 and 10% Tween 80] which was determined using agar diffusion method, showed a marked inhibitory effect on the tested standard strains of Gram positive and negative microorganisms

Bio-pharmaceutical evaluation of tenoxicam suppositories

With the object of reducing hepatic first-pass elimination of tenoxicam, the drug was formulated in suppository form using different suppository bases. The bases used include Witepsols, Suppocires, Novatas in addition to PEGs an cacao butter. The effect of different additives, surfactants and gels, on drug suppository formulation in Witepsol H15 was also investigated. Suppositories containing tenoxicam solid dispersions were also evaluated, using PEG 4000 and 6000, PVP K25, the hydrotropes sodium benzoate and sodium salicylate, urea, lactose, sorbitol, mannitol, and the electrolytes sodium chloride, magnesium carbonate and aluminum hydroxide. The suppositories prepared were evaluated for in vitro drug release, when fresh and on storage. Selected formulae were also evaluated through tenoxicam relative bioavailability and its anti-inflammatory activity compared to indomethacin as reference drug

Evaluation of ketoprofen B-cyclodextrin inclusion complex formulated into tablets, capsules and suppositories

Ketgoprofen beta Cyclodextrin [beta CD] inclusion complexes prepared by co-grinding, freeze drying and evaporation under vacuum were formulated into tablets, capsules and suppositories. The prepared ketoprofen dosage forms were evaluated with regard to their dissolution, behavior and compared to comercial ketoprofen dosage forms. Directly compressed ketoprofen beta -CD tablets showed relatively better dissolution characteristics than a commercial ketoprofen capsule dosage from. Manually filled hard gelatin capsules of either the spray dried complex or the ground mixture showed a very fast dissolution rate compared to the tested commercial ketoprofen capsules. on the other hand, suppositories containing ether the freeze dried complex or the ground mixture gave rise to a relatively faster in vitro release than those containing non-treated ketopfrofen or the tested commercial ketoprofen suppositories