effect of binder type and major diluent on the migration and bioavailability of riboflavin sodium phosphate during tablet making

The migration of riboflavin sodium phosphate [RSP] upon drying of its wet granules was studied through the formulation of granules using different diluents [lactose monohydrate and anhydrous dibasic calcium phosphate], different binders of different concentrations; polyvinyl pyrrolidone [PVP k[25]], methylcellulose [MC], hydroxypropylmethyl cellulose [HPMC] and gelatin at different drying temperatures [50°C and 70°C]. The prepared granules were compressed into tablets and evaluated. In vitro drug release from the formulated tablets was performed. In addition, in vivo study was conducted on some selected tablet batches. The results showed that, the granules prepared with dibasic calcium phosphate showed lower migration for the drug than those prepared with lactose. Also, drug migration decreased with increasing the binder concentration and viscosity. The degree of tablet mottling was inversely proportional to the binder concentration. Tablets prepared with 10% w/w gelatin were found to be the least mottled ones. In addition, they showed the least friability percentage, the highest hardness value and the highest disintegration time. Tablets prepared with 0.5% MC showed the highest dissolution rate, however, those prepared with 10% gelatin had the lowest dissolution rate. Generally, increasing the binder concentration resulted in slowing the in vitro drug release from tablets. The in vivo study showed that, tablets prepared with 10% w/w gelatin showed the lowest excretion rate and the highest T[max] [1.5 hours]. Meanwhile, tablets prepared using 0.5% w/w MC exhibited higher excretion rate and T[max] of 0.5 hour

Bioviability of formulated glafenine suppositories in humans

Glafenine hydrochloride was prepared in the form of suppositories using Witepsol H15. Glafenine suppositories were prepared using the coprecipitate of glafenine with Tween 60 [1:1 w/w] to give the equivalence of 200 mg of pure drug and incorporated with Witepsol H15. Suppositories were made using the fusion method. The available commercial br and of glafenine suppository was used for the same investigation. Both commercial br and and the formulated suppositories were subjected to bioavailability study using a group of six adult healthy male volunteers. The urine was collected quantitatively each hour for three hours, then at intervals of 6, 12 and 24 hours. Glafenine in urine was determined spectrophotometrically at 360 nm. It was found that the cumulative amount of glafenine excreted over 24 hours were 32.53, 19.04 and 24.48 mg from prepared glafenine hydrochloride, glafenine-Tween 60 coprecipitate and commercial br and, respectively

Study on the effect of the combination of propranolol hydrochloride and pilocarpine hydrochloride on intraocular pressure of rabbit's eye

Pilocarpine hydrochloride and /or propranolol hydrochloride were formulated in aqueous solutions and gel form using methyl cellulose and sodium carboxymethylcellulose as thickening and gelling agents, respectively. Both formulations were instilled into normal rabbit's eyes and the changes in the intraocular pressure [IOP] were determined. It was found that the action of both drugs on the intraocular pressure was significantly increased in the presence of the added polymers. Moreover, the optimum decrease in IOP was reached in a shorter time with aqueous solution [2 h] and gel form [3 h] than with control drugs without polymer [4 h]. The peak heights of such decrease were in percentage for pilocarpine hydrochloride 7.2, 27.5 and 17.9, for propranolol hydrochloride 12.5, 18.4 and 17.3 and for their mixture 15.4, 15.4, 15.4 and 16 as aqueous solution, aqueous solution with methylcellulose and gel form, respectively. The study showed that the use of propranolol hydrochloride with pilocarpine hydrochloride with pilocarpine hydrochloride in a concentration of 1% each causes a maximal decrease in IOP in presence of methylcellulose as a thickening agent

Treatment of phenylbutazone ulcerogenicity using effervescent granules containing certain adjuvants

The effect of pure phenylbutazone and prepared granules containing the drug in combination with pectin, quercetin, citric acid, tartaric acid and sodium bicarbonate was investigated in course of experimental ulcer lesion. One-day course showed a marked ulcer lesion characterised by large ulcer [2-10 mm] and two animal with 10 mm ulcer in case of pure drug. Prepared granules exhibited a 2-fold less in number of 2-10 mm ulcer and no ulcers of 10 mm and Pauls' index was also decreased. In 3-day course, the number of animals that showed 10 mm. ulcer was increased by 3-fold in case of pure drug than that observed with tested formulation, and Pauls' index was decreased by 32.7%

Influence of microcapsule size on the bioavailability of acetylsalicylic acid

Preparation of ethylcellulose microcapsules containing ASA were achieved. Four microcapsule sizes were separated using standard sieves set. The percent release as well as the bioavailability of each size were studied to get a correlation between in-vitro and in-vivo drug availability. Larger size microcapsules were found to show a lower bio-availability when compared with smaller ones. The same was observed in-vitro. A good correlation between in-vitro and in-vivo data was noticed in testing the dissolution rate of microcapsules alter 15 and 30 min. with percent excretion of ASA after one hour