PubMed · 5159811
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F M Polack. 1971. Corneal optical prostheses.. https://doi.org/10.1136/bjo.55.12.838
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The residence time of apomorphine mucoadhesive preparations incorporating 99mTc labeled colloidal albumin in rabbit nasal cavity was evaluated by gamma scintigraphy. This technique was used to compare the nasal clearance of preparations based either on Carbopol 971P((R)) or lactose (control), each with and without apomorphine, or carboxymethylcellulose with apomorphine. The planar 1-min images showed an excipient-dependent progressive migration of radioactivity with time from the nasal cavity to the stomach and intestine. Thirty minutes post insufflation, the percentages of the formulations cleared from the nasal cavity were 47% for lactose, 26% for lactose/apomorphine, 10% for Carbopol 971P((R)), and 3% for both Carbopol 971P((R))/apomorphine and carboxymethylcellulose/apomorphine. Three hours post insufflation, the percentages of the formulations cleared from the nasal cavity were 70% for lactose, 58% for lactose/apomorphine, 24% for Carbopol 971P((R)), 12% for Carbopol 971P((R))/apomorphine, and 27% for carboxymethylcellulose/apomorphine. Apomorphine inhibited nasal mucociliary clearance since migration of the radioactivity administered with apomorphine containing preparations was in all cases slower than that of the corresponding powder without apomorphine. The peak plasma concentration of apomorphine was attained while all the formulations were still within the nasal cavity. The use of mucoadhesive polymers such as Carbopol 971P((R)) or carboxymethylcellulose in nasal dosage forms increases their residence time within the nasal cavity and provides the opportunity for sustained nasal drug delivery.
Adsorption and controlled release of terbinafine hydrochloride (TER-HCl) to and from pH sensitive poly(acrylamide/maleic acid) (P(AAm/MA)) hydrogels were investigated. P(AAm/MA) hydrogels were prepared by irradiating the ternary mixtures of AAm/MA/and water by gamma-rays at ambient temperature. Antifungal drug, TER-HCl containing hydrogels, at different drug to polymer ratios, was prepared by direct adsorption method. The influence of MA content in the gel on the adsorption capacities of hydrogel and the effect of pH on the releasing behavior of TER-HCl from gel matrix were investigated. Terbinafine adsorption capacity of hydrogels are found to increase from 2 to 38 mg TER-HCl per g dry gel with increasing amount of MA in the gel system. In vitro drug release studies in different buffer solutions show that the basic parameters affecting the drug release behavior of hydrogel are the pH of the solution and MA content of hydrogel.
The use of ammonio methacrylate copolymer (Eudrgit RS, RL) to form a sustained-release solid dispersion of Misoprostol can improve and enhance two important physical and chemical properties of Misoprostol. First, the solid dispersion matrix formed by the copolymer can protect Misoprostol from being degraded by water so that its stability is improved. Second, Misoprostol can be slowly released by diffusion from the copolymer matrix. Accelerated stability studies of Misoprostol-Eudragit solid dispersion after storing at various temperatures for different time periods were carried out. According to high performance liquid chromatography (HPLC) analyses, the stability of Misoprostol in a series of Eudragit appeared significantly improved at different ratios. The Misoprostol-Eudragit dispersion can be used in a powder form, filled in capsules, or compressed into tablets. The dissolution profiles of Misoprostol-Eudragit solid dispersion and its tablets in water, pH 1. 2, 4.5 and 6.8, dissolution media show that this stable solid dispersion is a sustained-release type.