Reference

Controlled release tablet

Controlled release tablet. Shah, Dhiren; Gilbert, Deborah A.; Copeland, Robert D. (Merrell Dow Pharmaceuticals, Inc., USA). Eur. Pat. Appl. EP 126453 A2 28 Nov 1984, 18 pp. DESIGNATED STATES: R: AT, BE, CH, DE, FR, GB, IT, LI, LU, NL, SE. (English). (European Patent Organization). CODEN: EPXXDW. CLASS: IC: A61K009-22. APPLICATION: EP 84-105664 18 May 1984. PRIORITY: US 83-496025 19 May 1983. DOCUMENT TYPE: Patent CA Section: 63 (Pharmaceuticals) Controlled release of an active ingredient is obtained by differentially compressed tablets manufd. with a sloped or slanted tableting punch face. The thinner side of the tablet is harder and releases the active ingredient more slowly than the thicker side which is softer. Due to size limitations the tablets should not exceed 500 mg active ingredient. Thus, the controlled released effect was demonstrated with compression gradient tablets of 500 mg each at 439.4 kg/cm2 compressional force, angle of inclination equal to 10 and 25° of arc, and contg. d-pseudoephedrine-HCl [345-78-8] 12, Methocels E4M and K4M each 30, Lubritab 12.5, lactose 15, and Mg stearate 0.5%.

Bioavailability assessment of a new liquid controlled-release pseudoephedrine product

Bioavailability assessment of a new liquid controlled-release pseudoephedrine product. Graves, David A.; Rotenberg, Keith S.; Woodworth, James R.; Amsel, Lewis P.; Hinsvark, Orville N. (Med. Res. Div., Pennwalt Pharm. Div., Rochester, NY 14623, USA). Clin. Pharm., 4(2), 199-203 (English) 1985. CODEN: CPHADV. ISSN: 0278-2677. DOCUMENT TYPE: Journal CA Section: 63 (Pharmaceuticals) Section cross-reference(s): 1 Two bioequivalence studies were conducted of a controlled-release pseudoephedrine (I) [90-82-4] liq. In a single-dose study involving 20 subjects, the bioavailabilities of 5 controlled-release suspensions with a broad range of drug-release rates were compared with an immediate-release form of I-HCl [345-78-8] in a 4-way crossover, incomplete block, sequence-randomized study. Serial blood sampling up to 36 h after drug ingestion provided area-under-the-curve (AUC), max. plasma concn. (Cmax), and time to peak (tmax). In the multiple-dose study, involving 18 subjects, the bioavailability of the optimal formulation detd. from the single-dose study was compared with a ref. I-HCl syrup. Serial blood sampling up to 12 h after drug ingestion was performed to det. AUC, Cmax, and tmax. The single-dose investigation showed that all formulations were bioequiv. except the product with the slowest release rate, which had lower AUC and Cmax values. The results of the multiple-dose study confirmed these findings with the ref. syrup. The use of a series of drug formulations with a wide range of release rates permitted selection of an optimal product in addn. to the information needed to ensure continuous prodn. of bioequivalent. products.