Evaluation of paracetamol suppositories by a pharmacopoeial dissolution test--comments on methodology.

Ph.Eur. and BP have introduced a dissolution apparatus for suppositories. Suitability of the apparatus for quality control of paracetamol suppositories was evaluated and the effect of experimental conditions on dissolution profiles was studied. Paracetamol suppositories containing 80-500 mg of the drug, on fatty base, were obtained from four manufacturers (A, B, C, D). The diffusion cell was modified by incorporation of an in-built thermoprobe and large difference (up to 1.7 degrees C) between temperature in the water-bath and in the dissolution chamber was observed. This effect was avoided by increasing the length of tubing immersed in the thermostat at the inlet of the cell. The most reproducible results were observed for A and C suppositories, however from suppository C the total dose of paracetamol was released after 3.5-4.5 h while the release from suppository A was slow with only 40-87% of the total dose liberated during 6 h. Suppositories B did not melt at 37 degrees C and less than 5% of the drug was released. Fast release was observed after melting when the temperature was elevated to 39.5 degrees C. The results demonstrate clearly that essentially complete melting of a suppository in the dissolution chamber is required for an appropriate dissolution of paracetamol in vitro. Disintegration time, softening time, drop point and particle size of the suspended drug were measured and the relevance of these parameters for dissolution behaviour of the preparations was discussed.

[Pharmacotherapy of arterial hypertension and pharmacoeconomic aspects of hypotensive therapy in elderly patients in Poland]. / Leczenie farmakologiczne nadcisnienia tetniczego oraz wybrane aspekty farmakoekonomiczne terapii hipotensyjnej u chorych w starszym wieku w Polsce.

The aim of our study was to examine the use of pharmacological therapy and to evaluate the economical aspects of treating hypertension (HT) in elderly patients in Poland. Two hundred and sixty eight elderly persons (147 females, 121 males; mean age: 72.2 +/- 6.0 years) were selected from Polish population by stratified and cluster random sampling with quotas. BP measurement was performed 3 times every 2 minutes at respondents home. In the questionnaire, awareness of HT was assessed. Prevalence of hypertension among subjects aged 65 years and over by JNC VI criteria (SAP > or = 140 mm Hg, DAP > or = 90 mm Hg or hypotensive therapy) was 74%. Awareness of HT was equal to 61%. Eleven percent of all hypertensives were well controlled. Among hypertensives, 71% took prescribed antihypertensive drugs on a regular basis. Patients with HT were taking the following antihypertensive drugs: diuretics 16%, diuretics and reserpine 20%, beta-blockers 19%, ACE inhibitors 53%, calcium antagonists 30%, and other 3%. Newer drugs were prescribed in 7%, and multi-source (generic) products in 93%. The average cost of treatment with one drug was 147 PLN (37.5 USD) per year (newer drugs: 413 PLN; multi-source product 126 PLN). Assuming those data and number of elderly people in Poland (4.335 mln), we estimated that 3.208 mln of subjects have had hypertension according to JNC VI criteria. Only 1.957 mln of patients with HT have been detected and only 0.353 mln of hypertensives have been well controlled. The approximate global cost of antihypertensive drugs per year in elderly patients in Poland has been equal to 285 mln PLN (72.8 mln USD). In hypothetical situation with optimal (100%) detection and control of HT the global cost by the actual rate of regularity in taking drugs would increase to 569 mln PLN (145.3 mln USD). The prevalence of HT in elderly people in Poland is very high. In elderly hypertensives ACE inhibitors are used most often. More than 90% of prescribed drugs are multi-source products. An optimal improvement of HT detection and control would cause a two-fold augmentation of the costs of pharmacological therapy.