Oral sustained release pellets of diltiazem HCL with Kollicoat SR30

An aqueous dispersion of polyvinyl acetate [Kollicoat SR30] was selected for the development and in vitro evaluation of diltiazem sustained release pellets. Five coating levels based on theoretical weight gains of 7, 8, 9, 10 and 11% were examined onto drug pellets using fluidized bed technique. Coated pellets were thermally treated at 37°C, 40°C, 50°C and 60°C for 24 hours. In vitro dissolution tests were performed in distilled water while selected batches were compared to the release data in test media having pH 1, 4 and 7. The release profiles of coated pellets were found to be inversely proportional to the thickness of Kollicoat SR30 coat and desirable controlled release characteristics could be achieved by manipulating the coating levels. Plasticizers [propylene glycol/triethyl citrate] and anti-adherent [magnesium stearate] in the formulation of coated pellets reduced the release rates. Thermally treated pellets also showed reduction in the release rates at 60°C compared to initial release profile at 37°C. However, the drug release rates was found to be fairly independent of dissolution media [pH 1,4 and 7]

study on the in vitro evaluation of Guar Gum as a carrier for oral controlled drug delivery

The objective of the study is to evaluate guar gum as a carrier in the design of oral controlled drug delivery systems. Drugs with varying solubility such as diltiazem HC1 [freely soluble], theophylline [slightly soluble] and glipizide [practically insoluble] were chosen as model drugs. Matrix tablets of diltiazem HC1, theophylline and glipizide using different proportions of guar gum were prepared and subjected to in vitro drug release studies. When the cumulative amount of drug released at different time intervals was plotted, all the guar gum matrix formulations provided controlled drug delivery comparable with the respective commercial sustained release tablets. The results indicated that guar gum is a potential carrier in the design of oral controlled drug delivery systems

Angina inestable: los calcibloqueantes sin betabloqueantes no previenen la recurrencia de la angina, los procedimientos intervencionistas, ni la insuficiencia cardíaca / Calcium channel bloquer agentes, not associated to betabloquers, do not prevent recurrent angina, further invasive procedures or pump failure in patients hospitalized for unstable angina

Antecentes. Los calciantagonistas (CA) deberían ser eficaces en reducir la mortalidad y el infarto (IAM) no fatal en la angina inestable (AI). Se ha demostrado que los CA proporcionan alivio sintomático y mejor evolución. Objetivo. Investigar si los CA en la AI disminuyen la muerte y el IAM no fatal, previenen la recurrencia de la angina y mejoran la evolución. Material y métodos. Análisis en la base de datos del estudio ENAI (Enalapril en la Angina Inestable) que sigue durante 7 días a 1022 pacientes con AI. Indicación de betabloqueantes (BB) y CA a criterio de los participantes. Resultados. La angina recurrente y los procedimientos invasivos no son diferentes en la AI previamente tratada con CA (RR 1,02; IC95 0,74 - 1,40; P 0,8958). En 1022 pacientes los eventos secundarios aumentan en los no tratados (53,3 por ciento en 629) en relación a los tratados con CA cuando se asocian a los BB (46,7 por ciento en 392; RR 1,39; IC95 1,19 - 1,62; P 0,00003) Para Diltiazem-BB los eventos secundarios disminuyen desde un 61,3 por ciento al 38,7 por ciento (RR 1,74; ; IC95 1,39 - 2,18; P 0,0000), similar con otros CA-BB. Reducen los eventos secundarios del 66 por ciento al 34 por ciento en el grupo con SD del ST/ST normal (RR del 1,92; IC95 1,05 - 3,51; P 0,0335). Conclusiones. La indicación de CA sin BB en AI no disminuye los eventos isquémicos secundarios ni el desarrollo de insuficiencia cardíaca. Indicados en AI con SD del ST.

Diltiazem versus nitroglicerina por vía endovenosa en el tratamiento de la angina inestable: estudio randomizado / Diltiazem versus nitroglycerin by endovenous way in the treatment of unstable angina: randomized study

Prognosis of unstable angina pectoris is related to admission EKG changes and prompt symptoms control. The aim of this study was to compare the clinical effects of intravenous diltiazem (DTZ) or nitroglycerin (NTG) in patients with unstable angina pectoris. We studied 43 patients admitted to the hospital with a history of rest angina within the last 48 hours, associated with EKG evidence of ischemia. All subjects received intravenous heparin and oral aspirin, 23 were randomly assigned to receive intravenous DTZ and 20 to recieve intravenous NTG. Both groups had similar baseline features and the endpoints of treatment were recurrence of angina, myocardial infarction, death during hospitalization and secondary side effects. Treatment with DTZ, when compared to NTG, resulted in a significant reduction of recurrent angina (8.7 and 59 percent respectively; p<0.05), number of angina episodes per patient (0.18ñ0.5 and 0.9ñ1.2 respectively; p<0.05) and lower need for dose increment to control symptoms (3 and 9 patients respectively; p<0.05). The most common side effects observed were cephalea with NTG (60 percent of patients) and asymptomatic sinus bradicardia with DTZ (28 percent of patients). In each group, one patient had a myocardial infarction and one patient died. It is concluded that intravenous DTZ reduces myocardial ischemia to a greater extent than NTG and can be safely used in patients with unstable angina pectoris

Effect of gugulipid on bioavailability of diltiazem and propranolol.

The effect of single oral dose of 1 gm gugulipid was studied on bioavailability of single oral dose of propranolol (40 mg) and diltiazem (60 mg) in 10 and 7 normal healthy male volunteers respectively. It was a randomised within group crossover study. Blood samples were collected at hourly intervals upto 8 hrs. Gugulipid significantly reduced (P < .01) peak plasma concentration (Cmax) and area under curve (AUC 0-8 hrs) of both the drugs in normal volunteers. Such interaction in patients receiving propanolol or diltiazem with gugulipid may lead to diminished efficacy or nonresponsiveness due to significant reduction in bioavailability.