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PubMed1997

Setting dissolution specifications for modified-release dosage forms.

Dissolution specifications are used for quality assurance and may also serve as a surrogate for in vivo bioavailability. These limits can guide formulation development and eliminate the need for bioavailability studies for scale up and post approval changes. Several methods for setting dissolution specifications have been reviewed in this chapter. A summary of the advantages and disadvantages for each method can be found in Table 1. When choosing a method for setting dissolution specifications, it is important to 1) have a discriminating dissolution system, 2) incorporate in vivo data, 3) include intersubject variability, and 4) predict plasma concentration-time profiles. Predicting plasma concentration curves allows one to see how the change in formulation or dissolution limits perform in vivo. Dissolution specifications should be set so that all formulations that have dissolution profiles within the limits of the specifications are bioequivalent. This can be assured if the boundaries are tested for bioequivalence. Minimally, the formulations that have dissolution profiles within the limits of the specifications should be bioequivalent to the pivotal batch. A population prediction of the plasma concentration-time profiles for the upper and lower limit would incorporate the true intersubject variability for the formulation.

Data Interpretation, Statistical↗
PubMed1994

Pharmacokinetics and haemodynamic effects of ISDN following different dosage forms and routes of administration.

The pharmacokinetics and haemodynamic effects of isosorbide dinitrate (ISDN) have been investigated following administration of single doses as a sublingual (SL) spray (2.5 mg), sublingual tablet (5 mg) and peroral tablet (10 mg) in a randomised, placebo-controlled double-blind cross-over trial in 16 healthy volunteers. After the sublingual spray Cmax was higher (39.0 ng.ml-1) and tmax was shorter (3.9 min) than after the sublingual (22.8 ng.ml-1 and 13.8 min) and peroral (16.9 ng.ml-1 and 25.6 min) tablets. The AUC of ISDN did not differ following any of the three formulations (1031; 879; 997 ng.ml-1.min, for the spray, SL tablet and PO-tablet, respectively). Mononitrate metabolites of ISDN (IS-2-MN and IS-5-MN) and total nitrates in plasma increased in proportion to the administered dose. This indicates that the fraction of the dose absorbed was the same for all the formulations but that the extent of first-pass metabolism increased in the order sublingual spray < sublingual tablet < peroral tablet. Thus, compared to the spray, the relative bioavailability of ISDN was 48% and 28% from the sublingual and peroral tablets, respectively. The haemodynamic effects were quantified using the a/b ratio of the finger pulse wave and the systolic blood pressure and heart rate under orthostatic conditions.(ABSTRACT TRUNCATED AT 250 WORDS)

Administration, Oral↗
PubMed1985

Pharmacokinetics of an extended-release dosage form of molsidomine in patients with coronary heart disease.

Molsidomine (N-carboxy-3-morpholino-sydnonimine-ethylester; Cassella-Riedel Pharma GmbH, Frankfurt/M. FRG) has an antianginal effect for up to 3-5 h after oral administration of 2 mg Corvaton [1]. Plasma levels of the parent drug can be measured during this interval. A new galenic formulation (Corvaton retard) has been developed to prolong the duration of the therapeutic action and to improve patient compliance. The present study was carried out to establish whether the in vitro dissolution profile of the tablet was reflected in vivo, thus permitting prediction of plasma molsidomine levels in patients with coronary heart disease.

Aged↗
PubMed1984

Comparative pharmacokinetic analysis of a novel sustained-release dosage form of theophylline in humans.

The pharmacokinetics and relative bioavailability of theophylline from a new sustained-release formulation ( Theotard ) and from a standard sustained-release formulation (Theo-Dur) were compared in 6 healthy, adult, male volunteers. After a single oral dose of 300 mg Theotard , a mean maximal plasma concentration ( Cbmax of 3.49 +/- 1.05 mg/l was obtained after 8 h (tmax). After an identical dose of Theo-Dur, a peak plasma concentration of 4.68 +/- 1.33 mg/l was obtained after 6.33 h. The mean relative bioavailability of theophylline from Theotard was 1.02 +/- 0.16 relative to that of Theo-Dur. In 5 of the volunteers the Theotard formulation exhibited a more prolonged and uniform absorption rate and yielded more sustained plasma levels.

Adult↗
PubMed1978

Controlled trial of a new dosage form of carbenoxolone (Pyrogastrone) in the treatment of reflux esophagitis.

A new preparation combining carbenoxolone sodium with alginate antacid (Pyrogastrone), taken for 8 weeks, was compared with alginate antacid alone (Gaviscon-like) in a controlled double-blind study in 37 patients with endoscopically proved reflux esophagitis. Complete remission or persistence of only minimal symptoms was obtained in 89%, and esophageal ulcer healing was achieved in 100% of subjects taking Pyrogastrone, compared with only 50% (P less than 0.025) and 33% (P equal 0.02), respectively, on control treatment. Complete endoscopic healing or persistence of only minimal inflammation was seen in 95% on Pyrogastrone and 67% of controls (P less than 0.05). Mild biochemical and clinical changes were noted in 9 of 19 patients on Pyrogastrone and 6 of 18 on the control drug, but none required treatment or alteration in regime. Thus Pyrogastrone is more effective in the treatment of reflux esophagitis than the most efficacious compound in current use.

Adult↗
PubMedDate not supplied

Controlled release dosage forms: from ground to space.

Controlled release of drugs is one of the most significant advances in pharmacy. Due to the proposition of new routes for drug administration, today it is considered as a part of 'drug delivery'. Developments in biotechnology producing natural molecules, peptides and proteins have allowed high activity substances that require careful formulation for administration. Drug delivery is the discipline striving to sole the problem of optimisation of drug efficacy. In this contribution the last 25 years of drug delivery research have been examined pointing out the most significant break-through steps.

Delayed-Action Preparations↗
PubMed2004

[Interferon therapy of multiple sclerosis. Synopsis of various dosage forms].

In addition to the clinical efficacy, which is similar for the three approved interferon-beta preparations, the compliance and acceptance of interferon therapy are determined by several other factors. These include the mode of application, formulation, storing conditions, and injection methods. Some of these factors have been modified recently. In this article we provide a synopsis of the current application formats of the different interferon-beta preparations, and discuss the respective advantages and drawbacks.

Clinical Trials as Topic↗
PubMed1999

[Effectiveness and tolerance of 1 dosage forms (subcutaneous and intramuscular) of decapeptyl depot in patients with advanced prostate carcinoma].

The intramuscular (i.m.) administration of Decapeptyl Depot has been approved in Germany for the treatment of advanced hormone dependent prostate cancer since July 1990. In this study a reformulated Decapeptyl Depot, administered as a first-line endocrine therapy, was injected intramuscularly (i.m.) or subcutaneously (s.c.) every 28 days for 6 months. At 12 different hospitals, 52 prostate cancer patients were treated, whereby 25 patients received a s.c. injection and 27 patients a i.m. injection. Testosterone was measured as the main parameter: after 28 days, both the s.c. and the i.m. application form of Decapeptyl Depot successfully reduced initial testosterone levels of at least 2.3 ng/ml to steady-state castration levels below 1.2 ng/ml, maintaining this complete suppression for the entire length of the trial (168 days). Decapeptyl Depot was well tolerated and very acceptable to the patients in both groups. Side effects were few and predictable, being largely associated with decreased testosterone concentrations. No cumulation in triptorelin serum levels was observed within the 6 months of treatment. Decapeptyl Depot, administered subcutaneously or intramuscularly was effective and safe in the treatment of patients with advanced prostate cancer.

Antineoplastic Agents, Hormonal↗
PubMed2002

Electrochemical study of fluvastatin sodium--analytical application to pharmaceutical dosage forms, human serum, and simulated gastric juice.

The oxidation of fluvastatin sodium on a glassy carbon electrode has been studied by use of a variety of voltammetric techniques. Different conditions were investigated to optimize the determination of fluvastatin sodium. The dependence of the intensities of currents and potentials on pH, concentration, scan rate, and nature of the buffer was investigated. Oxidation of fluvastatin sodium was found to be diffusion-controlled and irreversible. The best results for the determination of fluvastatin sodium were obtained by using differential pulse and square-wave voltammetric techniques in Britton-Robinson buffer at pH 10.04. Differential pulse and square-wave voltammetry at a glassy carbon electrode resulted in linear calibration in the range 8x10(-6) to 6x10(-4) mol L(-1) and detection limits of 1.07x10(-6) and 7.99x10(-7) mol L(-1), respectively. The proposed methods were successfully applied to the determination of the drug in capsules and biological fluids. Excipients did not interfere with the determination. Statistical validation revealed that the methods were free from significant systematic errors.

Electrochemistry↗
PubMed2003

Differential-pulse polarography (DPP) determination of betamethasone valerate in dosage form.

The electrochemical reduction of betamethasone valerate (BV) in a pharmaceutical formulation containing neomycin has been carried out in Britton-Robinson buffer (BRB) (0.04 mol L(-1)) by differential-pulse polarography (DPP). BV exhibits a well-defined irreversible reduction peak at -1.03 V/ref. The influence of pH on the reduction of BV was studied in Britton-Robinson buffer (pH range 1.7-10). A method for the analysis of BV in BRB (0.04 mol L(-1)), which allows quantification over the range 3.9x10(-6)-1.1x10(-4) mol L(-1), was proposed and successfully applied to the determination of BV in tablets with mean recovery and relative standard deviation of 100.81% and 0.45%, respectively.

Betamethasone Valerate↗
PubMed2003

Chemometrics-assisted simultaneous determination of atenolol and chlorthalidone in synthetic binary mixtures and pharmaceutical dosage forms.

Resolution of binary mixtures of atenolol (ATE) and chlorthalidone (CTD) with minimum sample pre-treatment and without analyte separation has been successfully achieved, using a new and rapid method based on partial least squares (PLS1) analysis of UV spectral data. The simultaneous determination of both analytes was possible by PLS1 processing of sample absorbances between 255 and 300 nm for ATE and evaluation of absorbances in the 253-268 nm region for CTD. The mean recoveries for synthetic samples were 100.3 +/- 1.0% and 100.7 +/- 0.7% for ATE and CTD, respectively. Application of the proposed method to two commercial tablet preparations in the content uniformity test showed them to contain 103.5 +/- 0.8% and 104.9 +/- 1.8% ATE respectively, as well as 103.4 +/- 1.2% and 104.5 +/- 2.2% CTD. Use of this method also allowed the elaboration of dissolution profiles of the drugs in two commercial combined formulation products, through the simultaneous determination of both drugs during the dissolution test. At the dissolution time of 45 min specified by USP XXIV, both pharmaceutical formulations complied with the test.

Algorithms↗
PubMed2004

Absorption kinetics and pharmacodynamics of two oral dosage forms of flecainide in patients with an episode of paroxysmal atrial fibrillation.

OBJECTIVES: The objectives were to study the absorption kinetics and pharmacodynamics of two oral formulations of flecainide in patients with atrial fibrillation (AF) and to assess the relationship between pharmacokinetic parameters and the efficacy in restoring sinus rhythm. METHODS: The data of 54 patients included in a randomised, open, parallel-group study were used. Patients received an oral solution containing 300 mg flecainide and 20 mg cisapride or three tablets each containing 100 mg flecainide. The pharmacokinetic profile of flecainide was fitted using a one-compartment model with lag-time and first-order absorption. RESULTS: The tablets gave a maximum concentration (C (max\ fit)) of 0.43+/-0.14 mg/l at 2.37+/-1.20 h. The oral solution resulted in a much faster peak concentration at 1.05+/-0.71 h (P<0.0001). The C (max\ fit) of the oral solution of 0.60+/-0.17 mg/l was higher (P=0.0002) than that of the tablets, and interindividual variabilities of C (max\ fit) were 28% and 33%, respectively. The absorption rate constant (ka) of the oral solution was twofold larger (P<0.0001). A higher ka (P=0.04) and a duration of AF less than 24 h (P=0.006) increased the probability of cardioversion. If atrial fibrillation lasted less than 24 h, only ka (P=0.016) was obtained as a significant variable in multivariate analysis. The linear models of QRS interval changes versus flecainide concentrations of both formulations had similar slopes with similar interindividual variabilities. CONCLUSIONS: The probability of cardioversion after an oral loading dose of flecainide in patients with AF is dependent on ka. Rapid loading of the effect compartment, i.e. the atria, appears to be critical to reach cardioversion. Higher flecainide serum concentrations and a more rapid absorption does not increase interindividual variability of pharmacokinetics and pharmacodynamics, which is important when safety is considered.

Administration, Oral↗