Captopril Tablets Research Articles

Determination of Captopril in Human Plasma by Liquid Chromatography/Tandem Mass Spectrometry

In this study, a fast and sensitive liquid chromatography/tandem mass spectrometry method for the determination of captopril in human plasma was developed and validated. The analyte and enalaprilat, used as the internal standard, were extracted from plasma using methanol directly precipitate protein. Analysis was performed on a Lichrospher CN column with water (containing 0.1% formic acid) and methanol (60∶40, v/v) as the mobile phase. Linearity was assessed from 6.25 to 800 ng/ml in plasma. The analytical method proved to be applicable in a pharmacokinetic study of captopril after oral administration of 20 mg captopril tablet to 20 healthy volunteers.

Variations in captopril formulations used to treat children with heart failure: a survey in the United kingdom

Background and objective: Different liquid formulations of a drug prepared for use in children cannot be assumed to have therapeutic equivalence. The objective of this study was to ascertain the...

A selective and rapid method for the quantification of captopril in human plasma using liquid chromatography/selected reaction monitoring mass spectrometry

A specific hyphenated high performance liquid chromatography–mass spectrometric (LC–MS/MS) assay was developed for the determination of captopril in plasma. The drug was extracted from plasma using liquid–liquid extraction with a mixture of diethylether:dichloromethane. After the addition of the internal standard, samples were applied to a prepacked C 8 Waters Symmetry column. The ion trap MS/MS detector was equipped with electrospray ionization (ESI) source operating in the positive ion mode. Drug determination was accomplished monitoring captopril at molecular ion m/ z 218 and MS/MS (daughter) at m/ z 171.6. The method was applied to captopril determination in human plasma after the administration of captopril 50 mg tablets to healthy volunteers who have participated in a pharmacokinetic study. The method was proved to be specific and precise by testing six different plasma batches. Linearity was established for the range of concentrations 25–3000 ng/ml with a regression factor of 0.9995. Intra-day accuracy ranged from 90.16 to 96.18%, while the intra-day precision ranged from 2.60 to 9.66% at the concentrations of 75, 1440 and 2500 ng/ml. Inter-day precision of the method ranged from 5.04 to 10.10%. This validated method of analysis was successfully applied to human plasma analyses after the administration of a single dose of 50 mg captopril tablets to healthy volunteers.

Preparation and in-vitro evaluation of floating sustained-release captopril tablets and capsules

Preparation and in-vitro evaluation of floating sustained-release captopril tablets and capsules

Water determination in drugs containing thiols

A new rapid analytical method is applied for water determination in α-Mono-thioglycerol and Captopril tablets containing thiols, and therefore, not amenable for direct Karl Fischer titration. The method is based on the consecutive titration first of thiol by a novel reagent, and then of water by a conventional K. Fischer reagent in the same sample and cell with the electrometric ‘dead-stop’ location of the end point in both titrations. The new reagent consists of iodine, potassium iodide and sodium acetate in non-aqueous medium. Estimated repeatability and accuracy of both water and thiol determinations are satisfactory.

Instrumental evaluation of color of solid dosage forms during stability testing

The principles of color measurement established by the Commission International de I'Éclairage (CIE) have been applied to determine color formation during long-term storage and stability testing of four white commercial solid dosage forms. The products tested were preparations of captopril tablets, flucloxacillin sodium capsules, cefoxitin sodium powder for injection and theophylline controlled release tablets in their original packaging. Different batches of medicines were examined for color formation and chemical stability under ambient conditions and a single batch was monitored on accelerated testing. Only flucloxacillin sodium and cefoxitin sodium showed statistically significant degradation of active drug on ambient storage accompanied by color formation (yellowing) in the latter case. On accelerated testing, linear relationships were observed between color formation and drug content for all formulations except theophylline where color formation occurred without significant drug degradation. The rate of color formation obeyed the Arrhenius equation in every case. Color change can be quantified according to the CIE system and may be useful for potency predictions where a causal relationship between color change and drug decomposition can be established. Even where a causal relationship does not exist, patient confidence in a pharmaceutical product may be undermined by perceptible color change. In this situation, the shelf-life could be specified using the CIE colour system.

Clinical observation on diabetic nephropathy treated with alcohol extraction of Flos Abelmoschus manihot

Sixty-eight cases of Non-Insulin Dependent Diabetes Mellitus complicated with Nephropathy were randomly divided into two groups: the treated group, 35 cases treated with alcohol extraction of Flos A-belmoschus manihot, Gliclazide and Captopril Tablets; and the control group, 33 cases treated with Gliclazide and Captopril Tablets, over a period of 8 weeks. The total effective rate in the treated and control group were 83.87% and 31.03% respectively (P<0.01), urinary micro-albumin were 31.7 and 76.3mg/L (P<0.05), proteinuria were 0.41 and 0.77g/24hr (P<0.01), blood β-microglobulin were 3317.8 and 3473. 1 hg/ml (P<0.05), urinary β-microglobulin were 367.2 and 641.5ng/ml (P<0.01), urinary N-acetyl-β-glucosaminidase (NAG) were 26.3 and 66. 7u/L (P<0.01), plasma lipid peroxide (LPO) were 6.13 and 8.78 nmol/L (P<0. 05), and plasma superoxide anion were 8.36 and 10.42 kcpm respectively (P<0.05). It was suggested that alcohol extraction ofAbelmoschus manihot could eliminate oxygen free radicals, alleviate renal tubular-interstitial diseases, improve renal function, and reduce proteinuria.

Captopril, Nifedipine and Their Combination for Therapy of Hypertensive Urgencies

Abstract Twenty patients with acute severe hypertension were randomised to therapy with either nifedipine capsules (10 mg) or captopril tablets (25 mg) given sublingually and the blood pressure recorded for 240 minutes. Oral monotherapy with either agent followed for 3 weeks, then the agents were combined for a further 2 weeks and in the final 6 weeks of the trial a beta-blocker and diuretic were added, if needed. Thirteen patients completed the trial. The major results were: (i) nifedipine decreased blood pressure more rapidly than captopril 60 minutes after first ingestion but at 240 minutes equal degrees of fall in blood pressure had been obtained; (ii) neither agent given as sustained monotherapy was able to reduce blood pressure adequately, although nifedipine was better than captopril; and (iii) combination therapy with both agents was conspicuously successful in achieving reduction in blood pressure. It is suggested that combination nifedipine-captopril therapy be subject to a formal trial for early therapy in acute severe hypertension.

Stability of captopril in tap water

The stability of captopril in tap water was studied. Twenty 25-mg captopril tablets were crushed separately, added to 25 mL of tap water in individual volumetric flasks, and shaken vigorously. Five flasks each were incubated at 25, 50, and 75 degrees C in a shaking water bath and refrigerated at 5 degrees C. Samples were taken from each flask immediately after dissolving the drug and at intervals up to 28 days for 5 and 25 degrees C, 15 days for 50 degrees C, and 16 days for 75 degrees C. Captopril concentrations were analyzed by high-performance liquid chromatography. First-order rate constants were calculated for each temperature setting, and the Arrhenius plot was applied to estimate the shelf life of captopril at 5 degrees C. More than 90% of the initial concentration of captopril remained after 28 days at 5 degrees C. Captopril concentration in the samples stored at 75, 50, and 25 degrees C decreased to 90% of the initial concentration at calculated times (mean +/- S.E.) of 2.1 +/- 0.1, 3.6 +/- 0.4, and 11.8 +/- 1.2 days, respectively. The estimated time required for the concentration of a 1-mg/mL solution of captopril stored at 5 degrees C to decrease to 90% of initial concentration was 27 days. The shelf life of a solution of captopril 1 mg/mL in tap water stored at 5 degrees C was 27 days.

Survey of chlorinated hydrocarbons and other organic volatile impurities in captopril raw materials and tablets.

Survey of chlorinated hydrocarbons and other organic volatile impurities in captopril raw materials and tablets.

本態性高血圧症の血圧リズム変動に対するｃａｐｔｏｐｒｉｌ持効性製剤（ｃａｐｔｏｐｒｉｌ‐Ｒ）１日２回投与法の効果について Ｃａｐｔｏｐｒｉｌ錠１日３回投与法との比較

本態性高血圧症の血圧リズム変動に対するｃａｐｔｏｐｒｉｌ持効性製剤（ｃａｐｔｏｐｒｉｌ‐Ｒ）１日２回投与法の効果について Ｃａｐｔｏｐｒｉｌ錠１日３回投与法との比較

Suicide by Captopril Overdose

We report a case of a 75 year-old male who committed suicide by taking an overdose of captopril. He took approximately ninety 12.5 mg captopril tablets. The postmortem plasma concentration of captopril was 60.4 mg/L. A review of the medical literature revealed five cases of captopril overdose all from unsuccessful suicide attempts. To our knowledge, this is the first case report of fatal captopril overdose with the measurement of plasma concentration of the drug.

Captopril Overdose and Hypotension

To the Editor.— The article by Augenstein et al 1 raises a question about the role of alprazolam in producing hypotension. Their review of prior cases of overdose seems to reveal a more benign course than that of their patient; for example, a 3-year-old child who ingested eight to ten 25-mg captopril tablets surely ingested, on the basis of body size, a proportionally greater amount than the 20 to 30 tablets taken by the obese 33-year-old patient yet the child was essentially asymptomatic. Similarly, the two French patients were not even seen until a day after overdosing, and one had transient orthostatic hypotension. The authors' patient, however, had an initial and two later episodes of hypotension at 18.5 and 24.5 hours after ingestion, all requiring vigorous intervention with fluids and dopamine. The authors assume that the hypotension was due to the captopril since benzodiazepines rarely cause hypotension in overdosage. However,

Captopril in human blood and breast milk.

Blood and milk concentrations of captopril, a new antihypertensive agent, were studied in 12 lactating normotensive subjects after the administration of 100 mg captopril tablets on a three times daily regimen for a total of seven doses. Peak blood concentrations (+/- S.E.M.) of captopril after the administration of the seventh 100-mg tablet averaged 713.1 +/- 140.6 ng/ml, as compared to average peak milk concentrations of 4.7 +/- 0.7 ng/ml. Time to peak blood concentrations averaged 1.1 +/- 0.2 hour, while time to peak milk concentrations averaged 3.8 +/- 0.6 hours. The data suggest that the human breast selectively restricts the passage of captopril from blood into milk.

Development and Evaluation of Controlled Release Mucoadhesive Tablets of Captopril

The present investigation focuses on the development of mucoadhesive tablets of captopril which are designed to prolong the gastric residence time after oral administration. Matrix tablets of captopril were formulated using four mucoadhesive polymers namely guar gum, xanthan gum, HPMC K4M and HPMC K15M and studied for parameters such as weight variation, thickness, hardness, content uniformity, swelling index, mucoadhesive force and in vitro drug release. Tablets formulated Xanthan gum or HPMC K4M with HPMC K15M provide slow release of captopril over period of 12 hr and were found suitable for maintenance portion of oral controlled release tablets. The cumulative % of drug release of formulation F9 and F10 were 90 and 92, respectively. In vitro release from these tablets was diffusion controlled and followed zero order kinetics. The ‘n’ values obtained from the pappas-karsemeyer equation suggested that all the formulation showed drug release by non-fickian diffusion mechanism. Tablets formulated Xanthan gum or HPMC K4M with HPMC K15M (1:1) were established to be the optimum formulation with optimum bioadhesive force, swelling index &amp; desired invitro drug release. This product was further subjected to stability study, the results of which indicated no significant change with respect to Adhesive strength and in vitro drug release study.