Ordinary Tablets Research Articles

Fast Dissolving Tablet

Fast dissolving tablets (FDTs) are a sort of oral strong measurement structure that crumbles or disintegrates rapidly in the oral cavity, bringing about fast medication retention and beginning of activity. These tablets have acquired fame because of their benefits over ordinary tablets, including simplicity of organization, expanded patient consistence, and further developed bioavailability .FDTs can be ready by different strategies, including direct pressure, freeze-drying, sublimation, splash drying, and hot-soften expulsion. They can be intended to deliver the medication quickly upon contact with spit or after a particular time delay, contingent upon the medication's physicochemical properties and restorative prerequisites. The definition of FDTs includes the utilization of different excipients, for example, super disintegrants , sugars, flavors, and oils, to work on the tablet's taste, mouthfeel, and crumbling time. The decision of excipients relies upon the medication's properties and the ideal disintegration profile. FDTs have tracked down applications in different remedial regions, including analgesics, antiemetics, allergy meds, and cardiovascular medications. They are especially valuable for drugs with a limited restorative window, where quick beginning of activity is basic, and for patients who experience issues gulping ordinary tablets. All in all, FDTs are a promising medication conveyance framework that gives a helpful, patient-accommodating, and compelling approach to managing drugs. With the rising interest for effective and simple to-regulate drug items, the FDT market is supposed to fill fundamentally before very long.

The Effect of Cellulose Nanofibers on the Manufacturing of Mini-Tablets by Direct Powder Compression.

Mini-tablets (MTs) contain a small amount of active pharmaceutical ingredients in one small tablet. MTs are advantageous because they can be fine-tuned according to the age and weight of pediatric patients and they are easy for children and the elderly to swallow. However, there are manufacturing concerns such as the difficulty in achieving both hardness and disintegration of a small tablet and it is difficult to keep the tablet weight and drug content consistent in MTs because the mold used for its production is special. In this study, we aimed to determine if an additive such as cellulose nanofibers (CNF), which has been studied in various fields in recent years, could be used to manufacture MTs without difficulties. In this study, an MT was manufactured using a rotary tableting press with a compression force of 2, 5, and 8 kN, and the weight variation, drug content variation, tensile strength, friability, disintegration time, and drug dissolution were evaluated. Of note, the tensile strength of MTs produced with a compression force of ≥5 kN was ≥1.3 MPa, which was comparable to that of an ordinary tablet with an 8 mm diameter and a hardness of ≥30 N. The disintegration time of the MT which was 20-30% CNF was ≤30 s at any compression force. MTs with CNF showed similar disintegration to MTs with other common disintegrants. Therefore, we found that CNF is a functional additive capable of manufacturing MTs by direct powder compression which has both strength and disintegration.

DEVELOPMENT AND EVALUATION OF TASTE MASKED ORO-DISINTEGRATING TABLETS OF ITOPRIDE HCl USING DIFFERENT CO-PROCESSED EXCIPIENTS: PHARMACOKINETICS STUDY ON RABBITS

Objective: This study aimed to mask the bitter taste of itopride HCl using the solid dispersion method by solvent evaporation technique and formulate an oral disintegrating tablet (ODT) by direct compression method using different co-processed excipients. Methods: Nine formulae of solid dispersion were prepared to mask the bitter taste of Itopride HCl using Eudragit EPO® and mannitol at different ratios after compatibility studies using infrared spectroscopy (IR). The prepared formulae were subjected to different physicochemical characterization, in vivo taste evaluation, and drug content. The best-selected formulae were used to formulate 10 different ODTs. The prepared tablets were evaluated through hardness, drug content, in vivo-in vitro disintegration, IR, wetting time, and finally, dissolution studies. The selected formula was subjected to a pharmacokinetic study compared to the brand. Results: F5, drug: Eudragit EPO® (1:2) and F8, Drug: Mannitol: Eudragit EPO® (1:1:2) formulae were selected as the best taste-masked formulae based on in vivo taste evaluation, which were used to formulate ten ODTs. The dissolution rate for the prepared ODTs was rapid if compared with the ordinary oral tablets. Statistical significance was obtained using one-way ANOVA among ODT formulae. The optimum tablet Prosolv SMCC 90® based formula (T10) had friability 0.15, wetting time 4±0.35 sec, in vitro dissolution 100.08±0.028% just after 2 min, where the in vitro disintegration time and in vivo disintegration time were 4±0.12 sec and 12±0.049 sec respectively. The relative bioavailability of ODT containing Prosolv SMCC 90®was increased significantly compared to the brand. Conclusion: The obtained results successfully confirmed the potential of the promising Prosolv SMCC 90® based formula (T10) to produce rapid onset action and in-time drug release instead of ordinary tablets containing itopride HCl and that provide by-passing the excessive degradation of drug by first-pass metabolism increasing the oral bioavailability from 60% of marketed drug Ganaton® to 88% for the prepared ODT (T10).

Pharmacokinetic comparison of four arbidol hydrochloride preparations in beagle dogs.

This study aimed to compare the pharmacokinetic properties of four preparations (dispersible tablets, ordinary tablets, capsules and granules) of arbidol hydrochloride, a broad-spectrum antiviral drug, in beagle dogs. Briefly, a single dose of 100 mg of the four preparations of arbidol hydrochloride was orally administered to dogs; blood was then collected from the veins of the foreleg at different times after administration to prepare plasma samples. The plasma concentration of arbidol hydrochloride was measured using a validated liquid chromatography-tandem mass spectrometry (LC-MS/MS). The results showed that when orally administered with dispersible tablets, ordinary tablets, capsules and granules suspended with water, there were no significant differences in the pharmacokinetic parameters (including peak time, peak concentration, elimination half-life, area under the curve (AUC0-t ), and mean retention time) of arbidol hydrochloride. However, in the case of the dispersible tablets, the pharmacokinetics of arbidol hydrochloride was significantly affected by the mode of administration. Compared with direct feeding, peak time [0.50 (0.13, 0.50) vs. 1.00 (0.50, 2.00)] was significantly shortened (P = 0.033) and the AUC0-48 h (8726.5 ± 2509.3 vs. 3650.8 ± 1536.9ng h/ml) was significantly increased (P = 0.012) when the dispersible tablets were orally administered as water dispersion. In conclusion, the pharmacokinetics of four preparations of arbidol hydrochloride were not significant different in beagle dogs. However, compared with direct feeding, the absorption of arbidol hydrochloride was faster and the bioavailability was better when the dispersible tablets were orally administered as water dispersion.

Bioequivalence of Oral Drug Products in the Healthy and Special Populations: Assessment and Prediction Using a Newly Developed In Vitro System "BE Checker".

In order to assess and predict the bioequivalence (BE) of oral drug products, a new in vitro system “BE checker” was developed, which reproduced the environmental changes in the gastrointestinal (GI) tract by changing the pH, composition, and volume of the medium in a single chamber. The dissolution and membrane permeation profiles of drugs from marketed products were observed in the BE checker under various conditions reflecting the inter-patient variations of the GI physiology. As variable factors, initial gastric pH, gastric emptying time, and GI agitation strength were varied in vitro. Dipyridamole, a basic drug, showed rapid and supersaturated dissolution when the paddle speed in the donor chamber was 200 rpm, which corresponds to the high agitation strength in the stomach. In contrast, supersaturated dissolution disappeared, and the permeated amount decreased under the conditions with a slow paddle speed (100 and 50 rpm) and short gastric emptying time (10 min). In those conditions, disintegration of the formulation was delayed, and the subsequent dissolution of dipyridamole was not completed before the fluid pH was changed to neutral. Similar results were obtained when the initial gastric pH was increased to 3.0, 5.0, and 6.5. To investigate that those factors also affect the BE of oral drug products, dissolution and permeation of naftopidil from its ordinary and orally disintegrating (OD) tablets were observed in the BE checker. Both products showed the similar dissolution profiles when the paddle speed and gastric emptying time were set to 100 rpm and 10 or 20 min, respectively. However, at a low paddle speed (50 rpm), the dissolution of naftopidil from ordinary tablets was slower than that from the OD tablets, and the permeation profiles became dissimilar. These results indicated the possibility of the bioinequivalence of some oral formulations in special patients whose GI physiologies are different from those in the healthy subjects. The BE checker can be a highly capable in vitro tool to assess the BE of oral drug products in various populations.

Preparation and in vitro/in vivo evaluation of a clonidine hydrochloride drug–resin suspension as a sustained-release formulation

Objective The purpose of the present study was to prepare a clonidine hydrochloride (CH) sustained-release suspension. Methods The processes involved in the drug formulation included drug loading, impregnating, and suspension preparation. Clonidine hydrochloride drug–resin complexes (CH-DRC) were prepared using the bath method and the CH-DRC impregnated before the microencapsulation process. Based on the bottom spray fluidized bed coating method, the CH microencapsulated drug–resin complexes (CH-MC) were also prepared using Surelease® (the suspension of ethyl cellulose aqueous dispersion) as the coating material. The effects of coating (process/formulation) on the in vitro release of coating microcapsule were evaluated via single factor investigation and orthogonal design optimization. The CH-MC with optimized formulation was further dispersed in a suitable medium to obtain a sustained-release suspension. Rats were given commercial CH ordinary tablets and the CH sustained-release suspension via intragastric administration. The plasma concentration–time curve and related pharmacokinetic parameters were investigated using the non-compartment model. Results The T max of the CH sustained-release suspension was delayed from 2 h to 5 h compared with the CH ordinary tablets. Similarly, the C max was reduced from 32.138 µg·mL−1 to 18.150 µg·mL−1 with the concentration–time curve being more gentle compared with the commercially CH ordinary tablets. After oral administration, the relative bioavailability of CH sustained-release suspension (AUC0–24 of 137.703 µg·h·mL−1) to its CH ordinary tablets (AUC0–24 of 123.337 µg·h·mL−1) was 111.65%. Conclusions The findings showed that the CH sustained-release suspension for oral administration was successfully formulated.

Pharmacokinetics of diltiazem hydrochloride delay-onset sustained-release pellet capsules in healthy volunteers

The pharmacokinetics (PK) of ordinary tablets and sustained release capsules of diltiazem hydrochloride in human clinical trials had been studied. The PK of diltiazem hydrochloride delay-onset sustained-release pellet capsules, a new dosage form, has not been reported, although it is very important to clinical use. In this paper, we investigated the PK of diltiazem hydrochloride delay-onset sustained-release pellet capsules and the food influence in Chinese healthy volunteers. The PK parameters indicated that the diltiazem hydrochloride delay-onset sustained-release pellet capsules appeared marked characteristics of delayed and controlled release. An opened-label, randomized and parallel clinical trial was conducted in 36 Chinese healthy volunteers with single oral dose (90 mg, 180 mg or 270 mg) and a multiple oral dose (90 mg d-1×6 d) administration. The effect of food on the PK of one single oral dose (360 mg) was investigated in 24 healthy Chinese volunteers. Plasma diltiazem concentration was determined by reversed-phase high-performance liquid chromatography (RP-HPLC) and the main pharmacokinetic parameters were analyzed by PKSolver (Ver 2.0). All clinical studies were conducted in the Clinical Pharmacological Center (No. JDX1999064) of Xiangya Hospital Affiliated Central South University, China. The PK parameters suggested that the new formulation had marked characteristics of delayed and controlled release of diltiazem, and food intake did not alter significantly diltiazem pharmacokinetic parameters.

2. Latin from A to P: The TLL in the 20th Century

after more than a century, the basic look of the TLL, with its two eightyfour line columns per page, remains reassuringly familiar. Yet this superficial continuity masks real changes, not least in the basic corpus of material. Obviously the Thesaurus reflects the discovery of new texts. Some of these, like the new Gallus, are familiar to almost any classicist. Others may be more familiar to specialists, especially students of late antiquity: new letters and sermons of Augustine, new passages of Rutilius Namatianus’s De reditu suo and Tiberius Claudius Donatus’s commentary on the Aeneid, portions of a gospel epic by one Severus, the “Appendix Maximiana.”1 And to these literary texts must be added the constant stream of newly published inscriptions, bringing with them new senses, new constructions, new spellings. On the flip side, the TLL’s corpus has also grown smaller. Users of the 1990 Index are familiar with the annotations non iam affertur and its even more disapproving cousin, nunc spernimus. Most often the work has been dropped because a reattribution or redating pushes it beyond the TLL’s terminus of 600 c.e. But other cases are more curious (for additional instances see Kromer 2003). The 1990 Index still includes a text it refers to as “Epist. Vinisii.” This is a brief text published by Nicholson in 1904, a letter from a fourth-century bishop in Roman Britain warning a parishioner against an Arian rival, a certain Biliconus. Or so it was believed. A little over ten years ago, Roger Tomlin showed, in perhaps the wittiest article ever published in ZPE, that this text is in fact an ordinary curse tablet, one of scores or hundreds that survive from the sacred spring in Bath. The saintly “Bishop Vinisius,” his correspondent “Nigra,” and the dastardly “Biliconus” existed only in the first editor’s fantasy; it did not help that he was trying to read the tablet upside down. Less obtrusive—but far more important in the aggregate—are incremental improvements in familiar texts. New commentaries and other works have 2. Latin from A to P: The TLL in the 20th Century

Preparation and characterizationin vitro of sustained-release captopril/Chitosan-gelatin net-polymer microspheres (Cap/CGNPMs)

The captopril/Chitosan-gelatin net-polymer microspheres (Cap/CGNPMs) were prepared using Chitosan (CS) and gelatin (Gel) by the methods of emulsification. A cross linked reagent alone or in combination with microcrystalline cellulose (MCC) was added in the process of preparation of microspheres to eliminate dose dumping and burst phenomenon of microspheres for the improvement of the therapeutic efficiency and the decrease of the side effects of captopril (Cap). The results indicate that Cap/CGNPMs have a spherical shape, smooth surface morphology and integral inside structure and no adhesive phenomena and good mobility, and the size distribution is mainly from 220 to 280 μm. Researches on the Cap release test in vitro demonstrate that Cap/CGNPMs are of the role of retarding release of Cap compared with Cap ordinary tablets (COT), embedding ratio (ER), drug loading (DL), and swelling ratio (SR), and release behaviors of CGNPMS are influenced by process conditions of preparation such as experimental material ratio (EMR), composition of cross linking reagents. Among these factors, the EMR(1/4), CLR (FOR+TPP) and 0.75% microcrystalline cellulose (MCC) added to the microspheres are the optimal scheme to the preparation of Cap/CGNPMs. The Cap/CGNPMs have a good characteristic of sustained release of drug, and the process of emulsification and cross-linking process is simple and stable. The CGNPMs is probable to be one of an ideal sustained release system for water-soluble drugs.

Comparison of efficacy and quality of life in type 2 diabetics treated with controlled-release-gliclazide and ordinary gliclazide tablets

目的 对Ⅱ期随机对照临床试验中应用格列齐特控释片和格列齐特普通片治疗2型糖尿病的临床疗效和生存质量进行比较.方法48例符合入组标准的2型糖尿病患者随机分为两组各24例,A组予格列齐特控释片(30 mg)2片早餐前服用,安慰剂2片晚餐前服用;B组予格列齐特普通片(80 mg)和安慰剂各1片,每日2次(早餐前和晚餐前)服用.共治疗12周.所有患者均测定相关临床指标,并完成糖尿病患者生存质量特异性量表和简明健康状况调查表(SF36).结果两组患者的空腹及餐后2 h静脉血糖和糖化血红蛋白均较治疗前显著降低(P＜0.01),C肽水平明显升高(P＜0.01),所有临床参数和生存质量参数组间比较差异均无统计学意义.两组患者SF36评分中躯体疼痛和社会功能治疗后均较治疗前显著改善(P＜0.01).A组和B组不良反应发生率分别为20.8%和8.3%,差异有统计学意义(P＜0.05),均为轻度.结论格列齐特控释片治疗2型糖尿病的临床疗效和对生存质量的影响与格列齐特普通片相似。

ブロチゾラム口腔内崩壊錠の自動分包機調剤後における形状および色調変化の検討と服用性に関する患者意識調査

Orally disintegrating tablets are generally highly hygroscopic and less resistant to physical damage than other types of tablets. In consideration of this, we examined orally disintegrating brotizolam tablets (D tablets), for damage sustained in dispensing using an automatic packaging machine as well as for changes in form and color after being packaged in the cassette. There was no damage to or changes in the form or color of the D tablets due to the automatic packaging machine, suggesting that it is strong enough for daily dispensing using such machines.We also conducted a questionnaire survey of inpatients taking D tablets to find out how useful they were. Only 26% of the 62 inpatients surveyed took the D tablet without water because many of them were taking other drugs simultaneously. We therefore assumed that the D tablet would be useful when taken as a single drug in elderly and other patients in whom there are restrictions on water intake. There was no difference in numbers of patients who wished to continue taking the D tablet and the ordinary brotizolam tablet.In conclusion, the D tablet appears to be as resistant as other types of tablets to unit dose packaging, and it should be selected in favour of the ordinary tablet in accordance with the preference and condition of each patient. With a view to improving QOL and patient compliance, pharmacists should provide the necessary information on such tablets.

A Double‐Blind Comparison of Metoprolol CR/ZOK 50 mg and Atenolol 50 mg Once Daily for Uncomplicated Hypertension

In a double-blind study with parallel groups, the clinical bioequivalence of the antihypertensive effect of metoprolol CR/ZOK (controlled release formulation) 50 mg and atenolol 50 mg in ordinary tablets given once daily for uncomplicated hypertension was investigated. Clinical bioequivalence was defined as difference in blood pressure reduction less than 8 mmHg. The study involved 195 patients, 98 on metoprolol CR/ZOK and 97 on atenolol. All patients were taken off antihypertensive therapy during a 2-week placebo run-in period. Thereafter the patients were randomly allocated to metoprolol CR/ZOK 50 mg or atenolol 50 mg for 4 weeks. In patients with a diastolic blood pressure remaining above 90 mmHg, the dose was increased to 100 mg daily of the respective drug. After 4 weeks treatment with 50 mg of the two therapies, blood pressure and heart rate was significantly reduced in both treatment groups. At this dose, clinical bioequivalence was found regarding both blood pressure and heart rate reductions. After 8 weeks of therapy (100 mg doses given to 31 in the metoprolol group and 43 in the atenolol group), clinical bioequivalence according to stated definition was found for blood pressures and heart rate reductions, although the reductions of systolic and diastolic blood pressures at rest as well as diastolic blood pressure during exercise were significantly greater in the metoprolol group. In an evaluation of the responder rate after the 8 weeks of treatment, 89% of the patients in the metoprolol CR/ZOK group and 74% in the atenolol group (P less than .05) had a diastolic blood pressure reduction to 90 mmHg or less.(ABSTRACT TRUNCATED AT 250 WORDS)

Controlled-release therapeutic systems: technology applicable to the treatment of oral disease.

Controlled-release therapeutic systems are designed to deliver a pre-determined amount of drug to a specific anatomical site for an extended period of time. A single controlled-release delivery system no larger than an ordinary tablet or capsule and placed at the desired site of drug action can produce long-term therapeutic effects that previously could only be achieved through multiple administration of conventional dosage forms. Transient spikes in drug concentration seen with multiple dose regimens are eliminated, decreasing the chance of adverse reactions. Because they are effective for an extended period of time, controlled-release therapeutic systems minimize the involvement of the patient in drug administration , a factor which can increase both patient compliance with a prescribed regimen and patient satisfaction with the treatment schedule compared with conventional therapy. Controlled-release technology can be utilized to deliver therapeutic agents ranging in size from small ions to macromolecules. Clinically-proven controlled-release drug delivery systems are currently available with durations of action ranging from several days (e.g., for the prevention and treatment of angina pectoris and motion-induced nausea and the treatment of glaucoma) to one year (e.g. for contraception). A therapeutic system for contraception with a five-year effective lifetime is in clinical trial. Intra-oral controlled-release therapeutic systems are being investigated for the delivery of fluoride and antibiotics. A system for fluoride has reduced experimental dental caries in rats by over 50% and has significantly elevated salivary fluoride concentrations during a six-month trial in adolescents. Tetracycline-containing polymeric fibers can provide site-specific delivery of the antibiotic to periodontal pockets for 10 days or more. An intra-oral controlled-release pellet for tetracycline with a duration of action of one to two weeks is being developed, and additional possibilities exist for the intra-oral use of this versatile technology.

Pharmacokinetic and pharmacodynamic evaluation of gelatin microcapsule containing piretanide in beagle dogs.

A sustained-release property of gelatin microcapsules of piretanide was evaluated by pharmacodynamic parameters. The gelatin microcapsules of piretanide showed long-lasting, slow-release properties, when compared with its ordinary tablet form in the plasma piretanide level, piretanide excretion rate, urine excretion rate and urinary electrolyte (Na+, K+, Cl-) excretion rate without any loss in diuretic and saluretic activities, which fully satisfied the criteria for a sustained-release preparation.

Gossypol: a potential antifertility agent for males.

The discussion provides a general review of gossypol as a potential male contraceptive, focusing on the pharmacological features not discussed in previous review articles. Attention is directed to the chemistry of gossypol, the antifertility effect of gossypol, its metabolism and toxicity, the genetic and endocrine effects of gossypol; clinical trails of gossypol; hypokalemic paralysis; and the site and mechanism of action. Gossypol is a yellowish phenolic compound ocurring naturally in certain species of cotton plants of the family Malvaciae, mostly in the seeds and root bark. The Hubei Provincial group documented the antispermatogenic effects of crude cottonseed oil in rats and monkeys, and since then a number of workers have investigated the active principle(s) in cottonseed and cotton root bark. The work on gossypol as an antifertility agent, initiated by Liu (1957) and pursued actively, has stimulated nationwide attention. After publication of a review article by the National Coordinating Group, it attracted universal interest. 3 forms of gossypol -- gossypol, gossypol acetic acid, and gossypol formic acid -- have been used in laboratory investigations and clinical trials. They are very much the same in their biological activities and are discussed as a whole under the generic name gossypol. Unless psecified otherwise, the term refers to the racemate administered orally. There are pronounced differences among animal species in their sensitivity to the antifertility action of gossypol. Gossypol is absorbed through the intestine as well as through the epithelial lining of the stomach. In an attempt to mitigate the gastric side effects of gossypol, 1 group of clinicians adopted enteric-coated tablets for the clinical trial. They found that both the antifertiltiy effect and the systemic side effects of these tablets were much less than those of ordinary tablets. Gossypol is an effective antispermatogenic agent for certain susceptible animals and humans and represents the only approach which has a reasonable chance to reach the stage of large scale clinical testing before the end of this decade. Much work must be done, particularly in regard to its toxicology, before it (or 1 of its analogues) can be developed into a practical male antifertility drug. The following points suggest the main directions for future research in the scope of pharmacology and toxicology: hypokalemia -- exploration of the contributing factor(s), means to prevent its occurrence, mechanism(s) of development, production of animal model; irreversibility; general toxicological assessment; and studies on the mechanism of action, which also may be helpful in the development of gossypol analogue(s) exhibiting satisfactory antifertility and minimal toxic effects.

A comparison of sustained-release terbutaline and ordinary terbutaline in bronchial asthma

The effects and side effects in steady state of a sustained-release preparation of terbutaline 7.5 mg twice daily were compared with ordinary tablets 5 mg three times daily. The study performed for two weeks was double-blind, double-dummy, cross-over with randomized allocation of the drugs. 20 patients completed the trial and the results show higher mean morning PEFR values and a tendency to milder side effects with depot tablets.

Metoprolol excretion into breast milk.

British Journal of Clinical PharmacologyVolume 9, Issue 5 p. 518-519 Free Access Metoprolol excretion into breast milk. B. Sandstrom, B. SandstromSearch for more papers by this authorCG Regardh, CG RegardhSearch for more papers by this author B. Sandstrom, B. SandstromSearch for more papers by this authorCG Regardh, CG RegardhSearch for more papers by this author First published: May 1980 https://doi.org/10.1111/j.1365-2125.1980.tb05850.xCitations: 34AboutPDF ToolsRequest permissionExport citationAdd to favoritesTrack citation ShareShare Give accessShare full text accessShare full-text accessPlease review our Terms and Conditions of Use and check box below to share full-text version of article.I have read and accept the Wiley Online Library Terms and Conditions of UseShareable LinkUse the link below to share a full-text version of this article with your friends and colleagues. Learn more.Copy URL Share a linkShare onFacebookTwitterLinkedInRedditWechat No abstract is available for this article. References ERVIK, M. (1975). Quantitative determination of metoprolol in plasma and urine by gas chromatograhy. Acta pharmac. tox., 36, (suppl. V) 136– 144. JOHNSSON, G., JORDÖ, L., LUNDBORG, P., REGARDH, C.-G. & RÖN, O. (1980). Plasma levels and pharmacological effects of metoprolol administered as controlled release (Durules) and ordinary tablets in healthy volunteers. Int. J. clin. Pharmac. Biopharm. (in press). RASMUSSEN, F. (1958). Mammary excretion of sulphonamides. Acta pharmac. tox., 15, 139– 148. RASMUSSEN, F. (1959). Mammary excretion of benzyl-penicillin, erythromycin and penethamate hydroiodide. Acta pharmac. tox. 16, 194– 200. REGÅRDH, C.-G., BORG, K.O., JOHANSSON, R., JOHNSSON, G. & PALMER, L. (1974. Pharmacokinetic studies on the selective β1-receptor antagonist metoprolol in man. J. Pharmacokinet. Biopharm., 2, 347– 363. SANDSTRÖM, B. (1978). Antihypertensive treatment with the adrenergic β-receptor blocker, metoprolol, during pregnancy. Gynec. Obstet. Invest., 9, 195– 204. VON BAHR, C., COLLSTE, P., FRISK-HOLMBERG, M., HAGLUND, K., JORFELT, L., ORME, M., ÖSTMAN, J. & SJÖQVIST, F. (1976). Plasma levels and effects of metoprolol on blood pressure, adrenergic β-receptor blockade, and plasma renin activity in essential hypertension. Clin. Pharmac. Ther., 20, 130– 137. Citing Literature Volume9, Issue5May 1980Pages 518-519 ReferencesRelatedInformation

Moisture permeation of typical unit does repackaging materials

The moisture permeation of unit does repackaging materials used by various hospital and community pharmacies in a metropolitan area was studied. Commercial desiccant pellets were packaged in the same manner used for ordinary tablets and capsules. The samples were weighed and placed in a controlled chamber at about 75% relative humidity and 22 C, and tested for weight gain over a period of 4-10 days. Four types of packages were evaluated: (1) heat-sealed polyethylene bag, (2) polyvinyl chloride cups adhesive-sealed to multiple-ply paper, (3) heat-sealed "polycel-polyfoil" strip packages and (4) polyvinyl chloride/foil multiple-cup blister packs. A wide range of results was found. None of the containers tested was a good moisture barrier, although some offered protection for a limited time. Several needs were identified by this survey. Pharmacists need more information and an increased awareness concerning the permeation characteristics of repackaging materials, suitable operating procedures and the stability of pharmaceutical products. Standards must be established for repackaging materials as well as limits on storage periods for the repackaged pharmaceuticals. Procedures for pharmacists to test their own packaging systems, and a checklist of some important guidelines for repackaging in unit dose containers, are presented.

ALPRENOLOL IN ANGINA PECTORIS A COMPARATIVE STUDY OF THE TABLET FORM AND SLOW‐RELEASE FORMULATION

In a double-blind crossover trial in angina pectoris patients, alprenolol in a slow-release formulation (Aptin Durules) was compared with ordinary Aptin tablets. Four hundred mg per day in tablets given four times a day produced the same increase in exercise tolerance five hours after last intake as did an equivalent dose of slow-release formulation given twice per day nine hours after intake. Aptin Durules in double the dosage had a considerably greater effect. An optimal, sustained and antianginal effect of alprenolol is best achieved by giving 400 to 800 mg per day of slow-release formulation with 10 to 12 hours' dosage interval.

Rapid, Sensitive Colorimetric Method for Determination of Ethinyl Estradiol

A colorimetric procedure, based on the formation of an azo dye by condensation of diazotized 5‐chloro‐2, 4‐dinitroaniline with ethinyl estradiol, was developed. An alkaline solution of ethinyl estradiol is reacted with the reagent, and the resulting color is measured at 450nm. Absorbance versus concentration is linear up to 10 μg/ml; the lower limit of detection is 1 μg/ml under the conditions studied. Replicate analysis showed good agreement, and an average recovery of 99.6 ± 0.3% was obtained for analyses of synthetic mixtures. Vitamins and minerals likely to be present along with ethinyl estradiol in certain geriatric formulations, as well as ordinary tablet excipients and coating materials, do not interfere with the precision of the method or development of the color. The method is applicable to progestin‐estrogen preparations. Assay results on various single‐component as well as contraceptive commercial samples are reported.