Galenical Preparations Research Articles

The life path of A.M. Khaletsky

Many brilliant scientists, professors, whose life and fate were directly connected with the history of the university, worked at the St. Petersburg State Chemical and Pharmaceutical University. Our national pharmacy owes their talent and enthusiasm.
 Based on unpublished archival records, the article reconstructs the biography, professional, scientific and social activities of Abram Mikhailovich Khaletsky, a wellknown chemist, professor, Doctor of Chemistry, who made a great contribution to the development of Russian science, who for many years worked as the Head of the Department of Pharmaceutical Chemistry of the Leningrad Pharmaceutical Institution. A graduate of the Medical Department of Kazan University, a student of Academy A.E. Favorsky, he took an active part in the reformation of the educational process of the LCPI. It was A.M. Khaletsky who proposed a new form of appraisal of pharmacists at that time the defense of theses, the first of them were performed at the Department of Organic Chemistry. Among the scientific achievements made under the leadership of A.M. Khaletsky: studies of isomeric changes of keto-alcohol, technology for the production of standard galenical preparations, the method of isolation of -sitosterol, improvement of hormone technology and the search for new hormonal drugs, and many others. Actively promoted the integration of scientific developments in the pharmaceutical industry. Research by Professor A. M. Khaletsky undoubtedly enriched the theory and practice of organic and pharmaceutical chemistry, made the contribution to the science of the relationships between biological structure and activity, replenished the range of medicine with new drugs and methods of their analysis.
 The article provides information about the work of one of the oldest departments of the Leningrad Chemical and Pharmaceutical Institute - pharmaceutical chemistry during the leadership of A.M. Khaletsky (1950-x).

The strategic importance of vaccination for national defense and security

Public health is the most important power factor of a nation, from which all other factors derive. Infectious diseases are the most important cause of morbidity and mortality in humans. Vaccination is the most important method of prophylaxis of infectious-contagious diseases. Mass implementation of vaccination prevents the occurrence of epidemics, epizootic diseases or homonymous pandemics, and at the individual level ensures the specific active immunity (total or partial). So the vaccination of the population and/or the risk groups is of strategic importance to the nation, both in peacetime and in time of war. The national antidote production along with anti-infectives (vaccines, therapeutic serums, immunomodulators, antimicrobial chemotherapies and pesticides) has a strategic importance for the health of the population and of the troops. Biological crisis situations are cases of force majeure, where the Medicines Law provides the exception for manufacturing and use, even without a ""marketing authorization"". The military scientific research could make micro-production of specific drugs (antidotes, antiinfectives) for the needs of the army and the risk groups of the population. An example would be the preparation of vaccines for the prophylaxis of diseases caused by BWA and bioterrorism as niche products. Nothing hinders the preparation of any medication, such as magistral and galenical preparations, or pilot batch, provided there is adequate space, equipment, staff and procedures according to the law or the exception.

TECHNOLOGY OF MEDICINES AND GALENICAL PREPARATIONS: THE CASE OF PRESCRIPTION FORMULASFROM “ANTIDOTARIUM” NICOLAI BY NICHOLAS OF SALERNO

Introduction. This study deals with the problem of similarity of the principles and approaches of drug technologies in the medieval manuscript “Antidotarium Nicolai” by Nicholas of Salerno with modern pharmaceutical technologies.The aim of study is a textual investigation of “Antidotarium Nicolai”, a detailed research of the content of the manuscript, recipes and technologies for making medicines.Materials and methods. In order to achieve this goal, eighty-five recipes of “Antidotarium Nicolai” have been identified, systematized and analyzed in a documentary translation from medieval French. An interdisciplinary study of the content of the manuscript was carried out with the help of factor analysis of the historical source and modern scientific literature.Results and discussion. Having described the content and aspects of the prescriptions of “Antidotarium Nicolai”, the authors note the similarity of the technologies of drugs and galenical preparations with modern pharmaceutical technology, in particular, with the technology of pharmacy production. In “Antidotarium Nicolai” it is stated that preparations based on herbal medicinal raw materials may be second-line therapy agents for completing treatment after the application of basic pharmacological preparations.Conclusion. The results of this work reveal the potential for the use of herbal medicines in the conditions of modern evidence-based medicine, in particular, in the organization of long-term treatment and secondary prevention of chronic diseases in patients who need to maintain their ability to work, and provide them with a sufficiently high level of quality of life. A detailed translation of the full text of the manuscript, the analysis of its content in accordance with the requirements of rational pharmacotherapy and phytotherapy, further favors to identify the prospects for the development of new drugs, multi-component in their chemical composition with a wide range of therapeutic effects.

TECHNOLOGICAL PARAMETERS OF COUNTERCURRENT EXTRACTION: DERIVING BIOACTIVE COMPOUNDS FROM PLANT RAW MATERIALS

Wild-growing plants produce a wide range of vitamins, macro- and microelements, mineral salts and other biologically active substances. Even in minute quantities, these constituents can mediate the healing effect on a human body. To date, the most promising method of extracting biologically active compounds from crude wild plant material is solvent extraction. The intensification of the extraction process has seen a new development in the last few years. This paper focuses on obtaining maximum yield of bioactive compounds from wild-growing plants, such as ordinary cowberry, prickly wild rose, sea-buckthorn, ordinary rowan, guelder-rose by a countercurrent extraction method, a continuous process where the plant material moves against the solvent. With that, it examines various extraction agents and their mixtures in relation to the extractives and total flavonoid content, the optimal time of the duration of the extraction. The optimal temperature of the process was found to be corresponding to the boiling point of the solvent. In the future, this study might contribute to the development of high quality new galenical preparations with maximum content of biologically active substances identical to the composition of the source plants to produce pharmaceutical drugs, food supplements, functional foods and cosmetics.

CP-048 Multidisciplinary management as a resource for metabolic diseases: cooperation between clinicians and pharmacists in an Italian centre for rare diseases

BackgroundThere are almost 8,000 rare diseases (RD) (80% are genetically based) and 50% of them affect children. They are often highly complex metabolic diseases (MD): factors include heterogeneity (age of...

Total Phenolic Content and Antioxidative Properties of Commercial Tinctures Obtained from Some Lamiaceae Plants

The antioxidant level of commercial tinctures from three Lamiaceae plants, Salvia officinalis, Mentha piperita, and Melissa officinalis, have been determined by the Folin-Ciocalteu method, the 2.2-diphenyl-2-picrylhydracyl hydrate (DPPH) radical scavenging technique and ABTS assay. Total phenolic content was expressed as GAE (gallic acid equivalent) and ranged from 0.24 to 3.99 mg/mL. Antioxidant activity in the ABTS assay, calculated as TEAC (Trolox equivalent antioxidant capacity), ranged from 23.5 to 35.6 micromol Trolox/mL, while in the DPPH method, the EC50 value ranged from 0.04 to 0.07 mL/assay. Radical scavenging activity was correlated with total phenolic content. Correlations between ABTS and F-C methods, DPPH and F-C methods and ABTS and DPPH methods were calculated. The obtained results can be useful as additional information about the antioxidant activity of galenical preparations.

Tratamiento de la hipercolesterolemia y prevención de las enfermedades cardiovasculares mediante la inhibición de la reabsorción de ácidos biliares con resincolestiramina

Cholestyramine resin is a bile acid sequestrant that reduces low-density-lipoprotein cholesterol (LDL-c) through partial interruption of enterohepatic bile acid circulation. This drug has no systemic effects and consequently can be used in women of reproductive age, in children and in patients with muscular, liver or renal disorders. Cholestyramine resin should be administered separately from other drugs. This agent boosts the lipidlowering effect of statins, as well as that of fibrates, nicotinic acid and ezetimibe. Adding cholestyramine resin to statin therapy reduces LDL-c by an additional 20%, equivalent to a 3-fold increase in the statin dose. A meta-analysis of eight clinical trials found that resins reduced mortality from cardiac causes by 30% (OR 0.70; 95% CI 0.50–0.99), a figure not lower than that observed with statins. Cholestyramine resin reduces postprandial glycemia and glycosylated hemoglobin and consequently is of particular interest in the treatment of hypercholesterolemia in patients with metabolic syndrome or type 2 diabetes who have failed to achieve LDL-c targets with statin monotherapy. Previously used resin preparations often produced gastrointestinal intolerance, while the new galenical preparations of cholestyramine resin used at a dose of 4–8 grams (1–2 sachets) per day – sufficient to obtain a lipid-lowering effect – are usually well tolerated.

The determination of morphine in opium and some of its galenical preparations.

Abstract A method of assay for morphine in opium depending upon precipitation of the dinitrophenylether with 1-fluoro-2:4-dinitrobenzene has been critically examined. The morphine is first separated from other alkaloids and extraneous matter by elution from an alumina column with an organic solvent and subsequent extraction with alkali. The method, which is rapid, has been applied to many galenical preparations and, in cases where the pharmacopoeial method based on the colorimetric nitroso reactions may give high results, figures in accordance with the expected values have been obtained.

The colorimetric determination of morphine in galenical preparations.

Abstract Methods by which morphine may be determined colorimetrically are discussed and the present official method criticised. The reaction described by Pride and Stern, which depends upon the oxidation of morphine with iodic acid followed by treatment with ammonium bicarbonate and nickel chloride to give a green colour has been found satisfactory. Improved extraction procedures for the separation of morphine from extraneous material in a number of galenical preparations are suggested and application of the colorimetric reaction to morphine residues so obtained, is described.

A Photoelectric Colorimetric Method for the Estimation of Khellin

Summary A photoelectric colorimetric method for the assay of khellin is described. This method is recommended for the assay of pure khellin in pharmaceutical preparations. The assay is carried out within the limits of 0ṁ1 to 1 mg. of khellin. Work is proceeding for the application of this method on galenical and other pharmaceutical preparations. The results will be compared with those obtained by the other colorimetric methods. The authors wish to express their thanks to the Memphis Chemical Co. for the help extended to them in carrying out this work and for the supply of pure khellin and instruments involved.

Vegetable purgatives containing anthracene derivatives. Part III. Galenical preparations of senna pod.

Journal Article Vegetable Purgatives Containing Anthracene Derivatives: Part III. Galenical Preparations of Senna Pod Get access J W Fairbairn, J W Fairbairn Pharmacognosy Research Laboratory, School of Pharmacy, University of London, and the Westminster Laboratories, Ltd., London, N.W.1 Search for other works by this author on: Oxford Academic Google Scholar I Michaels I Michaels Pharmacognosy Research Laboratory, School of Pharmacy, University of London, and the Westminster Laboratories, Ltd., London, N.W.1 Search for other works by this author on: Oxford Academic Google Scholar Journal of Pharmacy and Pharmacology, Volume 2, Issue 1, September 1950, Pages 813–830, https://doi.org/10.1111/j.2042-7158.1950.tb13004.x Published: 12 April 2011 Article history Received: 06 July 1950 Published: 12 April 2011

A double‐blind dose‐escalating trial comparing novel mesalazine pellets with mesalazine tablets in active ulcerative colitis

Mesalazine as the treatment standard for ulcerative colitis can be applied in different galenical preparations. A novel formulation of mesalazine pellets with delayed and prolonged release characteristics was compared with conventional Eudragit L-coated tablets. Furthermore, the effect of mesalazine dose escalation on nonresponders was evaluated in both treatment groups. A total of 233 patients with mild to moderately active ulcerative colitis were randomized to receive either mesalazine (1.5 g/day in three doses) as pellets (n = 115) or tablets (n = 118) for 8 weeks. At insufficient response, the dose was increased to 3.0 g. The clinical remission rate (clinical activity index < or = 4) for pellets was 67% vs. 68% for tablets which statistically proved to be not inferior (significance level alpha = 2.5%). In patients without dose increase, the remission rate was 47% (pellets) vs. 42% (tablets). Endoscopic improvement was observed in 80% (pellets) vs. 83% (tablets), and histological improvement in 48% (pellets) vs. 52% (tablets) of patients. Mesalazine pellets are as effective as tablets in the treatment of mild to moderately active ulcerative colitis. Dose escalation to 3.0 g/day is a valid option for nonresponders to a starting dose of 1.5 g/day.

The rise and fall of strophanthin

The strophanthins, which we now know to be steroidal cardiac glycosides, were isolated from African plant sources (arrow poisons) in the late 19th century. By the 1880s, galenical preparations of strophanthus were commonly prescribed for cardiac patients as a substitute for digitalis. Intravenous (IV) strophanthin-K was popularised for the treatment of cardiac failure between 1910 and 1935. Experimental use of strophanthin-G (ouabain) in animals undergoing hypovolaemic shock in the 1940s prompted its IV use for the treatment of shock in man in the 1950s. Textbooks of anaesthesia recommended the strophanthins for resuscitation and treatment of shock until the 1970s, but by the 1980s, such use had waned.

Drug release in vitro--an aid in clinical trials?

The topic of this article is biopharmacy. Using delayed release tablets with the active ingredient theophylline as a practical example, it was demonstrated that prior to clinical trials, galenical preparations can be characterized according to drug release in vitro and, that profiles of in vitro drug release can be compared with each other (LEVY-plot). Drug release from the retard tablets was examined following the Cube Root Law which describes the dependency of release rate on surface and agitation. Comparing profiles of in vitro release to a hypothetical or even known profile of in vivo release, produce results that are open to interpretation (LEVY-plot). A postulated correlation between the nonanalogous parameters, relative bioavailability and the mean in vitro dissolution time was confirmed. Due to established in vitro/in vivo correlations, we can in our case, predict the hypothetical in vivo release profiles for tablets showing more or less retarded release profiles in vitro and the relative bioavailability can be estimated. In addition, prediction of blood level is possible. In vitro/in vivo correlations can also provide information about residence times of the delayed release tablets in components of the gastrointestinal tract (stomach, small bowel and large bowel). Thus, using these methods, delayed release tablets (with the active ingredient theophylline) can be optimized for their use in clinical trials.

Wirksamkeit und Verträglichkeit von Dexamethasonpalmitat i.a.: Vergleich mit Dexamethason-Kristallsuspension im entzündlichen Schub

Liposomes and lipid microspheres are completely new galenical preparations that can deliver the necessary amount of drugs to the target disease sites (drug targeting) by working as suitable drug carrier vehicles. In a controlled multicentre clinical trial efficacy and tolerance of Lipotalon (dexamethasone palmitate incorporated in lipidmicrospheres) and dexamethasonacetate crystalline suspension were compared in 196 patients suffering from gonarthrosis in the acute phase. 98 patients were given 3 ml dexamethasonepalmitate (= 7.5 mg dexamethasone) in lipidmicrospheres into their inflamed knee joint and 98 patients got an intra-articular injection of 2 ml dexamethasoneacetate (= 7.23 mg dexamethasone). Efficacy was evaluated by the activityindex, need for a second injection and judgement of the doctors. Tolerance was judged by the number of adverse events. Significant improvements were observed in all parameters at all times of evaluation in both groups, After 14 days Lipotalon showed better improvements than dexamethasoneacetate, but there were no significant difference between the two groups during the whole 3 months of treatment. The number of patients with adverse events after Lipotalon (9 patients) did not differ significantly from that of dexamethasoneacetate (12 patients), but in contrast to crystalline formulations, crystalline-induced synovitis is not to be expected. Based to these results, Lipotalon is an outstanding drug with potent anti-inflammatory properties for the treatment of acute inflammatory states in rheumatoid arthritis, leading to fast and long-lasting antiphlogosis and analgesia.

Measurement by isotope dilution mass spectrometry of 17 alpha-ethynyloestradiol-17 beta and norethisterone in serum of women taking oral contraceptives.

The highly specific and accurate technique of isotope dilution mass spectrometry has been used for the measurement of 17 alpha-ethynyloestradiol-17 beta and norethisterone in serum. Serum samples were obtained from female volunteers who received 2.5 mg lynestrenol and 50 micrograms 17 alpha-ethynyloestradiol-17 beta in two different galenical preparations. The determination of total 17 alpha-ethynyloestradiol-17 beta (conjugated and non-conjugated) was carried out by the following procedure: (1) adsorption of the steroids from 1 ml serum to Amberlite XAD-2; (2) enzyme hydrolysis of the conjugated steroid; (3) addition of 1 ng [6,7-3H2] 17 alpha-ethynyloestradiol-17 beta as internal standard; (4) column chromatography on Sephadex LH 20; (5) derivative formation with heptafluorobutyric anhydride; (6) isotope dilution mass spectrometry at m/z 474 and 478 using a glass capillary gas-liquid chromatography column. For the measurement of norethisterone, which is the major metabolite of lynestrenol, 1 ng [7-3H]norethisterone was added to 0.5 ml serum. The labelled and the non-labelled steroids were extracted and purified by column chromatography on Sephadex LH 20. The norethisterone was reacted to form the 3-enol-17 beta-trimethylsilyl ether of norethisterone and [3H]norethisterone. For isotope dilution mass spectrometry the derivative was injected into the glass capillary column which was coupled to the mass spectrometer. The instrument was adjusted to m/z 442 and 444, corresponding to the molecular ions of the ether derivatives of norethisterone and [7-3H]norethisterone. Accuracy was achieved by the use of highly specific technique of mass spectrometry and the exact control of recovery using the isotope dilution principle. The precision was 4.5% (CV) for the determination of 17 alpha-ethynyloestradiol-17 beta and 2.5% (CV) for norethisterone. The lower limit of detection was at 20 pg ml-1 for both methods.

Editorial: The ADR numbers game.

Since the first galenical preparations were administered to sick individuals, physicians have known that the drugs themselves have the potential of producing adverse and, occasionally, fatal effects. Indeed, iatrogenic disease resulting from drugs is a recognized and accepted hazard of medical practice. The aim of rational drug therapy, therefore, is to choose the course of treatment that will achieve the desired therapeutic results with the least amount of drug-associated toxicity. Although these facts are obvious to all physicians, the lay public has recently been subjected to a macabre numbers game about fatal adverse drug reactions (ADRs) that is as alarming as it is sensational. In 1972, Talley and Laventurier 1 presented a paper in which they estimated that 30,000 deaths caused by ADRs occurred the previous year in the United States. This figure lay fallow until late 1973, when it was picked up by Senator Kennedy during the drug hearings

An improved method for the colorimetric assay of thiacetazone in pharmaceutical preparations.

An improved colorimetric procedure for the determination of thiacetazone (tibione) has been developed. It is based on the complete hydrolysis of tibione in a concentrated alkaline medium, after which the hydrolytic product is subjected to diazotisation and coupling with α-naphthylethylenediamine dihydrochloride. The procedure suggested in this paper eliminates some disadvantages of the original method and affords reproducible assay results for tibione in galenical preparations.

A Quantitative Radiometric Determination of Alkaloids Using Labelled Potassium Tetra-iodomercurate

Introduction A microquantitative radiometric method for the determination of alkaloids in galenical and pharmaceutical preparations was thougt to be valuable specially when spectrophotometric methods are not reliable.

Crude Vegetable Drugs And Their Galenical Preparations Versus Active Principles Derived Therefrom

Crude Vegetable Drugs And Their Galenical Preparations Versus Active Principles Derived Therefrom