Abstract: Certain amine containing phenolic pyrazines of formula III possess eukalemic diuretic properties and are of value in treating diseases and conditions in which a eukalemic diuretic effect is required, for example in treating edema, hypertension and/or related conditions.

Abstract: The invention concerns novel AVP-binding peptides having the formula:Thr-Met-X-Val-Leu-Thr-Gly-Ser-Pro-Bwherein X is selected from the group consisting of Lys, Arg, and Asp; B is OH, NH.sub.2, NHAlK, wherein Alk is lower alkyl of 1-4 carbons, inclusive. These peptides block AVP function, and, therefore, are useful in many areas among which is the control of hypertension.

Abstract: Antihypertension action is achieved without diuresis by administration of a thiazide diuretic in an amount which while being sufficient to achieve antihypertension is insufficient to achieve diuresis. Such administration in a non-diuretic amount is effected in 4-8 consecutive hourly doses to achieve reduction of blood pressure without high urine output. The invention further relates to complexes of thiazides with mixed cation-anion exchange resins, to insoluble basic metal hydroxy thiazide salts, the salts of thiazide with calcium disodium edetate or disodium edetate, to molecular complexes of thiazides with long chain polymers such as hydroxy alkyl cellulose polymers, carboxy methyl cellulose and polyvinylpyrrolidone, to beta-adrenergic blocking amine-thiazide salts and to amiloride thiazide salts.

Abstract: The present invention provides an aqueous, alkaline injection solution of torasemide ready for injection, which contains a physiologically compatible alkaline buffer with a pH value of from 9.3 to 9.9 and with a buffer capacity of up to 0.1 val/liter together with an organic solvent in an amount of from 5 to 20% by weight selected from the group of polyethylene glycols with a molecular weight of from 100 to 1500, polypropylene glycols with a molecular weight of from 50 to 1000, glycerol, propylene glycol, ethanol and propanol, the torasemide being present in a concentration of from 2 to 40 mg/ml. Torasemide solutions are useful to inhibit inflammation or promote diuresis.The present invention also provides a process for the preparation of this solution, wherein torasemide is suspended in the above organic solvent brought into solution by the addition of aqueous alkali, adding the buffer and other adjuvants and adjusting the pH value to 9.3 to 9.9.

Abstract: A diuretically active combination comprising furosemide and triamterene in a ratio of 1:1 to 1:2, in which furosemide is in the form of controlled release so as to facilitate solubilization of the furosemide in triamterene micelles to stabilize the combination as mixed micelles of low polydispersity yielding dissolution rates in in vitro tests of furosemide of not more than about 1.5% after about one hour at pH 1.5 to 3.5 and a slow release of not more than about 4.5% at pH 5.5 concurrent with a release of triamterene of about 60-70% and 80%, respectively, and with a release of not more than 85% furosemide after eight hours at pH 7.5 in salt solutions of adjusted pH.

Abstract: Xanthone derivatives of the formula (I): ##STR1## wherein W, X, Y and Z which may be the same or different represent a hydrogen atom, a halogen atom or a lower alkyl group having 1 to 4 carbon atoms; A is a hydrogen atom B is a hydroxymethyl group, a lower alkoxycarbonyl group having 1 to 4 carbon atoms, or a carboxyl group, provided that a --O--CH.sub.2 --B group is bonded to the 2- or 3-position of the xanthone ring and that there is no case in which X, Y, and Z are each a hydrogen atom concurrently; as well as intoxic salts thereof when B is a carboxyl group, and a process for preparing the same are disclosed.The compounds of formula (I) in accordance with the present invention are useful as diuretics having uricosuric activity and can be used in the treatment of edema or hypertension.

Abstract: A pharmaceutical composition comprises magnesium oxide, hydroxide or a non-toxic salt of magnesium in a slow-release carrier; this material may be combined with or co-prescribed with a diuretic or cardiac glycoside or adrenergic receptor blocking agent or a calcium antagonist for the treatment of hypertension or angina pectoris.

Abstract: Novel 1,2-benzisoxazoloxyacetic acids and related compounds, methods for preparing same and methods of treatment by administering compositions containing such a compound are described. These compounds are useful as diuretic, uricosuric and antihypertensive agents.

Abstract: Pharmaceutical preparations having diuretic activity and comprising a peptide of the formula ##STR1## wherein (a) R.sub.1 and R.sub.2 are hydrogen and R.sub.3 is --OH, or ##STR2## or Y, or wherein (b) R.sub.1 is hydrogen, R.sub.2 is CH.sub.2 OH or ##STR3## and R.sub.3 is --OH or Y, or wherein (c) R.sub.1 is --CH.sub.2 OH and R.sub.2 is hydrogen or ##STR4## and R.sub.3 is --OH or Y, or wherein (d) R.sub.1 is ##STR5## R.sub.2 is hydrogen or --CH.sub.2 OH and R.sub.3 is --OH, --NHCH.sub.2 COOH, or Y, andwhereinX is hydrogen, methyl, prolyl, or an N-protective group, andY is --NH.sub.2, --OR.sub.4, wherein R.sub.

Abstract: Microdroplets of water-insoluble drugs coated with a phospholipid are prepared by sonication. As an example, microdroplets of the general anesthetic methoxyfluorane coated by a unimolecular layer of dimysistoyl phosphatidylcholine are prepared by sonication. The microdroplets so prepared remain stable in physiologically-compatible solution, and are suitable for injection, typically intradermally or intraveneously, into a patient for inducing local anesthesia. These methoxyflurane-containing microdroplets have been demonstrated to cause long-term local anesthesia when injected intradermally, giving duration of anesthesia 28 times longer than with other anesthetics, such as lidocaine and 11 times longer than with bupivacaine. The latter is considered longest acting conventional local anesthetic.

Abstract: A controlled release pharmaceutical composition including a solution or suspension vehicle and a pharmaceutically active agent. The composition is administered to the body in a normally liquid formulation and thereafter forms a semi-solid gel-like matrix in the environment of the stomach thereby effecting controlled release of the pharmaceutically active agent.

Abstract: A gelatin capsule dosage form containing triamterene, 2,4,7-triamino-6-phenylpteridine, which results in rapid dissolution of the active ingredient. The dosage form comprises the pharmaceutical binder methylcellulose in combination with low doses of a surfactant or a carbonate salt as disintegrants.

Abstract: Muscle protein breakdown or degradation may be reduced or inhibited in mammals, particularly humans recovering from surgery or suffering from a muscle wasting disorder, by administering daily doses of alpha-ketoisocaproic acid (ketoleucine) or an appropriate salt of the acid. Seventy millimoles per day of sodium alpha-ketoisocaproate administered for five days after major abdominal surgery was found to significantly reduce urinary 3-methylhistidine/creatinine, which is a measure of muscle protein breakdown, and thereby to improve nitrogen balance.

Abstract: Imidazothiadiazolealkenecarboxamides of the formula ##STR1## in which R.sup.1 is hydrogen, aryl, substituted aryl or a cyclic or aliphatic hydrocarbon radical which is optionally interrupted by O, S, N, N-alkyl, N-aryl or N-aralkyl and which is optionally substituted,R.sup.8 having the meaning indicated for R.sup.1, andX representing oxygen, sulphur or the radical NR.sup.9 R.sup.10,the other radical having various definitions, and acid addition salts thereof, exhibit hypotensive activity.

Abstract: Diuretic and natriuretic extracts, at least partially characterized as peptides, have been obtained by homogenization of mammalian heart atria with an aqueous solution of a lower carboxylic acid. After precipitation of impurities by pH adjustment, the extract may be further purified chromatographically. Extracts injected into text rats resulted in 30-40 fold increases in sodium and chloride excretions within 5-10 minutes of injection. Urine volume rose 10-15 fold and potassium excretion doubled. The response was complete in 20 minutes and no similar changes in renal function were observed following injection of a similarly obtained ventricular extract.

Abstract: Diuretics containing an efficient amount of L- or DL-threo-3-(3,4-dihydroxyphenyl)-serine or a pharmaceutical acceptable salt thereof are applied orally or parenterally. They are effected particularly to anasarca patients. They will also be effective to myxedema, Addison's disease and other ADH-excessive syndrome patients. They are applied in the form of tablet, capsules, syrup, suspension or liquid.

Abstract: Acylcarnitines used as drug absorption enhancing agents for orally and rectally administered drugs.

Abstract: A storage-stable highly active muzolimine composition comprising by weight about(a) 100 parts of muzolimine(b) 40-500 parts of starch(c) 20-100 parts of cellulose(d) 0.2-5 parts of silica, and(e) 0.1-3 parts of stearic acid, Ca stearate, Mg stearate and/or talc.

Abstract: This invention relates to derivatives of 3-propionylsalicylic acid represented by the formula (1) ##STR1## wherein R represents a hydrogen atom, a lower alkyl group or a group ##STR2## (wherein R.sup.1 and R.sup.2 represent a lower alkyl group or R.sup.1 and R.sup.2, when taken together with the nitrogen atom to which they are attached, may form a heterocyclic ring with or without an intervening hetero atom, and n is an integer of 1 to 4), and X represents a hydrogen atom or a halogen atom, R being the group ##STR3## when X is a hydrogen atom. This invention also relates to processes for preparing the same.

Abstract: Rapid dissolving uniform compositions of low water solubility drugs are formed from a dry mixture of the drug having a reduced particle size in combination with properly selected and sized excipients including microcrystalline cellulose, dibasic calcium phosphate, starches and a lubricant.