Abstract: A method of formulating insulin compositions comprises preparing a carrier having a phosphatidylcholine component which entraps insulin, stabilizing insulin compositions at room temperatures.

Abstract: The present invention relates to compositions and methods for transdermal drug delivery comprising formulating a phosphatidylcholine carrier composition containing the drug and applying the composition to the skin.

Abstract: A stable composition of a drug comprising a carrier having a phosphatidylcholine component which entraps the drug is applied to the skin for transdermal delivery of the drug.

Abstract: The invention relates to a combined pharmaceutical preparation comprising parathyroid hormone and a bone resorption inhibitor, said preparation being adapted for (a) the administration of parathyroid hormone during a period of approximately 6 to 24 months; (b) after the administration of parathyroid hormone has been terminated, the administration of a bone resorption inhibitor during a period of approximately 12 to 36 months.

Abstract: A method of spherifying a sustained release ionic conjugate which contains a free carboxyl group-containing polymer and a free amino group-containing drug which are ionically bonded to each other.

Abstract: Pharmaceutical compositions that include a drug-oligomer conjugate, a fatty acid component, and a bile salt component are described. The drug is covalently coupled to an oligomeric moiety. The fatty acid component and the bile salt component are present in a weight-to-weight ratio of between 1:5 and 5:1. Methods of treating diseases in a subject in need of such treatment using such pharmaceutical compositions are also provided, as are methods of providing such pharmaceutical compositions.

Abstract: A method for oral administration of an active principle includes the steps of incorporating an active principle in multilamellar vesicles having a diameter of between 0.1 and 25 &mgr;m, and a lamellar liquid-crystal internal structure formed, from the center to the periphery of the vesicles, of a stack of concentric bilayers based on amphiphilic agents alternating with layers of water, aqueous solution or solution of a polar liquid, and orally administering a composition containing the active principle incorporated within the vesicles.

Abstract: Calcitonins and calcitonin derivatives such as are employed for therapy for, for example, osteoporosis. Paget's disease or hypercalcemia. The calcitonins and calcitonin derivatives are distinguished by a bridging of the amino acids present in the positions 17 and 21. In this case, by means of a suitable choice of the amino acids present in these positions an 18- or 19-membered ring is produced. This ring leads to an increased conformational stability and to an increased activity of the modified calcitonin. A particularly suitable hCt (human Ct) analog is the cyclo17,21-[Asp17, Orn21]-hCt according to the invention having a 19-membered ring structure between the lactam-bridged Asp17 and Orn21.

Abstract: A method of treating an individual to increase the individual's bone mineral density (BMD) is disclosed. The method includes co-administering a calcitonin-like agent and a DHEA-like agent. Also disclosed are methods for potentiating the effect of treatment with a calcitonin-like agent on BMD and for increasing BMD in an individual being treated with DHEA, e.g., for treatment of systemic lupus erythematosus (SLE).

Abstract: A mixed micellar aerosol pharmaceutical formulation includes a micellar proteinic pharmaceutical agent, an alkali metal lauryl sulphate, at least three micelle forming compounds, a phenol and a propellant. The micelle forming compounds are selected from the group consisting of lecithin, hyaluronic acid, pharmaceutically acceptable salts of hyaluronic acid, glycolic acid, lactic acid, chamomile extract, cucumber extract, oleic acid, linoleic acid, linolenic acid, monoolein, monooleates, monolaurates, borage oil, evening of primrose oil, menthol, trihydroxy oxo cholanyl glycine and pharmaceutically acceptable salts thereof, glycerin, polyglycerin, lysine, polylysine, triolein, polyoxyethylene ethers and analogues thereof, polidocanol alkyl ethers and analogues thereof. The amount of each micelle forming compound is present in a concentration of from 1 to 20 wt./wt. % of the total formulation, and the total concentration of micelle forming compounds are less than 50 wt./wt. % of the formulation.

Abstract: A composition for enteral administration having a non-ionic vegetable oil GIT absorption enhancer capable of increasing the enteral absorbability of drugs, especially oral absorbability of hydrophilic and macromolecular drugs. The non-ionic vegetable oil GIT absorption enhancer, particularly Babassu oil or a derivative thereof, is capable of enhancing the uptake of a drug from the gastrointestinal tract so as to allow therapeutically effective amounts of the drug to be transported across the GIT of an animal such as a human without significant toxic side effects.

Abstract: Superpotent calcitonin analogs have greatly increased hypocalcemic action in vivo. These calcitonins and calcitonin derivatives are employed for the therapy of, for example, osteoporosis, Paget's disease or hypercalcemia. The calcitonins and calcitonin derivatives are distinguished by a bridging of the amino acids present in the positions 17 and 21. By means of suitable choice of the amino acids present in these positions an 18-membered or 19-membered ring is produced. This ring leads to an increased conformational stability and to an increased activity of the modified calcitonin. A particularly suitable hCt (human calcitonin analog) is a cyclo17,21-[Asp17, Orn21]-hCt having a 19-membered ring structure between the lactam-bridged Asp17 and Orn21.

Abstract: A composition for permucosal administration characterized by containing Antago-3 or a physiologically acceptable salt thereof, and a sucrose fatty acid ester. With the composition for permucosal administration of the invention there is provided a long-term stable preparation having the high permucosal absorption of physiologically active peptide Antago-3 without irritation.

Abstract: Disclosed is a sustained release pharmaceutical composition. The composition includes a polyester containing a free COOH group ionically conjugated with a bioactive polypeptide comprising at least one effective ionogenic amine, wherein at least 50% by weight of the polypeptide present in the composition is ionically conjugated to the polyester.

Abstract: Pharmaceutical compositions and methods for the treatment of osteoporosis in mammals are disclosed. The compositions are suitable for parenteral administration and comprise Insulin-Like Growth Factor I (IGF-I) and a pharmaceutically acceptable carrier. The compositions for use in the methods may also include bone antiresorptive compounds.

Abstract: Peptides useful in the regulation of calcium metabolism are disclosed. Also disclosed are pharmaceutical compositions of matter containing such peptides as well as a method for the regulation of calcium metabolism in a patient in need of such treatment. The peptides contain modified or unmodified portions of an amino acid sequence at the 8- to 32-positions of native calcination.

Abstract: Bioavailability of peptide active agents to be administered orally is enhanced by a pharmaceutical composition providing targeted release of the peptide to the intestine by virtue of an acid-resistant protective vehicle which transports components of the invention through the stomach. The composition includes an absorption enhancer and a sufficient amount of a pH-lowering agent to lower local intestinal pH. All components are released together into the intestine with the peptide.

Abstract: This invention relates to novel salts composed of a cation derived from a peptide containing at least one basic group and an anion derived from a carboxy-terminated polyester, processes for the manufacture of such salts, and the use of such salts in the manufacture of extended release pharmaceutical compositions. The salts of the invention possess a variety of properties which are useful in the formulation of extended release pharmaceutical compositions, whether the salts are in pure form or are in admixture with either an excess of the peptide in its free, unbound form or an excess of the free polyester.

Abstract: Compositions useful in the delivery of active agents are provided. These delivery compositions include (a) an active agent; and either (b)(1) a carrier of (i) at least one amino acid and (ii) at least one diketopiperazine or (b)(2) at least one mono-N-substituted, di-N-substituted, or unsubstituted diketopiperazine. Methods for preparing these compositions and administering these compositions are also provided.

Abstract: Tasteless, hydrolyzed collagen from gelatin, gelatin or animal collagenic connective tissue having an average molecular weight of from 1 to 40 kD for the preparation of agents for the treatment of osteoporosis. It may be combined with conventional agents for combatting osteoporosis, such as calcitonin, calcium salts, and/or progesterone.

Abstract: Microemulsion preparation in which a plurality of specified surfactants are combined such that aqueous-phase droplets that contain a physiologically active substance of low absorption and which have an average size of 0.4-100 nm are dispersed in an oil-phase dispersion medium. In order to improve its low transdermic or transmucosal absorbability, the physiologically active substance is allowed to be present as dissolved in the aqueous-phase droplets in the W/O emulsion. The preparation is low in local irritation and uses neither malodorous substances such as higher alcohols nor conventional absorption enhancers.

Abstract: This invention relates to novel salts composed of a cation derived from a peptide containing at least one basic group and an anion derived from a carboxy-terminated polyester, processes for the manufacture of such salts, and the use of such salts in the manufacture of extended release pharmaceutical compositions. The salts of the invention possess a variety of properties which are useful in the formulation of extended release pharmaceutical compositions, whether the salts are in pure form or are in admixture with either an excess of the peptide in its free, unbound form or an excess of the free polyester.

Abstract: Disclosed is a sustained release pharmaceutical composition. The composition includes a polyester containing a free COOH group ionically conjugated with a bioactive polypeptide comprising at least one effective ionogenic amine, wherein at least 50% by weight of the polypeptide present in the composition is ionically conjugated to the polyester.

Abstract: The present invention relates to an improved intravaginal preparation containing a physiologically active peptide, which comprises a physiologically active peptide, a sucrose fatty acid ester and an organic acid with a pharmaceutically acceptable carrier or diluent, by which the physiologically active peptide can be absorbed safely and efficiently.

Abstract: Pharmaceutical compositions for nasal administration comprising i) a calcitonin, and ii) benzalkonium chloride, and/or iv) a surfactant, suitable for application to the nasal mucosa, in iii) a liquid diluent or carrier, suitable for application to the nasal mucosa. The compositions are suitably adapted for administration in the form of a nasal spray.

Abstract: Pharmaceutical compositions for nasal administration comprising i) a calcitonin, and ii) benzalkonium chloride, and/or iv) a surfactant, suitable for application to the nasal mucosa, in iii) a liquid diluent or carrier, suitable for application to the nasal mucosa. The compositions are suitably adapted for administration in the form of a nasal spray.

Abstract: Pharmaceutical compositions comprising a calcitonin and a polyglycolysed glyceride and a method of enhancing the transdermal or transmucosal absorption of calcitonin in a mammal are disclosed.

Abstract: Derivatized calcitonin molecules, pharmaceutical compositions comprising derivatized calcitonins, and methods of reducing serum calcium in a patient using the derivatized calcitonins are disclosed. The molecules are characterized by a derivatized amino terminus formed by combining a calcitonin with a cyclic, polycyclic or heterocyclic moiety. Multimeric forms of the molecules are also disclosed.

Abstract: Compositions useful in the delivery of active agents are provided. These delivery compositions include (a) an active agent; and either (b)(1) a carrier of (i) at least one amino acid and (ii) at least one diketopiperazine or (b)(2) at least one mono-N-substituted, di-N-substituted, or unsubstituted diketopiperazine. Methods for preparing these compositions and administering these compositions are also provided.

Abstract: Nanoparticles containing an active substance and a ketalized polytartramidic acid, process for their preparation, and use thereof. Nanoparticles containing an active substance and a ketalized polytartramidic acid are suitable as vehicles for active substances, in particular for peptides and proteins. Processes for the preparation of the nanoparticles are described.

Abstract: A composition including a polyester containing one or more free COOH groups ionically conjugated with a bioactive polypeptide comprising at least one effective ionogenic amine, wherein the polyester contains a member selected from the group of L-lactic acid, D-lactic acid, DL-lactic acid, .epsilon.-caprolactone, p-dioxanone, .epsilon.-caprolic acid, alkylene oxalate, cycloalkylene oxalate, alkylene succinate, .beta.-hydroxybutyrate, substituted or unsubstituted trimethylene carbonate, 1,5-dioxopan-2-one, 1,4-dioxepan-2-one, glycolide, glycolic acid, L-lactide, D-lactide, DL-lactide, meso-lactide, and any optically active isomers, racemates or copolymers thereof, and at least 50%, by weight, of the polypeptide present in the composition is ionically conjugated to said polyester.

Abstract: A prolonged releasing pharmaceutical preparation is provided carrying a physiologically active substance, particularly, calcitonin gene-related peptide (CGRP) or a maxadilan (MAX). This pharmaceutical preparation can attain the expected effects by incorporating the physiologically active substance into a combination, as carriers for the physiologically active substance, of a cellulosic polymer and at least one auxiliary component selected from the group consisting of fats and oils, waxes, fatty acids, saccharides and polyacrylate ester derivatives. The pharmaceutical preparation can conveniently be used, in living bodies, particularly as an intrathecal implantation-type preparation.

Abstract: The invention provides a polypeptide of calcitonin analogue and use thereof. The polypeptide has such an amino acid sequence that proline-amide residue (Pro-NH.sub.2) at C-terminal of native eel calcitonin is substituted to a homoserine amide residue (Hse.multidot.NH.sub.2).

Abstract: A method for treating a patient suffering from any of osteoporosis, Paget's disease and hypercalcemia by intranasally administering to said patient by spray a calcitonin solution consisting of calcitonin dissolved in a 0.9% aqueous sodium chloride solution free of quaternary ammonium compounds and surfactants, the calcitonin being in a concentration of 100-5000 IU per ml. of composition.

Abstract: A pharmaceutical composition in the form of a colloidal suspension of nanocapsules, comprising an oily phase consisting essentially of an oil containing dissolved therein a surfactant and suspended therein a plurality of nanocapsules having a diameter of less than 500 nanometers, said nanocapsules encapsulating an aqueous phase consisting essentially of a solution or a suspension of a therapeutically active substance, a surfactant and optionally ethanol; a process for preparing the said composition is also described. The walls of said nanocapsules are formed from a poly(alkyl 2-cyanoacrylate) wherein the alkyl radical has 1 to 6 carbon atoms. This composition is particularly suitable for oral administration of polypeptides and polysaccharides.

Abstract: A pharmaceutical composition is prepared in the form of microparticles or of an implant comprising a biodegradable polymer selected from poly-1,4-butylene succinate, poly-2,3-butylene succinate, poly-1,4-butylene fumarate and poly-2,3-butylene succinate, incorporating as the active substance the pamoate, tannate, stearate or palmitate of a natural or of a synthetic peptide comprising 3 to 45 amino acids, such as LH-RH, somatostatin, GH-RH or calcitonin, or one of their synthetic analogues or homologues. The preparation comprises dry blending the ingredients in the form of powders, pre-compressing and preheating the mixture and then extruding the pre-compressed and pre-heated mixture. The product resulting from the extrusion step can then be comminuted and finally sieved.

Abstract: A freeze-dried pharmaceutical composition for parenteral administration which includes a therapeutically effective amount of a calcitonin, as the active ingredient, and human albumin.The injectable solution which is obtained by dissolving the freeze-dried composition in a physiologically acceptable solvent is also described.

Abstract: A large intestinal dissociative hard capsule comprising a capsule mainly composed of chitosan, the viscosity at 20.degree. C. of a solution obtained by dissolving the chitosan in an aqueous 1% by weight acetic acid solution being not higher than 100 cps and the degree of deacetilation of the chitosan being from 60 mol % to 98 mol %, having a coated layer of a polymer soluble in a liquid having pH of at least 5 on the surface of the capsule.

Abstract: The present invention is to provide emulsion preparations for nasal administration containing calcitonins, which are safely and effectively administrated compared with the conventional calcitonin preparations. The emulsions are prepared by using a calcitonin as the active ingredient, an azacycloalkane derivative as the absorption promotor such as 1-[2-(decylthio)ethyl] azacyclopentan-2-one, and glycyrrhizic acid or its salt.

Abstract: A new use of calcitonin, as an active principle, is provided for the preparation of topically appliable medications in the treatment of pre-senile and senile idiopathic cataract; and a pharmaceutical composition containing elcatonin as active principle for the preparation of a collyrium.

Abstract: A method for preparing a pharmaceutical composition in the form of microparticles, the composition thus obtained and its use for preparing injectable suspensions.

Abstract: Suppositories comprising a suppository base, a calcitonin and taurocholic acid or a pharmaceutically acceptable salt thereof exhibit improved bioavailability and are well tolerated.

Abstract: A liquid composition for nasal administration of polypeptide/s containing ammonium tartrate and a buffer together with optional adiuvants.

Abstract: Pharmaceutically active substances are administered in aerosol form by applying to a mucosal surface of the body a composition comprising a medically effective amount of a pharmaceutically active substance, a biocompatible amphiphilac steroid and a bicompatible (hydro/fluoro)carbon propellant.

Abstract: Compositions for the administration of protein or peptide drugs across membranes show low toxicity and efficient permeation when the medium is a mixture of a bile salt or fusidate with a nonionic detergent. Various specific compositions are exemplified.

Abstract: Solid nasal inserts of calcitonin and other peptides have particularly interesting drug absorption profiles.

Abstract: The present invention provides an aqueous solution composition containing elcatonin as an active ingredient used for hypercalcemia or bone Paget's disease or improvement of pain in osteoporosis, etc. and which is highly stable against shaking, light and heat. This composition contains an effective amount of elcatonin as an active ingredient and a monocarboxy compound and/or its water soluble salt thereof in a molar concentration of 0.05-20 mmol and has a pH of 5.0-6.5 and an ionic strength of .mu.=0.01-0.5. Preferred examples of the monocarboxy compound and its salts are acetic acid, lactic acid, L-histidine, sodium acetate, potassium acetate, sodium lactate, potassium lactate and L-histidine hydrochloride.

Abstract: Medicinal compositions containing a water soluble absorption promoter having chelating activity, preferably in the presence of a salt at a concentration exhibiting higher osmotic pressure than isotonic sodium chloride solution, to promote absorption of the medicine through a gastrointestinal organ such as colon or rectum, and through the vagina.

Abstract: The invention relates to a substance from the calcitonin group, which substance can be isolated from the human body or can be obtained in a different manner, but clearly differs from the known human calcitonin-(1-32), the said substance having hypocalcaemic activity.

Abstract: A liposome-entrapped calcitonin composition and method of use is disclosed. The composition when parenterally administerd to a host mammal, produces an enhanced and prolonged hypocalcemic effect in said mammal and thus is useful in treating diseases related to abnormal skeletal metabolism. The liposomes are substantially free of cholesterol and may be single or multilamellar.