Abstract: Biological control agents such as pathogenic bacteria and viruses have been encapsulated in a protective, starch matrix without the use of chemical crosslinking agents. The agent is blended into a dispersion of pregelatinized starch, which is thereafter subjected to conditions suitable for retrogradation. Dispersions can be formulated either for recovery of dry granules or as sprayable liquids. Encapsulated products are useful in controlling insects and other pest species having chewing mouth parts and amylase digestive enzymes.

Abstract: The present invention relates to an ingestible aggregate comprising a pre-swelled substantially anhydrous hydrocolloid and a substrate. More particularly this invention relates to an aggregate having as a substrate a dietary fiber and/or drug wherein the composition can be administered in a therapeutically effective amount. Hydrocolloids useful include natural and modified gums, celluloses, modified celluloses, pectins, mucillages, modified starches, noncellulose polysaccharides, algal polysaccharides and mixtures thereof. The aggregate should be in the size range of about 4 to about 70 U.S. mesh. The unpleasant taste and mouthfeel of the fiber and/or drug is effectively masked and substantial hydration is delayed until the composition reaches the stomach. The compositions are substantially more platable, devoid of graininess, bitterness or fibrous texture. The pleasant taste of the composition encourages patient compliance with their fiber or drug therapy.

Abstract: 5-Amino or substituted amino 1,2,3-triazoles are disclosed as a new class of antiproliferative agents useful in the treating and managing of psoriasis, inflammatory bowel syndrome, cutaneous leishmanilisis and certain types of cancer.

Abstract: The invention provides an immunizing agent or preparation e.g. a vaccine for parenteral administration comprising particles of coalesced and covalently interlinked physiologically compatible proteinaceous molecules and, entrapped in these particles, an immunogen adapted to be released by the gradual proteolysis of the particles and, when so released, being of sufficient size to elicit an immuno response to characteristic immunogenic determinants of the immunogen. The proteinaceous molecules are preferably homotypic for the animal to be immunized. Preferably, the particles or molecules carrying the immunogenic determinants are crosslinked to the proteinaceous molecules.

Abstract: A biocompatible, biodegradable, bioerodible composite polymer matrix comprising interleukin-2 in an appropriate polymer. The polymer may be a polymer or copolymer of lactic acid, lactide, glycolide, glutamic acid, or it may be collagen or albumin. The material contains from 10.sup.2 to 10.sup.8 U IL-2/g of polymer. Also disclosed is a method for making the composite polyer matrix and a method for implanting the material. A soft, malleable controlled-release composite material may be used for intracranial or other implantation and may be shaped or molded to fit the site from which malignant tissue has been removed, opposing the residual tumor, complementing hemostasis, compatible with anatomical structure, and functioning as an implantable immunotherapeutic adjuvant.

Abstract: Anti-smoking oral preparations are provided containing a silver compound as the anti-smoking agent and a sweetener in which the silver compound is present in amounts of from 0.1 mg. to 2.5 mg. and the ratio of sweetness intensity based on sucrose to silver compound content is from 100:1 to 2500:1.

Abstract: The invention involves a method for making uniformly sized particles from water-insoluble drugs or other organic compounds. First, a suitable solid organic compound is dissolved in an organic solvent, and the solution can be diluted with a non-solvent. Then, an aqueous precipitating liquid is infused, precipitating non-aggregated particles with substantially uniform mean diameter. The particles are then separated from the organic solvent. Depending on the organic compound and the desired particle size, the parameters of temperature, ratio of non-solvent to organic solvent, infusion rate, stir rate, and volume can be varied according to the invention.

Abstract: Controlled release drug delivery systems comprised of spherical microporous polymeric network of interconnecting channels containing pore incorporated drugs or other agents wherein the drugs or agents are confined within the pore channel are described. Also disclosed are processing parameters in connection with the novel method of the invention for obtaining drug delivery systems especially suited for parenteral as well as oral administration.

Abstract: Virtually any material may be encapsulated in a starch matrix by combining the material with a high temperature-stabilized dispersion of starch, optionally in the presence of salt. The temperature-stabilized starch dispersion acts as a protective colloid, encasing the material to be encapsulated. Upon subsequent rapid cooling of this mixture on a chilled surface the starch polymer chains collapse upon themselves, forming a firm sheet or the like and encapsulating the core material. The sheet can then be cut, chopped or sliced in the wet state, then dried and ground to yield particles.

Abstract: A controlled release treatment composition and method of use are disclosed. The composition includes a bioadhesive and an effective amount of a treating agent. The bioadhesive is a water-swellable, but water-insoluble, fibrous, cross-linked carboxy-functional polymer containing (a) a plurality of repeating units of which at least about 80 percent contain at least one carboxyl functionality, and (b) about 0.05 to about 1.5 percent cross-linking agent substantially free from polyalkenyl polyether.

Abstract: A controlled-release pharmaceutical unit dosage form is provided comprising a gelatin capsule enclosing a solid matrix formed by the cation-assisted gellation of a liquid fill incorporating vegatable gum and a pharmaceutically-active compound, as well as methods for the preparation thereof.

Abstract: Novel compositions for topical application of a water-insoluble bioactive reagent, e.g. a pesticide, comprising an aqueous emulsion of a polymer swellable by the sebum and other "skin oils" and which will agglomerate or coagulate near the skin, the polymer having the bioactive agent encapsulated or dispersed therein; and novel methods employing the same for controlled release of the bioactive reagent over an extended period of time.

Abstract: A mixture of a cyclodextrin and an alkoxy silane compound, e.g., tetraethoxy silane, is admixed with water and an acidic or alkaline catalyst, e.g., acetic acid, to effect ligand exchange and hydrolysis of the alkoxy silane followed by gelation into a gelled mass which is dried and, preferably, leached with water to remove excess of the cyclodextrin. The thus obtained gelled material is a composite having a structure in which the cyclodextrin molecules are incorporated into the matrix of amorphous silica presumably by forming Si-O-C linkages. The composite has characteristics as a combination of the properties of both of the component materials and can expand the applicability of the materials, for example, as a carrier of catalysts and immobilized enzymes, absorbent and adsorbent and so on.

Abstract: The present invention relates to a new oral pharmaceutical composition having an improved release of the therapeutically active compound present therein, in the lower part of the gastro-intestinal duct having a pH exceeding 4.5, comprising as a core a therapeutically active compound in the form of a weak base, or a weak acid, on which core there is applied a first, inner layer of a diffusion membrane in the form of ethyl cellulose, and/or a copolymer of polyethyl methacrylate-methyl methacrylate-trimethylammonium ethyl methacrylate chloride, and thereabove a second layer is applied of at least one anionic polymer and/or fatty acid having a pk.sub.a of 4.5 to 7.The invention further relates to a process for the preparation of said composition, a pharmaceutical composition containing said composition, and a method for the treatment using such a composition.

Abstract: The invention relates to a novel method of producing slow-release pharmaceutical forms administered per os, by simultaneously employing two resins having anionic character, the proportions of said resins being variable.By varying the ratio of the amounts of active principles on the respective two resins, it is possible to modify the release kinetics of active principle; and by independently varying the amount of carboxylic resin it is possible to produce stabile pharmaceutical preparations which are in liquid, semi-liquid, or solid form.

Abstract: As a composition for transdermal drug delivery, the gelation reaction product of a mixture of an organic polysaccharide gum, polyethylene glycol, and m-, p- or o-hydroxybenzoic acid in an amount effective in forming from such mixture a gel having adhesive properties for adhesion to skin and being sufficiently pliant to conform to the shape of body contours.

Abstract: A miticidal composition for controlling spider mite populations is formed by impregnating a controlled release substrate with farnesol and nerolidol to form a flowable liquid concentrate or wettable powder. The flowable liquid concentrate or wettable powder is added to a liquid spray base to which a miticide has been added, and mixed therewith to form the miticidal composition. The resulting composition is applied by conventional tank spray equipment to the foliage of plants or trees to control spider mite populations therein.

Abstract: A solid sustained-release preparation in the form of a needle-like or bar-like shape, which consists essentially of an active ingredient and a pharmaceutically acceptable biodegradable carrier (e.g. proteins, preferably collagen, gelatin, and a mixture thereof). The sustained-release preparation can be administered to the body or implanted into the body by injection or an injection-like method and can release the active ingredient at an effective level for a long period of time when administered.

Abstract: A medicament adsorbate of analgesics and process for making same. The medicament adsorbate comprises a complex magnesium aluminum silicate having sorbed therein an analgesic. The complex magnesium aluminum silicate has the following typical chemical analysis:______________________________________ Ratio to Percent by Weight Aluminum Oxide ______________________________________ Silicon dioxide 56 to 59 14.0 to 29.5 Magnesium oxide 21 to 24 5.2 to 12.0 Aluminum oxide 2.0 to 4.0 1 Ferric oxide 0.4 to 0.6 Calcium oxide 1.1 to 1.5 Sodium oxide 2.5 to 3.5 Potassium oxide 0.5 to 1.0 Ignition Loss 5.5 to 12.

Abstract: The rectal absorption of the beta-lactam antibiotic ceftriaxone in a solid dosage form is enhanced with chenodeoxycholic acid or its sodium salt, in the presence of a carrier consisting of a mixture of two or more glycerides of C.sub.12 to C.sub.18 fatty acids.

Abstract: A medicament adsorbate of decongestants and process for making same. The medicament adsorbate comprises a complex magnesium aluminum silicate having sorbed therein a decongestant. The complex magnesium aluminum silicate has the following typical chemical analysis:______________________________________ Ratio to Percent by Weight Aluminum Oxide ______________________________________ Silicon dioxide 56 to 59 14.0 to 29.5 Magnesium oxide 21 to 24 5.2 to 12.0 Aluminum oxide 2.0 to 4.0 1 Ferric oxide 0.4 to 0.6 Calcium oxide 1.1 to 1.5 Sodium oxide 2.5 to 3.5 Potassium oxide 0.5 to 1.0 Ignition Loss 5.5 to 12.

Abstract: A medicament adsorbate of antiasthmatics and process for making same. The medicament adsorbate comprises a complex magnesium aluminum silicate having sorbed therein an antiasthmatic. The complex magnesium aluminum silicate has the following typical chemical analysis:______________________________________ Ratio to Percent by Weight Aluminum Oxide ______________________________________ Silicon dioxide 56 to 59 14.0 to 29.5 Magnesium oxide 21 to 24 5.2 to 12.0 Aluminum oxide 2.0 to 4.0 1 Ferric oxide 0.4 to 0.6 Calcium oxide 1.1 to 1.5 Sodium oxide 2.5 to 3.5 Potassium oxide 0.5 to 1.0 Ignition Loss 5.5 to 12.

Abstract: A synthetic resin matrix system for the delayed and extended duration delivery of drugs to humans and animals is disclosed consisting of a polymer, such as poly(2-hydroxyethylmethacrylate), referred to as PHEMA, an organic solvent, such as polyethylene glycol (PEG), and a hydrogen binding plasticizer, such as dimethylsulfoxide (DMSO). The plasticizer regulates the set-up time of the synthetic resin so that the more plasticizer present, the shorter the set-up time. The plasticizer also has a direct shortening effect upon the cure time and also profoundly influences many of the physical characteristics of the resultant synthetic resin matrix system. A variety of drugs can be embodied in the fabricated matrix system and administered to the patient (or animal) by different modes of application, including but not limited to oral, topical, rectal, subcutaneous implant, or organ-specific implant such as in the conjunctival sac of the eye.

Abstract: Dump release microcapsules are formed of a water-reswellable gel having dispersed therein a sorbtive filler material having a median particle size of not more than 1 micron, such as fumed or precipitated silica. The filler material has an active substance absorbed therein and/or adsorbed thereon. The active material can be 2-chloro-6-(trichloromethyl) pyridine and the gel formed from crosslinked lignin or a lignosulphonate.

Abstract: This disclosure recognizes the fact that the technology of making vesicles from lecithin and lecithin-like molecules, although well known and highly developed, is associated with problems of instability. It is known that vesicles coalesce, rupture and spill their contents long before the vesicle is used for its intended purpose.It has been discovered and disclosed herein that the deterioration of the vesicle delivery system is due in part to the rupture of the bipolar lipid vesicle membrane by the contents of the core volume or by an external agent. For example, the more detergent-like the properties of the pharmacological agent within the vesicle core volume, the more pronounced will be the attack on the vesicle wall interior. These events in turn will lead to vesicle membrane rupture.

Abstract: The release of an active composition from a solid tablet can be delayed by employing a fine particle sized hydroxypropyl methylcellulose ether composition.

Abstract: Suppositories containing as the active substance a therapeutically effective amount of ceftriaxone, a pharmaceutically compatible salt thereof or a hydrate of one of these compounds, a stabilizer consisting of a mono-, di- or triglyceride of a C.sub.12 -C.sub.18 -fatty acid or of a mixture of such glycerides, a potentiator consisting of an aliphatic C.sub.2 -C.sub.18 -fatty acid, a mono-, di- or triglyceride of a C.sub.2 -C.sub.12 -fatty acid, a partial ester or complete ester of propylene glycol, polyethylene glycol or a carbohydrate with a C.sub.2 -C.sub.12 -fatty acid, a pharmaceutically compatible ester or ether thereof or of a mixutre of the said potentiators and, if desired, customary therapeutically inert adjuvants for suppositories, and their manufacture are described. These have valuable antimicrobial properties.

Abstract: The invention relates to topical antiinflammatory medicament formulations which also have analgesic activity and contain 2-(2-hydroxyethoxy)-ethyl N-(.alpha.,.alpha.,.alpha.,-trifluoro-m-tolyl) anthranilate as the active ingredient and an adjuvant which is preferably a triglyceride.

Abstract: The invention comprises pharmaceutical preparations consisting generally of a drug with a substantially low water solubility and an amorphous, water-soluble cyclodextrin-based mixtures. In these preparations a stable amorphous state can be achieved. This improves the dissolution properties of the drug and hence its absorption by the body. The required cyclodextrin-based mixtures were prepared from .alpha.-, .beta.-, or .gamma.-cyclodextrin which were rendered amorphous through non-selective alkylation. The alkylation agents suitable for that purposes are exemplified by propylene oxide, glycidol, iodoacetamide, chloroacetate, or 2-diethylaminoethylchloride; their reactions with cyclodextrins were performed in a manner to yield mixtures containing many components, a circumstance which effectively prevents crystallization processes within the above pharmaceutical preparation.

Abstract: A synthetic resin matrix dressing is disclosed consisting essentially of a polymer, such as poly(2-hydroxyethylmethacrylate), referred to as PHEMA, an organic solvent, such as polyethylene glycol (PEG), and a hydrogen bonding plasticizer, such as dimethylsulfoxide (DMSO). The plasticizer regulates the set-up time of the synthetic resin so that the more plasticizer present, the shorter the set-up time. The dressing may be applied to the treatment site in veterninary use in the form of a paste for the in-situ curing or setting thereof, or the dressing may be preformed and then applied to the treatment site. A variety of drug agents may be incorporated in the synthetic resin matrix so as to result in the time released administration of the drug agent to the area of the skin covered by the dressing. A method of treatment using this dressing is also disclosed.

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 absorption diltiazem formulation for oral administration comprises a pellet having a core of diltiazem or a pharmaceutically acceptable salt thereof in association with an organic acid and a lubricant, and an outer membrane which permits release of diltiazem in an aqueous medium at a controlled rate which is substantially pH independent. The pellet has a dissolution rate in vitro, which when measured according to the Paddle Method of U.S. Pharmacopoeia XX, is not more than 10% of the total diltiazem after 2 hours of measurement in a buffered medium. Not more than 30% of the total diltiazem is released after a total of 4 hours measurement and not more than 40% of the total diltiazem is released after a total of 6 hours. 100% release is achieved after 12 hours, with a maximum of 80% of the total diltiazem being released after 8 hours.

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 controlled absorption methyldopa formulation for oral administration comprises a pellet having a core of methyldopa or a pharmaceutically acceptable salt thereof in association with an organic acid, and an outer membrane which permits release of methyldopa in an aqueous medium at a controlled rate which is substantially pH independent. The pellet has a dissolution rate in vitro, which when measured in a Basket Assembly according to U.S. Pharmacopoeia XX at 37.degree. C. and 75 r.p.m., is not more than 50% of the total methyldopa after one hour of measurement. Not more than 80% of the total methyldopa is released after a total of 3 hours of measurement and 100% release is achieved after a total of 7 hours.

Abstract: The invention relates to a device for the controlled release of one or more active ingredients to a liquid, particularly a controlled release pharmaceutical tablet obtained by compressing a mixture of two granulates in a weight ratio of 30:70 to 70:30, said granulates having particle sizes of 0.4-2.0 mm. One of the granulates, the restraining phase granulate, comprises one or more active ingredients dispersed in a matrix of an insoluble substance, and the other granulate, the housing phase granulate, comprises a soluble material and a penetration rate limiting material, one material optionally having both functions. In the compressed device, the granulates form two distinct phases, each of which is continuous. The housing phase fills large continuous pores in the restraining phase. A zero-order release rate can be obtained with the devices.

Abstract: A vehicle which provides rapid release of a drug and prolonged release of a drug is disclosed.

Abstract: Solid tablets of a therapeutically active composition exhibit sustained release properties when compressed with a fine particle sized hydroxypropyl cellulose ether composition.

Abstract: A transdermal therapeutic system using a subsaturated matrix is provided having improved approved release characteristics. Reinforcing means preferably in the form of a fabric are embedded in the upper surface of the subsaturated matrix. At least a portion of the reinforcing means is selected such that the active agent to be delivered to the skin has a solubility, C.sub.r therein which is lower than the initial solubility C.sub.o of the agent in the matrix. In addition, the relationship between the diffusion coefficients of the agent in the matrix D.sub.m and the portion of reinforcing means D.sub.r and the solubilities is given by the relationship: D.sub.r .multidot.C.sub.r <D.sub.m .multidot.C.sub.o. In operation the agent dissolved in the reinforcing means acts as a secondary reservoir improving the release characteristics of the system. Specific embodiments of the invention are particularly adapted for scrotal and labial delivery of drugs such as testosterone and progesterone.

Abstract: A rectally administered unit dosage form comprising a therapeutically effective amount of an analgesic , an antipyretic or an anti-inflammatory agent capable of being absorbed into the bloodstream from a rectal compartment and an adjuvant, said adjuvant comprising lecithin present in said dosage form in a sufficient amount to be effective in enhancing and prolonging the absorption rate of said analgesic, antipyretic or anti-inflammatory agent from the rectal compartment into the bloodstream, in conjunction with a nontoxic, pharmaceutically acceptable carrier and the methods of using said unit dosage form.

Abstract: A delivery system useful in chewing gum, confectionary and pharmaceutical products comprising:(a) an insolubolized active ingredient; and(b) a cross-linked hydrocolloid multivalent cation alginate or carageenenate matrix entrapping said insolubolized active ingredient.A process of preparation is also disclosed.

Abstract: Delivery vehicles comprised of a polymeric bead having a network of pores with an active ingredient held within the network are provided for use in a method to provide controlled release of the active ingredient. The network of pores is substantially non-collapsible upon removal of the active ingredient and the delivery vehicles are polymerized by a process in which the active ingredient also comprises the porogen during formation of the network of pores.

Abstract: Particles containing a releasable fill material and method of preparing same. A particle comprises a continuous polyurea surface layer, and an interior portion comprising a polyurea matrix, said matrix having a fill material contained therein, said matrix forming a continuum extending from the surface layer into the interior of the particle.

Abstract: A delivery device for zero-order release of an active principle into a dissolution fluid includes a reservoir consisting of a solid matrix of a homogeneous mixture of a polymer material, at least a portion of the active principle and an additive soluble in the dissolution fluid with negative heat of solution, a coating on the solid matrix-type reservoir of a first, release rate-controlling insoluble membrane which modulates the active principle release according to the desired kinetics; and a second, protective membrane on the release rate-controlling membrane of a soluble polymer material.

Abstract: A novel pharmaceutical composition is disclosed. It comprises a sustained release pharmaceutical carrier suitable for admixture with active ingredients comprising:(a) 5.5-98.5% by weight of hydroxypropyl methylcellulose;(b) 0.25-4.5% by wieght of hydroxypropyl cellulose;(c) 1-90% by weight of a carboxyvinyl polymer.

Abstract: Pharmaceutical compositions are provided which contain hollow fine tube drug delivery systems. The compositions comprise a pharmaceutically suitable carrier, preferably in the form of a capsule, tablet, suspension, or suppository, and at least one drug delivery system which consists essentially of (1) a polymeric tube having a membrane outer sheath and a hollow core, and (2) at least one drug compound contained within the core, said system contained in the composition in an amount sufficient to deliver a therapeutic amount of the drug contained therein at a predetermined rate over a predetermined period of time. By varying the polymer, the permeability of the outer sheath, the drug, the drug concentration in the hollow core of the tube, the tube diameter, the tube length, the tube core diameter, and the sealing of the tube ends, a wide variety of drug therapeutic amounts, rates and dosing times can be achieved.

Abstract: A controlled release implant composition which includes a core comprising a macromolecular drug and a water insoluble polymer and a homogeneous outer polymeric membrane formed by coating said core with an organic solution of a water insoluble polymer and a water soluble pore-forming agent.

Abstract: A compressed powder formulation which consists essentially of an organophilic clay and at least one topical agent. The formulation maintains its physical integrity upon handling thereby permitting the preparation of the formulation in the form of self-supporting sticks and exhibits an acceptable level of payout. Additionally, the formulation retains an acceptable level of payout even when contacted with water. A process of making the formulation by compressing a powderous mixture is also set forth.

Abstract: A slow-release composite having pyroglutamyl-histidyl-triptophyl-seryl-tyrosyl-D-leucyl-leucyl-arginyl-pro line ethylamide or a salt thereof encapsulated in a polymer matrix and a process the same are herein disclosed.

Abstract: A process for the preparation of solid pharmaceutical products, wherein, in a first step, spherical single crystals of a pharmaceutical active compound or assistant are prepared by agitating a saturated aqueous, organic or organic-aqueous solution in high speed stirred crystallizers or draft-tube crystallizers at 50-500 revolutions per minute and seeding the solution with finely ground seed crystals of particle size less than 100 .mu.m, while ensuring that at the time of addition of the seed crystals and during the growth thereof the solution is at all times only minimally supersaturated, this being achieved by slow cooling at a rate of not more than 50 K/h or corresponding slow evaporation of the solution, and in a second step the resulting spherical single crystals with diameters of 0.1-3 mm, preferably 0.5-2 mm, are separated from the solution, dried at 40.degree.-200.degree. C.

Abstract: Treatment of cellular disorders involving abnormal solid cellular growths involves introduction of cytotoxic reagents dispersed in a physiologically acceptable proteinaceous matrix into the solid cellular growth or area of an existing or removed solid cellular growth. Enhanced effectiveness of the drug is observed, with reduced cytotoxic effects on cells distant from the site of introduction. Other drugs may be included to enhance therapeutic gain and reduce adverse affects to normal tissue.