138 results about "Intestinal fluid" patented technology

A pharmaceutical composition comprising a cyclosporin solid-state microemulsion is disclosed. In a preferred embodiment, the composition comprises a cyclosporin microemulsion dispersed in an enteric carrier. The composition does not dissolve in external phases such as artificial gastric fluid, but dissolves rapidly in artificial intestinal fluid, whereby it releases the cyclosporin microemulsion, providing rapid delivery of cyclosporin. The composition effectively maintains a therapeutic blood concentration of cyclosporin with once a day dosing, providing for convenience of administration and avoiding adverse effects induced by increasing peak blood cyclosporin concentrations associated with conventional cyclosporin formulations.

There is provided an orally-administrable formulation for the controlled release or stable storage of a granulated isoflavone-enriched fraction or mixture of such fractions, comprising at least one granulated isoflavone-enriched fraction and at least one carrier, diluent or excipient therefor. Preferably, the formulation is characterized in that the total in vitro dissolution time of said formulation required for release of 75% of the active ingredients available from the formulation is between about 4 and about 18 hours, as determined by the U.S.P. XXIII paddle method at a paddle speed of 75 rpm, using simulated intestinal fluid without the digestive enzymes normally found in intestinal fluid, at pH 6.8, and a temperature of 37° C. A process for the preparation of such a formulation is also provided.

Enteric compositions comprising one or more tight junction agonists and/or one or more tight junction antagonists are provided. Compositions of the invention may comprise a delayed-release coating disposed over a tight junction agonist and/or tight junction antagonist layer which may be disposed over an inert core. Delayed-release coatings may be substantially stable in gastric fluid and substantially unstable in intestinal fluid, thus providing for substantial release of the tight junction agonist and/or antagonist from the composition in the duodenum or jejunum of the small intestine.

The invention discloses lactobacillus plantarum with the inhibitory activity to alpha-glucosidase. The lactobacillus plantarum is classified and named as Lactobacillus plantarum, is preserved on August 29, 2017 in China General Microbiological Culture Collection Center and has a preservation number of CGMCC NO.14573. By screening, the lactobacillus plantarum has in-vitro inhibitory activity to alpha-glucosidase; the survival rate of the lactobacillus plantarum reaches up to 71.04% under an acid condition that the pH value is 2.0 and is 77.14% in 2.0% cholate deionized water, the tolerances of the lactobacillus plantarum to artificially simulated saliva and intestinal fluid are higher than 90%, the tolerance of the lactobacillus plantarum to gastric fluid reaches 52.49%, and after artificially simulated fluid is sequentially digested, the survival rate reaches 88.27%; the lactobacillus plantarum has good effects on the prevention and treatment of diabetes mellitus type 2; the lactobacillus plantarum is added with a protection agent so as to prepare freeze-drying battier powder with a high viable count, and the viable count reaches up to 87% of the viable count before freeze-drying; and besides, the lactobacillus plantarum further has a good fermentation effect.

The invention relates to a method for preparing a Lactobacillus casei microcapsule. 2-6 percent of microporous starch solution and 2-6 percent of sodium alginate solution are respectively taken as inner and outer wall materials of the microcapsule; the characteristic that small holes overspread on the surface of the microporous is utilized to absorb a bacteria solution; then sodium alginate and calcium chloride are utilized to generate ion exchange to form a sodium alginate coating; and double layer embedment is carried out on Lactobacillus casei. After the Lactobacillus casei microcapsule is dried at the temperature of 2-6 DEG C for 36-72h, the obtained microcapsule has stronger acid resistance and cholate resistance and high storage stability, i.e. the microcapsule is not dissolved in simulated gastric fluid basically and does not leak but is immediately disintegrated in simulated intestinal fluid; after the Lactobacillus casei microcapsule is treated in 0.3 percent of cholate solution for 1h, the thalli survival rate is 88 percent, and the number of viable bacteria is increased to 1.24*109cfu/g from 5.80*109cfu/g after the Lactobacillus casei microcapsule is stored at the temperature of 4 DEG C for 1 month. The invention greatly increases the survival rate of Lactobacillus casei in products and the use ratio of Probiotics and also enriches the variety of the Probiotics microcapsule.

Formulations have been developed to improve the solubility of corticosteroids such as fluticasone proprionate in a composition designed to achieve localized release of the drug in the small intestine and/or colon. In one embodiment, solid dispersions of fluticasone are prepared wherein the drug is blended with or coated onto a highly water soluble substrate such as nonpareil (sugar beads) then coated with a layer of polymer soluble in small intestinal fluid, then coated with an enteric coating. The inner polymer layer controls release of the drug, and the enteric coating, a pH sensitive polymer that is broken down in the ileum and colon, controls localized release of drug at various sites within the gastrointestinal tract. The multilayer pharmaceutical composition can be in the form of pellets, tablets compressed from pellets or pellets packed into capsules. The release profile of the drug can be manipulated by (1) altering size or shape (i.e., surface area) and solubility of the inert substrate; (2) the ratio of drug to polymer, the polymer composition and solubility, the porosity of the polymer; (3) the drug form (i.e., free base or salt, or which salt); and the thickness and/or surface area of the drug/polymer and/or enteric coating. In a preferred embodiment, the composition is administered orally. This may also be packaged to provide for an escalating or tapering dosage.

The present invention relates to a delayed release drug delivery system containing omeprazole capable of site-specific delivery and pulsatile (bolus) kinetics for once-a-day dosage comprised of an alkaline core structure sequentially layered with suspensions of omeprazole; a separation barrier; and an enteric barrier. The separation barrier is coated with a pH-dependent enteric membrane, which is relatively insoluble in gastric fluid but rapidly to immediately soluble in intestinal fluid, whereby the drug is released in a pulsatile manner in the proximal segment of the gastrointestinal tract.

The invention discloses an enteric soluble hollow capsule and a preparation method thereof. The outer surface of a capsule body of the hollow capsule is covered with an enteric coating; the capsule body consists of hydroxypropyl methylcellulose, gel and water; the enteric coating consists of low-acyl gellan gum, a curing agent and water; the hollow capsules comprise the following components in percentage by weight: 70-80% of hydroxypropyl methylcellulose, 2-5% of gel, 10.5-14% of low-acyl gellan gum, 0.05-2% of a curing agent and the balance of water. The enteric soluble hollow capsule has the characteristics of being stably maintained and not disintegrated within 2 hours or even longer in simulated gastric fluid, and disintegrated within 1 hour in simulated intestinal fluid, and provisions of Chinese Pharmacopoeia on enteric soluble hollow capsules can be met; the enteric soluble hollow capsule is prepared by using a process of two times of gum dipping, one time of calcification and 1 time of drying molding, the preparation method is simple and easy to operate, and particularly no organic solvent or preservative is used in the preparation process, so that the enteric soluble hollow capsule is safe and reliable and environment-friendly, and current hollow capsule development tendency is met.

The invention discloses a device for simulation of digestion in small intestine and a use method thereof. The device comprises a small intestine reactor, a stirrer, a water-bath control device, a computer monitoring system and a small intestine evacuation pump. A small intestinal fluid is added into the small intestine reactor, a solution or a dispersion liquid to be detected is added into the small intestine reactor, a simulator simulates small intestine peristalsis, the water-bath control device controls a temperature in the small intestine reactor, the computer monitoring system monitors an internal temperature, a pH value and digestion time of the small intestine reactor, the small intestine evacuation pump simulates small intestine evacuation, the digested product is collected, pancreatin and trypsin activity is eliminated, the digestion simulation process is repeated three times, and a digestion case of the material to be detected is detected. The device realizes first simulation of specific and detailed digestion in small intestine, realizes observation of digestion of various active materials or nutrients in the human small intestine, carries out simulation in a simulation environment designed according to a human physiological environment, has high conformity to the small intestine digestion and has high accuracy in simulation environment control.

The invention discloses a preparation method of a duck simulated intestinal fluid. The method comprises the following steps of: putting collected duck intestinal chyme in a reagent bottle to shake uniformly, putting in a centrifuge bottle to perform centrifuging treatment, and collecting a supernatant fluid; filtering the supernatant fluid, freezing and concentrating into a mixed concentrated liquid; after dialyzing the mixed concentrated liquid and removing impurities, freezing and drying into lyophiled powder; measuring the activities of alpha-amylase, lipase, trypsin and chymotrypsin in the lyophiled powder, and measuring the activities of corresponding digestive enzymes in the reagent level alpha-amylase, lipase, trypsin and chymotrypsin; and according to the principal that the gross activities of various digestive enzymes in the duck simulated intestinal fluid and the targeted duck intestinal fluid are equal, adding corresponding capacity reagent level alpha-amylase, corresponding weight reagent level lipase, corresponding weight reagent level trypsin, corresponding weight reagent level chymotrypsin and a corresponding capacity water solution in the lyophiled powder with a set weight. The method can be carried out in a low-cost way, and can also be used for preparing the duck simulated intestinal fluid basically homologous with four digestive enzymes in a real duck body.

The invention discloses an artificially simulated pig stomach and intestine digestive fluid, a preparation method and application of the digestive fluid. The preparation method comprises the following steps: mixing pig compound feed and artificial gastric fluid according to a ratio of 1g to (3-3.5mL), adjusting the pH to be 1.5-2.0, oscillating at 39+/-1 DEG C for 1-2 hours, cooling to 4+/-1 DEG C, centrifuging 8000-9000g at 4+/-1 DEG C for 5-10 minutes, and taking liquid supernatant as the artificially simulated pig stomach digestive fluid; and adding artificial intestinal fluid which is 3 times of the volume of a sediment obtained by centrifuging, adjusting the pH to be 6.8+/-0.2, oscillating at 39+/-1 DEG C for 1-2 hours, cooling to 4+/-1 DEG C, centrifuging 18000-20000g at 4+/-1 DEG C for 5-10 minutes, and taking liquid supernatant as the artificially simulated pig intestine digestive fluid. According to the artificially simulated pig stomach and intestine digestive fluid, the conditions such as the pH value and the temperature are consistent with the condition of a pig gastrointestinal tract; by virtue of digestion of special feed, the soluble components in the feed are introduced and are relatively consistent with the component of the pig digestive fluid, in the actual production; the scientific, objective and accurate in-vitro evaluation is carried out on adsorption rate of a mycotoxin absorbent in the pig; the method is simple and quick.

The invention provides a production method of an insulin oral sustained-release preparation and belongs to the technical field of biological medicines. According to the production method, pegylated chitosan (PEG-CS) is taken as an encapsulating material and insulin-loaded pegylated chitosan microspheres are prepared by use of an ionic gel method; in other words, firstly, the PEG-CS solution of a certain concentration is mixed with an insulin solution, low-concentration sodium tripolyphosphate (TPP) of a low concentration is added dropwise under magnetic stirring, the pH is regulated to 5.5 by use of hydrochloric acid, after the reaction is completed, the suspension is centrifuged and then the microspheres are just collected. The production method is simple and mild in conditions; the obtained microspheres are good in biocompatibility, can be stably released in a simulated intestinal fluid for 7 days, and have a sustained-release function; besides, the biological activity of the medicine can be guaranteed, and the oral medication of the insulin is expected to be realized.

The present invention relates to methods for treating or preventing intestinal fluid balance disorders and modulating intestinal fluid secretion and absorption using calcimimetics and calcilytics.

The present invention provides an intestinal tract targeting and pH-sensitive complex coacervation microcapsule transmission system and a preparation method and an application thereof. Carboxymethyl chitosan and arabic gum are polycations and polyanions to constitute a complex coacervationsystem. By adjusting pH value, the carboxymethyl chitosan and the arabic gum are subjected to complex coacervation reaction, and the complex coacervation phase is collected by centrifugation, crosslinked by genipin, and freeze-dried to obtain the intestinal tract targeting and pH-sensitive complex coacervation microcapsule transmission system. The intestinal tract targeting and pH-sensitive complex coacervation microcapsule transmission system can be used either for embedding water-soluble functional components, but also for embedding fat-soluble functional components, can protect core materials against damage caused by strongly acidic gastric environment, safely delivery the core materials to the intestinal tracts to conduct targeted releases, and expand the practical application field of the complex coacervation microencapsulation technology. The intestinal tract targeting and pH-sensitive complex coacervation microcapsule transmission system does not dissociate in a simulated gastric fluid and swells in a simulated intestinal fluid, and has a strong stability, and the process is simple, safe, efficient, and easy for mass production.

The invention discloses a double-balloon intestine fistulization catheter for preventing anastomotic fistula after a colorectal surgery. The double-balloon intestine fistulization catheter comprises a catheter body, a first balloon, a second balloon, a threaded compressed tablet, a first water injection opening and a second water injection opening, wherein the first balloon and the second balloon are two hollow balloons which sleeve the catheter body and are made of an elastic material; the first balloon is close to the head end; the threaded compressed tablet sleeves the part between the second balloon and the tail end; a side hole is formed in the wall, between the first balloon and the head end, of the catheter body; the first water injection opening and the second water injection opening are positioned at the tail end of the catheter body, and are respectively communicated with the first balloon and the second balloon. According to the invention, when the catheter is inserted into the intestinal tract after an intestinal surgery, the circulation of the small intestine is blocked after the first balloon is injected with water to enable intestinal fluid to be led out of the body through the head end and side hole of the catheter; after being injected with water, the second balloon and the threaded compressed tablet positioned outside the body are coordinated to fix the catheter to prevent slipping or shifting of the catheter, and at the same time, the intestinal wall of the cecum is clung to and adhered with the abdominal wall to prevent intestinal fluid from leaking outwards to the abdominal cavity.

The invention discloses a mesalazine enteric-coated sustained release tablet. The mesalazine enteric-coated sustained release tablet is characterized by consisting of the following components in a unit dose: 1.2g of mesalazine, 0.1-0.3g of a sustained release material, 0.004.0.03g of a lubricant and 0.02-0.1g of enteric-coated powder. The release of the mesalazine enteric-coated sustained release tablet in one hour in simulated intestinal fluid of which the pH value is 7.2 is less than 30%, the release in four hours is not more than 70%, and the release in eight hours exceeds 80%.

An immunogenic complex, essentially consisting of neisserial outer membrane protein proteosomes hydrophobically complexed to native purified bacterial lipopolysaccaride and formulated in accordance with the current invention for mucosal delivery such as via the oral or intranasal route is used as a vaccine. Specifically, a vaccine using shigella lipopolysaccharides complexed to proteosomes for such mucosal administration induces IgG and IgA antibodies in sera and in respiratory and intestinal fluids. Furthermore, such antibodies are associated with protection against shigella infection and these vaccines are herein demonstrated to protect against mucosal infection with shigella.

An immunogenic complex, essentially consisting of neisserial outer membrane protein proteosomes hydrophobically complexed to native purified bacterial lipopolysaccharide and formulated in accordance with the current invention for mucosal delivery such as via the oral or intranasal route is used as a vaccine. Specifically, a vaccine using shigella lipopolysaccharides complexed to proteosomes for such mucosal administration induces IgG and IgA antibodies in sera and in respiratory and intestinal fluids. Furthermore, such antibodies are associated with protection against shigella infection and these vaccines are herein demonstrated to protect against mucosal infection with shigella.

The invention provides bifidobacterium lactis (Bifidobacterium lactis) capable of preventing osteoporosis and an application of the bifidobacterium lactis capable of preventing osteoporosis, and belongs to the technical field of microorganisms. The bifidobacterium lactis provided by the invention has properties of being resistant to gastric acid and intestinal juice, when the bifidobacterium lactis is treated for 30min in gastric acid liquid having pH being 2.5, the survival rate of viable bacteria is 62% or above, when the bifidobacterium lactis is treated for 2 hours, the survival rate of the viable bacteria is 61% or above, and when the bifidobacterium lactis is treated for 2 hours in small intestine liquid having pH being 6.8, the survival rate of the viable bacteria is 70% or above. The bifidobacterium lactis can significantly reduce loss of bone mass caused by lack of estrogen, promote blood calcium and blood phosphorus, restrain the number of in vivo osteoclasts, restrain the absorption effects of the in vivo osteoclasts on bones, and increase the level of protein through promoting the expression protein of bone synthesis and metabolism correlation factor genes so as to promote formation of new bones. The strain disclosed by the invention can be used for preparing foods and the like capable of preventing osteoporosis, and has great application prospects.

The invention provides an enteric algal polysaccharide vacant capsule and a preparation method thereof. The enteric algal polysaccharide vacant capsule is prepared from the following raw materials: sodium alginate, hydroxymethyl starch, a plasticizer, a colorant and titanium dioxide. Meanwhile, the invention also discloses a preparation method of the enteric algal polysaccharide vacant capsule. The enteric algal polysaccharide vacant capsule disclosed by the invention has the benefits of reasonable matching, and simple and feasible preparation method; a main material of a finished capsule produced by the invention is sodium alginate; in a simulated gastric environment, sodium alginate easily forms hydrophilic colloid which is not easily digested, has high tolerance of acid, and changes thedisintegrating property of the capsule, so that the capsule can be kept in the stomach for 2 hours without disintegration, the drug release speed is effectively controlled, and the irritation of a drug to the stomach is reduced; however, the capsule can be all disintegrated in the simulated intestinal fluid environment within 1 hour, which shows that the capsule can be used for efficacy release of specific drugs in the intestine and has a good application prospect in the drug release aspect.

The invention belongs to the field of pharmaceutical technologies, and particularly relates to an in-situ preparation method for a starch-ibuprofen clathrate compound of a V-type crystal structure. The method includes the steps that with potato starch as the raw material, ibuprofen is dissolved in a diluted ethanol solution, a certain amount of potato starch is added, an NaOH solution is slowly added, mixing and sufficient constant-temperature stirring are performed, and the mixed solution is kept reacting for certain time; then, the mixed solution is titrated through a hydrochloric acid ethanol solution to have the pH of 7.0 and slowly stirred for certain time, and extraction, washing, drying and smashing are performed to obtain the starch-ibuprofen clathrate compound. The starch-ibuprofen clathrate compound is structurally characterized by being of the V-type crystal structure, the preparation process is simple, and cost is low. The accumulative release rate of the starch-ibuprofen clathrate compound in simulated gastric fluid (pH 1.2) is smaller than 7%, and an active compound is slowly released in simulated intestinal fluid (pH 7.4) under the action of enzyme to take effect, so that drug bioavailability is improved, and the side effect of stimulating the gastrointestinal tract is avoided.