36results about How to "Good correlation between in vitro and in vivo" patented technology

The invention provides double-layer osmotic pump tablets of tamsulosin ehydrochloride and a process for preparation. The medicament contains tamsulosin ehydrochloride and acceptable medical polymeric excipient, and is characterized in that the invention has excellent zero-level controlled releasing, pH level of environment, movements of the stomach and intestine, and food, has little effect on releasing action and food, and has no effect on the internal pharmacokinetics parameter. According to the percentage by weight, the preparation contains tamsulosin ehydrochloride 0-2%, excipient in pastille layer with the function of controlled-releasing 30-70% excipient in boosting layer with the function of controlled releasing 30-70%, and the rest percentage of other excipient. The of process for preparation the double layer permeable pump controlled-release tablets of tamsulosin ehydrochloride comprises (1) the preparation of pastille layer, (2) the preparation of boosting layer, (3) the compressing of the two layers, (4) the coating of the double layer tablets, (5) the perforating of the coated tablets, (6) the packing of moisture proof cost. The invention is clinically used for the treatment of paruria symptom like frequent micturition, diuresis at night, dysuria caused by prostatic hyperplasia.

The invention provides a ginkgolide osmotic pump tablet and a preparation method thereof. The ginkgolide osmotic pump tablet provided by the invention is a double-layer tablet composed of a drug-containing layer and a push layer, and is coated, wherein the drug-containing layer comprises drug release holes. The ginkgolide osmotic pump tablet uses ginkgolide at effective positions of the ginkgo biloba extract as an active component, and a total amount of ginkgolide A, ginkgolide B, ginkgolide Cand bilobalide is not less than 70 %. According to the invention, by combining a solid dispersion solubilising technique and an osmotic pump tablets control-release technology, the ginkgolide is firstly prepared into the solid dispersion, and then further prepared into the ginkgolide osmotic pump tablet on a basis of improving solubility of poorly soluble components, thereby realizing synchronous slow release of complex components in the ginkgolide, reducing drug administration times and improving patient compliance.

The invention belongs to the technical field of pharmaceutical preparations and discloses a paliperidone bi-layer osmotic pump progressively-increased controlled release tablet and a preparation method thereof. The osmotic pump preparation comprises a tablet core and a semipermeable coating film, wherein the tablet core comprises a medicine containing layer and a boosting layer, the semipermeable coating film envelops the tablet core and is provided with medicine release holes, the medicine containing layer contains middle molecular polyoxyethylene (average molecular weight is 900, 000-1, 000,,000) and an osmotic active substance in a certain proportion so that the hydration rate of the medicine containing layer is proper, the release of the active medicine basically presents a progressively-increased release trend and the progressively-increased release can be kept for 14-24 hours by using the bi-layer tablet core and the single-layer coating. By adopting the preparation, the adverse reaction of the medicine can be reduced greatly, the compliance of a patient can be improved, simultaneously, the preparation is simple to prepare, the preparation process of the progressively-increased osmotic pump preparation is simplified greatly, and the preparation is more conductive to industrialized production.

The invention belongs to medical technique field, and relates to osmotic pump controlled-release tablets of alfuzosin hydrochloride and the preparation method, which comprises tablet core, clothing sheet membrane and controlled-release pore. The solid medicine and osmotic active substance and shaping agent forms the tablet core; the coating membrane is insoluble controlled-release clothing sheet that is water permeable but not medical permeable. Said pore is on the clothing sheeting membrane. The comprised raw material of tablet core and clothing sheet membrane and proportion by weight are as follows: table core: alfuzosin hydrochloride 0.5-50%, packing agent 5-80%, penetration -promoting agent 5-80%, lubricating agent 0.2-3%, adhesive agent 0.01-10%; clothing sheet membrane: semi-permeable membrane clothing sheet high polymer material 70-99%, plasticizing agent 1-30%. The invention is characterized by stable and continuous release, long retention time for effective blood concentration and reduced peak-to-valley of blood concentration phenomena.

The invention provides a phencynonate hydrochloride double-layer osmotic pump controlled release tablet and a preparation method thereof. The tablet comprises, from interior to exterior, a double-layer tablet core prepared through compaction of a drug-containing layer and a boosting layer, a semipermeable coating film with drug releasing holes and a moistureproof coating film, wherein the drug-containing layer contains an effective amount of phencynonate hydrochloride, a suspending aid, an osmotic pressure promoter and other pharmaceutic adjuvants, the boosting layer contains a propellant, an osmotic pressure promoter, a sustained releasing agent and other pharmaceutic adjuvants, and the semipermeable coating film is perforated with more than one drug releasing hole in one side close to the drug-containing layer. According to the invention, the phencynonate hydrochloride double-layer osmotic pump controlled release tablet has a substantial zero order drug release characteristic and enables drugs to enter into a human body at a constant speed; drug release behavior is not affected by gastrointestinal peristalses, pH values, food effects and the like, individual difference of the drug release behavior is small, and blood concentration is steady; the tablet has long-lasting drug effects, is taken once per day, has little toxic and side effects and good compliance in administration and can be used for preventing or treating motion sickness syndrome, Parkinson' disease, Parkinson' disease syndrome, acute attack of vertigo and epilepsy.

The invention discloses simvastatin monolayer osmotic pump sustained release tablets. Each simvastatin monolayer osmotic pump sustained release tablet comprises a tablet core and a controlled-release film coated layer, wherein the tablet core contains the following components in percentage by weight: 1 to 20 percent of simvastatin serving as a main medicine, 1 to 25 percent of filling agent, 50 to 90 percent of penetrating agent, 1 to 15 percent of adhesive, 0.5 to 5 percent of release conditioning agent and 0.5 to 3 percent of lubricating agent; the controlled-release film coated layer comprises a controlled-release film-forming material, a plasticizer and/or a pore-forming agent; the filling agent comprises microcrystalline cellulose and dextrin; and the penetrating agent contains cane sugar and lactose.

The invention provides a nifedipine controlled release capsule and a preparation method thereof. The controlled release capsule is prepared by filling a capsule shell with nifedipine, polyoxyethyleneand organic acid and coating the capsule shell. The mass ratio of nifedipine, polyoxyethylene and organic acid is (10-90):(1-15):(1-30); the coating is prepared from cellulose, a plasticizer and a pore-forming agent by mixing in a weight ratio of (10-50):(0-15):(1-25). Double-layer tabletting, laser or mechanical punching are not required, the preparation process is simple, the cost is low, the drug release rate is stable, zero-order release is basically achieved within 24 hours, and drug release is complete; the capsule is administered once a day, and thus, patient compliance is improved.

The invention discloses an indapamide monolayer osmotic pump sustained-release tablet, which comprises a tablet core and a controlled-release film coating layer, wherein the tablet core contains 0.5-2% of indapamide as a monarch drug, 1-20% of filling agent, 50-90% of penetration enhancer, 1-15% of adhesive, 1-20% of release regulator and 0.5-3% of lubricant; the controlled-release film coating layer comprises a controlled-release film forming material, a plasticizer and/or a pore-forming agent; and the filling agent comprises agar powder.

A tablet of the dispersed hydroxy camptothecine solid released under the control of osmotic pump is composed of a tablet core containing dispersed hydroxy camptothecine solid, release controlling auxiliaries, and carrier and a perforated coated layer. Its preparing process includes preparing tablet core, coating and perforating.

The invention belongs to the field of medicinal preparation and specifically provides a posaconazole double-layer osmotic pump controlled release tablet and a preparation method thereof. The tablet comprises a tablet core and a semipermeable controlled release film. The tablet core comprises a drug containing layer and a boosting layer. The drug containing layer is located inside the controlled release film which is provided with a drug releasing hole. The boosting layer is located inside the controlled release film at a place far away from the drug releasing hole. One end of the water-permeable controlled release film is provided with one or more drug releasing holes. The release curve of the preparation drug shows a zero-order release pattern, and thus the problem of drug resistance caused by long-term use of posaconazole dosage forms on the market is solved. Besides, the problems that the preparation technology is complex, the preparation cost is high, and the drug is unsuitable for industrialized mass production due to the adoption of a hot-melt extrusion technology are solved. Simultaneously, the in vivo-in vitro correlation of the drug is better ensured and the clinical monitoring of plasma concentration is better facilitated.

The invention discloses a single-chamber osmotic pump controlled release tablet containing pregabalin. The tablet comprises a single-layer piece core, a controlled release film coating layer and at least one laser hole in a controlled release film. The basic composition of the piece core includes pregabalin or salt or hydrate thereof, diluent, adhesive and lubricant, and does not include an expansible polymer. The adopted accessories are simple and economical, the tablet can be prepared through a simple direct tabletting process, and the controlled release film coating layer includes a film forming material, a pore-foaming agent and plasticizer. According to the drug release mechanism, water and a physiological medium dissolve water-soluble active components and the diluent in the piece core through the controlled release film to form trans-film osmotic pressure, the dissolved active components are released out of the piece core through the small holes in the controlled release film, the controlled release tablet can release a therapeutic drug within a certain time range at a constant drug release rate, and the influence of the stomach and intestine difference between different individuals on drug absorption can be minimized.

The invention belongs to the technical field of medicines, and particularly relates to a nifedipine microporous osmotic pump core-encapsulating tablet with an expanding tablet core and a preparation method thereof. The expanding tablet core is contained in the microporous osmotic pump core-encapsulating tablet, a nifedipine medicine-containing layer and a semipermeable membrane are sequentially arranged on the surface of the expanding tablet core, and the weight proportion of all the components is: expanding tablet core:nifedipine medicine-containing layer:semipermeable membrane=(5-55):(5-75):(5-30). The nifedipine microporous osmotic pump core-encapsulating tablet containing the expanding tablet core which is prepared by adopting the invention is almost equivalent to a medicine released at a zero-order release rate, moreover, perforation is not required, and the production process is mature, and can be industrially scaled up.

The invention provides a metoprolol pulse osmotic pump controlled release tablet and a preparation method thereof. The controlled release tablet comprises a tablet core, a time lag coating layer and a controlled release coating layer with a release orifice from inside to outside, wherein the tablet core consists of a drug containing layer and a boosting layer, based on the gross weight of the drug containing layer, the drug containing layer comprises 5-65 wt% of metoprolol as active material and 35-95 wt% of pharmaceutically acceptable carrier; based on the gross weight of the boosting layer, the boosting layer comprises 30-85 wt% of swelling agent and 15-70 wt% of osmotic pressure promoting agent; the weight gain of the time lag coating layer is 5-50 wt% of the tablet core; and the weight gain of the controlled release coating layer is 3-30 wt% of the tablet core. The metoprolol pulse osmotic pump controlled release tablet has three-stage release behavior, and is characterized in that the tablet has 2-5 hours time lag at the initial period after being taken orally, increased release is showed at the intermediate period, and release at constant speed is showed at the later period.

The invention discloses a quality evaluation and control method of florfenicol sustained-release granules, which comprises the following steps of: obtaining in-vitro disintegration and release processes of florfenicol sustained-release granule medicines through a dissolution test, and establishing correlation with the in-vivo process of the medicines, so that the in-vitro dissolution limit of the medicines is formulated as follows: in simulated gastric juice, the in-vitro disintegration and release processes of the florfenicol sustained-release granules are subjected to the in-vitro disintegration and release processes of the florfenicol sustained-release granules; the cumulative release rate within 30 minutes does not exceed 20%, and the cumulative release rate within 2 hours does not exceed 50%; and in simulated intestinal juice, the cumulative release rate within 30 minutes does not exceed 25%, the cumulative release rate within 4 hours does not exceed 75%, and the cumulative release rate within 8 hours is greater than 85%. By taking the dissolution limit of the florfenicol sustained-release product as a quality standard and evaluating the in-vitro dissolution of the florfenicol sustained-release product, the product quality of preparation production is controlled, the consistency of in-vivo metabolic processes of products of different production batches is ensured, and a basis is provided for product quality control and evaluation.

The invention belongs to the technical field of medicines and in particular discloses a nifedipine micro-porous osmotic pump particle taking polyoxyethylene-containing particles as an expanded pill core and a preparation method thereof. The micro-porous osmotic pump particle takes the polyoxyethylene particles as the expanded pill core. The nifedipine micro-porous osmotic pump particle prepared bythe invention is capable of releasing drugs at a nearly zero release rate and is simple in production process and capable of easily realizing industrialized enlargement.