20 results about "Drug release rate" patented technology

The present invention relates to a prodrug and drug having a controllable drug release rate. Specifically provided are a prodrug or a stereoisomer, deuterated substance, solvate, polymorph or pharmaceutically acceptable salt thereof. The prodrug contains a drug and a linker, wherein the drug is linked to the linker, and the linker contains a structure as represented by formula (1). The prodrug has a long half-life, does not require an enzymatic or redox environment, can controllably and spontaneously release the drug under physiological conditions, and exhibits a high drug delivery efficiency. The released drug exhibits a complete activity and is not affected by the linker or a macromolecular carrier.

This invention relates to the field of biomedical technology, specifically disclosing an anti-inflammatory and bone-promoting rhodioloside composite hydrogel and its preparation method. The thermosensitive carrier is a triple-response system, which enhances the drug release rate only in a specific microenvironment at 37°C, with a pH of 5.5-6.5 at the site of inflammation, and in which MMPs are overexpressed. MMPs are highly expressed at the implant periodontitis site, and MMP-sensitive peptides can be specifically degraded by this enzyme. This process can trigger the precise release of rhodioloside and quercetin active ingredients in the gel, avoiding systemic drug diffusion that could lead to drug waste or side effects at other sites. Rhodioloside and quercetin synergistically downregulate the expression levels of inflammatory factors such as IL-6 and TNF-α, while nisin and chitosan-ε-polylysine grafts inhibit the growth of Porphyromonas gingivalis. Runx2 / CON expression is increased, achieving a closed-loop treatment of anti-inflammatory, antibacterial, and bone-promoting effects.

This invention relates to a choleretic traditional Chinese medicine composition, its preparation method, and its application, belonging to the field of traditional Chinese medicine preparation technology. The microcapsules prepared from this choleretic traditional Chinese medicine composition consist of a core and a coating. The core contains a traditional Chinese medicine extract, pregelatinized starch, sodium alginate, and croscarmellose sodium. The coating contains hydroxypropyl cellulose and hydroxypropyl methylcellulose E5, PEG4000, and talc. The traditional Chinese medicine extract is made from Artemisia capillaris, Lysimachia christinae, Rheum palmatum, Scutellaria baicalensis, Taraxacum mongolicum, Forsythia suspensa, Curcuma longa, Curcuma longa, Bupleurum chinense, Citrus aurantium, and Aucklandia lappa. This choleretic traditional Chinese medicine composition has the effects of promoting bile flow and expelling gallstones, detoxifying and reducing swelling, with a stable drug release rate, definite efficacy, and few toxic side effects. It can be used for the prevention and / or treatment of acute and chronic gallstones and / or cholecystitis.

The application discloses a traditional Chinese medicine plaster for lumbar disc herniation and a preparation method thereof, and relates to the technical field of biological medicine. In the microneedle layer, macromolecular antler active components are loaded, and a liposome transition depot layer and an enzyme-responsive hydrogel controlled-release layer are constructed on the surface of the microneedle layer. Through the system integration of the three-layer structure, a complete treatment chain of puncture, transdermal penetration, transition depot, intelligent response and controlled release is constructed. The microneedle layer breaks through the physical barrier of the stratum corneum, directly delivers the antler active components and analgesic anti-inflammatory components to the dermis layer, and realizes rapid effect. The liposome transition depot layer provides secondary release and protection, maintains the drug concentration platform, and realizes continuous supply. The enzyme-responsive hydrogel controlled-release layer intelligently adjusts the drug release rate according to the pathological state of the lesion, and realizes on-demand drug release. The antler active components promote the repair of nucleus pulposus cells and nerve regeneration, and the CeO2@PDA nanoenzyme removes ROS to improve the microenvironment, realizing the treatment of both the symptoms and the root cause.

This invention relates to a drug delivery method for a membrane-covered stent, comprising the following steps: 1) preparing a coating solution and atomizing it; 2) applying a drug coating to the stent and drying it; 3) covering the stent surface with a thin film; 4) preparing a coating solution, atomizing the membrane-covered stent, and applying the coating solution to the surface of the membrane-covered stent; 5) atomizing the membrane-covered stent with a solvent and drying it. The beneficial effects of this invention are that the design of the inner and outer drug coatings on the stent and the membrane surface can flexibly achieve multifunctional composite effects according to different drug delivery purposes, drug delivery sites, and drug delivery methods, and the inner and outer drug coatings do not affect each other, with controllable drug release rates, achieving the purpose of preventing restenosis and reducing thrombus formation.

This invention belongs to the field of traditional Chinese medicine technology and discloses a high-release drug drop pill and its preparation method. In addition to the main drug extract as the core component for efficacy, the high-release drug drop pill contains a water-soluble matrix as the main framework and solid dispersion carrier, a rapid-disintegrating pore-forming agent to accelerate water penetration, sucrose fatty acid esters as surfactants, alkyl glycosides as penetration enhancers, poloxamer as crystal inhibitors, and phospholipid dispersants to accelerate transmembrane transport. These components work synergistically to improve the high-release properties of the drop pill. The multi-component surfactants synergistically form mixed micelles or lipid microparticles, encapsulating the hydrophobic drug within them to form a thermodynamically stable dispersion system, constructing a solid dispersion and achieving amorphous dispersion of drug molecules. The rapid-disintegrating pore-forming agent achieves overall disintegration, avoiding gelation blockage and increasing the contact area between the drug and the dissolution medium, thereby improving the drug release rate.

This invention discloses a sustained-release granule of traditional Chinese medicine and its preparation method, relating to the field of traditional Chinese medicine preparation technology. It is prepared from the following materials in parts: 100-600 parts of active extract of traditional Chinese medicine, 50-450 parts of beeswax, 20-400 parts of aralia elata gelatin, 22-400 parts of modified gelatin, 15-50 parts of polyphosphate ester, 20-220 parts of sepiolite, 10-120 parts of ethyl cellulose aqueous dispersion and 5-30 parts of calcium phosphate salt. This invention uses beeswax as a hydrophobic sustained-release barrier, which can effectively inhibit the rapid dissolution of drugs in the early stage, avoiding gastrointestinal irritation and drug efficacy fluctuations caused by a sudden increase in blood drug concentration after administration. Combined with a hydrophilic gel skeleton composed of aralia elata and modified gelatin, it slowly swells and erodes upon contact with gastrointestinal fluid, achieving a stable release of drugs in the early and middle stages. At the same time, ethyl cellulose aqueous dispersion forms a dense hydrophobic coating film, which precisely controls the drug release rate in the later stage. The multiple sustained-release mechanisms work together to overcome the poor adaptability of traditional systems and effectively avoid the problems of sudden release, delayed release, and incomplete drug release.

This invention discloses a miR-141 / near-infrared light dual-response synergistic drug delivery system, relating to the fields of biomedicine and nanomedicine. The system uses DNA-modified gold nanocages as carriers, loading doxorubicin (a chemotherapy drug) and methylene blue (a photosensitizer). H-type DNA nanolocks formed by thiol-modified A and B chains achieve specific recognition of miR-141 and dual response to near-infrared light. miR-141 binding triggers initial unwinding of the nanolocks, followed by complete unwinding and drug release via 808nm near-infrared light irradiation (photothermal effect). A 650nm laser excites methylene blue to generate reactive oxygen species, simultaneously completing quantitative detection of miR-141 (fluorescence / SERS signal complementarity) and synergistic treatment in three modes: chemotherapy + photothermal + photodynamic therapy. In vitro experiments show a miR-141 detection sensitivity of 5.0 × 10⁻⁶. ‑12 M, with a dual-response drug release rate exceeding 60%; in vivo experiments have demonstrated a tumor inhibition rate exceeding 70% and good biocompatibility. This system solves the problems of single-response and separation of diagnosis and treatment in existing delivery systems, and is suitable for precision treatment of miR-141 positive solid tumors such as MCF-7.

The present application belongs to the technical field of biological medicine, and particularly relates to a composition for promoting synthesis of an OAHFA derivative family, a microneedle patch and application thereof in preventing and treating dry eye syndrome. The present application first selects an OAHFA derivative as a dry eye treatment target and relies on activation of a PPARγ signal pathway to exert drug efficacy. The composition is compounded from 0.2% to 0.5% PPARγ agonists, 2.0% to 4.0% super-long chain fatty acids and 0.3% to 0.8% ceramides, three effective components. The super-long chain fatty acids supply synthesis substrates, and the ceramides stabilize the interface. The three components synergistically improve the curative effect. The composition described in the present application adopts soluble microneedles for local administration, and the drug release rate is not less than 70% in 30 min. The effect is rapid and the puncture is painless, and the patient compliance is excellent. Local administration eliminates systemic exposure of the drug, and the drug safety is high, and there is no serious adverse reaction.

This invention provides a process for preparing ileal-targeted empty capsules, relating to the field of pharmaceutical excipients technology. The process includes the following steps: preparing the following raw materials: gelatin, titanium dioxide, and sodium stearate; dissolving the gelatin in water at 60-70°C, heating and stirring, adding titanium dioxide and sodium stearate, mixing well, and allowing to stand to obtain a film-forming gel. This invention utilizes a preparation mechanism involving the mixing of water-soluble polyacrylic acid resin IV, polyacrylic acid resin III, and polyvinyl alcohol, with the remaining materials added in steps, to achieve the predetermined goal of ileal disintegration. Furthermore, based on the synergistic effect of polyacrylic acid resin III with water-soluble polyacrylic acid resin IV and polyvinyl alcohol, the drug release rate of the empty capsule is improved, allowing the drug to rapidly reach an effective concentration in the ileum and exert its therapeutic effect more effectively.

This invention relates to the field of pharmaceutical technology, specifically disclosing a method for preparing and applying acid-sensitive environment-responsive PEGylated self-assembled micelles. The key technical points are as follows: the micelles are formed by the self-assembly of a 0831A-Hyd-mPEG conjugate in an aqueous solution. This conjugate is prepared through the following steps: first, monomethoxy polyethylene glycol (mPEG) is reacted with p-aldehyde benzoic acid to generate mPEG-CHO, which is then linked to 0831A (SKLB060-methionine) via an acylhydrazone bond; wherein the number-average molecular weight of mPEG is 2000; the average particle size of the micelles is approximately 157 nm, exhibiting significant pH-responsive drug release characteristics, with a cumulative drug release rate of 69.46±2.13% after 48 hours at pH 5.0, compared to only 22.94±0.67% at pH 7.4. The micelle structure of the present invention is well-defined and easy to prepare. It can effectively prolong the in vivo circulation time of the drug and significantly reduce its systemic toxicity while retaining the antitumor activity of 0831A. It is particularly suitable for preparing drugs for treating malignant tumors such as colorectal cancer.

This invention discloses a testing device and evaluation method for balloon coating adhesion and in vitro drug release rate, belonging to the technical field of vascular interventional device evaluation. It includes an in vitro release performance testing device; the in vitro release performance testing device comprises: a media liquid constant temperature circulation device, a pulse generator, a flow control unit, a testing operation platform, and an defoaming and particle capture unit connected in sequence. Based on the special circumstances of testing under simulated human body flow conditions, this invention uses a gas-driven diaphragm pulse generator and an electro-proportional valve to adjust and achieve a pulse flow environment under physical conditions.

This invention relates to the field of chemical pharmaceutical formulation manufacturing technology, and discloses a shikonin composition for inhibiting non-specific inflammation of the reproductive system, comprising: nanomicelles formed by encapsulating shikonin with tocopherol polyethylene glycol 1000 succinate, phenylboronic acid-modified sodium hyaluronate, and a lactic acid buffer system. The phenylboronic acid-modified sodium hyaluronate constructs a gel anchoring layer by complexing the phenylboronic acid groups with the ortho-dihydroxy structure on the action surface. This invention utilizes hydrogen peroxide to induce an oxidative deboronization reaction at the inflammatory lesion, causing an in-situ phase transition from a gel state to a sol state in the gel anchoring layer, eliminating drug diffusion resistance, and resolving the mismatch between mucosal clearance and drug release rate. The composition enhances the chemical stability of shikonin while achieving feedback regulation of drug dosage and inflammation degree, effectively repairing the mucosal barrier and maintaining local microecological balance.

In this specification, anew expandable dosage form is presented where the post-expansion mechanical properties and the drug release rate can be independently controlled. The dosage form generally comprises a three-dimensional structural framework of one or more substantially orderly arranged fluid-absorptive elements, a mechanically strengthening semi-permeable layer substantially encapsulating said fluid-absorptive elements, and a drug-containing solid applied outside said encapsulated elements.

In this specification, a new design of an expandable, gastroretentive dosage form is presented where the post-expansion mechanical properties and the drug release rate can be independently controlled. The dosage form generally comprises a drug-laden formulation attached to an expandable, gastroretentive solid.

The application relates to the fields of biological medicine and high polymer materials, and discloses a sustained-release implant type biodegradable stent loaded with an antitumor active component, which is composed of polylactic acid-glycolic acid copolymer, doxorubicin hydrochloride, citric acid-terminated polyethylene glycol polymer, zinc acetate dihydrate and N-acetyl cysteine. The metastable complex structure is constructed by in-situ coordination reaction between the components, so that the rapid release of the water-soluble doxorubicin hydrochloride in the initial implantation stage is blocked. After implantation, N-acetyl cysteine is preferentially dissociated and released, so that the zinc ion coordination unsaturated sites are generated in the coordination network; with the hydrolysis of the polylactic acid-glycolic acid copolymer, the generated lactic acid molecules intervene in the above unsaturated sites to generate a competitive coordination reaction, so that the coordination skeleton is destroyed and the antitumor drug is released. The application realizes the synchronization of the drug release rate and the high polymer matrix degradation rate, and the acetate dissociated from the zinc acetate can effectively buffer the pH value of the degradation microenvironment.

The application provides a composition of rasagiline mesylate, a patch and a preparation method and application thereof. The matrix material of the composition of rasagiline mesylate of the application adopts at least one of DURO-TAK 387-2054 acrylate pressure-sensitive adhesive, DURO-TAK 87-2074 acrylate pressure-sensitive adhesive and MAS acrylate copolymer, compared with conventional acrylate pressure-sensitive adhesive as a matrix, the patch of the application can maintain more stable and continuous drug transdermal flux during use, which is beneficial to realize stable blood drug concentration. The patch of the application of rasagiline mesylate has good drug transdermal flux and drug release rate, and also has good skin compatibility and application experience: the initial adhesion, holding adhesion and peeling strength of the patch to the skin are balanced well, and pain is not easy to be generated and no residue is left during peeling.

This invention discloses a dual-wavelength photoacoustic probe for ultrasound-triggered drug release monitoring and its preparation method, belonging to the field of biomedical imaging and drug delivery technology. It includes a hydrophobic polymer matrix, a drug, and FD-1080 photoacoustic sensing molecules. FD-1080 is in a monomeric state, and the probe generates a photoacoustic response in the 1040–1064 nm wavelength range. After ultrasound triggering, the polymer matrix ruptures, and FD-1080 transforms from a monomeric state to an H-aggregate state. The photoacoustic response of the probe is enhanced in the 750–780 nm wavelength range and weakened in the 1040–1064 nm wavelength range. The drug release rate is characterized by calculating the amplitude ratio of the two photoacoustic signals. This invention integrates ultrasound-controlled release, in-situ implantation delivery, and dual-wavelength ratiometric photoacoustic monitoring into a single system, reducing the influence of probe concentration on release judgment in single-wavelength detection and improving the accuracy of drug release monitoring.

This invention discloses a method for preparing and studying the drug-loading properties of PEGMA-g-PEGMA-b-PCL polymer micelles, belonging to the field of drug carrier technology. The method first synthesizes a triblock graft copolymer using the ATRP method, then completes micelle self-assembly through solution dropwise addition, rotary evaporation, and membrane filtration. Using a hydrophobic antitumor drug as a model, drug-loaded micelles are prepared, and drug loading, release, stability, and cytotoxicity are simultaneously tested. This invention designs a hydrophilic grafted PEGMA-g-PEGMA structure and optimizes the preparation process parameters. The resulting micelles have a spherical core-shell structure with a particle size of 80-180 nm, exhibiting good self-assembly stability and pH response characteristics. The drug loading is ≥8.5%, the encapsulation efficiency is ≥80%, drug release is slow under physiological conditions, and the cumulative drug release rate in the tumor microenvironment is 75%-90% after 72 hours. Furthermore, it exhibits good storage stability and excellent biocompatibility, enabling efficient drug encapsulation and tumor microenvironment-responsive release. This method has significant application value in the preparation of targeted therapeutic carriers for hydrophobic antitumor drugs.

In recently or concurrently filed disclosures, we have presented expandable, gastroretentive dosage forms with independently controllable gastric residence time and drug release rate. In this specification, a method for producing such and similar dosage forms is disclosed. The method comprises preparing a three-dimensional structural framework of one or more fibers, and attaching a controlled amount of drug-containing matter to said three-dimensional fiber structural framework.