A high-efficacy, long-acting formulation of silibinin, comprising silibinin solid dispersion, silibinin-loaded silica nanoparticles, slow-release matrix material and release enhancer, wherein the mass ratio of these components is silibinin solid dispersion:silibinin-loaded silica nanoparticles:slow-release matrix material:release enhancer=1:0.5˜1.25:0.1˜0.3:0.1˜0.3; the drug loading rate of the said silibinin-loaded silica nanoparticles is 51.29˜51.77%; the said silibinin solid dispersion contains povidone K30, soybean lecithin, acrylic resin IV, wherein the mass ratio between silibinin and other medical accessories is silibinin:povidone K30:soybean lecithin:acrylic resin IV=1:1˜3:0.3˜0.8:0.2˜0.5. Compared with the existing formulations, the half life of the high-efficacy, long-acting formulation of silibinin disclosed in this invention is 14.8 times longer while the mean residence time (MRT) of which is 4.52 times longer; when tested in vivo in Beagle dogs, this new formulation of silibinin presents a smoother concentration-time curve and reaches the continuous release for 72 hours. This invention discloses its preparation method.

formulation of silibinin with high efficacy and prolonged action and the preparation method thereof

The invention relates to a novel controlled release pellet preparation and its preparation method, and especially relates to a tamsulosin hydrochloride controlled release pellet preparation and its preparation method. The controlled release pellet adopts a drug-loaded controlled release layer to coat a blank pellet and an enteric coating to coat the drug-loaded controlled release layer in order to control the drug release, the drug release can be realized in an acidic or weakly alkaline environment, and good absorption is realized when the pellet enters a body. The pellet has the advantages of good release degree homogeneity, simple preparation technology and good repeatability. The invention further provides a novel drug controlled release pellet suitable for small-dimension drugs. The novel drug controlled release pellet still well controls the drug release when the drug load amount reduces to 10% or less of a total weight.

Controlled release pellet preparation and its preparation method

The invention relates to a silibinin injection. By combining inherent physicochemical properties of silibinin, composition and dosage of a formula which matches silibinin are selected. That is to say, the formula is composed of silibinin, sulfobutyl ether-beta-cyclodextrin and an organic solvent for injection. If necessary, the formula also can contain a cosolvent, a freeze-drying proppant, a pH regulator, water for injection and the like. The preparation is safe and stable and has high drug loading capacity. Thus, insufficiency of low bioavailability of existing silibinin oral preparations is fundamentally overcome; pharmacologic action of silibinin is expected to be further performed to the maximum; and a foundation is laid for clinical application and research of silibinin.

Silibinin injection and preparation method thereof

The present invention discloses silibinin double-layer slow-release tablets, which comprise an immediate release layer and a slow-release layer, wherein the immediate release layer mainly comprise a silibinin solid dispersion, a filler, a disintegrating agent and a lubricant, the slow-release layer mainly comprises silibinin, a slow-release material, a filler, a lubricant and a binder, a weight ratio of the silibinin content in the immediate release layer to the silibinin content in the slow-release layer is 2:8-3:7, and a weight ratio of the immediate release layer to the slow-release layer is (1.5-2.4):1. A purpose of the present invention is to provide the silibinin double-layer slow-release tablets with characteristics of good patient compliance, low side effect, rapid effect, and lasting maintenance of stable effective blood drug level. The present invention further discloses a preparation method for the silibinin double-layer slow-release tablets. The method of the present invention has characteristics of good reproducibility and high production efficiency, and is suitable for industrial mass production. In addition, the prepared double-layer slow-release tablets have good release uniformity.

Silibinin double-layer slow-release tablets and preparation method thereof

The invention discloses a tamsulosin hydrochloride sustained-release pellet preparation. The tamsulosin hydrochloride sustained-release pellet preparation comprises a tamsulosin hydrochloride sustained-release pellet core, a sustained-release coating layer, and an enteric soluble coating layer; and is a capsule preparation. Three slow release methods including skeleton slow-release, membrane control slow-release, and enteric coating are adopted for preparation of the tamsulosin hydrochloride sustained-release pellet preparation; the obtained tamsulosin hydrochloride sustained-release pellet capsule preparation is capable of controlling releasing from the stomach to the intestine, so that adverse reaction caused by large amount absorption of tamsulosin hydrochloride in a short time is prevented. A preparation method of the tamsulosin hydrochloride sustained-release pellet preparation is simple; and in vivo release of tamsulosin hydrochloride can be controlled stably and effectively.

Tamsulosin hydrochloride sustained-release pellet preparation

The invention discloses tamsulosin hydrochloride sustained-release pellets, which are prepared by coating medicament-containing blank pellets, wherein the blank pellets contain microcrystalline cellulose, soluble starch, lactose and croscarmellose sodium. Two layers of coating liquid are a Surelease sustained-release coating material and an enteric-coating material Kolicoat MAE 30DP respectively and the tamsulosin hydrochloride sustained-release pellets are capsules. The tamsulosin hydrochloride sustained-release pellets of the invention adopt the sustained-release coating material and the enteric-coating material to control the release of medicaments. The prepared tamsulosin hydrochloride sustained-release pellet capsules release less than 40 percent of medicaments in hydrochloric acid solution with a pH value of 1.2 in two hours and release 40 to 70 percent (about 60 percent) of medicaments in phosphate buffer solution with a pH value of 6.8 in three hours and over 70 percent (about 90 percent) of medicaments in five hours, so the prepared tamsulosin hydrochloride sustained-release pellet capsules meet the requirements of quality standards. The invention discloses a preparation method of the tamsulosin hydrochloride sustained-release pellets.

Tamsulosin hydrochloride sustained-release pellets and preparation method thereof

The invention relates to a hollow silica nano sustained-release preparation loaded with capsicine. In the hollow silica nano sustained-release preparation loaded with capsicine, the diameter of hollow silica nanoparticles ranges from 200 nm to 250 nm; and a mass ratio of capsicine to the hollow silica nanoparticles is 1:0.28-1. A preparation technology of the hollow silica nanoparticles is simpler; and the prepared capsicine-hollow silica nanoparticles significantly increase solubility and bioavailability of capsicine. Both in-vitro and in-vivo research results show that the hollow silica nanoparticles loaded with medicines have obvious long-acting sustainable-released characteristics. The invention also discloses a preparation method of the hollow silica nano sustained-release preparation.

Hollow silica nano sustained-release preparation loaded with capsicine, and preparation method thereof

The invention provides a silybin nano medicinal preparation, which comprises liposome nano particles of silybin, the liposome material is the mixture of soya bean lecithin, vitamin E and soyabean oil by the mass ratio of 1:2.5:12.5-1:15:24, the mass ratio of silybin and lipsome material is 1:32-1:400, the grain diameter of the liposome nano particles is less than 500 nanometer. The invention also discloses the preparing process of the preparation.

Nanometer preparation of silybin and preparation method thereof

The present invention relates to a high-effective oral silibinin (SLB) slow-released preparation Its composition includes (by mass component portion) 1 portion of silibinin, 15-25 portions of polyvidone-K30, 023-058 portion of hydroxypropyl methyl cellulose 4000cPaS, 046-138 portions of low-substituted hydroxypropyl cellulose Said invention adopts the combination of solid dispersion technique and slow-released hydrophilic gel skeleton technique to raise the dissolubility of silibinin

High-efficient oral silibinin sustained-release preparation and preparation method thereof

Disclosed is a preparation drug of precursor multiphase liposome of water grind processing thistle bingham, which contains the precursor multiphase liposome of the water grind processing thistle bingham. The preparation drug is mainly composed of the following mass abundance components : 1 portion of water grind processing thistle bingham, 2 to 10 portions of phospholipid, 0.1 to 0.6 portion of cholesterol, 1 to 5 portions of isopropyl myristate, 1 to 5 portions of sodium cholate, and 2 to 10 portions of cane sugar powder. Observed by the sem, the appearance of the prepared precursor multiphase liposome powder of the water grind processing thistle bingham is ball-shaped or similar to the shape of the ball; the surface of the prepared precursor multiphase liposome powder of the water grind processing thistle bingham is smooth; the particle size and the distribution of the prepared precursor multiphase liposome powder of the water grind processing thistle bingham are measured by photon correlation spectroscopy, and the average particle size is 106 nm; the redispersion in the water is good; no burst effect occurs; and the storage stability is good. The total entrapment efficiency of the precursor multiphase liposome of the water grind processing thistle bingham is 96 percent, wherein, 85 percent of the water grind processing thistle bingham is entrapped inside the liposome, and a small part is entrapped inside emulsion and micelle. With high entrapment efficiency, good stability, simple operation and low cost, the precursor multiphase liposome of the water grind processing thistle bingham is easy to be filled , does not need special equipment and is convenient for industrial production. The invention discloses the preparation method of the precursor multiphase liposome of the water grind processing thistle bingham.

Silybin precursor multiphase lipidosome pharmaceutics and preparing method thereof

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