81 results about "Letrozole" patented technology

Novel injectable compositions are provided comprising an active agent which is tamsulosin or letrozole or its pharmaceutically acceptable salts, derivatives, isomers, polymorphs, solvates, hydrates, analogues, enantiomers, tautomeric forms or mixtures thereof and one or more pharmaceutically acceptable excipient(s) wherein the compositions are preferably formulated as biodegradable microparticles or nanoparticles which can optionally be reconstituted with an aqueous, hydro-alcoholic or oily liquid vehicle prior to administration. The novel injectable compositions of the present invention preferably form a depot upon administration in vivo and are in the form of an in situ gelling composition or an implant composition which provides a prolonged release of tamsulosin or letrozole for extended periods of time. Also described are process for preparation of such novel compositions and method of using them.

The invention provides a high-yield process for the preparation of letrozole having a high purity, without the need for removal of the 4-[1-(1,3,4-triazolyl)methyl]benzonitrile impurity at the intermediate stage. The invention also provides a process for the synthesis of letrozole in which formation of the impurity 4-[1-(1,3,4-triazolyl)methyl]benzonitrile during the first stage is minimized. In the process, a 4-(halomethyl)benzonitrile is reacted with a salt of 1H-1,2,4-triazole, reducing the formation of the impurity. Preferably, the preparation is conducted as a one-pot process.

The present invention discloses a kind of micronized letrozole and its composite. Said invention utilizes a micronization process to micronize said letrozole and make the micronized letrozole be combined with a proper carrier so as to obtain a micronized letrozol preparation with proper dissolubility. Said preparation can be used for effectively curing mammary cancer.

The invention discloses a dispersible tablet containing letrozole which has letrozole action ingredient and pharmaceutical accessories. The tablet is applied to the treatment of post-menopausal breast cancer.

Provided is a method for preparing letrozole, which includes reacting an activated bis-(4-cyanophenyl)-methane with a triazole to produce letrozole, and, optionally, purifying the letrozole. Also provided are highly pure letrozole, and a method of purifying letrozole, which method includes precipitating letrozole, e.g., by selective precipitation from a reaction mixture and / or by subjecting the letrozole to one or more crystallizations.

A process for preparing letrozole, and purified letrozole.

The invention relates to a capsule containing palbociclib and a preparation method thereof, belonging to the technical field of pharmaceutical preparations. This product can be used in combination with letrozole for patients with advanced breast cancer. The capsule contains palbociclib, diluent, disintegrant and lubricant, wherein the mass ratio of palbociclib is 10% to 40%, and the mass ratio of diluent is 30% to 80%, The mass proportion of the disintegrating agent is 1%-10%, and the consumption amount of the lubricant is 0.5-5%. In addition, the present invention also discloses a method for preparing palbociclib capsules. The palbociclib capsules prepared by the method of the present invention have simple process and operation, and are particularly suitable for industrial production. The prepared The palbociclib capsule has good stability and good dissolution rate.

The invention provides a large-scale cultivation method of all-female Nibea albiflora. The method mainly includes the steps of firstly, inducing the gynogenesis diploid of Nibea albiflora; inducing and identifying pseudo-male Nibea albiflora; thirdly, allowing the pseudo-male Nibea albiflora to mate with normal female Nibea albiflora to reproduce all-female Nibea albiflora. The method has the advantages that aromatase inhibitor letrozole is used to induce pseudo-male Nibea albiflora reproduction on the basis that the Nibea albiflora gynogenesis technology is built, the mating of the pseudo-male Nibea albiflora and the normal female Nibea albiflora is utilized to obtain the all-female Nibea albiflora for the first time; the built large-scale all-female Nibea albiflora cultivation method issimple to operate, safe, efficient and the like, the cultivated all-female Nibea albiflora is fast in growth, stable in character and the like, and strong technical support is provided for the realizing of Nibea albiflora unisexual cultivation.

The process of synthesizing letrozole includes the first reducing 4, 4'-dicyan diphenyl ketone with sodium borohydride in alcohol solvent to produce 4, 4'-dicyan diphenyl methanol; the subsequent halogenating 4, 4'-dicyan diphenyl methanol in non-polar solvent to produce 4, 4'-dicyan diphenyl methane halide; and the final condensation reaction between 4, 4'-dicyan diphenyl methane halide and 1, 2, 4-triazole in non-polar solvent to produce letrozole. The process has simple operation, high safety and low material cost, and is suitable for industrial production of letrozole.

Provided is a process for purifying a letrozole product that contains an isoletrozole impurity, which process preferably includes converting at least a portion of the isoletrozole impurity into 4,4′-dicyanobenzophenone and removing 4,4′-dicyanobenzophenone, to produce a purified letrozole product.

The invention relates to a preparation method for letrozole tablets with good stability, and belongs to the technical field of pharmaceutical preparations. The preparation method comprises the following steps: dissolving 20-30 parts of letrozole in 120-180 parts of alcohol; adding 5-10 parts of titanium oxide, 3-6 parts of heavy magnesium carbonate and 10-20 parts of micro powder silica gel; reducing pressure and evaporating the alcohol to dryness; taking out the dried composition; screening the composition; adding 70-90 parts of a filling agent, 5-10 parts of a disintegrating agent and 4-8 parts of a lubricant; mixing the materials uniformly; directly conducting tabletting to obtain the letrozole tablets. The prepared letrozole tablets are good in medicine stability, and dissolution rate, and avoid sticking of the tablets.

The invention aims at providing a method for breeding full-feminization rainbow trout. The method comprises the steps of first feeding a mixed feed containing a feed for common fishes and letrozole and then feeding the feed for common fishes in the breeding of first upward floating fries obtained in first fertilized ovum incubation; taking sperms of false milter with female genotype and male phenotype from adult fish to perform second fertilization together with ovum of the rainbow trout, and finally obtaining second adult fish, namely the full-feminization rainbow trout. The mixed feed containing the letrozole is used in the first feeding process, thereby facilitating control of gender of larval fish. Parameters of the method are reasonably set in two-time incubation and feeding steps, and various factors produce synergistic effect, thereby facilitating the incubation of the fertilized ovum to obtain upward floating fries and enabling the upward floating fries to grow to be adult fish. Various operation methods in the method are simple, convenient and easy to perform, and the method is good in adaptability and suitable for being popularized and used in vast numbers of farmers.

Letrozole cutaneous penetration patch and its preparation method, it involves a cutaneous penetration patch and the patch preparation methods. The invention solves problems of the present Letrozole available dosage form drugs in the treatment of postmenopausal women with advanced aspects in short effective time, frequent administration, a more dverse reactions. It consists of matrix layer, back lining and protective film. The matrix layer of letrozole cutaneous penetration patch includes letrozole, adhesives and organic solvents. Their preparation methods: (a) spraid the mixture of letrozole, adhesives and organic solvents evenly on the back lining; (b) after they are dried, cover the protective membrane on the other surface of the patch matrix layer, then the letrozole cutaneous penetration patch is obtained. The patches matrix layer of the invention has good compatibility and adhesiveness with skin, good stability. The invention of the patches maintains constant speed, uniform release, obvious treatment results and long effective time, long recurrence interval, low recurrence rate. Preparation of the present invention patch method is simple and easy to operate.

The invention provides a high-yield process for the preparation of letrozole having a high purity, without the need for removal of the 4-[1-(1,3,4-triazolyl)methyl]benzonitrile impurity at the intermediate stage. The invention also provides a process for the synthesis of letrozole in which formation of the impurity 4-[1-(1,3,4-triazolyl)methyl]benzonitrile during the first stage is minimized. In the process, a 4-(halomethyl)benzonitrile is reacted with a salt of 1H-1,2,4-triazole, reducing the formation of the impurity. Preferably, the preparation is conducted as a one-pot process.

The invention relates to a letrozole tablet and a preparation method thereof. The letrozole tablet comprises the following main auxiliary materials: microcrystalline cellulose, lactose, sodium starch glycolate, L-HPC (low-substituted hydroxypropyl cellulose), sodium lauryl sulfate, Tween 80, magnesium stearate and starch; the preferable sodium lauryl sulfate:Tween 80 ratio is 2:1, and the sodium starch glycolate:L-HPC ratio is 5:1. The tablet has stable product quality, obviously enhances the letrozole dissolution, and effectively enhances the bioavailability; and the tablet preparation technique is simple, does not need special equipment, and is convenient to operate and suitable for industrial production.

The invention discloses a method for controlling hoplobatrachus tigerinus sex ratio and application of the method and belongs to the technical field of hoplobatrachus tigerinus artificial culture. The method includes: placing hatched tadpoles into a cultivation pond according to cultivation density of 3-4 / liter, using feed containing 0.08-0.12 milligram of testosterone or letrozole in each gram to feed the tadpoles under 29-34 DEG C for two weeks, and then using feed which does not contain the testosterone or letrozole to feed the tadpoles until metamorphosis is completed. By the method, the sex ratio after the metamorphosis can be adjusted effectively, and the cultivation efficiency of hoplobatrachus tigerinus can be increased greatly. Compared with feeding under natural conditions, the method has the advantages that a metamorphosis cycle can be shortened greatly, and metamorphosis rate can be increased.

The invention discloses a Letrozole tablet with high dissolubility and a preparation method thereof. An effective component of the tablet is Letrozole, and polyvinylpyrrolidone K30, tween 80, mannitol, lactose, microcrystalline cellulose, cross-linked polyvinylpolypyrrolidone and magnesium stearate are used as accessories. The product of the tablet has stable quality and high dissolubility, enables absorption of Letrozole in a human body to be increased and bioavailability to be effectively improved and is easy to prepare and applicable to industrial production.

The invention provides a preparation method of letrozole (6). The preparation method comprises the following steps: reacting a compound (1) with a compound (3) under the effect of an alkaline matter; performing a bromination reaction of the compound (3) to obtain a compound (4); condensing the compound (4) and 4-amino-1,2,4-triazole (5); and performing diazotization to remove the amino to obtain letrozole (6). According to the method provided by the invention, the route is simple; the cheap and easily available p-chlorobenzonitrile and p-tolunitrile are adopted as starting raw materials, and the target product letrozole is obtained through 3 steps of reactions in total; and the preparation method has the advantages of mild reaction conditions, simple and convenient operation, high yield, good chemical selectivity and low production cost, is suitable for industrial production and brings relatively great practical application value and social economic benefits.

The invention discloses a preparation method of letrozole. In the method, a process reaction post-processing operation process does not contain a reduced pressure distillation process, so that the reaction time is greatly shortened, the industrial cost is reduced, and the product yield is improved. According to the invention, the use of low-polarity highly-flammable reagents such as n-heptane and the like in the prior art is avoided, the operation risk is reduced, and the production safety is improved; reagents adopted in the invention are all common reagents, therefore, the method is more environment-friendly and economic; and the method is suitable for industrialized mass production.

The invention discloses a compound medicine containing letrozole and a preparation method of the compound medicine. The medicine contains the letrozole, copovidone, mannitol, cellulose, crosslinked povidone, magnesium stearate, polyethylene glycol, lactose and starch. The formula of the medicine consists of 8-20 parts of the letrozole, 80-150 parts of the copovidone, 1-3 parts of the mannitol, 4-6 parts of the cellulose, 1-2 parts of the crosslinked povidone, 1-2 parts of the magnesium stearate, 1-3 parts of the polyethylene glycol, 0.5-1 part of the lactose and 1-2 parts of the starch. The compound medicine provided by the invention can significantly improve a letrozole dissolution rate and can further improve bioavailability and clinical treatment effect of medicinal active ingredients; and in addition, a release speed can be reduced, so that the purpose of uniform administration is achieved; therefore, drug tolerance is enhanced.

The invention relates to the cream and the ointment of Letrozole tablet percutaneous administration and the preparation method of the cream and the ointment thereof, and relates to the cream and the ointment of the percutaneous administration and the preparation method of the cream and the ointment thereof. The invention solves the problems that the prior Letrozole tablet oral preparation cannot avoid the first pass effect of liver and the bad reaction is numerous. The cream and the ointment of the percutaneous administration are characterized in that the cream and the ointment of the percutaneous administration comprise raw materials and penetrating agent with the following percentages: 0.01 to 20 percent of Letrozole tablet and 0.1 to 20 percent of percutaneous penetrating agent. The invention has the method that through vitro and a skin penetration test, the Letrozole tablet only with oral preparation is filtered out a formula with good non-steady state / steady state distribution by a skin release curve, and then the cream and the ointment of the percutaneous administration are prepared, so as to lead principal medicine to avoid the liver first pass effect of oral administration to directly reach mammary gland target tissue, and to lead the concentration of target tissue internal medicine to be improved. Compared with the prior preparation at home and at abroad, the invention technically has the advantages that the prepared external preparation can reduce the side effect of Letrozole tablet and improve the curative effect of the Letrozole tablet, thereby the invention has good promotion and application value.

Crystalline forms of letrozole can be made by precipitation and are useful in making pharmaceutical compositions.

The present disclosure relates to the field of cancer treatment, and more specifically to the field of treatment of primary malignant brain tumors. Provided herein are methods of treating primary brain tumors, including gliomas, by administering to a patient in need thereof a therapeutically effective amount of the aromatase inhibitor letrozole.

Provided is a method for preparing letrozole, which includes reacting an activated bis-(4-cyanophenyl)-methane with a triazole to produce letrozole, and, optionally, purifying the letrozole. Also provided are highly pure letrozole, and a method of purifying letrozole, which method includes precipitating letrozole, e.g., by selective precipitation from a reaction mixture and / or by subjecting the letrozole to one or more crystallizations.

Provided herein are compositions and methods for treating ER+, HER2- HRG+ breast cancer (e.g., metastatic ER+, HER2- breast cancer) in a patient by administering to the patient an anti-ErbB3 antibody(e.g., seribantumab), a CDK4 / 6 inhibitor (e.g., palbociclib), and an endocrine based therapy (e.g., letrozole or fulvestrant) according to a particular clinical dosage regimen (i.e., at a particular dose amount and according to a specific dosing schedule). Also provided herein are compositions and methods for treating ER+, HER2- HRG+ breast cancer (e.g., metastatic ER+, HER2- breast cancer) in a patient by administering to the patient an anti-ErbB3 antibody (e.g., seribantumab) and an endocrine based therapy (e.g., letrozole or fulvestrant) according to a particular clinical dosage regimen (i.e., at a particular dose amount and according to a specific dosing schedule).

The invention belongs to the technical field of medicine and relates to a letrozole dispersing tablet dosage form. A lot of clinical surveys prove that necessity of the letrozole dispersing tablet dosage form is confirmed and the letrozole dispersing tablet dosage form improves patient compliance and medicine bioavailability. The letrozole dispersing tablet dosage form can be used for treatment on breast cancer of postmenopausal women.

The invention relates to a process for preparing letrozole with high degree of purity.

Novel injectable compositions are provided comprising an active agent which is tarnsulosin or letrozole or its pharmaceutically acceptable salts, derivatives, isomers, polymorphs, solvates, hydrates, analogues, enantiomers, tautomeric forms or mixtures thereof and one or more pharmaceutically acceptable excipient(s) wherein the compositions are preferably formulated as biodegradable microparticles or nanoparticles which can optionally be reconstituted with an aqueous, hydro-alcoholic or oily liquid vehicle prior to administration. The novel injectable compositions of the present invention preferably form a depot upon administration in vivo and are in the form of an in situ gelling composition or an implant composition which provides a prolonged release of tamsulosin or letrozole for extended periods of time.; Also described are process for preparation of such novel compositions and method of using them.