116 results about "Ganciclovir" patented technology

A prodrug composition is provided which includes a pharmaceutical species and an amino acid having a covalent bond to the pharmaceutical species. The pharmaceutical species is characterized by bioavailability of 30% or less and a molecular weight in the range of 100-1000 Daltons. The composition is characterized further in that the pharmaceutical species is not acyclovir, ganciclovir, BRL44385, or penciclovir. Also described is an inventive method of delivering a pharmaceutical species to an individual including the step of orally administering an inventive prodrug to an individual. In one embodiment the prodrug includes a pharmaceutical species characterized by bioavailability of 30% or less, wherein the pharmaceutical species has a molecular weight in the range of 100-1000 Daltons. The inventive prodrug is transported from the gastrointestinal lumen by a specific transporter and is enzymatically cleaved to yield the pharmaceutical species, such that the pharmaceutical species is delivered to the individual.

The invention mainly belongs to the technical field of gene editing and particularly relates to an SSA (single-strand annealing) repair-based gene seamless editing method utilizing a CRISPR/Cas9 technology. According to the gene seamless editing method, CRISPR/Cas9 expression vectors CCR5.CRISPR/Cas9 and eGFP.CRISPR/Cas9 targeting CCR5 and eGFP are constructed firstly, a donor CCR5-Donor vector is constructed, a CCR5-Donor plasmid vector adopts the pXL-BACII-L-arm-CAG-TK-PGK-Puro<R>-T2A-eGFP-bGH pA-R-arm structure, L-arm and R-arm are left and right homologous arms, and CAG-TK-PGK-Puro<R>-T2A-eGFP-bGH pA between L-arm and R-arm is a screening marking component; through two times of transfection, seamless editing is completed by using HR and SSA repair mechanisms in the CRISPR-Cas9 system and cells through positive and negative screening of puromycin and ganciclovir of the cells.

The invention discloses a method for inhibiting target gene expression by antisense lncRNA-mediated cis-regulation. The method for inhibiting gene expression by antisense lncRNA-mediated cis-regulation is characterized in that by utilizing the characteristic that the lncRNA has the effect of competing endogenous target RNA, a strong promoter is inserted on a target gene by taking RNA as a genome positioning tool through a CRISPR Cas9 gene editing method, and a lot of antisense lncRNA complementary with the target gene is synthesized to realize in situ cis-competitive inhibition of expression of the endogenous target gene. The method comprises the following steps: firstly, constructing a targeting vector and a homologous template strand donor vector, simultaneously transfecting the constructed vectors into host cells, performing target cloning by puromycin and ganciclovir co-screening, and finally, performing detection and functional research on expression of the target gene.

Described herein are compositions and methods for the treatment of cancer, and particularly brain cancer (e.g., glioma) in a mammal. In various embodiments of the invention, a combined therapeutic approach including TK with systemic ganciclovir administration and Flt3L are used in connection with gene therapeutic techniques or direct peptide injection for the aforementioned indications. Kits useful in practicing the inventive method are also disclosed, as are animal models useful for studying brain cancer.

The invention relates to a Ganciclovir freeze-dry preparation for injection, comprising 50-250 parts of Ganciclovir and 100-200 parts of hydroxypropyl-beta-cyclodextrin. The invention also relates to a preparation method of the Ganciclovir freeze-dry preparation for injection. In the preparation process of the Ganciclovir freeze-dry preparation, Ganciclovir freeze-dry preparation can be dissolved into solvent when the pH value is almost neutral to improve the compliance for clinical application; freeze-dry time is shortened to be 22-26 hours, thus improving product quality, saving energy and lowering consumption.

The invention discloses a multifunctional microemlusion gel preparation and a preparation process thereof, and belongs to the technical field of medicines. The preparation mainly comprises bulk pharmaceutical chemicals (such as non-steroidal anti-inflammatory drugs-diclofenac sodium, ibuprofen, indometacin, antifungal drugs-ornidazole, antiviral drugs-ganciclovir, hormone drugs-dexamethasone, local anesthesia drugs-lidocaine and irritants-menthol), a cationic polymer and a microemlusion, can further comprise gel or a thickener, and can be used for transdermal drug delivery and local drug delivery. The preparation process is simple, convenient, good in stability and pollution-free. Compared with existing cream and gel, the preparation has the advantages that a novel action mechanism is adopted, the accumulative penetration amount of unit area of drugs is remarkably increased, a certain slow-release effect is achieved, and the drug delivery frequency and the drug delivery amount can be reduced; a chemical penetration enhancer and a conventional preservative are not added, a certain bacterial inhibition effect is achieved, the skin irritation is avoided, and the use safety of the drugs is improved.

A method is disclosed for encapsulating plasmids, oligonucleotides or negatively-charged drugs into liposomes having a different lipid composition between their inner and outer membrane bilayers and able to reach primary tumors and their metastases after intravenous injection to animals and humans. The formulation method includes complex formation between DNA with cationic lipid molecules and fusogenic/NLS peptide conjugates composed of a hydrophobic chain of about 10-20 amino acids and also containing four or more histidine residues or NLS at their one end. The encapsulated molecules display therapeutic efficacy in eradicating a variety of solid human tumors including but not limited to breast carcinoma and prostate carcinoma. Combination of the plasmids, oligonucleotides or negatively-charged drugs with other anti-neoplastic drugs (the positively-charged cis-platin, doxorubicin) encapsulated into liposomes are of therapeutic value. Also of therapeutic value in cancer eradication are combinations of encapsulated the plasmids, oligonucleotides or negatively-charged drugs with HSV-tk plus encapsulated ganciclovir.

A method for encapsulating cisplatin and other positively-charged drugs into liposomes having a different lipid composition between their inner and outer membrane bilayers is disclosed. The liposomes are able to reach primary tumors and their metastases after intravenous injection to animals and humans. The encapsulated cisplatin has a high therapeutic efficacy in eradicating a variety of solid human tumors including but not limited to breast carcinoma and prostate carcinoma. Combination of the encapsulated cisplatin with encapsulated doxorubicin or with other antineoplastic drugs are claimed to be of therapeutic value. Also of therapeutic value in cancer eradication are claimed to be combinations of encapsulated cisplatin with a number of anticancer genes including but not limited to p53, IL-2, IL-12, angiostatin, and oncostatin encapsulated into liposomes as well as combinations of encapsulated cisplatin with HSV-tk plus encapsulated ganciclovir.

Compositions, methods and systems for treating disordered epithelial tissues, such as is caused by pathogens and/or by toxins produced thereby. The invention relates to the use of an anti-infective and/or antimicrobial active agent in a carrier, with vigorous agitation of the disordered epithelial tissue for topical treatment thereof under such conditions sufficient to achieve clinically discernable improvement of the disordered epithelial tissue. The preferred anti-infective and/or antimicrobial active agent comprises a nucleoside, such as acyclovir, valcyclovir, penciclovir, famciclovir, ganciclovir, cidofovir, adefovir, and tenofovir, and derivatives, analogs, or metabolites thereof, or a mixture thereof, or 1-docosanol, optionally in combination with an organohalide. The inventive compositions and methods may employ the use of an applicator adapted for use in promoting the penetration of the treatment composition and/or the vigorous agitation of the disordered tissue.

The invention relates to a ganciclovir composition for injection, which is freeze-dried powder composed of ganciclovir and sodium hydroxide, wherein the weight ratio of the ganciclovir to the sodium hydroxide is (6.6-7.0):1, the average particle size of the freeze-dried powder is 80-100nm, and the porosity is 94-98%. The preparation method comprises the following steps: 1) preparation: weighing ganciclovir and sodium hydroxide, putting the ganciclovir and sodium hydroxide into a preparation tank, adding water for injection, and stirring until the ganciclovir and sodium hydroxide are completely dissolved and evenly mixed; 2) sterile filtration and packaging; and 3) vacuum freeze drying. The invention has the advantages of simple formula, advanced technique, uniform quality and high stability, and has higher redissolution performance and clinical application safety.

The invention relates to the technical field of chemical refining, in particular to a refining method for ganciclovir. The refining method specifically comprises the following steps of: heating to dissolve the ganciclovir by using lower fatty acid aqueous solution; filtering off insoluble substances therein; cooling, crystallizing and suction-filtering filtrate; treating through inorganic alkali solution and then adjusting to be neutral, wherein the content of guanine impurity in the ganciclovir is reduced by a method of obtaining solid through crystallization. According to the method of reducing the content of the guanine impurity in the ganciclovir adopted in the refining method, the content of the guanine impurity can be reduced to be below 0.50 percent; and the method has the advantages of no need of repeating crystallization operation, short refining period, low energy consumption and high yield and is suitable for large-scale industrial production.

The invention discloses ganciclovir for injection and a preparation method thereof. The preparation is formed by regulating the pH of a solution containing ganciclovir and sodium chloride to 10.0-11.5 by adopting a pH regulator, and freezing and drying repetitively. The freeze-dried powder injection of the ganciclovir for injection has the advantages of high yield, good re-dissolubility, more stable quality and the like; change of related substances during the period of accelerated test is not obvious; and the ganciclovir for injection is safer for clinical application.

A method of treating ocular disorders (such as, for example, proliferative vitreoretinopathy or PVR) associated with replicating ocular cells by transfecting replicating ocular cells in vivo with a polynucleotide encoding an agent which is capable of providing for the inhibition, prevention, or destruction of the growth of the replicating ocular cells upon expression of the agent. The agent may be a viral thymidine kinase, and the polynucleotide encoding the agent may be contained in a retroviral vector. Once the replicating ocular cells are transduced with the retroviral vector, the patient is given a chemotherapeutic or interaction agent, such as ganciclovir, which kills the transfected replicating ocular cells.

The invention belongs to the technical field of the analytical chemistry and in particular discloses a valganciclovir hydrochloride impurity HPLC (High Performance Liquid Chromatography) analytical detecting method, and more specifically, the invention relates to a method for analytically detecting guanine, ganciclovir, methoxymethylguanine, ganciclovir 1-N-methyl-valine, mono acetoxyl ganciclovir, mono chloro ganciclovir or a medicine or a preparation containing the above six impurities. A solution to be detected is filled in a high performance liquid chromatographic column taking phenylsilane bonded silica gel as a filling agent, a moving phase prepared by an amine-containing aqueous inorganic salt solution and a chromatographically pure organic solvent is adopted to wash and separate, and then ultraviolet analysis and detection is carried out. According to the method, ammonium acetate or ammonium formate with certain concentration is firstly added in the moving phase creatively, and difficult problems that the main peak and the impurity peak and the adjacent impurity peaks are separated difficultly are thoroughly solved, the operation is simple, the separation degree is high, the sensitivity is high, the accuracy is good, and no similar literature is reported through literature retrieval.

The invention discloses a pharmaceutical composition containing a ganciclovir compound, and a preparation method thereof. The pharmaceutical composition is composed of ganciclovir, polysorbate 80, sodium hydroxide and dextran. The ganciclovir pharmaceutical composition overcomes the irritation of the existing ganciclovir lyophilized powder injections on an injection site, and improves the stability of the ganciclovir lyophilized powder injection and the compliance of patients.

The invention discloses a liposome medicinal composition with tumor targeting, in-vivo tracing and treating functions and a preparation method thereof. The medicinal composition is a liposome targeting medicament which is resistant to CD44 antibody coupling, has a molecular imaging function simultaneously, and can be used for monitoring the in-vivo distribution of a medicament in real time in a living body state. In particular, plasmids containing three fusion genes, including renilla luciferase, red fluorescent proteins and suicide gene thymidine kinase, are coupled to CD44 antibody mediation-resistant immunoliposome, the specificity of liposome nanoparticles in a liver cancer in-situ model of an in-vivo targeting NOD/SCID (Non-Obese Diabetic/Severe Combined Immune-Deficiency) mouse is monitored by detecting a renilla luciferase signal with a living body imaging system, and apoptosis of liver cancer cells is induced by applying target thymidine kinase of ganciclovir; and moreover, a targeted liposome can be coated with adriamycin for inducing apoptosis of the liver cancer cells. The liposome medicinal composition provided by the invention does not have any toxic or side effect, has small damage and a good effect, and is suitable to be applied for a long time.

Stereochemically defined dipeptide esters of nucleoside-analogous antiviral agents including acyclovir and ganciclovir are provided. Certain of these stereochemically defined dipeptide esters are found to have unexpectedly enhanced delivery to and uptake by ocular tissues, crossing the blood-ocular barrier more effectively than other stereochemically defined dipeptide esters. For example, (L-Val)-(D-Val)-acyclovir was found to be taken up more effectively into corneal tissue than were underivatized acyclovir, monoesters (L-Val)-acyclovir or (D-Val)-acyclovir, or diester (L-Val)-(L-Val)-acyclovir.

The present invention relates to a process for the preparation of N2-Acetyl-9-(1,3-diace-toxy-2-propoxymethyl) guanine, referred to here as N-9 alkylated isomer of structural formula I, and to the use of this compound as an intermediate for the preparation of antiviral compound, ganciclovir.

The invention relates to the technical field of medicine, and provides a nano drug-carrying system. The nano drug-carrying system comprises a magnetic-mesoporous silicon dioxide nanorod carrier, a pro-drug GCV (ganciclovir) carried on the carrier, and a graft copolymer PLL-g-PEG (poly-L-lysine graft polyethylene glycol) formed by PLL and PEG, wherein the PLL-g-PEG also carries a suicide gene TK. The magnetic-mesoporous silicon dioxide nanorods are used as the magnetic targeted carrier to carry the suicide gene TK/pro-drug GCV to enter cells, thereby implementing the time and space consistency of the suicide gene and pro-drug transfer, and further implementing accurate drug release. The magnetic-mesoporous silicon dioxide silicon dioxide nanorods and suicide gene/pro-drug treatment method are effectively combined, thereby enhancing the combined treatment effect on the liver cancer. The preparation method of the nano drug-carrying system is simple in technique and suitable for large-scale industrial production.

The invention belongs to medical detection field, relates to an analysis detection method of drug in the body of a person, and specifically relates to the method that the densities of antiviral drugs in blood plasma of the person such as acyclovir, ganciclovir and penciclovir can be detected at the same time. The method in the invention is characterized in that pilot sample is pretreated; as acyclovir, ganciclovir and penciclovir have the character of strong fluorescence absorption, acyclovir, ganciclovir and penciclovir can be separated from each other in an acidity flowing phase chromatographic column and be detected by a fluorescence detector. The method in the invention has the advantages of little sample, simple, swift and sensitive pretreatment, short analysis period and low cost; furthermore, the invention doesn't need expensive equipment and reagent and is suitable for the detection of clinical conventional blood drug density of acyclovir, ganciclovir and penciclovir.

The invention relates to the technical field of chemical compound recovery, and particularly relates to a method of converting a ganciclovir condensation compound isomer into a ganciclovir condensation compound. The method utilizes a characteristic that the ganciclovir condensation compound isomer can be converted into the ganciclovir condensation compound by structural transformation in a solution, and the ratio of the ganciclovir condensation compound isomer to the ganciclovir condensation compound in the solution is in a dynamic equilibrium relationship of about 35:65. By adoption of the technical scheme, the purity of the obtained ganciclovir condensation compound can be more than 98.0%, wherein the content of the ganciclovir condensation compound isomer is less than 0.5% and the yield is about 50%. The method effectively overcomes treatment problems of the ganciclovir condensation compound isomer, increases the total yield of the ganciclovir condensation compound, indirectly reduces the raw material cost of the ganciclovir condensation compound, reduces environment pollution and is suitable for popularization and application.

The invention discloses a method for synthesizing acyclovir and ganciclovir by carbon-hydrogen bond activation and belongs to the field of organic synthesis. The method comprises that inexpensive guanine as a raw material undergoes methyl protection on 9th NH, a high-valent iodine reagent and monoacetyl-protected ethylene glycol or 1, 2-isopropylidene-protected glycerol are added into the raw material under catalysis of palladium acetate, the mixture undergo a heating reaction to produce acetyl-protected acyclovir or acetyl-protected ganciclovir, and the acetyl group is removed by an inorganicalkali alcohol solution so that acyclovir and ganciclovir are obtained. The method utilizes cheap and easily available raw materials, prevents use risk and corrosive reagents, has the advantages of short reaction route, simple operation, high atomic economy and high total product yield, provides a novel synthesis route of acyclovir and ganciclovir and has a potential application prospect.