Penciclovir ophthalmic temperature sensitivity in situ gel preparation and preparation method thereof

An in-situ gel, penciclovir technology, applied in the directions of non-active ingredients medical preparations, sensory diseases, antiviral agents, etc., can solve the problem of eye discomfort, unfavorable absorption, short drug retention time and action time and other problems, to achieve the effect of easy and accurate dose control, good biocompatibility, and improved bioavailability

Inactive Publication Date: 2008-05-28
MEDICINE & BIOENG INST OF CHINESE ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Common ophthalmic preparations are mostly eye drops made of water-soluble drugs, and their main defects include: short residence time and action time of drugs in the eye, frequent administration; pulse-type entry of drugs after medication; nasolacrimal duct drainage systemic adverse effects and lack of effective drug delivery systems into the posterior segment of the eye
Possible disadvantages of poloxamer gels include poor mechanical strength of the gel, rapid erosion (i.e., dissolution from the surface), abiotic degradation of PEO-PPO-PEO chains, therefore, it is necessary to combine poloxamers with other biological Adhesive polymers used together
[0008] Poloxamers can be used to prepare ophthalmic in-situ gels, but it is difficult to obtain a system with a suitable concentration and phase transition temperature when used alone. High concentrations will cause low phase transition temperatures, which brings inconvenience to patients. The temperature of the preparation If it is too low, it will easily cause discomfort to the eyes, causing physiological reactions such as tearing and blinking, which is not conducive to absorption
[0009] After searching the literature, no report was found on the preparation of PCV ophthalmic in situ gel with a suitable phase transition temperature and certain adhesion ability by using poloxamer and bioadhesive in combination

Method used

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  • Penciclovir ophthalmic temperature sensitivity in situ gel preparation and preparation method thereof
  • Penciclovir ophthalmic temperature sensitivity in situ gel preparation and preparation method thereof
  • Penciclovir ophthalmic temperature sensitivity in situ gel preparation and preparation method thereof

Examples

Experimental program
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Embodiment 1

[0027]PCV ophthalmic in situ gel containing carbomer: Weigh 0.3% carbomer 934P, add distilled water, stir fully, place until completely dissolved, and use it as solution I; weigh 18% PF127, add distilled water, stir to make Partially dissolve, put it in the refrigerator for at least 24 hours until completely dissolved, and use it as solution II; dissolve 0.2% PCV, 5% mannitol, and 0.01% benzalkonium chloride in distilled water, stir to dissolve, and pass through 0.30μm Filter through a microporous membrane, combine the filtrate with solution I and solution II, adjust the pH value to 6.5 with 1mol / L sodium hydroxide solution, add distilled water to the full amount, and stir evenly to obtain the product.

Embodiment 2

[0029] PCV ophthalmic in situ gel containing hydroxypropyl methylcellulose (HPMC): Weigh 0.4% HPMC K4M, add distilled water, heat to 70°C, stir fully, place until completely dissolved, as solution I; weigh Add 18% PF127 into distilled water, stir to partially dissolve, place in the refrigerator for at least 24 hours until completely dissolved, and use it as solution II; dissolve 0.1% PCV, 0.9% sodium chloride, and 0.01% benzalkonium chloride in Stir to dissolve in distilled water, filter through a 0.30 μm microporous membrane, combine the filtrate with solution I and solution II, adjust the pH value to 7.5 with 1mol / L sodium hydroxide solution, add distilled water to the full amount, and stir evenly, that is have to.

Embodiment 3

[0031] PCV ophthalmic in-situ gel containing polyvinylpyrrolidone (PVP): Weigh 20% PF127, add it into distilled water, stir to partially dissolve it, place it in the refrigerator for at least 24 hours until it is completely dissolved, and use it as solution I; Dissolve 0.1% PCV, 0.8% PVP K30, 0.9% sodium chloride, and 0.01% benzalkonium chloride in distilled water, stir to dissolve, filter through a 0.30 μm microporous membrane, combine the filtrate with solution I, and use 1mol / L sodium hydroxide solution to adjust the pH value to 6.5-7.5, add distilled water to the full amount, stir evenly, and get ready.

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Abstract

The invention provides an in situ eye gel preparation of penciclovir. The compositions and weight percentages thereof are 0.01-2.0wt% of penciclovir, 5-40wt% of poloxamer, 0.1-5wt% of tackifier high polymer base, 0.8-10wt% of osmotic regulation agent, 0.001-0.5wt% of antiseptics and the rest is distilled water. Meanwhile, the preparation method is also provided. The in situ gel preparation has good biocompatibility and glutinousness; compared with a liquid preparation, the invention can increase retention time of drug in the eyes and delay elimination, thus improving the bioavailability of the eyes and reducing the times of administration; meanwhile, the invention avoids weaknesses that operation is inconvenient during gel administration, the preparation is not easy to spread in eyes, the dosage can not be controlled accurately, etc.

Description

technical field [0001] The invention relates to a novel ophthalmic drug delivery system, that is, an in-situ gel preparation, in particular to a penciclovir ophthalmic temperature-sensitive in-situ gel preparation and a preparation method thereof. Background technique [0002] Penciclovir (Penciclovir, referred to as PCV) is an antiviral drug successfully developed by British SKB company. base) butyl]-guanine. PCV is used to treat herpes simplex virus (HSV-1, HSV-2) and herpes zoster virus (VZV) infections. In virus-infected cells, viral thymidine kinase phosphorylates this product to PCV monophosphate, and then cellular kinase converts it to PCV triphosphate. PCV is as effective as acyclovir, but its triphosphate has a longer half-life than acyclovir triphosphate. In addition to thymidine kinase mutant HSV isolates resistant to this product, many acyclovir-resistant virus strains are sensitive to this product. PCV is usually given as a cream or a solution for intravenou...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/522A61K9/00A61K47/34A61K47/36A61K47/38A61K47/40A61P27/02A61P31/22A61K47/10
Inventor 李桂玲李眉
Owner MEDICINE & BIOENG INST OF CHINESE ACAD OF MEDICAL SCI
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