Penciclovir microemulsion gel preparation and preparing method thereof

Abstract

The invention relates to a penciclovir micro-emulsified gel and preparation process, belonging to medicine technology field, which comprises penciclovir surfactant, assistant surfactant, oil phase, water and carbomer and is used for transdermal drug delivery, the processing method is simple, the quality is easy to be controlled, and the stability of the gel is good, compared with present cream, the unit area accumulation infiltration amount of drugs can be improved obviously, and detained dosage in epidermis and dermis can be improved, moreover the invention has certain sustained-release function so that drug treating times and drug amounts can be reduced, and the using process of the drug is convenient, no pollution is caused to clothes, so the medicine is suitable for clinical wide application.

Description

technical field

[0001] The invention relates to a penciclovir microemulsion gel preparation and a preparation method thereof, belonging to the technical field of medicine. Background technique

[0002] Penciclovir (Penciclovir, PCV) is a third-generation nucleoside broad-spectrum antiviral drug, which is a derivative of acyclovir. , herpes simplex virus type II (HSV-I, II), varicella-zoster (VZV), hepatitis B virus (HBV), African lymphoma virus (EBV) and cytomegalovirus (CMV) and other viruses are inhibited effect. Penciclovir rapidly enters herpesvirus-infected and uninfected cells, but exerts its selective antiviral effect only in herpesvirus-infected cells. The half-life of its active form in cells is 14 times higher than that of acyclovir and it is easily concentrated by cells. It is a more effective antiviral drug than ACV. However, penciclovir is poorly absorbed in the gastrointestinal tract, and its oral bioavailability is only 5% to 10%, and the effect is better w...

Examples

Embodiment 1

[0032] Embodiment 1. Penciclovir microemulsion gel preparation, component is as follows:

[0033] Solution A: Penciclovir 0.6g

[0034] Polyoxyethylene castor oil (surfactant) 20g

[0035] Ethanol (co-surfactant) 30g

[0036] Oleic acid (oil phase) 5g

[0037] Add water to 100g

[0038] Solution B: Carbomer 940 (gel matrix) 0.8g

[0039] Water 19.2g.

[0040] The preparation method is as follows:

[0041] (1) Preparation of liquid A: Weigh 5 g of oleic acid, 20 g of polyoxyethylene castor oil, and 30 g of ethanol, stir to mix evenly, add water to a total weight of 99.4 g, stir and balance for 30 minutes to obtain a clear and transparent blank microemulsion; Add 0.6g Penciclovir in the milk, stir to obtain a clear and transparent Penciclovir microemulsion.

[0042] (2) Preparation of liquid B: Weigh 0.8 g of Carbomer 940, add water to 20 g, stir and let stand for 24 hours to completely swell.

[0043] (3) Slowly add liquid A into liquid B, keep ...

Embodiment 2

[0045] Embodiment 2. Penciclovir microemulsion gel preparation, component is as follows:

[0046] Liquid A: Penciclovir 0.5g

[0047] Tween 80 (surfactant) 30g

[0048] Polyethylene glycol 400 (co-surfactant) 25g

[0049] Ethyl oleate (oil phase) 4g

[0050] Add water to 100g

[0051] Solution B: Carbomer 940 (gel matrix) 1.0g

[0052] Water 19.0g.

[0053] The preparation method is as follows:

[0054](1) Preparation of liquid A: Weigh 4 g of ethyl oleate, 30 g of Tween-80, and 25 g of polyethylene glycol 400, stir to mix evenly, add water to a total weight of 99.5 g, stir and balance for 30 minutes to obtain a clear and transparent blank microsphere. Milk; Add 0.5g Penciclovir in blank microemulsion, stir to get clear and transparent Penciclovir microemulsion.

[0055] (2) Preparation of liquid B: Weigh 1.0 g of Carbomer 940, add water to 20 g, stir and let stand for 24 hours to completely swell.

[0056] (3) Slowly add liquid A into liquid B...

Embodiment 3

[0058] Embodiment 3. Penciclovir microemulsion gel preparation, component is as follows:

[0059] Liquid A: Penciclovir 0.5g

[0060] Caprylic / capric macrogol glycerides (surfactant) 23g

[0061] Diethylene glycol monoethyl ether (co-surfactant) 21g

[0062] Isopropyl myristate (oil phase) 6g

[0063] Add water to 100g

[0064] Liquid B: Carbomer (gel matrix) 934 1.2g

[0065] Water 18.8g.

[0066] The preparation method is as follows:

[0067] (1) Preparation of liquid A: Weigh 6g of isopropyl myristate, 23g of caprylic / capric macrogol glyceride, 21g of diethylene glycol monoethyl ether, stir to mix evenly, add water to a total weight of 99.5g, stir And balance for 30min to obtain a clear and transparent blank microemulsion; add 0.5g of penciclovir to the blank microemulsion, and stir to obtain a clear and transparent penciclovir microemulsion.

[0068] (2) Preparation of liquid B: Weigh 9341.2 g of carbomer, add water to 20 g, stir and let sta...

technical field

[0001] The invention relates to a penciclovir microemulsion gel preparation and a preparation method thereof, belonging to the technical field of medicine. Background technique

[0002] Penciclovir (Penciclovir, PCV) is a third-generation nucleoside broad-spectrum antiviral drug, which is a derivative of acyclovir. , herpes simplex virus type II (HSV-I, II), varicella-zoster (VZV), hepatitis B virus (HBV), African lymphoma virus (EBV) and cytomegalovirus (CMV) and other viruses are inhibited effect. Penciclovir rapidly enters herpesvirus-infected and uninfected cells, but exerts its selective antiviral effect only in herpesvirus-infected cells. The half-life of its active form in cells is 14 times higher than that of acyclovir and it is easily concentrated by cells. It is a more effective antiviral drug than ACV. However, penciclovir is poorly absorbed in the gastrointestinal tract, and its oral bioavailability is only 5% to 10%, and the effect is better w...

Examples

Embodiment 1

[0032] Embodiment 1. Penciclovir microemulsion gel preparation, component is as follows:

[0033] Solution A: Penciclovir 0.6g

[0034] Polyoxyethylene castor oil (surfactant) 20g

[0035] Ethanol (co-surfactant) 30g

[0036] Oleic acid (oil phase) 5g

[0037] Add water to 100g

[0038] Solution B: Carbomer 940 (gel matrix) 0.8g

[0039] Water 19.2g.

[0040] The preparation method is as follows:

[0041] (1) Preparation of liquid A: Weigh 5 g of oleic acid, 20 g of polyoxyethylene castor oil, and 30 g of ethanol, stir to mix evenly, add water to a total weight of 99.4 g, stir and balance for 30 minutes to obtain a clear and transparent blank microemulsion; Add 0.6g Penciclovir in the milk, stir to obtain a clear and transparent Penciclovir microemulsion.

[0042] (2) Preparation of liquid B: Weigh 0.8 g of Carbomer 940, add water to 20 g, stir and let stand for 24 hours to completely swell.

[0043] (3) Slowly add liquid A into liquid B, keep ...

Embodiment 2

[0045] Embodiment 2. Penciclovir microemulsion gel preparation, component is as follows:

[0046] Liquid A: Penciclovir 0.5g

[0047] Tween 80 (surfactant) 30g

[0048] Polyethylene glycol 400 (co-surfactant) 25g

[0049] Ethyl oleate (oil phase) 4g

[0050] Add water to 100g

[0051] Solution B: Carbomer 940 (gel matrix) 1.0g

[0052] Water 19.0g.

[0053] The preparation method is as follows:

[0054](1) Preparation of liquid A: Weigh 4 g of ethyl oleate, 30 g of Tween-80, and 25 g of polyethylene glycol 400, stir to mix evenly, add water to a total weight of 99.5 g, stir and balance for 30 minutes to obtain a clear and transparent blank microsphere. Milk; Add 0.5g Penciclovir in blank microemulsion, stir to get clear and transparent Penciclovir microemulsion.

[0055] (2) Preparation of liquid B: Weigh 1.0 g of Carbomer 940, add water to 20 g, stir and let stand for 24 hours to completely swell.

[0056] (3) Slowly add liquid A into liquid B...

Embodiment 3

[0058] Embodiment 3. Penciclovir microemulsion gel preparation, component is as follows:

[0059] Liquid A: Penciclovir 0.5g

[0060] Caprylic / capric macrogol glycerides (surfactant) 23g

[0061] Diethylene glycol monoethyl ether (co-surfactant) 21g

[0062] Isopropyl myristate (oil phase) 6g

[0063] Add water to 100g

[0064] Liquid B: Carbomer (gel matrix) 934 1.2g

[0065] Water 18.8g.

[0066] The preparation method is as follows:

[0067] (1) Preparation of liquid A: Weigh 6g of isopropyl myristate, 23g of caprylic / capric macrogol glyceride, 21g of diethylene glycol monoethyl ether, stir to mix evenly, add water to a total weight of 99.5g, stir And balance for 30min to obtain a clear and transparent blank microemulsion; add 0.5g of penciclovir to the blank microemulsion, and stir to obtain a clear and transparent penciclovir microemulsion.

[0068] (2) Preparation of liquid B: Weigh 9341.2 g of carbomer, add water to 20 g, stir and let sta...

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