CN104523611A - Acyclovir composition chewable tablet and preparation method thereof - Google Patents
Acyclovir composition chewable tablet and preparation method thereof Download PDFInfo
- Publication number
- CN104523611A CN104523611A CN201410735482.5A CN201410735482A CN104523611A CN 104523611 A CN104523611 A CN 104523611A CN 201410735482 A CN201410735482 A CN 201410735482A CN 104523611 A CN104523611 A CN 104523611A
- Authority
- CN
- China
- Prior art keywords
- acyclovir
- chewable tablet
- medicinal liquid
- drug
- containing dish
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
Landscapes
- Medicinal Preparation (AREA)
Abstract
Relating to the technical field of medicine and medicine production, the invention provides an acyclovir composition chewable tablet and a preparation method thereof. The acyclovir composition chewable tablet includes acyclovir, starch and sucrose. The tablet overcomes the shortcomings of ordinary chewable tablets, and reduces the variety and dosage of excipients in the acyclovir chewable tablet. The pharmaceutical preparation has the advantages of excellent performance, high bioavailability, good stability, high patient acceptability and no gravel sense, and has important clinical application value.
Description
Technical field
The present invention relates to medicine and medical production technical field, be specifically related to a kind of Acyclovir composition chewable tablet and preparation method thereof.
Background technology
Tablet quality is stable, taking convenience, is basic, the most the most frequently used a kind of dosage form.But for the patient of child, old man and dysphagia, conventional tablet often takes difficulty, and Long-term taking medicine even can make it produce psychological phenomenon of refusing to take medicine, and chewable tablet then can remedy such and insufficient.Chewable tablet is the tablet under a class can chew posterior phraynx in oral cavity, and size is general identical with conventional tablet, can make difform Special-shaped sheet as required.Tablet is convenient to swallow after chewing, and coat tablets is long-pending to be increased, and can promote medicine dissolving in vivo, absorption.For the medicine of difficult disintegrate, make chewable tablet and can accelerate its disintegrate, improve drug effect.Chewable tablet taking convenience, even if also can medication on time under the condition of hydropenia, be specially adapted to the patient that children's, old man, dysphagia or gastrointestinal function are poor, can reduces medicine and bear gastrointestinal.Therefore, chewable tablet application is extensively got up gradually.
Acyclovir (acyclic bird former times, acyclovir), chemistry 9-(2-'-hydroxyethoxy methyl) guanine by name, 9-(2-hydroxyethoxymethyl) guanine, be the guanosine class antiviral agents of open loop of a wide spectrum of Burroughs Wellcome company of Britain exploitation, efficient, low toxicity, all have significant curative effect to the infection that herpesvirus, cytomegalovirus and Ai Positan-epstein-Barr virus etc. cause.Acyclovir is also applicable to disease such as treatment ophthalmology, department of dermatologry etc.Its chemical structural formula is as follows:
Acyclovir was in listing in 1981, so far existing more than 60 countries sell, the pharmaceutical preparation of the acyclovir gone on the market has conventional tablet, injection, emulsifiable paste, capsule, granule, eye drop, chewable tablet etc., wherein acyclovir chewable tablet supplementary product kind and quantity more, generally to use filler, lubricant, disintegrating agent, adhesive, correctives etc., and at least will use 4 kinds of adjuvants.Increasing research shows that impurity in the incompatibility of the toxic and side effects of adjuvant itself, adjuvant and principal agent, adjuvant etc. all can have an impact to the safety of medicine.
Therefore, select suitable adjuvant and technique, reduce supplementary product kind and the consumption of acyclovir chewable tablet, improve bioavailability and the stability of acyclovir chewable tablet, for ensureing that the safety of clinical application has positive effect.
Starch is polymerized by glucose molecule, it is the basic adjuvant of oral solid formulation, be usually used in chewable tablet, making adhesive, diluent and disintegrating agent, and starch all extracts from the natural materials such as Semen Maydis, Maninot esculenta crantz., safe and reliable, cheap and easy to get, but being used alone starch has no report as adjuvant for the production of chewable tablet.
Summary of the invention
Technical problem to be solved by this invention is the defect overcoming prior art, and propose a kind of Acyclovir composition chewable tablet and preparation method thereof further, said preparation adjuvant is few, good stability, and bioavailability is high.
Technical problem to be solved by this invention realizes by the following technical solutions:
A kind of Acyclovir composition chewable tablet, comprise acyclovir, starch, sucrose, this tablet overcomes the shortcoming of above-mentioned common chewable tablet, decrease supplementary product kind and consumption in acyclovir chewable tablet, this pharmaceutical preparation function admirable, bioavailability is high, have good stability, patient acceptance is high, without sand type, has important clinical value.
A kind of Acyclovir composition chewable tablet, is prepared from by following raw material:
A preparation method for Acyclovir composition chewable tablet, comprises step as follows:
A, take the starch of component amount, add a certain amount of purified water and stir, by pH adjusting agent, the pH value of solution is controlled between 4 ~ 9, be then heated to 72 DEG C, be incubated 120 minutes, make the gelatinizing corn starch solution of 5 ~ 15% (W/V);
B, measure purified water 45ml, boil, add 85g sucrose, stir, after dissolving, continue to be heated to 100 DEG C, filter with purified cotton, the appropriate hot distilled water of filter is cleaned, and washing liquid and filtrate merge, and let cool, add appropriate distilled water, make full dose become 100m L, stir evenly, obtain B solution;
The solution that C, the medicinal liquid and the step B that steps A are obtained obtain mixes, and fully stirs 30 minutes, after medicinal liquid be down to room temperature obtain gelatinizing Semen Maydis-sucrose system medicinal liquid;
D, to take acyclovir 50g gram (by 1000 calculations), add 1L gelatinizing Semen Maydis-sucrose system medicinal liquid, stir 25 ~ 35 minutes;
E, the medicinal liquid sampling and measuring acyclovir content obtained step D, control with sodium hydroxide or hydrochloric acid between 5.0 ~ 7.0 by pH value;
After acyclovir content measured by F, medicinal liquid, be sub-packed in drug-containing dish by loading amount by medicinal liquid, each drug-containing dish fills about 1.0ml, then utilizes drug-containing dish lid malcompression state to cover drug-containing dish, and drug-containing dish is the cylindric medicine carrying packaging that plastics or other materials are made;
G, the drug-containing dish that medicinal liquid is housed is put into freeze drying box, be cooled to subzero 45 DEG C, keep 2 hours, evacuation, then 0 DEG C is warming up to gradually, keep 2 hours, then be cooled to subzero 45 DEG C, keep 2 hours, be warming up to 0 DEG C gradually again, keep 2 ~ 4 hours, then be warming up to 28 ~ 32 DEG C of dryings 4 ~ 6 hours gradually, whole process vacuum remains on below 10 handkerchiefs; Finally the drug-containing dish lid of powder charge is covered tightly, and load aluminium foil bag and carry out sealing and obtain acyclovir chewable tablet.
The preparation method of a kind of acyclovir chewable tablet of the present invention, in described steps A, pH adjusting agent is sodium hydroxide or hydrochloric acid, preferably controls 6.5 by the pH value of solution; Mixing time preferably 30 minutes in step C; In step D, pH value preferably controls 6.0, is preferably warming up to 0 DEG C gradually again in step F, keeps 3 hours, then is warming up to 30 DEG C of dryings 5 hours gradually; Described starch selects corn starch.
Beneficial effect of the present invention is:
A kind of Acyclovir composition chewable tablet provided by the invention and preparation method thereof, it adopts unique processing step, special process process is carried out to common corn starch, the bonding of starch in chewable tablet, disintegration can be improved, improve the molding of chewable tablet.And dosage of sucrose is 8.5% (W/V) in acyclovir chewable tablet, it is the hardness reinforcer of this tablet, and plays flavored action.Acyclovir chewable tablet only needs starch and sucrose two kinds of adjuvants, reduces the kind of required adjuvant; Because the technique of two liters falls in freeze-dry process employing two, twice cooling, twice intensification can make chewable tablet mouldability better, and improve stability and the dissolution of product, improve quality and the bioavailability of product.Therefore the preparation method of a kind of acyclovir chewable tablet provided by the invention has easy to operate, and prescription is simple, and technique is unique, the feature that product stability, safety are high.
Accompanying drawing explanation
Fig. 1 is the dissolution correlation curve figure of acyclovir in experiment.
Detailed description of the invention
The technological means realized to make the present invention, creation characteristic, reaching object and effect is easy to understand, below in conjunction with specific embodiment, set forth the present invention further, but following embodiment being only the preferred embodiments of the present invention, and not all.Based on the embodiment in embodiment, those skilled in the art under the prerequisite not making creative work obtain other embodiment, all belong to the protection domain of this patent.
Acyclovir content is for 50mg/ sheet.
Embodiment 1
Prescription: 1000 amounts
A, take the corn starch of 100g, the purified water adding 900ml stirs, and controls 6.5, is then heated to 72 DEG C, keep 120 minutes, make the gelatinizing corn starch solution of about 10% (W/V) by pH adjusting agent by the pH value of solution.
B, measure purified water 45ml, boil, add 85g sucrose, stir, after dissolving, continue to be heated to 100 DEG C, filter with purified cotton, the appropriate hot distilled water of filter is cleaned, and washing liquid and filtrate merge, and let cool, add appropriate distilled water, make full dose become 100m L, stir evenly, obtain B solution.
The solution that C, the medicinal liquid and the step B that steps A are obtained obtain mixes, and fully stirs 30 minutes, after medicinal liquid be down to room temperature obtain gelatinizing Semen Maydis-sucrose system medicinal liquid.
D, take acyclovir 50g (by 1000 calculations), add 1L gelatinizing Semen Maydis-sucrose system medicinal liquid, stir 30 minutes.
E, the medicinal liquid sampling and measuring acyclovir content obtained step D, control pH value 6.0 with sodium hydroxide or hydrochloric acid.
After acyclovir content measured by F, medicinal liquid, be sub-packed in drug-containing dish by loading amount by medicinal liquid, each drug-containing dish fills about 1.0m l, then utilizes drug-containing dish lid malcompression state to cover drug-containing dish, and drug-containing dish is the cylindric medicine carrying packaging that plastics or other materials are made.
G, the drug-containing dish that medicinal liquid is housed is put into freeze drying box, be cooled to subzero 45 DEG C, keep 2 hours, evacuation, then 0 DEG C is warming up to gradually, keep 2 hours, be cooled to subzero 45 DEG C, keep 2 hours, be warming up to 0 DEG C gradually again, keep 3 hours, then be warming up to 30 DEG C of dryings 5 hours gradually, whole process vacuum remains on below 10 handkerchiefs.Finally the drug-containing dish lid of powder charge is covered tightly, and load aluminium foil bag and carry out sealing and obtain a kind of acyclovir chewable tablet.
Embodiment 2
Prescription: 1000 amounts
A, take the corn starch of 150g, the purified water adding 900m l stirs, and controls 6.5, is then heated to 72 DEG C, keep 120 minutes, make the gelatinizing corn starch solution of about 5 ~ 15% (W/V) by pH adjusting agent by the pH value of solution.
B, measure purified water 45ml, boil, add 85g sucrose, stir, after dissolving, continue to be heated to 100 DEG C, filter with purified cotton, the appropriate hot distilled water of filter is cleaned, and washing liquid and filtrate merge, and let cool, add appropriate distilled water, make full dose become 100m L, stir evenly, obtain B solution.
The solution that C, the medicinal liquid and the step B that steps A are obtained obtain mixes, and fully stirs 30 minutes, after medicinal liquid be down to room temperature obtain gelatinizing Semen Maydis-sucrose system medicinal liquid.
D, take acyclovir 50g (by 1000 calculations), add 1L gelatinizing Semen Maydis-sucrose system medicinal liquid, stir 30 minutes.
E, the medicinal liquid sampling and measuring acyclovir content obtained step D, control pH value 6.0 with sodium hydroxide or hydrochloric acid.
After acyclovir content measured by F, medicinal liquid, be sub-packed in drug-containing dish by loading amount by medicinal liquid, each drug-containing dish fills about 1.0ml, then utilizes drug-containing dish lid malcompression state to cover drug-containing dish, and drug-containing dish is the cylindric medicine carrying packaging that plastics or other materials are made.
G, the drug-containing dish that medicinal liquid is housed is put into freeze drying box, be cooled to subzero 45 DEG C, keep 2 hours, evacuation, then 0 DEG C is warming up to gradually, keep 2 hours, be cooled to subzero 45 DEG C, keep 2 hours, be warming up to 0 DEG C gradually again, keep 3 hours, then be warming up to 30 DEG C of dryings 5 hours gradually, whole process vacuum remains on below 10 handkerchiefs.Finally the drug-containing dish lid of powder charge is covered tightly, and load aluminium foil bag and carry out sealing and obtain a kind of acyclovir chewable tablet.
Experimental data
A kind of Acyclovir composition chewable tablet that above-described embodiment is obtained carries out following quality research test:
1, hardness, friability, mouthfeel contrast test
The acyclovir chewable tablet prepared according to above-described embodiment and commercially available acyclovir chewable tablet (commercially available) detect friability and hardness by " Chinese Pharmacopoeia " version in 2010 two annex X G inspection techniques, contrast, the results are shown in following table:
| Sample | Hardness (N) | Friability | Mouthfeel |
| Embodiment 1 | 64 | <1％ | Without grains of sand sense, crisp |
| Embodiment 2 | 62 | <1％ | Without grains of sand sense, crisp |
| Ordinary tablet | 70 | <1％ | There is grains of sand sense, more firmly |
Experimental data shows, the more commercially available acyclovir chewable tablet of acyclovir chewable tablet without significant difference, meets " Chinese Pharmacopoeia " version in 2010 to the requirement of chewable tablet, and mouthfeel is greatly improved, make it the demand more meeting patient on friability and hardness.
2, dissolution contrast test
(No. 1 to No. 3 is embodiment 1 to get acyclovir chewable tablet (commercially available) and acyclovir chewable tablet respectively, No. 4 to No. 6 is embodiment 2) each 6, respectively according to dissolution method (" Chinese Pharmacopoeia " version in 2010 two annex X C second methods), with acetate buffer pH 6.0 solution 900ml for dissolution medium, rotating speed is 100r/min, operates in accordance with the law.
Sample respectively at 5min, 10min, 15min, 25min, 40min, 60min, get dissolution fluid appropriate, filter, get subsequent filtrate, according to " Chinese Pharmacopoeia " version in 2010 two annex IV A ultraviolet spectrophotometrys, under 260nm wavelength, measure its absorbance; Another precision takes acyclovir reference substance and is about 10mg, puts in 25mL measuring bottle, and add stripping medium dissolves and be diluted to scale, shaking up, precision measures 2mL, puts in 100mL measuring bottle, adds stripping medium to scale, shakes up, be measured in the same method, calculate the stripping quantity of every sheet.Calculate every sheet stripping quantity, investigate stripping curve, result is as follows.
Acyclovir chewable tablet (No. 1 to No. 3 is embodiment 1, and No. 4 to No. 6 is embodiment 2)
Acyclovir chewable tablet (commercially available)
Respectively with catch cropping Dissolution profiles during average dissolution pair as Fig. 1.
As stated above to the acyclovir chewable tablet comparative determination of acyclovir chewable tablet of the present invention and commercial reference preparation, the dissolution of acyclovir chewable tablet of the present invention when 15min (87.4%) is suitable with acyclovir chewable tablet (commercially available) dissolution when 60min (87.7%), and the dissolution of acyclovir chewable tablet of the present invention when 60min (96.1%) comparatively acyclovir chewable tablet (commercially available) dissolution when 60min (87.7%) is higher, comparatively acyclovir chewable tablet (commercially available) dissolution time is shorter to show acyclovir chewable tablet of the present invention, dissolution is higher, further show that acyclovir chewable tablet bioavailability of the present invention is better than acyclovir chewable tablet (commercially available).
2, stability study
Sample source: self-control
Sample lot number: 20140701 (embodiments 1), 20140702 (embodiments 2)
Investigation project: character, content, related substance, hardness, dissolution
Investigation method: according to " Chinese Pharmacopoeia " version in 2010 two annex XIXC crude drug and pharmaceutical preparation stability test guideline, investigate the accelerated stability (January, February, March, June) of this product and long-time stability (March, June, JIUYUE, December), result of the test is as following table:
As can be seen from the above table, in acceleration 6 months, all there is not significant change in long-term 12 months, show that this product has good stability in acyclovir chewable tablet indices of the present invention.
More than show and describe ultimate principle of the present invention, principal character and advantage of the present invention.The technical staff of the industry should understand; the present invention is not restricted to the described embodiments; what describe in above-described embodiment and description is only preference of the present invention; be not used for limiting the present invention; without departing from the spirit and scope of the present invention; the present invention also has various changes and modifications, and these changes and improvements all fall in the claimed scope of the invention.Application claims protection domain is defined by appending claims and equivalent thereof.
Claims (2)
1. an Acyclovir composition chewable tablet, is characterized in that, is prepared from by following raw material:
2. a preparation method for Acyclovir composition chewable tablet according to claim 1, is characterized in that: comprise step as follows:
A, take the starch of component amount, add a certain amount of purified water and stir, by pH adjusting agent, the pH value of solution is controlled between 4 ~ 7, be then heated to 72 DEG C, be incubated 120 minutes, make the gelatinizing corn starch solution of 5 ~ 15% (W/V);
B, measure purified water 45ml, boil, add 85g sucrose, stir, after dissolving, continue to be heated to 100 DEG C, filter with purified cotton, the appropriate hot distilled water of filter is cleaned, and washing liquid and filtrate merge, and let cool, add appropriate distilled water, make full dose become 100ml, stir evenly, obtain B solution;
The solution that C, the medicinal liquid and the step B that steps A are obtained obtain mixes, and fully stirs 30 minutes, after medicinal liquid be down to room temperature obtain gelatinizing Semen Maydis-sucrose system medicinal liquid;
D, take acyclovir 50g (by 1000 calculations), add 1L gelatinizing Semen Maydis-sucrose system medicinal liquid, stir 25 ~ 35 minutes;
E, the medicinal liquid sampling and measuring acyclovir content that step D is obtained;
After acyclovir content measured by F, medicinal liquid, be sub-packed in drug-containing dish by loading amount by medicinal liquid, each drug-containing dish fills about 1.0ml, then utilizes drug-containing dish lid malcompression state to cover drug-containing dish, and drug-containing dish is the cylindric medicine carrying packaging that plastics or other materials are made;
G, the drug-containing dish that medicinal liquid is housed is put into freeze drying box, be cooled to subzero 45 DEG C, keep 2 hours, evacuation, then 0 DEG C is warming up to gradually, keep 2 hours, then be cooled to subzero 45 DEG C, keep 2 hours, be warming up to 0 DEG C gradually again, keep 2 ~ 4 hours, then be warming up to 28 ~ 32 DEG C of dryings 4 ~ 6 hours gradually, whole process vacuum remains on below 10 handkerchiefs; Finally the drug-containing dish lid of powder charge is covered tightly, and load aluminium foil bag and carry out sealing and obtain Acyclovir composition chewable tablet.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410735482.5A CN104523611A (en) | 2014-12-05 | 2014-12-05 | Acyclovir composition chewable tablet and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410735482.5A CN104523611A (en) | 2014-12-05 | 2014-12-05 | Acyclovir composition chewable tablet and preparation method thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN104523611A true CN104523611A (en) | 2015-04-22 |
Family
ID=52839373
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201410735482.5A Pending CN104523611A (en) | 2014-12-05 | 2014-12-05 | Acyclovir composition chewable tablet and preparation method thereof |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN104523611A (en) |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1286629A (en) * | 1997-12-29 | 2001-03-07 | 宝洁公司 | Tablet composition |
| CN102204887A (en) * | 2011-06-09 | 2011-10-05 | 浙江浙北药业有限公司 | In-situ formed acyclovir spraying agent and preparation method thereof |
-
2014
- 2014-12-05 CN CN201410735482.5A patent/CN104523611A/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1286629A (en) * | 1997-12-29 | 2001-03-07 | 宝洁公司 | Tablet composition |
| CN102204887A (en) * | 2011-06-09 | 2011-10-05 | 浙江浙北药业有限公司 | In-situ formed acyclovir spraying agent and preparation method thereof |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CN104490925A (en) | Vitamin D calcium composition chewable tablets and preparation method thereof | |
| CN104434972A (en) | Calcium hydrophosphate composite chewable tablet and preparation method thereof | |
| CN104490814A (en) | Zinc gluconate composition chewable tablets and preparation method thereof | |
| CN104523611A (en) | Acyclovir composition chewable tablet and preparation method thereof | |
| CN104490924A (en) | Sucralfate composition chewable tablets and preparation method thereof | |
| CN104490813A (en) | Dextromethorphan hydrobromide composition chewable tablets and preparation method thereof | |
| CN104490811A (en) | Aspirin composition chewable tablet and preparation method thereof | |
| CN104490807A (en) | Ambroxol hydrochloride composition chewable tablet and preparation method thereof | |
| CN104434834A (en) | Mebendazole composition chewable tablet and preparation method thereof | |
| CN104490819A (en) | Loratadine composition chewable tablets and preparation method thereof | |
| CN104523613A (en) | Montelukast sodium composition chewable tablet and preparation method thereof | |
| CN104490805A (en) | Simvastatin composition chewable tablets and preparation method thereof | |
| CN104490820A (en) | Gentamicin sulfate composition chewable tablets and preparation method thereof | |
| CN104490816A (en) | Chewable tablet prepared from ferrous fumarate composition and preparation method thereof | |
| CN104490804A (en) | Cimetidine composition chewable tablets and preparation method thereof | |
| CN104490806A (en) | Vitamin C composition chewable tablets and preparation method thereof | |
| CN104490926A (en) | Calcium carbonate composition chewable tablet and preparation method thereof | |
| CN104490826A (en) | Albendazole composition chewable tablet and preparation method thereof | |
| CN104523612A (en) | Calcium lactate composition chewable tablet and preparation method thereof | |
| CN104546766A (en) | Mercaptopurine composition freeze-drying tablet and preparation method thereof | |
| CN104490808A (en) | Cefixime composition chewable tablets and preparation method thereof | |
| CN104434830A (en) | Erythromycin ethylsuccinate chewable tablet and preparation method thereof | |
| CN104490818A (en) | Famotidine composition chewable tablet and preparation method thereof | |
| CN104473890A (en) | Fenofibrate composition chewable tablet and preparation method thereof | |
| CN104490753A (en) | Furosemide composition freeze-dried tablet and preparation method thereof |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C02 | Deemed withdrawal of patent application after publication (patent law 2001) | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20150422 |