CN104721171A

CN104721171A - Terramycin enteric capsule

Info

Publication number: CN104721171A
Application number: CN201510155181.XA
Authority: CN
Inventors: 刘颖
Original assignee: Chengdu Hui Zhi Distant View Science And Technology Ltd
Current assignee: Chengdu Hui Zhi Distant View Science And Technology Ltd
Priority date: 2015-04-02
Filing date: 2015-04-02
Publication date: 2015-06-24

Abstract

The invention relates to a terramycin enteric capsule. The terramycin enteric capsule comprises an active ingredient of terramycin and also comprises a diluting agent, a lubricating agent, an adhesive, a disintegrating agent and an enteric coating material. The diluting agent is one or more of lactose, starch, microcrystalline cellulose and mannitol; the lubricating agent is one or more of talc powder, stearic acid, polyethylene glycol and micro powder silica gel; the adhesive is one or more of hydroxypropyl methylcellulose, povidone and dextrin; and the disintegrating agent is one or more of crosslinked sodium carboxymethylcellulose, crosslinked povidone and low-substituted hydroxypropyl cellulose. The enteric coating material is a composition of hydroxypropyl cellulose phthalate, ethyl cellulose and polyvinyl alcohol.

Description

A kind of oxytetracycline enteric coated capsule

Technical field

The application relates to a kind of enteric coated capsule, particularly, is oxytetracycline enteric coated capsule.

Background technology

Oxytetracycline (oxytetracycline) is the broad-spectrum antibiotic found in the culture fluid of actinomycetic be full of cracks Streptothrix (Streptomyces rimosus) by (1950) such as Finleys (A.C Finlay).Can various antibacterial, rickettsia and chlamydial growth be suppressed and be widely used in treatment.The mechanism of action of oxytetracycline is that medicine can be combined with the A position of bacterial ribosome 30S subunit specifically, suppresses the growth of peptide chain and affects the synthesis of bacterioprotein.Existing oxytetracycline preparation comprises tablet, capsule, ointment, eye ointment etc.Be used for the treatment of dysentery, trachoma, conjunctivitis, pneumonia, otitis media, scytitis etc., be also used for the treatment of ameba enteritis and intestinal infection.

Summary of the invention

The present invention, in order to solve the shortcoming of existing oxytetracycline preparation targeting difference, has invented oxytetracycline enteric coated capsule.

Applicant finds, oxytetracycline is prepared into enteric coated capsule in conjunction with specific adjuvant, has the advantage that stability is high, targeting is strong and bioavailability is high.

The application provides a kind of oxytetracycline enteric coated capsule, and wherein active component is oxytetracycline.

The application provides a kind of oxytetracycline enteric coated capsule, wherein also comprises diluent, lubricant, binding agent, disintegrating agent and enteric coating material.

The application provides a kind of enteric coated capsule of oxytetracycline, comprising:

In this application, described diluent be lactose, starch, microcrystalline Cellulose, mannitol one or more, lubricant be Pulvis Talci, stearic acid, Polyethylene Glycol, micropowder silica gel one or more, binding agent be hypromellose, polyvidone, dextrin one or more, disintegrating agent be cross-linking sodium carboxymethyl cellulose, polyvinylpolypyrrolidone, low-substituted hydroxypropyl cellulose one or more.

The inventive point of the application is the selection of enteric coating material, inventor is found by great many of experiments, a small amount of polyvinyl alcohol (PVA) is added in part by weight is the hydroxypropyl cellulose phthalate ester of 3:7-8 and the compositions of ethyl cellulose, pharmacy security can be made by stomach in intestinal disintegrate, there is extraordinary enteric effect, and significantly improve the stability of preparation.Preferably, the weight ratio of polyvinyl alcohol and hydroxypropyl cellulose phthalate ester and the compositions both ethyl cellulose is 1:15-17.

Experiment proves, not any pharmacy customary adjuvant is all applicable to preparing oxytetracycline enteric coated capsule, and the effect of oxytetracycline enteric coated capsule in targeting, stability, dissolution etc. selecting this specific adjuvant to prepare is better than the oxytetracycline enteric coated capsule that other adjuvants prepare far away.

Metering of the present invention is weight.

Preferably, the prescription of oxytetracycline enteric coated capsule is (by weight, part):

All the other adjuvants were pulverized 80 mesh sieves by the preparation method of enteric coated capsule: oxytetracycline was pulverized 100 mesh sieves; Accurately take the supplementary material of the recipe quantity except enteric coating material, mix homogeneously, add suitable quantity of water and mixture furnishing paste is granulated on granulator, 18 mesh sieve granulate, for subsequent use.By enteric coating material mix homogeneously, add suitable quantity of water furnishing enteric coating liquid.The granule prepared before is placed in coating pan, with nebulization, enteric coating liquid is evenly sprayed at particle surface.40-50 DEG C of drying, loads hungry area softgel shell by obtained granule.

Embodiment 1 prescription

Preparation method:

Oxytetracycline was pulverized 100 mesh sieves, all the other adjuvants were pulverized 80 mesh sieves, for subsequent use; Accurately take the supplementary material of the recipe quantity except hydroxypropyl cellulose phthalate ester, ethyl cellulose and polyvinyl alcohol, mix homogeneously, add suitable quantity of water and mixture furnishing paste is granulated on granulator, 18 mesh sieve granulate, for subsequent use.By the mixing of hydroxypropyl cellulose phthalate ester, ethyl cellulose and polyvinyl alcohol evenly, suitable quantity of water furnishing enteric coating liquid is added.The granule prepared before is placed in coating pan, with nebulization, enteric coating liquid is evenly sprayed at particle surface.40-50 DEG C of drying, loads hungry area softgel shell by obtained granule.

Embodiment 2 prescription

Preparation method is with embodiment 1.

Comparative example 1

Preparation method is with embodiment 1.

Comparative example 2

Preparation method is with embodiment 1.

Comparative example 3

Preparation method is with embodiment 1.

Comparative example 4

Preparation method is with embodiment 1.

Comparative example 5

Preparation method is with embodiment 1.

Comparative example 6

Preparation method is with embodiment 1.

Comparative example 7

Preparation method is with embodiment 1.

Comparative example 8

Preparation method is with embodiment 1.

Comparative example 9

Preparation method is with embodiment 1.

Comparative example 10

Preparation method is with embodiment 1.

In above-mentioned comparative example 1-10, just enteric coating material changes to some extent, and other supplementary materials are all identical with embodiment 1.The situation of change of following table 1. couples of comparative example 1-10 gathers as follows:

Table 1.

Different enteric coating material is on the impact of oxytetracycline enteric coated capsule

Test method: oxytetracycline enteric coated capsule embodiment 1,2 and comparative example 1-10 prepared measures release rate respectively in simulated gastric fluid environment and simulation intestinal environment.Assay method is with this area conventional method.The results are shown in Table 2.

Table 2.

As can be seen from table 2 data, embodiment 1 and embodiment 2 discharge hardly in gastric juice environment, can almost all strippings in intestinal environment, have extraordinary targeting.Although and the release rate difference of comparative example 1-10 in gastric juice environment and intestinal environment is also very large, relative to embodiment 1 and embodiment 2, in gastric juice environment, burst size is too many, differs tens times and even hundreds of times with embodiment 1 and embodiment 2.Table 2 data show to adopt oxytetracycline enteric coated capsule of the present invention to use specific enteric coating material (compositions of hydroxypropyl cellulose phthalate ester, ethyl cellulose and polyvinyl alcohol), be enteric coating material or consumption proportion be all specific, change one and namely greatly can reduce targeting.

Oxytetracycline enteric coated capsule stability test

Factors influencing has been carried out to the outward appearance of the granule in the enteric coated capsule of embodiment 1,2 and comparative example 1-10, oxytetracycline content and related substance.

(1) hot test: the granule in Example 1,2 and comparative example 1-10 sample capsules is laid in culture dish in right amount, the calorstat being placed in 60 DEG C is placed 10 days, and in the 0th, 5,10 days this periods, taking sample determination respectively, measurement result was in table 3.

(2) high wet test: the granule in sample thief capsule is laid in culture dish in right amount, places 10 days under the condition of 25 DEG C of relative humidity RH90% ± 5%, and in the 0th, 5,10 days this periods, taking sample determination respectively, measurement result was in table 3.

(3) strong illumination test, the granule in sample thief capsule is laid in culture dish in right amount, is placed in the condition illumination 10 day of light cupboard at 4500Lx ± 500Lx, and in the 0th, 5,10 days this periods, taking sample determination respectively, measurement result was in table 3.

Particle high-temperature high humidity in each embodiment enteric coated capsule of table 3. and high light stability inferior

As can be seen from the experimental data of table 3, the stability of embodiment 1 and embodiment 2 is significantly better than comparative example 1-10, and the oxytetracycline enteric coated capsule that this explanation is obtained by specific enteric coating material has relative to the enteric coated capsule that other enteric materials obtain and obviously has different stability.

Claims

1. an oxytetracycline enteric coated capsule, wherein active component is oxytetracycline.

2. a kind of oxytetracycline enteric coated capsule as claimed in claim 1, wherein also comprises diluent, lubricant, binding agent, disintegrating agent and enteric coating material.

3. a kind of oxytetracycline enteric coated capsule as claimed in claim 2, comprising:

4. a kind of oxytetracycline enteric coated capsule as claimed in claim 3, wherein said diluent be lactose, starch, microcrystalline Cellulose, mannitol one or more, lubricant be Pulvis Talci, stearic acid, Polyethylene Glycol, micropowder silica gel one or more, binding agent be hypromellose, polyvidone, dextrin one or more, disintegrating agent be cross-linking sodium carboxymethyl cellulose, polyvinylpolypyrrolidone, low-substituted hydroxypropyl cellulose one or more.

5. a kind of oxytetracycline enteric coated capsule as described in one of Claims 2 or 3, wherein enteric coating material is the compositions of hydroxypropyl cellulose phthalate ester, ethyl cellulose and polyvinyl alcohol.

6. a kind of oxytetracycline enteric coated capsule as claimed in claim 5, wherein the weight ratio of the compositions of polyvinyl alcohol and hydroxypropyl cellulose phthalate ester, both ethyl celluloses is 1:15-17.