JPH072638B2 - Preparation for oral administration - Google Patents
Preparation for oral administrationInfo
- Publication number
- JPH072638B2 JPH072638B2 JP17576186A JP17576186A JPH072638B2 JP H072638 B2 JPH072638 B2 JP H072638B2 JP 17576186 A JP17576186 A JP 17576186A JP 17576186 A JP17576186 A JP 17576186A JP H072638 B2 JPH072638 B2 JP H072638B2
- Authority
- JP
- Japan
- Prior art keywords
- preparation
- weight
- present
- oral administration
- pana
- 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.)
- Expired - Lifetime
Links
Landscapes
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Description
【発明の詳細な説明】 〔産業上の利用分野〕 本発明は経口投与用製剤に関する。DETAILED DESCRIPTION OF THE INVENTION [Field of Industrial Application] The present invention relates to a preparation for oral administration.
薬物の生体吸収性を製剤的に改善する方法としては結晶
の微細化、界面活性剤の併用などが知られている。As a method for improving the bioabsorbability of a drug in a pharmaceutical form, it is known to make crystals finer and to use a surfactant together.
しかし、キノキサリン系合成抗菌剤又はジテルペン系抗
生物質の吸収性を改善する方法は知られていない。However, there is no known method for improving the absorbability of quinoxaline synthetic antibacterial agents or diterpene antibiotics.
〔問題点を解決のための手段〕 そこで本発明者らは種々検討した結果キノキサリン系合
成抗菌剤又は、ジテルペン系抗生物質１重量部に対し0.
01〜80重量部のポリアクリル酸ナトリウム（以下「PAN
a」という）を添加するとキノキサリン系合成抗菌剤又
はジテルペン系抗生物質の体内吸収性が大幅に向上する
ことを見い出した。[Means for Solving Problems] Therefore, the present inventors have conducted various studies, and as a result, the quinoxaline-based synthetic antibacterial agent or the diterpene-based antibiotic is 0.
01 to 80 parts by weight of sodium polyacrylate (hereinafter referred to as "PAN
It was found that the absorption of a quinoxaline-based synthetic antibacterial agent or a diterpene-based antibiotic is significantly improved by the addition of "a").
本発明は上記知見に基づいて完成されたものである。The present invention has been completed based on the above findings.
即ち、本発明は（ａ）キノキサリン系合成抗菌剤又はジ
テルペン系抗生物質製剤及び（ｂ）PANaを含有し、その
含量割合が（ａ）成分１重量部に対し（ｂ）成分が0.01
〜80重量部である経口投与製剤に関する 本発明で使用されるキノキサリン系合成抗菌剤又はジテ
ルペン系抗生物質としては例えば、オラキンドックス、
カルバドックス又はチアムリンがあげられる。That is, the present invention contains (a) a quinoxaline-based synthetic antibacterial agent or a diterpene-based antibiotic preparation and (b) PANa, and the content ratio is 0.01 parts of (b) component to 1 part by weight of (a) component.
Examples of the quinoxaline-based synthetic antibacterial agent or diterpene-based antibiotic used in the present invention relating to a formulation for oral administration, which is ˜80 parts by weight, include olaquindox,
Examples include carbadox or tiamulin.
本発明で使用するPANaは食品添加物、飼料添加物に指定
されているもので、その分子量は100万〜600万好ましく
は400〜500万程度のものがよい。The PANa used in the present invention is designated as a food additive and a feed additive, and its molecular weight is preferably 1,000,000 to 6,000,000, preferably about 4,000,000 to 5,000,000.
PANaとキノキサリン系合成抗菌剤又はジテルペン系抗生
物質の使用割合は該薬剤１重量部に対しPANa0.01〜80重
量部好ましくは0.1〜80重量部程度がよい。The proportion of PANa and quinoxaline-based synthetic antibacterial agent or diterpene-based antibiotic used is 0.01 to 80 parts by weight, preferably 0.1 to 80 parts by weight, of PANa per 1 part by weight of the drug.
又、製剤全体に対するPANaの量は0.1〜95w/w％、好まし
くは１〜95w/w％さらに好ましくは５〜90w/w％であり、
又、キノキサリン系合成抗菌剤又はジテルペン系抗生物
質の量は１〜99w/w％、好ましくは５〜99w/w％さらに好
ましくは10〜95w/w％程度である。Further, the amount of PANa with respect to the whole preparation is 0.1 to 95 w / w%, preferably 1 to 95 w / w%, more preferably 5 to 90 w / w%,
The amount of the quinoxaline-based synthetic antibacterial agent or diterpene-based antibiotic is 1 to 99 w / w%, preferably 5 to 99 w / w%, more preferably 10 to 95 w / w%.
本発明の製剤には賦形剤、増量剤などが含まれていても
よく、その量は製剤全量に対し０〜90w/w％、好ましく
は、10〜80w/w％程度である。本発明の製剤は、粉末
剤、散財、顆粒剤、錠剤などの形態で人または家畜に投
与されるが、家畜に投与する場合は散剤や粉末剤の形態
で、家畜に直接又は飼料に混合して投与される。The formulation of the present invention may contain an excipient, a filler and the like, and the amount thereof is 0 to 90 w / w%, preferably about 10 to 80 w / w% with respect to the total amount of the formulation. The preparation of the present invention is administered to humans or livestock in the form of powder, powder, granules, tablets, etc., but when administered to livestock, it is directly added to livestock or mixed with feed in the form of powder or powder. Administered.
次に本発明の製剤のすぐれた効果を実験例により説明す
る。Next, the excellent effect of the preparation of the present invention will be described with reference to experimental examples.
実験例 （１）試料 オラキンドックス4g（1,000mg力価/g）及び粒径48メッ
シュパスのPANa（分子量500万）16gを均一に混合した粉
末剤を試料とした。オラキンドックスを対照試料とし
た。チアムリン22.5g（20mg力価/g）及び粒径48メッシ
ュパスのPANa（分子量500万）18gを均一に混合した粉末
剤とした。チアムリンを対照試料とした。Experimental Example (1) Sample A powder agent in which 4 g of Olaquindox (1,000 mg titer / g) and 16 g of PANa (molecular weight 5 million) having a particle size of 48 mesh pass were uniformly mixed was used as a sample. Olaquindox served as a control sample. 22.5 g of tiamulin (20 mg titer / g) and 18 g of PANa (molecular weight 5 million) having a particle size of 48 mesh pass were uniformly mixed to obtain a powder. Tiamulin served as a control sample.
（２）実験方法 試験Ｉ 体重37.4〜47.4kgの子豚を試験動物とした。飼料は体重
の４％の試験前日まで給与し、当日は２％給与した。試
料はオラキンドックス10mg力価/kgとなるように、飼料
約100gに混合し５分以内に食べきったのを確認してから
残りの飼料を補給した。(2) Experimental method Test I Piglets weighing 37.4 to 47.4 kg were used as test animals. The feed was fed until the day before the test for 4% of the body weight, and 2% was fed on the day. The sample was mixed with about 100 g of the feed so that the olaquindox had a titer of 10 mg / kg, and it was confirmed that the sample had been eaten within 5 minutes, and then the rest of the feed was supplemented.
試料投与前及び投与後、1,2,4,8時間後に採血し、血清
中のオラキンドックスの量を高速液体クロマトグラフに
て測定した。Blood samples were collected before, 1, 2, 4 and 8 hours after the sample administration, and the amount of olaquindox in the serum was measured by high performance liquid chromatography.
試験II 体重41.0〜51.0kgの子豚を試験動物とした。飼料は体重
の４％を試験前日まで給与し、当日は２％給与した。試
料はチアムリン10mg力価/kgとなるように、飼料約100g
に混合し、５分以内に食べきったのを確認してから残り
の飼料を補給した。試料投与前及び投与後、1,2,4,8時
間後に採血し、血清中チアムリンの量を微生物定量法に
より定量した。Test II Piglets weighing 41.0 to 51.0 kg were used as test animals. For the feed, 4% of the body weight was fed until the day before the test, and 2% was fed on the day. Approximately 100 g of feed is used so that the sample has a titer of 10 mg titer / kg.
And mixed within 5 minutes, and after confirming that the food had been eaten, the rest of the feed was supplemented. Blood was collected before and 1, 2, 4, and 8 hours after the administration of the sample, and the amount of thiamulin in the serum was quantified by the microorganism quantification method.
（３）結果 試験Ｉの結果を表−１に、試験IIの結果を表−２に示
す。(3) Results The results of Test I are shown in Table-1, and the results of Test II are shown in Table-2.
この表から明らかなように対照品では、投与２時間後に
オラキンドックスの血中濃度がピークとなり、その量は
4.6μｇ力価/mlであった。これに対し、本発明では投与
１時間後にピークとなり、その量も9.3μｇ力価/mlと２
倍以上の血中濃度を示した。 As is clear from this table, in the control product, the blood concentration of olaquindox reached a peak 2 hours after administration, and the amount thereof was
It was 4.6 μg titer / ml. On the other hand, in the present invention, it peaked 1 hour after administration, and its amount was 9.3 μg titer / ml and 2
The blood concentration was more than doubled.
この表から明らかなように対照品では、投与２時間後に
チアムリンの血中濃度がピークになりその量は0.426μ
ｇ力価/mlであった。これに対し、本発明では投与１時
間にピークとなりその量も0.825μｇ液価/mlと2.5倍以
上の血中濃度を示した。 As is clear from this table, in the control product, the blood concentration of thiamulin peaked at 2 hours after administration and the amount was 0.426μ.
It was g titer / ml. On the other hand, in the present invention, it peaked 1 hour after administration, and the amount thereof was 0.825 μg liquid value / ml, which was 2.5 times or more the blood concentration.
従って、表−１、表−２に示したとおり本発明の製剤に
よると薬剤の生体吸収性を大幅に向上させることができ
る。Therefore, as shown in Tables 1 and 2, according to the formulation of the present invention, the bioabsorbability of the drug can be significantly improved.
次に実施例により本発明を具体的に説明する。Next, the present invention will be specifically described with reference to examples.
実施例1.粉末剤 粒度48メッシュパスのPANa（分子量500万）100gとオラ
キンドックス400g及び増量剤としてバレイショデンプン
を500g均一にＶ型混合機で混合し、粉末剤を得た。Example 1. Powder agent 100 g of PANa (molecular weight 5 million) having a particle size of 48 mesh, 400 g of olaquindox and 500 g of potato starch as an extender were uniformly mixed with a V-type mixer to obtain a powder agent.
実施例2. 粒度48メッシュパスのPANa（分子量500万）50gとチアム
リン500g及び増量剤としてバレイショデンプンを450g均
一にＶ型混合機で混合し、粉末剤を得た。Example 2 50 g of PANa (molecular weight 5,000,000) having a particle size of 48 mesh pass, 500 g of tiamulin and 450 g of potato starch as an extender were uniformly mixed in a V-type mixer to obtain a powder.
Claims (1)
ルペン系抗生物質製剤及び（ｂ）ポリアクリル酸ナトリ
ウムを含有し、その含量割合が（ａ）成分１重量部に対
し（ｂ）成分が0.01〜80重量部である経口投与製剤1. A composition comprising (a) a quinoxaline-based synthetic antibacterial agent or a diterpene-based antibiotic preparation and (b) sodium polyacrylate, the content ratio of which is 0.01 part of (b) component to 1 part by weight of (a) component. ~ 80 parts by weight for oral administration
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP17576186A JPH072638B2 (en) | 1986-07-28 | 1986-07-28 | Preparation for oral administration |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP17576186A JPH072638B2 (en) | 1986-07-28 | 1986-07-28 | Preparation for oral administration |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JPS6333330A JPS6333330A (en) | 1988-02-13 |
| JPH072638B2 true JPH072638B2 (en) | 1995-01-18 |
Family
ID=16001791
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP17576186A Expired - Lifetime JPH072638B2 (en) | 1986-07-28 | 1986-07-28 | Preparation for oral administration |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JPH072638B2 (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN114983944A (en) * | 2022-07-18 | 2022-09-02 | 山东国邦药业有限公司 | Preparation method of tiamulin fumarate soluble powder |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CO5390081A1 (en) | 2001-11-28 | 2004-04-30 | Novartis Ag | ORGANIC COMPOUNDS |
-
1986
- 1986-07-28 JP JP17576186A patent/JPH072638B2/en not_active Expired - Lifetime
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN114983944A (en) * | 2022-07-18 | 2022-09-02 | 山东国邦药业有限公司 | Preparation method of tiamulin fumarate soluble powder |
| CN114983944B (en) * | 2022-07-18 | 2022-10-28 | 山东国邦药业有限公司 | Preparation method of tiamulin fumarate soluble powder |
Also Published As
| Publication number | Publication date |
|---|---|
| JPS6333330A (en) | 1988-02-13 |
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