TW201431561A - The enteric capsule with oil coating - Google Patents

The enteric capsule with oil coating Download PDF

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Publication number
TW201431561A
TW201431561A TW102105059A TW102105059A TW201431561A TW 201431561 A TW201431561 A TW 201431561A TW 102105059 A TW102105059 A TW 102105059A TW 102105059 A TW102105059 A TW 102105059A TW 201431561 A TW201431561 A TW 201431561A
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Taiwan
Prior art keywords
ester
capsule
oil film
dosage form
content
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TW102105059A
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Chinese (zh)
Inventor
Wei-Chih Chang
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Wei-Chih Chang
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Priority to TW102105059A priority Critical patent/TW201431561A/en
Publication of TW201431561A publication Critical patent/TW201431561A/en

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Abstract

In this enteric capsule with oil coating, powdered or garrulous contents meant to fill the capsule is mixed with a dose of ester containing sesaminol triglucosides or coixenolide. With the feature that emulsification arises while ester containing Sesaminol Triglucosides or coixenolide is integrated with the bile in human body, so that the activity of pharmacological molecules can be prevented, the pharmacological molecules of the contents is able to be coated by ester, forming carriers which are the ester oil film protecting the pharmacological activity of small molecules and ensuring that they can be transported to the small intestine. In this way, the capsule will prevent the pharmacological molecules of the contests from being decomposed by gastric acid when the capsule passes through it. Before entering the small intestine, with the emulsification brought about by the combination of ester oil film and bile, the pharmacological molecules of the contents can remain active for the optimum pharmacological activity after their entrance into the small intestine, decomposition, emulsification, and transportation into the blood. The absorptivity of the capsule will be enhanced when it is consumed. As a consequence, chances that the consumption of the capsule with pharmacological molecules causes the irritation of stomach will be effectively reduced, and stomach health will be protected.

Description

油膜包覆腸溶劑型 Oil film coated intestinal solvent type

本發明系關於一種油膜包覆腸溶劑型,尤指其一供藥分子劑型可活性進入小腸消化道分解乳化以達到最適化狀態與吸收率及得以減少刺激胃與保護胃健康之油膜包覆腸溶劑型。 The invention relates to an oil film coated enteric solvent type, in particular to a drug molecule dosage form which can be activated into the intestinal digestive tract to decompose and emulsify to achieve an optimal state and absorption rate and to reduce the oil film coating intestine which stimulates the stomach and protects the stomach health. Solvent type.

按,一般常見以膠囊包裏有藥品或健康食品之劑型,其作用在於攜帶方便與便於服用,然,被膠囊包裏之內容物在經由口服到人體之胃部後,胃酸會迅速將膠囊溶解,使內容物成分溶出,因此,習用之膠囊劑型,在進入人體胃部中除易刺激胃部而傷胃外,更會因被胃酸裂解、破壞且崩解時間偏長,吸收效率未達最適化狀態,而無法完全釋放出來進入消化道分解,故在腸道之吸收率就會降低,導致成分到達小腸被人體吸收之比例不高且難完全確保其活性與吸收效果,實有改善之必要。 According to the general prescription, there is a pharmaceutical or health food dosage form in the capsule, which is convenient to carry and easy to take. However, after being orally administered to the stomach of the human body, the stomach acid will quickly dissolve the capsule. In order to dissolve the contents of the contents, the capsule type which is conventionally used, in addition to easily irritating the stomach and injuring the stomach, is more likely to be cracked and destroyed by gastric acid and has a long disintegration time, and the absorption efficiency is not optimal. The state of the disease, but can not be completely released into the digestive tract decomposition, so the absorption rate in the intestine will be reduced, resulting in the proportion of ingredients reaching the small intestine absorbed by the body is not high and it is difficult to fully ensure its activity and absorption effect, it is necessary to improve .

有鑑於此,本發明人係憑藉著長期對於相關產業之研究及融會貫通之構思意念,遂以多年的經驗加以設計,經多方探討並試作樣品試驗,乃推出本發明。 In view of this, the present inventors have developed the present invention by virtue of long-term research and integration of relevant industries, and have been designed with many years of experience, and have been explored and tested for sample testing.

本發明之主要目的,乃在提供一種油膜包覆腸溶劑型,其利用取有芝麻木質酚(芝麻素)或薏苡酯之酯質物將其劑型內容物為粉狀或粒狀之藥物分子包覆形成載體供保護小分子藥活性輸送至小腸之酯質油膜層設計,俾使劑型通過胃酸崩解殼層後可保有內容物之藥物活性不被胃酸分解而進入小腸前之酯質油膜層與膽汁結合乳化後,從中之內容物得以保其活性狀態並瞬間釋放直達小腸有效吸收,令內容物之藥物分子可活性進入小腸消化道分解乳化後輸出人體血液中而達到最適化之狀態與提升吸收之效 率,減少刺激胃部與保護胃部健康,藉此以提供胃潰瘍病患有良好之服用方式與達到提升劑型食用之吸收率為目的者。 The main object of the present invention is to provide an oil film-coated enteric solvent type which is coated with a drug substance having a dosage form of powdered or granular form using an ester substance of sesame lignan (sesol) or decyl ester. The carrier is formed to protect the small molecule drug from being transported to the small intestine of the ester oil film layer, so that the dosage form can prevent the drug activity of the content from being decomposed by gastric acid into the small intestine before the small intestine and the bile by the gastric acid disintegrating the shell layer. After the combination of emulsification, the content from the contents can be kept in an active state and instantly released to the small intestine for effective absorption, so that the drug molecules of the content can enter the intestinal digestive tract, decompose and emulsifie, and then output into the human blood to achieve an optimal state and enhance absorption. effect Rate, reduce the stimulation of the stomach and protect the health of the stomach, in order to provide a good way to take gastric ulcer disease and achieve the absorption rate of the enhanced dosage form.

10‧‧‧劑型 10‧‧‧ dosage form

11‧‧‧殼層 11‧‧‧ shell

12‧‧‧內容物 12‧‧‧ contents

121‧‧‧藥物分子 121‧‧‧ drug molecules

122‧‧‧酯質油膜層 122‧‧‧ester oil film

13‧‧‧核心空間 13‧‧‧ core space

第1圖係本創作之製作流程圖。 The first picture is the production flow chart of this creation.

第2圖係本創作之組合立體圖。 Figure 2 is a combined perspective view of the creation.

第3圖係本創作之組合剖面圖。 Figure 3 is a combined sectional view of the creation.

第4圖係本創作之藥物分子剖視放大圖。 Figure 4 is an enlarged cross-sectional view of the drug molecule of the present invention.

茲配合圖式將列舉出較佳之實施例,詳細說明本發明之內容如下:請參閱第1~4圖所示,本發明係提供一種油膜包覆腸溶劑型(10),其係取一劑量含有芝麻木質酚(芝麻素)或薏苡酯之酯質物,將一預備填充於劑型(10)內為粉末或顆粒物質之內容物(12,可設藥品或健康食品)與該酯質物相混溶,藉由酯質物含有芝麻木質酚(芝麻素)或薏苡酯之酯質因子可與人體膽汁結合而乳化並保其內容物(12)藥物分子活性之特性,令內容物(12)之藥物分子(121)受酯質物包覆形成載體供保護小分子藥活性輸送至小腸之酯質油膜層(122),其上所述之內容物(12)亦可設為三帖類和多醣體,該三帖類和多醣體係由芝麻木質酚與牛樟或由芝麻素與薏苡酯以超臨界二氧化碳萃取出,該劑型(10)亦可為膠囊而包含有一殼層(11)及一核心空間(13),於核心空間(13)內填充上述之內容物(12),而藉由含有芝麻木質酚(芝麻素)或薏苡酯之酯質物包覆其藥物分子(121)所形成之酯質油膜層(122)與人體膽汁結合而乳化以供包裏於核心空間(13)內之內容物(12)保持活性之特性,當本創作之膠囊劑型(10)包裏其內容物(12,如三帖類和多醣體)經由口服到人體之胃部後,利用酯質物包覆藥物分子(121)所構成酯質油膜防護膜之酯質油膜層(122),俾使劑型(10)通過胃酸崩解殼層(11)後可達到內容物(12)之藥物分子(121)可保其活性狀態並具有加乘效果而不被 胃酸分解,且進入小腸前之酯質油膜層(122)與膽汁結合乳化後,從中之內容物(12)得以保其活性狀態並瞬間釋放直達小腸有效吸收,令藥物分子(121)進入小腸消化道分解乳化後輸出人體血液中而達到最適化之狀態與提升吸收之效率,改善膠囊之內容物(12)易受胃酸裂解破壞之現像,藉此,令其劑型食用上可減少刺激胃部與保護胃部健康,達到提供胃潰瘍病患有良好之服用方式,且達到提升藥分子劑型食用之吸收率(等同於注射劑量)為目的者。 DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENT A preferred embodiment will be described in detail with reference to the following detailed description of the present invention. Referring to Figures 1 to 4, the present invention provides an oil film coated enteric solvent type (10) which is dosed. An ester containing sesame lignan (sesol) or decyl ester, and a content of the powder or granule substance (12, which can be used as a medicine or a health food) which is prepared to be filled in the dosage form (10) is miscible with the ester substance. By using an ester substance containing sesame lignan (sesol) or an ester of an oxime ester to bind to human bile and emulsifying and retaining the content of the drug (12), the drug molecule of the content (12) (121) being coated with an ester substance to form a carrier for protecting the small molecule drug from being transported to the ester oil film layer (122) of the small intestine, and the content (12) described above may also be set as a triplet and a polysaccharide. The three-type and polysaccharide system is extracted from sesame lignan and burdock or by sesamin and decyl ester by supercritical carbon dioxide. The dosage form (10) may also be a capsule and comprises a shell layer (11) and a core space (13). ), filling the above content (12) in the core space (13), and by containing the zhi The esterified oil film layer (122) formed by the ester of lignan (sesol) or oxime ester coated with the drug molecule (121) is emulsified in combination with human bile for inclusion in the core space (13). The property (12) maintains the characteristics of activity. When the contents (12, such as three-posts and polysaccharides) of the capsule type (10) of the present invention are orally administered to the stomach of the human body, the drug substance is coated with the ester substance. (121) The ester oil film layer (122) constituting the ester oil film protective film, and the drug substance (121) which can reach the content (12) after the drug form (10) is disintegrated by the gastric acid (11) Its active state and has a multiplier effect without being The gastric acid is decomposed, and the ester oil film layer (122) before entering the small intestine is emulsified in combination with the bile, and the content (12) is preserved from the contents thereof and instantly released to the small intestine for effective absorption, so that the drug molecule (121) enters the small intestine for digestion. After decomposing and emulsification, it is exported to the human body to achieve the optimal state and improve the efficiency of absorption, and improve the content of the capsule (12) which is susceptible to decomposition by gastric acid lysis, thereby reducing the stimulation of the stomach and the dosage form. To protect the health of the stomach, to provide a good way to take gastric ulcer disease, and to achieve the absorption rate of the drug dosage form (equivalent to the injected dose).

綜上所述,當知本發明確實可為相關產業廣為利用,極具有進步性與新穎性,且本發明於申請前未見公開,已符合專利法之規定,爰依法提出發明專利申請,懇請 鈞局明察,惠准專利,實為感禱。 In summary, it is known that the present invention can be widely utilized by related industries, and is extremely progressive and novel, and the present invention has not been disclosed before the application, has complied with the provisions of the Patent Law, and has filed an invention patent application according to law. I would like to ask the bureau to observe and benefit from patents.

惟以上所述者,僅為本發明之其中較佳實施例而已,當不能以之限定本發明實施之範圍;即大凡依本發明申請專利範圍所作之均等變化與修飾,皆應仍屬本發明專利涵蓋之範圍內。 The above is only the preferred embodiment of the present invention, and the scope of the present invention is not limited thereto; that is, the equivalent changes and modifications made by the scope of the present invention should still belong to the present invention. Within the scope of the patent.

10‧‧‧劑型 10‧‧‧ dosage form

11‧‧‧殼層 11‧‧‧ shell

12‧‧‧內容物 12‧‧‧ contents

121‧‧‧藥物分子 121‧‧‧ drug molecules

122‧‧‧酯質油膜層 122‧‧‧ester oil film

13‧‧‧核心空間 13‧‧‧ core space

Claims (4)

一種油膜包覆腸溶劑型,其係取一劑量含有芝麻木質酚(芝麻素)或薏苡酯之酯質物,將一預備填充於劑型內為粉末或顆粒物質之內容物與該酯質物相混溶,藉由酯質物含有芝麻木質酚(芝麻素)或薏苡酯之酯質因子可與人體膽汁結合而乳化並保其內容物藥物分子活性之特性,使內容物之藥物分子受酯質物包覆形成載體供保護小分子藥活性輸送至小腸之酯質油膜層,令劑型通過胃酸時,其包裏於劑型內之內容物可保其活性狀態並具有加乘效果而不被胃酸分解以進入小腸消化道分解乳化後輸出人體血液中,進而達到食用劑型可得最適化之狀態與提升劑型食用之吸收率。 An oil film coated enteric solvent type, which is obtained by taking a dose of an ester containing sesame lignan (sesol) or oxime ester, and mixing a content of a powder or a granular substance in a dosage form with the ester substance. The ester substance containing sesame lignan (sesol) or oxime ester can be emulsified by binding to human bile and retaining the characteristics of the drug molecule activity of the content, so that the drug molecule of the content is coated with the ester substance. The carrier is used for protecting the activity of the small molecule drug to the ester oil film layer of the small intestine, so that when the dosage form passes through the stomach acid, the content in the dosage form can maintain its active state and have a multiplying effect without being decomposed by gastric acid to enter the small intestine for digestion. The road is decomposed and emulsified and exported to the human blood, thereby achieving the optimum state of the edible dosage form and the absorption rate of the enhanced dosage form. 如請求項1所述之油膜包覆腸溶劑型,其中劑型係可為膠囊而包含有一殼層及一填充有上述內容物之核心空間。 The oil film according to claim 1 is coated with an enteric solvent type, wherein the dosage form is a capsule and comprises a shell layer and a core space filled with the above contents. 如請求項1所述之油膜包覆腸溶劑型,其中內容物係可設為粉未或顆粒物質之藥品或健康食品。 The oil film according to claim 1 is coated with an enteric solvent type, wherein the content is a medicine or a health food which is a powder or a particulate matter. 如請求項3所述之油膜包覆腸溶劑型,其中內容物係可設為三帖類和多醣體,該三帖類和多醣體係由芝麻木質酚與牛樟或由芝麻素與薏苡酯以超臨界二氧化碳萃取出。 The oil film according to claim 3 is coated with an enteric solvent type, wherein the content system can be set as three kinds of polysaccharides and polysaccharides, and the three types of polysaccharides and polysaccharides are composed of sesame lignan and burdock or by sesamin and decyl ester. Supercritical carbon dioxide is extracted.
TW102105059A 2013-02-08 2013-02-08 The enteric capsule with oil coating TW201431561A (en)

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Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2016109856A1 (en) 2015-01-02 2016-07-07 Melaleuca, Inc. Multi-supplement compositions
WO2016109852A2 (en) 2015-01-02 2016-07-07 Melaleuca, Inc. Bacterial compositions
US10137164B2 (en) 2015-01-02 2018-11-27 Melaleuca, Inc. Dietary supplement compositions

Cited By (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2016109856A1 (en) 2015-01-02 2016-07-07 Melaleuca, Inc. Multi-supplement compositions
WO2016109852A2 (en) 2015-01-02 2016-07-07 Melaleuca, Inc. Bacterial compositions
US10137164B2 (en) 2015-01-02 2018-11-27 Melaleuca, Inc. Dietary supplement compositions
US10576112B2 (en) 2015-01-02 2020-03-03 Melaleuca, Inc. Bacterial compositions
US11207388B2 (en) 2015-01-02 2021-12-28 Melaleuca, Inc. Multi-supplement compositions
US11273195B2 (en) 2015-01-02 2022-03-15 Melaleuca, Inc. Dietary supplement compositions
EP3973972A1 (en) 2015-01-02 2022-03-30 Melaleuca, Inc. Multi-supplement compositions
EP4019028A1 (en) 2015-01-02 2022-06-29 Melaleuca, Inc. Bacterial compositions
US11433107B2 (en) 2015-01-02 2022-09-06 Melaleuca, Inc. Bacterial compositions

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