JPS5818317A - Soft capsule of highly unsaturated long-chain fatty acid - Google Patents

Abstract

PURPOSE:The titled pharmaceutical preparation storable for a long time, having extremely improved oxidative deterioration, good taste and fragrance, comprising a content liquid obtained by dissolving highly unsaturated long-chain fatty acid or its derivative in a middle-chain fatty acid triglyceride. CONSTITUTION:A higly unsaturated long-chain fatty acid (e.g., 5,8,11,14,17- eicosapentaenoic acid, etc.) or its derivative is dissolved in a middle-chain fatty acid triglyceride (MCT). The amount of MCT is an amount to make 0.01- 50wt% highly unsaturated long-chain fatty acid in the solution. The prepared solution is used as a content liquid, to give a soft capsule pharmaceutical preparation of highly unsaturated long-chain fatty acid. EFFECT:The titled capsule can be obtained by a conventional means without being subjected to a specific atmosphere and without using a specific device.

Description

DETAILED DESCRIPTION OF THE INVENTION The present invention relates to a soft capsule formulation of polyunsaturated fatty acid 117i acid 1 or its derivatives.

Nagahora advanced non-filling liquid Vj acid, e.g. 5.8.11゜141
117-Nicosapentaenoic acid (hereinafter abbreviated as 'JApA), 7,l0113.16.19-docosapentaenoic acid (hereinafter abbreviated as DpA).

) or 4 (, 7, 10 The fatty acids containing several double bonds in the molecule have the effect of reducing constyol and inhibiting the production of platelets, so they have the effect of inhibiting the production of platelets. It is known to be effective in preventing cancer, stroke, thrombosis, cerebral infarction, myocardial compartment, and angina pectoris.

These long-chain highly unsaturated fat U3 acids are mainly extracted from cod liver oil and herring oil hemorrhoids:! Because it is made of clay, it emits a distinctive odor,
When you eat these, you will be impressed by the taste.

Therefore, when administering these to humans, it is desirable to formulate them into tablets or capsules, as it is painful for the recipient to take them directly due to their bitter taste and odor.

However, since long-chain high-rotivity unsaturated lipolytics have 5 or 6 double bonds in the molecule, they are very easy to quantify and difficult to store for long periods of time. In order to convert these materials, it is necessary to add a large amount of crystals and an inert gasifying agent. To make these into tablet or capsule formulations,
The process had to be carried out under an inert gas atmosphere, with low rinsing, and in the presence of proprietary antioxidants, using special helicopter equipment, and under strict process control.

The inventors 1j under an inert gas atmosphere, low humidity or (d
Multi°, +1 ;iE @ in the presence of a oxidizing agent, and special/, [, ′・! S:i':'! i ft)
f! 4"l Il"l Ite, Nagahora High 11i For the purpose of sweeping unsaturated rice n7i acid European capsule formulation! ijt
Hakuka Koshida, Takashi Nagaura [When unsaturated fatty acids - Madashiyoso derivatives are dissolved in medium-chain 1J triblycerides (hereinafter abbreviated as MOT), their deterioration due to oxidation is reversed to the extent of JTE. The present invention has been completed by obtaining a soft capsule formulation that is good in terms of texture, taste, and odor, and that it is possible to use a conventional device to administer the soft capsule formulation. It arrived.

The V:, highly unsaturated fatty acid 11-fatty acid capsules and formulations of the present invention contain long-chain highly saturated fatty acids or derivatives thereof by dissolving them in 1riOT. It is characterized in that the obtained both sides are used as the liquid content.

The present invention has 1 carbon
It has a double bond of 17 to 21 and 6 and 11d in the molecule, and Ep8, DpA and DHA are 1 to 1. Its derivatives include terms and esters, and esters (
4C(4)' thyl ester, ethyl ester, Mc'
I' (d carbon - 11 of medium chain fatty acids with 8 primes and 1 to 10
It is a triglyceride with a weight of 1 to 2 c tons, and its use 11 is a triglyceride with a long chain polyunsaturated fatty acid of 0.01 lr to 50 tons in solution. ? K
It is a perfect fit. If the magnetic field exceeds 50, the safety will improve by 1 degree (7'IC).

The long-chain highly unsaturated fat-free capsule formulation of the present invention contains long-chain highly unsaturated fatty acids and their derivatives having various medicinal effects under a special atmosphere (1) and using special equipment. It can be made into a soft capsule preparation by manual immersion in a right circle, and the unpleasant feeling of long-chain highly unsaturated 11Ff folic acid is eliminated by C., and it is stabilized for a long period of time.

Next, the present invention will be explained using demonstration examples and comparative examples. Note that the soft capsule formulation is one filled in soft gelatin capsules.

Example I 5g of EPA ethyl ester (purity 59g) was added to MC
T (h grill?shun: capric acid molar ratio is 85:15
Mixed acid triglyceride] 95I was mixed with 95I, and this was used as the content liquid to fill 250 m4 per capsule to make a soft capsule preparation. Also.

Example 2 EPA (purity 9096) 1054 was dissolved in 90 g of the same IVIOT as used in Example 1, and this was used as the content liquid to fill each capsule with 250 η19 to obtain a soft capsule preparation.

Example 3 20 g of EPA (purity 65%) was dissolved in caprylic acid triglyceride 801, and this was used as the content liquid to prepare 250 capsules per capsule.

Example 4 Nagauta polyunsaturated fat (νzO2) consisting of EP'A 52%, D)IA 48% was dissolved into MGT80!7-, the same as that used in Example 1, and this was made into 1 capsule with content 11. A soft capsule formulation was obtained by filling 2,501,119 yen.

Example 5 20 g of long-chain highly unsaturated fatty acids consisting of 55% EPA, 25% DPA, and 20% DI (A) was dissolved in 80 g of the same MOT used in Example 1, and this was used as an internal solution of 25 (1+!7) per capsule. Fill it to obtain a soft capsule/preparation.

Comparative Example] The same EPAIOl used in Example 2 was dissolved in 90g-Q of purified sesame oil, and this was used as the content liquid at 25θn19it per capsule to obtain a soft capsule preparation.

[Storability and sensory test of soft capsule formulation] Example 1
5 and Comparative Example], each soft capsule formulation was stored in a room for 6 months, and the peroxide value of the capsule contents was measured immediately after production and after 6 months storage, and a sensory test was conducted at the time of administration. The results are shown in Table 1.The sensory test was conducted by a panel of 10 people, and those who felt discomfort or pain when taking the drug were judged as poor, and those who could take it without resistance were judged to be good. It shows.

As is clear from the table, the content of the capsule is a solution obtained by dissolving its derivative in MOT. Discomfort is reduced and JP7 special equipment, long 11JI can be used as a capsule in the usual way without special conditions.
It was invited to stabilize over C1.

Patent applicant: NOF Corporation Representative Patent Attorney Tsukasa Tano

Claims (1)

[Claims] Long-cut high-grade non-tobiwa fat i! Highly unsaturated fat 1171i□□□I with i or its induction/salary as medium steel l PORT 8 force jiJ) Liglyceride C.
Drinking capsule formulation