JP2003261442A - Soft capsule preparation containing pseudoephedrine hydrochloride - Google Patents

Abstract

<P>PROBLEM TO BE SOLVED: To provide a soft capsule preparation at least containing pseudoephedrine hydrochloride as an active component. <P>SOLUTION: This soft capsule preparation contains a filling liquid produced by dispersing pseudoephedrine hydrochloride arbitrarily in combination with other drugs in an oily liquid carrier containing a surfactant. <P>COPYRIGHT: (C)2003,JPO

Description

Detailed Description of the Invention

[0001]

BACKGROUND OF THE INVENTION The present invention relates to a soft capsule containing at least pseudoephedrine hydrochloride as an active ingredient.

As a symptom of a common cold including influenza infection, there are many symptoms caused by nasal depression, such as runny nose, sneezing and stuffy nose. Nasal or oral administration of antidepressants is effective for amelioration of these symptoms, and phenylpropanolamine hydrochloride has been often used conventionally.

However, in recent years, pseudoephedrine hydrochloride has tended to be used in place of phenylpropanolamine hydrochloride because of its toxicity, especially the concern about accidents when accidentally taking a large dose. However, pseudoephedrine hydrochloride has a short duration of action, and the daily dose of 70 to 120 mg per adult for oral administration must be divided and frequently administered. In particular, in the case of oral preparations containing pseudoephedrine hydrochloride to be administered in combination with other active ingredients, for example, cold remedies, the frequency of administration is limited by other drugs having a long duration, and the determined frequency of administration, for example, 4 times a day.
In some cases, pseudoephedrine hydrochloride does not exhibit its effect sufficiently with a single administration. Therefore, it is desired to develop a new preparation containing pseudoephedrine hydrochloride as an active ingredient.

[0004]

The present invention provides a soft capsule containing a filler solution of pseudoephedrine hydrochloride, dispersed or not, optionally in combination with other active ingredients, in a liquid oily carrier containing a surfactant. Regarding agents.

[0005] This soft capsule can exhibit its medicinal effect sufficiently by administering a daily dose of 70 to 120 mg as pseudoephedrine hydrochloride in 3 to 4 divided doses.

[0006]

Preferred Embodiment The main component of the capsule filling liquid is a natural vegetable oil such as corn oil or olive oil, or medium chain fatty acid triglyceride. Waxes such as beeswax, paraffin and / or a small proportion of liquid polyethylene glycol such as Macrogol 400 may be included to control the viscosity of the fill liquid.

The surfactant serves to emulsify the oily carrier in which the drug is dispersed into an emulsion in the digestive tract and help the absorption of the drug. Preferred surfactants are nonionic type surfactants. Nonionic surfactants have relatively low HLB (HLB <8), such as sorbitan sesquioleate and glycerin fatty acid ester, and relatively high HLB.
High Activator (HLB> 8) eg Polysorbate 80
The combination with is preferred.

Typical examples of other drugs used in combination with pseudoephedrine hydrochloride for administration as a cold drug include antihistamines such as d-chlorpheniramine maleate, sympathomimetics such as theophylline, aminophylline and salbutamol (bronchodilators). , A parasympathetic blocker such as belladonna total alkaloids, analgesic and antipyretic agents such as ibuprofen, aspirin, acetaminophen, tranilast, antiallergic agents such as ketotifen fumarate, and caffeine. If desired, known herbal medicines,
It may also include antitussives, expectorants and the like.

These active drug components are dispersed or suspended in a liquid oil carrier by a conventional method to prepare a capsule filling liquid,
Fill with soft capsule shell.

[0010]

EXAMPLE The following formulation example is a formulation of a daily filling liquid, which is divided into 4 equal parts and filled into gelatin soft capsule shells by a conventional method.

[0011] Prescription example 1 d-Chlorpheniramine maleate 6 mg Anhydrous caffeine 75mg Belladonna total alkaloid 0.4 mg Pseudoephedrine hydrochloride 79 mg Corn oil 518.6mg Macrogol 400 24mg White beeswax 28 mg Sorbitan sesquioleate 18mg Polysorbate 80 18mg Glycerin fatty acid ester 28mg ────────────────────────────── Total 795mg

[0012] Prescription example 2 d-Chlorpheniramine maleate 12 mg Anhydrous caffeine 75mg Belladonna total alkaloid 0.4 mg Pseudoephedrine hydrochloride 79 mg Medium chain fatty acid triglyceride 568.6 mg White beeswax 20 mg Polysorbate 80 20 mg Glycerin fatty acid ester 20mg ────────────────────────────── Total 795mg

[0013] Prescription example 3 d-Chlorpheniramine maleate 6 mg Anhydrous caffeine 120mg Belladonna total alkaloid 0.6 mg Pseudoephedrine hydrochloride 120 mg Medium chain fatty acid triglyceride 898.74 mg White beeswax 71 mg Sorbitan sesquioleate 31mg Polysorbate 80 31mg Glycerin fatty acid ester 71mg ────────────────────────────── Total 1349.34 mg

[0014] Prescription example 4 d-Chlorpheniramine maleate 6 mg Anhydrous caffeine 120mg Belladonna total alkaloid 0.6 mg Pseudoephedrine hydrochloride 120 mg Medium chain fatty acid triglyceride 900.74mg Macrogol 400 10 mg White beeswax 64 mg Sorbitan sesquioleate 31mg Polysorbate 80 31mg Glycerin fatty acid ester 64mg Sodium edetate 2mg ────────────────────────────── Total 1349.34 mg

[0015] Prescription example 5 d-Chlorpheniramine maleate 6 mg Anhydrous caffeine 120mg Belladonna total alkaloid 0.6 mg Pseudoephedrine hydrochloride 120 mg Medium chain fatty acid triglyceride 896.74 mg Macrogol 400 10 mg White beeswax 64 mg Sorbitan sesquioleate 31mg Polysorbate 80 31mg Glycerin fatty acid ester 64mg Tocopherol acetate 6mg ────────────────────────────── Total 1349.34 mg

[0016] Prescription example 6 dl-chlorpheniramine maleate 12 mg Caffeine 120mg Belladonna total alkaloid 0.4 mg Pseudoephedrine hydrochloride 75 mg Corn oil 483mg Perilla oil 5mg Macrogol 400 24mg White beeswax 19.8mg Sorbitan sesquioleate 18mg Polysorbate 80 18mg Glycerin fatty acid ester 19.8mg ────────────────────────────── Total 795mg

[0017] Prescription example 7 dl-chlorpheniramine maleate 12 mg Caffeine 120mg Belladonna total alkaloid 0.4 mg Pseudoephedrine hydrochloride 75 mg Corn oil 471.6mg Macrogol 400 24mg White beeswax 28 mg Sorbitan sesquioleate 18mg Polysorbate 80 18mg Glycerin fatty acid ester 28mg ────────────────────────────── Total 795mg

─────────────────────────────────────────────────── ─── Continuation of front page (51) Int.Cl. ⁷ Identification code FI theme code (reference) A61P 11/06 A61P 11/06 F term (reference) 4C076 AA56 AA66 BB01 CC15 DD07 DD08 DD09 DD46 EE23 EE42 EE53 EE54 FF31 4C206 AA01 AA02 FA10 KA01 MA02 MA03 MA05 MA29 MA57 MA72 NA12 ZA34 ZA59

Claims (5)

[Claims] 1. A soft capsule containing a filling liquid in which pseudoephedrine hydrochloride optionally in combination with another drug is dispersed in a liquid oily carrier containing a surfactant. 2. The soft capsule of claim 1, wherein the liquid oily carrier is vegetable oil and / or medium chain fatty acid triglyceride. 3. The soft capsule according to claim 1 or 2, wherein the surfactant is a mixture of a nonionic surfactant having a relatively low HLB and a nonionic surfactant having a relatively high HLB. 4. A drug selected from pseudoephedrine hydrochloride as an active ingredient, in addition to an antihistamine, a sympathomimetic, a parasympathetic blocker, an analgesic / antipyretic drug, an antiallergic drug, a crude drug, or caffeine. One of the soft capsules. 5. The soft capsule according to claim 1, wherein the indication is depressive symptoms associated with a cold.