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WO2000037044A1 - Composition douce et a macher pour soulager de la toux et du rhume - Google Patents

Composition douce et a macher pour soulager de la toux et du rhume Download PDF

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Publication number
WO2000037044A1
WO2000037044A1 PCT/US1999/029661 US9929661W WO0037044A1 WO 2000037044 A1 WO2000037044 A1 WO 2000037044A1 US 9929661 W US9929661 W US 9929661W WO 0037044 A1 WO0037044 A1 WO 0037044A1
Authority
WO
WIPO (PCT)
Prior art keywords
composition
cough
soft
cold
group
Prior art date
Application number
PCT/US1999/029661
Other languages
English (en)
Inventor
Subraman R. Cherukuri
Khoa M. Nguyen
Original Assignee
Biovail International Ltd.
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Biovail International Ltd. filed Critical Biovail International Ltd.
Priority to AU21824/00A priority Critical patent/AU2182400A/en
Publication of WO2000037044A1 publication Critical patent/WO2000037044A1/fr

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0053Mouth and digestive tract, i.e. intraoral and peroral administration
    • A61K9/0056Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605Excipients; Inactive ingredients
    • A61K9/1617Organic compounds, e.g. phospholipids, fats
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/02Nasal agents, e.g. decongestants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/14Antitussive agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents

Definitions

  • the present invention relates to a soft and chewable cough and cold relief composition, and specifically to a storage-stable formulation containing one or more active ingredients which provide rapid and substantial relief from cough and cold symptoms.
  • Medications for cough and cold relief are known in the art. A large number of these are available as over-the-counter preparations in the form of cough drops, lozenges, chewing gums, and other confectionery-based formulations. Many of these are hard and sugary, to be placed in the mouth so that the action of saliva can release the active ingredients over the course of several minutes.
  • compositions containing one or more cough and cold actives which is soft and chewable, and which releases the active(s) quickly to promote rapid relief as well as sustained relief thereafter.
  • Active ingredients can include antitussives, antihistamines, nasal decongestants and analgesics.
  • composition of the invention while storage stable for extended periods, dissolves quickly in the mouth upon chewing to release the active ingredients.
  • the composition of the invention is easily pliable inside the mouth, and can be administered like a soft nougat-type formulation.
  • a confectionery-type composition which provides active ingredients for relief from many cough and cold symptoms.
  • the composition herein provided is soft, chewable and dissolves quickly in the mouth. Sufferers of cold and flu symptoms, as well as other nasal/respiratory conditions, attain prompt relief which lasts for an extended period. Such conditions can include stuffy head, runny nose, nasal and sinus congestion and the like.
  • the composition provides as a first component at least one member selected from the group consisting of saccharide-based material. Examples include the mono-, di-, tri- and polysaccharides available in the food and confectionery industry, including oligomers, and oligosaccharides, as well as mixtures of any of the foregoing.
  • sugars such as sucrose, glucose (corn syrup), dextrose, invert sugar, fructose, and mixtures thereof may be useful. Less or non-sweet sugars and polysaccharide material such as maltodextrin, corn syrup solids and polydextrose may also be utilized.
  • “sugar-free” or “non-sucrose” materials, or even “non- saccharide” compounds, either in whole or in part, may be especially desirable.
  • other compounds may be selected from the group consisting of aspartame, acesulfame, saccharin and its various salts such as the sodium and calcium salts, cyclamic acid and its various salts, dipeptide sweeteners, chlorinated sugar derivatives such as sucralose, dihydrochalcone, glycyrrhin, Stevia rebaudiana (Stevioside), and sugar alcohols such as sorbitol, sorbitol syrup, mannitol, xylitol, hexa-resorcinol and the like, including mixtures of any of the foregoing, are contemplated for use herein.
  • Hydrogenated starch hydrolysate, (lycasin), and the potassium, calcium and sodium salts of 3,6-dihydro-6-methyl-l-l,2,3- oxathiazin-4-on3-2,2-dioxide are also within the scope of the invention as a saccharide material.
  • saccharide-based materials include sucrose, corn syrup solids, maltodextrin, xylitol and aspartame. Aspartame is desirable as a non-saccharide sweetener.
  • the saccharide-based component will typically comprise about 25 to 99.5% of the final formulation (unless otherwise stated, all weight percentages herein are based on the total weight of the final composition). More typically, the composition will contain about 40 to 95%, and even more desirably about 70 to 90% of saccharide-based material.
  • the saccharide-based component be in substantially dry form, that is, without any added liquid. In this way, it should bind substantially more easily with the binding component, hereinafter described.
  • a food-grade binding component In admixture with the saccharide-based component is a food-grade binding component.
  • the binding component is one which is used to mix and functionalize the other ingredients so as to provide a cohesive final mass.
  • the binding material or binder is selected from materials in the art with demonstrative ability to bind and hold the other ingredients.
  • the binding material may be selected from the group consisting of food grade gums, carrageenan and proteinaceous material, as well as mixtures thereof. Especially preferred are gum arabic, gum acacia and gelatin. Water is also included as part of the binding material.
  • water When added, water will comprise about 30 to 70% of the binding material, and more preferably, be included as about 40 to 60% thereof.
  • the binding component acts to imbibe and absorb the dry saccharide-based component.
  • a humectant or wetting agent is also preferably included as part of the binding material. Polyols are preferred for this purpose; in particular, glycerol. Glycerine is also contemplated. It is desirable that the binding material contain about 25 to 45% of humectant, more preferably about 30 to 40%. Either or both of the saccharide-based and binding components may be provided in shearform matrix by means of flash-flow processing.
  • Either or both of the saccharide- based component and the binding component may be admixed together using flash-flow processing.
  • This method of processing helps to ensure intimate admixture of all ingredients, thereby providing shearform matrix attributes.
  • Flash-flow processing and apparatus is described in U.S. Patent Nos. 5,236,734, 5,238,696, 5,518,730, 5,387,431, 5,429,836, 5,549,917, 5,556,652, 5,582,855 and most recently, 5,834,033.
  • a spinner head includes a base and a cover spaced apart from the base. A plurality of discrete spaced apart elongate heating elements are positioned between the base and the cover and define a chamber for accommodating feedstock material therein.
  • the chamber is spun and the feedstock material is heated and is expelled through the spaces between the heating elements.
  • Feedstock engagement surfaces are positioned in alignment with each of the spaces between the heating elements so as to engage the expelled feedstock to alter the direction of travel of the expelled product.
  • Other means to provide shearform matrix includes high and low shear processing using such mixers as Littleford, Hobart and Guittard mixers, including mixers with paddle type blades and those which provide propeller-type, highly localized and focused mixing action.
  • Active ingredients are those known in the pharmaceutical industry, especially the over-the-counter pharmaceutical industry, which cure, relieve, alleviate or lessen one or more symptoms associated with ailments like colds, flu, fevers, certain allergies and cough, etc.
  • Symptoms can include stuffy head, congestion, sinus pressure, aches, pains, sore throat, fever, etc.
  • Active ingredients to help relieve these symptoms can therefore include various antitussives, antihistamines, nasal decongestants and analgesics.
  • Other actives include those which may be recognized as preventive in nature as well. All of the foregoing are therefore to be encompassed by the term "cough and cold active".
  • menthol, eucalyptol or other eucalyptus derivative, and zinc are especially contemplated for inclusion in the product of the invention.
  • Zinc ion salts are particularly preferred.
  • Zinc acetate dihydrate is just one example of a suitable zinc compound.
  • Other broad classes of compounds with applicability herein may also be included as actives in the final composition.
  • nutraceutical substances derived from plant material with some demonstrated ability to relieve cough and cold symptoms may also be included.
  • the active ingredient(s) together will comprise from about 0.1 to 40% of the final cough and cold formulation. More desirably, one or more actives will make up about 0.5 to 5% of the final composition.
  • the active may be provided according to recommendations known in the art. For example, published guidelines from the U.S. Food & Drug Administration, or other industry sources, may be utilized to provide an optimal dosing level.
  • One or more of the active ingredients are preferably provided in the form of encapsulations.
  • An encapsulated active ingredient matrix seems to provide for more content uniformity in the final composition.
  • Encapsulation may also impart a greater degree of stability to the cough and cold actives during relatively prolonged periods of commercial storage. Encapsulation may be accomplished by methods known in the art.
  • one or more food-grade materials are employed as processing aids. These edible materials can include oleaginous substances (fats and oils), as well as certain waxes, saccharides, phosphatides, proteins and other non- toxic polymeric material, especially those with emulsifying properties.
  • Highly suitable encapsulation processing aids are preferably oleaginous material and any one or more oleaginous food and pharmaceutical grade materials may be utilized for this purpose. It is believed that the encapsulating material surrounds and enrobes tiny individual particles of the active substance, thereby creating a matrix of several thousand or more individually enrobed particles once combined into the final confectionery nougat-like composition. Especially volatile active substances are further rendered less volatile as a result of encapsulation.
  • Especially suitable oleaginous encapsulating material includes various food-grade oils and fats available in the industry. Of these, those with emulsifying properties are particularly preferred. Vegetable and animal oils and fats may be utilized for this purpose.
  • Stearine for example, may be utilized as an encapsulating agent, while certain mono- and diglyceride-based fat products are also efficacious.
  • Canola, cottonseed and soybean oils may be preferred as well in certain embodiments.
  • MCT medium chain triglyceride
  • Waxes such as carnauba are also particularly useful in certain embodiments.
  • Phosphatides such as lecithin are highly desirable as well.
  • the encapsulating material itself will typically comprise about 0.1 to 10% of the final confectionery, cough and cold formulation, and more desirably, will be within the range of from about 0.5 to 5% thereof.
  • the encapsulating material comprise about 0.5 to 3% of the composition.
  • Other material may be utilized as plasticizers, thickening agents or absorbents in the encapsulation.
  • Certain polymeric materials are especially useful for this purpose. These include certain cellulosic materials, including hydroxyalkylcellulosic and hydroxyalkylalkylcellulosic polymers. Of these, hydroxymethyl-, hydroxyethyl-, hydroxypropyl- and hydroxypropylmethylcelluose (HPMC) are desirable.
  • Other material such as silicon dioxide or silica gel may be utilized as well as, for example, to provide bulk.
  • Low and high shear mixing apparatus are especially useful for preparing encapsulations of the active ingredient(s).
  • Spray-drying and extrusion methods are also available and are known in the art.
  • Other highly suitable methods include flash-flow processing as described in U.S. Patent Nos. 5,236,734, 5,238,696, 5,518,730, 5,387,431, 5,429,836, 5,549,917, 5,556,652, 5,582,855, and 5,834,033.
  • the heretofore described method set forth in U.S. Patent No. 5,380,473 is especially useful for preparing encapsulations.
  • the method of the '473 reference helps to provide a microparticulate dispersion of the active ingredient throughout the entire matrix of the final composition, when the active is mixed with the saccharide and binding components to form the final composition.
  • a combination of any of the foregoing encapsulation methods is also within the scope of the invention.
  • any of the other ingredients constituting the final formulation including any flavorants, hereinafter described, be encapsulated as well.
  • Other ingredients which may be included as part of the final cough and cold formulation include certain flavorants. These may be selected from any of the industry- available natural and synthetically-derived food and pharmaceutical flavors in whatever form. Especially preferred are those materials which impart a cooling and/or vaporizing sensation upon ingestion.
  • peppermint, spearmint, wintergreen, cinnamon, menthol and menthone flavors, oils and derivatives are desirable.
  • Other flavors, such as fruit flavors, and in particular, cherry flavor, are also desirable.
  • Flavorants will typically comprise from about 0.1 to 5% of the final formulation.
  • compositions of the invention are highly storage stable since encapsulation of the active ingredients helps to prevent their premature dissipation upon exposure to ambient atmospheric conditions.
  • a soft, chewy confectionery formulation was prepared having the following composition:
  • Saccharide Component - included a mix of sugar (48%), high maltose corn syrup solids (18%), maltodextrin (15%) and xylitol (2.5%).
  • Binding Component - included gelatin (2.25%), gum arabic (0.60%), glycerine (3.70%), water (5.25%) and sucrose super-saturated solution. Active Ingredients were zinc acetate dihydrate (0.34%, preferred range of about 0.1 to 0.6%) and menthol (2.33%, preferred range of about 0.5 to 10%). Encapsulation materials for the actives included MCT oil (1.0%) and lecithin (0.70%). The actives were encapsulated using a combination of Hobart and Littleford mixers. All the ingredients were then admixed together using low shear mixing apparatus. The batch was then cut into approximately 5.3 gram serving sizes. The formulation was soft and chewy and provided an almost instantaneous cooling and vaporizing action.

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pulmonology (AREA)
  • Epidemiology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Otolaryngology (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Immunology (AREA)
  • Zoology (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Medicinal Preparation (AREA)

Abstract

L'invention concerne une composition contre la toux et le rhume. Ladite composition douce et à mâcher, libère au moins un agent actif, y compris le zinc et le menthol, pour diminuer les symptômes.
PCT/US1999/029661 1998-12-21 1999-12-14 Composition douce et a macher pour soulager de la toux et du rhume WO2000037044A1 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU21824/00A AU2182400A (en) 1998-12-21 1999-12-14 Soft and chewy cough and cold relief composition

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
IE981080 1998-12-21
IE981080 1998-12-21
US43517699A 1999-11-05 1999-11-05
US09/435,176 1999-11-05

Publications (1)

Publication Number Publication Date
WO2000037044A1 true WO2000037044A1 (fr) 2000-06-29

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Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US1999/029661 WO2000037044A1 (fr) 1998-12-21 1999-12-14 Composition douce et a macher pour soulager de la toux et du rhume

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AU (1) AU2182400A (fr)
WO (1) WO2000037044A1 (fr)

Cited By (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004037237A1 (fr) * 2002-10-24 2004-05-06 Immupharm A/S Compositions pharmaceutiques comprenant des flavonoides et du menthol
WO2004098571A1 (fr) * 2003-04-30 2004-11-18 Zicam, Llc Composition pour traiter les refroidissements comprenant des sels de zinc
WO2004070017A3 (fr) * 2003-02-04 2005-01-27 Bennes Inc Formes galeniques aromatisees de longue duree pour la liberation prolongee d'agents benefiques dans la bouche
WO2005079598A1 (fr) * 2004-01-23 2005-09-01 Firmenich Sa Grosses perles vitreuses
WO2008033155A1 (fr) * 2006-09-15 2008-03-20 Auriga Laboratories, Inc. Trousses de prévention et traitement de la rhinite
CN102397361A (zh) * 2011-11-26 2012-04-04 苏州派腾生物医药科技有限公司 一种感冒止咳颗粒的制备方法
WO2014117265A1 (fr) * 2013-02-01 2014-08-07 Ddrops Company Compositions de menthol liquides

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0227603A2 (fr) * 1985-12-20 1987-07-01 Warner-Lambert Company Système de libération de substances actives sous forme d'une sucrerie
EP0788746A1 (fr) * 1995-09-05 1997-08-13 Yasui Confectionery Co., Ltd. Gomme et son procede de preparation
WO1999062351A1 (fr) * 1998-06-05 1999-12-09 Fuisz Technologies Ltd. Formulation de confiserie a macher contenant des elements nutritifs

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0227603A2 (fr) * 1985-12-20 1987-07-01 Warner-Lambert Company Système de libération de substances actives sous forme d'une sucrerie
EP0788746A1 (fr) * 1995-09-05 1997-08-13 Yasui Confectionery Co., Ltd. Gomme et son procede de preparation
WO1999062351A1 (fr) * 1998-06-05 1999-12-09 Fuisz Technologies Ltd. Formulation de confiserie a macher contenant des elements nutritifs

Cited By (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7585890B2 (en) 2002-10-24 2009-09-08 Immunpharm A/S Pharmaceutical compositions comprising flavonoids and menthol
WO2004037237A1 (fr) * 2002-10-24 2004-05-06 Immupharm A/S Compositions pharmaceutiques comprenant des flavonoides et du menthol
US7671086B2 (en) 2002-10-24 2010-03-02 Immupharm A/S Pharmaceutical compositions comprising flavonoids and menthol
US8236348B2 (en) 2003-02-04 2012-08-07 Bennes, Inc. Long-lasting, flavored dosage forms for sustained release of beneficial agents within the mouth
WO2004070017A3 (fr) * 2003-02-04 2005-01-27 Bennes Inc Formes galeniques aromatisees de longue duree pour la liberation prolongee d'agents benefiques dans la bouche
WO2004098571A1 (fr) * 2003-04-30 2004-11-18 Zicam, Llc Composition pour traiter les refroidissements comprenant des sels de zinc
WO2005079598A1 (fr) * 2004-01-23 2005-09-01 Firmenich Sa Grosses perles vitreuses
US8227014B2 (en) 2004-01-23 2012-07-24 Firmenich Sa Large glassy beads
US8691319B2 (en) 2004-01-23 2014-04-08 Firmenich Sa Large glassy beads
WO2008033155A1 (fr) * 2006-09-15 2008-03-20 Auriga Laboratories, Inc. Trousses de prévention et traitement de la rhinite
CN102397361A (zh) * 2011-11-26 2012-04-04 苏州派腾生物医药科技有限公司 一种感冒止咳颗粒的制备方法
WO2014117265A1 (fr) * 2013-02-01 2014-08-07 Ddrops Company Compositions de menthol liquides
US9999602B2 (en) 2013-02-01 2018-06-19 Ddrops Company Liquid menthol compositions

Also Published As

Publication number Publication date
AU2182400A (en) 2000-07-12

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